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Merck Sharp & Dohme Corp patents


Recent patent applications related to Merck Sharp & Dohme Corp. Merck Sharp & Dohme Corp is listed as an Agent/Assignee. Note: Merck Sharp & Dohme Corp may have other listings under different names/spellings. We're not affiliated with Merck Sharp & Dohme Corp, we're just tracking patents.

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Thiadiazolyl - oximinoacetic acid derivative compounds

Thiadiazolyl-oximinoacetic acid derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds. Compound (1) (TATD) is commercially available (CAS No. 76028-96-1). It has now been discovered that the thiadiazolyl-oximinoacetic acid derivative compound (1) (TATD) can be prepared from dimethyl malonate (SM 1, CAS No. 108-59-8) according... Merck Sharp & Dohme Corp

 new patent  Isoquinoline derivatives as mgat2 inhibitors

The compounds of Formula I act as MGAT2 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.... Merck Sharp & Dohme Corp

 new patent  Inhibitors of the renal outer medullary potassium channel

The present invention provides compounds of Formula I (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure... Merck Sharp & Dohme Corp

 new patent  Imidazopyrazine analogs with 3-tertiary carbon substitutions as btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, Formula (I) or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I... Merck Sharp & Dohme Corp

Factor xia inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.... Merck Sharp & Dohme Corp

(s)-n-(3-(6-isopropoxypyridin-3-yl)-1h-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2h)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide compositions for pharmaceutical preparations

The invention includes a granular composition comprising the active ingredient (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3- carboxamide, wherein a total amount of active ingredient comprises by weight % about 60-90% (5)-N-(3-(6-isopro-poxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-di-hydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide Form 1 HCl, about 10-30% (5)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous HCl, and about 0-5% (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide amorphous free base.... Merck Sharp & Dohme Corp

4'-substituted nucleoside reverse transcriptase inhibitors

and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.... Merck Sharp & Dohme Corp

Solid dispersion formulations of antiviral compounds

The present disclosure is directed to solid dispersion formulations comprising an NS5A inhibitor compound, elbasvir (dimethyl N,N′-([(6S)-6-phenylindolo [1,2- c][1,3]benzoxazine-3,10-diyl]bis {1H-imidazole-5,2-diyl-(2S)-pyrrolidine-2,1-diyl[(2S)-3-methyl-l-oxobutane-1,2-diyl]})di-carbamate), or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable polymer, and optionally a pharmaceutically acceptable surfactant. The present disclosure is also directed to solid dispersion formulations, blended compositions and pharmaceutical... Merck Sharp & Dohme Corp

5,5-bicyclic oxazole orexin receptor antagonists

The present invention is directed to 5,5-bicyclic oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

Thiadiazolyl - oximinoacetic acid derivative compounds

Thiadiazolyl-oximinoacetic acid derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds. Compound (1) (TATD) is commercially available (CAS No. 76028-96-1). It has now been discovered that the thiadiazolyl-oximinoacetic acid derivative compound (1) (TATD) can be prepared from dimethyl malonate (SM 1, CAS No. 108-59-8) according... Merck Sharp & Dohme Corp

Compounds, compositions and methods

The disclosed subject matter provides certain polymorphic forms of Compound (I) as well as pharmaceutical compositions comprising Compound (I) or such polymorphic forms, and methods of using or making such compounds and pharmaceutical compositions. It has now been discovered that Compound (I) can exist in multiple crystalline forms (polymorphs). One... Merck Sharp & Dohme Corp

Iminothiadiazine dioxides bearing an amine-linked substituent as bace inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, and n are as defined herein. The novel compounds of... Merck Sharp & Dohme Corp

Tricyclic gyrase inhibitors

Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.... Merck Sharp & Dohme Corp

Novel tricyclic compounds as inhibitors of mutant idh enzymes

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I). The present invention is also directed to uses of the tricyclic compounds described herein in the potential treatment or prevention of cancers in which one or more mutant... Merck Sharp & Dohme Corp

Formulations for cathepsin k inhibitors

The instant invention relates to pharmaceutical compositions containing cathespin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.... Merck Sharp & Dohme Corp

Novel tricyclic compounds as inhibitors of mutant idh enzymes

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes: (I); wherein A is —C(R1)= or —N═; and X is selected from the group consisting of: (II-i), (II-ii), (I) (II-iii), and (II-iv). The present invention is also directed to... Merck Sharp & Dohme Corp

Co-agonists of the glucagon and glp-1 receptors

Described are peptide analogs of glucagon, which have been modified to be resistant to cleavage and inactivation by dipeptidyl peptidase IV (DPP-IV) and to increase in vivo half-life of the peptide analog while enabling the peptide analog to have relatively balanced agonist activity at the glucagon-like peptide 1 (GLP-1) receptor... Merck Sharp & Dohme Corp

Dengue virus vaccine compositions and methods of use thereof

The present invention relates to dengue virus vaccine compositions comprising a first and a second dengue vaccine, wherein the first dengue vaccine comprises at least one live, 5 attenuated dengue virus or live, attenuated chimeric dengue virus and the second dengue vaccine is a recombinant dengue subunit vaccine, a DNA... Merck Sharp & Dohme Corp

Pyrazolyl carboxylic acid and pyrazolyl urea derivative compounds

Pyrazolyl carboxylic acid and pyrazolyl urea derivatives have been synthesized, which are useful in the manufacture of cephalosporin antibiotic compounds.... Merck Sharp & Dohme Corp

(s)-n-(3-(6-isopropoxypyridin-3-yl)-1h-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1h-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2h)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide compositions for pharmaceutical preparations

A composition comprising (S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.... Merck Sharp & Dohme Corp

Novel tricyclic compounds as inhibitors of mutant idh enzymes

The present invention is directed to tricyclic compounds of formula (I) which are inhibitors of one or more mutant IDH enzymes (I); wherein A is —C(R1)═ or —N═; and X is selected from the group consisting of: (II-i), and (II-ii). The present invention is also directed to uses of the... Merck Sharp & Dohme Corp

Process for the preparation of tert-butyl 4-((2s,5r)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carboxylate and analogs thereof

The present invention relates to processes for preparing compounds of Formula I. Such compounds include intermediates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound... Merck Sharp & Dohme Corp

Benzamide imidazopyrazine btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the... Merck Sharp & Dohme Corp

Biarylether imidazopyrazine btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the... Merck Sharp & Dohme Corp

C5-c6-oxacyclic fused iminopyrimidinone compounds as bace inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The... Merck Sharp & Dohme Corp

Spirocyclic heterocycle compounds useful as hiv integrase inhibitors

The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2, R3 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic... Merck Sharp & Dohme Corp

Glycan-based antibody-drug conjugates

Genetically engineered antibodies containing non-native N-glycosylated sites, preparation of the antibodies in yeast and fungi, site-specific conjugation of drugs to these antibodies, and methods of treatment utilizing these antibodies are described herein.... Merck Sharp & Dohme Corp

Formulation inhibiting effects of low acid environment

The present invention is directed to formulations comprising PVP polymer, a dispersion of a compound of Formula I (API), and citric acid, which formulations mitigate the effects of coadministering the compound of Formula I with a proton pump inhibitor compound.... Merck Sharp & Dohme Corp

Ethyldiamine orexin receptor antagonists

The present invention is directed to ethyldiamne compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is... Merck Sharp & Dohme Corp

Insulin receptor partial agonists

Insulin dimers and insulin analog dimers that act as partial agonists at the insulin receptor are disclosed.... Merck Sharp & Dohme Corp

Anti-gitr antibodies

Antibodies to human GITR are provided, as well as uses thereof, e.g., in treatment of proliferative and immune disorders.... Merck Sharp & Dohme Corp

Anti-coagulation factor xi antibodies

Antibodies that bind the apple 3 domain of human coagulation Factor XI and inhibit activation of FXI by coagulation factor XIIa as well as activation of FIX by FXIa are described.... Merck Sharp & Dohme Corp

Beta-amino heterocyclic dipeptidyl peptidase inhibitors for the treatment or prevention of diabetes

The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to... Merck Sharp & Dohme Corp

Non-nucleoside reverse transcriptase inhibitors

are HIV reverse transcriptase inhibitors, wherein R1, R2, RE, L, M and Z are defined herein. The compounds of Formula I and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the... Merck Sharp & Dohme Corp

12/07/17 / #20170349593

Btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I) in the... Merck Sharp & Dohme Corp

11/30/17 / #20170340610

Rorgammat inhibitors

The present invention relates to compounds according to Formula (I) or a pharmaceutically acceptable salt or solvate thereof. Such compounds can be used in the treatment of RORgammaT-mediated diseases or condition.... Merck Sharp & Dohme Corp

11/30/17 / #20170340631

Btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula (I), or pharmaceutically acceptable salts or stereoisomers thereof, or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula (I)... Merck Sharp & Dohme Corp

11/30/17 / #20170340738

Stable acidic insulin formulations

While the present invention is described herein with reference to illustrated embodiments, it should be understood that the invention is not limited hereto. Those having ordinary skill in the art and access to the teachings herein will recognize additional modifications and embodiments within the scope thereof. Therefore, the present invention... Merck Sharp & Dohme Corp

11/30/17 / #20170342052

Pyrrolidine orexin receptor antagonists

The present invention is directed to pyrrolidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is... Merck Sharp & Dohme Corp

11/30/17 / #20170342053

Crystal forms of a ccr5 antagonist

The present disclosure relates to forms of a CCR5 inhibitory compound, (4,6-dimethylpyrimidin-5-yl)(4-((3S)-4-((1R)-2-methoxy-1-(4-(trifluoromethyl)phenyl)ethyl)-3-methyl-piperazin-1-yl)-4-methylpiperidin-1-yl)methanone.... Merck Sharp & Dohme Corp

11/30/17 / #20170342076

Tertiary alcohol imidazopyrazine btk inhibitors

The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I... Merck Sharp & Dohme Corp

11/30/17 / #20170342397

Process for refolding recombinant chymotrypsin

A process for refolding recombinant chymotrypsin produced from prokaryote host cells is described. In particular, the present invention provides a process for refolding recombinant chymotrypsin produced from E. coli is described.... Merck Sharp & Dohme Corp

11/23/17 / #20170334924

Spirocyclic heterocyclic compounds useful as hiv integrase inhibitors

The present invention relates to Spirocyclic Heterocycle Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, R1, R2 and R4 are as defined herein. The present invention also relates to compositions comprising at least one Spirocyclic Heterocycle Compound, and methods of using the Spirocyclic Heterocycle... Merck Sharp & Dohme Corp

11/23/17 / #20170334926

Process for preparing substituted indole compounds

The present invention is directed to a process for preparing Substituted Indole Compounds of Formula (I): wherein R1, R2, R3 and R4 are as defined herein. These indole compounds are useful as synthetic intermediates for making inhibitors of HCV NS5A.... Merck Sharp & Dohme Corp

11/23/17 / #20170335308

Process for producing recombinant trypsin

A process for producing recombinant trypsin from prokaryote host cells in high yield and high specific activity is described. In particular, a process for producing recombinant trypsin from E. coli is described.... Merck Sharp & Dohme Corp

11/23/17 / #20170335359

Biocatalytic transamination process

employing dynamic kinetic resolution (DKR). The DKR process involves an enzymatic enantioselective amination reaction catalyzed by transaminases. The process can be used to manufacture key intermediates in the preparation of poly (ADP-ribose) polymerase (PARP) inhibitors which may be useful for the treatment of cancer.... Merck Sharp & Dohme Corp

11/23/17 / #20170335360

Bacillus megaterium recombinant protein expression system

The present invention relates to isolated or purified asporogenous Bacillus megaterium (B. megaterium) strains comprising a B. megaterium genome, wherein said genome is modified in that the spo0A gene is deleted or functionally deleted and the strain does not produce spores. The aspororogenous strains of the invention may be further... Merck Sharp & Dohme Corp

11/16/17 / #20170327490

Piperidine isoxazole and isothiazole orexin receptor antagonists

The present invention is directed to piperidine isoxazole and isothiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.... Merck Sharp & Dohme Corp

11/16/17 / #20170327817
11/09/17 / #20170319560

Pyrazole, triazole and tetrazole orexin receptor antagonists

The present invention is directed to pyrazole, triazole and tetrazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the pyrazole, triazole, and tetrazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin... Merck Sharp & Dohme Corp

11/09/17 / #20170320856

Amidoethyl azole orexin receptor antagonists

The present invention is directed to amidoethyl azole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

11/09/17 / #20170320865

Oxazole orexin receptor antagonists

The present invention is directed to oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the oxazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

11/09/17 / #20170320874

6,5-bicyclic octahydropyrrolopyridine orexin receptor antagonists

The present invention is directed to 6,5-bicyclic octahydropyrrolopyridine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

11/09/17 / #20170320876

Bridged diazepane orexin receptor antagonists

The present invention is directed to bridged diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

11/09/17 / #20170320882

Novel compounds that are erk inhibitors

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof. Also disclosed are methods of treating cancer using the compounds of formula (I).... Merck Sharp & Dohme Corp

11/09/17 / #20170320884

Hydroxmethyl piperidine orexin receptor antagonists

The present invention is directed to hydroxymethyl piperidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

11/02/17 / #20170312222

Taste-masked formulations of raltegravir

Disclosed are taste-masked pharmaceutical formulations of raltegravir comprising coated API granules mixed with a screened powder excipient blend in either tablet or sachet form. The core and coated granules are produced using a Wurster process for enhanced control of particle size. Also disclosed are methods of treating HIV, e.g., in... Merck Sharp & Dohme Corp

11/02/17 / #20170313684

Pyrazole orexin receptor antagonists

The present invention is directed to pyrazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the pyrazole compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

11/02/17 / #20170313693

Piperidine oxadiazole and thiadiazole orexin receptor antagonists

The present invention is directed to piperidine oxadiazole and thiadiazole orexin compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved.... Merck Sharp & Dohme Corp

11/02/17 / #20170313718

Inhibitors of hif prolyl hydroxylase

The present invention concerns compounds of formula I or a pharmaceutically acceptable salt thereof which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising... Merck Sharp & Dohme Corp

11/02/17 / #20170313722

Tetrahydronaphthyridine and related bicyclic compounds for inhibition of rorgamma activity and the treatment of disease

The invention provides tetrahydronaphthyridine and related compounds, pharmaceutical compositions, methods of inhibiting RORγ activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydronaphthyridine and related compounds.... Merck Sharp & Dohme Corp

10/26/17 / #20170304262

Sglt-2 inhibitors for treating metabolic disorders in patients with renal impairment or chronic kidney disease

The present invention relates to certain SGLT-2 inhibitors, such as ertugliflozin or a co-crystal or a pharmaceutically acceptable salt thereof, for treating and/or preventing metabolic disorders, such as type 1 or type 2 diabetes mellitus or pre-diabetes, in patients with renal impairment or chronic kidney disease (CKD). The present invention... Merck Sharp & Dohme Corp

10/26/17 / #20170305902

Tetrahydronaphthyridine derivatives as mglur2-negative allosteric modulators, compositions, and their use

The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, L, X1, X2, and X3, are as defined herein. The compounds of the invention, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising them, are useful as non-competitive... Merck Sharp & Dohme Corp

10/26/17 / #20170305916

Methyl diazepane orexin receptor antagonists

The present invention is directed to methyl diazepane compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

Patent Packs
10/26/17 / #20170305923

Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, X, Y, m, R1, R5, Ra and Rb are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of... Merck Sharp & Dohme Corp

10/26/17 / #20170305924

Nargenicin compounds and uses thereof as antibacterial agents

The present invention relates to novel nargenicin related compounds which can inhibit DnaE and have antibacterial, particularly antimycobacterial activity against Mycobacterium tuberculosis. The present invention also relates to method for inhibiting growth of mycobacterial cells as well as a method of treating mycobacterial infections by Mycobacterium tuberculosis by administering an... Merck Sharp & Dohme Corp

10/12/17 / #20170290914

Anti-lag3 antibodies and antigen-binding fragments

The present invention includes antibodies and antigen-binding fragments thereof that specifically bind to human or cynomolgous monkey LAG3 as well as immunoglobulin chains thereof and polynucleotides encoding the same along with injection devices comprising such antibodies or fragments. Vaccines including such antibodies and fragments as well as compositions comprising the... Merck Sharp & Dohme Corp

10/05/17 / #20170283416

Inhibitors of the renal outer medullary potassium channel

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and... Merck Sharp & Dohme Corp

09/28/17 / #20170273965

Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2

The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof. The compounds of formula (I) are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may... Merck Sharp & Dohme Corp

09/28/17 / #20170273966

Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2

The present invention relates to a compound represented by formula I:and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be... Merck Sharp & Dohme Corp

09/28/17 / #20170274074

Combination of a pd-1 antagonist and an alk inhibitor for treating cancer

The present disclosure describes combination therapies comprising an antagonist of Programmed Death 1 receptor (PD-1) and an Anaplastic Lymphoma Kinase (ALK) inhibitor, and the use of the combination therapies for the treatment of cancer, and in particular for treating cancers that test positive for ALK, PD-L 1, or both ALK... Merck Sharp & Dohme Corp

09/28/17 / #20170275260

Allosteric modulators of nicotinic acetylcholine receptors

The present disclosure relates to compounds of formula I that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and... Merck Sharp & Dohme Corp

09/28/17 / #20170275274

Isoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2

The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may... Merck Sharp & Dohme Corp

09/28/17 / #20170275283

Inhibitors of the renal outer medullary potassium channel

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and... Merck Sharp & Dohme Corp

09/28/17 / #20170275292

Inhibitors of the renal outer medullary potassium channel

The present invention provides compounds of Formula I: (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure... Merck Sharp & Dohme Corp

09/28/17 / #20170275297

Inhibitors of irak4 activity

The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.... Merck Sharp & Dohme Corp

09/28/17 / #20170275298

Inhibitors of the renal outer medullary potassium channel

The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and... Merck Sharp & Dohme Corp

09/28/17 / #20170275300

Synthesis of cephalosporin compounds

Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a... Merck Sharp & Dohme Corp

09/28/17 / #20170275302

Inhibitors of the renal outer medullary potassium channel

The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and... Merck Sharp & Dohme Corp

Patent Packs
09/28/17 / #20170275315

Forms of r)-3-(4-(2-(2-methyltetrazol-5-yl)pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate

A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci... Merck Sharp & Dohme Corp

09/28/17 / #20170275327

Substituted phosphoramidate compounds and uses thereof

The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R1, R2, R3 and R4 are defined above herein. The present invention is also directed to uses of the compounds of Formula (I) to add phosphoramidate groups onto organic alcohols.... Merck Sharp & Dohme Corp

09/21/17 / #20170266167

Erk inhibitors

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a pharmaceutical composition comprising an effective amount of at least one compound of Formula (I) and a pharmaceutically acceptable carrier. The invention also provides... Merck Sharp & Dohme Corp

09/21/17 / #20170267695

Erk inhibitors

The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are ERK2 inhibitors. The invention also provides a method of inhibiting ERK2 in a patient in need of such treatment comprising administering to said patient an effective amount of at least... Merck Sharp & Dohme Corp

09/21/17 / #20170267759

Anti-lag3 antibodies and antigen-binding fragments

The present invention includes antibodies and antigen-binding fragments thereof that specifically bind to human or cynomolgous monkey LAGS as well as immunoglobulin chains thereof and polynucleotides encoding the same along with injection devices comprising such antibodies or fragments. Vaccines including such antibodies and fragments as well as compositions comprising the... Merck Sharp & Dohme Corp

09/14/17 / #20170260136

Heteroaryl orexin receptor antagonists

The present invention is directed to heteroaryl compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is... Merck Sharp & Dohme Corp

09/14/17 / #20170260177

Methyl oxazole orexin receptor antagonists

The present invention is directed to methyl oxazole compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention... Merck Sharp & Dohme Corp

09/14/17 / #20170260181

S-imino-s-oxo iminothiazine compounds as bace inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2A, R2B, R2, R3, RN, ring A, RA, m, ring B, RB, and n are as... Merck Sharp & Dohme Corp

09/07/17 / #20170254798

Method for screening drug-saccharide conjugates

Methods for identifying drug-saccharide conjugates that bind the mannose receptor, C type 1, (MRC1) and may be taken up by cells expressing MRC1, and the use of such drug-saccharide conjugates for treatment of particular diseases are described. In particular, the methods for identifying insulin-saccharide conjugates that bind the MRC1 receptor... Merck Sharp & Dohme Corp

08/31/17 / #20170246198

Process for making nucleoside phosphoramidate compounds

The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).... Merck Sharp & Dohme Corp

08/31/17 / #20170246300

C5-c6-fused tricyclic iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain C5-C6 fused tricyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R2, R3, RA, ring A, RA, m, -L1-, and RL are as defined herein. The novel... Merck Sharp & Dohme Corp

08/31/17 / #20170247336

Substituted pyrimidines as inhibitors of hif prolyl hydroxylase

The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical... Merck Sharp & Dohme Corp

08/31/17 / #20170247377

Diazine-fused amidines as bace inhibitors, compositions, and their use

In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2, RA, ring A, RA, m, L1, RL, ring C, RC, and p are as defined... Merck Sharp & Dohme Corp

08/31/17 / #20170247388

Inhibitors of irak4 activity

The present invention relates to inhibitors of IRAK4 of Formula I and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases.... Merck Sharp & Dohme Corp

08/31/17 / #20170248580

Method for screening drug-saccharide conjugates

Methods for identifying drug-saccharide conjugates that bind the mannose receptor, C type 1, (MRC1) and may be taken up by cells expressing MRC1, and the use of such drug-saccharide conjugates for treatment of particular diseases are described. In particular, the methods for identifying insulin-saccharide conjugates that bind the MRC1 receptor... Merck Sharp & Dohme Corp

08/24/17 / #20170240511

Substituted pyridine inhibitors of hif prolyl hydroxylase

The present invention concerns compounds of formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical... Merck Sharp & Dohme Corp

08/24/17 / #20170240513

Substituted pyrimidines as inhibitors of hif prolyl hydroxylase

The present invention concerns compounds of Formula I that inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions comprising such a compound and a pharmaceutical... Merck Sharp & Dohme Corp

08/24/17 / #20170240523

Factor xia inhibitors

The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoaguability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.... Merck Sharp & Dohme Corp

08/24/17 / #20170240524

Factor xia inhibitors

The present invention provides a compound of Formula (I) (Formula(I)) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma... Merck Sharp & Dohme Corp

08/24/17 / #20170240539

Preparation and use of cyclic sulfonamide derivatives as par-1 receptor antagonists

The present invention relates to cyclic sulfonamide derivatives of Formula (I) or a pharmaceutically acceptable salt thereof.... Merck Sharp & Dohme Corp

08/24/17 / #20170240555

Inhibitors of hif prolyl hydroxylase

The present invention concerns a compound of formula I or a pharmaceutically acceptable salt thereof, which inhibit HIF prolyl hydroxylase, their use for enhancing endogenous production of erythropoietin, and for treating conditions associated with reduced endogenous production of erythropoietin such as anemia and like conditions, as well as pharmaceutical compositions... Merck Sharp & Dohme Corp

08/24/17 / #20170240567

Ethyl n-boc piperidinyl pyrazolo pyridones as janus kinase inhibitors

The instant invention provides compounds of Formula (I) which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer. The present invention provides novel compounds which are inhibitors of JAKs. The invention also provides a method for the... Merck Sharp & Dohme Corp








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