Abstract: The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof. Such compounds are useful for inhibiting Janus Kinase (JAK). This invention also is directed to compositions comprising methods for making such compounds, and methods for treating and preventing conditions mediated by JAK.

Abstract: The disclosure provides methods of treating cancer in a subject in need thereof comprising administering to the subject a therapeutically effective amount of PF-07104091, as a monotherapy or in combination with an endocrine therapy agent and/or a CDK4/6 inhibitor.

Abstract: The invention provides solid forms of 2-[(4-{6-[(4-Cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid, 1,3-dihydroxy-2-(hydroxymethyl) propan-2-amine salt for example, Form 1 or Form 2; as well as pharmaceutical compositions, and the uses thereof in treating diseases, conditions or disorders modulated by GLP-1R in a mammal, such as a human.

Abstract: Described herein are compounds of Formula I: I and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R7, RF, t1, Y1, and Y2 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.

Abstract: The invention relates to compounds of Formula (I)-(III) and pharmaceutically acceptable salts thereof to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds the present invention may be useful in the treatment, prevention, suppression and amelioration diseases, disorders and conditions such as cancers.

Abstract: The present invention provides novel antibodies that specifically bind to GUCY2c and uses thereof in the treatment of cancer. The present invention further provides novel bispecific antibodies comprising such antibodies and uses thereof in the treatment of cancer.

Abstract: The present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof a combination of a benzoxazole derivative transthyretin stabilizer or a pharmaceutically acceptable salt or prodrug thereof and an additional therapeutic agent for the treatment of transthyretin amyloidosis. Particularly, the present invention relates to pharmaceutical compositions and methods of treatment comprising administering to a patient in need thereof 2-(3,5-dichlorophenyl)-1,3-benzoxazole-6-carboxylic acid or a pharmaceutically acceptable salt or prodrug thereof and one or more additional therapeutic agent for the treatment of transthyretin amyloidosis.

Abstract: The present disclosure provides deuterated compounds that are inducers of KLF2 and pharmaceutical compositions comprising the same. The present disclosure further provides method of treating an inflammatory disease or endothelial dysfunction comprising administering a therapeutically effective amount of the deuterated compounds disclosed herein.

Abstract: The invention relates to compounds of Formula I? wherein R, R1, R2, R3, p, q and q? are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.

Abstract: Method for treating moderate to severe chronic hand eczema in a subject in need thereof, which method comprises the step of administering to said subject a therapeutically effective amount of the compound of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide, or a pharmaceutically acceptable salt thereof.

Abstract: Described herein is a crystalline form of (2R)-2-(5-fluoro-2-methoxypyridin-4-yl)-1-[(2S)-7-methyl-6-(pyrimidin-2-yl)-3,4-dihydro-1H-spiro[1,8-naphthyridine-2,3-pyrrolidin]-1-yl]propan-1-one having a powder X-ray diffraction pattern comprising at least one characteristic peak, in terms of 2? at a copper wavelength, selected from 8.7±0.2, 11.1±0.2, and 13.3±0.2.

Abstract: The combination of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide or pharmaceutically acceptable salt thereof, and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4?-piperidine]-1?-carbonyl)-6-methoxypyridin-2-yl)benzoic acid or pharmaceutically acceptable salt thereof, for treatment of diseases, including non-alcoholic steatohepatitis (NASH), in mammals are described herein.

Abstract: Solid forms of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5-carboxamide, including crystalline forms and an amorphous form, in addition to pharmaceutical compositions, processes for preparing, and their use to treat diseases, conditions and disorders modulated by the activity of the diacylglycerol acyltransferase 2 (DGAT2) in a mammal such as a human are described herein.

Abstract: The present disclosure relates generally to methods of preparing glycoconjugates containing a saccharide conjugated to a carrier protein by use of stable nitroxyl radical related agent/oxidant as an oxidizing agent, to immunogenic compositions comprising such glycoconjugates, and to methods for the use of such glycoconjugates and immunogenic compositions.

Abstract: The invention provides antibodies, and antigen-binding fragments thereof, that specifically bind to GDF15, as well as methods and uses for the antibodies.

Abstract: Benzodiazepine derivatives of formula (I): (I) wherein: each of R1 and R2 is independently H or halo; either (i) T is N, Z is C, and are bonds, and and are absent; or (ii) T is C, Z is N, and are bonds, and and are absent; each of R3 and R4 is independently halo, —OR6, —NR6R7, —COR8, —C(O)OR8, —CON(R8)2 or —R6; R5 is H or halo; each of R6 and R7 is independently H or a group selected from C1-C6 alkyl, C3-C10 cycloalkyl, C6-C10 aryl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, the group being unsubstituted or substituted; R8 is H or C1-C6 alkyl, each R8 being the same or different when two are present; n is 0 or 1; and one of V, W, X and Y is N or CH and the other three are CH; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.

Abstract: The invention relates to compounds of Formula (I) wherein Y1a, Y1b, Y2a, Y2b, Y2c, Y2d, Y2e, Y2f, Y2g, Y2h and Y2i are as defined herein and to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The compounds of Formula (I) may be useful in the treatment of coronavirus infections and coronavirus infection related disorders.

Abstract: The present disclosure relates to the treatment of cancer and/or cancer-associated disease. Certain aspects relate to the treatment of an individual having cancer or cancer-associated disease by administering to the individual a combination therapy of a first therapeutic agent that is an EZH2 inhibitor, a second therapeutic agent that is a CDK inhibitor, and a third therapeutic agent that is a selective estrogen receptor degrader.

Abstract: This disclosure relates to combination therapies for use in treating cancer, comprising a CDK2 inhibitor of Formula (I) and a selective CDK4 inhibitor of Formula (II), each as further described herein, optionally in further combination with an additional anti-cancer agent.