Schering Corporation

Ligand Pharmaceuticals, Inc.

Pharmacopeia Drug Discovery, Inc.

Venenum Biodesign, LLC

Pharmacopeia Inc.

Merck Sharp + Dohme Corp.

Brian F McGuinness

Stuart B Rosenblum

Joseph A Kozlowski

Douglas Walsh Hobbs

David J Diller

Gopinadhan N Anilkumar

Neng-Yang Shih

Koc-Kan Ho

Seong Heon Kim

Qingbei Zeng

Jeffrey John Letourneau

Yuefei Shao

Lin Zhi

Michael K C Wong

Cornelis Arjan Van Oeveren

Bijan Pedram

Yixing Shen

Jason Conrad Pickens

Andrew Graham Cole

David Rosen

Wensheng Yu

Guizhen Dong

Chia-Yu Huang

Axel Metzger

Lisa Guise Zawacki

Bandarpalle B Shankar

Grant E Gallagher

Gary L Schieven

Steven G Kultgen

Rukiye Nazan Eraslan

Jason Trama

James R Beasley

David E Kaelin

Michael S McQueney

John J Baldwin

Roland Ellwood Dolle

Philip D Stein

Suresh D Babu

De-Yi Yang

Kurt William Saionz

Steven David Paget

Thuy X H Le

Paul J Zavodny

Youheng Shu

Dongchuan Shi

Audrey Hospital

Jingqi Duo

Chung-Her Jenh

Andrew G Cole

Zahid Hussain

Yueheng Jiang

Venugopalareddy Bommireddy Venkata

Xiaoqing Xu

Ellen Sieber McMaster

Doublas W Hobbs

Cangmeng Yang

Carolyn Dilanni Carroll

David E Kaelin, Jr

William Ronald Solvibile, Jr

Jason C Pickens

Michael KC Wong

Changmeng Yang

Methods for treating bladder cancer and solid tumors are disclosed. The methods include administering to a patient a compound of formula 1 Pharmaceutical compositions of compound 1 are also disclosed.

Sting agonists for treating bladder cancer and solid tumors

Compounds and methods in the fields of chemistry and medicine are disclosed. Some of the disclosed embodiments include compounds, compositions and methods of using heterocycle amines. Some of the disclosed embodiments include heterocycle amines useful to treat inflammatory disorders.

Heterocycle amines and uses thereof

The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs. 

Non-systemic TGR5 agonists

The present invention provides compounds of Formula I': wherein, W, X, Y, Z, Z, Z, R, R, R, Rand Rare as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are effective at modulating the STING protein and thus can be used as medicaments for treating or preventing disorders affected by the agonism of STING.

Sting agonists

The present invention relates to tricyclic compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present tricyclic compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing tricyclic compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs.

The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin. The compounds provided include those of the general formula I: 

Biaryl oxyacetic acid compounds

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof, wherein the various moieties are defined herein. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

Heterocyclic substituted piperazines with CXCR3 antagonist activity

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

Heterocyclic substituted pyridine compounds with CXCR3 antagonist activity

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts, solvates or esters of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: or a pharmaceutically acceptable salt, solvate or ester thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, zenograft rejection), infectious diseases (e.g., tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

Heterocyclic substituted piperazine compounds with CXCR3 antagonist activity

The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates or esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.

Heteroaryl substituted pyrazinyl-piperazine-piperidines with CXCR3 antagonist activity

Growing community of inventors

Plainsboro, NJ, United States of America

Brian F McGuinness