Cara Therapeutics, Inc.

Other

Accutar Biotechnology Inc.

Chromocell Corporation

Cera Therapeutics, Inc.

Avon Products, Inc.

Robert Zhiyong Luo

Yimin Qian

John W Lyga

Derek T Chalmers

Claudio Daniel Schteingart

Guangcheng Jiang

Frédérique Menzaghi

Javier Sueiras-Diaz

Robert H Spencer

Roberta Vezza Alexander

Gary Gustafson

David Palling

Janet L Ralbovsky

R Paul Beckett

Olga Babich

Yanlin Wang-Fischer

Srinivasan P Venkatachalan

Ann-Marie Campbell

Stephen J O'Connor

Jie Fan

Tatiana Shelekhin

Ke Liu

Wei He

Jason S Newcom

Jie Su

Hao Zhou

Stuart Hayden

Tina Garyantes

Carla M Gauss

Hui Zhang

Richard Foster

Christelle Henault

Peter Ottensmeyer

Mary-Margaret E Zablocki

Cecil Yip

Jolanta Idkowiak Baldys

Purvi Shah

Kevin Curran

The present disclosure relates to novel compounds of Formula (I) that degrade Bruton's tyrosine kinase (BTK), pharmaceutical compositions containing such compounds, and their use in prevention and treatment of conditions modulated by BTK. 

Substituted pyrrolopyrimidine and pyrazolopyrimidine as Bruton's tyrosine kinase (BTK) degraders

The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low PCYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: These compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.

Synthetic peptide amides

Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I:  In particular, provided herein are processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions comprising, and therapeutic methods comprising administering such compounds. In particular, provided herein are compounds for the treatment of pain.

Sodium channel modulators for the treatment of pain

The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low PCYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.

Provided herein are sodium channel modulating Compounds, in particular NaV1.7 modulating compounds of Formula I or compounds of Formula I':  In particular, provided herein are processes for the preparation of, intermediates used in the preparation of, pharmaceutical compositions comprising, and therapeutic methods comprising administering such compounds. In particular, provided herein are compounds for the treatment of pain and diabetes.

Sodium channel modulators for the treatment of pain and diabetes

The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-&#x3b1;, IL-1&#x3b2;, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.

Uses of kappa opioid synthetic peptide amides

The invention relates to methods of use of synthetic peptide amides that are ligands of the kappa opioid receptor in the treatment and prevention of kappa opioid receptor-associated diseases and conditions; and particularly to uses of these agonists in the prophylaxis, inhibition and treatment of pain, inflammation and pruritis associated with a variety of diseases, disorders and conditions. Inflammatory conditions preventable or treatable by the methods of the invention include diseases and conditions associated with elevated levels of a proinflammatory cytokines, such as TNF-&#x3b1;, IL-&#x3b2;, IL-6, MMP-1 and MMP-3. Such diseases and conditions include cardiovascular inflammation, neurological inflammation, skeletal inflammation, muscular inflammation, gastrointestinal inflammation, ocular inflammation, otic inflammation, inflammation due to insect bites and inflammation due to wound healing; atherosclerosis, ischemia, restenosis and vasculitis; of asthma, Sjogren's syndrome, pulmonary inflammation, chronic airway inflammation and chronic obstructive pulmonary disease (COPD), allergy, psoriasis, psoriatic arthritis, eczema, scleroderma, atopic dermatitis and systemic lupus erythematosus, arthritis, synovitis, osteomyelitis, rheumatoid arthritis, osteoarthritis and ankylosing spondylitis; septicemia and septic shock, diabetes, glucose intolerance, insulin resistance and obesity, colitis, ulcerative colitis, Crohn's disease, IBD and IBS, and the inflammatory diseases and conditions due to tumor proliferation, tumor metastasis or transplantation rejection.

The present invention provides substituted imidazoheterocycles having the general structure of formula I: wherein Y is chosen from &#x2014;O&#x2014;, &#x2014;OCRR&#x2014;, &#x2014;CRRO&#x2014;, &#x2014;CRR&#x2014;, &#x2014;(CRR)&#x2014;, &#x2014;NR&#x2014;, &#x2014;CRRNR&#x2014; and &#x2014;NRCRR&#x2014;. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Substituted imidazoheterocycle derivatives

The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents R, Rand Rare described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Bicyclic pyrazolo-heterocycles

The present invention provides substituted imidazoheterocyclic compounds having the structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

Substituted imidazoheterocycles

The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I  Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.

The invention includes the fitted quaternary structure of insulin receptor. It also includes methods of identifying compounds that modulate insulin receptor activity by producing a compound that interacts with all or part of the fitted quaternary structure of insulin receptor or a fragment or derivative thereof and which thereby modulates insulin receptor activity.

Identification of compounds for modulating dimeric receptors

Growing community of inventors

New City, NY, United States of America

Robert Zhiyong Luo