Pfizer Corporation

Other

Pfizer Products Inc.

Jotham Wadsworth Coe

Paige Roanne Palmer Brooks

Takushi Kaneko

Brian Thomas O'Neill

Christopher John O'Donnell

Christoph Martin Dehnhardt

Peter M Jones

Gavin Alistair Whitlock

Stanton F McHardy

Eric R Larson

Anton F Fliri

Florian Michel Wakenhut

Matthew Frank Brown

Mark Edward Flanagan

Adam Matthew Gilbert

Matthew Merrill Hayward

Atli Thorarensen

Rayomand Jal Unwalla

John Isidro Trujillo

Ye Che

Justin Ian Montgomery

Agustin Casimiro-Garcia

Jonathan David Langille

Jean-Baptiste Telliez

Joseph Walter Strohbach

Jaclyn Louise Henderson

Yogesh Anil Sabnis

Yogesh Sabnis

Michael Aaron Brodney

Patrick Robert Verhoest

Lee Daniel Arnold

Chakrapani Subramanyam

Christopher John Helal

Scot Richard Mente

Jennifer Elizabeth Davoren

Ivan Viktorovich Efremov

Travis T Wager

Thomas Allen Chappie

Steven Victor O'Neil

Amy Beth Dounay

David Lawrence Firman Gray

Spiros Liras

Joseph Scott Warmus

Bethany Lyn Kormos

Yuan Zhang

Martin Youngjin Pettersson

Derek Lawrence Tickner

John Anthony Ragan

Daniel P Brannegan

Antonia Friederike Stepan

Matthew Richard Reese

Karen Jean Coffman

Paul Galatsis

Martin Patrick Allen

Brian C Vanderplas

Jinshan Michael Chen

Michelle Renee Garnsey

Mikel Paul Moyer

Ravi G Kurumbail

Lawrence Albert Vincent

Luis Angel Martinez-Alsina

Chris John Helal

John I Trujillo

Colin Richard Rose

John Arthur Allen

Edward Raymond Guilmette

Anthony Richard Harris

Deane Milford Nason

Wenjian Xu

Steven Wade Korturn

Steven Wade Kortum

Crystal G Bashore

Steven Victor O'neil

Stanton Furst Mchardy

David Lawrence Gray

Crystal Gayle Bashore

Deane Milford Ii Nason

The present invention provides a method for treating alopecia using certain pharmaceutically active pyrrolo[2,3-d]pyrimidinyl acrylamides having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description.

Pyrrolo[2,3-d]pyrimidinyl, pyrrolo[2,3-b]pyrazinyl and pyrrolo[2,3-d]pyridinyl acrylamides

The present invention provides novel imidazo[4,5-c]quinoline derivatives of Formula (I), and the pharmaceutically acceptable salts thereof I wherein R, Rand Rare as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula I and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy. 

Imidazo[4,5-C]quinoline derivatives as LRRK2 inhibitors

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylam ides and analogues thereof, having the structure: or a pharmaceutically acceptable salt thereof, as set forth in the Description. 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.

A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A' are C or N, where C may be substituted by halo or C-Calkyl; R and Rare selected from the group consisting of H, C-Calkyl, &#x2014;(CH)&#x2014;W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, &#x2014;NR&#x2033;SO&#x2014;R&#x2032;, etc., where R&#x2032; and R&#x2033; are C-Calkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and Ro and the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; Ris H, halo or cyano; Rand Rare H, C-Calkyl, etc.; X is a bond, etc.; Ris H, C-Calkyl, etc.; Y is a bond, &#x2014;(CH)&#x2014;, etc. The invention also relates to compositions and uses in the treatment of various diseases.

Pyrazolopyridines and pyrazolopyrimidines

The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced &#x3b2;-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

Heteroaromatic compounds and their use as dopamine D1 ligands

The present invention provides pharmaceutically active pyrrolo[2,3-d]pyrimidinyl and pyrrolo[2,3-d]pyridinyl acrylamides and analogues thereof, having the structure: or a pharmaceutically acceptable salt or solvate thereof, or an enantiomer or diastereomer thereof, as set forth in the Description. 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.

A compound having the structure: or a pharmaceutically acceptable salt or solvate thereof, wherein A and A' are C or N, where C may be substituted by halo or C-Calkyl; R and Rare selected from the group consisting of H, C-Calkyl, &#x2014;(CH)&#x2014;W, etc., where W is 5- or 6-membered heteroaryl or heterocyclic containing N, S and/or O atoms, &#x2014;NR&#x2033;SO&#x2014;R&#x2032;, etc., where R&#x2032; and R&#x2033; are C-Calkyl, etc.; wherein each alkyl, etc., may be substituted; or, R and Rand the N atom to which they are bonded together to form a monocyclic or bicyclic heterocyclic ring, etc.; Ris H, halo or cyano; Rand Rare H, C-Calkyl, etc.; X is a bond, etc.; Ris H, C-Calkyl, etc.; Y is a bond, &#x2014;(CH)&#x2014;, etc. The invention also relates to compositions and uses in the treatment of various diseases.

A method of treating a disease or condition for which a JAK inhibitor is indicated in a subject in need of such treatment, comprising administering to the subject a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, and particularly, a method for the treatment of various inflammatory diseases, particularly psoriasis, asthma and COPD.

Indazoles

The present invention relates to compounds of formula (I): to pharmaceutically acceptable salts therefore and to pharmaceutically acceptable solvates of said compounds and salts, wherein the substituents are defined herein; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly asthma and COPD.

The subject invention relates to 2-azabicyclo[3.3.1]nonane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, including alcohol addiction, depression, anxiety, schizophrenia and eating disorders, among others, as are more fully described herein.

2-azabicyclo[3.3.1]nonane derivatives

The present invention provides a compound having the structure of formula I: wherein Ris hydrogen, (C&#x2013;C) alkyl, unconjugated (C&#x2013;C) alkenyl, benzyl, YC(&#x2550;O)(C&#x2013;C) alkyl or &#x2014;CHCH&#x2014;O&#x2014;(C&#x2013;C) alkyl; X is CHor CHCH; Y is (C&#x2013;C) alkylene; Z is (CH), CF, or C(&#x2550;O), where m is 0, 1 or 2; Rand Rare selected independently from hydrogen, halogen, &#x2014;(C&#x2013;C) alkyl optionally substituted with from 1 to 7 halogen atoms, and &#x2014;O(C&#x2013;C) alkyl optionally substituted with from 1 to 7 halogen atoms, or Rand Reach together with the atom to which it is connected independently form C(&#x2550;O), S&#x2192;O, S(&#x2550;O), or N&#x2192;O; and is a 5- to 7-membered monocyclic heteroaryl group selected from pyridinyl, pyridone, pyridazinyl, imidazolyl, pyrimidinyl, pyrazolyl, triazolyl, pyrazinyl, furyl, thienyl, isoxazolyl, thiazolyl, oxazolyl, isothiazolyl, pyrrolyl, cinnolinyl, triazinyl, oxadiazolyl, thiadiazolyl and furazanyl groups.

Heteroaryl fused azapolycyclic compounds

The present invention relates to a compounds of formula I: wherein A, B, D, E and F are defined herein; that are useful in treating central nervous system (CNS) diseases, disorders and conditions, such as but not limited to nicotine addiction, schizophrenia, depression, Alzheimer's disease, Parkinson's disease and ADHD. The present invention further comprises pharmaceutical compositions containing such compounds and methods of treatment comprising the use of such compounds.

Diazabicyclic compounds useful in the treatment of CNS and other disorders

The present invention relates to compounds of formula I  The substituent designations are as disclosed. At least one of B, Q, D and E is nitrogen. The present invention also provides a method of treating disorders of the Central Nervous System such as schizophrenia and cognitive dysfunction.

Pharmaceutical composition for the treatment of CNS and other disorders

The subject invention relates to 3-azabicyclo[3.2.1]octane derivatives, pharmaceutical compositions comprising such derivatives and methods of using such derivatives to treat disease states, disorders and conditions mediated by opioid receptors. The subject invention also particularly relates to using such derivatives to treat certain disorders and conditions, for example irritable bowel syndrome, drug addiction, depression, anxiety, schizophrenia and eating disorders, among others.

3-azabicyclo[3.2.1]octane derivatives

This invention is directed to compounds of the formula (I): and their pharmaceutically acceptable salts, wherein R, R, and Rare as defined herein; intermediates for the synthesis of such compounds, pharmaceutical compositions containing such compounds; and methods of using such compounds in the treatment of neurological and psychological disorders.

Aryl fused azapolycyclic compounds

Growing community of inventors

Niantic, CT, United States of America

Jotham Wadsworth Coe