Osi Pharmaceuticals, Inc.

Arno G Steinig

Mark Joseph Mulvihill

An-Hu Li

Jing Wang

Andrew Philip Crew

Hanqing Dong

Radoslaw Laufer

Douglas S Werner

Xin Chen

Qinghua Weng

Andrew Kleinberg

Arlindo Lucas Castelhano

Heather Renee Coate

Bijoy Panicker

Meizhong Jin

Bryan McKibben

Kenneth W Foreman

Anthony Innocenzo Nigro

Lee Daniel Arnold

Eric W Collington

Ayako Honda

Yingchuan Sun

Kristen Michelle Mulvihill

Tao Zhang

Kam W Siu

Quinghua Weng

Cara Cesario

Michael J Wyle

Dan Maarten Berger

Han-Qing Dong

James G Tarrant

Robin Wilkes

Keith Hornberger

Ramesh C Gupta

Mridula Kadalbajoo

Lifu Ma

Qun-Sheng Ji

Lydia Saroglou

Ti Wang

Rajaram Sangem

Melzhong Jin

Bryan Mckibben

Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention.

Substituted pteridinones for the treatment of cancer

6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors

Compounds of Formula I, as shown below and defined herein: (I) pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers mediated at least in part by Ron and/or Met. 

Substituted pyrrolo[2,3-b]-pyridines and -pyrazines

Compounds of Formula I, as shown below and defined herein:  pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven at least in part by at least one of RON, MET or ALK. This Abstract is not limiting of the invention.

Fused bicyclic kinase inhibitors

Compounds of Formula 1, as shown below and defined herein: 

7-aminofuropyridine derivatives

2-Aminopyridine compounds having the structure of Formula I, and pharmaceutically acceptable salts of these compounds. Compounds of Formula I inhibit the activity of tyrosine kinase enzymes in animals, including humans, and are useful in the treatment and/or prevention of various diseases and conditions. In particular, compounds disclosed herein are inhibitors of kinases, in particular, but not limited to, KDR, Tie-2, Flt3, FGFR3, Ab1, Aurora A, c-Src, IGF-1R, ALK, c-MET, RON, PAK1, PAK2, and TAK1, and can be used in the treatment of proliferative diseases, such as, but not limited to, cancer. The present invention is also directed to a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula I, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. The present invention is further directed to a method of treating a patient having a condition which is mediated by protein kinase activity by administering to the patient a therapeutically effective amount of the above-mentioned pharmaceutical composition. 

2-aminopyridine kinase inhibitors

Furo[3,2-c]Pyridine and Thieno[3,2-c]pyridine compounds of Formula I, and pharmaceutically acceptable salts thereof, preparation, intermediates, pharmaceutical compositions, and use, such as in disease treatment, including cancers, including conditions in which EMT is involved, including conditions mediated by protein kinase activity such as RON and/or MET. 

Furo[3,2-C]pyridines

Compounds of the formula  and pharmaceutically acceptable salts thereof, wherein X, X, X, X, X, X, X, R, and Qare defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

The subject invention provides compounds having the structure: 

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Compounds of the formula and pharmaceutically acceptable salts thereof, wherein X, X, X, and Qare defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of hyperproliferative diseases such as cancer, inflammation, psoriasis, allergy/asthma, disease and conditions of the immune system, disease and conditions of the central nervous system.

Substituted thienol[2,3-d]pyrimidines as kinase inhibitors

The subject invention provides compounds having the structure: wherein Ris substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or Rand Rare joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present Ris oxygen; Rand Rare each independently substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or RNRtogether form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms;

Compounds of the formula and pharmaceutically acceptable salts thereof, wherein Qand Rare defined herein, inhibit the IGF-1R enzyme and are useful for the treatment and/or prevention of various diseases and conditions that respond to treatment by inhibition of tyrosine kinases.

Imidazopyrazine tyrosine kinase inhibitors

The subject invention provides compounds having the structure:wherein Ris substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; Ris hydrogen, or a substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or Rand Rare joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present Ris oxygen; Rand Rare each independently substituted or unsubstituted alkyl, &#x2014;C(O)-alkyl, &#x2014;C(O)&#x2014;O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or RNRtogether form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; Ris hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the Aadenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

Pyrimidine A2b selective antagonist compounds, their synthesis and use

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East Northport, NY, United States of America

Arno G Steinig