1
Beigelman Leonid, Seiwert Scott D, Blatt Lawrence M, Andrews Steven, Haas Julia: Compounds and methods for inhibiting hepatitis c viral replication. Intermune, Array Biopharma, Beigelman Leonid, Seiwert Scott D, Blatt Lawrence M, Andrews Steven, Haas Julia, MALLON Joseph J, April 19, 2007: WO/2007/044893 (56 worldwide citation)

Macrocyclic compounds having the structures described herein arc useful for inhibiting replication of the hepatitis C virus (HCV). In preferred embodiments, the compounds are active against both the NS3 protease and the NS3 helicase of HCV. Formulae (I), (II), (III), (IV) and (V).


2

3
Inaba Takashi, Haas Julia, Shiozaki Makoto, Littman Nicole M, Yasue Katsutaka, Andrews Steven W, Sakai Atushi, Fryer Andrew M, Matsuo Takafumi, Laird Ellen R, Suma Akira, Shinozaki Yuichi, Hori Yoshikazu, Imai Hiroto, Negoro Tamotsu: Cyclopropane compounds and pharmaceutical use thereof. Japan Tobacco, Inaba Takashi, Haas Julia, Shiozaki Makoto, Littman Nicole M, Yasue Katsutaka, Andrews Steven W, Sakai Atushi, Fryer Andrew M, Matsuo Takafumi, Laird Ellen R, Suma Akira, Shinozaki Yuichi, Hori Yoshikazu, Imai Hiroto, Negoro Tamotsu, GARRETT Arthur S, June 30, 2005: WO/2005/058884 (26 worldwide citation)

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is - (CH2) m-X- (CH2)n-A1 et ...


4
Fryer Andrew M, Shiozaki Makoto, Littmann Nicole M, Inaba Takashi, Andrews Steven W, Yasue Katsutaka, Laird Ellen R, Yokota Masahiro, Haas Julia, Imai Hiroto, Maeda Katsuya, Shinozaki Yuichi, Hori Yoshikazu: N-substituted-n-sulfonylaminocyclopropane compounds and pharmaceutical use thereof. Japan Tobacco, Fryer Andrew M, Shiozaki Makoto, Littmann Nicole M, Inaba Takashi, Andrews Steven W, Yasue Katsutaka, Laird Ellen R, Yokota Masahiro, Haas Julia, Imai Hiroto, Maeda Katsuya, Shinozaki Yuichi, Hori Yoshikazu, GARRETT Arthur S, June 30, 2005: WO/2005/058808 (21 worldwide citation)

The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a N-substituted-N-sulfonylaminocyclopropane compound of formula (1) : wherein R ...


5
HAAS JULIA: SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS. ARRAY BIOPHARMA, Harris Robert J, April 29, 2010: WO/2010/048314 (18 worldwide citation)

Compounds of Formula (I) in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.


6

7

8
Beigelman Leonid, Andrews Steven W, Condroski Kevin R, Gunawaradana Indrani, Haas Julia: Inhibitors of viral replication. Intermune, Beigelman Leonid, Andrews Steven W, Condroski Kevin R, Gunawaradana Indrani, Haas Julia, MALLON Joseph J, April 26, 2007: WO/2007/047146 (5 worldwide citation)

The embodiments provide compounds of the general Formulas I-IV, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver ...


9
ANDREWS STEVEN WADE , CONDROSKI KEVIN RONALD , HAAS JULIA , JIANG YUTONG , KOLAKOWSKI GABRIELLE R , SEO JEONGBEOB , YANG HONG WOON , ZHAO QIAN : [de] Makrocyclische Verbindungen als TRK-Kinasehemmer, [en] Macrocyclic compounds as TRK kinase inhibitors, [fr] Composés macrocycliques comme inhibiteurs de la kinase TRK. ARRAY BIOPHARMA  , September 16, 2015: EP2918588-A1

[en] Compounds of Formula I : and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R 2 , R 2a , R 3 , R 3a , and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain inf ...


10
HAAS JULIA , ANDREWS STEVEN W , JIANG YUTONG , ZHANG GAN : [de] SUBSTITUIERTE PYRAZOLO[1,5-A]PYRIMIDIN-VERBINDUNGEN ALS TRK-KINASEHEMMERN, [en] SUBSTITUTED PYRAZOLO[1,5-]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS, [fr] PYRAZOLO [1,5-] PYRIMIDINE EN TANT QUINHIBITEURS DE KINASES TRK. ARRAY BIOPHARMA  , December 21, 2016: EP3106463-A1

[en] Compounds of Formula (I) in which R 1 , R 2 , R 3 , R 4 , X, Y and n have the meanings given in the specification, are inhibitors of Trk kinases and are useful in the treatment of diseases which can be treated with a Trk kinase inhibitor.