公开(公告)号：WO2011029027A1

公开(公告)日：2011-03-10

申请号：PCT/US2010/047856

申请日：2010-09-03

Applicant: ARRAY BIOPHARMA INC. ,  ANDREWS, Steven W. ,  CONDROSKI, Kevin Ronald ,  DE MEESE, Lisa A. ,  FELL, Jay Bradford ,  FISCHER, John P. ,  LE HUEROU, Yvan ,  JOSEY, John A. ,  KOCH, Kevin ,  MIKNIS, Gregory F. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  WALLACE, Eli M. ,  XU, Rui

Inventor： ANDREWS, Steven W. ,  CONDROSKI, Kevin Ronald ,  DE MEESE, Lisa A. ,  FELL, Jay Bradford ,  FISCHER, John P. ,  LE HUEROU, Yvan ,  JOSEY, John A. ,  KOCH, Kevin ,  MIKNIS, Gregory F. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  WALLACE, Eli M. ,  XU, Rui

IPC: C07D487/04 ,  A61K31/519

CPC classification number: C07D487/04

Abstract: Compounds of Formula I: and salts thereof in which R 1 , R 2 , R 2a , R 3 , n, X and ring B have the meanings given in the specification, are inhibitors of mTOR and are useful in the treatment of diseases which are sensitive to inhibition of mTOR, such as cancers.

Abstract translation: 式I化合物及其盐，其中R 1，R 2，R 2a，R 3，n，X和环B具有本说明书中给出的含义，是mTOR的抑制剂，可用于治疗对抑制作用敏感的疾病 mTOR，如癌症。

公开(公告)号：WO0204412A3

公开(公告)日：2002-08-22

申请号：PCT/US0141271

申请日：2001-07-05

Applicant: ARRAY BIOPHARMA INC ,  BURGESS LAURENCE E ,  GAUDINO JOHN ,  GRONEBERG ROBERT D ,  NORMAN MARK H ,  RODRIGUEZ MARTHA E ,  SUN XICHENG ,  WALLACE ELI M ,  AMGEN INC

Inventor： BURGESS LAURENCE E ,  GAUDINO JOHN ,  GRONEBERG ROBERT D ,  NORMAN MARK H ,  RODRIGUEZ MARTHA E ,  SUN XICHENG ,  WALLACE ELI M

IPC: A61K31/192 ,  A61K31/194 ,  A61K31/196 ,  A61K31/341 ,  A61K31/4045 ,  A61K31/41 ,  A61K31/4402 ,  A61P3/10 ,  A61P7/12 ,  A61P35/00 ,  A61P43/00 ,  C07C237/22 ,  C07C311/13 ,  C07C311/19 ,  C07C311/29 ,  C07D209/14 ,  C07D209/16 ,  C07D213/40 ,  C07D257/04 ,  C07D307/52 ,  A61K31/165 ,  A61K31/166

CPC classification number: C07D213/40 ,  C07C237/22 ,  C07C311/13 ,  C07C311/19 ,  C07C311/29 ,  C07D209/14 ,  C07D209/16 ,  C07D257/04 ,  C07D307/52

Abstract: Disclosed are compounds of the Formula (I), and pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, R , R , R , R and R are as defined in the specification. Such compounds are tyrosine phosphatase inhibitors and useful in the treatment or prevention of Type II Diabetes Mellitus. Also encompassed by the invention are formulations comprising the noted compounds, processes for preparing such compounds, a method for treating or preventing Type II Diabetes Mellitus.

Abstract translation: 公开了式（I）化合物及其药学上可接受的盐和前药，其中A，B，R 1，R 2，R 3，R 4和R 5如上所定义 在规范中。 这些化合物是酪氨酸磷酸酶抑制剂，可用于治疗或预防II型糖尿病。 本发明还包括包含所述化合物的制剂，制备这些化合物的方法，治疗或预防II型糖尿病的方法。

公开(公告)号：WO0220526A3

公开(公告)日：2002-05-30

申请号：PCT/US0127007

申请日：2001-08-30

Applicant: BAYER AG ,  BULLOCK WILLIAM H ,  KLUENDER HAROLD C E ,  COLLIBEE WILLIAM L ,  DALLY ROBERT ,  RODRIGUEZ MARTHA E ,  WANG MING

Inventor： BULLOCK WILLIAM H ,  KLUENDER HAROLD C E ,  COLLIBEE WILLIAM L ,  DALLY ROBERT ,  RODRIGUEZ MARTHA E ,  WANG MING

IPC: C07D295/12 ,  A61K31/136 ,  A61K31/155 ,  A61K31/395 ,  A61K31/40 ,  A61K31/403 ,  A61K31/426 ,  A61K31/438 ,  A61K31/439 ,  A61K31/445 ,  A61K31/47 ,  A61K31/496 ,  A61K31/5375 ,  A61K31/55 ,  A61P5/24 ,  A61P5/42 ,  A61P15/00 ,  A61P15/02 ,  A61P15/04 ,  A61P15/06 ,  A61P15/08 ,  A61P15/12 ,  A61P19/08 ,  A61P19/10 ,  A61P35/00 ,  A61P43/00 ,  C07C257/14 ,  C07D207/22 ,  C07D209/52 ,  C07D209/54 ,  C07D211/14 ,  C07D211/72 ,  C07D215/38 ,  C07D221/20 ,  C07D221/22 ,  C07D223/12 ,  C07D223/14 ,  C07D223/32 ,  C07D225/02 ,  C07D235/26 ,  C07D265/30 ,  C07D277/04 ,  C07D295/125 ,  C07D453/06 ,  C07D487/08 ,  A61K31/435 ,  C07D295/13

CPC classification number: C07D295/125 ,  A61K31/136 ,  A61K31/395 ,  A61K31/40 ,  A61K31/438 ,  A61K31/445 ,  A61K31/47 ,  A61K31/5375 ,  A61K31/55 ,  C07C257/14 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07D207/22 ,  C07D211/72 ,  C07D221/22 ,  C07D223/32 ,  C07D487/08

Abstract: Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.

Abstract translation: 公开了环状和非环状脒基，含有这种脒的药物组合物及其在治疗或预防孕酮受体介导的疾病或病症如骨质减少和骨质疏松症中的用途。

公开(公告)号：WO2020081848A1

公开(公告)日：2020-04-23

申请号：PCT/US2019/056786

申请日：2019-10-17

Applicant: ARRAY BIOPHARMA INC. ,  BLAKE, James F. ,  BOYS, Mark Laurence ,  CHICARELLI, Mark Joseph ,  COOK, Adam ,  ELSAYED, Mohamed S. A. ,  FELL, Jay B. ,  FISCHER, John P. ,  HINKLIN, Ronald Jay ,  MCNULTY, Oren T. ,  MEJIA, Macedonio J. ,  RODRIGUEZ, Martha E. ,  WONG, Christina E.

Inventor： BLAKE, James F. ,  BOYS, Mark Laurence ,  CHICARELLI, Mark Joseph ,  COOK, Adam ,  ELSAYED, Mohamed S. A. ,  FELL, Jay B. ,  FISCHER, John P. ,  HINKLIN, Ronald Jay ,  MCNULTY, Oren T. ,  MEJIA, Macedonio J. ,  RODRIGUEZ, Martha E. ,  WONG, Christina E.

IPC: C07D401/04 ,  C07D471/04 ,  C07D519/00 ,  A61P35/00 ,  A61K31/498 ,  A61K31/4985

Abstract: Compounds of Formula la or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases in the view of their ability to inhibit SHP2. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro , in situ , and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.

公开(公告)号：WO2011079076A1

公开(公告)日：2011-06-30

申请号：PCT/US2010/061341

申请日：2010-12-20

Applicant: ARRAY BIOPHARMA INC. ,  BOYS, Mark Laurence ,  BRADLEY, Michael ,  DELISLE, Robert Kirk ,  HENNINGS, D. David ,  KENNEDY, April L. ,  MARMSATER, Fredrik P. ,  MEDINA, Matthew ,  MUNSON, Mark C. ,  RAST, Bryson ,  RIZZI, James P. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  ZHAO, Qian

Inventor： BOYS, Mark Laurence ,  BRADLEY, Michael ,  DELISLE, Robert Kirk ,  HENNINGS, D. David ,  KENNEDY, April L. ,  MARMSATER, Fredrik P. ,  MEDINA, Matthew ,  MUNSON, Mark C. ,  RAST, Bryson ,  RIZZI, James P. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  ZHAO, Qian

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/437 ,  A61K31/4985 ,  A61P9/00 ,  A61P19/08 ,  A61P29/00 ,  A61P35/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R 1 , R 2 , R 3 , R 4 and R 5 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain.

Abstract translation: 其中R1，R2，R3，R4和R5具有本说明书中给出的含义的式（I）化合物及其药学上可接受的盐是cFMS的抑制剂，可用于治疗骨相关疾病，癌症，自身免疫 疾病，炎性疾病，心血管疾病和疼痛。

公开(公告)号：WO2010080864A1

公开(公告)日：2010-07-15

申请号：PCT/US2010/020304

申请日：2010-01-07

Applicant: ARRAY BIOPHARMA INC. ,  RODRIGUEZ, Martha, E. ,  MARESKA, David, A. ,  HANS, Jeremy, J. ,  HARVEY, Darren, M. ,  GRONEBERG, Robert, D. ,  O'SULLIVAN, Michael

Inventor： RODRIGUEZ, Martha, E. ,  MARESKA, David, A. ,  HANS, Jeremy, J. ,  HARVEY, Darren, M. ,  GRONEBERG, Robert, D. ,  O'SULLIVAN, Michael

IPC: A01N43/42

CPC classification number: C07D413/14 ,  A61K31/445 ,  C07D401/12 ,  C07D401/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/06 ,  C07D417/14 ,  C07D471/04

Abstract: A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I) wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.

Abstract translation: 一种预防和/或治疗代谢性疾病，脑血管疾病等的方法，其包括向哺乳动物施用有效量的式（I）化合物，其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂合物或其前药。 和式（I-1）的新化合物：其中所有符号具有与说明书中定义的相同的含义; 其盐，其N-氧化物，其溶剂化物或其前药具有抗糖尿病作用和神经保护作用。 因此，式（I）的化合物和式（I-1）的化合物可用于预防和/或治疗诸如糖尿病，脑血管疾病如中风等的代谢疾病的方法。

公开(公告)号：WO2012082689A1

公开(公告)日：2012-06-21

申请号：PCT/US2011/064549

申请日：2011-12-13

Applicant: ARRAY BIOPHARMA INC. ,  BOYS, Mark Laurence ,  DELISLE, Robert Kirk ,  HICKEN, Erik James ,  KENNEDY, April L. ,  MARESKA, David A. ,  MARMSATER, Fredrik P. ,  MUNSON, Mark C. ,  NEWHOUSE, Brad ,  RAST, Bryson ,  RIZZI, James P. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  ZHAO, Qian

Inventor： BOYS, Mark Laurence ,  DELISLE, Robert Kirk ,  HICKEN, Erik James ,  KENNEDY, April L. ,  MARESKA, David A. ,  MARMSATER, Fredrik P. ,  MUNSON, Mark C. ,  NEWHOUSE, Brad ,  RAST, Bryson ,  RIZZI, James P. ,  RODRIGUEZ, Martha E. ,  TOPALOV, George T. ,  ZHAO, Qian

IPC: C07D471/04 ,  A61K31/437 ,  A61P35/00

CPC classification number: C07D471/04 ,  A61K31/496 ,  A61K45/06

Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof in which R 1 , R 2 , R 3 , R 4 , R 5 and R 6 have the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of fibrosis, bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases, pain and burns in a mammal.

Abstract translation: 式I化合物及其药学上可接受的盐，其中R 1，R 2，R 3，R 4，R 5和R 6具有说明书中给出的含义，是cFMS的抑制剂，可用于治疗纤维化，骨相关疾病，癌症 ，自身免疫性疾病，炎性疾病，心血管疾病，哺乳动物的疼痛和灼伤。