公开(公告)号：US20070027118A1

公开(公告)日：2007-02-01

申请号：US11398810

申请日：2006-04-06

申请人： Hengmiao Cheng ,  Stephan Cripps ,  Klaus Dress ,  Buwen Huang ,  Sajiv Nair ,  Yong Wang

发明人： Hengmiao Cheng ,  Stephan Cripps ,  Klaus Dress ,  Buwen Huang ,  Sajiv Nair ,  Yong Wang

IPC分类号： A61K31/655 ,  A61K31/44 ,  A61K31/4439 ,  C07D401/02 ,  C07D213/72

CPC分类号： C07D213/76 ,  C07D213/85 ,  C07D215/38 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/10

摘要： The present invention relates to compounds with formula (I) or a pharmaceutically acceptable salt thereof: wherein; T is a (4 to 10)-membered heterocyclyl and wherein R1, R2 and R3 are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of the 11-β-hsd-1 enzyme.

摘要翻译： 本发明涉及具有式（I）的化合物或其药学上可接受的盐：其中： T是（4至10）个杂环基，其中R 1，R 2和R 3如说明书中所定义。 本发明还涉及包含式（I）化合物的药物组合物和治疗通过调节11-β-hsd-1酶介导的病症的方法。

公开(公告)号：US20050261290A1

公开(公告)日：2005-11-24

申请号：US11122599

申请日：2005-05-04

申请人： Hengmiao Cheng ,  Stephan Cripps ,  Klaus Dress ,  Jacqui Hoffman ,  Buwen Huang ,  Stanley Kupchinsky ,  Phuong Le ,  Sajiv Nair ,  Timothy Parrott ,  Christopher Smith ,  Yong Wang ,  Yi Yang

发明人： Hengmiao Cheng ,  Stephan Cripps ,  Klaus Dress ,  Jacqui Hoffman ,  Buwen Huang ,  Stanley Kupchinsky ,  Phuong Le ,  Sajiv Nair ,  Timothy Parrott ,  Christopher Smith ,  Yong Wang ,  Yi Yang

IPC分类号： A61K31/401 ,  A61K31/4025 ,  A61K31/445 ,  A61K31/5375 ,  A61K31/5377 ,  C07D207/16 ,  C07D211/26 ,  C07D211/60 ,  C07D211/96 ,  C07D241/24 ,  C07D265/30 ,  C07D277/06 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D413/02 ,  C07D413/06 ,  C07D413/12 ,  C07D453/06 ,  C07D471/04 ,  C07D43/02

CPC分类号： C07D211/26 ,  C07D207/16 ,  C07D211/60 ,  C07D211/96 ,  C07D241/24 ,  C07D265/30 ,  C07D277/06 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D405/06 ,  C07D413/06 ,  C07D413/12 ,  C07D453/06 ,  C07D471/04

摘要： The present invention relates to compounds with the formulas (I), (II), and (III), or a pharmaceutically acceptable salt thereof: wherein T is a (4 to 10)-membered heterocyclyl selected from the group consisting of and wherein R1, R2 and R3 are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formulas (I), (II), and (III) and methods of treating a condition that is mediated by the modulation of the 11-β-hsd-1 enzyme, the method comprising administering to a mammal an effective amount of a compound of formulas (I), (II), and (III).

摘要翻译： 本发明涉及具有式（I），（II）和（III）的化合物或其药学上可接受的盐：其中T是选自下组的（4至10）元素的杂环基，其中R R 1，R 2和R 3如说明书中所定义。 本发明还涉及包含式（I），（II）和（III）化合物的药物组合物和治疗由11-β-hsd-1酶的调节介导的病症的方法，所述方法包括 向哺乳动物施用有效量的式（I），（II）和（III）的化合物。

公开(公告)号：US06869962B2

公开(公告)日：2005-03-22

申请号：US10460010

申请日：2003-06-11

申请人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

发明人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

IPC分类号： A61K31/4365 ,  A61K31/444 ,  A61K31/506 ,  A61K31/5377 ,  A61P1/18 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P11/00 ,  A61P13/08 ,  A61P15/08 ,  A61P17/00 ,  A61P17/06 ,  A61P17/12 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D495/04 ,  C07D409/14

CPC分类号： A61K31/4743 ,  C07D495/04

摘要： The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.

摘要翻译： 本发明涉及由式I表示的化合物及其前体药物或代谢物，或所述化合物，所述前药和所述代谢产物的药学上可接受的盐或溶剂合物，其中Z，Y，R 11和R 14， R 16，R 17和R 17如本文所定义。 本发明还涉及含有式I化合物的药物组合物和通过施用式I化合物来治疗哺乳动物中过度增殖性疾病的方法。

公开(公告)号：US20060079548A1

公开(公告)日：2006-04-13

申请号：US11256477

申请日：2005-10-21

申请人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Palmer ,  William Romines ,  Ru Zhou

发明人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Palmer ,  William Romines ,  Ru Zhou

IPC分类号： A61K31/4743 ,  C07D498/02

CPC分类号： A61K31/4743 ,  C07D495/04

摘要： The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.

摘要翻译： 本发明涉及由式I表示的化合物及其前体药物或代谢物，或所述化合物，所述前药和所述代谢产物的药学上可接受的盐或溶剂合物，其中Z，Y，R 11和R R 15，R 16，R 16和R 17如本文所定义。 本发明还涉及含有式I化合物的药物组合物和通过施用式I化合物来治疗哺乳动物中过度增殖性疾病的方法。

公开(公告)号：US20050124662A1

公开(公告)日：2005-06-09

申请号：US10992146

申请日：2004-11-18

申请人： Robert Kania ,  Steven Bender ,  Allen Borchardt ,  Stephan Cripps ,  Cynthia Louise Palmer ,  Anna Maria Tempczyk-Russell ,  Michael Varney ,  Michael Raymond Collins

发明人： Robert Kania ,  Steven Bender ,  Allen Borchardt ,  Stephan Cripps ,  Cynthia Louise Palmer ,  Anna Maria Tempczyk-Russell ,  Michael Varney ,  Michael Raymond Collins

IPC分类号： C07D209/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  A61K31/4439 ,  A61K31/416

CPC分类号： C07D401/12 ,  C07D209/18 ,  C07D401/14 ,  C07D403/12

摘要： Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

公开(公告)号：US07045528B2

公开(公告)日：2006-05-16

申请号：US10796226

申请日：2004-03-09

申请人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

发明人： Michael Collins ,  Stephan Cripps ,  Judith Deal ,  Robert Steven Kania ,  Jihong Lou ,  Mingying He ,  Cynthia Louise Palmer ,  William Henry Romines, III ,  Ru Zhou

IPC分类号： A61K31/4365 ,  C07D495/04

CPC分类号： A61K31/4743 ,  C07D495/04

摘要： The invention relates to compounds represented by the formula I and to prodrugs or metabolites thereof, or pharmaceutically acceptable salts or solvates of said compounds, said prodrugs, and said metabolites, wherein Z, Y, R11 and R14, R15, R16, and R17 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.

公开(公告)号：US20050148631A1

公开(公告)日：2005-07-07

申请号：US11016152

申请日：2004-12-17

申请人： Hengmiao Cheng ,  Stephan Cripps ,  Martin Edwards ,  Theodore Johnson ,  Sajiv Nair ,  Michael Siu ,  Christopher Smith ,  Wendy Taylor ,  Yong Wang

发明人： Hengmiao Cheng ,  Stephan Cripps ,  Martin Edwards ,  Theodore Johnson ,  Sajiv Nair ,  Michael Siu ,  Christopher Smith ,  Wendy Taylor ,  Yong Wang

IPC分类号： A61K31/44 ,  A61K31/4436 ,  A61K31/4545 ,  C07C311/36 ,  C07C311/37 ,  C07D209/08 ,  C07D213/02 ,  C07D213/76 ,  C07D215/38 ,  C07D235/06 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D513/04 ,  C07D41/02 ,  C07D49/02

CPC分类号： C07D209/08 ,  C07D213/76 ,  C07D215/38 ,  C07D235/06 ,  C07D239/42 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D513/04

摘要： The present invention relates to compounds with the formula (I), or a pharmaceutically acceptable salt thereof: The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) or formula (II) and methods of treating a condition that is mediated by the modulation of 11-β-hsd-1, the method comprising administering to a mammal an effective amount of a compound of formula (I) or formula (II).

摘要翻译： 本发明涉及具有式（I）化合物或其药学上可接受的盐：本发明还涉及包含式（I）或式（II）化合物的药物组合物和治疗由 调节11-β-hsd-1，所述方法包括向哺乳动物施用有效量的式（I）或式（II）化合物。

公开(公告)号：US06833456B2

公开(公告)日：2004-12-21

申请号：US10371337

申请日：2003-02-21

申请人： William Henry Romines, III ,  Robert Steven Kania ,  Jihong Lou ,  Stephan Cripps ,  Ru Zhou ,  Mingying He

发明人： William Henry Romines, III ,  Robert Steven Kania ,  Jihong Lou ,  Stephan Cripps ,  Ru Zhou ,  Mingying He

IPC分类号： C07D49504

CPC分类号： C07D495/04

摘要： The invention relates to compounds represented by the formula I and to prodrugs thereof, pharmaceutically acceptable salts or solvates of said compounds or said prodrugs, wherein X, R1 and R11 are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formula I and to methods of treating hyperproliferative disorders in a mammal by administering the compounds of formula I.

摘要翻译： 本发明涉及由式I表示的化合物及其前药，所述化合物或所述前药的药学上可接受的盐或溶剂合物，其中X，R 1和R 11如本文所定义。 本发明还涉及含有式I化合物的药物组合物和通过施用式I化合物来治疗哺乳动物中过度增殖性疾病的方法。