公开(公告)号：US06881743B2

公开(公告)日：2005-04-19

申请号：US10071073

申请日：2002-02-08

申请人： Nicole Chantel Barvian ,  David Thomas Connor ,  Patrick Michael O'Brien ,  Daniel Fred Ortwine ,  William Chester Patt ,  Kevon Ray Shuler ,  Michael William Wilson

发明人： Nicole Chantel Barvian ,  David Thomas Connor ,  Patrick Michael O'Brien ,  Daniel Fred Ortwine ,  William Chester Patt ,  Kevon Ray Shuler ,  Michael William Wilson

IPC分类号： A61K20060101 ,  A61K31/44 ,  A61K31/4427 ,  A61P20060101 ,  A61P9/00 ,  A61P9/04 ,  A61P19/00 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D20060101 ,  C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D521/00 ,  A61K31/4412 ,  C07D405/12

CPC分类号： C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR4R5, CN, or CF3, E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted, n is an integer of from 0 to 6.

摘要翻译： 选择性MMP-13抑制剂是下式的吡啶衍生物或其药学上可接受的盐，其中：R 1和R 2独立地是氢，卤素，羟基，C

公开(公告)号：US07015237B2

公开(公告)日：2006-03-21

申请号：US10842863

申请日：2004-05-10

申请人： Nicole Chantel Barvian ,  David Thomas Connor ,  Patrick Michael O'Brien ,  Daniel Fred Ortwine ,  William Chester Patt ,  Michael William Wilson

发明人： Nicole Chantel Barvian ,  David Thomas Connor ,  Patrick Michael O'Brien ,  Daniel Fred Ortwine ,  William Chester Patt ,  Michael William Wilson

IPC分类号： A61K31/4412 ,  C07D213/53

CPC分类号： C07D213/80 ,  C07D213/81 ,  C07D213/82 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： Selective MMP-13 inhibitors are pyridine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R1 and R2 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.

摘要翻译： 选择性MMP-13抑制剂是下式的吡啶衍生物或其药学上可接受的盐，其中：R 1和R 2独立地是氢，卤素，羟基，C

公开(公告)号：US06906094B2

公开(公告)日：2005-06-14

申请号：US10362104

申请日：2001-05-08

申请人： Nicole Chantel Barvian ,  Patrick Michael O'Brien ,  William Chester Patt ,  Joseph Armand Picard ,  Drago Robert Sliskovic

发明人： Nicole Chantel Barvian ,  Patrick Michael O'Brien ,  William Chester Patt ,  Joseph Armand Picard ,  Drago Robert Sliskovic

IPC分类号： C07D295/08 ,  A61K31/27 ,  A61K31/381 ,  A61K31/40 ,  A61K31/404 ,  A61K31/5375 ,  A61P9/00 ,  A61P9/10 ,  A61P11/06 ,  A61P17/06 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C307/10 ,  C07C311/48 ,  C07C311/60 ,  C07D207/08 ,  C07D209/14 ,  C07D209/48 ,  C07D213/30 ,  C07D295/088 ,  C07D333/16 ,  C07D209/04

CPC分类号： C07D209/48 ,  C07D209/14 ,  C07D213/30 ,  C07D295/088 ,  C07D333/16

摘要： The present invention provides compounds of formula (I) wherein R, Z, Y, W, R5, V, and X are as defined in the description, and pharmaceutically acceptable salts thereof, which are useful for the treatment of diseases responsive to the inhibition of the enzyme 15-lipoxygenase. Thus, the compounds of formula (I) and their pharmaceutically acceptable salts are useful for treating diseases with an inflammatory component, including atherosclerosis, diseases involving chemotaxis of monocytes, inflammation, stroke, coronary artery disease, asthma, arthritis, colorectal cancer, and psoriasis.

摘要翻译： 本发明提供式（I）化合物，其中R，Z，Y，W，R 5，V和X如说明书中所定义，及其药学上可接受的盐，其可用于 对抑制酶15-脂肪氧合酶的疾病的治疗。 因此，式（I）化合物及其药学上可接受的盐可用于治疗具有炎性成分的疾病，包括动脉粥样硬化，涉及单核细胞趋化性疾病，炎症，中风，冠状动脉疾病，哮喘，关节炎，结肠直肠癌和牛皮癣的疾病 。

公开(公告)号：US07214712B2

公开(公告)日：2007-05-08

申请号：US11238502

申请日：2005-09-29

申请人： Nicole Chantel Barvian ,  David Thomas Connor ,  Richard Dennis Dyer ,  Adam Richard Johnson ,  William Chester Patt

发明人： Nicole Chantel Barvian ,  David Thomas Connor ,  Richard Dennis Dyer ,  Adam Richard Johnson ,  William Chester Patt

IPC分类号： C07C229/00 ,  A61K31/195 ,  A61K31/19

CPC分类号： C07D213/30 ,  C07C69/80 ,  C07C69/90 ,  C07C69/92 ,  C07C229/60 ,  C07C233/66 ,  C07C233/69 ,  C07C233/73 ,  C07C233/75 ,  C07C233/78 ,  C07C235/60 ,  C07D285/14 ,  C07D317/54 ,  C40B50/14

摘要： Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.

摘要翻译： 选择性MMP-13抑制剂是下式的间苯二甲酸衍生物，其中：R 1，R 2和R 3独立地是氢，卤素， 羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， C 1 -C 6亚烷基，C 2 -C 6炔基，NO 2，NR 2， 4，R 5，CN或CF 3; E独立地为O或S; A和B独立地为OR 4或NR 4 R 5; 每个R 4和R 5独立地是H，C 1 -C 6烷基，C 2 C 1 -C 6亚烷基，C 2 -C 6炔基，（CH 2 2） （CH 2）2芳基，（CH 2）2芳基，（CH 2 CH 2）n个杂芳基， 或R 4和R 5与它们所连接的氮原子一起形成3至8元环，任选含有选自O，S的杂原子 ，或NH，并且任选取代或未取代; n为0〜6; 或其药学上可接受的盐。 该化合物可用于治疗由MMP酶介导的哺乳动物中的疾病。

公开(公告)号：US06995151B2

公开(公告)日：2006-02-07

申请号：US10075918

申请日：2002-02-13

申请人： Nicole Chantel Barvian ,  David Thomas Connor ,  Richard Dennis Dyer ,  Adam Richard Johnson ,  William Chester Patt

发明人： Nicole Chantel Barvian ,  David Thomas Connor ,  Richard Dennis Dyer ,  Adam Richard Johnson ,  William Chester Patt

IPC分类号： A61K31/541 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/4025

CPC分类号： C07D213/30 ,  C07C69/80 ,  C07C69/90 ,  C07C69/92 ,  C07C229/60 ,  C07C233/66 ,  C07C233/69 ,  C07C233/73 ,  C07C233/75 ,  C07C233/78 ,  C07C235/60 ,  C07D285/14 ,  C07D317/54 ,  C40B50/14

摘要： Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.

摘要翻译： 选择性MMP-13抑制剂是下式的间苯二甲酸衍生物：化学式id =“CHEM-US-00001”num =“000

公开(公告)号：US06686355B2

公开(公告)日：2004-02-03

申请号：US10074667

申请日：2002-02-13

申请人： Nicole Chantel Barvian ,  Patrick Michael O'Brien ,  William Chester Patt ,  Drago Robert Sliskovic

发明人： Nicole Chantel Barvian ,  Patrick Michael O'Brien ,  William Chester Patt ,  Drago Robert Sliskovic

IPC分类号： C07D27912

CPC分类号： C07D417/12 ,  C07D279/12

摘要： Inhibitors of MMP enzymes are cyclic sulfonamides of Formula I or a pharmaceutically acceptable salt thereof, and cyclic sulfonamides of Formula III or a pharmaceutically acceptable salt thereof, wherein R1 and R2 include hydrogen, alkyl, and substituted alkyl; R3 and R4 include hydrogen, halo, and alkyl; X is OH or NHOH: Z is (CH2)n: and Y is S, SO or SO2. The compounds of Formulas I and III are useful for the treatment of diseases mediated by an MMP enzyme, including cancer, osteoarthritis, rheumatoid arthritis, heart failure, and inflammation.

摘要翻译： MMP酶的抑制剂是式I的环状磺酰胺或其药学上可接受的盐，以及式III的环状磺酰胺或其药学上可接受的盐，其中R 1和R 2包括氢，烷基和取代的烷基; R 3和R 4包括氢，卤素和烷基; X是OH或NHOH：Z是（CH 2）n：Y是S，SO或SO 2。 式I和III的化合物可用于治疗由MMP酶介导的疾病，包括癌症，骨关节炎，类风湿性关节炎，心力衰竭和炎症。

公开(公告)号：US06936616B2

公开(公告)日：2005-08-30

申请号：US10075909

申请日：2002-02-13

申请人： Nicole Chantel Barvian ,  William Chester Patt

发明人： Nicole Chantel Barvian ,  William Chester Patt

IPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/541 ,  A61P9/04 ,  A61P19/02 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07D239/28 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D413/02 ,  C07D417/02 ,  C07D43/02

CPC分类号： C07D239/28 ,  A61K31/505 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/541 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

摘要： Selective MMP-13 inhibitors are pyrimidine derivatives of the formula or a pharmaceutically acceptable salt thereof, wherein: R2 is hydrogen, halo, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, C2-C6 alkenyl, C2-C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; R4 and R5 independently are H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring containing carbon atoms and optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is an integer of from 0 to 6.

摘要翻译： 选择性MMP-13抑制剂是下式的嘧啶衍生物或其药学上可接受的盐，其中：R 2是氢，卤素，羟基，C 1 -C 3烷基， C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6亚烯基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6亚烷基，C NO 2，NO 2，SO 2，NO 3，CN ，或CF 3 3; E独立地为O或S; A和B独立地为OR 4或NR 4 R 5; R 4和R 5独立地是H，C 1 -C 6烷基，C 2， C 1 -C 6亚烷基，C 2 -C 6亚炔基，（CH 2 CH 2） （CH 2）2芳基，（CH 2 CH 2）n - 环烷基，（CH 2 CH 2）n - 杂芳基，或 当与它们相连的氮原子一起连接时，R 4和R 5可以形成含有碳原子的3-8元环，并且任选含有选自O ，S或NH，并且任选取代或未取代; n为0〜6的整数。

公开(公告)号：US20090105349A1

公开(公告)日：2009-04-23

申请号：US11572760

申请日：2005-08-08

申请人： Nicole Chantel Barvian ,  Daniel Yunlong Du ,  Lain-Yen Hu ,  Donna Michele Iula ,  Bruce Allen Lefker ,  Huangshu Lei ,  Raj Kumar Raheja ,  Yvonne Dorothy Smith

发明人： Nicole Chantel Barvian ,  Daniel Yunlong Du ,  Lain-Yen Hu ,  Donna Michele Iula ,  Bruce Allen Lefker ,  Huangshu Lei ,  Raj Kumar Raheja ,  Yvonne Dorothy Smith

IPC分类号： A61K31/135 ,  A61P5/26

CPC分类号： A61K31/275

摘要： The present invention is directed to the discovery of a new class of androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease sebum secretion and to stimulate hair growth.

摘要翻译： 本发明涉及新型雄激素受体调节剂的发现。 本发明的其它方面涉及这些化合物减少皮脂分泌和刺激毛发生长的用途。