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131. 发明授权

US07662966B2 Benzoimidazole compounds 有权
公开(公告)号：US07662966B2
公开(公告)日：2010-02-16
申请号：US12229892
申请日：2008-08-26
申请人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
发明人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
IPC分类号： C07D211/68 , C07D211/80 , C07D213/02
CPC分类号： C07D235/18 , C04B35/632 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07K16/00 , C07K2317/50 , C07K2317/53 , C07K2318/10
摘要： Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

132. 发明申请

US20090281096A1 CYCLOTHIOCARBAMATE DERIVATIVES AS PROGESTERONE RECEPTOR MODULATORS 失效
标题翻译：环磷酰胺衍生物作为孕激素受体调节剂
公开(公告)号：US20090281096A1
公开(公告)日：2009-11-12
申请号：US12420085
申请日：2009-04-08
申请人： Puwen Zhang , Andrew Fensome , Eugene A. Terefenko , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Jay E. Wrobel , Mark A. Collins
发明人： Puwen Zhang , Andrew Fensome , Eugene A. Terefenko , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley , Jay E. Wrobel , Mark A. Collins
IPC分类号： A61K31/536 , C07D265/18 , C07D265/14 , A61P5/00
CPC分类号： A61K31/536 , A61K31/538 , C07D265/18 , C07D413/04
摘要： Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.
摘要翻译：提供使用孕酮受体激动剂用于避孕的化合物和单独或与雌激素受体激动剂或孕酮受体拮抗剂联合治疗孕激素相关性疾病的方法。这些化合物具有以下结构：其中R1，R2，R3，R4，R5和Q1如本文所定义。

133. 发明申请

US20090270613A1 Benzoimidazole compounds 有权
公开(公告)号：US20090270613A1
公开(公告)日：2009-10-29
申请号：US12229781
申请日：2008-08-26
申请人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
发明人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
IPC分类号： C07D243/08 , C07D403/02 , C07D235/04 , C07D401/14 , C07D403/14 , C07D401/02
CPC分类号： C07D235/18 , C04B35/632 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07K16/00 , C07K2317/50 , C07K2317/53 , C07K2318/10
摘要： Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

134. 发明申请

US20090270366A1 Benzoimidazole compounds 有权
公开(公告)号：US20090270366A1
公开(公告)日：2009-10-29
申请号：US12229890
申请日：2008-08-26
申请人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
发明人： James P. Edwards , Michael D. Hack , David E. Kindrachuk , Jennifer D. Venable
IPC分类号： A61K31/551 , A61K31/497 , A61K31/4525 , A61K31/4545 , A61P37/08 , A61K31/4178 , A61K31/55
CPC分类号： C07D235/18 , C04B35/632 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07K16/00 , C07K2317/50 , C07K2317/53 , C07K2318/10
摘要： Benzoimidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.

135. 发明申请

US20080194630A1 LTA4H modulators and uses thereof 审中-公开
标题翻译： LTA4H调节剂及其用途
公开(公告)号：US20080194630A1
公开(公告)日：2008-08-14
申请号：US12069943
申请日：2008-02-14
申请人： William T. Barchuk , Paul J. Dunford , James P. Edwards , Anne M. Fourie , Lars Karlsson , Joanne M. Quan
发明人： William T. Barchuk , Paul J. Dunford , James P. Edwards , Anne M. Fourie , Lars Karlsson , Joanne M. Quan
IPC分类号： A61K31/4535 , A61K31/426 , A61K31/423 , A61P43/00
CPC分类号： A61K31/423 , A61K31/426 , A61K31/4535
摘要： Leukotriene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and/or conditions associated with inflammation.
摘要翻译：白细胞三烯A4水解酶（LTA4H）抑制剂，含有它们的组合物，以及用于抑制LTA4H酶活性以及治疗，预防或抑制与炎症相关的炎症和/或病症的方法。

136. 发明申请

US20080194577A1 2-Aminopyrimidine modulators of the histamine H4 receptor 有权
标题翻译：组胺H 4受体的2-氨基嘧啶调节剂
公开(公告)号：US20080194577A1
公开(公告)日：2008-08-14
申请号：US12070051
申请日：2008-02-14
申请人： Hui Cai , Frank Chavez , James P. Edwards , Anne E. Fitzgerald , Jing Liu , Neelakandha S. Mani , Danielle K. Neff , Michele C. Rizzolio , Brad M. Savall , Deborah M. Smith , Jennifer D. Venable , Jianmei Wei , Ronald L. Wolin
发明人： Hui Cai , Frank Chavez , James P. Edwards , Anne E. Fitzgerald , Jing Liu , Neelakandha S. Mani , Danielle K. Neff , Michele C. Rizzolio , Brad M. Savall , Deborah M. Smith , Jennifer D. Venable , Jianmei Wei , Ronald L. Wolin
IPC分类号： A61K31/496 , C07D239/48 , A61K31/505 , A61P37/08 , C07K14/705 , A61P17/00 , A61P29/00 , C07D403/04
CPC分类号： C07D498/04 , C07D239/48 , C07D239/70 , C07D239/95 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/10 , C07D519/00
摘要： 2-Aminopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
摘要翻译：描述了2-氨基嘧啶化合物，其可用作H 4 S 5受体调节剂。这样的化合物可以用于治疗由H 4 S受体活性介导的疾病状态，病症和病症的药物组合物和方法，例如过敏，哮喘，自身免疫疾病和瘙痒症。

137. 发明授权

US07265102B2 Substituted pyrazoles 有权
标题翻译：取代的吡唑
公开(公告)号：US07265102B2
公开(公告)日：2007-09-04
申请号：US11147923
申请日：2005-06-08
申请人： Hui Cai , James P. Edwards , Steven P Meduna , Barbara A. Pio , Jianmei Wei
发明人： Hui Cai , James P. Edwards , Steven P Meduna , Barbara A. Pio , Jianmei Wei
IPC分类号： A61K31/4155 , A61P11/06 , C07D401/14 , C07D403/06
CPC分类号： C07D413/14 , A61K31/275 , A61K31/4155 , A61K31/4439 , A61K31/454 , A61K31/495 , A61K31/55 , C07D401/14 , C07D409/14 , C07D471/04 , C07D471/14
摘要： Substituted pyrazoles of general formula methods of manufacturing them, compositions containing them, and methods of using them to, for example, treat autoimmune diseases mediated by cathepsin S, and inhibit cathepsin S activity, are described.
摘要翻译：描述了制备它们的通式的取代吡唑，含有它们的组合物，以及将其用于例如治疗由组织蛋白酶S介导的自身免疫性疾病和抑制组织蛋白酶S活性的方法。

138. 发明授权

US07253200B2 Imidazole compounds 有权
标题翻译：咪唑化合物
公开(公告)号：US07253200B2
公开(公告)日：2007-08-07
申请号：US11088488
申请日：2005-03-24
申请人： Daniel J. Buzard , James P. Edwards , David E. Kindrachuk , Jennifer D. Venable
发明人： Daniel J. Buzard , James P. Edwards , David E. Kindrachuk , Jennifer D. Venable
IPC分类号： A01N43/50 , C07D233/02
CPC分类号： C07D471/04 , C07D233/64 , C07D235/18 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/14
摘要： Imidazole compounds, compositions, and methods of using them in leukocyte recruitment inhibition, in modulating H4 receptor expression, and in treating conditions such as inflammation, H4 receptor-mediated conditions, and related conditions.
摘要翻译：咪唑类化合物，组合物及其在白细胞募集抑制中的用途，调节H4受体表达以及治疗诸如炎症，H 4受体介导的病症和相关条件。

139. 发明授权

US07084168B2 Indoline derivatives 失效
公开(公告)号：US07084168B2
公开(公告)日：2006-08-01
申请号：US10456892
申请日：2003-06-06
申请人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H.W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Andrew Fensome , Lori L. Miller , John W. Ullrich , Reinhold H.W. Bender , Puwen Zhang , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31/404 , C07D209/34
CPC分类号： C07D209/34 , C07D209/96 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04 , C07D491/10
摘要： This invention relates to substituted indoline derivative compounds which are antagonists of the progesterone receptor, their preparation and pharmaceutical utility, particularly including contraception and treatment of benign or malignant neoplastic diseases, having the general structure: wherein R1 and R2 may be single substituents or fused to form spirocyclic rings.

140. 发明授权

US06982261B2 Cyanopyrroles 失效
标题翻译：青色
公开(公告)号：US06982261B2
公开(公告)日：2006-01-03
申请号：US10342719
申请日：2003-01-15
申请人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
发明人： Mark A. Collins , Valerie A. Mackner , Jay E. Wrobel , Lin Zhi , Todd K. Jones , James P. Edwards , Christopher M. Tegley
IPC分类号： A61K31/54 , A01K31/535 , C07D279/16 , C07D498/00
CPC分类号： C07D403/04 , A61K31/405 , A61K31/5415 , C07D413/04
摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1–5; p=1–4; q=1–4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl, or a pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供具有其中T为O，S或不存在的结构的式1的孕酮受体拮抗剂; R 1，R 2和R 2各自独立地为氢，烷基，取代的烷基; 或R 1和R 2一起形成环，并且一起含有-CH 2（CH 2）2 CH 2 CH 2 - ， - CH 2 CH 2 CH 2 CH 2 N 2 CH 2 2 CH 2 - ， - O（CH 2）2 CH 2 - ， - （CH 2 CH 2） O（CH 2 CH 2）q O - ， - CH 2 CH 2 OCH 2 - / SUB CH 2，或CH 2 CH 2，NR 7，CH 2，CH 2， CH 2 - ; n = 1-5; p = 1-4; q = 1-4; R 3是氢，OH，NH 2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或COR A。 R A是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 4是氢，卤素，CN，NH 2，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 5是氢，烷基或取代的烷基; R 6是氢，烷基，取代的烷基或COR B; R B是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 7是氢或烷基，或其药学上可接受的盐。

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