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1. 发明授权

US06919343B2 N-biphenyl(substituted methyl) aminocycloalkane-carboxamide derivatives 有权
标题翻译： N-联苯（取代甲基）氨基环烷基 - 甲酰胺衍生物
公开(公告)号：US06919343B2
公开(公告)日：2005-07-19
申请号：US10354674
申请日：2003-01-30
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
IPC分类号： A61K31/166 , A61K31/24 , A61K31/41 , A61K31/42 , A61K31/4245 , A61K31/505 , A61P1/02 , A61P1/04 , A61P1/16 , A61P1/18 , A61P9/10 , A61P11/00 , A61P11/06 , A61P11/08 , A61P13/10 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/08 , A61P21/00 , A61P25/04 , A61P25/06 , A61P25/28 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , C07C237/24 , C07D213/82 , C07D239/28 , C07D257/04 , C07D261/18 , C07D271/06 , C07D403/12 , C07D413/12 , A61K31/165
CPC分类号： C07D257/04 , C07D213/82 , C07D239/28 , C07D261/18 , C07D271/06 , C07D403/12 , C07D413/12
摘要： N-Biphenyl(substituted methyl)aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-联苯（取代的甲基）氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

2. 发明授权

US07790754B2 Alpha-hydroxy amides as bradykinin antagonists or inverse agonists 有权
标题翻译： α-羟基酰胺作为缓激肽拮抗剂或反向激动剂
公开(公告)号：US07790754B2
公开(公告)日：2010-09-07
申请号：US10583675
申请日：2004-12-17
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
IPC分类号： A61K31/4439 , C07D413/10
CPC分类号： C07D239/26 , C07C235/06 , C07C235/08 , C07C235/12 , C07C235/26 , C07C235/34 , C07C235/40 , C07C2601/02 , C07C2601/04 , C07C2601/18 , C07D209/12 , C07D213/56 , C07D213/61 , C07D257/04 , C07D271/06 , C07D275/06 , C07D401/10 , C07D413/10
摘要： α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3) (CH2)nNRbSO2Rd. (4) (CH2)nNRbCO2Ra. (5) (CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6) (CH2)kCO2Ra. and (7) (CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl.
摘要翻译：通式（I）的α-羟基酰胺衍生物是可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状的缓激肽B1拮抗剂或反向激动剂。 R2a选自（1）选自Ra的基团。（2）（CH2）nNRbC（O）Ra。（3）（CH2）nNRbSO2Rd。（4）（CH2）nNRbCO2Ra。（5）（CH2）k-杂环，其任选被1至3个独立地选自卤素，硝基，氰基，硫代C 1-4烷基和C 1-3卤代烷基的基团取代，其中所述杂环是（a）5元杂芳族环，其具有选自NO和S的环杂原子，并且任选地具有至多3个另外的环氮原子，其中所述环任选地被苯并稠合; 或（b）含有1至3个环氮原子的6-元杂环和其N-氧化物。其中所述环任选地被苯并稠合。（6）（CH2）kCO2Ra。和（7）（CH 2）C（O）NR b R c。 R2b是OH或选自R2a的基团; 或R 2a和R 2b与它们所连接的碳原子一起形成任选被1至4个独立地选自卤素的基团取代的3至7元碳环。 ORa。 C 1-4烷基和C 1-4卤代烷基。

3. 发明授权

US07091380B2 N-biphenylmethyl aminocycloalkanecarboxamide derivatives 有权
标题翻译： N-联苯甲基氨基环烷烃甲酰胺衍生物
公开(公告)号：US07091380B2
公开(公告)日：2006-08-15
申请号：US10503502
申请日：2003-02-04
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Dong-Mei Feng , Scott D. Kuduk , Dai-Shi Su , Jenny Miu-chun Wai
IPC分类号： C07C233/05 , C07C233/65 , A61K31/165
CPC分类号： C07C237/24 , C07C237/22 , C07C2601/02 , C07D209/48 , C07D213/81 , C07D213/82 , C07D231/12 , C07D237/24 , C07D239/28 , C07D241/44 , C07D249/08 , C07D249/10 , C07D257/04 , C07D261/18 , C07D263/34 , C07D271/06 , C07D307/68 , C07D317/68 , C07D333/38 , C07D333/70 , C07D403/12 , C07D413/12
摘要： N-Biphenyl(substituted methyl) aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-联苯（取代的甲基）氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

4. 发明申请

US20080318976A1 Alpha-Hydroxy Amides as Bradykinin Antagonists or Inverse Agonists 有权
标题翻译： α-羟基酰胺作为缓激肽拮抗剂或反激动剂
公开(公告)号：US20080318976A1
公开(公告)日：2008-12-25
申请号：US10583675
申请日：2004-12-17
申请人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
发明人： Michael R. Wood , Neville J. Anthony , Mark G. Bock , Scott D. Kuduk
IPC分类号： A61K31/4439 , C07D413/10 , C07C229/36 , A61K31/505 , A61P25/00 , C07D239/24 , A61K31/24
CPC分类号： C07D239/26 , C07C235/06 , C07C235/08 , C07C235/12 , C07C235/26 , C07C235/34 , C07C235/40 , C07C2601/02 , C07C2601/04 , C07C2601/18 , C07D209/12 , C07D213/56 , C07D213/61 , C07D257/04 , C07D271/06 , C07D275/06 , C07D401/10 , C07D413/10
摘要： α-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2)(CH2)nNRbC(O)Ra. (3)(CH2)nNRbSO2Rd. (4)(CH2)nNRbCO2Ra.(5)(CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6)(CH2)kCO2Ra. and (7)(CH2)C(O)NRbRc. R2b is OH or a group selected from R2a; or R2a and R2b together with the carbon atom to which they are attached form a 3- to 7-membered carbocyclic ring optionally substituted with 1 to 4 groups independently selected from halogen. ORa. C1-4 alkyl and C1-4 haloalkyl;
摘要翻译：通式（I）的α-羟基酰胺衍生物是可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状的缓激肽B1拮抗剂或反向激动剂。 R2a选自（1）选自Ra的基团。（2）（CH2）nNRbC（O）Ra。（3）（CH2）nNRbSO2Rd。（4）（CH2）nNRbCO2Ra（5）（CH2）k-杂环，任选被1至3个独立地选自卤素，硝基，氰基，硫代C 1-4烷基和C 1-3卤代烷基的基团取代，其中所述杂环是（a）具有选自NO和S的环杂原子并且任选具有至多3个另外的环氮原子的5元杂芳环，其中所述环任选地被苯并稠合; 或（b）含有1至3个环氮原子的6-元杂环和其N-氧化物。其中所述环任选地被苯并稠合。（6）（CH2）kCO2Ra。和（7）（CH 2）C（O）NR b R c。 R2b是OH或选自R2a的基团; 或R 2a和R 2b与它们所连接的碳原子一起形成任选被1至4个独立地选自卤素的基团取代的3至7元碳环。 ORa。 C 1-4烷基和C 1-4卤代烷基;

5. 发明授权

US07163951B2 N-biarylmethyl aminocycloalkanecarboxamide derivatives 失效
标题翻译： N-二芳基甲基氨基环烷甲酰胺衍生物
公开(公告)号：US07163951B2
公开(公告)日：2007-01-16
申请号：US10523911
申请日：2003-08-25
申请人： Scott D. Kuduk , Michael R. Wood , Mark G. Bock
发明人： Scott D. Kuduk , Michael R. Wood , Mark G. Bock
IPC分类号： A61K31/4427 , C07D401/12
CPC分类号： C07D417/12 , C07D213/40 , C07D213/61 , C07D239/28 , C07D239/42 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/10 , C07D413/12
摘要： N-Biarylmethylaminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.
摘要翻译： N-二芳基甲基氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。

6. 发明申请

US20110190334A1 Heterocyclic Sulfonamide Derivatives 失效
标题翻译：杂环磺酰胺衍生物
公开(公告)号：US20110190334A1
公开(公告)日：2011-08-04
申请号：US12938583
申请日：2010-11-03
申请人： Mark G. Bock , Dinesh Chikkanna , Clive McCarthy , Henrik Moebitz , Chetan Pandit
发明人： Mark G. Bock , Dinesh Chikkanna , Clive McCarthy , Henrik Moebitz , Chetan Pandit
IPC分类号： A61K31/437 , C07D471/04 , A61P35/00
CPC分类号： C07D471/04 , C07D498/04 , C07D513/04
摘要： The present invention relates to compounds of Formula I where R1a, R1b, X, R2a, R2b, W, R3, R4, and R5 are as defined herein as well as pharmaceutically acceptable salts thereof. The compounds have been shown to act as MEK inhibitors which may be useful in the treatment of hyperproliferative diseases, like cancer and inflammation.
摘要翻译：本发明涉及其中R1a，R1b，X，R2a，R2b，W，R3，R4和R5如本文所定义的式I化合物及其药学上可接受的盐。已经显示这些化合物作为MEK抑制剂，其可用于治疗过度增殖性疾病如癌症和炎症。

7. 发明授权

US5977115A Alpha 1a adrenergic receptor antagonists 失效
标题翻译： Alpha 1a肾上腺素能受体拮抗剂
公开(公告)号：US5977115A
公开(公告)日：1999-11-02
申请号：US973624
申请日：1997-12-04
申请人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello , Randall C. Newton
发明人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello , Randall C. Newton
IPC分类号： A61K31/445 , A61P13/02 , A61P15/00 , C07D211/64 , C07D295/155 , A61K31/495 , C07D295/12
CPC分类号： C07D295/155 , C07D211/64
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译： PCT No.PCT / US96 / 09425 Sec。 371 1997年12月4日第 102（e）1997年12月4日PCT PCT 1996年6月6日PCT公布。出版物WO96 / 40136 日期：1996年12月19日本发明涉及某些新型化合物及其衍生物，其合成及其作为选择性α-1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

8. 发明授权

US5834464A Imidazolinobenzodiazepines 失效
标题翻译：咪唑啉二苯并氮杂
公开(公告)号：US5834464A
公开(公告)日：1998-11-10
申请号：US640730
申请日：1996-05-06
申请人： Mark G. Bock , Robert M. DiPardo , Roger M. Freidinger
发明人： Mark G. Bock , Robert M. DiPardo , Roger M. Freidinger
IPC分类号： C07D487/04 , A61K31/395
CPC分类号： C07D487/04
摘要： Imidazolinobenzodiazepines are cholecystokinin B (CCK-B) antagonists useful as anxiolytic agents. The compounds have structures such as: ##STR1##
摘要翻译： PCT No.PCT / US94 / 13325 Sec。 371日期：1996年5月6日 102（e）日期1996年5月6日PCT 1994年11月18日PCT PCT。 WO95 / 14693 PCT出版物日期1995年6月1日咪唑啉二氮卓类是可用作抗焦虑剂的胆囊收缩素B（CCK-B）拮抗剂。化合物具有如下结构：

9. 发明授权

US5661163A Alpha-1a adrenergic receptor antagonists 失效
标题翻译： α-1a肾上腺素受体拮抗剂
公开(公告)号：US5661163A
公开(公告)日：1997-08-26
申请号：US488272
申请日：1995-06-07
申请人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello
发明人： Michael A. Patane , Mark G. Bock , Roger M. Freidinger , Rose Ann Ponticello
IPC分类号： A61K31/445 , A61P13/02 , A61P15/00 , C07D211/64 , C07D295/155 , C07D211/36
CPC分类号： C07D295/155 , C07D211/64
摘要： This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as selective alpha-1a adrenergic receptor antagonists. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing orthostatic hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia are achieved.
摘要翻译：本发明涉及某些新化合物及其衍生物，其合成及其作为选择性α-1a肾上腺素能受体拮抗剂的用途。这些化合物的一个应用是治疗良性前列腺增生。这些化合物在其能够松弛富含α1a受体亚型的平滑肌组织的能力方面具有选择性，而不会同时引起体位性低血压。发现一个这样的组织围绕尿道衬里。因此，本发明化合物的一个用途是通过允许较少的受阻尿流量来对患有良性前列腺增生的男性提供急性缓解。通过与人5-α还原酶抑制化合物的组合提供本发明化合物的另一种用途，使得可以实现急性和慢性缓解来自良性前列腺增生的作用。

10. 发明授权

US5206237A Benzodiazepine analogs 失效
标题翻译：苯并嗪类似物
公开(公告)号：US5206237A
公开(公告)日：1993-04-27
申请号：US699849
申请日：1991-05-14
申请人： Roger M. Freidinger , Mark G. Bock , Ben E. Evans
发明人： Roger M. Freidinger , Mark G. Bock , Ben E. Evans
IPC分类号： A61K31/55 , A61K31/551 , A61P25/04 , A61P25/20 , A61P25/30 , A61P27/02 , A61P35/00 , C07D243/14 , C07D401/12 , C07D403/04
CPC分类号： A61K31/55
摘要： Pharmaceutical compositions containing benzodiazepines of the formula: ##STR1## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.

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