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31. 发明授权

US06228985B1 Derivatives of aminobenzoic and aminobiphenylcarboxylic acids useful as anti-cancer agents 失效
标题翻译：用作抗癌剂的氨基苯甲酸和氨基联苯羧酸的衍生物
公开(公告)号：US06228985B1
公开(公告)日：2001-05-08
申请号：US09082787
申请日：1998-05-21
申请人： Christine H. Blood , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Christine H. Blood , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： C07K200
CPC分类号： C07C229/38 , A61K38/00 , C07C237/36 , C07D209/18 , C07D209/20
摘要： The present invention provides compounds having the formula: wherein n is 0 or 1; R is —NH2 or wherein R1 and R2 are independently selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, carboxy, carboxyalkyl, and carbamoyl; Q is R3C(O)— or wherein R5 is selected from the group consisting of H, alkyl, aralkyl, heteroaralkyl, and carbamoylalkyl, and R3 and R4 are selected from the group consisting of H, alkyl, alkoxy, arylalkoxy, aralkyl, heteroaralkyl, and carbamoylalkyl; the Q—NH—(CH2)n— and the —C(O)R substituents of the compound of formula I are independently positioned ortho, meta, orpara relative to the carbon atoms that form the bond between the two phenyl groups to which said substituents are bound, with the proviso that said substituents are not both positioned ortho; and the Q—NH—(CH2)n and the —C(O)R substituents of the compound of formula II are positioned meta orpara to each other; or a biolabile ester thereof, or a pharmaceutically acceptable salt thereof. The compounds are useful for treating uPA- or uPAR-mediated disorders, e.g., tumor metastasis, tumor angiogenesis, restenosis, chronic inflammation, or corneal angiogenesis.
摘要翻译：本发明提供具有下式的化合物：其中n为0或1; R为-NH 2，其中R1和R2独立地选自H，烷基，芳烷基，杂芳烷基，羧基，羧基烷基和氨基甲酰基; Q为R3C （O） - 或其中R 5选自H，烷基，芳烷基，杂芳烷基和氨基甲酰基烷基，R 3和R 4选自H，烷基，烷氧基，芳基烷氧基，芳烷基，杂芳烷基和氨基甲酰基烷基; 式I化合物的Q-NH-（CH 2）n - 和-C（O）R取代基相对于形成所述取代基的两个苯基之间的键的碳原子独立地位于邻位，间位或对位条件是所述取代基不都位于邻位; 和式II化合物的Q-NH-（CH 2）n和-C（O）R取代基彼此定位在间或其生物不稳定酯或其药学上可接受的盐中。该化合物可用于治疗uPA或uPAR介导的病症，例如肿瘤转移，肿瘤血管发生，再狭窄，慢性炎症或角膜血管生成。

32. 发明授权

US4840772A Antiglaucoma compositions and methods 失效
标题翻译：抗青光眼组合物和方法
公开(公告)号：US4840772A
公开(公告)日：1989-06-20
申请号：US227954
申请日：1988-08-03
申请人： Robert Watkins , Ronald J. Doll , Bernard R. Neustadt , Elizabeth M. Smith , Charles V. Magatti , Elijah H. Gold
发明人： Robert Watkins , Ronald J. Doll , Bernard R. Neustadt , Elizabeth M. Smith , Charles V. Magatti , Elijah H. Gold
IPC分类号： A61K38/00 , C07K5/02
CPC分类号： C07K5/0222 , C07K5/022 , A61K38/00 , Y10S435/81 , Y10S436/808
摘要： The present invention relates to ophthalmological pharmaceutical compositions comprising (benzothiadiazine, benzamide and benzenesulfonyl)phenyl-substituted carboxyalkyl dipeptide compounds and to methods for using said composition in reducing intraocular pressure, e.g., in the treatment of glaucoma.
摘要翻译：本发明涉及包含（苯并噻二嗪，苯甲酰胺和苯磺酰基）苯基取代的羧烷基二肽化合物的眼科药物组合物以及使用所述组合物降低眼内压的方法，例如用于治疗青光眼。

33. 发明授权

US4511569A Tricyclic lactams and derivatives useful in increasing cardiac contractility 失效
标题翻译：可用于增加心脏收缩力的三环内酰胺和衍生物
公开(公告)号：US4511569A
公开(公告)日：1985-04-16
申请号：US411764
申请日：1982-08-26
申请人： Elizabeth M. Smith , Ronald J. Doll , Bernard R. Neustadt
发明人： Elizabeth M. Smith , Ronald J. Doll , Bernard R. Neustadt
IPC分类号： C07D221/06 , A61K31/47 , A61K31/473 , A61P9/04 , C07D221/10 , C07D221/16 , C07D471/04 , C07D491/04 , C07D491/052 , C07D491/14 , C07D495/04 , C07D495/14 , A61K31/44 , C07D215/22
CPC分类号： C07D471/04 , C07D221/10 , C07D221/16 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要： Disclosed are 5,6-dihydro benzo[f]quinolines and derivatives which are effective in increasing cardiac contractility. These compounds are useful in the treatment of congestive heart failure.
摘要翻译：公开了有效增加心脏收缩力的5,6-二氢苯并[f]喹啉和衍生物。这些化合物可用于治疗充血性心力衰竭。

34. 发明授权

US4474786A Tricyclic lactams and derivatives useful in increasing cardiac contractility 失效
标题翻译：可用于增加心脏收缩力的三环内酰胺和衍生物
公开(公告)号：US4474786A
公开(公告)日：1984-10-02
申请号：US505050
申请日：1983-06-16
申请人： Elizabeth M. Smith , Ronald J. Doll , Bernard R. Neustadt
发明人： Elizabeth M. Smith , Ronald J. Doll , Bernard R. Neustadt
IPC分类号： C07D221/10 , C07D221/16 , C07D471/04 , C07D491/04 , C07D491/052 , C07D491/14 , C07D495/04 , C07D495/14 , A61K31/435 , C07D491/044 , C07D513/04
CPC分类号： C07D471/04 , C07D221/10 , C07D221/16 , C07D491/04 , C07D491/14 , C07D495/04 , C07D495/14
摘要： Disclosed are tricyclic lactams and derivatives which are effective in increasing cardiac contractility in humans. These compounds are useful in the treatment of congestive heart failure.
摘要翻译：公开了三环内酰胺和衍生物，其有效地增加人的心脏收缩力。这些化合物可用于治疗充血性心力衰竭。

35. 发明授权

US4470972A 7-Carboxyalkylaminoacyl-1,4-dithia-7-azaspiro[4.4]-nonane-8-carboxylic acids 失效
标题翻译： 7-羧基烷基氨基酰基-1,4-二硫杂-7-氮杂螺[4.4] - 壬烷-8-羧酸
公开(公告)号：US4470972A
公开(公告)日：1984-09-11
申请号：US446929
申请日：1982-12-06
申请人： Elijah H. Gold , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Elijah H. Gold , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： A61K38/00 , C07K5/02 , A61K37/00 , A61K31/40
CPC分类号： C07K5/0222 , A61K38/00
摘要： This invention relates to 7-carboxyalkyl-aminoacyl-1,4-adithia-7-azaspiro[4.4]nonane-8-carboxylic acids. The compounds of the invention are useful in the treatment of cardiovascular disorders and especially as antihypertensive agents.
摘要翻译：本发明涉及7-羧基烷基 - 氨基酰基-1,4-二硫杂-7-氮杂螺[4.4]壬烷-8-羧酸。本发明的化合物可用于治疗心血管疾病，特别是作为抗高血压药物。

36. 发明授权

US07638526B2 Azetidine derivatives useful in treating pain, diabetes and disorders of lipid metabolism 失效
标题翻译：可用于治疗疼痛，糖尿病和脂质代谢紊乱的氮杂环丁烷衍生物
公开(公告)号：US07638526B2
公开(公告)日：2009-12-29
申请号：US11854600
申请日：2007-09-13
申请人： Brian A. McKittrick , Elizabeth M. Smith , Chad E. Bennett , Joel M. Harris , Eugenia Y. Kiselgof , Chad E. Knutson , Peter Korakas , Deen Tulshian , Hyunjin Kim
发明人： Brian A. McKittrick , Elizabeth M. Smith , Chad E. Bennett , Joel M. Harris , Eugenia Y. Kiselgof , Chad E. Knutson , Peter Korakas , Deen Tulshian , Hyunjin Kim
IPC分类号： A61K31/438 , C07D471/10
CPC分类号： C07D471/08
摘要： Disclosed are compounds of the formula: and compounds of the formula: wherein R1, R2, R3, R4, R5, u and v are as defined herein. Also disclosed are methods of treating pain (e.g., inflammatory pain, chronic pain, and neuropathic pain), methods of treating diabetes, and methods of inhibiting the absorption of cholesterol using compounds of formula I or IIA.
摘要翻译：公开了下式的化合物和下式的化合物：其中R 1，R 2，R 3，R 4，R 5，u和v如本文所定义。还公开了治疗疼痛（例如炎性疼痛，慢性疼痛和神经性疼痛）的方法，治疗糖尿病的方法，以及使用式I或IIA化合物抑制胆固醇吸收的方法。

37. 发明授权

US5389610A Carboxyalkylcarbonyl aminoacid endopeptidase inhibitors 失效
标题翻译：羧基烷基羰基氨基酸内肽酶抑制剂
公开(公告)号：US5389610A
公开(公告)日：1995-02-14
申请号：US849036
申请日：1992-04-21
申请人： Bernard R. Neustadt , Elizabeth M. Smith , Martin F. Haslanger
发明人： Bernard R. Neustadt , Elizabeth M. Smith , Martin F. Haslanger
IPC分类号： A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/22 , A61K38/55 , A61P3/00 , A61P9/00 , A61P9/12 , C07C233/47 , C07C233/63 , C07C235/40 , C07C237/12 , C07C237/24 , C07C319/20 , C07C323/59 , C07C323/60 , C07C323/64 , C07D207/325 , C07D209/14 , C07D209/18 , C07D217/26 , C07D307/68 , C07D307/79 , C07D333/38 , C07K5/08 , A61K39/02
CPC分类号： C07C323/59 , C07C233/63 , C07C235/40 , C07C2101/08
摘要： Carboxyalkylcarbonyl aminoacid inhibitors of endopeptidases of the formula: ##STR1## or pharmaceutically acceptable salt thereof, wherein R.sup.1 is H, alkyl, arylalkyl, aryl or aryloxyalkyl; R.sup.2 is alkyl, alkenyl, alkynyl, alkoxy or alkylthio, wherein the alkyl portion is substituted with 0-3 substituents independently selected from the group consisting of hydroxy, alkoxy, alkoxyalkoxy, alkylthio, aryl, alkoxyalkylthio, arylalkoxy and arylalkylthio; R.sup.3 and R.sup.4 are independently alkyl or arylalkyl; or R.sup.3 and R.sup.4 together with the carbon to which they are attached form an optionally substituted 5-, 6- or 7-membered ring wherein said ring comprises 0 to 1 heteroatoms selected from the group consisting of sulfur and oxygen; R.sup.5 is H, alkyl, alkoxyalkyl, alkylthioalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, arylalkoxyalkyl or arylalkylthioalkyl; R.sup.6 is H, hydroxy, alkoxy, alkyl, arylalkoxy, alkoxyalkyl, alkylthioalkyl, arylalkoxyalkyl, arylalkylthioalkyl, aryl or heteroaryl; R.sup.7 is hydroxy, alkoxy, aryloxy, arylalkoxy, amino, alkylamino or dialkylamino; m is 0 or 1; and n is 0, 1, 2 or 3, use of the compounds, alone or in combination with an ACE inhibitor or an ANF, in the treatment of cardiovascular disorders such as hypertension, congestive heart failure, edema and renal insufficiency, use of the compounds in the treatment of nephrotoxicity and pain conditions, and pharmaceutical compositions containing said compounds are disclosed.
摘要翻译： PCT No.PCT / US90 / 06655 Sec。一九九二年四月二十一日 102（e）日期1992年4月21日PCT 1990年11月20日PCT PCT。出版物WO91 / 07386 1991年5月30日。具有下式的内肽酶的羧基烷基羰基氨基酸抑制剂或其药学上可接受的盐，其中R 1是H，烷基，芳基烷基，芳基或芳氧基烷基; R2是烷基，烯基，炔基，烷氧基或烷硫基，其中烷基部分被独立选自羟基，烷氧基，烷氧基烷氧基，烷硫基，芳基，烷氧基烷硫基，芳基烷氧基和芳基烷硫基的0-3个取代基取代。 R3和R4独立地是烷基或芳基烷基; 或R 3和R 4与它们所连接的碳一起形成任选取代的5-，6-或7-元环，其中所述环包含0至1个选自硫和氧的杂原子; R 5是H，烷基，烷氧基烷基，烷硫基烷基，芳基，芳基烷基，杂芳基，杂芳基烷基，芳基烷氧基烷基或芳基烷硫基烷基; R6是H，羟基，烷氧基，烷基，芳基烷氧基，烷氧基烷基，烷基硫代烷基，芳基烷氧基烷基，芳基烷硫基烷基，芳基或杂芳基; R7是羟基，烷氧基，芳氧基，芳基烷氧基，氨基，烷基氨基或二烷基氨基; m为0或1; 和n为0,1,2或3，单独使用或与ACE抑制剂或ANF组合使用化合物治疗心血管疾病如高血压，充血性心力衰竭，水肿和肾功能不全的用途公开了治疗肾毒性和疼痛病症的化合物和含有所述化合物的药物组合物。

38. 发明授权

US5219886A Mercapto-acylamino acids 失效
标题翻译：巯基 - 酰氨基酸
公开(公告)号：US5219886A
公开(公告)日：1993-06-15
申请号：US768647
申请日：1991-10-01
申请人： Elizabeth M. Smith , Philip M. DeCapite , Bernard R. Neustadt
发明人： Elizabeth M. Smith , Philip M. DeCapite , Bernard R. Neustadt
IPC分类号： A61K38/22 , A61K31/16 , A61K31/195 , A61K31/215 , A61K31/265 , A61K31/38 , A61K31/40 , A61K31/47 , A61K31/55 , A61K31/675 , A61K38/55 , A61K45/06 , A61P3/00 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , A61P43/00 , C07C319/12 , C07C323/00 , C07C323/56 , C07C323/60 , C07C327/06 , C07C327/32
CPC分类号： C07C327/32 , A61K38/2242 , A61K38/556 , C07C323/60
摘要： Novel mercapto-acylamino acids of the formula ##STR1## wherein Q is hydrogen or R.sup.7 CO--;R.sup.1 is lower alkyl, cyclolower alkyl, aryl or heteroaryl;R.sup.2 is hydrogen; lower alkyl; cyclolower alkyl; lower alkyl substituted with hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl; aryl; or heteroaryl;R.sup.3 is --OR.sup.5 or --NR.sup.5 R.sup.6 ;R.sup.4 and R.sup.9 are independently --(CH.sub.2).sub.q R.sup.8, provided that when R.sup.4 and R.sup.9 are both hydrogen, R.sup.2 is biphenylyl, phenoxyphenyl, phenylthiophenyl, naphthyl, heteroaryl, or lower alkyl substituted with hydroxy, lower alkoxy, mercapto or lower alkylthio;R.sup.5 and R.sup.6 are independently selected from the group consisting of hydrogen, lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl and aryl lower alkyl, or R.sup.5 and R.sup.6 together with the nitrogen to which they are attached form a 5-7 membered ring;R.sup.7 is hydrogen, lower alkyl or aryl;R.sup.8 is hydrogen, hydroxy, lower alkoxy, mercapto, lower alkylthio, aryl or heteroaryl;n is 1 or 2;p is 0 or 1;q is 0, 1 or 2; andt is 0 or 1; and the pharmaceutically acceptable salts thereof useful in the treatment of cardiovascular disorders and pain conditions and combinations of mercapto-acrylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating cardiovascular disorders are disclosed.
摘要翻译： PCT No.PCT / US90 / 01787 Sec。 371日期1991年10月1日 102（e）1991年10月1日授权PCT 1990年4月6日提交。式IMA的新型巯基酰基氨基酸其中Q为氢或R7CO-; R 1是低级烷基，环己烷基，芳基或杂芳基; R2是氢; 低级烷基环状烷基; 被羟基，低级烷氧基，巯基，低级烷硫基，芳基或杂芳基取代的低级烷基; 芳基; 或杂芳基; R3为-OR5或-NR5R6; R 4和R 9独立地为 - （CH 2）q R 8，条件是当R 4和R 9均为氢时，R 2为联苯基，苯氧基苯基，苯硫基苯基，萘基，杂芳基或被羟基，低级烷氧基，巯基或低级烷硫基取代的低级烷基; R 5和R 6独立地选自氢，低级烷基，羟基低级烷基，低级烷氧基低级烷基和芳基低级烷基，或者R 5和R 6与它们所连接的氮一起形成5-7元环; R7是氢，低级烷基或芳基; R8是氢，羟基，低级烷氧基，巯基，低级烷硫基，芳基或杂芳基; n为1或2; p为0或1; q是0,1或2; t为0或1; 和其可用于治疗心血管疾病和疼痛病症的药学上可接受的盐，以及用于治疗心血管疾病的巯基丙烯酰胺酸和心房利钠因子或血管紧张素转换酶抑制剂的组合。

39. 发明授权

US5061710A Mercapto-acylamino acid antihypertensives 失效
标题翻译：丙烯酰胺酰胺酸抗坏血酸
公开(公告)号：US5061710A
公开(公告)日：1991-10-29
申请号：US133669
申请日：1987-12-16
申请人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
发明人： Martin F. Haslanger , Bernard R. Neustadt , Elizabeth M. Smith
IPC分类号： A61K31/16 , A61K31/165 , A61K31/195 , A61K31/215 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/395 , A61K31/40 , A61K31/401 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/55 , A61K38/00 , A61K38/22 , A61K38/55 , A61K45/06 , A61P9/12 , A61P43/00 , C07C67/00 , C07C313/00 , C07C323/22 , C07C323/25 , C07C323/41 , C07C323/42 , C07C323/56 , C07C323/58 , C07C323/59 , C07C323/60 , C07C325/00 , C07C327/22 , C07C327/32 , C07C329/06 , C07C333/16 , C07D209/14 , C07D209/20 , C07D211/60 , C07D213/83 , C07D233/64 , C07D295/18 , C07D307/54 , C07D307/68 , C07D307/81 , C07D333/24 , C07D333/60 , C07D401/04 , C07D403/12 , C07D405/04 , C07D409/04 , C07D487/04 , C07K5/06 , C07K5/062 , C07K5/065 , C07K14/575 , C07K14/81
CPC分类号： C07K14/8146 , A61K45/06 , C07K5/06026 , C07K5/06078 , A61K38/00
摘要： Novel mercapto-acylamino acids useful in the treatment of hypertension and combinations of mercapto-acylamino acids and atrial natriuretic factors or angiotensin converting enzyme inhibitors useful for treating hypertension are disclosed.
摘要翻译：公开了可用于治疗高血压的新型巯基酰基氨基酸和用于治疗高血压的巯基酰基氨基酸和心房利钠因子或血管紧张素转换酶抑制剂的组合。

40. 发明授权

US4431644A Antihypertensive agents 失效
标题翻译：抗高血压药
公开(公告)号：US4431644A
公开(公告)日：1984-02-14
申请号：US355638
申请日：1982-03-08
申请人： Elizabeth M. Smith , Joseph T. Witkowski , Ronald J. Doll
发明人： Elizabeth M. Smith , Joseph T. Witkowski , Ronald J. Doll
IPC分类号： C07D209/44 , A61K38/00 , A61K38/55 , A61P9/12 , C07D207/444 , C07D209/46 , C07D209/48 , C07D215/48 , C07D217/26 , C07K1/113 , C07K5/02 , C07K5/06 , C07K14/81 , C07D285/24 , A61K31/40 , A61K31/54 , C07D417/12
CPC分类号： C07K5/0222 , A61K38/00 , Y10S514/869
摘要： Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2 and R.sup.4 are independently selected from hydrogen and lower alkyl; R.sup.3 is hydrogen, lower alkyl or amino lower alkyl; A and B taken together with the carbons to which they are attached form an alkylene ring having six carbon atoms or A and B are hydrogen; and Z is ##STR2## are disclosed. The compounds are useful as anti-hypertensive agents.
摘要翻译：式“IMAGE”的化合物及其药学上可接受的盐，其中R 1，R 2和R 4独立地选自氢和低级烷基; R3是氢，低级烷基或氨基低级烷基; A和B与它们所连接的碳一起形成具有6个碳原子的亚烷基环或A和B是氢; 而Z是 + TR 。该化合物可用作抗高血压药。

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