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1. 发明授权

US5250548A Angiotensin II receptor antagonists 失效
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：US5250548A
公开(公告)日：1993-10-05
申请号：US844351
申请日：1992-03-02
申请人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
发明人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Andrew S. Tasker , Thomas W. von Geldern , Jeffrey A. Kester , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
IPC分类号： C07D239/42 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/14 , A61K31/44
CPC分类号： C07D239/42 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/14
摘要： Compounds are disclosed having the formula: ##STR1## The compounds of the invention are angiotensin II receptor antagonists.
摘要翻译：公开了具有下式的化合物：本发明的化合物是血管紧张素II受体拮抗剂。

2. 发明授权

US5326776A Angiotensin II receptor antagonists 失效
标题翻译：血管紧张素II受体拮抗剂
公开(公告)号：US5326776A
公开(公告)日：1994-07-05
申请号：US21839
申请日：1993-02-24
申请人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Kenneth P. Spina , Thomas W. von Geldern , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
发明人： Martin Winn , Biswanath De , Thomas M. Zydowsky , Daniel J. Kerkman , John F. DeBernardis , Saul H. Rosenberg , Kazumi Shiosaki , Fatima Z. Basha , Kenneth P. Spina , Thomas W. von Geldern , Steven Boyd , Diane M. Yamamoto , Anthony K. L. Fung
IPC分类号： C07D403/12 , C07D413/12 , C07D417/12 , A61K31/41 , A61K31/415 , C07D403/10
CPC分类号： C07D403/12 , C07D413/10 , C07D417/12
摘要： Compounds are disclosed having the formula: ##STR1## wherein the substituents are defined herein. The compounds of the invention are angiotensin II receptor antagonists.
摘要翻译：公开了具有下式的化合物：其中取代基在本文中定义。本发明的化合物是血管紧张素II受体拮抗剂。

3. 发明授权

US4963568A Dopamine agonists 失效
标题翻译：多巴胺激动剂
公开(公告)号：US4963568A
公开(公告)日：1990-10-16
申请号：US359448
申请日：1989-05-31
申请人： Robert W. Schoenleber , John W. Kebabian , Yvonne C. Martin , Michael P. DeNinno , Richard J. Perner , David M. Stout , Chi-Nung W. Hsiao , Stanley DiDomenico, Jr. , John F. DeBernardis , Fatima Z. Basha , Michael D. Meyer , Biswanath De
发明人： Robert W. Schoenleber , John W. Kebabian , Yvonne C. Martin , Michael P. DeNinno , Richard J. Perner , David M. Stout , Chi-Nung W. Hsiao , Stanley DiDomenico, Jr. , John F. DeBernardis , Fatima Z. Basha , Michael D. Meyer , Biswanath De
IPC分类号： A61K31/13 , A61K31/135 , A61K31/16 , A61K31/335 , A61K31/40 , A61K31/403 , A61K31/404 , A61K38/00 , A61P9/00 , A61P25/00 , A61P25/18 , A61P25/30 , C07C41/02 , C07C215/48 , C07C215/64 , C07C217/56 , C07C217/74 , C07C219/28 , C07C233/18 , C07C237/08 , C07C271/16 , C07C271/44 , C07C309/65 , C07C323/60 , C07D207/08 , C07D209/08 , C07D209/62 , C07D221/06 , C07D221/10 , C07D221/20 , C07D311/76 , C07D311/78 , C07D311/96 , C07D313/08 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/04 , C07D407/12 , C07D493/10 , C07K5/06
CPC分类号： C07D207/08 , C07C215/64 , C07C217/74 , C07C219/28 , C07C233/18 , C07C237/08 , C07C271/16 , C07C271/44 , C07C309/65 , C07C323/60 , C07D209/62 , C07D221/10 , C07D221/20 , C07D311/76 , C07D311/78 , C07D311/96 , C07D313/08 , C07D405/04 , C07D405/06 , C07D405/12 , C07D407/04 , C07D407/12 , C07D493/10 , C07K5/06026 , A61K38/00 , C07C2101/14 , C07C2102/10 , C07C2102/28 , C07C2103/28 , C07C2103/74 , C07C2103/93
摘要： Novel compounds which are selective dopamine agonists are useful for treating disorders characterized by abnormal dopamine levels, such as Parkinson's Disease, as well as cardiovascular disorders.
摘要翻译：作为选择性多巴胺激动剂的新型化合物可用于治疗以异常多巴胺水平为特征的疾病，例如帕金森病，以及心血管疾病。

4. 发明授权

US5268374A Non-peptide renin inhibitors 失效
标题翻译：非肽肾素抑制剂
公开(公告)号：US5268374A
公开(公告)日：1993-12-07
申请号：US700185
申请日：1991-05-22
申请人： Anthony K. L. Fung , William R. Baker , Yoek-Lin Armiger , Saul H. Rosenberg , Biswanath De , Jacob J. Plattner , Steven A. Boyd , Dale J. Kempf , Hing L. Sham , Hollis D. Kleinert , Robert A. Mantei
发明人： Anthony K. L. Fung , William R. Baker , Yoek-Lin Armiger , Saul H. Rosenberg , Biswanath De , Jacob J. Plattner , Steven A. Boyd , Dale J. Kempf , Hing L. Sham , Hollis D. Kleinert , Robert A. Mantei
IPC分类号： C07C237/08 , C07C317/28 , C07C323/58 , C07D203/18 , C07D211/44 , C07D211/62 , C07D211/96 , C07D233/54 , C07D295/185 , C07D401/12 , C07D407/12 , C07D413/12 , A61K37/43 , C07K5/08
CPC分类号： C07D233/64 , C07C237/08 , C07C317/28 , C07C323/58 , C07D203/18 , C07D211/44 , C07D211/62 , C07D211/96 , C07D295/185 , C07D401/12 , C07D407/12 , C07D413/10 , C07C2101/14
摘要： The present invention relates to renin inhibiting compounds of the formula: ##STR1##
摘要翻译：本发明涉及下式的肾素抑制化合物：

5. 发明授权

US5164388A Heterocyclic peptide renin inhibitors 失效
标题翻译：杂环肽肾素抑制剂
公开(公告)号：US5164388A
公开(公告)日：1992-11-17
申请号：US678266
申请日：1991-04-18
申请人： Biswanath De , Thomas N. Zydowsky , William R. Baker , Joseph F. Dellaria , Saul H. Rosenberg , Hwan S. Jae
发明人： Biswanath De , Thomas N. Zydowsky , William R. Baker , Joseph F. Dellaria , Saul H. Rosenberg , Hwan S. Jae
IPC分类号： A61K38/00 , C07D211/14 , C07D211/76 , C07D213/74 , C07D233/54 , C07D239/42 , C07D241/04 , C07D241/08 , C07D243/08 , C07D263/10 , C07D263/22 , C07D295/15 , C07D403/06 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/06 , C07K5/078
CPC分类号： C07D233/64 , C07D211/14 , C07D211/76 , C07D213/74 , C07D239/42 , C07D241/04 , C07D241/08 , C07D243/08 , C07D263/10 , C07D263/22 , C07D295/15 , C07D403/06 , C07D413/04 , C07D413/06 , C07D413/14 , C07D417/06 , C07K5/06139 , A61K38/00 , C07C2101/14
摘要： A renin inhibiting compound of the formula ##STR1## wherein X is N, O or CH; R.sub.1 is absent or a functional group; A and L are independently selected from absent, C.dbd.O, SO.sub.2 and CH.sub.2 ; D is C.dbd.O, SO.sub.2 or CH.sub.2 ; Y is N or CH; R.sub.2 is hydrogen, loweralkyl or substituted alkyl; Z is a functional group; R.sub.3 is loweralkyl or substituted alkyl; n is 0 or 1; and T is a mimic of the Leu-Val cleavage site of angiotensinogen; or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译：其中X是N，O或CH的式（Ⅰ）的肾素抑制化合物; R1不存在或官能团; A和L独立地选自C = O，SO 2和CH 2; D是C = O，SO 2或CH 2; Y为N或CH; R2是氢，低级烷基或取代的烷基; Z是功能组; R3是低级烷基或取代的烷基; n为0或1; T是模拟血管紧张素原的Leu-Val切割位点; 或其药学上可接受的盐，酯或前药。

6. 发明授权

US4994477A Heterocyclic renin inhibitors 失效
标题翻译：杂环肾素抑制剂
公开(公告)号：US4994477A
公开(公告)日：1991-02-19
申请号：US173382
申请日：1988-03-24
申请人： Dale J. Kempf , Saul H. Rosenberg , Jacob J. Plattner , Hing L. Shan , Biswanath De
发明人： Dale J. Kempf , Saul H. Rosenberg , Jacob J. Plattner , Hing L. Shan , Biswanath De
IPC分类号： A61K38/00 , C07D233/54 , C07D405/12 , C07D417/12 , C07K5/02 , C07K5/078
CPC分类号： C07D233/64 , C07D405/12 , C07D417/12 , C07K5/0207 , C07K5/06139 , A61K38/00
摘要： A renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; R.sub.1 is loweralkyl, loweralkenyl, alkoxyalkyl, [(alkoxy)alkoxy]alkyl, alkoxycarbonylalkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; R.sub.2 is hydrogen, loweralkyl, cycloalkylmethyl or benzyl; D is a substituent; or pharmaceutically acceptable salts or esters thereof.Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
摘要翻译：下式的肾素抑制化合物：其中A是取代基; R1是低级烷基，低级烯基，烷氧基烷基，[（烷氧基）烷氧基]烷基，烷氧基羰基烷基，羧基烷基，（硫代烷氧基）烷基，苄基或杂环取代的甲基; R2是氢，低级烷基，环烷基甲基或苄基; D是取代基; 或其药学上可接受的盐或酯。还公开了肾素抑制组合物，治疗高血压的方法，制备肾素抑制化合物的方法和可用于制备肾素抑制化合物的中间体。

7. 发明授权

US5120718A Candida acid protease inhibiting compounds 失效
标题翻译：假丝酵母酸蛋白酶抑制化合物
公开(公告)号：US5120718A
公开(公告)日：1992-06-09
申请号：US714820
申请日：1991-06-13
申请人： Robert C. Goldman , William R. Baker , Hwan-Soo Jae , Biswanath De , Thomas M. Zydowsky , Edwin de Lara
发明人： Robert C. Goldman , William R. Baker , Hwan-Soo Jae , Biswanath De , Thomas M. Zydowsky , Edwin de Lara
IPC分类号： C07D207/26 , C07D207/273 , C07D295/215 , C07D295/26 , C07D401/06 , C07D417/06
CPC分类号： C07D207/273 , C07D295/215 , C07D295/26 , C07D401/06 , C07D417/06
摘要： Compounds which inhibit Candida acid protease are disclosed which have the formula: ##STR1## wherein R.sub.1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, arylalkyl or (heterocyclic)alkyl;R.sub.2 is loweralkyl, cycloalkylalkyl or arylalkyl;R.sub.3 is --OH or --NH.sub.2 ;R.sub.4 is(a) --CH(OH)--R.sub.5 wherein R.sub.5 is loweralkyl, cycloalkyl or cycloalkylalkyl or(b) --CH.sub.2 CH(R.sub.6)C(O)NHR.sub.7 wherein R.sub.6 is loweralkyl and R.sub.7 is loweralkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl or (heterocyclic)alkyl; andA is ##STR2## wherein R.sub.8 is arylalkyl, B is --C(O) or --S(O).sub.2 -- and R.sub.9 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or ##STR3## wherein R.sub.10 is arylalkyl and R.sub.11 is (a) --C(O)R.sub.12 wherein R.sub.12 is alkoxy, arylalkoxy, aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl or (b) --S(O).sub.2 --R.sub.13 wherein R.sub.13 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译：公开了抑制假丝酵母酸蛋白酶的化合物，其具有下式：其中R 1是低级烷基，低级烯基，环烷基，环烯基，环烷基烷基，环烯基烷基，芳基烷基或（杂环）烷基; R2是低级烷基，环烷基烷基或芳基烷基; R3是-OH或-NH2; R4是（a）-CH（OH）-R5，其中R5是低级烷基，环烷基或环烷基烷基或（b）-CH2CH（R6）C（O）NHR7，其中R6是低级烷基，R7是低级烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，，烷氧基烷基，硫代烷氧基烷基，羧基烷基，烷氧基羰基烷基，氰基烷基或（杂环）烷基; （A）其中R8是芳基烷基，B是-C（O）或-S（O）2-，R9是芳基，芳烷基，杂环或（杂环）烷基; （b）其中R 10是芳烷基，R 11是（a）-C（O）R 12，其中R 12是烷氧基，芳基烷氧基，芳基，芳烷基，杂环或（杂环）烷基或（b）-S（O）2 -R13其中R13是芳基，芳烷基，杂环或（杂环）烷基; 或其药学上可接受的盐，酯或前药。

8. 发明授权

US5210206A 1,3-oxazolyl substituted biphenyl 失效
标题翻译： 1,3-恶唑基取代的联苯
公开(公告)号：US5210206A
公开(公告)日：1993-05-11
申请号：US819537
申请日：1992-01-10
申请人： Howard E. Morton , Biswanath De , Daniel J. Kerkman
发明人： Howard E. Morton , Biswanath De , Daniel J. Kerkman
IPC分类号： C07D239/42 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/14
CPC分类号： C07D239/42 , C07D257/04 , C07D401/12 , C07D403/12 , C07D405/14 , Y02P20/55
摘要： The present invention relates to a process for the preparation of a compound of the formula: ##STR1## wherein R.sub.1 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, lower alkenyl, lower alkynyl, cycloalkyl and cycloalkylalkyl; R.sub.2 is selected from the group consisting of hydrogen, loweralkyl, loweralkoxy-substituted loweralkyl, halogen and loweralkoxy; R.sub.3 is selected from hydrogen, loweralkyl, and halogen; R* and R** are independently selected from loweralkyl and P.sub.1 is hydrogen or an nitrogen-protecting group; or an acid addition salt thereof.
摘要翻译：本发明涉及一种制备下式化合物的方法：其中R 1选自氢，低级烷基，低级烷氧基取代的低级烷基，低级烯基，低级炔基，环烷基和环烷基烷基; R2选自氢，低级烷基，低级烷氧基取代的低级烷基，卤素和低级烷氧基; R3选自氢，低级烷基和卤素; R *和R **独立地选自低级烷基，P1是氢或氮保护基; 或其酸加成盐。

9. 发明授权

US07041696B2 Interleukin-1β converting enzyme inhibitors 失效
标题翻译：白细胞介素-1β转换酶抑制剂
公开(公告)号：US07041696B2
公开(公告)日：2006-05-09
申请号：US10457181
申请日：2003-06-09
申请人： John August Wos , David Lindsey Soper , Steven Victor O'Neil , Yili Wang , Kofi Abeka Oppong , Michael Christopher Laufersweiler , Jian Chen , Biswanath De , Thomas Prosser Demuth, Jr.
发明人： John August Wos , David Lindsey Soper , Steven Victor O'Neil , Yili Wang , Kofi Abeka Oppong , Michael Christopher Laufersweiler , Jian Chen , Biswanath De , Thomas Prosser Demuth, Jr.
IPC分类号： C07D487/04 , A61K31/403 , A61P29/00
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention relates to interleukin-1β converting enzyme inhibitors having the formula: R is a carbocyclic or heterocyclic ring; R1 is a cysteine trap; R2a, R2a′, R2b, and R2b′ are each independently hydrogen, C1–C4 alkyl, C1–C4 alkoxy, and mixtures thereof; or R2a′ and R2b′ can taken together to form a double bond; L and L1 are linking groups having the formula: T is selected from the group consisting of: i) —NR6—; ii) —O—; iii) —NR6S(O)2—; iv) —S(O)2NR6—; and v) mixtures thereof; R6 is hydrogen, substituted or unsubstituted C1–C20 linear, branched, or cyclic alkyl, C6–C20 aryl, C7–C20 alkylenearyl, and mixtures thereof; the indices w, w1, and w2 are each independently 0 or 1; i) hydrogen; ii) C1–C4 linear, branched, and cyclic alkyl; iii) R3a and R3b or R4a, and R4b can be taken together to form a carbonyl unit; iv) two R3a or two R3b units from adjacent carbon atoms or two R4a or two R4b units from adjacent carbon atoms can be taken together to form a double bond; and v) mixtures thereof; the index m is from 0 to 5; the index n is from 0 to 5.
摘要翻译：本发明涉及具有下式的白细胞介素-1β转换酶抑制剂：R是碳环或杂环; R 1是半胱氨酸阱; R 2a，R 2a，R 2b和R 2b'各自独立地为氢，C

10. 发明授权

US06787555B2 Triazole compounds useful in treating diseases associated with unwanted cytokine activity 失效
公开(公告)号：US06787555B2
公开(公告)日：2004-09-07
申请号：US10132981
申请日：2002-04-24
申请人： Joshua Spector Tullis , John Charles Van Rens , Michael Philip Clark , Benjamin Eric Blass , Michael George Natchus , Biswanath De
发明人： Joshua Spector Tullis , John Charles Van Rens , Michael Philip Clark , Benjamin Eric Blass , Michael George Natchus , Biswanath De
IPC分类号： A61K31506
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/04
摘要： The present invention relates to 4-aryl triazoles having the formula: wherein R1 is independently selected from the group consisting of: lower alkyl, lower alkenyl, lower alkynyl, lower heteroalkyl, lower heteroalkenyl, lower heteroalkynyl, heterocycloalkyl, heteroaryl, halo, CN, OR4, SR4, S(O)R4, S(O)2R4, and NR4R5; and Q is has the general formula: said compounds are useful in treating diseases associated with unwanted cytokine activity, inter alia, interleukin-1 (IL-1) and tumor necrosis factor (TNF) from cells.

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