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1. 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。

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

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。

4. 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

5. 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.

6. 发明授权

US06727364B2 Triazole compounds useful in treating diseases associated with unwanted cytokine activity 失效
标题翻译：可用于治疗与不想要的细胞因子活性相关的疾病的三唑化合物
公开(公告)号：US06727364B2
公开(公告)日：2004-04-27
申请号：US10133044
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： C07D40104
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14
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.
摘要翻译：本发明涉及具有下式的4-芳基三唑：其中R 1独立地选自：低级烷基，低级烯基，低级炔基，低级杂烷基，低级杂烯基，低级杂炔基，杂环烷基，杂芳基，卤素，CN，OR 4，SR 4，S（O）R 4，S（O）2 R 4和NR 4 R 5; 并且Q具有以下通式：所述化合物可用于治疗与不想要的细胞因子活性相关的疾病，尤其是来自细胞的白细胞介素-1（IL-1）和肿瘤坏死因子（TNF）。

7. 发明授权

US06677337B2 1,2-dihydropyrazol-3-ones which controls inflammatory cytokines 失效
标题翻译：控制炎性细胞因子的1,2-二氢吡唑-3-酮
公开(公告)号：US06677337B2
公开(公告)日：2004-01-13
申请号：US10382060
申请日：2003-03-05
申请人： Matthew John Laufersweiler , Cynthia Monesa Crago Clark , Michael Philip Clark , Jane Far-Jine Djung , Biswanath De , Michael George Natchus
发明人： Matthew John Laufersweiler , Cynthia Monesa Crago Clark , Michael Philip Clark , Jane Far-Jine Djung , Biswanath De , Michael George Natchus
IPC分类号： A61K31513
CPC分类号： C07D401/14 , A61K31/505 , C07D403/04 , C07D403/14 , C07D405/14 , C07D407/14 , C07D417/14
摘要： The present invention relates to compounds which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, or enantiomeric and diasteriomeric forms or pharmaceutically acceptable salts thereof, have the formula: wherein R is an ether or amino unit, R1 is substituted phenyl, each R2 and R3 unit is independently selected from the group consisting of: a) hydrogen; and b) substituted or unsubstituted C1-C10 hydrocarbyl selected from the group consisting of: i) C1-C10 linear, branched or cyclic alkyl; ii) C1-C10 aryl; iii) C1-C10 heterocyclic; iv) C1-C10 heteroaryl.
摘要翻译：本发明涉及能够防止炎性细胞因子，所述化合物或对映异构体和非对映体形式或其药学上可接受的盐的细胞外释放的化合物，其具有下式：其中R是醚或氨基单元，R 1是取代的苯基，每个R 2和R 3单元独立地选自：a）氢; 和）b）C 1 -C 10杂环; iv）C 1 -C 10杂芳基。

8. 发明授权

US06569855B2 Substituted cyclic amine metalloprotease inhibitors 失效
标题翻译：取代的环状胺金属蛋白酶抑制剂
公开(公告)号：US06569855B2
公开(公告)日：2003-05-27
申请号：US09888675
申请日：2001-06-25
申请人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
发明人： Michael George Natchus , Biswanath De , Stanislaw Pikul , Neil Gregory Almstead , Roger Gunnard Bookland , Yetunde Olabisi Taiwo , Menyan Cheng
IPC分类号： A61K31401
CPC分类号： C07D207/42
摘要： The invention provides compounds which are useful as inhibitors of metalloproteases, and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to a compound having a structure according to Formula (I). Also disclosed are compounds, pharmaceutical compositions and methods of treating diseases characterized by metalloprotease activity using these compounds or the pharmaceutical compositions containing them.
摘要翻译：本发明提供了可用作金属蛋白酶抑制剂的化合物，其有效治疗以这些酶的过量活性为特征的病症。特别地，本发明涉及具有式（I）结构的化合物。还公开了使用这些化合物或含有它们的药物组合物治疗以金属蛋白酶活性为特征的疾病的化合物，药物组合物和方法。

9. 发明授权

US06566357B1 Spirocyclic-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines 失效
标题翻译：控制炎症细胞因子的螺环-6,7-二氢-5H-吡唑并[1,2-a]吡唑-1-酮
公开(公告)号：US06566357B1
公开(公告)日：2003-05-20
申请号：US10246499
申请日：2002-09-18
申请人： Matthew John Laufersweiler , Michael Philip Clark , Jane Far-Jine Djung , Adam Golebiowski , Todd Andrew Brugel , Biswanath De
发明人： Matthew John Laufersweiler , Michael Philip Clark , Jane Far-Jine Djung , Adam Golebiowski , Todd Andrew Brugel , Biswanath De
IPC分类号： C07D40104
CPC分类号： C07D487/04 , C07D491/20 , C07D495/20
摘要： The present invention relates to compound which are capable of preventing the extracellular release of inflammatory cytokines, said compounds, including all enantiomeric and diasteriomeric forms and pharmaceutically acceptable salts thereof, have the formula: wherein R comprises ethers or amines; R1 is: a) substituted or unsubstituted aryl; or b) substituted or unsubstituted heteroaryl; two R2 units on the same carbon atom are taken together to form a spirocyclic ring having from 4 to 7 atoms, the balance of the R2 units are independently selected from the group consisting of: a) hydrogen; b) —O(CH2)jR8; c) —(CH2)jNR9aR9b; d) —(CH2)jCO2R10; e) —(CH2)jOCO2R10 f) —CH2)jCON(R10)2; and g) two R2 units can be taken together to form a carbonyl unit; R8, R9a, R9b, and R10 are each independently hydrogen, C1-C4 alkyl, and mixtures thereof; R9a and R9b can be taken together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; two R10 units can be take together to form a carbocyclic or heterocyclic ring comprising from 3 to 7 atoms; j is an index from 0 to 5; the index n is from 3 to 5.
摘要翻译：本发明涉及能够防止炎性细胞因子细胞外释放的化合物，所述化合物包括所有对映异构体和非对映体形式及其药学上可接受的盐，具有下式：其中R包括醚或胺; R 1是：a）取代或未取代的芳基; 环）取代或未取代的杂芳基;同一碳原子上的两个R2单元一起形成具有4至7个原子的螺环，其余的R2单元独立地选自：a）氢; b ） - （CH2）jR8; c） - （CH2）jNR9aR9b; d） - （CH2）jCO2R10; e） - （CH2）jOCO2R10f）-CH2）jCON（R10）2; 和g）两个R2单元可以一起取代形成羰基单元; R8，R9a，R9b和R10各自独立地为氢，C1-C4烷基及其混合物; R9a和R9b可以一起形成包含3至7个原子的碳环或杂环; 两个R 10单元可以一起形成包含3至7个原子的碳环或杂环; j是从0到5的索引; 索引n为3到5。

10. 发明授权

US06372730B1 2-decarboxy-2-phosphinico Prostaglandin F analogs 有权
标题翻译： 2-decarboxy-2-phosphinico前列腺素F类似物
公开(公告)号：US06372730B1
公开(公告)日：2002-04-16
申请号：US09632256
申请日：2000-08-03
申请人： Mitchell Anthony deLong , John August Wos , Biswanath De , Frank Hallock Ebetino
发明人： Mitchell Anthony deLong , John August Wos , Biswanath De , Frank Hallock Ebetino
IPC分类号： A61K3166
CPC分类号： C07F9/303
摘要： The invention provides novel Prostaglandin F analogs. In particular, the present invention is directed to compounds having a structure according to the following formula: wherein R1, R2, X, Y, V, a, b, W, and Z are defined below. This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically—acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of a variety of diseases and conditions, such as bone disorders and glaucoma. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for bone disorders and glaucoma using these compounds or the compositions containing them.
摘要翻译：本发明提供了新型前列腺素F类似物。特别地，本发明涉及具有下式结构的化合物：其中R1，R2，X，Y，V，a，b，W和Z定义如下。本发明还包括光学异构体，非对映异构体和上式的对映异构体及其药学上可接受的盐，生物可水解的酰胺，酯和酰亚胺。本发明的化合物可用于治疗多种疾病和病症，例如骨骼疾病和青光眼。因此，本发明还提供包含这些化合物的药物组合物。本发明还提供了使用这些化合物或含有它们的组合物治疗骨病和青光眼的方法。

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