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1. 发明授权

US06841671B2 Spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译：螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06841671B2
公开(公告)日：2005-01-11
申请号：US10047592
申请日：2001-10-23
申请人： Mark C. Noe , Martin J. Wythes , Brian S. Bronk
发明人： Mark C. Noe , Martin J. Wythes , Brian S. Bronk
IPC分类号： C07D471/10 , C07D487/10
CPC分类号： C07D471/10 , C07D487/10
摘要： The present invention relates to 5-spiro-pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein said “A” is a 5-7 membered heterocyclic ring as defined in the specification and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及式Ⅳ所示的5-螺 - 嘧啶-2,4,6-三酮金属蛋白酶抑制剂，所述“A”是本说明书中定义的5-7元杂环，以及治疗炎症的药物组合物和方法，癌症等疾病。

2. 发明授权

US06706723B2 Pyrimidine-2,4,6-trione metalloproteinase inhibitors 失效
标题翻译：嘧啶-2,4,6-三酮金属蛋白酶抑制剂
公开(公告)号：US06706723B2
公开(公告)日：2004-03-16
申请号：US10032837
申请日：2001-10-25
申请人： Mark C. Noe , Lawrence A. Reiter , Martin J. Wythes
发明人： Mark C. Noe , Lawrence A. Reiter , Martin J. Wythes
IPC分类号： C07D23962
CPC分类号： C07D239/62 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to pyrimidine-2,4,6-trione metalloproteinase inhibitors of the formula wherein X, Y, A, B and R1 are as defined in the specification, and to pharmaceutical compositions and methods of treating inflammation, cancer and other disorders.
摘要翻译：本发明涉及X，Y，A，B和R 1的嘧啶-2,4,6-三酮金属蛋白酶抑制剂，如本说明书中所定义，以及治疗炎症，癌症和其他疾病。

3. 发明授权

US5607960A Indole derivatives as 5-HT1-like agonists for use in migraine 失效
标题翻译：吲哚衍生物作为用于偏头痛的5-HT1样激动剂
公开(公告)号：US5607960A
公开(公告)日：1997-03-04
申请号：US532573
申请日：1995-10-20
申请人： Martin J. Wythes
发明人： Martin J. Wythes
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/445 , A61P1/08 , A61P3/04 , A61P25/04 , A61P25/06 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/16 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/14 , A61K31/405 , C07D401/06
CPC分类号： C07D401/04 , C07D209/16 , C07D401/14 , C07D403/04 , C07D403/06 , C07D405/14
摘要： The present invention relates to 3,5-disubstituted indole compounds which are selective agonists which act on 5-hdroxytryptamine receptors useful in the treatment of migraine.
摘要翻译： PCT No.PCT / EP94 / 01121 Sec。 371 1995年10月20日第 102（e）日期1995年10月20日PCT 1994年4月11日PCT PCT。公开号WO94 / 24127 日期：1994年10月27日本发明涉及作为用于治疗偏头痛的5-羟色胺受体的选择性激动剂的3,5-二取代吲哚化合物。

4. 发明授权

US5607951A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5607951A
公开(公告)日：1997-03-04
申请号：US470392
申请日：1995-06-06
申请人： John E. Macor , Martin J. Wythes
发明人： John E. Macor , Martin J. Wythes
IPC分类号： A61K31/40 , C07D401/06 , C07D403/06
CPC分类号： A61K31/40 , C07D401/06 , C07D403/06
摘要： Compounds of the formula ##STR1## wherein the substituents are as defined in the description and the pharmaceutically acceptable salts thereof are new. These compounds are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate.
摘要翻译：其中取代基如说明书及其药学上可接受的盐所定义的式ⅠA的化合物是新的。这些化合物是有用的精神治疗药物，是有效的5-羟色胺（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛，慢性阵发性血尿素和与血管相关的头痛疾病，以及其它由缺乏血清素能神经传递引起的疾病。该化合物也可用作中枢作用的抗高血压药和血管扩张剂。通过二卤化中间体的过渡金属催化环化形成吲哚的方法。

5. 发明授权

US06686357B1 FKBP inhibitors 失效
公开(公告)号：US06686357B1
公开(公告)日：2004-02-03
申请号：US09699752
申请日：2000-10-30
申请人： Martin J. Wythes , Michael J. Palmer , Mark I. Kemp , Malcolm C. MacKenny , Robert J. Maguire , James F. Blake, Jr.
发明人： Martin J. Wythes , Michael J. Palmer , Mark I. Kemp , Malcolm C. MacKenny , Robert J. Maguire , James F. Blake, Jr.
IPC分类号： A61K31535
CPC分类号： C07D211/60 , A61K31/423 , A61K31/428 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/14
摘要： Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.

6. 发明授权

US06495549B1 FKBP inhibitors 失效
标题翻译： FKBP抑制剂
公开(公告)号：US06495549B1
公开(公告)日：2002-12-17
申请号：US09699878
申请日：2000-10-30
申请人： Martin J. Wythes , Michael J. Palmer , Mark I. Kemp , Malcolm C. MacKenny , Robert J. Maguire , James F. Blake, Jr.
发明人： Martin J. Wythes , Michael J. Palmer , Mark I. Kemp , Malcolm C. MacKenny , Robert J. Maguire , James F. Blake, Jr.
IPC分类号： A61K31535
CPC分类号： C07D211/60 , A61K31/423 , A61K31/428 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/14
摘要： Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.
摘要翻译：式（I）化合物，其盐和溶剂化物，其中取代基如本文所述，是FKBP抑制剂。

7. 发明授权

US5545644A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5545644A
公开(公告)日：1996-08-13
申请号：US466644
申请日：1995-06-06
申请人： John E. Macor , Martin J. Wythes
发明人： John E. Macor , Martin J. Wythes
IPC分类号： A61K31/40 , C07D401/06 , C07D403/06
CPC分类号： C07D401/06 , A61K31/40 , C07D403/06
摘要： Compounds of the formula ##STR1## wherein n is 0, 1, or 2; X is hydrogen, chlorine, bromine or iodine; R.sub.1 is hydrogen; R.sub.3 is selected from hydrogen and C.sub.1 to C.sub.6 linear or branched alkyl; and R.sub.2 is as defined in the specification and the pharmaceutically acceptable salts thereof are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate is also disclosed.
摘要翻译：式（Ⅰ）化合物其中n为0,1或2; X是氢，氯，溴或碘; R1是氢; R3选自氢和C1至C6直链或支链烷基; 和R2如说明书中所定义，其药学上可接受的盐是有用的精神治疗药物，并且是有效的5-羟色胺（5-HT1）激动剂，可用于治疗抑郁症，焦虑症，进食障碍，肥胖症，药物滥用，丛集性头痛，偏头痛，疼痛，慢性阵发性高血压和与血管疾病相关的头痛，以及由血清素能神经传递缺陷引起的其他障碍。该化合物也可用作中枢作用的抗高血压药和血管扩张剂。还公开了通过二卤代中间体的过渡金属催化环化形成吲哚的方法。

8. 发明授权

US6166011A FKBP inhibitors 失效
公开(公告)号：US6166011A
公开(公告)日：2000-12-26
申请号：US354193
申请日：1999-07-15
申请人： Martin J. Wythes , Michael J. Palmer , Mark I. Kemp , Malcolm C. MacKenny , Robert J. Maguire , James F. Blake, Jr.
发明人： Martin J. Wythes , Michael J. Palmer , Mark I. Kemp , Malcolm C. MacKenny , Robert J. Maguire , James F. Blake, Jr.
IPC分类号： C07D401/14 , A61K31/4184 , A61K31/423 , A61K31/428 , A61K31/445 , A61K31/5377 , A61P21/00 , A61P21/04 , A61P25/14 , A61P25/16 , A61P25/28 , A61P43/00 , C07D211/60 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/14 , A61K31/535
CPC分类号： C07D401/04 , A61K31/423 , A61K31/428 , C07D211/60 , C07D413/04 , C07D413/14 , C07D471/14
摘要： Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors. ##STR1##

9. 发明授权

US5192800A Glutaramide diuretic agents 失效
标题翻译：戊酰胺利尿剂
公开(公告)号：US5192800A
公开(公告)日：1993-03-09
申请号：US707559
申请日：1991-05-30
申请人： Ian T. Barnish , John C. Danilewicz , Keith James , Gillian M. B. Samuels , Nicholas K. Terrett , Michael T. Williams , Martin J. Wythes
发明人： Ian T. Barnish , John C. Danilewicz , Keith James , Gillian M. B. Samuels , Nicholas K. Terrett , Michael T. Williams , Martin J. Wythes
IPC分类号： C07D209/46 , C07D213/56 , C07D241/12 , C07D261/10 , C07D277/36 , C07D277/46 , C07D295/185 , C07D307/16 , C07D307/68 , C07D321/08 , C07D333/34 , C07D521/00
CPC分类号： C07D241/12 , C07D209/46 , C07D213/56 , C07D231/12 , C07D233/56 , C07D249/08 , C07D261/10 , C07D277/36 , C07D277/46 , C07D295/185 , C07D307/16 , C07D307/68 , C07D321/08 , C07D333/34
摘要： A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6- membered carbocyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3,4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.
摘要翻译：已经制备了一系列新的螺取代的戊二酰胺衍生物，包括其药学上可接受的盐和其生物前体，其中螺 - 取代基完成5-或6-元碳环并且位于与氨基甲酰基相邻的碳原子。这些特定化合物是中性肽链内切酶E.C.3,4.24.11酶的抑制剂，因此可用于治疗高血压，心力衰竭，肾功能不全和其他疾病的利尿剂。提供了从已知原料制备这些化合物的方法。

10. 发明授权

US5030654A Glutaramide diuretic agents 失效
标题翻译：戊酰胺利尿剂
公开(公告)号：US5030654A
公开(公告)日：1991-07-09
申请号：US354170
申请日：1989-05-19
申请人： Ian T. Barnish , John C. Danilewicz , Keith James , Gillian M. R. Samuels , Nicholas K. Terrett , Michael T. Williams , Martin J. Wythes
发明人： Ian T. Barnish , John C. Danilewicz , Keith James , Gillian M. R. Samuels , Nicholas K. Terrett , Michael T. Williams , Martin J. Wythes
IPC分类号： A61K31/16 , A61K31/335 , A61K31/395 , C07C235/52 , C07C235/82 , C07C237/24 , C07C311/01 , C07D207/30 , C07D209/46 , C07D213/02 , C07D213/56 , C07D231/00 , C07D233/00 , C07D235/00 , C07D237/00 , C07D239/00 , C07D241/12 , C07D261/10 , C07D277/36 , C07D277/46 , C07D295/00 , C07D295/185 , C07D307/04 , C07D307/16 , C07D307/68 , C07D309/02 , C07D319/00 , C07D321/02 , C07D321/08 , C07D321/12 , C07D333/34 , C07D521/00
CPC分类号： C07D241/12 , C07D209/46 , C07D213/56 , C07D231/12 , C07D233/56 , C07D249/08 , C07D261/10 , C07D277/36 , C07D277/46 , C07D295/185 , C07D307/16 , C07D307/68 , C07D321/08 , C07D333/34
摘要： A series of novel spiro-substituted glutaramide derivatives have been prepared, including the pharmaceutically acceptable salts thereof and bioprecursors therefor, wherein the spiro-substituent completes a 5- or 6-membered carbocycyclic ring and is located at the carbon atom adjacent to the carbamoyl group. These particular compounds are inhibitors of the neutral endopeptidase E.C.3.4.24.11 enzyme and are therefore useful in therapy as diuretic agents for the treatment of hypertension, heart failure, renal insufficiency and other disorders. Methods for preparing these compounds from known starting materials are provided.

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