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1. 发明授权

US5476873A Acetylene derivatives having lipoxygenase inhibitory activity 失效
标题翻译：具有脂氧合酶抑制活性的乙炔衍生物
公开(公告)号：US5476873A
公开(公告)日：1995-12-19
申请号：US229860
申请日：1994-04-19
申请人： Dee W. Brooks , Andrew O. Stewart , Daniel J. Kerkman , Pramila A. Bhatia , Anwer Basha , Jonathan G. Martin
发明人： Dee W. Brooks , Andrew O. Stewart , Daniel J. Kerkman , Pramila A. Bhatia , Anwer Basha , Jonathan G. Martin
IPC分类号： C07C275/64 , C07D213/40 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/68 , C07D213/69 , C07D215/22 , C07D215/227 , C07D217/24 , C07D239/34 , C07D241/18 , C07D263/56 , C07D277/34 , C07D307/52 , C07D307/56 , C07D307/58 , C07D307/64 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/34 , C07D333/58 , C07D405/12 , C07D407/12 , C07D409/12 , C07C259/06 , A61K31/17 , C07C273/18
CPC分类号： C07D213/40 , C07C275/64 , C07D213/643 , C07D213/65 , C07D213/68 , C07D213/69 , C07D215/227 , C07D217/24 , C07D239/34 , C07D241/18 , C07D263/56 , C07D277/34 , C07D307/52 , C07D307/56 , C07D307/58 , C07D307/64 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/34 , C07D333/58 , C07D405/12 , C07D407/12 , C07D409/12
摘要： Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：结构的化合物，其中p和q为0或1，但不能都相同，M为药学上可接受的阳离子或代谢可裂解基团，B为价键或直链或支链亚烷基，R为烷基，环烷基或-NR1R2，其中R1和R2是氢，烷基，环烷基或烷酰基，A是任选取代的碳环芳基，呋喃基，苯并[b]呋喃基，噻吩基或苯并[b]噻吩基是脂氧合酶从而抑制白细胞三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

2. 发明授权

US5559144A Furyl and thienyl alkynyl-N-hydroxy urea derivatives 失效
标题翻译：呋喃基和噻吩基炔基-N-羟基脲衍生物
公开(公告)号：US5559144A
公开(公告)日：1996-09-24
申请号：US435399
申请日：1995-05-05
申请人： Dee W. Brooks , Andrew O. Stewart , Daniel J. Kerkman , Pramila A. Bhatia , Anwer Basha , Jonathan G. Martin
发明人： Dee W. Brooks , Andrew O. Stewart , Daniel J. Kerkman , Pramila A. Bhatia , Anwer Basha , Jonathan G. Martin
IPC分类号： C07C275/64 , C07D213/40 , C07D213/64 , C07D213/643 , C07D213/65 , C07D213/68 , C07D213/69 , C07D215/22 , C07D215/227 , C07D217/24 , C07D239/34 , C07D241/18 , C07D263/56 , C07D277/34 , C07D307/52 , C07D307/56 , C07D307/58 , C07D307/64 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/34 , C07D333/58 , C07D405/12 , C07D407/12 , C07D409/12 , A61K31/34 , A61K31/38 , C07D307/46 , C07D333/22
CPC分类号： C07D213/40 , C07C275/64 , C07D213/643 , C07D213/65 , C07D213/68 , C07D213/69 , C07D215/227 , C07D217/24 , C07D239/34 , C07D241/18 , C07D263/56 , C07D277/34 , C07D307/52 , C07D307/56 , C07D307/58 , C07D307/64 , C07D307/81 , C07D333/20 , C07D333/28 , C07D333/32 , C07D333/34 , C07D333/58 , C07D405/12 , C07D407/12 , C07D409/12
摘要： Compounds of the structure ##STR1## where p and q are zero or one, but cannot both be the same, M is a pharmaceutically acceptable cation or a metabolically cleavable group, B is a valence bond or a straight or branched alkylene group, R is alkyl, cycloalkyl or --NR.sup.1 R.sup.2, where R.sup.1 and R.sup.2 are hydrogen, alkyl, cycloalkyl or alkanoyl, and A is optionally substituted carbocyclic aryl, furyl, benzo[b]furyl, thienyl, or benzo[b]thienyl are potent inhibitors of lipoxygenase enzymes and thus inhibit the biosynthesis of leukotrienes. These compounds are useful in the treatment or amelioration of allergic and inflammatory disease states.
摘要翻译：结构的化合物，其中p和q为0或1，但不能都相同，M为药学上可接受的阳离子或代谢可裂解基团，B为价键或直链或支链亚烷基，R为烷基，环烷基或-NR1R2，其中R1和R2是氢，烷基，环烷基或烷酰基，A是任选取代的碳环芳基，呋喃基，苯并[b]呋喃基，噻吩基或苯并[b]噻吩基是脂氧合酶的有效抑制剂从而抑制白细胞三烯的生物合成。这些化合物可用于治疗或改善过敏性和炎性疾病状态。

3. 发明授权

US4970210A Triazinone lipoxygenase compounds 失效
标题翻译：三嗪酮脂氧合酶化合物
公开(公告)号：US4970210A
公开(公告)日：1990-11-13
申请号：US210806
申请日：1988-06-28
申请人： Dee W. Brooks , Anwer Basha , Bruce P. Gunn , Pramila A. Bhatia
发明人： Dee W. Brooks , Anwer Basha , Bruce P. Gunn , Pramila A. Bhatia
IPC分类号： A61K31/50 , A61K31/52 , A61K31/522 , A61K31/53 , A61K31/535 , A61P11/00 , A61P27/16 , A61P29/00 , A61P43/00 , C07D237/04 , C07D253/06 , C07D273/04 , C07D401/04 , C07D401/10 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/10 , C07D409/04 , C07D413/04 , C07D413/10 , C07D417/04 , C07D417/10 , C07D473/08
CPC分类号： C07D253/06 , C07D237/04 , C07D273/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04
摘要： Pyridazinone, triazinone and oxapyridazinone compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.

4. 发明授权

US5288751A [(Substituted) phenyalkyl]furylalkynyl-and [substituted) phenyalkyl] thienylalkynyl-N-hydroxyurea inhibitors or leukotriene biosynthesis 失效
标题翻译： [（取代的）烷基]呋喃基炔基和[取代的]烷基]噻吩基炔基-N-羟基脲抑制剂或白三烯生物合成
公开(公告)号：US5288751A
公开(公告)日：1994-02-22
申请号：US973100
申请日：1992-11-06
申请人： Dee W. Brooks , Andrew O. Stewart , Anwer Basha , Pramila Bhatia , James D. Ratajczyk
发明人： Dee W. Brooks , Andrew O. Stewart , Anwer Basha , Pramila Bhatia , James D. Ratajczyk
IPC分类号： A61K31/17 , A61K31/38 , A61K31/381 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4433 , A61P9/00 , A61P9/10 , A61P11/00 , A61P17/00 , A61P25/00 , A61P27/16 , A61P29/00 , A61P37/08 , A61P43/00 , C07C273/18 , C07C275/24 , C07C275/64 , C07D213/61 , C07D277/28 , C07D307/52 , C07D333/20 , C07D333/22 , C07D405/06 , C07D409/04 , C07D409/06 , C07D417/04 , C07D307/36 , A61K31/34
CPC分类号： C07D405/06 , C07C275/64 , C07D213/61 , C07D277/28 , C07D307/52 , C07D333/20 , C07D409/06
摘要： The present invention relates to compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein Z is selected from optionally substituted phenyl, furyl, thienyl or thiazolyl; which inhibits leukotriene biosynthesis and is useful in the treatment of inflammatory disease states; also disclosed are leukotriene biosynthesis inhibiting compositions and a method for inhibiting 5-lipoxygenase activity and leukotriene biosynthesis.
摘要翻译：本发明涉及式IMA的化合物及其药学上可接受的盐，其中Z选自任选取代的苯基，呋喃基，噻吩基或噻唑基; 其抑制白细胞三烯生物合成并且可用于治疗炎性疾病状态; 还公开了白三烯生物合成抑制组合物和抑制5-脂氧合酶活性和白三烯生物合成的方法。

5. 发明授权

US5292900A O-substituted N-hydroxyurea derivatives 失效
标题翻译： O-取代的N-羟基脲衍生物
公开(公告)号：US5292900A
公开(公告)日：1994-03-08
申请号：US992389
申请日：1992-12-18
申请人： Anwer Basha , Dee W. Brooks
发明人： Anwer Basha , Dee W. Brooks
IPC分类号： C07C275/64 , C07D309/12 , C07D333/58 , C07D209/04
CPC分类号： C07D333/58 , C07C275/64 , C07D309/12 , Y02P20/55
摘要： The present invention provides compounds useful as intermediates for the preparation of 5-lipoxygenase inhibiting compounds. The intermediates of this invention have the structure ##STR1## wherein R.sup.1 is an O-protecting group selected from the group consisting of ##STR2## In the above, X is oxygen or sulfur.
摘要翻译：本发明提供了可用作制备5-脂氧合酶抑制化合物的中间体的化合物。本发明的中间体具有结构（*化学结构*），其中R1是选自（*化学结构*）（*化学结构*）的O-保护基。在上述中，X是氧或硫。

6. 发明授权

US5086052A Substituted 1,4,5,6-tetrahydro-2H-pyridazin-3-one and -3-thione compounds having lipoxygenase inhibitory activity 失效
标题翻译：取代的具有脂氧合酶抑制活性的1,4,5,6-四氢-2H-哒嗪-3-酮和-3-硫酮化合物
公开(公告)号：US5086052A
公开(公告)日：1992-02-04
申请号：US546337
申请日：1990-06-28
申请人： Dee W. Brooks , George W. Carter , Anwer Basha , Bruce P. Gunn , Richard D. Dyer
发明人： Dee W. Brooks , George W. Carter , Anwer Basha , Bruce P. Gunn , Richard D. Dyer
IPC分类号： C07D237/04 , C07D253/06 , C07D273/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04
CPC分类号： C07D253/06 , C07D237/04 , C07D273/04 , C07D401/04 , C07D403/04 , C07D405/04 , C07D413/04 , C07D417/04
摘要： Pyridazinone, triazinone and oxapyridazinone compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.
摘要翻译：哒嗪酮，三嗪酮和氧哒嗪酮化合物，其可用于抑制脂氧合酶，特别是5-脂氧合酶。

7. 发明授权

US4963541A Pyrimido-pyrimidine lipoxygenase inhibiting compounds 失效
标题翻译：嘧啶 - 嘧啶脂氧合酶抑制化合物
公开(公告)号：US4963541A
公开(公告)日：1990-10-16
申请号：US314008
申请日：1989-02-22
申请人： Dee W. Brooks , Anwer Basha
发明人： Dee W. Brooks , Anwer Basha
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： Compounds of the formula: ##STR1## wherein A is selected from NR.sub.1 R.sub.2 and N(OR.sub.6)R.sub.2 ; and B and C are chloro when A is N(OR.sub.6)R.sub.2 or are independently selected from NHR.sub.3 and NR.sub.4 R.sub.5 where R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are independently selected from the group consisting of alkyl, cycloalkyl and alkylaryl each of which may be unsubstituted or substituted with one or more substituents selected from the group consisting of hydroxy, OR, NRR, OCOR, OCONRR, NRCOR and NRCONRR where R is selected from the group consisting of hydrogen, alkyl, aryl, alkylaryl, alkoxy and hydroxy or R.sub.1 and R.sub.2 or R.sub.4 and R.sub.5 together can form a heteroaryl group and R.sub.6 is a member selected from the group consisting of hydrogen, alkyl, alkylaryl and trialkylsilyl; and the pharmaceutically acceptable salts thereof.These compounds are useful as inhibitors of lipoxygenase enzymes.
摘要翻译：下式的化合物：其中A选自NR1R2和N（OR6）R2; 当A为N（OR 6）R 2时，B和C为氯，或独立地选自NHR 3和NR 4 R 5，其中R 1，R 2，R 3，R 4和R 5独立地选自烷基，环烷基和烷芳基，其各自可以是未取代或被一个或多个选自羟基，OR，NRR，OCOR，OCONRR，NRCOR和NRCONRR的取代基取代，其中R选自氢，烷基，芳基，烷基芳基，烷氧基和羟基或R 1和 R2或R4和R5一起可以形成杂芳基，R6是选自氢，烷基，烷基芳基和三烷基甲硅烷基的成员; 及其药学上可接受的盐。这些化合物可用作脂氧合酶的抑制剂。

8. 发明授权

US07001895B2 Prostaglandin endoperoxide H synthase biosynthesis inhibitors 失效
标题翻译：前列腺素内过氧化物H合成酶生物合成抑制剂
公开(公告)号：US07001895B2
公开(公告)日：2006-02-21
申请号：US10417959
申请日：2003-04-17
申请人： Lawrence A. Black , Anwer Basha , Teodozyj Kolasa , Michael E. Kort , Huaqing Liu , Catherine M. McCarty , Meena Patel , Jeffrey J. Rohde , Michael J. Coghlan , Andrew O. Stewart
发明人： Lawrence A. Black , Anwer Basha , Teodozyj Kolasa , Michael E. Kort , Huaqing Liu , Catherine M. McCarty , Meena Patel , Jeffrey J. Rohde , Michael J. Coghlan , Andrew O. Stewart
IPC分类号： A61K31/50 , A61K31/675 , C07D237/16
CPC分类号： C07D405/04 , C07D237/14 , C07D409/04
摘要： The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
摘要翻译：本发明描述了配方的哒嗪酮化合物

9. 发明授权

US06307047B1 Prostaglandin endoperoxide H synthase biosynthesis inhibitors 失效
标题翻译：前列腺素内过氧化物H合成酶生物合成抑制剂
公开(公告)号：US06307047B1
公开(公告)日：2001-10-23
申请号：US09427768
申请日：1999-10-27
申请人： Lawrence A. Black , Anwer Basha , Teodozyj Kolasa , Michael E. Kort , Huaqing Liu , Catherine M. McCarty , Meena Patel , Jeffrey J. Rohde , Michael J. Coghlan , Andrew O. Stewart
发明人： Lawrence A. Black , Anwer Basha , Teodozyj Kolasa , Michael E. Kort , Huaqing Liu , Catherine M. McCarty , Meena Patel , Jeffrey J. Rohde , Michael J. Coghlan , Andrew O. Stewart
IPC分类号： C07D23716
CPC分类号： C07D405/04 , C07D237/14 , C07D409/04
摘要： The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
摘要翻译：本发明描述了式I的哒嗪酮化合物，其是环氧合酶（COX）抑制剂，特别是环氧合酶-2（COX-2）的选择性抑制剂。 COX-2是与炎症相关的诱导型同种型，与组成型异环霉素（COX-1）相反，环氧合酶-1（COX-1）是许多组织中重要的“内服”酶，包括胃肠道（GI）和肾脏。这些化合物对COX-2的选择性最小化了目前市售的非甾体抗炎药（NSAID）所见的不希望的GI和肾脏副作用。

10. 发明申请

US20090042888A1 Prostaglandin endoperoxide H synthase biosynthesis inhibitors 审中-公开
标题翻译：前列腺素内过氧化物H合成酶生物合成抑制剂
公开(公告)号：US20090042888A1
公开(公告)日：2009-02-12
申请号：US11473633
申请日：2006-06-23
申请人： Lawrence A. Black , Anwer Basha , Teodozyj Kolasa , Michael E. Kort , Huaqing Liu , Catherine M. McCarty , Meena Patel , Jeffrey J. Rohde , Michael J. Coghlan , Andrew O. Stewart
发明人： Lawrence A. Black , Anwer Basha , Teodozyj Kolasa , Michael E. Kort , Huaqing Liu , Catherine M. McCarty , Meena Patel , Jeffrey J. Rohde , Michael J. Coghlan , Andrew O. Stewart
IPC分类号： A61K31/50 , A61P35/00
CPC分类号： C07D405/04 , C07D237/14 , C07D409/04
摘要： The present invention describes pyridazinone compounds of formula I which are cyclooxygenase (COX) inhibitors, and in particular, are selective inhibitors of cyclooxygenase-2 (COX-2). COX-2 is the inducible isoform associated with inflammation, as opposed to the constitutive isoform, cyclooxygenase-1 (COX-1) which is an important “housekeeping” enzyme in many tissues, including the gastrointestinal (GI) tract and the kidneys. The selectivity of these compounds for COX-2 minimizes the unwanted GI and renal side-effects seen with currently marketed non-steroidal anti-inflammatory drugs (NSAIDs).
摘要翻译：本发明描述了作为环加氧酶（COX）抑制剂的式I的哒嗪酮化合物，特别是环氧合酶-2（COX-2）的选择性抑制剂。 COX-2是与炎症相关的诱导型同种型，与组成型异环霉素（COX-1）相反，环氧合酶-1（COX-1）是许多组织中重要的“内服”酶，包括胃肠道（GI）和肾脏。这些化合物对COX-2的选择性最小化了目前市售的非甾体抗炎药（NSAID）所见的不希望的GI和肾脏副作用。

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