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1. 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.

2. 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。

3. 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。

4. 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。

5. 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。

6. 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。

7. 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。

8. 发明授权

US5183818A Arylalkylether and arylalkylthioether inhibitors of lipoxygenase enzyme activity 失效
标题翻译：芳基烷基醚和芳烷基硫醚抑制剂的脂氧合酶活性
公开(公告)号：US5183818A
公开(公告)日：1993-02-02
申请号：US750362
申请日：1991-08-27
申请人： Dee W. Brooks , Andrew O. Stewart , Jonathan G. Martin
发明人： Dee W. Brooks , Andrew O. Stewart , Jonathan G. Martin
IPC分类号： C07D307/38 , C07D307/42 , C07D333/16 , C07D333/34 , C07D333/56 , C07D495/04
CPC分类号： C07D307/42 , C07D307/38 , C07D333/16 , C07D333/34 , C07D333/56 , C07D495/04
摘要： The present invention provides compounds having the structureY-Het-[Q.sub.1 ]-X-[Q.sub.2 ]-Zwhich inhibit the catalytic action of lipoxygenase enzymes, particularly 5-lipoxygenase, and thereby reduce the biosynthesis of leukotrienes B.sub.4, C.sub.4, D.sub.4, and E.sub.4.In the generic formula given above, X is oxygen or sulfur and Het is a heteroaryl group selected from the group consisting of furyl, thienyl, 2-, 3-, and 4-pyridyl, 2- and 3-benzo[b]furyl, 2- and 3-benzo[b]thienyl and thienothienyl.Y is one or two substituents independently selected from hydrogen, hydroxy, halogen, cyano, alkyl, haloalkyl, alkoxy, alkylthio, alkoxyaryl), alkylthioaryl, arylalkoxy, arylalkylthio, aryloxy, arylthio, alkylamido, cycloalkyl, alkanoyl, alkoxycarbonyl, amino, alkylamino, dialkylamino, and the following groups wherein R, at each occurrence, is independently selected from hydrogen and alkyl of from one to six carbon atoms: --CRROR, --NRC(O)R, --NRC(O)OR, and --C(O)NRR.The group Q.sub.1 is absent or is divalent alkylene of from one to six carbon atoms, and Q.sub.2 is divalent alkylene from from two to ten carbon atoms.The group Z is N(OR.sub.1)COR.sub.2 where R.sub.1 is selected from hydrogen or a pharmaceutically suitable salt. R.sub.2 is selected from hydrogen; alkyl; cycloalkyl; amino; alkylamino, optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; dialkylamino in which the alkyl groups are independently are optionally substituted by hydroxyl, halogen, alkoxy or carboxyl; cycloalkylamino; 2-hydroxyethylamino; N-morpholino; N-thiomorpholino; N-piperazine; N'-alkyl-N-piperazine and cyclopropylmethylamino.
摘要翻译：本发明提供具有抑制脂氧合酶，特别是5-脂氧合酶的催化作用的结构为Y-Het- [Q1] -X- [Q2] -Z的化合物，从而减少白三烯B4，C4，D4的生物合成，和E4。在上述通式中，X是氧或硫，Het是选自呋喃基，噻吩基，2-，3-和4-吡啶基，2-和3-苯并[b]呋喃基的杂芳基， 2-和3-苯并[b]噻吩基和噻吩并噻吩基。 Y是一个或两个独立地选自氢，羟基，卤素，氰基，烷基，卤代烷基，烷氧基，烷硫基，烷氧基芳基），烷基硫代芳基，芳基烷氧基，芳基烷硫基，芳氧基，芳硫基，烷基酰氨基，环烷基，烷酰基，烷氧基羰基，氨基，烷基氨基，二烷基氨基和下列基团，其中R 1在每次出现时独立地选自氢和1至6个碳原子的烷基：-CRROR，-NRC（O）R，-NRC（O）OR和-C（O ）NRR。基团Q1不存在或为1至6个碳原子的二价亚烷基，Q 2为2至10个碳原子的二价亚烷基。基团Z是N（OR 1）COR 2，其中R 1选自氢或药学上合适的盐。 R2选自氢; 烷基; 环烷基氨基; 任选被羟基，卤素，烷氧基或羧基取代的烷基氨基; 其中烷基独立的二烷基氨基任选被羟基，卤素，烷氧基或羧基取代; 环烷基氨基; 2-羟基乙基氨基; N-吗啉代; N-硫代吗啉代 N-哌嗪; N'-烷基-N-哌嗪和环丙基甲基氨基。

9. 发明授权

US5514702A Arylamidoalkyl-N-hydroxyurea compounds having lipoxygenase inhibitory activity 失效
标题翻译：具有脂氧合酶抑制活性的芳酰胺基烷基-N-羟基脲化合物
公开(公告)号：US5514702A
公开(公告)日：1996-05-07
申请号：US178237
申请日：1994-01-10
申请人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
发明人： Joseph F. Dellaria , Dee W. Brooks , Jimmie L. Moore , Kevin J. Sallin
IPC分类号： A61K31/165 , A61K31/17 , A61K31/34 , A61K31/341 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61K31/47 , A61P29/00 , A61P43/00 , C07C275/64 , C07C311/13 , C07C311/18 , C07C311/27 , C07C311/29 , C07C311/35 , C07C311/41 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D213/30 , C07D213/32 , C07D213/34 , C07D213/38 , C07D213/64 , C07D213/65 , C07D213/68 , C07D215/48 , C07D233/64 , C07D233/68 , C07D233/70 , C07D233/88 , C07D239/26 , C07D277/20 , C07D277/24 , C07D277/26 , C07D277/28 , C07D277/56 , C07D307/38 , C07D307/42 , C07D307/52 , C07D307/68 , C07D307/79 , C07D307/80 , C07D307/81 , C07D307/84 , C07D307/85 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/36 , C07D333/38 , C07D333/54 , C07D333/56 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12 , C07D333/32 , C07D333/34
CPC分类号： C07D213/64 , C07C275/64 , C07C311/18 , C07C317/40 , C07C317/44 , C07C323/41 , C07C323/60 , C07D207/34 , C07D215/48 , C07D277/56 , C07D307/68 , C07D307/85 , C07D333/20 , C07D333/38 , C07D333/70 , C07D405/12
摘要： The present invention provides certain (substituted carbocyclic aryl)amidoalkyl- and (substituted heterocyclic aryl)amidoalkyl-N-Hydroxy urea compounds which inhibit lipoxygenase enzyme activity and are thus useful in the treatment of allergic and inflammatory disease states.
摘要翻译： PCT No.PCT / US92 / 05715 Sec。 371日期1994年1月10日 102（e）日期1994年1月10日PCT提交1992年7月7日PCT公布。出版物WO93 / 02037 日期：1993年2月4日。本发明提供了某些（取代的碳环芳基）酰氨基烷基 - 和（取代的杂环芳基）酰氨基烷基-N-羟基脲化合物，其抑制脂氧合酶活性，因此可用于治疗过敏性和炎性疾病状态。

10. 发明授权

US5354865A Phenylmethyl derivatives having lipoxygenase inhibitory activity 失效
标题翻译：具有脂氧合酶抑制活性的苯甲基衍生物
公开(公告)号：US5354865A
公开(公告)日：1994-10-11
申请号：US942870
申请日：1992-09-10
申请人： Joseph F. Dellaria , Linda J. Dorn , Dee W. Brooks
发明人： Joseph F. Dellaria , Linda J. Dorn , Dee W. Brooks
IPC分类号： C07D305/06 , C07D309/04 , C07D309/06 , C07D309/10 , C07D405/12 , C07D235/26 , C07D215/227 , C07D265/36
CPC分类号： C07D405/12 , C07D305/06 , C07D309/04 , C07D309/06 , C07D309/10
摘要： Compounds of the structure ##STR1## where Ar is optionally substituted carbocyclic aryl, 5- or 6-membered heterocyclic aryl, 10-membered bicyclic heterocyclic aryl containing one or two nitrogen atoms, 9- or 10-membered heterocyclic containing one or two nitrogen atoms and optionally containing a further nitrogen or oxygen atom and one oxo or thioxo substituent, benzo[b]furyl, benzo[b]thienyl, A.sub.1 is propynylene, methylene, or a valence bond, X is O, S, SO.sub.2, or NR.sub.2, Y is selected from alkyl, haloalkyl, alkoxy, halogen, and hydrogen, A.sub.2 is selected from ##STR2## and methylene where Z is OR.sub.5 or NHR.sub.5 where R.sub.5 is hydrogen or alkyl, R.sub.1 is hydrogen, alkyl, or OR.sub.5, and m and n are integers having a value of 1 or 2 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：其中Ar是任选取代的碳环芳基，5-或6-元杂环芳基，含有一个或两个氮原子的10元双环杂环芳基，含有一个或两个氮原子的9元或10元杂环的结构化合物并且任选地含有另外的氮或氧原子和一个氧代或硫代取代基，苯并[b]呋喃基，苯并[b]噻吩基，A 1是亚丙炔基，亚甲基或价键，X是O，S，SO 2或NR 2， Y选自烷基，卤代烷基，烷氧基，卤素和氢，A2选自：其中Z是OR 5或亚甲基，其中R 5是氢或烷基，R 1是氢，烷基或OR 5，和m和n 是具有1或2值的整数是脂氧合酶的有效抑制剂，因此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。

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