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1. 发明申请

WO1996032377A1 LIPOXYGENASE AND CYCLOOXYGENASE INHIBITING COMPOUNDS 审中-公开
标题翻译： LIPOXYGENASE和CYCLOOXYGENASE抑制化合物
公开(公告)号：WO1996032377A1
公开(公告)日：1996-10-17
申请号：PCT/US1996003907
申请日：1996-03-22
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , BROOKS, Clint, D., W. , STEWART, Andrew, O. , BASHA, Anwer , BELL, Randy, L.
IPC分类号： C07C275/64
CPC分类号： C07D409/12 , C07C275/64 , C07D307/52 , C07D333/20 , C07D333/58
摘要： Compounds having the structure of general formula (I) or a pharmaceutically acceptable salt thereof have activity as inhibitors of cyclooxygenase and 5-lipoxygenase, reduce the biosynthesis of leukotrienes B4, C4, D4, and E4 and cyclooxygenase products such as prostaglandins and thromboxane and are useful in the treatment of inflammatory and allergic disease states. The compounds have the structure indicated above wherein A is selected from (a) optionally susbtituted carbocyclic aryl, (b) optionally substituted furyl, (c) optionally substituted benzo[b]furyl, (d) optionally substituted thienyl, (e) optionally substituted pyridyloxy, (f) optionally substituted pyridylalkyl, (g) optionally substituted benzo[b]thienyl, (h) optionally substituted pyridyl, (i) optionally substituted quinolyl, and (j) optionally substituted indolyl; X is selected from (a) optionally susbtituted alkyl, (b) optionally substituted alkenyl, and (c) optionally substituted alkynyl; R and R are independently selected from hydrogen, hydroxy, and alkyl; and Z is a residue of a non-steroidal anti-inflammatory drug of the general formula Z-COOH.
摘要翻译：具有通式（I）结构的化合物或其药学上可接受的盐具有作为环加氧酶和5-脂氧合酶抑制剂的活性，降低了白三烯B4，C4，D4和E4以及环氧合酶产物如前列腺素和血栓素的生物合成，可用于治疗炎症和过敏性疾病状态。化合物具有上述结构，其中A选自（a）任选取代的碳环芳基，（b）任选取代的呋喃基，（c）任选取代的苯并[b]呋喃基，（d）任选取代的噻吩基，（e）吡啶基氧基，（f）任选取代的吡啶基烷基，（g）任选取代的苯并[b]噻吩基，（h）任选取代的吡啶基，（i）任选取代的喹啉基，和（j）任选取代的吲哚基; X选自（a）任选的取代的烷基，（b）任选取代的烯基，和（c）任选取代的炔基; R 1和R 2独立地选自氢，羟基和烷基; Z为通式Z-COOH的非甾体抗炎药物的残基。

2. 发明申请

WO1994026264A1 (4-ALKOXYPYRAN-4-YL) SUBSTITUTED ARYLALKYLARYL-, ARYLALKENYLARYL-, AND ARYLALKYNYLARYLUREA INHIBITORS OF 5-LIPOXYGENASE 审中-公开
标题翻译：（4-ALKOXYPYRAN-4-YL）取代的芳基乙烯基-L-亚苄基胆碱酯酶和5-氯吡咯烷酮的芳基烯丙基胺抑制剂
公开(公告)号：WO1994026264A1
公开(公告)日：1994-11-24
申请号：PCT/US1994005341
申请日：1994-05-12
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , DELLARIA, Joseph, F. , BASHA, Anwer , BLACK, Lawrence, A. , CHERNESKY, Linda, J. , LEE, Wendy
IPC分类号： A61K31/335
CPC分类号： C07D405/12 , C07D309/12
摘要： Compounds of structure (I), wherein W is selected from (a), and (b), where Q is oxygen or sulfur, R and R are hydrogen or alkyl, or R and R , together with the nitrogen atoms to which they are attached, define a radical of formula (II) or (III), R is selected from hydrogen, alkyl, haloalkyl, optionally substituted phenyl, hydroxyalkyl, aminoalkyl, carboxyalkyl, (alkoxycarbonyl)alkyl, and (alkylaminocarbonyl)alkyl; Z is -CH2-, oxygen, sulfur, or -NR where R is hydrogen or alkyl, L and L are selected from a valence bond, alkylene, propenylene, and propynylene, R , R , R , and R are independently selected from alkyl, haloalkyl, halogen, cyano, amino, alkoxycarbonyl, and dialkylaminocarbonyl, Y is selected from oxygen, -NR , where R is hydrogen or alkyl, and (c), where n = 0, 1, or 2, and R is alkyl, 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W选自（a）和（b）中的结构（I）的化合物，其中Q是氧或硫，R 6和R 7是氢或烷基，或R 6和R 6，（II）或（III）的基团，其中R 8与它们所连接的氮原子一起定义为式（II）或（III）的基团，R 8选自氢，烷基，卤代烷基，任选取代的苯基，羟基烷基，氨基烷基，羧基烷基，（烷氧基羰基）烷基和（烷基氨基羰基）烷基; Z是-CH 2 - ，氧，硫或-NR 9，其中R 9是氢或烷基，L 1和L 2选自价键，亚烷基，亚丙烯基和亚丙炔基，R R 1，R 2，R 3和R 4独立地选自烷基，卤代烷基，卤素，氰基，氨基，烷氧基羰基和二烷基氨基羰基，Y选自氧，-NR 10，其中R 10是氢或烷基，和（c）其中n = 0,1或2，R 5是烷基，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. 发明申请

WO2005028477A1 SUBSTITUTED DIAZABICYCLOALKANE DERIVATIVES AS LIGANDS AT ALPHA 7 NICOTINIC ACETY LCHOLINE RECEPTORS 审中-公开
标题翻译：取代的双唑胆碱衍生物作为ALPHA的配体7 NICOTINIC乙酰胆碱受体
公开(公告)号：WO2005028477A1
公开(公告)日：2005-03-31
申请号：PCT/US2004/030735
申请日：2004-09-17
申请人： ABBOTT LABORATORIES , LI, Tao , BASHA, Anwer , BUNNELLE, William, H. , DART, Michael, J. , GALLAGHER, Megan, E. , JI, Jianguo , PACE, Jennifer, M. , RYTHER, Keith, B. , TIETJE, Karin, R. , MORTELL, Kathleen, H. , NERSESIAN, Diana, L. , SCHRIMPF, Michael, R.
发明人： BASHA, Anwer , BUNNELLE, William, H. , DART, Michael, J. , GALLAGHER, Megan, E. , JI, Jianguo , PACE, Jennifer, M. , RYTHER, Keith, B. , TIETJE, Karin, R. , MORTELL, Kathleen, H. , NERSESIAN, Diana, L. , SCHRIMPF, Michael, R.
IPC分类号： C07D471/04
CPC分类号： C07D487/08 , C07D471/04 , C07D471/08 , C07D487/04
摘要： Compounds of formula (I) Z-Ar 1 -Ar 2 wherein Z is a diazabicyclic amine, Ar 1 is a 5- or 6-membered aromatic ring, and Ar 2 is selected from the group consisting of an unsubstituted or substituted 5- or 6-membered heteroaryl ring; unsubstituted or substituted bicyclic heteroaryl ring; 3,4-(methylenedioxy)phenyl; carbazolyl; tetrahydrocarbazolyl; naphthyl; and phenyl; wherein the phenyl is substituted with 0, 1, 2, or 3 substituents in the meta- or para-positions. The compounds are useful in treating conditions or disorders prevented by or ameliorated by α7 nAChR ligands. Also disclosed are pharmaceutical compositions comprising compounds of formula (I) and methods for using such compounds and compositions.
摘要翻译：式（I）化合物Z-Ar 1 -Ar 2其中Z是二氮杂双环胺，Ar 1是5-或6-元芳环，Ar 2选自未取代或取代的5-或 6元杂芳基环; 未取代或取代的双环杂芳基环; 3,4-（亚甲二氧基）苯基; 咔唑; tetrahydrocarbazolyl; 萘; 和苯基; 其中苯基在间位或对位被0,1,2或3个取代基取代。该化合物可用于治疗由α7nAChR配体预防或改善的病症或病症。还公开了包含式（I）化合物和使用这些化合物和组合物的方法的药物组合物。

4. 发明申请

WO1990009996A1 PYRIMIDO-PYRIMIDINE LIPOXYGENASE INHIBITING COMPOUNDS 审中-公开
标题翻译：吡咯烷基 - 吡咯烷酮LIPOXYGENASE抑制化合物
公开(公告)号：WO1990009996A1
公开(公告)日：1990-09-07
申请号：PCT/US1990000689
申请日：1990-02-07
申请人： ABBOTT LABORATORIES
发明人： ABBOTT LABORATORIES , BROOKS, Dee, W. , BASHA, Anwer
IPC分类号： C07D223/02
CPC分类号： C07D487/04
摘要： Compounds of the formula (I), wherein A is selected from NR1R2 and N(OR6)R2; and B and C are chloro when A is N(OR6)R2 or are independently selected from NHR3 and NR4R5 where R1, R2, R3, R4 and R5 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 R1 and R2 or R4 and R5 together can form a heteroaryl group and R6 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.

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