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41. 发明专利

JP2003081937A Benzenesulfonamide derivative 审中-公开
标题翻译：苯并呋喃衍生物
公开(公告)号：JP2003081937A
公开(公告)日：2003-03-19
申请号：JP2001272327
申请日：2001-09-07
申请人： Bayer Ag , バイエルアクチェンゲゼルシャフト
发明人： RI EIFU , WATANABE AKIHIKO , LOWINGER TIMOTHY B , BACON KEVIN B , KAWAMURA NORIHIRO , SHINTANI TAKUYA , KIKUCHI TETSUO , MORIWAKI TOSHIYA
IPC分类号： A61K31/18 , A61K31/40 , A61K31/4025 , A61K31/4035 , A61K31/437 , A61K31/4375 , A61K31/4406 , A61K31/445 , A61K31/4453 , A61K31/4465 , A61K31/4523 , A61K31/454 , A61K31/495 , A61K31/496 , A61K31/4985 , A61K31/5375 , A61K31/551 , A61P5/16 , A61P9/10 , A61P11/02 , A61P11/06 , A61P25/28 , A61P27/16 , A61P29/00 , A61P31/18 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/08 , A61P43/00 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D209/44 , C07D211/14 , C07D211/26 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/70 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/12 , C07D295/13 , C07D295/194 , C07D295/22 , C07D295/26 , C07D307/14 , C07D333/38 , C07D333/40 , C07D471/04 , C07D487/04 , C07D487/08
CPC分类号： C07D213/70 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/13 , C07D295/194 , C07D295/26 , C07D307/14 , C07D333/38 , C07D471/04 , C07D487/04 , C07D487/08
摘要： PROBLEM TO BE SOLVED: To provide a benzenesulfonamide derivative useful as an active ingredient of pharmaceuticals. SOLUTION: This benzenesulfonamide derivative has CCR3 (CC-type chemokine receptor 3) antagonistic activity, therefore can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis, and other inflammatory/immunological disorders.
摘要翻译：待解决的问题：提供可用作药物活性成分的苯磺酰胺衍生物。解决方案：该苯磺酰胺衍生物具有CCR3（CC型趋化因子受体3）拮抗活性，因此可用于预防和治疗与CCR3活性相关的疾病，特别是用于治疗哮喘，特应性皮炎，过敏性鼻炎等炎性/免疫学障碍。

43. 发明专利

JP2002540198A 失效
公开(公告)号：JP2002540198A
公开(公告)日：2002-11-26
申请号：JP2000607998
申请日：2000-03-23
IPC分类号： C07D295/08 , A61K31/435 , A61K31/4545 , A61K31/473 , A61K31/495 , A61K31/496 , A61P1/00 , A61P1/04 , A61P7/02 , A61P11/00 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/14 , A61P27/16 , A61P29/00 , A61P37/00 , A61P37/08 , A61P39/02 , A61P43/00 , C07C275/64 , C07D295/00 , C07D295/084 , C07D295/088 , C07D295/092 , C07D295/096 , C07D295/12 , C07D295/125 , C07D295/13 , C07D295/135 , C07D295/14 , C07D295/15 , C07D307/14 , C07D307/52 , C07D401/04 , C07D401/06 , C07D401/08 , C07D403/06 , C07D405/06
摘要： The present invention provides 1,4 substituted piperazines, 1,4 substituted piperidines, and 1-substituted, 4-alkylidenyl piperidines compounds. The compounds of the invention are dual acting molecules having both leukotriene inhibition properties as well as antihistaminergic properties. The compounds of the invention are useful for treating conditions in which there is likely to be a histamine and/or leukotriene component. These conditions include preferably asthma, seasonal and perennial allergic rhinitis, sinusitus, conjunctivitis, food allergy, scombroid poisoning, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, chronic obstructive pulmonary disease, thrombotic disease and otitis media. Also provided are methods of treating asthma and rhinitis by administering an effective asthma and rhinitis-relieving amount of the compounds to a subject in need thereof.

44. 发明专利

JP2002537282A 失效
公开(公告)号：JP2002537282A
公开(公告)日：2002-11-05
申请号：JP2000599728
申请日：2000-02-12
IPC分类号： C07D295/04 , A61K31/138 , A61K31/341 , A61K31/4453 , A61P3/08 , A61P9/02 , A61P9/06 , A61P9/10 , A61P25/04 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , C07B57/00 , C07B61/00 , C07C213/02 , C07C213/06 , C07C217/48 , C07D233/48 , C07D295/08 , C07D295/088 , C07D307/22 , C07D307/52 , C07D309/14

45. 发明专利

JP2002531545A 失效
公开(公告)号：JP2002531545A
公开(公告)日：2002-09-24
申请号：JP2000586686
申请日：1999-12-06
IPC分类号： A61K31/17 , A61K31/343 , A61K31/472 , A61P31/22 , C07C275/42 , C07C335/18 , C07C335/20 , C07C335/22 , C07D217/26 , C07D295/088 , C07D307/81 , C07D307/85
摘要： Compounds of formula (I), wherein R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, -CN, -NO2, -CO2R6, -COR6, -OR6, -SR6, -SOR6, -SO2R6, -CONR7R8, -NR6N(R7R8), -N(R7R8) or W-Y-(CH2)n-Z provided that at least one of R1-R5 is not hydrogen; or R2 and R3 or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl; R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl; R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or R7 and R8, taken together may form a 3 to 7 membered heterocycloalkyl; R9-R12 are independently hydrogen, alkyl of 1 to 4 carbon atoms, perhaloalkyl of 1 to 4 carbon atoms, halogen, alkoxy of 1 to 4 carbon atoms, or cyano, or R9 and R10 or R11 and R12 may be taken together to form aryl of 5 to 7 carbon atoms; provided that at least one of R9-12 is not hydrogen; W is O, NR6, or is absent; Y is -(CO)- or -(CO2)-, or is absent; Z is alkyl of 1 to 4 carbon atoms, -CN, -CO2R6, COR6, -CONR7R8, -OCOR6, -NR6COR7, -OCONR6, -OR6, -SR6, -SOR6, -SO2R6, SR6N(R7R8), -N(R7R8) or phenyl; G is aryl or fused bicyclic heteroaryl; and X is a bond, -NH, alkyl of 1 to 6 carbon atoms, alkenyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, thioalkyl of 1 to 6 carbon atoms, alkylamino of 1 to 6 carbon atoms, or (CH)J; J is alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl or benzyl; and n is an integer from 1 to 6, in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.

46. 发明专利

JP2002515408A 失效
公开(公告)号：JP2002515408A
公开(公告)日：2002-05-28
申请号：JP2000549166
申请日：1999-05-10
IPC分类号： C07D295/12 , A61K31/4427 , A61K31/4439 , A61K31/445 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/542 , A61P9/12 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P27/02 , A61P43/00 , C07D209/08 , C07D211/22 , C07D217/04 , C07D295/088 , C07D295/13 , C07D401/12 , C07D513/04

47. 发明专利

JP2002507589A 失效
公开(公告)号：JP2002507589A
公开(公告)日：2002-03-12
申请号：JP2000537841
申请日：1999-03-15
IPC分类号： C07D295/08 , A61K8/00 , A61K8/40 , A61Q5/10 , C07C211/63 , C07C215/76 , C07C217/84 , C07C229/52 , C07C235/60 , C07C271/28 , C07D295/088 , C07D295/092 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/15 , A61K7/13

48. 发明专利

JP2001524548A 失效
公开(公告)号：JP2001524548A
公开(公告)日：2001-12-04
申请号：JP2000523202
申请日：1998-11-26
IPC分类号： C07D295/08 , A61K31/495 , A61P11/08 , A61P17/00 , A61P25/08 , A61P37/08 , A61P43/00 , C07D295/084 , C07D295/088
摘要： The present invention relates to new pseudopolymorphic forms of 2-Ä2-Ä4-Äbis(4-fluorophenyl)methylÜ-1-piperazinylÜethoxyÜacetic acid dihydrochloride, namely, anhydrous 2-Ä2-Ä4-Äbis(4-fluorophenyl)methylÜ-1-piperazinylÜethoxyÜacetic acid dihydrochloride and 2-Ä2-Ä4-Äbis(4-fluorophenyl)methylÜ-1-piperazinylÜethoxyÜacetic acid dihydrochloride monohydrate. It also relates to processes for the preparation of these pseudopolymorphic forms and to pharmaceutical compositions containing them.

49. 发明专利

JP3088020B2 失效
公开(公告)号：JP3088020B2
公开(公告)日：2000-09-18
申请号：JP51718097
申请日：1996-10-04
IPC分类号： C07D295/08 , A61K31/138 , A61K31/40 , A61P3/04 , A61P3/06 , A61P5/32 , A61P9/00 , A61P9/10 , A61P13/02 , A61P15/00 , A61P15/06 , A61P15/12 , A61P15/18 , A61P17/10 , A61P19/10 , A61P35/00 , A61P43/00 , C07D295/088 , C07D295/092
摘要： PCT No. PCT/IB96/01049 Sec. 371 Date Apr. 28, 1998 Sec. 102(e) Date Apr. 28, 1998 PCT Filed Oct. 4, 1996 PCT Pub. No. WO97/16434 PCT Pub. Date May 9, 1997(-)Cis-6(S)-phenyl-5(R)-[4-(2-pyrrolidin-1-yl ethoxy)phenyl]-5,6,7,8-tetrahydro-naphthalen-2-ol D-tartrate, pharmaceutical compositions comprising this compound, and an advantageous process for preparing the compound.

50. 发明专利

JP3074109B2 失效
公开(公告)号：JP3074109B2
公开(公告)日：2000-08-07
申请号：JP5208594
申请日：1994-03-23
IPC分类号： A61K31/495 , A61P9/10 , A61P25/00 , A61P25/28 , C07D295/08 , C07D295/088 , C07D295/096

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