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71. 发明申请

WO00069822A1 HYDROXAMIC AND CARBOXYLIC ACID DERIVATIVES 审中-公开
标题翻译：羟基和羧酸衍生物
公开(公告)号：WO00069822A1
公开(公告)日：2000-11-23
申请号：PCT/GB2000/001804
申请日：2000-05-12
IPC分类号： A61P7/00 , A61P11/00 , A61P29/00 , A61P35/00 , C07D211/96 , C07D221/20 , A61K31/438 , A61K31/445
CPC分类号： C07D221/20 , C07D211/96
摘要： Compounds of the formula (I): B-X-(CH2)m-CR R -(CH2)n-CO-Y, in which X is S(O)1-2, Y is OH or NHOH, and the other variables are as defined in the claims, have therapeutic utility as inhibitors of metalloproteinases, etc.
摘要翻译：式（I）的化合物：其中X是S（O）1-2，Y是OH或NHOH的BX-（CH2）m-CR 1 R 2 - （CH 2）n -CO- ，其他变量如权利要求中所定义，具有作为金属蛋白酶抑制剂等的治疗用途

72. 发明申请

WO0004012A9 COMPOUNDS SPECIFIC FOR THE HUMAN alpha 1d ADRENERGIC RECEPTOR AND USES THEREOF 审中-公开
公开(公告)号：WO0004012A9
公开(公告)日：2000-10-26
申请号：PCT/US9916101
申请日：1999-07-16
申请人： SYNAPTIC PHARMA CORP , KONKEL MICHAEL , WETZEL JOHN M , NOBLE STEWART , GLUCHOWSKI CHARLES , CRAIG DOUGLAS A
发明人： KONKEL MICHAEL , WETZEL JOHN M , NOBLE STEWART , GLUCHOWSKI CHARLES , CRAIG DOUGLAS A
IPC分类号： C07D295/06 , A61K31/00 , A61K31/438 , A61K31/4747 , A61K31/495 , A61K31/496 , A61P9/12 , A61P13/00 , A61P43/00 , C07D221/20 , C07D295/08 , C07D401/06 , A61K31/45 , C07D403/06
CPC分类号： A61K31/495 , A61K31/00 , A61K31/4747 , A61K31/496
摘要： This invention is directed towards a method of inhibiting activation of a human alpha 1d adrenergic receptor which comprises contacting the receptor with a compound so as to inhibit activation of the receptor, wherein the compound binds selectively to a human alpha 1d adrenergic receptor. This invention provides for a compound which binds selectively to a human alpha 1d adrenergic receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier. This invention further provides for a method of treating a subject afflicted with a disease which is susceptible to treatment by antagonism of the human alpha 1d adrenergic receptor which comprises administering to the subject an amount of the above defined compound to treat the disease.

73. 发明申请

WO99052876A1 AZACYCLOALKANE DERIVATIVES, PREPARATION AND THERAPEUTIC APPLICATION 审中-公开
标题翻译：齐克洛尔衍生物，制剂和治疗应用
公开(公告)号：WO99052876A1
公开(公告)日：1999-10-21
申请号：PCT/FR1999/000851
申请日：1999-04-13
IPC分类号： C07D295/18 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/407 , A61K31/435 , A61K31/4365 , A61K31/438 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4525 , A61K31/454 , A61K31/495 , A61K31/5375 , A61K31/54 , A61P3/04 , A61P3/10 , A61P29/00 , C07D207/12 , C07D209/44 , C07D209/52 , C07D209/54 , C07D209/72 , C07D211/16 , C07D211/22 , C07D211/62 , C07D211/76 , C07D221/20 , C07D241/04 , C07D263/04 , C07D295/185 , C07D401/04 , C07D405/04 , C07D405/06 , C07D471/10 , C07D487/04 , C07D491/04 , C07D491/056 , C07D491/10 , C07D491/113 , C07D495/10 , C07D407/04 , A61K31/405
CPC分类号： C07D221/20 , C07D209/44 , C07D209/54 , C07D209/72 , C07D211/76 , C07D263/04 , C07D295/185 , C07D401/04 , C07D491/04 , C07D491/10 , C07D495/10
摘要： The invention concerns azacycloalkane derivatives of general formula (I) wherein: R1 represents a hydrogen atom, hydroxyl, a C1-C4 alkyl, a 1-C4 hydroxyalkyl, a C4-C7 cycloalkyl, a C1-C4 alkyloxy C1-C4alkyl group, an aminocarbonyl group, a benzyl, a heterocycloalkyl or heteroaryl group comprising 4 to 5 carbon atoms and a heteroatom, such as nitrogen, sulphur or oxygen, the heterocycloalkyl or herteroaryl group being optionally substituted by one or two substituents such as a hydroxyl, a C1-C4 alkyl group or a halogen; or R1 and R2 together form a C3-C6 alkylene group, a C2-C3 alkylene dioxy group, a C2-C3 alkylene dithio group, -(O2)S-C2-3 alkylene S(O2)-or a CH2NHC(O)CH2- group, or R2 and R3 together form a propylene or butylene group, a C1-C3 alkylene dioxy group, a carbonyldioxy or a 2-butenylene group; R6 represents an aromatic group selected among the groups: (a); (b); (c); (d) or when R2 and R3 together form a C1-C3 alkylene dioxy or carbonyl dioxy group, a benzyl, or R6 represents a hydrogen, when R5 represents a 1-indanyl group; X represents a carbon, nitrogen, sulphur atom or a sulphonyl group; Y represents an oxygen or sulphur atom. The invention is applicable in therapeutics.
摘要翻译：本发明涉及通式（I）的氮杂环烷烃衍生物，其中：R1表示氢原子，羟基，C1-C4烷基，1-C4羟烷基，C4-C7环烷基，C1-C4烷氧基C1-C4烷基，氨基羰基，苄基，杂环烷基或杂芳基，其包含4至5个碳原子和杂原子如氮，硫或氧，杂环烷基或杂芳基任选被一个或两个取代基取代，例如羟基，C1- C4烷基或卤素; 或者R 1和R 2一起形成C 3 -C 6亚烷基，C 2 -C 3亚烷基二氧基，C 2 -C 3亚烷基二硫基， - （O 2）S-C 2-3亚烷基S（O 2）或CH 2 NHC（O）或R 2和R 3一起形成丙烯或亚丁基，C 1 -C 3亚烷基二氧基，羰基二氧基或2-亚丁烯基; R6表示选自以下组中的芳族基团：（a）; （B）; （C）; （d）或当R 2和R 3一起形成C 1 -C 3亚烷基二氧基或羰基二氧基时，苄基或R 6表示氢，当R 5表示1-二氢化茚基时; X表示碳，氮，硫原子或磺酰基; Y表示氧或硫原子。本发明适用于治疗。

74. 发明申请

WO99040070A1 N-ACYL CYCLIC AMINE DERIVATIVES 审中-公开
标题翻译： N-乙酰环胺衍生物
公开(公告)号：WO99040070A1
公开(公告)日：1999-08-12
申请号：PCT/JP1999/000462
申请日：1999-02-03
IPC分类号： C07D211/26 , C07D211/58 , C07D211/70 , C07D221/20 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10 , A61K31/445 , A61K31/46 , A61K31/55
CPC分类号： C07D221/20 , C07D211/26 , C07D211/58 , C07D211/70 , C07D471/08 , C07D471/10 , C07D487/08 , C07D487/10
摘要： Compounds represented by general formula (I) wherein Ar represents aryl or heteroaryl optionally substituted by halogeno, lower alkyl or lower alkoxy; R represents optionally fluorinated C3-6 cycloalkyl; R and R represent each hydrogen, -(A )m-NH-B, etc.; R and R represent each hydrogen, aliphatic C1-6 hydrocarbyl optionally substituted by lower alkyl, etc.; n is 0 or 1; and X represents oxygen or sulfur. These compounds have selective muscarine M3 receptor antagonism and are excellent in oral activity, duration of action and dynamics in vivo, which makes them useful as safe and efficacious drugs with little side effects for treating respiratory diseases, urologic diseases or digestive diseases.
摘要翻译：由通式（I）表示的化合物，其中Ar表示任选被卤代低级烷基或低级烷氧基取代的芳基或杂芳基; R 1表示任选氟化的C 3-6环烷基; R 2和R 4各自代表氢， - （A 1）m-NH-B等; R 3和R 5各自表示氢，任选被低级烷基取代的脂族C 1-6烃基等; n为0或1; X表示氧或硫。这些化合物具有选择性毒蕈碱M3受体拮抗作用，口服活性，作用时间和体内动力学优异，使其成为安全有效的药物，对治疗呼吸系统疾病，泌尿系统疾病或消化系统疾病具有很小的副作用。

75. 发明申请

WO99015504A1 4-PHENYLTETRAHYDROCHINOLINE UTILIZED AS AN INHIBITOR OF THE CHOLESTEROL ESTER TRANSFER PROTEIN 审中-公开
标题翻译： 4- PHENYLTETRAHYDROCHINOLINE AS CHOLESTEROLESTERTRANSFERPROTEINS抑制剂的
公开(公告)号：WO99015504A1
公开(公告)日：1999-04-01
申请号：PCT/EP1998/005658
申请日：1998-09-07
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/506 , A61P3/06 , A61P9/10 , C07D215/20 , C07D221/20 , C07D401/06 , C07D417/06
CPC分类号： C07D221/20 , C07D215/20 , C07D401/06 , C07D417/06
摘要： According to the invention, the tetrahydrochinoline can be produced in which corresponding substituted tetrahydrochinoline-aldehyde is condensed with suitable substances and afterwards the existing substituents are varied according to usual methods. The tetrahydrochinoline is suited for additives in medicaments, especially in medicaments for treating arteriosclerosis and dyslipidaemia.
摘要翻译：的四氢喹啉可通过与合适的物质冷凝适当取代的四氢喹啉醛来制备，并随后通过常规的方法不同的取代基。适合作为药物在药物用于动脉粥样硬化和治疗血脂异常的活性成分，特别是四氢喹啉。

76. 发明申请

WO98051298A1 ARYLSUBSTITUTED PIPERAZINES USEFUL IN THE TREATEMENT OF BENIGN PROSTATIC HYPERLASIA 审中-公开
标题翻译：用于治疗预防性高血压的ARYLSUTITUTED PIPERAZINES
公开(公告)号：WO98051298A1
公开(公告)日：1998-11-19
申请号：PCT/US1998/009023
申请日：1998-05-08
IPC分类号： C07D295/12 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/402 , A61K31/4025 , A61K31/445 , A61K31/496 , A61K31/55 , A61P13/08 , C07D205/08 , C07D207/12 , C07D207/26 , C07D207/27 , C07D207/28 , C07D209/44 , C07D209/48 , C07D211/40 , C07D211/76 , C07D221/20 , C07D223/10 , C07D225/02 , C07D225/08 , C07D241/04 , C07D295/08 , C07D295/13 , C07D401/12 , C07D403/12 , A61K31/33 , A61K31/395 , A61K31/495
CPC分类号： C07D207/27 , C07D207/28 , C07D209/48 , C07D211/76 , C07D223/10 , C07D295/13
摘要： This invention relates to a series of arylsubstituted piperazines, of Formula (I), pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the alpha -1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this and other disease.
摘要翻译：本发明涉及式（I）的一系列芳基取代哌嗪，含有它们的药物组合物和用于其制备的中间体。本发明的化合物选择性地抑制与α-1肾上腺素能受体的结合，α受体是牵涉到良性前列腺增生的受体。因此，这些化合物在治疗这种和其它疾病中潜在有用。

77. 发明申请

WO98046569A1 BENZENE DERIVATIVES 审中-公开
标题翻译：苯苯衍生物
公开(公告)号：WO98046569A1
公开(公告)日：1998-10-22
申请号：PCT/JP1998/001629
申请日：1998-04-08
IPC分类号： C07D221/20 , C07D211/60 , A61K31/445 , A61K31/495 , C07D401/12 , C07D471/10
CPC分类号： C07D221/20
摘要： Benzene derivatives represented by general formula (1) or pharmaceutically acceptable salts thereof, which are useful as growth hormone liberation promoters, etc. wherein ring A represents an optionally substituted benzene ring, etc.; X represents -CO- or -SO2-; Y represents oxygen or a single bond; R represents a single bond or C1-3 alkylene; R represents a single bond or C1-2 alkylene; R represents hydrogen, optionally hydroxylated alkyl, etc.; and R represents an optionally substituted, saturated nitrogen-containing heterocycle, etc.; or R and R may form together with the nitrogen atom (a), wherein E represents optionally substituted ethylene, optionally substituted vinylene, -CH2NR - or -NR CH2- (wherein R represents hydrogen, lower alkyl, lower alkanoyl or lower alkylsulfonyl); and R represents a substituent.
摘要翻译：通式（1）表示的苯衍生物或其药学上可接受的盐，可用作生长激素释放促进剂等，其中环A表示任选取代的苯环等; X表示-CO-或-SO 2 - ; Y表示氧或单键; R 3表示单键或C 1-3亚烷基; R 4表示单键或C 1-2亚烷基; R 5表示氢，任选羟基化的烷基等; R 6表示任选取代的饱和含氮杂环等; 或R 1和R 2可以与氮原子（a）一起形成，其中E表示任选取代的亚乙基，任选取代的亚乙烯基，-CH 2 NR 9 - 或-NR 9 CH 2 - （其中R' 9>代表氢，低级烷基，低级烷酰基或低级烷基磺酰基）; R 8表示取代基。

78. 发明申请

WO1998000404A1 ANTHRANILIC ACID DIAMIDES DERIVATIVES, THEIR PREPARATION AND PHARMACEUTICAL USE AS ANTI-GASTRIN AGENTS 审中-公开
标题翻译：抗坏血酸衍生物，其制备和药物用作抗胃酸剂
公开(公告)号：WO1998000404A1
公开(公告)日：1998-01-08
申请号：PCT/EP1997003361
申请日：1997-06-26
申请人： ROTTA RESEARCH LABORATORIUM S.P.A. , MAKOVEC, Francesco , PERIS, Walter , ROVATI, Lucio, Claudio , ROVATI, Luigi, Angelo
发明人： ROTTA RESEARCH LABORATORIUM S.P.A.
IPC分类号： C07D221/20
CPC分类号： C07D221/20
摘要： Compounds which can be represented by general formula (I) indicated below, and in which the anthranilic acid aromatic ring may be mono- or di-substituted by the R1 group which can be selected independently from hydrogen, methyl and chloro, and in which the substituents at the chiral centre (marked with an asterik in formula (I)) have the R (Rectus) configuration.
摘要翻译：可以由下述通式（I）表示的化合物，其中邻氨基苯甲酸芳环可以被独立于氢，甲基和氯选择的R 1基团单取代或二取代，并且其中手性中心的取代基（在式（I）中用asterik标记））具有R（直角）构型。

79. 发明申请

WO1995007261A1 POLYAMIDIC ACID DERIVATIVES WITH ANTIGASTRIN ACTIVITY, A METHOD FOR THEIR PREPARATION, AND THEIR PHARMACEUTICAL USE 审中-公开
标题翻译：具有抗丝氨酸活性的聚酰胺酸衍生物，其制备方法及其药物用途
公开(公告)号：WO1995007261A1
公开(公告)日：1995-03-16
申请号：PCT/EP1994002983
申请日：1994-09-07
申请人： ROTTA RESEARCH LABORATORIUM S.P.A. , MAKOVEC, Francesco , PERIS, Walter , ROVATI, Lucio, Claudio , ROVATI, Luigi, Angelo
发明人： ROTTA RESEARCH LABORATORIUM S.P.A.
IPC分类号： C07D221/20
CPC分类号： C07D221/20 , A61K38/00 , C07D209/20 , C07D401/12 , C07D403/12 , C07K5/0215 , C07K5/06139
摘要： New derivatives of glutamic and aspartic acids of formula (I) are described. The compounds are potent receptor antagonists of gastrin at the peripheral level and of cholecystokinin at the level of the central nervous system.
摘要翻译：描述了式（I）的谷氨酸和天冬氨酸的新衍生物。这些化合物是外周水平的胃泌素的有效受体拮抗剂和中枢神经系统水平的胆囊收缩素。

80. 发明申请

WO9314760A3 METHODS 审中-公开
标题翻译：方法
公开(公告)号：WO9314760A3
公开(公告)日：1993-09-02
申请号：PCT/US9300730
申请日：1993-01-27
申请人： SMITHKLINE BEECHAM CORP
发明人： BADGER ALISON MARY
IPC分类号： C07D221/20 , A61K31/40 , A61K31/403 , A61K31/435 , A61K31/445 , A61P31/12 , A61P31/18 , A61P37/04 , C07D209/54 , A61K31/55 , A61K31/455
CPC分类号： A61K31/445 , A61K31/40
摘要： Invented is a method of preventing or delaying the occurrence of acquired immunodeficiency syndrome (AIDS) in human immunodeficiency virus (HIV) seropositive humans which comprises administering to such human an effective therefor amount of a substituted azaspirane.

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