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61. 发明申请

WO0059497A8 PYRROLIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY 审中-公开
标题翻译：氯霉素受体活性的吡咯烷酮调节剂
公开(公告)号：WO0059497A8
公开(公告)日：2001-02-15
申请号：PCT/US0009059
申请日：2000-04-05
申请人： MERCK & CO INC , BERK SCOTT , CALDWELL CHARLES , CHAPMAN KEVIN , HALE JEFFREY , LYNCH CHRISTOPHER , MACCOSS MALCOLM , MILLS SANDER G , WILLOUGHBY CHRISTOPHER
发明人： BERK SCOTT , CALDWELL CHARLES , CHAPMAN KEVIN , HALE JEFFREY , LYNCH CHRISTOPHER , MACCOSS MALCOLM , MILLS SANDER G , WILLOUGHBY CHRISTOPHER
IPC分类号： A61P9/10 , A61P31/18 , A61P37/06 , A61P37/08 , C07C259/06 , C07D401/06 , C07D401/14 , C07D405/14 , A61K31/165 , A61K31/215 , A61K31/24 , A61K31/40 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/433 , A61K31/435 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/445 , A61K31/4523 , A61K31/454 , A61K31/47 , A61K31/4709 , A61K31/4725 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/501 , A61K31/535 , A61K31/5355 , C07C233/59 , C07C233/60 , C07C233/61 , C07C233/63 , C07C233/64 , C07C233/66 , C07C233/68 , C07C233/70 , C07C233/77 , C07C235/02 , C07C235/26 , C07C235/30 , C07C235/32 , C07C235/36 , C07C235/38 , C07C235/42 , C07C235/70 , C07D207/04 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/04 , C07D211/06 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/34 , C07D211/38 , C07D211/40 , C07D211/44 , C07D211/60 , C07D211/62 , C07D211/68 , C07D211/70 , C07D211/72 , C07D211/74 , C07D213/04 , C07D213/06 , C07D213/24 , C07D213/28 , C07D213/30 , C07D213/36 , C07D213/44 , C07D213/46 , C07D213/55 , C07D213/56 , C07D215/02 , C07D215/04 , C07D239/24 , C07D239/26 , C07D241/04 , C07D241/10 , C07D241/12 , C07D241/36 , C07D241/38 , C07D241/40 , C07D243/02 , C07D243/08 , C07D295/04 , C07D403/06 , A61K42/427
CPC分类号： C07D401/06 , C07C259/06 , C07C2601/02 , C07C2601/04 , C07D401/14 , C07D405/14
摘要： The present invention is directed to pyrrolidine compounds of formula (I) wherein R , R , R , R , R , R and n are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-5 and/or CCR-3.
摘要翻译：本发明涉及式（I）的吡咯烷化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和n如本文所定义），其中可用作趋化因子受体活性的调节剂。特别地，这些化合物可用作趋化因子受体CCR-5和/或CCR-3的调节剂。

62. 发明申请

WO00027819A2 ANTRHRANILIC ACID AMIDES AND THE USE THEREOF AS MEDICAMENTS 审中-公开
标题翻译：邻氨基及其作为药物
公开(公告)号：WO00027819A2
公开(公告)日：2000-05-18
申请号：PCT/EP1999/008478
申请日：1999-11-09
IPC分类号： C07D213/36 , A61K31/166 , A61K31/403 , A61K31/404 , A61K31/4409 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4709 , A61K31/4725 , A61K31/506 , A61K31/517 , A61K31/536 , A61P1/16 , A61P3/10 , A61P9/10 , A61P9/14 , A61P13/12 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/06 , A61P35/00 , A61P43/00 , C07C237/30 , C07C237/32 , C07D209/04 , C07D213/40 , C07D213/75 , C07D265/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D213/38 , C07D213/61
CPC分类号： C07C237/32
摘要： The invention relates to anthranilic acid amides and the use thereof as medicaments for the treatment of diseases that are triggered by persistent angiogenesis, in addition to intermediate products in the production of anthranilic acid amides.
摘要翻译：有邻氨基苯甲酸酰胺以及它们作为药物用于由持续的血管生成以及它们的中间产品的邻氨基苯甲酸酰胺的制备引发的疾病的治疗中的用途。

63. 发明申请

WO00014086A1 CHEMOKINE RECEPTOR ANTAGONISTS AND METHODS OF USE THEREFOR 审中-公开
标题翻译：化疗受体拮抗剂及其使用方法
公开(公告)号：WO00014086A1
公开(公告)日：2000-03-16
申请号：PCT/US1999/001365
申请日：1999-01-21
IPC分类号： C07D491/107 , A61K31/4406 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5355 , A61K31/537 , A61K31/5377 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/28 , A61P29/00 , A61P31/18 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/36 , C07D213/38 , C07D401/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/10 , C07D491/10 , C07D495/10 , C07D498/10 , A61K31/44
CPC分类号： C07D401/06 , C07D213/38 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/10 , C07D491/10 , C07D495/10
摘要： Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by structural formula (A) and physiologically acceptable salts thereof.
摘要翻译：公开了新型化合物和治疗与异常白细胞募集和/或激活相关的疾病的方法。该方法包括向有需要的受试者施用有效量的由结构式（A）表示的化合物及其生理学上可接受的盐。

64. 发明申请

WO00007591A1 INDOLE sPLA2 INHIBITORS 审中-公开
标题翻译： INDOLE sPLA2抑制剂
公开(公告)号：WO00007591A1
公开(公告)日：2000-02-17
申请号：PCT/US1999/017460
申请日：1999-08-02
IPC分类号： A61K31/405 , A61K31/403 , A61K31/404 , A61P1/18 , A61P7/00 , A61P9/10 , A61P11/00 , A61P19/02 , A61P19/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/08 , A61P43/00 , C07D209/18 , C07D209/22 , C07D231/12 , C07D233/54 , C07D233/56 , C07D233/58 , C07D249/08 , A61K31/335 , A61K31/38 , A61K31/395 , A61K31/40 , A61K31/41 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/435 , A61K31/44 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/505 , A61K31/535 , C07D205/02 , C07D209/04 , C07D209/12 , C07D209/14 , C07D209/82 , C07D211/26 , C07D211/30 , C07D211/86 , C07D213/36 , C07D213/50 , C07D213/56 , C07D215/12 , C07D219/12 , C07D231/54 , C07D231/56 , C07D237/30 , C07D239/26 , C07D241/04 , C07D241/42 , C07D249/04 , C07D251/22 , C07D261/08 , C07D263/32 , C07D275/02 , C07D277/02 , C07D285/04 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D317/26 , C07D317/28 , C07D319/12 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14
CPC分类号： C07D209/18 , C07D209/22
摘要： A class of novel acylsulfonamide substituted indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock.
摘要翻译：公开了一类新的酰基磺酰胺取代的吲哚化合物以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎症性疾病如败血性休克的用途。

65. 发明申请

WO99032447A3 2,4,6-TRISUBSTITUTED PYRIDINES WITH ESTROGENIC ACTIVITY AND METHODS FOR THE SOLID PHASE SYNTHESIS THEREOF 审中-公开
标题翻译：具有雌激素活性的2,4,6-三唑并吡啶及其固相合成方法
公开(公告)号：WO99032447A3
公开(公告)日：1999-10-14
申请号：PCT/US1998/026363
申请日：1998-12-10
IPC分类号： C07D213/30 , C07D213/36 , C07D405/04 , C07D409/14 , A61K31/44
CPC分类号： C07D213/30 , C07D213/36 , C07D405/04 , C07D409/14
摘要： The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z is selected from the group: n is an integer of a 1 or 2; R is straight chain alkyl of 1 to 6 carbon atoms, branched chain alkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl, or phenyl substituted with fluoro, chloro, bromo, straight chain alkyl of 1 to 6 carbon atoms, branched chain alkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, phenyl, alkoxy of 1 to 6 carbon atoms, or methylenedioxy; and R is furanyl, pyridyl, thieny, naphthalenyl, phenyl, or phenyl substituted with fluoro, chloro, bromo, straight chain alkyl of 1 to 6 carbon atoms, branched chain alkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkoxy of 1 to 6 carbon atoms, or methylenedioxy, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
摘要翻译：本发明涉及式（I）的新的取代的吡啶化合物，其中Z部分选自：n是1或2的整数; R 1是1至6个碳原子的直链烷基，3至7个碳原子的支链烷基，3至7个碳原子的环烷基，苯基或被氟取代的苯基，氯，溴，直链烷基1 3-6个碳原子的支链烷基，3至7个碳原子的环烷基，苯基，1至6个碳原子的烷氧基或亚甲二氧基; R 2为呋喃基，吡啶基，噻吩基，萘基，苯基或被氟，氯，溴，1〜6个碳原子的直链烷基，3〜7个碳原子的支链烷基取代的苯基，3〜具有1至6个碳原子的烷氧基，具有雌激素活性的亚甲二氧基，其制备方法，组合文库和用于制备化合物文库的固相方法，利用化合物的文库用于药物发现，涉及治疗方法及其药物组合物。

66. 发明申请

WO99042446A1 CYCLIC AMIDE COMPOUNDS 审中-公开
标题翻译：环状化合物
公开(公告)号：WO99042446A1
公开(公告)日：1999-08-26
申请号：PCT/JP1999/000659
申请日：1999-02-16
IPC分类号： A61K31/45 , A61K31/496 , A61P37/08 , C07D211/26 , C07D211/34 , C07D211/58 , C07D213/36 , C07D213/38 , C07D213/70 , C07D295/185 , C07D295/192 , C07D401/06 , C07D401/14 , A61K31/445 , A61K31/495 , A61K31/55 , C07D243/08
CPC分类号： C07D213/70 , C07C2601/14 , C07D211/26 , C07D211/34 , C07D211/58 , C07D213/38 , C07D213/82 , C07D295/185 , C07D295/192 , C07D401/14
摘要： Compounds represented by general formula (1) and drugs containing the same, wherein A represents an optionally substituted aromatic compound, etc.; B represents nitrogen or CH; X represents optionally substituted lower alkylene, etc.; Y represents a single bond; Z represents an optionally substituted divalent residue of benzene, etc.; and m and n are each an integer of 1 to 4. Because of having an excellent IgE antibody production inhibitory effect, these compounds are useful as antiallergic agents, etc.
摘要翻译：由通式（1）表示的化合物和含有该化合物的药物，其中A表示任选取代的芳族化合物等。 B表示氮或CH; X表示任选取代的低级亚烷基等; Y表示单键; Z表示任意取代的苯等二价残基等。 m和n各自为1〜4的整数。由于具有优异的IgE抗体产生抑制作用，这些化合物可用作抗过敏剂等。

67. 发明申请

WO99032463A1 INHIBITION OF p38 KINASE USING SYMMETRICAL AND UNSYMMETRICAL DIPHENYL UREAS 审中-公开
标题翻译：使用对称和非对称性二苯醚的p38激酶的抑制
公开(公告)号：WO99032463A1
公开(公告)日：1999-07-01
申请号：PCT/US1998/027265
申请日：1998-12-22
IPC分类号： C07D295/18 , A61K31/17 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/403 , A61K31/4035 , A61K31/4166 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/535 , A61K31/5375 , A61P29/00 , A61P43/00 , C07C205/11 , C07C205/22 , C07C205/37 , C07C205/38 , C07C205/57 , C07C205/58 , C07C275/30 , C07C275/32 , C07C275/34 , C07C275/36 , C07C275/40 , C07C275/42 , C07C309/88 , C07C311/48 , C07C317/42 , C07C323/44 , C07C335/18 , C07D207/26 , C07D207/27 , C07D207/40 , C07D207/404 , C07D209/76 , C07D209/86 , C07D209/88 , C07D213/36 , C07D213/40 , C07D213/53 , C07D213/68 , C07D213/70 , C07D231/08 , C07D233/22 , C07D233/34 , C07D233/70 , C07D263/58 , C07D273/00 , C07D275/00 , C07D277/68 , C07D295/185 , C07D307/20 , C07D333/20 , C07D409/12
CPC分类号： C07D207/27 , A61K31/17 , A61K31/40 , A61K31/403 , A61K31/4035 , A61K31/425 , A61K31/428 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4436 , A61K31/4439 , A61K31/535 , A61K31/5375 , C07C205/11 , C07C205/22 , C07C205/37 , C07C205/38 , C07C205/57 , C07C205/58 , C07C275/30 , C07C275/34 , C07C275/36 , C07C275/40 , C07C275/42 , C07C309/88 , C07C311/48 , C07C317/42 , C07D207/26 , C07D207/404 , C07D209/76 , C07D209/86 , C07D209/88 , C07D213/40 , C07D213/53 , C07D213/68 , C07D213/70 , C07D231/08 , C07D233/22 , C07D233/70 , C07D263/58 , C07D277/68 , C07D295/185 , C07D307/20 , C07D333/20 , C07D409/12 , Y02A50/411
摘要： This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.
摘要翻译：本发明涉及一组芳基脲在治疗细胞因子介导的疾病和蛋白水解酶介导的疾病中的用途，以及用于这种治疗的药物组合物。

68. 发明申请

WO9932447A2 2,4,6-TRISUBSTITUTED PYRIDINES WITH ESTROGENIC ACTIVITY AND METHODS FOR THE SOLID PHASE SYNTHESIS THEREOF 审中-公开
标题翻译：具有雌激素活性的2,4,6-三唑衍生物及其固相合成方法
公开(公告)号：WO9932447A2
公开(公告)日：1999-07-01
申请号：PCT/US9826363
申请日：1998-12-10
申请人： AMERICAN HOME PROD
发明人： CHIU CHINGFAN , TANG ZHILIAN , ELLINGBOE JOHN WATSON
IPC分类号： C07D213/30 , C07D213/36 , C07D405/04 , C07D409/14 , C07D213/00
CPC分类号： C07D213/30 , C07D213/36 , C07D405/04 , C07D409/14
摘要： The present invention relates to novel substituted pyridine compounds of Formula (I) wherein the moiety Z, R , R and R are as herein defined, having estrogenic activity, to processes for their preparation, to a combinatorial library and solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, to methods of treatment and to pharmaceutical compositions thereof.
摘要翻译：本发明涉及式（I）的新的取代的吡啶化合物，其中Z，R 1，R 2和R 3的部分如本文所定义，具有雌激素活性，其制备方法，用于制备化合物文库的组合文库和固相方法，利用用于药物发现的化合物的文库，治疗方法及其药物组合物。

69. 发明申请

WO9214696A3 SUBSTITUTED (ALPHA)-AMINOALDEHYDES AND DERIVATIVES 审中-公开
标题翻译：取代（ALPHA） - 胺衍生物和衍生物
公开(公告)号：WO9214696A3
公开(公告)日：1993-02-18
申请号：PCT/US9201077
申请日：1992-02-21
申请人： DU PONT MERCK PHARMA
发明人： HODGE CARL NICHOLAS
IPC分类号： A61K31/16 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/215 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/415 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61K31/66 , A61K38/00 , C07C237/22 , C07C237/42 , C07C243/32 , C07C245/02 , C07C271/22 , C07C307/04 , C07C311/01 , C07C311/54 , C07C317/48 , C07C323/23 , C07C327/48 , C07C335/16 , C07D207/335 , C07D209/20 , C07D211/14 , C07D213/30 , C07D213/36 , C07D213/40 , C07D213/56 , C07D213/58 , C07D215/38 , C07D231/12 , C07D233/54 , C07D233/64 , C07D239/42 , C07D239/80 , C07D257/04 , C07D277/20 , C07D277/56 , C07D295/08 , C07D307/66 , C07D311/08 , C07D317/46 , C07D333/22 , C07D401/12 , C07F9/09 , C07K5/06 , C07K5/065 , C07K14/81 , A61K31/195 , A61K31/27 , C07C323/25
CPC分类号： C07D213/56 , A61K38/00 , C07C237/22 , C07C271/22 , C07C2601/02 , C07C2601/04 , C07K5/06078
摘要： This invention relates to substituted α-aminoaldehydes, pharmaceutical compositions containing them and methods for using such compounds as antiviral agents.

70. 发明申请

WO9110645A3 CHELANTS 审中-公开
标题翻译：螯合剂
公开(公告)号：WO9110645A3
公开(公告)日：1991-12-26
申请号：PCT/EP9100126
申请日：1991-01-18
申请人： COCKBAIN JULIAN R M , SALUTAR INC
发明人： CARVALHO JOAN F , CROFTS SHAUN P , ROCKLAGE SCOTT M
IPC分类号： A61K51/00 , A61K20060101 , A61K49/00 , A61K49/04 , A61K49/06 , A61K49/22 , A61K51/04 , C07C39/06 , C07C43/04 , C07C211/14 , C07C211/15 , C07C259/04 , C07C323/16 , C07D213/00 , C07D213/74 , C07D267/00 , C07D471/00 , C07D471/06 , C07D471/08 , C07D471/16 , C07D471/18 , C07D471/22 , C07D487/08 , C07D487/18 , C07D487/22 , C07F3/04 , C07F5/00 , C07F13/00 , C09K3/00 , C07D213/36
CPC分类号： B82Y5/00 , A61K49/0002 , A61K49/04 , A61K49/06 , A61K49/228 , A61K51/0482 , A61K2121/00 , A61K2123/00 , C07D213/74 , C07D471/08
摘要： There are provided novel chelating agents useful in the preparation of contrast media for diagnostic imaging or of radiotherapeutic or detoxification compositions.

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