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1. 发明专利

AU2001294196B2 Nitrogenous five-membered ring compounds 未知
公开(公告)号：AU2001294196B2
公开(公告)日：2005-11-17
申请号：AU2001294196
申请日：2001-10-05
申请人： TANABE SEIYAKU CO LTD
发明人： YASUDA KOSUKE , KAWANAMI SABURO , ARAKAWA KENJI , MORIMOTO HIROSHI , HIKOTA MASATAKA , MATSUMOTO TAKESHI
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61K031/4709 , A61K031/496 , A61P003/10 , C07D403/14 , A61K031/4035 , A61P043/00 , A61K031/437 , A61K031/4545 , C07D413/04 , A61K031/427 , A61K031/5377 , A61K031/426 , A61K031/506 , A61K031/4439 , A61K031/454 , A61K031/4178 , A61K031/423 , A61K031/497 , A61K031/4025 , A61K031/422 , A61K031/501 , A61K031/517 , A61K031/401
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula ÄIÜ : wherein symbols in the formula have the following meanings; A: -CH2- or -S-, B: CH or N, R : H, a lower alkyl group, etc., X: a single bonding arm, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, etc., R : hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R : (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is -CO-, then B is N, or a pharmaceutically acceptable salt thereof.

2. 发明专利

AU2001294197C1 Aliphatic nitrogenous five-membered ring compounds 未知
公开(公告)号：AU2001294197C1
公开(公告)日：2005-05-19
申请号：AU2001294197
申请日：2001-10-05
申请人： TANABE SEIYAKU CO LTD
发明人： ARAKAWA KENJI , MATSUMOTO TAKESHI , HIKOTA MASATAKA , KAWANAMI SABURO , MORIMOTO HIROSHI , YASUDA KOSUKE
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61P003/10 , A61P043/00 , C07D277/82 , C07D277/42 , C07D277/06 , A61K031/4155 , A61K031/41 , A61K031/4035 , A61K031/4365 , A61K031/4725 , A61K031/437 , A61K031/541 , A61K031/55 , A61K031/433 , A61K031/327 , A61K031/4025 , A61K031/454 , A61K031/4709 , A61K031/401 , A61K031/519 , A61K031/498 , A61K031/423 , A61K031/428 , A61K031/5377 , A61K031/497 , A61K031/501 , A61K031/506 , A61K031/4439 , C07D409/12 , C07D495/04 , C07D405/14
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula ÄIÜ : wherein symbols in the formula have the following meanings; A: -CH2- or -S-, B: CH or N, R : H, a lower alkyl group, etc., X: a single bonding arm, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, etc., R : hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R : (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is -CO-, then B is N, or a pharmaceutically acceptable salt thereof.

3. 发明专利

AU2001294197B2 Aliphatic nitrogenous five-membered ring compounds 未知
公开(公告)号：AU2001294197B2
公开(公告)日：2004-09-16
申请号：AU2001294197
申请日：2001-10-05
申请人： TANABE SEIYAKU CO
发明人： ARAKAWA KENJI , MATSUMOTO TAKESHI , HIKOTA MASATAKA , KAWANAMI SABURO , MORIMOTO HIROSHI , YASUDA KOSUKE
IPC分类号： A61P3/10 , A61P43/00 , C07D207/16 , C07D207/40 , C07D207/404 , C07D207/416 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/048 , C07D513/04 , A61P003/10 , A61P043/00 , C07D277/82 , C07D277/42 , C07D277/06 , A61K031/4155 , A61K031/41 , A61K031/4035 , A61K031/4365 , A61K031/4725 , A61K031/437 , A61K031/541 , A61K031/55 , A61K031/433 , A61K031/327 , A61K031/4025 , A61K031/454 , A61K031/4709 , A61K031/401 , A61K031/519 , A61K031/498 , A61K031/423 , A61K031/428 , A61K031/5377 , A61K031/497 , A61K031/501 , A61K031/506 , A61K031/4439 , C07D409/12 , C07D495/04 , C07D405/14
摘要： The present invention is to provide an aliphatic nitrogen-containing 5-membered ring compound represented by the formula ÄIÜ : wherein symbols in the formula have the following meanings; A: -CH2- or -S-, B: CH or N, R : H, a lower alkyl group, etc., X: a single bonding arm, -CO-, -Alk-CO-, -COCH2-, -Alk-O-, -O-CH2-, -SO2-, -S-, -COO-, -CON(R )-, -Alk-CON(R )-, -CON(R )CH2-, -NHCH2-, etc., R : hydrogen atom or a lower alkyl group, Alk: a lower alkylene group, and R : (1) a cyclic group which may be substituted, (2) a substituted amino group, etc., provided that when X is -CO-, then B is N, or a pharmaceutically acceptable salt thereof.

4. 发明申请

US20040266844A1 Antimicrobial and radioprotective compounds 审中-公开
标题翻译：抗菌和放射防护化合物
公开(公告)号：US20040266844A1
公开(公告)日：2004-12-30
申请号：US10481667
申请日：2004-08-26
发明人： Peter Prokofievich Denisenko , Nikolay Sergeevich Sapronov , Alexander Alexandrovich Tarasenko
IPC分类号： A61K031/428 , A61K031/423 , A61K031/4184
CPC分类号： A61K31/357 , A61K31/36 , A61K31/4184 , C07D235/06 , C07D235/08 , C07D263/56 , C07D317/46 , C07D317/52 , Y02A50/401 , Y02A50/409 , Y02A50/411 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/479 , Y02A50/481
摘要： The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising administering an effective amount of a compound of formula I as defined herein, or pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula I. Some of the compounds of formula I are novel and are also described in the present invention, together with pharmaceutical or veterinary compositions containing them.
摘要翻译：本发明涉及治疗和/或预防微生物感染的方法，包括施用有效量的本文定义的式I化合物或其药学上可接受的盐或衍生物，前药，互变异构体和/或异构体。本发明还涉及一种用于保护受试者免受辐射损伤的方法，癌症放射治疗的方法和用作式I化合物的抗微生物剂或放射防护剂。一些式I化合物是新颖的，也描述于本发明以及含有它们的药物或兽用组合物。

5. 发明申请

US20040198768A1 Method for inhibiting 5-lipoxygenase using a benzoxazole derivative or an analogue thereof 失效
标题翻译：使用苯并恶唑衍生物或其类似物抑制5-脂氧合酶的方法
公开(公告)号：US20040198768A1
公开(公告)日：2004-10-07
申请号：US10789725
申请日：2004-02-27
发明人： Hea Young Park Choo , Hyeun Wook Chang , Ju Hee Yoon , Hye Kyung Ju
IPC分类号： A61K031/4745 , A61K031/428 , A61K031/423
CPC分类号： C07D263/58 , A61K31/423 , A61K31/428 , A61K31/4745 , C07D277/64 , C07D277/66 , C07D417/04 , C07D513/04
摘要： Use of a benzoxazole derivative or an analogue thereof inhibits 5-lipoxygenase in a subject.
摘要翻译：苯并恶唑衍生物或其类似物在受试者中的用途抑制5-脂氧合酶。

6. 发明申请

US20040122002A1 Fused pyrrole compounds, pharmaceutical agents containing the same, and the use thereof 失效
标题翻译：熔融吡咯化合物，含有它们的药剂及其用途
公开(公告)号：US20040122002A1
公开(公告)日：2004-06-24
申请号：US10169988
申请日：2002-09-27
发明人： Hans Guenter Striegel , Stefan Laufer , Karola Tollmann , Susanne Tries
IPC分类号： A61K031/542 , A61K031/5383 , A61K031/519 , A61K031/4745 , A61K031/428 , A61K031/423 , A61K031/4184 , A61K031/407
CPC分类号： C07D487/04
摘要： The present invention relates to fused pyrrole compounds of the formula 1. 1 in which at least one of the radicals R1, R2, R3 is 4-sulphur-substituted phenyl. These compounds are in particular pyrrolizines, indolizines and heteroanalogues having selective inhibitory action on isoenzyme-2 of prostaglandin H synthase (COX-2). The invention also relates to pharmaceutical compositions which contain these compounds; and the use of these compounds for the treatment of disorders of the rheumatic type.
摘要翻译：本发明涉及式1的稠合吡咯化合物，其中基团R 1，R 2，R 3中的至少一个是4-硫取代的苯基。这些化合物特别是对前列腺素H合成酶（COX-2）的同工酶-2具有选择性抑制作用的吡咯烷，中氮茚和杂芳族化合物。本发明还涉及含有这些化合物的药物组合物; 以及这些化合物用于治疗风湿性疾病的用途。

7. 发明申请

US20040116488A1 Substituted 3-alkyl and 3-arylalkyl 1H-indol-1-yl acetic acid derivatives as inhibitors of plasminogen activator inhibitor-1 (PAI-1) 失效
标题翻译：取代的3-烷基和3-芳基烷基1H-吲哚-1-基乙酸衍生物作为纤溶酶原激活物抑制剂-1（PAI-1）的抑制剂
公开(公告)号：US20040116488A1
公开(公告)日：2004-06-17
申请号：US10730951
申请日：2003-12-09
申请人： Wyeth
发明人： Lee Dalton Jennings , Scott Lee Kincaid
IPC分类号： A61K031/423 , A61K031/405 , C07D413/02 , C07D49/02 , C07D45/02
CPC分类号： C07D409/06 , C07D209/10
摘要： The invention formula substituted 3-alkyl and 3-arylalkyl 1H indol-1yl acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor (PAI-1) useful for treating fibrinolytic disorders, the compounds having the structure 1 wherein: R1,R2, R3, R4, R5, R6, and R7 are as defined herein or a pharmaceutically acceptable salt or ester form thereof.
摘要翻译：本发明式取代的3-烷基和3-芳基烷基1H-吲哚-1-基乙酸衍生物，其可用作纤维蛋白溶解性疾病的纤溶酶原激活物抑制剂（PAI-1）的抑制剂，具有以下结构的化合物：其中：R1，R2，R3 ，R 4，R 5，R 6和R 7如本文所定义或其药学上可接受的盐或酯形式。

8. 发明申请

US20040106661A1 Broadspecturm 2-amino-benzoxazole sulfonamide hiv protease inhibitors 失效
标题翻译： Broadspecturm 2-氨基 - 苯并唑磺酰胺hiv蛋白酶抑制剂
公开(公告)号：US20040106661A1
公开(公告)日：2004-06-03
申请号：US10474485
申请日：2003-10-09
发明人： Dominique Louis Nestor Ghislain Surleraux , Sandrine Marie Helene Vendeville , Wim Gaston Verschueren , Marie-Pierre T.M.M.G De Bethune , Herman Augustinus De Rock , Abdellah Tahri
IPC分类号： A61K031/423 , C07D263/52
CPC分类号： C07D263/58 , C07D413/12 , C07D417/12 , C07D491/04 , C07D493/04 , C07D513/04
摘要： The present invention concerns the compounds having the formula 1 N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7 cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9null; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is nullC(nullO)null, nullOnullC(nullO)null, nullNR8nullC(nullO)null, nullC1-6alkanediyl-C(nullO)null, nullNR8nullC1-6alkanediyl-C(nullO)null, nullS(nullO)2-, nullOnullS(nullO)2null, nullNR9-S(nullO)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(nullO), carboxyl, aminoC(nullO), mono- or di(C1-4alkyl)aminoC(nullO), C3-7 cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl. It further relates to their use as broadspectrum HIV protease inhibitors, processes for their preparation as well as pharmaceutical compositions and diagnostic kits comprising them. It also concerns combinations thereof with another anti-retroviral agent, and to their use in assays as reference compounds or as reagents.
摘要翻译：本发明涉及具有式N-氧化物，盐，立体异构形式，外消旋混合物，前药，酯和代谢物的化合物，其中R 1和R 8各自为H，任选取代的C 1-6烷基，C 2-6烯基，C 3-7环烷基，芳基，Het 1，Het 2; R1也可以是式（R11aR11b）NC（R10aR10b）CR9-的基团; t为0,1或2; R2是H或C1-6烷基; L是-C（= O） - ， - OC（= O） - ， - NR 8 -C（= O） - ， - C 1-6烷二基-C（= O） - ， - NR 8 -C 1-6烷二基-C O） - ， - S（= O）2 - ， - OS（= O）2 - ， - NR 9 -S（= O） R 3是C 1-6烷基，芳基，C 3-7环烷基，C 3-7环烷基C 1-4烷基或芳基C 1-4烷基; R 4是H，C 1-4烷基OC（= O），羧基，氨基C（= O），单或二（C 1-4烷基）氨基C（= O），C 3-7环烷基，C 2-6烯基，C 2-6炔基或任选取代 C 1-6烷基; R5和R6是H或C1-6烷基。它还涉及它们作为广谱的HIV蛋白酶抑制剂，其制备方法以及药物组合物和包含它们的诊断试剂盒的用途。它还涉及与另一种抗逆转录病毒剂的组合，以及它们在测定中用作参考化合物或作为试剂。

9. 发明申请

US20040058915A1 Compounds containing a bicyclic ring system useful as alpha v beta 3 antagonists 审中-公开
标题翻译：含有双环体系的化合物可用作αvβ3拮抗剂
公开(公告)号：US20040058915A1
公开(公告)日：2004-03-25
申请号：US10363070
申请日：2003-08-18
发明人： Ish Kumar Khanna , Yi Yu , Devadas Balekudra , Hwang-Fun Lu , Nizal S. Chandrakumar
IPC分类号： A61K031/5415 , A61K031/538 , A61K031/517 , A61K031/502 , A61K031/498 , A61K031/47 , A61K031/428 , A61K031/423 , A61K031/4184
CPC分类号： C07D213/73 , C07D213/74 , C07D401/12 , C07D405/12 , C07D413/12 , C07D471/04
摘要： The present invention relates to a class of compounds represented by the Formula I or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising compounds of the Formula I, and methods of selectively inhibiting or antagonizing the nullvnull3 and/or nullvnull5 integrin. The ring A-B, is selected from the group consisting of the formula II all optionally substituted and bonded to X and Z1 at any position. 1
摘要翻译：本发明涉及一类由式I表示的化合物或其药学上可接受的盐，包含式I化合物的药物组合物，以及选择性抑制或拮抗阿尔法博乙和/或阿夫泊亭5整联蛋白的方法。环A-B选自式II，其全部任选地被取代并且与任何位置的X和Z 1键合。

10. 发明申请

US20040029858A1 2-(1h-indol-3-yl)-2-oxo-acetic acid amides with antitumor activity 失效
标题翻译：具有抗肿瘤活性的2-（1H-吲哚-3-基）-2-氧代 - 乙酸酰胺
公开(公告)号：US20040029858A1
公开(公告)日：2004-02-12
申请号：US10333754
申请日：2003-07-10
发明人： Ernesto Menta , Nicoletta Pescalli
IPC分类号： C07D417/02 , C07D413/02 , C07D43/02 , A61K031/55 , A61K031/541 , A61K031/5377 , A61K031/496 , A61K031/454 , A61K031/427 , A61K031/423 , A61K031/4178
CPC分类号： C07D403/12 , C07D413/12 , C07D417/12
摘要： 2-(III-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors. 1
摘要翻译：具有抗肿瘤活性的式（I）的2-（III-吲哚-3-基）-2-氧代 - 乙酰胺衍生物，特别是针对实体瘤，特别是结肠和肺肿瘤。

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