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91. 发明申请

US20040110824A1 2-Phenyl-1-[4(2-aminoethoxy)-benzyl]-indoles as estrogenic agents 有权
标题翻译： 2-苯基-1- [4（2-氨基乙氧基） - 苄基] - 吲哚作为雌激素剂
公开(公告)号：US20040110824A1
公开(公告)日：2004-06-10
申请号：US10720504
申请日：2003-11-24
申请人： Wyeth
发明人： Chris P. Miller , Michael D. Collini , Bach D. Tran , Arthur A. Santilli
IPC分类号： A61K031/405 , C07D209/16
CPC分类号： C07D403/12 , A61K31/404 , A61K31/405 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/55 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/30 , C07D209/42 , C07D405/04 , C07D405/12
摘要： The present invention relates to new 2-Phenyl-1-null4-(2-Aminoethoxy)-Benzylnull-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below: 1
摘要翻译：本发明涉及可用作雌激素剂的新的2-苯基-1- [4-（2-氨基乙氧基） - 苄基] - 吲哚化合物，以及使用这些化合物的药物组合物和治疗方法，其具有一般性结构如下：

92. 发明申请

US20040063724A1 2,7-Substituted indoles 失效
标题翻译： 2,7-取代的吲哚
公开(公告)号：US20040063724A1
公开(公告)日：2004-04-01
申请号：US10663314
申请日：2003-09-16
申请人： Roche Palo Alto LLC
发明人： Ann Marie Madera , Robert James Weikert
IPC分类号： A61K031/496 , A61K031/454 , C07D43/02
CPC分类号： C07D401/04 , C07D209/30
摘要： The present invention provides a compound of the formula: 1 a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, and n are those defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.
摘要翻译：本发明提供下式的化合物：其药学上可接受的盐或前药，其中R 1，R 2，R 3，R 4和n是本文定义的那些。本发明还提供了包含式I化合物的使用方法和方法的组合物。

93. 发明授权

US06673787B2 Sulfonamide-containing indole compounds 有权
标题翻译：含磺酰胺的吲哚化合物
公开(公告)号：US06673787B2
公开(公告)日：2004-01-06
申请号：US10098420
申请日：2002-03-18
申请人： Toru Haneda , Akihiko Tsuruoka , Junichi Kamata , Tadashi Okabe , Keiko Takahashi , Kazumasa Nara , Shinichi Hamaoka , Norihiro Ueda , Takashi Owa , Toshiaki Wakabayashi , Yasuhiro Funahashi , Taro Semba , Naoko Hata , Yuji Yamamoto , Yoichi Ozawa , Noako Tsukahara
发明人： Toru Haneda , Akihiko Tsuruoka , Junichi Kamata , Tadashi Okabe , Keiko Takahashi , Kazumasa Nara , Shinichi Hamaoka , Norihiro Ueda , Takashi Owa , Toshiaki Wakabayashi , Yasuhiro Funahashi , Taro Semba , Naoko Hata , Yuji Yamamoto , Yoichi Ozawa , Noako Tsukahara
IPC分类号： A61K3133
CPC分类号： C07D401/12 , C07D209/04 , C07D209/30 , C07D209/42 , C07D403/12 , C07D409/12
摘要： The present invention creates a novel antiangiogenic agent and provides an antitumor agent which shows high safety as compared with conventional antitumor agents, has a sure effect and is able to be administered for a long period. That is, it provides an indole compound represented by the following formula (I), its pharmacologically acceptable salt or hydrates thereof. In the formula, R1 represents hydrogen atom, a halogen atom or cyano group; R2 and R3 are the same as or different from and each represents hydrogen atom, a C1-C4 lower alkyl group or a halogen atom; R4 represents hydrogen atom or a C1-C4 lower alkyl group; and the ring A represents cyanophenyl group, aminosulfonylphenyl group, aminopyridyl group, aminopyrimidyl group, a halopyridyl group or cyanothiophenyl group, provided that the case where all of R1, R2 and R3 are hydrogen atoms, where both R2 and R3 are hydrogen atoms or where the ring A is aminosulfonyl group and both R1 and R2 are halogen atoms is excluded. Further, when the ring A is cyanophenyl group, 2-amino-5-pyridyl group or a 2-halo-5-pyridyl group and R1 is cyano group or a halogen atom, at least one of R2 and R3 should not be a hydrogen atom.
摘要翻译：本发明创造出一种新型抗血管生成剂，并提供与常规抗肿瘤剂相比显示出高安全性的抗肿瘤剂，具有确定的作用并且能够长时间施用。也就是说，其提供由下式（I）表示的吲哚化合物，其药理学上可接受的盐或其水合物。在式中，R 1表示氢原子，卤素原子或氰基; R 2和R 3各自表示氢原子，C 1 -C 4低级烷基或卤素原子; R 4表示氢原子或C 1 -C 4低级烷基; 并且环A表示氰基苯基，氨基磺酰基苯基，氨基吡啶基，氨基嘧啶基，卤代吡啶基或氰基噻吩基，条件是所有R 1，R 2和R 3均为氢原子的情况，其中 R 2和R 3都是氢原子，或者其中环A是氨基磺酰基并且R 1和R 2都是卤素原子。此外，当环A为氰基苯基，2-氨基-5-吡啶基或2-卤代-5-吡啶基，R 1为氰基或卤素原子时，R 2和 R 3不应该是氢原子。

94. 发明申请

US20030225109A1 Thio-oxindole derivatives 失效
标题翻译：硫氧吲哚衍生物
公开(公告)号：US20030225109A1
公开(公告)日：2003-12-04
申请号：US10420276
申请日：2003-04-22
申请人： Wyeth , Ligand Pharmaceuticals, Inc.
发明人： Andrew Fensome , Puwen Zhang , Marci C. Koko , Jay E. Wrobel , Edward G. Melenski , Lin Zhi , Todd K. Jones , Christopher M. Tegley , James P. Edwards
IPC分类号： A61K031/506 , A61K031/4439 , A61K031/405 , C07D43/02 , C07D47/02
CPC分类号： C07D209/40 , C07D209/08 , C07D209/30
摘要： This invention relates to compounds which are agonists of the progesterone receptor which have the general structure: 1 wherein: p1 R1, R2, R3, R4, R5 and Q1 are as defined herein, or a pharmaceutically acceptable salt thereof, as well as methods of using these compounds to induce contraception or treat progesterone-related carcinomas and adenocarcinomas.
摘要翻译：本发明涉及作为孕酮受体的激动剂的具有以下通式结构的化合物：其中：p1 R1，R2，R3，R4，R5和Q 1如本文所定义，或其药学上可接受的盐，以及使用这些化合物诱导避孕或治疗孕激素相关性癌和腺癌的方法。

95. 发明申请

US20030195244A1 Indole compounds 有权
公开(公告)号：US20030195244A1
公开(公告)日：2003-10-16
申请号：US10318337
申请日：2002-12-12
发明人： Hsing-Pang Hsieh , Jing-Ping Liou , Jang-Yang Chang , Chun-Wei Chang
IPC分类号： A61K031/405 , C07D209/56
CPC分类号： A61K31/405 , C07D209/08 , C07D209/12 , C07D209/14 , C07D209/30 , C07D401/06 , C07D405/06 , C07D491/04
摘要： Indole compounds of the formula: 1 wherein L1 is CO; L2 is a bond; R1 is aryl or heteroaryl; R2 is H, aryl, heteroaryl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRRnull, SO2R, SO3R, SO2NRRnull, SR, NRRnull, NRSO2NRnullRnull, NRSO2Rnull, NRSO3Rnull, NRC(O)Rnull, NRC(O)NRnullRnull, NRC(O)ORnull, NRC(N)NRnullRnull, C(O)OR, or C(O)NRRnull; each of Ra, Rb, Rc, and Rd, independently, is R, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRRnull, SO2R, SO3R, SO2NRRnull, SR, NRRnull, NRSO2NRnullRnull, NRSO2Rnull, NRSO3Rnull, NRC(O)Rnull, NRC(O)NRnullRnull, NRC(O)ORnull, NRC(N)NRnullRnull, C(O)R, C(O)OR, C(O)NRRnull, or Rb and Rc, Ra and Rb, or Rc and Rd taken together are O(CH2)nO; and Rc is H, alkyl, alkenyl, alkynyl, cyclyl, heterocyclyl, halogen, nitro, nitroso, cyano, azide, isothionitro, OR, OC(O)R, OC(O)OR, OC(O)NRRnull, SO2R, SO3R, SO2NRRnull, SR, NRRnull, NRSO2NRnullRnull, NRSO2Rnull, NRSO3Rnull, NRC(O)Rnull, NRC(O)NRnullRnull, NRC(O)ORnull, NRC(N)NRnullRnull, C(O)R, C(O)OR, or C(O)NRRnull; in which each of R, Rnull, and Rnull, independently, is H, alkyl, alkenyl, alkynyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and n is 1, 2, 3, 4, or 5.

96. 发明申请

US20030171591A1 Process for producing optically active sulfoxide derivative 有权
标题翻译：光学活性亚砜衍生物的制备方法
公开(公告)号：US20030171591A1
公开(公告)日：2003-09-11
申请号：US10276109
申请日：2002-10-24
发明人： Hideo Hashimoto , Tadashi Urai
IPC分类号： C07D43/02 , C07D235/28
CPC分类号： C07D401/12 , A61K31/4439 , C07D209/30 , C07D235/28 , C07D277/74 , C07D277/76 , C07D417/12
摘要： The present invention relates to a production method of an optically active form of a compound represented by formula (II) 1 wherein ring A is a benzene ring optionally having substituent(s); R1 is H, a hydrocarbon group optionally having substituent(s), an acyl group or an acyloxy group; R2, R3 and R4 are each H, an alkyl group optionally having substituent(s), an alkoxy group optionally having substituent(s) or an amino group optionally having substituent(s); X is N or CH; Y is N or CH; and * shows an asymmetric center, or a salt thereof, which includes reacting a compound represented by the formula (I) 2 wherein each symbol is as defined above, or a salt thereof, with an excess amount of an oxidizing agent in the presence of a catalyst for asymmetric induction, and provides an efficient production method of an optically active sulfoxide derivative in high yield on an industrial large scale by a convenient method, while achieving an extremely high enantiomer excess.
摘要翻译：本发明涉及式（II）表示的化合物的光学活性形式的制备方法，其中环A是任选具有取代基的苯环; R 1是H，任选具有取代基的烃基，酰基或酰氧基; R 2，R 3和R 4各自为H，任选具有取代基的烷基，任选具有取代基的烷氧基或任选具有取代基的氨基; X为N或CH; Y为N或CH; 和*表示不对称中心或其盐，其包括使式（I）表示的化合物或其盐，其中每个符号如上定义，或其盐与过量的氧化剂在用于不对称诱导的催化剂，并且通过方便的方法在工业上大规模提供高产率的光学活性亚砜衍生物的有效制备方法，同时实现极高的对映体过量。

97. 发明申请

US20030078431A1 Antithrombotic agents 审中-公开
公开(公告)号：US20030078431A1
公开(公告)日：2003-04-24
申请号：US10082429
申请日：2002-02-22
发明人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson JR. , Steven Edward Hall , David Kent Herron , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
IPC分类号： C07D213/55 , C07C069/76 , C07D215/00
CPC分类号： C07D401/14 , C07D209/08 , C07D209/30 , C07D231/56 , C07D235/06 , C07D401/12 , C07D403/12 , C07D409/12
摘要： This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

98. 发明授权

US06500851B2 Antithrombotic agents 失效
公开(公告)号：US06500851B2
公开(公告)日：2002-12-31
申请号：US10082453
申请日：2002-02-22
申请人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
发明人： Douglas Wade Beight , Trelia Joyce Craft , Jeffry Bernard Franciskovich , Theodore Goodson, Jr. , Steven Edward Hall , David Kent Herron , Valentine Joseph Klimkowski , Jeffrey Alan Kyle , John Joseph Masters , David Mendel , Guy Milot , Jason Scott Sawyer , Robert Theodore Shuman , Gerald Floyd Smith , Anne Louise Tebbe , Jennifer Marie Tinsley , Leonard Crayton Weir , James Howard Wikel , Michael Robert Wiley , Ying Kwong Yee
IPC分类号： A61K31416
CPC分类号： C07D401/14 , C07D209/08 , C07D209/30 , C07D231/56 , C07D235/06 , C07D401/12 , C07D403/12 , C07D409/12
摘要： This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

99. 发明申请

US20020052378A1 Novel compounds and compositions as protease inhibitors 失效
标题翻译：新型化合物和组合物作为蛋白酶抑制剂
公开(公告)号：US20020052378A1
公开(公告)日：2002-05-02
申请号：US09754962
申请日：2001-01-05
发明人： Renata Marcella Oballa , Petpiboon Prasit , Joel Stephane Robichaud , Elise Isabel , Eduardo Setti , Dan-Xiong Wang , Rohan V. Mendonca , Shankar Venkatraman
IPC分类号： A61K031/66 , A61K031/535 , A61K031/497 , A61K031/44 , A61K031/47 , A61K031/445 , A61K031/425 , A61K031/40
CPC分类号： C07D207/08 , C07C255/25 , C07C255/41 , C07C2601/04 , C07C2601/14 , C07C2602/02 , C07D207/14 , C07D209/16 , C07D209/30 , C07D211/34 , C07D213/56 , C07D213/61 , C07D215/12 , C07D239/42 , C07D263/22 , C07D277/36 , C07D277/40 , C07D277/42 , C07D277/48 , C07D277/58 , C07D277/68 , C07D295/155 , C07D319/18 , C07D333/34 , C07D417/04 , C07D471/04
摘要： The present invention relates to novel cysteine protease inhibitors of Formula I: 1 the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.
摘要翻译：本发明涉及式I的新型半胱氨酸蛋白酶抑制剂：其药学上可接受的盐和N-氧化物衍生物，它们作为治疗剂的用途及其制备方法。

100. 发明授权

US06291451B1 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents 有权
标题翻译： 2-苯基-1- [4-（2-氨基乙氧基） - 苄基] - 吲哚作为雌激素剂
公开(公告)号：US06291451B1
公开(公告)日：2001-09-18
申请号：US09779048
申请日：2001-02-08
申请人： Chris P. Miller , Michael D. Collini , Bach D. Tran , Arthur A. Santilli
发明人： Chris P. Miller , Michael D. Collini , Bach D. Tran , Arthur A. Santilli
IPC分类号： A61K3140
CPC分类号： C07D403/12 , A61K31/404 , A61K31/405 , A61K31/4523 , A61K31/454 , A61K31/496 , A61K31/55 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/30 , C07D209/42 , C07D405/04 , C07D405/12
摘要： The present invention relates to new 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds having the general structures below: which are useful in the treatment or inhibition of breast cancer.
摘要翻译：本发明涉及具有以下一般结构的新的2-苯基-1- [4-（2-氨基乙氧基） - 苄基] - 吲哚类化合物：其可用于治疗或抑制乳腺癌。

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