专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US06255339B1 Tetrahydronaphthofuranone derivatives and process for producing the same 失效
标题翻译：四氢萘并呋喃酮衍生物及其制备方法
公开(公告)号：US06255339B1
公开(公告)日：2001-07-03
申请号：US09117070
申请日：1998-07-21
申请人： Kenichi Kurihara , Rie Shinei , Kiyoshi Tanabe , Yasuo Yamamoto , Keiichi Ajito , Kaori Miyajima , Yuji Tabata , Shohei Yasuda , Kuniaki Tatsuta , Tsuneo Okonogi
发明人： Kenichi Kurihara , Rie Shinei , Kiyoshi Tanabe , Yasuo Yamamoto , Keiichi Ajito , Kaori Miyajima , Yuji Tabata , Shohei Yasuda , Kuniaki Tatsuta , Tsuneo Okonogi
IPC分类号： A61K3134
CPC分类号： C07D307/92 , C07D407/12 , C07D407/14 , C07D409/12 , C07D417/12
摘要： Compounds represented by the following formula (I) and pharmaceutically acceptable salts thereof are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as abortifacients, oral contraceptive pills, carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for endometriosis, meningioma, and myeloma, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. wherein R1 and R2 represent a hydroxyl group, alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, alkoxyalkyloxy, cycloalkyloxy containig one oxygen atom, aralkyloxy, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, cycloalkylcarbonyloxy, alkoxycarbonyloxy, aryloxy carbonyloxy, aralkylcarbonyloxy, aromatic acyloxy, heteroaromatic acyloxy, saturated heterocyclic carbonyloxy, alkylsulfonyloxy, aromatic sulfonyloxy, alkylcarbamoyloxy, aromatic carbamoyloxy, alkylcarbonylamino, or aromatic acylamino, provided that R1 may further represent a hydrogen atom, alkyl, alkenyl, or alkynyl; and R3, R4, and R5 each independently represent a hydrogen atom, alkyl or alkenyl.
摘要翻译：公开了由下式（I）表示的化合物及其药学上可接受的盐。所述化合物具有孕酮受体结合抑制活性，因此可用作孕酮相关疾病的治疗和预防剂。具体地说，它们可用作流产者，口服避孕药，乳腺癌和卵巢癌的制癌剂，子宫内膜异位症的治疗剂，脑膜瘤和骨髓瘤，以及骨质疏松症和更年期障碍的治疗和预防剂。其中R1和R2表示羟基，烷氧基，链烯氧基，炔氧基，环烷氧基，烷氧基烷氧基，含有一个氧原子的环烷氧基，芳烷氧基，烷基羰基氧基，链烯基羰基氧基，炔基羰氧基，环烷基羰基氧基，烷氧基羰基氧基，芳氧基羰基氧基，芳烷基羰基氧基，芳香酰氧基，杂芳基酰氧基，饱和杂环羰氧基，烷基磺酰氧基，芳香磺酰氧基，烷基氨基甲酰氧基，芳族氨基甲酰氧基，烷基羰基氨基或芳族酰氨基，条件是R 1可以进一步代表氢原子，烷基，烯基或炔基; 并且R 3，R 4和R 5各自独立地表示氢原子，烷基或链烯基。

2. 发明授权

US6077840A Tetrahydrobenzindolone derivatives 有权
标题翻译：四氢苯并吲哚酮衍生物
公开(公告)号：US6077840A
公开(公告)日：2000-06-20
申请号：US331294
申请日：1999-06-18
申请人： Kenichi Kurihara , Rie Shinei , Yasushi Kurata , Yuji Tabata , Kiyoshi Tanabe , Tsuneo Okonogi
发明人： Kenichi Kurihara , Rie Shinei , Yasushi Kurata , Yuji Tabata , Kiyoshi Tanabe , Tsuneo Okonogi
IPC分类号： C07D209/60 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D521/00 , A61K31/535 , A61K31/40 , A61K31/44 , A61K31/50 , C07D233/02
CPC分类号： C07D231/12 , C07D209/60 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12
摘要： Compounds represented by the following formula (I) or pharmaceutically acceptable salts thereof and a process for producing the same are disclosed. The compounds have progesterone receptor binding inhibitory activity and, hence, can be used as therapeutic and prophylactic agents for progesterone-related diseases. Specifically, they are useful as carcinostatic agents for breast cancer and ovarian cancer, therapeutic agents for hysteromyoma, endometriosis, meningioma, and myeloma, abortifacients, oral contraceptive pills, and therapeutic and prophylactic agents for osteoporosis and climacteric disturbance. ##STR1## wherein R.sup.1 represents alkyl or aralkyl; R.sup.2 represents a hydrogen atom, alkylcarbonyl, cycloalkylcarbonyl, aromatic acyl, heteroaromatic acyl, saturated heterocyclic acyl, alkyl, alkenyl, aralkyl, carbamoyl, alkylcarbamoyl, aromatic carbamoyl, aralkylcarbamoyl, alkylaminocarbonyl, cycloalkylcarbamoyl, alkoxycarbonyl, aryloxycarbonyl, heteroaromatic thiocarbonyl, saturated heterocyclic thiocarbonyl, or alkyl-thiocarbamoyl: and R.sup.3 represents a hydrogen atom, a hydroxyl group, alkyloxy, alkylcarbonyloxy, alkylthio, or arylthio.
摘要翻译： PCT No.PCT / JP97 / 04683 Sec。 371日期：1999年6月18日 102（e）1999年6月18日PCT 1997年12月18日PCT公布。第WO98 / 27059号公报日期：1998年6月25日公开了由下式（I）表示的化合物或其药学上可接受的盐及其制备方法。所述化合物具有孕酮受体结合抑制活性，因此可用作孕酮相关疾病的治疗和预防剂。具体地说，它们可用作乳腺癌和卵巢癌的制癌剂，子宫肌瘤，子宫内膜异位症，脑膜瘤和骨髓瘤的治疗剂，流产者，口服避孕药以及用于骨质疏松和更年期障碍的治疗和预防剂。其中R1表示烷基或芳烷基; R 2表示氢原子，烷基羰基，环烷基羰基，芳香族酰基，杂芳基酰基，饱和杂环酰基，烷基，烯基，芳烷基，氨基甲酰基，烷基氨基甲酰基，芳香族氨基甲酰基，芳烷基氨基甲酰基，烷基氨基羰基，环烷基氨基甲酰基，烷氧基羰基，芳氧基羰基，杂芳硫基羰基，饱和杂环硫代羰基，或烷基 - 硫代氨基甲酰基：和R3表示氢原子，羟基，烷氧基，烷基羰氧基，烷硫基或芳硫基。

3. 发明授权

US5849797A D-.beta.-lysylmethanediamine derivatives and preparation thereof 失效
标题翻译： D-β-赖氨酰基甲二胺衍生物及其制备
公开(公告)号：US5849797A
公开(公告)日：1998-12-15
申请号：US793912
申请日：1997-02-24
申请人： Shinichi Kondo , Yoko Ikeda , Tomio Takeuchi , Rie Shinei , Shuichi Gomi , Seiji Shibahara , Hiroo Hoshino
发明人： Shinichi Kondo , Yoko Ikeda , Tomio Takeuchi , Rie Shinei , Shuichi Gomi , Seiji Shibahara , Hiroo Hoshino
IPC分类号： A61K31/16 , A61P31/12 , A61P31/18 , A61P37/04 , C07C231/02 , C07C231/12 , C07C237/10 , C07C233/05
CPC分类号： C07C237/10
摘要： Now are provided (R)-3,6-diamino-N-(.omega.-aminoalkyl)-hexanamides which are novel compounds having the general formula (I): ##STR1## wherein n stands for 2-5, and which may be for example, (R)-3,6-diamino-N-(2-aminoethyl)hexanamide (n=2) and (R)-3,6-diamino-N-(3-aminopropyl)hexanamide (n=3). Their preparation process is also provided. These novel compounds and acid addition salts thereof have activities inhibitory against Gram-positive bacteria, Gram-negative bacteria and AIDS virus, as well as tumor cells and are chemically stable. These novel compounds and their salts are useful as chemotherapeutic agents for diseases caused by these bacteria or virus and also as antitumor agent.
摘要翻译： PCT No.PCT / JP95 / 01680 Sec。 371日期1997年2月24日 102（e）1997年2月24日PCT PCT 1995年8月24日PCT公布。公开号WO96 / 06069 日期：1996年2月29日提供（R）-3,6-二氨基-N-（ω-氨基烷基） - 己酰胺，它们是具有通式（I）的新化合物：其中n代表2 -5，其可以是例如（R）-3,6-二氨基-N-（2-氨基乙基）己酰胺（n = 2）和（R）-3,6-二氨基-N-（3-氨基丙基）己酰胺（n = 3）。还提供了他们的准备过程。这些新化合物及其酸加成盐具有抑制革兰氏阳性菌，革兰氏阴性菌和艾滋病病毒以及肿瘤细胞的活性，并具有化学稳定性。这些新化合物及其盐可用作由这些细菌或病毒引起的疾病的化学治疗剂，也可用作抗肿瘤剂。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式