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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

US5602106A 16-membered macrolide derivatives 失效
标题翻译： 16元大环内酯衍生物
公开(公告)号：US5602106A
公开(公告)日：1997-02-11
申请号：US271996
申请日：1994-07-08
申请人： Keiichi Ajito , Osamu Hara , Ken-ichi Kurihara , Nobue Kikuchi , Minako Araake , Akira Shimizu , Tsuneo Okonogi , Shigeharu Inouye , Seiji Shibahara
发明人： Keiichi Ajito , Osamu Hara , Ken-ichi Kurihara , Nobue Kikuchi , Minako Araake , Akira Shimizu , Tsuneo Okonogi , Shigeharu Inouye , Seiji Shibahara
IPC分类号： C07H17/08 , A61K31/70
CPC分类号： C07H17/08
摘要： 16-membered macrolide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom or a substituent group which protects a hydroxyl group; R.sup.2 represents a hydrogen atom or a substituent group which protects a hydroxyl group; R.sup.3 represents a hydrogen atom or a straight-chain aliphatic acyl group having 2 to 4 carbon atoms; and R.sup.4 represents a hydrogen atom or a straight-chain aliphatic or aromatic acyl group having 1 to 10 carbon atoms;or a pharmaceutically acceptable salt thereof are disclosed.A novel process for producing these 16-membered macrolide derivatives is also disclosed.
摘要翻译：由式（I）表示的16元大环内酯衍生物：其中R 1表示氢原子或保护羟基的取代基; R2表示氢原子或保护羟基的取代基; R3表示氢原子或碳原子数2〜4的直链脂肪族酰基， R 4表示氢原子或碳原子数1〜10的直链脂肪族或芳香族酰基，或其药学上可接受的盐。还公开了一种制备这些16元大环内酯衍生物的新方法。

4. 发明授权

US6043217A Amide derivative of amythiamicin 失效
标题翻译： amythiamicin的酰胺衍生物
公开(公告)号：US6043217A
公开(公告)日：2000-03-28
申请号：US915118
申请日：1997-08-20
申请人： Yasuhiko Muraoka , Hironobu Iinuma , Tomio Takeuchi , Tsuneo Okonogi
发明人： Yasuhiko Muraoka , Hironobu Iinuma , Tomio Takeuchi , Tsuneo Okonogi
IPC分类号： A61K38/00 , A61P31/04 , C07K5/02 , C07K5/078 , C07K14/41 , C07K5/00
CPC分类号： C07K5/06139 , A61K38/00
摘要： Novel amide derivatives of amythiamicin are now provided, which are soluble in water and exhibit antibacterial activities, some of which exhibit an excellent antibacterial activity against methicillin-resistant Staphylococcus aureus (MRSA).
摘要翻译：现在提供了新型的氨基安定胺衍生物，其可溶于水并具有抗菌活性，其中一些对耐甲氧西林金黄色葡萄球菌（MRSA）具有优异的抗菌活性。

5. 发明授权

US5294705A Process for the preparation of a 3-substituted thio-3-cephem compound 失效
标题翻译： 3-取代的硫代-3-头孢烯化合物的制备方法
公开(公告)号：US5294705A
公开(公告)日：1994-03-15
申请号：US853730
申请日：1992-06-03
申请人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
发明人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
IPC分类号： C07D501/00 , C07D501/04 , C07D501/59
CPC分类号： C07D501/00 , Y02P20/55
摘要： An ester of 7-acylamido-3-acylthio-3- or -2-cephem-4-carboxylic acid represented by general formula (1) ##STR1## wherein R.sup.1 is an acyl group, R.sup.2 is a carboxyl-protecting group, R.sup.3 is a lower alkyl group, an aryl group or a substituted aryl group, or a mixture of two or more of said ester is used as the starting compound and is reacted wit a tertiary amine and also a secondary amine. Then the tertiary amine salt compound as formed as the reaction product is reacted with a compound of formula (4)R.sup.4 --X (4)wherein R.sup.4 is a lower alkyl group, a cycloalkyl group or a heterocyclic group or a heterocyclic group-substituted methyl group and X is a leaving group, whereby the desired ester of 7-acylamido-3-substituted thio-3-cephem-4-carboxylic acid of formula (5) ##STR2## can be produced preferentially, conveniently and efficiently.
摘要翻译： PCT No.PCT / JP90 / 01599 Sec。 371日期：1992年6月3日 102（e）日期1992年6月3日PCT 1990年12月7日PCT PCT。公开号WO91 / 09037 1991年6月27日，由通式（1）表示的7-酰基氨基-3-酰硫基-3-或2-头孢烯-4-羧酸酯（*化学结构*）（1）其中R1为酰基，R2为羧基保护基，R3为低级烷基，芳基或取代芳基，或两种或多种所述酯的混合物用作起始化合物，并与叔胺以及仲胺。然后将作为反应产物形成的叔胺盐化合物与式（4）R4-X（4）的化合物反应，其中R4是低级烷基，环烷基或杂环基或杂环基取代的甲基并且X是离去基团，由此可以优选地，方便地制备所需的式（5）的7-酰基酰胺基-3-取代的硫代-3-头孢烯-4-羧酸的酯（*化学结构*）（5）并有效地。

6. 发明授权

US4785090A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US4785090A
公开(公告)日：1988-11-15
申请号：US704077
申请日：1985-02-21
申请人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
发明人： Takashi Tsuruoka , Seiji Shibahara , Katsuyoshi Iwamatsu , Tsuneo Okonogi , Satoru Nakabayashi , Yasushi Murai , Hiroko Ogino , Kiyoaki Katano , Takashi Yoshida , Shigeharu Inoue , Shunzo Fukatsu , Shinichi Kondo
IPC分类号： C07D213/64 , C07D213/68 , C07D221/04 , C07D501/36 , C07D501/38 , A61K31/545
CPC分类号： C07D221/04 , C07D213/64 , C07D213/68
摘要： This is a class of antibacterial compounds of the formula: ##STR1## wherein Y is straight or branched alkyl or alkenyl chain, cycloalkanomethyl of 3-6 carbon atoms, each group being optionally substituted by halogen, or a group ##STR2## wherein n is 0 or an integer of 1-3, A is a group --COR.sup.3 wherein R.sup.3 is hydroxy, a group ##STR3## wherein R.sup.4 and R.sup.5, which may be the same or different, are hydrogen or alkyl of 1-5 carbon atoms, a group ##STR4## or a 5- or 6-membered heterocyclic group containing nitrogen and/or sulfur, and R.sup.1 and R.sup.2, which may be the same or different, are hydrogen, alkyl of 1-5 carbon atoms, or R.sup.1 and R.sup.2 may be combined together to form cycloalkylidene of 3-5 carbon atoms, and Z is a group of the formula: ##STR5## wherein m is 0 or an integer of 3-5, R.sup.6 is hydrogen or alkyl of 1-3 carbon atoms, and R.sup.7, when m is an integer of 3-5, is alkyl of 1-5 carbon atoms, alkenyl, cyclopropyl, a group --(CH.sub.2).sub.p B wherein p is 0 or an integer of 1-3 and B is amino, alkyl-substituted amino, hydroxy, carboxy, carbamoyl, trifluoromethyl, sulfonic acid, sulfonic acid amide, alkylthio or cyano or, when m is 0, is alkyl of 1-5 carbon atoms, which may optionally be substituted by halogen, alkenyl, a group ##STR6## wherein R.sup.8 is hydrogen, alkyl of 1-4 carbon atoms or phenyl, or cyclopropyl, and a salt thereof.
摘要翻译：这是一类具有下式的抗菌化合物：其中Y是直链或支链烷基或烯基链，3-6个碳原子的环烷基甲基，每个基团任选被卤素取代，或基团< 其中n为0或1-3的整数，A为基团-COR 3，其中R 3为羟基，其中R 4和R 5可以相同或不同，为氢或1-5碳的烷基原子，基团或含有氮和/或硫的5-或6-元杂环基，R 1和R 2可以相同或不同，为氢，1-5个碳原子的烷基或R1 并且R 2可以组合在一起形成3-5个碳原子的亚烷基，Z是下式的基团：其中m是0或3-5的整数，R6是氢或1-3个碳的烷基原子和R 7，当m是3-5的整数时，是1-5个碳原子的烷基，烯基，环丙基，基团 - （CH 2）pB，其中p是0或1-3的整数，B是氨基，烷基取代的氨基羟基，羧基，氨基甲酰基，三氟甲基，磺酸，磺酸酰胺，烷硫基或氰基，或当m为0时，其为1-5个碳原子的烷基，其可任选被卤素，链烯基，基团其中R8是氢，1-4个碳原子的烷基或苯基，或环丙基及其盐。

7. 发明授权

US4534898A 1-Oxa-1-dethia-cephalosporin derivatives 失效
标题翻译： 1-氧杂-1-脱氢头孢菌素衍生物
公开(公告)号：US4534898A
公开(公告)日：1985-08-13
申请号：US515422
申请日：1983-07-20
申请人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Shunzo Fukatsu , Tadashi Wakazawa , Taro Niida , Burton G. Christensen
发明人： Seiji Shibahara , Tsuneo Okonogi , Yasushi Murai , Shunzo Fukatsu , Tadashi Wakazawa , Taro Niida , Burton G. Christensen
IPC分类号： C07D498/04 , C07D205/085 , C07D403/12 , C07D505/00 , C07F9/568 , C07D419/14
CPC分类号： C07D403/12 , C07D205/085 , C07D505/00 , C07F9/5683
摘要： This invention relates to 1-oxa-1-dethia-cephalosporins which are useful as anti-biotics.
摘要翻译：本发明涉及可用作抗生物素的1-氧杂-1-脱氢头孢菌素。

8. 发明授权

US4418070A Cardiotonic agents 失效
标题翻译：强心剂
公开(公告)号：US4418070A
公开(公告)日：1983-11-29
申请号：US345672
申请日：1982-02-04
申请人： Tsuneo Okonogi , Shunzo Fukatsu , Mitsugu Hachisu , Hiroko Kawashima , Keiko Shitoh , Yasuharu Sekizawa
发明人： Tsuneo Okonogi , Shunzo Fukatsu , Mitsugu Hachisu , Hiroko Kawashima , Keiko Shitoh , Yasuharu Sekizawa
IPC分类号： A61K31/425 , A61K31/426 , A61P9/04 , C07D277/20 , C07D277/22 , C07D277/32 , C07D277/34 , C07D277/36 , C07D277/40
CPC分类号： A61K31/425 , C07D277/34
摘要： A 5-phenylthiazole derivative represented by the formula: ##STR1## wherein R represents a hydrogen atom, a lower alkyl group, a hydroxyl group, an amino group or a mercapto group, or a pharmaceutically acceptable salt thereof shows a cardiac effect and a low toxicity to a human or animal with little influence on atrium rhythms.
摘要翻译：其中R表示氢原子，低级烷基，羟基，氨基或巯基的5-苯基噻唑衍生物或其药学上可接受的盐显示心脏效应和低对人或动物的毒性，对心房节律几乎没有影响。

9. 发明授权

US5334723A 2-piperidinecarboxylic acid derivative, oncogene suppressor and agent for obtaining revertants 失效
标题翻译： 2-哌啶羧酸衍生物，癌基因抑制剂和获得回复体的试剂
公开(公告)号：US5334723A
公开(公告)日：1994-08-02
申请号：US937112
申请日：1992-08-31
申请人： Tsuneo Okonogi , Osamu Makabe , Yuichi Yamamoto , Osamu Itoh , Tsutomu Tsuruoka , Takayuki Usui , Seiji Shibahara , Kozo Nagaoka , Shigeharu Inouye , Nobuko Okada , Susumu Nishimura
发明人： Tsuneo Okonogi , Osamu Makabe , Yuichi Yamamoto , Osamu Itoh , Tsutomu Tsuruoka , Takayuki Usui , Seiji Shibahara , Kozo Nagaoka , Shigeharu Inouye , Nobuko Okada , Susumu Nishimura
IPC分类号： C07D211/90 , C07D211/76 , C07D211/86 , C07D211/88
CPC分类号： C07D211/90
摘要： A novel 2-piperidinecarboxylic acid derivative represented by the formula: ##STR1## wherein X represents an oxygen atom, a sulfur atom or a nitrogen atom to which a hydrogen atom is bound; and * represents that the configuration of the carbon atom binding to the carboxyl group is (S), (R) or a mixture of (S) and (R); and a pharmaceutically acceptable salt thereof which exerts an antitumor effect over a wide range of tumor cells.
摘要翻译：由下式表示的新颖的2-哌啶羧酸衍生物：其中X表示与氢原子结合的氧原子，硫原子或氮原子; 和*表示与羧基结合的碳原子的构型是（S），（R）或（S）和（R）的混合物。和其药学上可接受的盐在广泛的肿瘤细胞上发挥抗肿瘤作用。

10. 发明授权

US5332731A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5332731A
公开(公告)日：1994-07-26
申请号：US623215
申请日：1990-12-06
申请人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
发明人： Yuichi Yamamoto , Tsuneo Okonogi , Seiji Shibahara , Shigeharu Inoue
IPC分类号： C07D501/00 , C07D501/59 , C07D501/36
CPC分类号： C07D501/00
摘要： A new class of cephalosporin derivatives is provided, which is useful as antibacterial agent to be particularly suitable for oral administrations in mammals including man, and which is represented by general formula (I) ##STR1## wherein R.sup.1 is a hydrogen atom or a lower alkyl group; R.sup.2 is a hydrogen atom or an ester-forming group capable of being cleaved easily with an esterase existing in the digestive tracts; n is an integer of zero or 1; Z is a saturated heterocyclic group containing one or two oxygen atoms as the hetero-atoms with or without one or more lower alkyl substituents, or a pharmaceutically acceptable salt thereof.
摘要翻译：提供了一类新的头孢菌素衍生物，其可用作特别适合于包括人在内的哺乳动物的口服给药的抗菌剂，其由通式（I）表示，其中R 1是氢原子或低级烷基; R2是能够容易地与存在于消化道中的酯酶裂解的氢原子或成酯基团; n是0或1的整数; Z是含有一个或两个氧原子作为具有或不具有一个或多个低级烷基取代基的杂原子的饱和杂环基，或其药学上可接受的盐。

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