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41. 发明授权

US5430025A Elastase-inhibiting peptides bearing a C-terminal trifluoromethylketone moiety 失效
标题翻译：带有C-末端三氟甲基酮部分的弹性蛋白酶抑制肽
公开(公告)号：US5430025A
公开(公告)日：1995-07-04
申请号：US158981
申请日：1993-11-30
申请人： Keiji Hemmi , Ichiro Shima , Keisuke Imai , Hirokazu Tanaka
发明人： Keiji Hemmi , Ichiro Shima , Keisuke Imai , Hirokazu Tanaka
IPC分类号： A61K31/16 , A61K31/24 , A61K31/40 , A61K31/535 , A61K31/5375 , A61K38/00 , A61K38/05 , A61P11/00 , A61P43/00 , C07C231/02 , C07C233/68 , C07C237/22 , C07C275/42 , C07D295/02 , C07K5/06 , C07K5/065 , A61K38/06
CPC分类号： C07K5/06191 , A61K38/00
摘要： Trifluoromethylketone compounds of the formula: ##STR1## wherein R.sup.1 is C.sub.1-6 alkyl which has one or two substituents selected from carboxy, esterified carboxy and di-C.sub.1-6 alkylcarbamoyl; phenyl(C.sub.1-6)alkyl, the phenyl moiety of which may have halogen or nitro or amino substituents and the alkyl moiety of which may have carboxy or esterified carboxy substituents; halo-phenyl; morpholino; or morpholino(C.sub.1-6)alkyl, R.sup.2 and R.sup.3 are each C.sub.1-6 alkyl, X is --or --NH--, and ##STR2## and pharmaceutically acceptable salts thereof are useful for inhibiting human elastase.
摘要翻译：其中R 1是具有一个或两个选自羧基，酯化羧基和二-C 1-6烷基氨基甲酰基的取代基的C 1-6烷基; 苯基（C 1-6）烷基，其苯基部分可以具有卤素或硝基或氨基取代基，其烷基部分可以具有羧基或酯化的羧基取代基; 卤代苯基; 吗啉代或吗啉代（C 1-6）烷基，R 2和R 3各自为C 1-6烷基，X为 - 或-NH-，且其药学上可接受的盐可用于抑制人弹性蛋白酶。

42. 发明授权

US5356897A 3-(heteroaryl)-pyrazololi[1,5-a]pyrimidines 失效
标题翻译： 3-（杂芳基） - 吡唑并[1,5-a]嘧啶
公开(公告)号：US5356897A
公开(公告)日：1994-10-18
申请号：US931093
申请日：1992-08-17
申请人： Teruo Oku , Yoshio Kawai , Hiroshi Marusawa , Hitoshi Yamazaki , Yoshito Abe , Hirokazu Tanaka
发明人： Teruo Oku , Yoshio Kawai , Hiroshi Marusawa , Hitoshi Yamazaki , Yoshito Abe , Hirokazu Tanaka
IPC分类号： A61K31/415 , A61K31/505 , A61K31/53 , A61P29/00 , A61P37/00 , A61P43/00 , C07D487/04
CPC分类号： C07D487/04
摘要： This invention relates to heterocyclic derivatives useful for inhibiting the production of Interleukin-1 (IL-1) and tumor necrosis factor (TNF) and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to uses thereof.
摘要翻译：本发明涉及可用于抑制白细胞介素-1（IL-1）和肿瘤坏死因子（TNF）等的产生的杂环衍生物，其可以由下式表示：（I）它们的生产，涉及含有该组合物的药物组合物及其用途。

43. 发明授权

US5284828A Peptide compound and its preparation 失效
标题翻译：肽化合物及其制备
公开(公告)号：US5284828A
公开(公告)日：1994-02-08
申请号：US696701
申请日：1991-05-07
申请人： Keiji Hemmi , Masahiro Neya , Naoki Fukami , Masashi Hashimoto , Hirokazu Tanaka , Hatsuko Kayakiri
发明人： Keiji Hemmi , Masahiro Neya , Naoki Fukami , Masashi Hashimoto , Hirokazu Tanaka , Hatsuko Kayakiri
IPC分类号： A61K38/55 , A61K38/00 , A61K38/06 , C07K1/02 , C07K1/113 , C07K5/02 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/083 , C07K5/103 , A61K37/02
CPC分类号： C07K5/06156 , C07K5/0202 , C07K5/0205 , C07K5/0207 , C07K5/021 , C07K5/0217 , C07K5/0808 , C07K5/101 , A61K38/00 , Y02P20/55
摘要： Novel peptides of the formula (I") ##STR1## in which R.sup.1 is hydrogen or acyl,R.sup.2.sub.c is lower alkyl,R.sup.3.sub.c is optionally N-substituted indolylmethyl,R.sup.4 is hydrogen, lower alkyl, C.sub.6-10 ar(lower)alkyl, amino(lower)alkyl, protected amino (lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic (lower)alkyl,R.sup.5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl,R.sup.7 is hydrogen or lower alkyl, andA is --O--, --NH--, lower alkylamino or lower alkylene,or a pharmaceutically acceptable salt thereof are disclosed.Additionally, the preparation of such peptides is described. The peptides are used to treat endothelin mediated diseases such as hypertension.
摘要翻译：式（I“）（*化学结构*）（I”）的新肽，其中R 1为氢或酰基，R 2c为低级烷基，R 3c为任选N-取代的吲哚基甲基，R 4为氢，低级烷基，C 6-10 芳基（低级）烷基，氨基（低级）烷基，被保护的氨基（低级）烷基，羧基（低级）烷基，被保护的羧基（低级）烷基或任选取代的杂环（低级）烷基，R5是羧基，被保护的羧基，羧基）烷基或受保护的羧基（低级）烷基，R7是氢或低级烷基，A是-O - ， - NH-，低级烷基氨基或低级亚烷基或其药学上可接受的盐。另外，描述了这种肽的制备。肽用于治疗内皮素介导的疾病，如高血压。

44. 发明授权

US5264438A Quinazoline derivatives 失效
标题翻译：喹唑啉衍生物
公开(公告)号：US5264438A
公开(公告)日：1993-11-23
申请号：US627417
申请日：1990-12-14
申请人： Norihiko Shimazaki , Hitoshi Yamazaki , Takumi Yatabe , Hirokazu Tanaka , Yoshikuni Itoh , Masashi Hashimoto
发明人： Norihiko Shimazaki , Hitoshi Yamazaki , Takumi Yatabe , Hirokazu Tanaka , Yoshikuni Itoh , Masashi Hashimoto
IPC分类号： A61K31/505 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/28 , C07D401/06 , C07D401/14 , C07D413/14
CPC分类号： C07D401/06
摘要： Compounds of the formula: ##STR1## are described wherein R.sup.1, R.sup.2, R.sup.3 and A are described in the claims. These compounds show significant dopamine receptor agonist activity.

45. 发明授权

US5210092A Angiotensin II antagonizing heterocyclic derivatives 失效
标题翻译： ANGIOTENSIN II拮抗杂环衍生物
公开(公告)号：US5210092A
公开(公告)日：1993-05-11
申请号：US748954
申请日：1991-08-23
申请人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuki Inoue , Yuki Saitoh , Akio Kuroda , Hirokazu Tanaka
发明人： Teruo Oku , Hiroyuki Setoi , Hiroshi Kayakiri , Shigeki Satoh , Takayuki Inoue , Yuki Saitoh , Akio Kuroda , Hirokazu Tanaka
IPC分类号： A61K31/415 , A61K31/435 , A61K31/52 , A61P9/00 , A61P9/12 , A61P43/00 , C07D403/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D473/00 , C07D487/04 , C07D495/04
CPC分类号： C07D403/14 , C07D471/04 , C07D495/04 , Y02P20/55
摘要： The invention concerns compounds of the formula ##STR1## represents a condensed or uncondensed imidazolyl ring and the rest of the variables are defined in the specification. They are angiotensin II antagonists useful for treating hypertension, etc.

46. 发明授权

US5184109A Overcharge preventive device for automotive batteries 失效
标题翻译：汽车电池过充电装置
公开(公告)号：US5184109A
公开(公告)日：1993-02-02
申请号：US641413
申请日：1991-01-15
申请人： Hirokazu Tanaka , Koichi Ito
发明人： Hirokazu Tanaka , Koichi Ito
IPC分类号： B60R16/02 , B60R16/03 , H02J7/00 , H02J7/14
CPC分类号： H02J7/1461 , H02J7/009 , B60R16/03
摘要： An overcharge preventive device for an automotive battery charging circuit comprises an odorant sensor 6 for detecting the amount of gas generated from the battery 1 during charging (FIG. 3). A detector circuit 7 generates an overcharge detection signal when the amount of gas exceeds a predetermined level. In response thereto, the display or monitor lamp 8 displays the overcharged state, and the interruptor circuit 9 separates the alternator 5 from the battery 1. Alternatively, when the automobile has an audio device such as radio, a voltage detector 19 detects the voltage across the load 4 and outputs a signal when the voltage exceeds a predetermined level, an alarm signal generator 20 generating an audio signal in response to the output signal of the voltage detector 19, such that an alarm sound or voice is produced by a loudspeaker 17 via the amplifier 16 (FIG. 4).
摘要翻译：用于汽车电池充电电路的过充电防止装置包括用于在充电期间检测从电池1产生的气体量的气味传感器6（图3）。当气体量超过预定水平时，检测器电路7产生过充电检测信号。响应于此，显示器或监视灯8显示过充电状态，并且断路器电路9将交流发电机5与电池1分离。或者，当汽车具有诸如无线电的音频设备时，电压检测器19检测电压负载4并且当电压超过预定电平时输出信号，报警信号发生器20响应于电压检测器19的输出信号产生音频信号，使得扬声器17通过扬声器17产生警报声音放大器16（图4）。

47. 发明授权

US5110811A Tricyclo compounds, a process for their production and a pharmaceutical composition containing the same 失效
标题翻译：三肽化合物，其生产方法和含有它们的药物组合物
公开(公告)号：US5110811A
公开(公告)日：1992-05-05
申请号：US491205
申请日：1990-03-09
申请人： Masakuni Okuhara , Hirokazu Tanaka , Toshio Goto , Tohru Kino , Hiroshi Hatanaka
发明人： Masakuni Okuhara , Hirokazu Tanaka , Toshio Goto , Tohru Kino , Hiroshi Hatanaka
IPC分类号： A01N43/38 , A61K31/00 , A61K31/33 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/4353 , A61K31/436 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/453 , A61K31/4745 , A61P31/00 , A61P31/04 , A61P37/00 , A61P37/06 , C07D491/14 , C07D498/04 , C07D498/14 , C07D498/18 , C07D519/00 , C07H19/01 , C12N1/20 , C12P17/16 , C12P17/18 , C12P19/44 , C12R1/465 , C12R1/55
CPC分类号： C07D498/18 , C07H19/01 , C12P17/188 , C12P19/44 , C12R1/465 , C12R1/55 , Y02P20/55 , Y10S435/886 , Y10S435/898
摘要： This invention relates to tricyclo compounds useful for treatment and prevention of resistance by transplantation, graft-versus-host diseases by medulla ossium transplantation, autoimmune diseases, infectious diseases, and the like, which can be represented by the following formula: ##STR1## to a process for their production, to a pharmaceutical composition containing the same and to a use thereof.

48. 发明授权

US4643990A N-acyl peptide, processes for their preparation and pharmaceutical compositions thereof 失效
标题翻译： N-酰基肽，其制备方法及其药物组合物
公开(公告)号：US4643990A
公开(公告)日：1987-02-17
申请号：US452827
申请日：1982-12-23
申请人： Kazuyoshi Umehara , Keizo Yoshida , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka
发明人： Kazuyoshi Umehara , Keizo Yoshida , Hirokazu Tanaka , Itsuo Uchida , Masanobu Kohsaka , Hiroshi Imanaka
IPC分类号： A61K38/00 , C07K5/06 , C07K5/065 , C07K5/068 , C07K5/072 , A61K37/43 , C07C67/02 , C07C69/52 , C07C101/26 , C07C101/30 , C07C143/12 , C07K5/08
CPC分类号： C07K5/06104 , C07K5/06052 , C07K5/06078 , C07K5/06086 , A61K38/00
摘要： N-acylpeptides are disclosed of the formula: ##STR1## wherein R.sup.1 is alkanoyloxy or alkenoyloxy; R.sup.2 is alkyl or alkenyl; R.sup.3 and R.sup.4 are each lower alkyl, hydroxy(lower)alkyl, ar(lower)alkyl, esterified carboxy(lower)alkyl, carboxy(lower)alkyl, protected amino(lower)alkyl or amino(lower)alkyl; R.sup.5 is hydrogen, hydroxy(lower)alkyl, protected amino(lower)alkyl, amino(lower)alkyl, carboxy(lower)alkyl or esterified carboxy(lower)alkyl; R.sup.6 is carboxy, esterified carboxy or sulfo(lower)alkyl; A.sup.1, A.sup.2 and A.sup.3 are each bond or lower alkylene; and m and n are each an integer of 0 or 1; or its pharmaceutically acceptable salt. These compounds have anti-complementary activity and fibrinolytic activity, and are useful as therapeutic agents for immune-complex diseases or autoimmune diseases such as nephritis, rheumatic diseases, systemic lupus erythematosus, etc. and thrombosis such as cerebral apoplexy, coronary insufficiency, pulmonary embolism, etc.
摘要翻译： N-酰基肽公开于下式：其中R 1是烷酰氧基或烯酰基氧基; R2是烷基或烯基; R 3和R 4各自为低级烷基，羟基（低级）烷基，芳（低级）烷基，酯化羧基（低级）烷基，羧基（低级）烷基，被保护的氨基（低级）烷基或氨基（低级） R5是氢，羟基（低级）烷基，被保护的氨基（低级）烷基，氨基（低级）烷基，羧基（低级）烷基或酯化羧基（低级）烷基; R6是羧基，酯化的羧基或磺基（低级）烷基; A1，A2和A3各自为键或低级亚烷基; m和n分别为0或1的整数; 或其药学上可接受的盐。这些化合物具有抗互补活性和纤维蛋白溶解活性，并且可用作免疫复合物疾病或自身免疫性疾病如肾炎，风湿性疾病，系统性红斑狼疮等的治疗剂，以及血栓形成如脑中风，冠状动脉功能不全，肺栓塞等等

49. 发明授权

US4512980A Peptide, process for preparation thereof and use thereof 失效
标题翻译：肽，其制备方法及其用途
公开(公告)号：US4512980A
公开(公告)日：1985-04-23
申请号：US402438
申请日：1982-07-28
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto
IPC分类号： A61K38/00 , A61P31/04 , A61P37/00 , A61P37/04 , C07C237/22 , C07K1/06 , C07K1/113 , C07K5/02 , C07K5/04 , C07K7/02 , C07K9/00 , C07C103/52 , A61K37/02
CPC分类号： C07C243/00 , C07K5/0215 , C07K9/005 , C12R1/465 , A61K38/00
摘要： The invention relates to novel peptides of pharmacological activity, of the formula ##STR1## wherein R.sup.1 is hydrogen or acyl;R.sup.2 is carboxy or protected carboxy or a group of the formula: --COHN--R.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl;R.sup.3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl or a group of the formula: ##STR2## wherein R.sub.a.sup.3 is hydrogen, amino, protected amino or acylamino, R.sub.b.sup.3 is carboxy or protected carboxy;R.sup.p is carboxy, protected carboxy, carbamoyl, carboxy (lower) alkyl or protected carboxy (lower) alkyl;l is an integer 0;m is an interger 3; andn is an integer 1, provided that when R.sup.1 is hydrogen or acyl,R.sup.2 is carboxy, protected carboxy or a group of the formula:--CONHR.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl,R.sup.p is carboxy, or protected carboxy,R.sup.3 is carbamoyl, lower alkyl or hydroxyphenyl or a group of the formula: ##STR3## wherein R.sub.a.sup.3 is hydrogen or acylamino and R.sub.b.sup.3 is carboxy or protected carboxy, andwhen R.sup.p is carbamoyl, thenR.sup.1 is acyl.

50. 发明授权

US4504584A Cultures of novel strains of Streptomyces 失效
标题翻译：链霉菌新菌株的培养
公开(公告)号：US4504584A
公开(公告)日：1985-03-12
申请号：US379851
申请日：1982-05-19
申请人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
发明人： Yoshihiko Kitaura , Osamu Nakaguchi , Keiji Hemmi , Matsuhiko Aratani , Hidekazu Takeno , Satoshi Okada , Hirokazu Tanaka , Masashi Hashimoto , Yoshio Kuroda , Eiko Iguchi , Masanobu Kohsaka , Hatsuo Aoki , Hiroshi Imanaka
IPC分类号： A61K38/00 , C07K5/02 , C07K5/06 , C07K5/062 , C07K5/072 , C07K9/00 , C12N1/20 , C12R1/465
CPC分类号： C07C243/00 , C07K5/0215 , C07K5/06026 , C07K5/06104 , C07K9/005 , C12R1/465 , A61K38/00 , Y10S435/886 , Y10S930/19
摘要： The invention relates to a biologically pure culture of new strains of the microorganism Streptomyces which are capable upon fermentation of producing a peptide of pharmacological activity.
摘要翻译：本发明涉及生物学纯培养的新型菌株的微生物链霉菌，其能够在发酵时产生药理活性肽。

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