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1. 发明授权

US4010149A Analogs of LH-RH and process for preparing the same 失效
标题翻译： LH-RH的类似物及其制备方法
公开(公告)号：US4010149A
公开(公告)日：1977-03-01
申请号：US565362
申请日：1975-04-07
申请人： Yoshihiko Baba , Yutaka Okada , Hiroyashi Horikoshi , Yuichiro Yabe
发明人： Yoshihiko Baba , Yutaka Okada , Hiroyashi Horikoshi , Yuichiro Yabe
IPC分类号： C07K14/575 , A61K38/00 , C07K7/23 , C07C103/52 , C07G7/00
CPC分类号： C07K7/23 , A61K38/00 , Y02P20/55 , Y10S514/80 , Y10S930/13
摘要： Peptides having the formulaN-Acetyl-N-methylglycyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-Y-L-leucyl-L-arginyl-L-prolyl-Zwherein Y is a D-.alpha.-alkylglycine residue of the formula ##STR1## in which n is an integer of 0 through 3 inclusive and Z is ethylamino group or an ethylamino group which is substituted with 1 to 3 fluorine atoms at the 2-position and pharmaceutically acceptable salts thereof. They show luteinizing hormone-releasing hormone like activities and are prepared by reactingL-histidyl-L-tryptophyl-L-seryl(or L-seryl having a protected hydroxyl group)-L-tyrosyl(or L-tyrosyl having a protected hydroxyl group)-Y-L-leucyl-L-arginyl(or L-arginyl having a protected guanidyl group)-L-prolyl-Zwherein Y and Z are as defined above witha reactive derivative of N-Acetyl-N-methylglycineAnd, if a protective group is attached, then removing the protective group, and, if necessary, converting further the resultant into an acid addition salt thereof in the usual manner.
摘要翻译：具有式N-乙酰基-N-甲基甘氨酰-L-组氨酰基-L-色氨酰-L-丝氨酰-L-酪氨酰-LY-亮氨酰-L-精氨酰-L-脯氨酰基-Z的肽，其中Y是D-α-烷基甘氨酸其中n为0〜3的整数，Z为乙氨基或2-位被氟原子取代的乙氨基的式“IMAGE”的残基及其药学上可接受的盐。它们显示促黄体激素释放激素样活性，并且通过使L-组氨酰-L-色氨酰-L-丝氨酰（或具有被保护的羟基的L-丝氨酰）-L-酪氨酰基（或具有被保护的羟基的L-酪氨酰基））-L-亮氨酰-L-精氨酰基（或具有保护的胍基的L-精氨酰基）-L-脯氨酰基-Z，其中Y和Z如上定义，与N-乙酰基-N-甲基甘氨酸的反应性衍生物反应，如果A 保护组附带，然后移除保护组，如果必要的话，将其转化为在该手册中的酸添加盐。

2. 发明授权

US4116774A Method for the determination of enzyme activities 失效
标题翻译：测定酶活性的方法
公开(公告)号：US4116774A
公开(公告)日：1978-09-26
申请号：US798938
申请日：1977-05-20
申请人： Sadamasa Minato , Atsushi Hattori , Yoshihiko Baba , Yuichiro Yabe , Seigo Ueda
发明人： Sadamasa Minato , Atsushi Hattori , Yoshihiko Baba , Yuichiro Yabe , Seigo Ueda
IPC分类号： G01N33/68 , C12Q1/34 , C12Q1/37 , C12Q1/52 , G01N33/00 , G01N31/14
CPC分类号： C12Q1/34
摘要： Improvement in determination of an enzyme activity in a substance having an enzymatic activity which comprises employing an aromatic primary amine derivative as a substrate and an iron complex treated with a peroxide as a color reagent.
摘要翻译：改进具有酶活性的物质中的酶活性的测定，其包括使用芳族伯胺衍生物作为底物和用过氧化物作为着色试剂处理的铁络合物。

3. 发明授权

US5364844A Renin-inhibitory oligopeptides, their preparation and use 失效
标题翻译：肾素抑制寡肽，其制备和用途
公开(公告)号：US5364844A
公开(公告)日：1994-11-15
申请号：US936883
申请日：1992-08-27
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Yasuteru Iijima , Hidekuni Takahagi , Tatsuo Kokubu , Kunio Hiwada
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Yasuteru Iijima , Hidekuni Takahagi , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： C07K5/02 , A61K37/02 , C07K5/06 , C07K5/08
CPC分类号： C07K5/0227 , C07K5/0207
摘要： Compounds of formula (I): ##STR1## A is a carbon-carbon bond or C.sub.1 -C.sub.3 alkylene; B is imino group or C.sub.1 -C.sub.2 alkylene; R.sup.1 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, heterocyclic or optionally substituted amino; R.sup.2 is optionally substituted phenyl or optionally substituted naphthyl; R.sup.3 is thiazolyl, isoxazolyl or imidazolyl; R.sup.4 is isopropyl or cyclohexyl; R.sup.5 and R.sup.6 are C.sub.1 -C.sub.4 alkyl, or, together with the carbon atom to which they are attached, C.sub.3 -C.sub.7 cycloalkyl; R.sup.7 is hydrogen, optionally substituted C.sub.1 -C.sub.6 alkyl group; and R.sup.8 is hydrogen or C.sub.1 -C.sub.4 alkyl. These compounds have renin-inhibitory and, hence, hypotensive activities. The invention also provides a method for the treatment or prophylaxis of hypertension induced by failures in the renin-angiotensin system.
摘要翻译：式（I）的化合物：A是碳 - 碳键或C1-C3亚烷基; B是亚氨基或C 1 -C 2亚烷基; R1是C1-C4烷基，C1-C4烷氧基，杂环或任选取代的氨基; R2是任选取代的苯基或任选取代的萘基; R3是噻唑基，异恶唑基或咪唑基; R4是异丙基或环己基; R 5和R 6是C 1 -C 4烷基，或者与它们所连接的碳原子一起是C 3 -C 7环烷基; R7是氢，任选取代的C 1 -C 6烷基; 并且R 8是氢或C 1 -C 4烷基。这些化合物具有肾素抑制，因此具有降血压活性。本发明还提供了用于治疗或预防由肾素 - 血管紧张素系统中的失败引起的高血压的方法。

4. 发明授权

US4698329A New renin-inhibitory peptides and their use 失效
标题翻译：新的肾素抑制肽及其用途
公开(公告)号：US4698329A
公开(公告)日：1987-10-06
申请号：US696334
申请日：1985-01-30
申请人： Rei Matsueda , Yuichiro Yabe , Mitsuo Yamazaki , Tatsuo Kokubu , Kunio Hiwada
发明人： Rei Matsueda , Yuichiro Yabe , Mitsuo Yamazaki , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： C07K14/81 , A61K38/00 , A61K38/05 , A61K38/06 , A61K38/55 , A61P9/12 , A61P43/00 , C07F9/30 , C07K5/02 , C07K5/083 , A61K37/64 , C07K5/08
CPC分类号： C07K5/0227 , C07F9/301 , Y10S530/86
摘要： Compounds of formulaR.sup.1 CO--NH--CH(R.sup.2)--CONH--CH(R.sup.3)--X[wherein:R.sup.1 represents alkyl having an .alpha.-amino or protected .alpha.-amino substituent and an aryl, heterocyclic or heterocyclic-dithio substituent;R.sup.2 represents a variety of aliphatic and cycloaliphatic hydrocarbon groups, which may be substituted;R.sup.3 represents isobutyl, sec-butyl, benzyl or (C.sub.3 -C.sub.8 cycloalkyl)methyl; andX represents a group of formula --CH(--A--R.sup.4)--Y (in which: A represents a single bond or an alkylene group; R.sup.4 represents a carboxy group; a protected carboxy group, a carbamoyl group, an N-substituted carbamoyl group, a carbazoyl group, an N-substituted carbazoyl group or an acyl group; and Y represents a hydroxy group, a mercapto group or a formyl group), ora group of formula --P(O) (R.sup.5)--OH (in which R.sup.5 represents a substituted alkyl group having at least one substituent selected from carboxy groups, protected carboxy groups, N-substituted carbamoyl groups, carbazoyl groups, N-substituted carbazoyl groups, C.sub.2 -C.sub.7 aliphatic carboxylic acyl groups and aromatic carboxylic acyl groups)];and their salts are renin inhibitors, which may be used in the treatment of angiotensin-induced hypertension.
摘要翻译：式R 1 CO-NH-CH（R 2）-CONH-CH（R 3）-X [其中：R 1表示具有α-氨基或被保护的α-氨基取代基和芳基，杂环或杂环二硫基取代基的烷基; R2表示可以被取代的各种脂族和脂环族烃基; R 3表示异丁基，仲丁基，苄基或（C 3 -C 8环烷基）甲基; 并且X表示式-CH（-A-R 4）-Y基团（其中：A表示单键或亚烷基; R 4表示羧基;被保护的羧基，氨基甲酰基，N-取代的氨基甲酰基，咔唑基，N-取代的咔唑基或酰基; Y表示羟基，巯基或甲酰基）或式-P（O）（R5）-OH（其中R 5表示具有至少一个选自羧基，保护的羧基，N-取代的氨基甲酰基，咔唑基，N-取代的咔唑基，C 2 -C 7脂族羧酸酰基和芳族羧酰基的取代基的烷基） ]; 其盐类为肾素抑制剂，可用于治疗血管紧张素诱导的高血压。

5. 发明授权

US5629406A Inhibitors of HIV protease 失效
标题翻译： HIV蛋白酶抑制剂
公开(公告)号：US5629406A
公开(公告)日：1997-05-13
申请号：US227588
申请日：1994-04-14
申请人： Susumu Higashida , Mitsuya Sakurai , Yuichiro Yabe , Takashi Nishigaki , Tomoaki Komai , Hiroshi Handa
发明人： Susumu Higashida , Mitsuya Sakurai , Yuichiro Yabe , Takashi Nishigaki , Tomoaki Komai , Hiroshi Handa
IPC分类号： C07K5/093 , A61K38/00 , A61K38/55 , A61P31/18 , C07D207/16 , C07D207/22 , C07D207/24 , C07D207/28 , C07D401/12 , C07D403/12 , C07D405/12 , C07D487/08 , C07D491/08 , C07K5/02 , C12N15/48 , A61K38/06
CPC分类号： C07D401/12 , C07D207/16 , C07D207/22 , C07D207/24 , C07D207/28 , C07D403/12 , C07D405/12 , C07D487/08 , C07D491/08 , C07K5/0202 , A61K38/00 , Y02P20/55
摘要： Compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, alkyl, aralkyl, --COR.sup.a, --COR.sup.b, --CSR.sup.a, --CSR.sup.b, --SO.sub.2 R.sup.b, --CONHR.sup.b, --CSNHR.sup.b, --CONR.sup.b R.sup.b or --CSNR.sup.b R.sup.b ; R.sup.2 is hydrogen or alkyl; R.sup.3 is hydrogen, alkylidene, substituted alkyl, or R.sup.b ; R.sup.4 is optionally substituted alkyl, cycloalkyl, or aryl; R.sup.5 is R.sup.b O--, R.sup.b R.sup.b N--, R.sup.b HN--, aralkyloxycarbonyloxy or aralkyloxycarbonylamino, or R.sup.5 is --(CH.sub.2).sub.p --D--(CH.sub.2).sub.r --, where D is a single bond, carbonyl, oxygen, sulfur, --NH--, --(CH.sub.2 .dbd.CH.sub.2)-- or --NHCO--; and p and r are each 0 or an integer from 1 to 5; A is --(CH.sub.2).sub.m --B--(CH.sub.2).sub.n -- where B is a single bond, carbonyl, oxygen, sulfur, --NH--, --(CH.sub.2 .dbd.CH.sub.2)-- or --NHCO--; and m and n are each 0 or an integer from 1 to 5; R.sup.a is alkoxy, aralkyloxy, aryloxy or alkoxycarbonyl; R.sup.b is optionally substituted alkyl, cycloalkyl, heterocyclic, aryl or arylalkenyl; and pharmaceutically acceptable salts and esters thereof and pro-drugs therefor, have the ability to inhibit the activity of HIV protease and may thus be used for the treatment and prophylaxis of AIDS.
摘要翻译：式（I）化合物：其中：R1是氢，烷基，芳烷基，-CORa，-CORb，-CSRa，-CSRb，-SO2Rb，-CONHRb，-CSNHRb，-CONRbRb或-CSNRbRb; R2是氢或烷基; R3是氢，亚烷基，取代的烷基或Rb; R4是任选取代的烷基，环烷基或芳基; R5是RbO-，RbRbN-，RbHN-，芳烷氧基羰氧基或芳烷氧基羰基氨基，或R5是 - （CH2）pD-（CH2）r-，其中D是单键，羰基，氧，硫，-NH-， - = CH 2） - 或-NHCO-; 和+ E，uns p + EE和+ E，uns r + EE各自为0或1至5的整数; A是 - （CH 2）m -B-（CH 2）n - ，其中B是单键，羰基，氧，硫，-NH-， - （CH 2 = CH 2） - 或-NHCO-; 和+ E，uns m + EE和+ E，uns n + EE各自为0或1至5的整数; R a是烷氧基，芳烷氧基，芳氧基或烷氧基羰基; Rb是任选取代的烷基，环烷基，杂环，芳基或芳基烯基; 及其药学上可接受的盐和酯及其前药具有抑制HIV蛋白酶活性的能力，因此可用于治疗和预防艾滋病。

6. 发明授权

US5378689A Peptides having renin inhibitory activity, their preparation and use 失效
标题翻译：具有肾素抑制活性的肽，其制备和用途
公开(公告)号：US5378689A
公开(公告)日：1995-01-03
申请号：US98746
申请日：1993-07-28
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Hidekuni Takahagi , Yasuteru Iijima , Tatsuo Kokubu , Kunio Hiwada
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Hiroyuki Koike , Hidekuni Takahagi , Yasuteru Iijima , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： A61K31/425 , C07D277/30 , C07D413/06 , A61K37/02 , C07K5/08
CPC分类号： C07D277/30
摘要： Compounds of formula (I): ##STR1## [in which: R.sup.1 is heterocyclic group having 5 or 6 ring atoms, or --NR.sup.7 R.sup.8, where R.sup.7 is alkyl and R.sup.8 is optionally substituted phenyl, optionally substituted phenylalkyl or cycloalkyl; R.sup.2 is optionally substituted phenyl or naphthyl; R.sup.3 is thiazolyl; R.sup.4 is cyclohexyl or isopropyl; R.sup.5 is alkyl; and R.sup.6 is alkyl] and salts thereof have renin-inhibitory and, hence, hypotensive activities and are of value in the diagnosis and treatment of hypertension induced by failures in the renin-angiotensin system. They may be prepared by reacting together appropriate amino acids or derivatives thereof.
摘要翻译：式（I）化合物：其中：R 1为具有5或6个环原子的杂环基或-NR 7 R 8，其中R 7为烷基，R 8为任选取代的苯基，任选取代的苯基烷基或环烷基 R2是任选取代的苯基或萘基; R3是噻唑基; R4是环己基或异丙基; R5是烷基; 和R6是烷基]，其盐具有肾素抑制作用，因此具有降血压活性，并且在肾素 - 血管紧张素系统失败引起的高血压的诊断和治疗中具有价值。它们可以通过使合适的氨基酸或其衍生物一起反应来制备。

7. 发明授权

US5378690A New renin-inhibitory oligopeptides, their preparation and their use 失效
标题翻译：新的肾素抑制性寡肽，其制备及其应用
公开(公告)号：US5378690A
公开(公告)日：1995-01-03
申请号：US99776
申请日：1993-07-30
申请人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Yasuteru Iijima , Hidekuni Takahagi , Hiroyuki Koike , Tatsuo Kokubu , Kunio Hiwada
发明人： Yasuhiro Morisawa , Mitsuru Kataoka , Yuichiro Yabe , Yasuteru Iijima , Hidekuni Takahagi , Hiroyuki Koike , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： C07D233/54 , C07D261/08 , C07D277/30 , C07D295/13 , C07D295/185 , C07D333/24 , C07K5/02 , A61K37/02 , C07K5/08
CPC分类号： C07D233/64 , C07D261/08 , C07D277/30 , C07D295/13 , C07D295/185 , C07D333/24 , C07K5/0205 , C07K5/0227
摘要： Oligopeptides of formula (I): ##STR1## where R.sup.1 -R.sup.5 are various organic groups, and A represents a group of formula --NH-- or --(CH.sub.2).sub.n --, in which n represents an integer of from 1 to 3, have renin-inhibitory activity and are particularly suitable for oral administration. They may be prepared by condensing their component amino acids or lower oligopeptides using conventional peptide synthesis reactions.
摘要翻译：式（I）的寡肽：其中R 1 -R 5是各种有机基团，A表示式-NH-或 - （CH 2）n - 的基团，其中n表示整数 1〜3具有肾素抑制活性，特别适合于口服给药。它们可以通过使用常规肽合成反应来缩合其组分氨基酸或低级寡肽来制备。

8. 发明授权

US4548926A Hypotensive peptides and their use 失效
标题翻译：低血压肽及其用途
公开(公告)号：US4548926A
公开(公告)日：1985-10-22
申请号：US618127
申请日：1984-06-07
申请人： Rei Matsueda , Yuichiro Yabe , Mitsuo Yamazaki , Tatsuo Kokubu , Kunio Hiwada
发明人： Rei Matsueda , Yuichiro Yabe , Mitsuo Yamazaki , Tatsuo Kokubu , Kunio Hiwada
IPC分类号： A61K38/00 , A61K38/55 , A61P9/12 , A61P43/00 , C07D233/54 , C07D233/64 , C07F7/18 , C07F9/38 , C07F9/6506 , C07K5/02 , C07K5/04 , C07K5/06 , C07K5/065 , C07K5/078 , C07K5/087 , C07K14/81 , A61K37/00
CPC分类号： C07D233/64 , C07F7/1852 , C07F9/3808 , C07K5/0227 , C07K5/06078 , C07K5/06156 , C07K5/06191 , C07K5/0812 , A61K38/00 , Y10S530/80 , Y10S530/86
摘要： Oligopeptides of formula (I) ##STR1## (wherein R.sup.1 CO-- is an acyl group. But is an isobutyl or sec-butyl group and X is a variety of organic groups) and salts and esters thereof have valuable renin inhibitory activity.
摘要翻译：式（I）的寡肽（I）（其中R1CO-是酰基，但是是异丁基或仲丁基，X是各种有机基团），其盐和酯具有有价值的肾素抑制活性。

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