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1. 发明授权

US5352659A Endothelin analogs and uses thereof 失效
标题翻译：内皮素类似物及其用途
公开(公告)号：US5352659A
公开(公告)日：1994-10-04
申请号：US837780
申请日：1992-02-14
申请人： Mitsuhiro Wakimasu , Takashi Kikuchi , Kazuki Kubo
发明人： Mitsuhiro Wakimasu , Takashi Kikuchi , Kazuki Kubo
IPC分类号： A61K38/00 , C07K14/575 , A61K37/02 , C07K7/10
CPC分类号： C07K14/57536 , A61K38/00
摘要： Disclosed are a peptide represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein M represents a mercaptoacyl group; P, Q, R, S, T, U, V, W, X, Y and Z each represent amino acid residues, wherein an amino acid side chain of Y is either a substituted saturated aliphatic hydrocarbon group having 1 to 15 carbon atoms or an unsubstituted saturated aliphatic hydrocarbon group having 4 to 15 carbon atoms other than (1S)-1-methylpropyl; (2) a method for producing the above-mentioned peptide or the salt thereof, which comprises subjecting a peptide represented by formula (II) or a salt thereof to an oxidation reaction:M-P-Cys-Q-R-S-T-Asp-U-Glu-Cys-Val-Tyr-V-Cys-His-W-X-Y-Ile-Z-OH(II)wherein M, P, Q, R, S, T, U, V, W, X, Y and Z are as diefined above; and (3) use of the above-mentioned peptide or the pharmaceutically acceptable salt thereof as an anti-endothelin agent.
摘要翻译：公开了由式（I）表示的肽或其药学上可接受的盐：巯基酰基; P，Q，R，S，T，U，V，W，X，Y和Z各自表示氨基酸残基，其中Y的氨基酸侧链是具有1至15个碳原子的取代的饱和脂族烃基或除（1S）-1-甲基丙基以外具有4〜15个碳原子的未取代的饱和脂肪族烃基; （2）上述肽或其盐的制造方法，其特征在于，将由式（II）表示的肽或其盐进行氧化反应：MP-Cys-QRST-Asp-U-Glu-Cys 其中M，P，Q，R，S，T，U，V，W，X，Y和Z的Val-Tyr-V-Cys-His-WXY-Ile-Z-OH（II）和（3）使用上述肽或其药学上可接受的盐作为抗内皮素剂。

2. 发明授权

US5306808A Peptide derivatives having vasodilating activity 失效
标题翻译：具有血管扩张活性的肽衍生物
公开(公告)号：US5306808A
公开(公告)日：1994-04-26
申请号：US768269
申请日：1991-10-17
申请人： Mitsuhiro Wakimasu , Takashi Kikuchi , Kazuki Kubo
发明人： Mitsuhiro Wakimasu , Takashi Kikuchi , Kazuki Kubo
IPC分类号： A61K38/00 , C07K14/575 , C07K7/10
CPC分类号： C07K14/57536 , A61K38/00
摘要： Disclosed are a peptide derivative represented by the formula [I] or a pharmaceutically acceptable salt thereof: ##STR1## wherein A, B, C, D, E and F each represent amino acid residues, and satisfy any one condition of (i) A=Ser, B=Ser, C=Ser, D=Leu, E=Met and F=Phe, (ii) A=Ser, B=Ser, C=Ser, D=Trp, E=Leu and F=Phe, and (iii) A=Thr, B=Phe, C=Thr, D=Tyr, E=Lys and F=Tyr; and W, X, Y and Z each represent amino acid residues, and satisfy any one condition of (i) at least one of W and Y is an amino acid residue other than an L-alanine residue or other than an L-cysteine residue, (ii) X is an amino acid residue other than an L-Lysine residue, and (iii) Z is an amino acid residue other than an L-aspartic acid residue; (2) a method for producing the peptide derivative or the salt thereof; and (3) an agent for improving a circulatory function mainly comprising the peptide derivative or the salt thereof, such as a vasodilator or a vasoconstrictor.
摘要翻译： PCT No.PCT / JP91 / 00165 Sec。 371日期1991年10月17日 102（e）日期1991年10月17日PCT 1991年2月12日提交PCT公布。出版物WO91 / 13089 1991年9月5日公开。公开是由式（I）表示的肽衍生物或其药学上可接受的盐：（*化学结构*）-Ile-Ile-Trp-OH其中A，B，C，D，E （i）A = Ser，B = Ser，C = Ser，D = Leu，E = Met和F = Phe的任何一个条件，（ii）A = Ser，B = Ser，C = Ser，D = Trp，E = Leu和F = Phe，和（iii）A = Thr，B = Phe，C = Thr，D = Tyr，E = Lys和F = Tyr; 并且W，X，Y和Z各自表示氨基酸残基，并且满足（i）W和Y中的至少一个是L-丙氨酸残基以外的氨基酸残基或L-半胱氨酸残基以外的任一条件，（ii）X是除L-赖氨酸残基以外的氨基酸残基，（iii）Z是除了L-天冬氨酸残基以外的氨基酸残基; （2）生成肽衍生物或其盐的方法; 和（3）主要由肽衍生物或其盐例如血管扩张剂或血管收缩剂改善循环功能的药剂。

3. 发明授权

US06346604B1 Method for controlling conformation of cyclopentapeptide 失效
标题翻译：控制环戊肽构象的方法
公开(公告)号：US06346604B1
公开(公告)日：2002-02-12
申请号：US08969007
申请日：1997-11-12
申请人： Mitsuhiro Wakimasu , Hiroshi Inooka , Satoshi Endo , Takashi Kikuchi
发明人： Mitsuhiro Wakimasu , Hiroshi Inooka , Satoshi Endo , Takashi Kikuchi
IPC分类号： C07K102
CPC分类号： C07K7/64 , A61K38/00
摘要： Cyclic pentapeptides having a &ggr;-turn and a &bgr;-turn wherein the cyclic pentapeptide has the following formula (I): Cyclo(—A1—A2—A3—A4—A5—) (I) wherein A1, A2, A3, A4 and A5 are amino acid residues; said pentapeptide having amino acid residues in positions 1-2-3 to form a &ggr;-turn, and amino acid residues in positions 3-4-5-1 to form a &bgr;-turn in combination with the &ggr;-turn; in which D-&agr;-amino acid residues are selected for A1, A3 and A5 and L-&agr;-amino acid residues are selected for A2 and A4 or wherein L-&agr;-amino acid residues are selected for A1, A3 and A5 and D-&agr;-amino acid residues are selected for A2 and A4; are provided. Compounds having &ggr;-turns and &bgr;-turns can be systhesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of &bgr;-turn and &ggr;-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.
摘要翻译：具有γ-匝和β-匝的环状五肽，其中环状五肽具有下式（I）：其中A1，A2，A3，A4和A5是氨基酸残基;所述五肽在1-2位具有氨基酸残基 -3以形成γ-匝数，以及位置3-4-5-1处的氨基酸残基与γ匝组合形成β-匝数;其中选择D-α-氨基酸残基用于A1， A2和A4选择A3和A5和L-α-氨基酸残基，或选择A1，A3和A5的L-α-氨基酸残基，A2和A4选择D-α-氨基酸残基; 具有γ-匝数和β-匝数的化合物可以被控制，而不管氨基酸残基的种类如何，并且可以合成将期望的氨基酸残基引入β-匝和γ-匝的位点的化合物基于它们从生物活性的角度的重要性。因此，本发明可用于设计具有生物活性的化合物。

4. 发明授权

US5948754A Cyclic hexapeptides, their production and use 失效
标题翻译：循环六肽，其生产和使用
公开(公告)号：US5948754A
公开(公告)日：1999-09-07
申请号：US739810
申请日：1996-10-30
申请人： Mitsuhiro Wakimasu , Takashi Kikuchi , Akira Kawada
发明人： Mitsuhiro Wakimasu , Takashi Kikuchi , Akira Kawada
IPC分类号： A61K38/00 , C07K14/575 , A61K38/12 , C07K7/64
CPC分类号： C07K14/57536 , A61K38/00
摘要： A cyclic hexapeptide represented by the formula:cyclo�A--Asp(R.sup.1)--Y--NH--CHR.sup.2 --CO--C--D--Trp(N.sup.in --R.sup.3)--! (I)wherein A is a D-acidic-.alpha.-amino acid residue; Y is an acidic-.alpha.-amino acid residue; C is an L-.alpha.-amino acid residue; R.sup.1 is a group represented by the formula: ##STR1## wherein X.sup.1 and X.sup.2 are independently H, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or nitro, and may bind together to form a ring in cooperation with the adjacent carbon atom; R.sup.2 is C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkyl-C.sub.1-3 alkyl, C.sub.1-6 alkylthio-C.sub.1-3 alkyl, C.sub.3-7 cycloalkylthio-C.sub.1-3 alkyl, C.sub.1-5 alkoxy-C.sub.1-3 alkyl, C.sub.3-7 cycloalkoxy-C.sub.1-3 alkyl, C.sub.1-6 alkylthio, C.sub.3-7 cycloalkylthio, C.sub.1-5 alkoxy or C.sub.3-7 cycloalkoxy; R.sup.3 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, --COR.sup.4, --COOR.sup.5 or --CONHR.sup.6 ; when X.sup.1, X.sup.2 and R.sup.3 are all hydrogen atoms, R.sup.2 is not an isobutyl group, or a salt thereof, which exhibits excellent antagonistic action against endothelin receptors, particularly endothelin B receptors.
摘要翻译：由式：环[A-Asp（R1）-Y-NH-CHR2-CO-CD-Trp（Nin-R3） - ]（I）表示的环状六肽其中A是D-酸性α-氨基酸残留物 Y是酸性α-氨基酸残基; C是L-α-氨基酸残基; R1是由下式表示的基团：其中X1和X2独立地是H，C1-6烷基，C1-6烷氧基，卤素或硝基，并且可以与相邻的碳原子一起结合形成环; R 2是C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1-3烷基，C 1-6烷硫基-C 1-3烷基，C 3-7环烷硫基-C 1-3烷基，C 1-5烷氧基-C 1-3 烷基，C 3-7环烷氧基-C 1-3烷基，C 1-6烷硫基，C 3-7环烷硫基，C 1-5烷氧基或C 3-7环烷氧基; R3是H，C1-6烷基，C3-7环烷基，-COR4，-COOR5或-CONHR6; 当X1，X2和R3都是氢原子时，R2不是对内皮素受体，特别是内皮素B受体具有优异拮抗作用的异丁基或其盐。

5. 发明授权

US5616684A Cyclic peptides and use thereof 失效
标题翻译：循环肽及其用途
公开(公告)号：US5616684A
公开(公告)日：1997-04-01
申请号：US231449
申请日：1994-04-20
申请人： Mitsuhiro Wakimasu , Takashi Kikuchi , Akira Kawada , Hideo Shirafuji
发明人： Mitsuhiro Wakimasu , Takashi Kikuchi , Akira Kawada , Hideo Shirafuji
IPC分类号： A61K38/00 , A61P3/06 , A61P9/00 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P29/00 , A61P35/00 , C07K7/64 , C07K14/575
CPC分类号： C07K14/57536 , C07K7/64 , A61K38/00 , Y02P20/55
摘要： Cyclic peptides and their salts have antagonistic activity on endothelin receptors and antagonistic activity on NK2 receptors. The peptides have the formula ##STR1## wherein X and Y each represent .alpha.-amino acid residues, A represents a D-acidic-.alpha.-amino acid residue, B represents a neutral .alpha.-amino acid residue, C represents an L-.alpha.-amino acid residue and D represents a D-.alpha.-amino acid residue having an aromatic ring group; wherein hydroxy, thiol, amino, imino and carboxyl groups can be substituted or unsubstituted. Pharmaceutical compositions containing such peptides are also described.
摘要翻译：环肽及其盐对内皮素受体具有拮抗作用，对NK2受体具有拮抗作用。肽具有下式：其中X和Y各自表示α-氨基酸残基，A表示D-酸性-α-氨基酸残基，B表示中性α-氨基酸残基，C表示L - α-氨基酸残基，D表示具有芳环基团的D-α-氨基酸残基; 其中羟基，硫醇，氨基，亚氨基和羧基可以是取代或未取代的。还描述了含有这些肽的药物组合物。

6. 发明授权

US5883075A Cyclic endothelin antagonists 失效
标题翻译：循环内皮素拮抗剂
公开(公告)号：US5883075A
公开(公告)日：1999-03-16
申请号：US680534
申请日：1996-07-09
申请人： Mitsuhiro Wakimasu , Takashi Kikuchi , Akira Kawada , Hideo Shirafuji
发明人： Mitsuhiro Wakimasu , Takashi Kikuchi , Akira Kawada , Hideo Shirafuji
IPC分类号： A61K38/00 , A61P3/06 , A61P9/00 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P29/00 , A61P35/00 , C07K7/64 , C07K14/575 , A61K38/12
CPC分类号： C07K14/57536 , C07K7/64 , A61K38/00 , Y02P20/55
摘要： Disclosed are (1) a cyclic hexapeptide represented by formula I or a salt thereof: ##STR1## wherein X and Y each represent .alpha.-amino acid residues, A represents a D-acidic-.alpha.-amino acid residue, B represents a neutral-.alpha.-amino acid residue, C represents an L-.alpha.-amino acid residue and D represents a D-.alpha.-amino acid residue having an aromatic ring group; and (2) a pharmaceutical composition comprising the peptide represented by formula I or a pharmaceutically aceptable salt thereof as an active ingredient.
摘要翻译：公开了（1）由式I表示的环状六肽或其盐：其中X和Y各自表示α-氨基酸残基，A表示D-酸性-α-氨基酸残基，B表示中性 α-氨基酸残基，C代表L-α-氨基酸残基，D代表具有芳环基团的D-α-氨基酸残基; 和（2）包含由式I表示的肽或其药学上可接受的盐作为活性成分的药物组合物。

7. 发明授权

US06610655B2 Pentapeptide with specific conformation, its production and use 失效
标题翻译：具有特定构象的五肽，其生产和使用
公开(公告)号：US06610655B2
公开(公告)日：2003-08-26
申请号：US09999432
申请日：2001-11-15
申请人： Mitsuhiro Wakimasu , Hiroshi Inooka , Satoshi Endo , Takashi Kikuchi
发明人： Mitsuhiro Wakimasu , Hiroshi Inooka , Satoshi Endo , Takashi Kikuchi
IPC分类号： C07K102
CPC分类号： C07K7/64 , A61K38/00
摘要： Cyclic pentapeptides are disclosed having the following formula (I)-Cyclo(-A1-A2-A3-A4-A5-)-wherein A1, A2, A3, A4 and A5 are amino acid residues. The pentapeptide has amino acid residues in positions 1-2-3 to form a &ggr;-turn, and amino acid residues in positions 3-4-5-1 to form a &bgr;-turn in combination with the &ggr;-turn. D-&agr;-amino acid residues are selected for A1, A3, and A5 and L-&agr;-amino acid residues are selected for A2 and A4. Compounds having &ggr;-turns and &bgr;-turns can be synthesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of &bgr;-turn and &ggr;-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.
摘要翻译：公开了具有下式（I）-Cyclo（-A1-A2-A3-A4-A5-））的环五肽 - 其中A1，A2，A3，A4和A5是氨基酸残基。五肽在1-2-3位具有氨基酸残基以形成γ-转角，并且3-4-5-1位置的氨基酸残基与γ转弯结合形成β-转角。选择A1，A3和A5的D-α-氨基酸残基，A2和A4选择L-α-氨基酸残基。可以合成具有γ-匝数和β-匝数的化合物，而不考虑氨基酸残基的种类，并且可以合成其中所需氨基酸残基被引入β-匝和γ-匝转位点的化合物从生物活动的角度来看重要。因此，本发明可用于设计具有生物活性的化合物。

8. 发明授权

US5965526A Pentapeptide with specific conformation, its production and use 失效
标题翻译：具有特定构象的五肽，其生产和使用
公开(公告)号：US5965526A
公开(公告)日：1999-10-12
申请号：US551251
申请日：1995-10-31
申请人： Mitsuhiro Wakimasu , Hiroshi Inooka , Satoshi Endo , Takashi Kikuchi
发明人： Mitsuhiro Wakimasu , Hiroshi Inooka , Satoshi Endo , Takashi Kikuchi
IPC分类号： A61K38/00 , C07K1/00 , C07K7/64 , A61K38/12
CPC分类号： C07K7/64 , C07K1/00 , A61K38/00
摘要： Cyclic pentapeptides are disclosed having the following formula (I) --Cyclo(-A.sub.1 -A.sub.2 -A.sub.3 -A.sub.4 -A.sub.5 -)-- wherein A.sub.1, A.sub.2, A.sub.3, A.sub.4 and A.sub.5, are amino acid residues. The pentapeptide has amino acid residues in positions 1-2-3 to form a .gamma.-turn, and amino acid residues in positions 3-4-5-1 to form a .beta.-turn in combination with the .gamma.-turn. D-.alpha.-amino acid residues are selected for A.sub.1, A.sub.3, and A.sub.5 and L-.alpha.-amino acid residues are selected for A.sub.2 and A.sub.4. Compounds having .gamma.-turns and .beta.-turns can be synthesized, regardless of the kinds of amino acid residues, and it is possible to synthesize compounds in which desired amino acid residues are introduced into sites of .beta.-turn and .gamma.-turn based on their importance from the viewpoint of biological activity. The present invention is therefore available for design of compounds having biological activity.
摘要翻译：公开了具有下式（I）-Cyclo（-A1-A2-A3-A4-A5-））的环五肽，其中A1，A2，A3，A4和A5是氨基酸残基。五肽在1-2-3位具有氨基酸残基以形成γ转角，并且3-4-5-1位置的氨基酸残基与γ转角组合形成β转角。 A1，A3和A5选择D-α-氨基酸残基，A2和A4选择L-氨基酸残基。可以合成具有γ-转角和β-转角的化合物，而不管氨基酸残基的种类如何，并且可以合成其中所需氨基酸残基被引入β-转角和γ转角的位点的化合物，基于它们从生物活动的角度来看重要。因此，本发明可用于设计具有生物活性的化合物。

9. 发明授权

US6147051A Methods and compositions for the prophylactic and/or therapeutic treatment of organ hypofunction 失效
标题翻译：用于器官功能减退的预防和/或治疗的方法和组合物
公开(公告)号：US6147051A
公开(公告)日：2000-11-14
申请号：US561096
申请日：1995-11-21
申请人： Toshifumi Watanabe , Mitsuhiro Wakimasu , Chieko Kitada
发明人： Toshifumi Watanabe , Mitsuhiro Wakimasu , Chieko Kitada
IPC分类号： A61K31/19 , A61K31/496 , A61K31/505 , A61K38/04 , A61K38/12
CPC分类号： A61K38/12 , A61K31/19 , A61K31/496 , A61K31/505 , A61K38/04
摘要： Compounds having antagonistic activity on endothelin receptors can be effectively used for prophylaxis and/or treatment of hypofunction of organs which occurs in their surgery or transplant.
摘要翻译：对内皮素受体具有拮抗作用的化合物可以有效地用于预防和/或治疗其手术或移植中出现的器官的功能低下。

10. 再颁专利

USRE35886E Phosphonic acid derivatives and use thereof 失效
标题翻译：膦酸衍生物及其用途
公开(公告)号：USRE35886E
公开(公告)日：1998-09-01
申请号：US680295
申请日：1996-07-12
申请人： Mitsuhiro Wakimasu , Masaaki Mori , Akira Kawada
发明人： Mitsuhiro Wakimasu , Masaaki Mori , Akira Kawada
IPC分类号： A61K38/00 , A61K38/55 , A61P9/00 , A61P9/12 , A61P13/02 , A61P15/00 , C07K1/06 , C07K1/113 , C07K5/06 , C07F9/22 , A61K33/42
CPC分类号： C07K5/06191 , A61K38/00 , Y02P20/55
摘要： A phosphonic acid derivative compound represented by formula �I ! or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrocarbon groups which may be substituted, except cases in which (1) R.sub.2 is unsubstituted methyl, ( 2 ) R.sub.3 is an unsubstituted hydrocarbon group having 1 to 3 carbon atoms, and (3) R.sub.1 is benzyloxycarbonylaminomethyl, R.sub.2 is isobutyl and R.sub.3 is isobutyl or phenylmethyl, which has endothelin-converting enzyme inhibiting activity and is useful as pharmaceutical drugs such as therapeutic agents for hypertension, cardiac or cerebral circulatory diseases and renal diseases. This is a Reissue of a Patent which was the subject of a Reexamination Certificate No. B1 5,330,978, dated Jun. 18, 1996, Request No. 90/00400, Oct. 18, 1995.
摘要翻译：由式[I]表示的膦酸衍生物或其药学上可接受的盐：其中R 1，R 2和R 3各自表示可以被取代的烃基，除了（1）R 2是未取代的甲基，（2）R3为未取代的碳原子数1〜3的烷基，（3）R1为苄氧羰基氨基甲基，R2为异丁基，R3为异丁基或苯甲基，具有内皮素转化酶抑制活性，可用作药物作为高血压，心脏或脑循环系统疾病和肾脏疾病的治疗剂。 + PR这是1996年10月18日，1996年10月18日申请号90/00400的1996年6月18日的复审证书B1 5,330,978的主题的重新发行。

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