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公开(公告)号:US4382923A
公开(公告)日:1983-05-10
申请号:US311899
申请日:1981-10-15
IPC分类号: C07K1/06 , A61K38/00 , A61P25/04 , C07C231/00 , C07K5/10 , C07K5/107 , C07K14/575 , C07K14/655 , A61K37/00 , C07C103/52
CPC分类号: C07K5/1016 , Y02P20/55 , Y10S514/80
摘要: Novel tetrapeptide acylhydrazides, inclusive of acid addition salts thereof, which have the formula: ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is lower alkyl; are useful as analgesics.
摘要翻译: 新型四肽酰基酰肼,包括其酸加成盐,其具有下式:其中R 1是氢或甲基,R 2是低级烷基; 作为镇痛剂是有用的。
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2.
公开(公告)号:US4337247A
公开(公告)日:1982-06-29
申请号:US213683
申请日:1980-12-05
IPC分类号: C07K5/10 , A61K38/00 , A61P25/04 , C07K1/06 , C07K5/087 , C07K5/107 , C07K14/575 , C07K14/655 , C07K14/70 , A61K37/00 , C07C103/52
CPC分类号: C07K5/0812 , C07K5/1016 , Y02P20/55
摘要: Novel tetrapeptidesemicarbazide derivatives, inclusive of a pharmacologically acceptable salt thereof, which has the general formula (I): ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or a D-.alpha.-amino acid side chain; R.sub.3 is hydrogen or lower alkyl; X is oxygen or sulfur, are useful as analgesics.
摘要翻译: 具有通式(I)的新型四肽氨基脲衍生物,包括其药理学上可接受的盐:其中R 1是氢或低级烷基; R2是氢或D-α-氨基酸侧链; R3是氢或低级烷基; X是氧或硫,可用作镇痛剂。
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公开(公告)号:US4073890A
公开(公告)日:1978-02-14
申请号:US726052
申请日:1976-09-23
CPC分类号: C07K5/1019 , C07K14/62 , C07K5/0812 , A61K38/00
摘要: Novel polypeptides of the formulaR.sub.1 --Arg--R.sub.2 --Phe--Phe--R.sub.3wherein R.sub.1 is hydrogen, or a basic or neutral amino acid residue, R.sub.2 is a neutral amino acid residue and R.sub.3 is NH.sub.2, Tyr--NH.sub.2, a residue of tyrosyl peptides consisting of 1 to 5 amino acid residues or amides of the tyrosyl peptides, provided that when R.sub.1 is hydrogen, R.sub.2 is Pro, are effectively used for treatment of insufficiency of carbohydrate metabolism and of lipid metabolism, especially for the treatment of diabetes by not only parenteral administration but also oral administration.
摘要翻译: 式R1-Arg-R2-Phe-Phe-R3的新型多肽,其中R1是氢,或碱性或中性氨基酸残基,R2是中性氨基酸残基,R3是NH2,Tyr-NH2,酪氨酰基的残基 由酪氨酰肽的1至5个氨基酸残基或酰胺组成的肽,条件是当R1为氢时,R2为Pro,可有效用于治疗碳水化合物代谢和脂质代谢不足,特别是用于治疗糖尿病 只有肠胃外给药,而且口服。
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4.
公开(公告)号:US4001199A
公开(公告)日:1977-01-04
申请号:US560092
申请日:1975-03-19
IPC分类号: C07K7/06 , A61K38/00 , A61K38/04 , A61K38/28 , A61P3/10 , C07K5/097 , C07K5/11 , C07K14/62 , C07C103/52 , A61K37/00
CPC分类号: C07K14/62 , C07K5/0821 , A61K38/00
摘要: Novel polypeptides of the formulaR.sub.1 --Arg--R.sub.2 --Phe--Phe--R.sub.3wherein R.sub.1 is hydrogen, or a basic or neutral amino acid residue, R.sub.2 is a neutral amino acid residue and R.sub.3 is NH.sub.2, Tyr--NH.sub.2, a residue of tyrosyl peptides consisting of 1 to 5 amino acid residues or amides of the tyrosyl peptides, provided that when R.sub.1 is hydrogen, R.sub.2 is Pro, are effectively used for treatment of insufficiency of carbohydrate metabolism and of lipid metabolism, especially for the treatment of diabetes by not only parenteral administration but also oral administration.
摘要翻译: 式R1-Arg-R2-Phe-Phe-R3的新型多肽,其中R1是氢,或碱性或中性氨基酸残基,R2是中性氨基酸残基,R3是NH2,Tyr-NH2,酪氨酰基的残基 由酪氨酰肽的1至5个氨基酸残基或酰胺组成的肽,条件是当R1为氢时,R2为Pro,可有效用于治疗碳水化合物代谢和脂质代谢不足,特别是用于治疗糖尿病 只有肠胃外给药,而且口服。
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公开(公告)号:US4358440A
公开(公告)日:1982-11-09
申请号:US226600
申请日:1981-01-21
IPC分类号: C07K14/655 , A61K38/00 , A61K38/22 , A61P25/04 , C07K1/06 , C07K14/575 , C07K14/675 , A61K37/00 , C07C103/52
CPC分类号: C07K14/675 , A61K38/00 , Y02P20/55 , Y10S514/809
摘要: Novel polypeptide of the formula:H-Tyr-Gly-Gly-Phe-Met-Lys-Pro-Tyr-Thr-Lys-Gln-Ser-His-Lys-Pro-Leu-Ile-Thr-Leu-Leu-Lys-His-Ile-Thr-Leu-Lys-Asn-Glu-Gln-OH is useful as an analgesic agent. Methods of its preparation are also disclosed.
摘要翻译: 下式的新型多肽:H-Tyr-Gly-Gly-Phe-Met-Lys-Pro-Tyr-Thr-Lys-Gln-Ser-His-Lys-Pro-Leu-Ile-Thr-Leu-Leu-Lys- His-Ile-Thr-Leu-Lys-Asn-Glu-Gln-OH可用作止痛剂。 还公开了其制备方法。
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6.
公开(公告)号:US3959245A
公开(公告)日:1976-05-25
申请号:US345328
申请日:1973-03-27
申请人: Nobuo Nakajima , Hisashi Aoki , Masahiko Fujino , Osamu Nishimura , Mitsuhiro Wakimasu , Mitsuhiko Mano
发明人: Nobuo Nakajima , Hisashi Aoki , Masahiko Fujino , Osamu Nishimura , Mitsuhiro Wakimasu , Mitsuhiko Mano
IPC分类号: A23L27/30 , C07K5/072 , C07K5/075 , A23L1/22 , C07C103/52
CPC分类号: C07K5/06113 , A23L27/32 , Y10S530/801
摘要: A novel dipeptide, L-aspartyl-aminomalonic acid methyl 2-methylcyclohexyl diester and its physiologically acceptable salts which are useful as a sweetener, and production thereof and sweetening compositions containing the dipeptide or its salt.
摘要翻译: 可用作甜味剂的新型二肽,L-天冬氨酰基 - 氨基马来酸甲基2-甲基环己基二酯及其生理学上可接受的盐及其生产物和含有二肽或其盐的甜味组合物。
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公开(公告)号:US5159061A
公开(公告)日:1992-10-27
申请号:US101199
申请日:1987-09-25
IPC分类号: C07K7/08 , A61K38/00 , A61P7/10 , A61P9/00 , A61P9/12 , A61P21/02 , C07K1/00 , C07K1/02 , C07K1/113 , C07K14/00 , C07K14/575 , C07K14/58 , C07K14/60 , D02G3/02 , D02G3/06 , D02G3/44
CPC分类号: C07K14/58 , C07K14/582 , C07K14/60 , A61K38/00
摘要: A peptide derivative of the formula ##STR1## wherein A is hydrogen or a hydrocarbon acyl having 2 to 18 carbon atoms which is substituted by an amino group at the .alpha.-position; B is F-Gly wherein F is a neutral .alpha.-amino acid residue, or NH-(CH.sub.2)nCO wherein n is an integer of 1 to 4; C is a neutral .alpha.-amino acid residue; and E is L-Arg or D-Arg; when A, B and C are hydrogen, Gly-Gly, and Met or Ile, respectively, E is D-Arg, or its pharmacologically acceptable salt has strong hypotensive and natriuretic activity; therefore it is useful as a therapeutic drug for hypertension, a diuretic, and a therapeutic drug for cardiac and cerebral circulatory diseases.
摘要翻译: 其中A是氢或具有2至18个碳原子的烃基,其被α-位上的氨基取代, ; B是F-Gly,其中F是中性α-氨基酸残基或NH-(CH 2)n CO,其中n是1至4的整数; C是中性α-氨基酸残基; 且E为L-Arg或D-Arg; 当A,B和C分别为氢,Gly-Gly和Met或Ile时,E为D-Arg,或其药理学上可接受的盐具有强烈的降血压和利尿钠活性; 因此作为心血管和脑循环系统疾病的高血压,利尿剂,治疗药物的治疗药物是有用的。
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公开(公告)号:US4476051A
公开(公告)日:1984-10-09
申请号:US436691
申请日:1982-10-26
IPC分类号: C07C43/205 , C07C231/00 , C07C311/29 , C07D233/54 , C07K1/06 , C07K5/083 , C07K5/097 , C07K14/00 , C07K14/575 , C07C103/52
CPC分类号: C07D233/64 , C07C309/00 , C07C43/205 , C07K1/063 , C07K1/064 , C07K14/57572 , C07K5/0806 , C07K5/0821 , Y02P20/55
摘要: An .omega.-amino group and/or .alpha.-amino group in an amino acid or a peptide can be protected with a 4-methoxy-2,3,6-trimethylbenzenesulfonyl group, and said group may easily be removed without affecting the amino acid or the peptide. Thus, the present invention is useful in the synthesis of peptide containing .omega.-amino group and/or .alpha.-amino group.
摘要翻译: 氨基酸或肽中的ω-氨基和/或α-氨基可以用4-甲氧基-2,3,6-三甲基苯磺酰基保护,并且所述基团可以容易地除去而不影响氨基酸或 肽。 因此,本发明可用于合成含有ω-氨基和/或α-氨基的肽。
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公开(公告)号:US4206199A
公开(公告)日:1980-06-03
申请号:US924553
申请日:1978-07-14
IPC分类号: C07K14/605 , A61K39/00 , A61K37/00 , C07C103/52
CPC分类号: C07K14/605
摘要: (a) A novel glucagon fragment (15-29) of the formula:H-Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asn-Thr-OH,(b) a novel product obtained by conjugating the glucagon fragment (15-29) with bovine serum albumin by means of glutalaldehyde,(c) a novel antibody specifically reactive to pancreatic glucagon produced by administering to a mammalian animal the product of the above (b), and(d) a novel peptide of the formula ##STR1## wherein R.sub.1 and R.sub.2 respectively mean H or radioactive I, R.sub.3 is an alkane residue having up to 4 carbon atoms which may optionally have NH.sub.2 or OH, R.sub.4 is a peptide fragment corresponding to the 1 to 5 amino acid residues ending with the 19-alanyl of pancreatic glucagon, and R.sub.5 is Met or Nle, being efficiently useful for estimation by radioimmunoassay of pancreatic glucagon levels in blood together with the antibody of the above (c).
摘要翻译: (a)下式的新型胰高血糖素片段(15-29):H-Asp-Ser-Arg-Arg-Ala-Gln-Asp-Phe-Val-Gln-Trp-Leu-Met-Asn-Thr-OH, (b)通过用戊二醛与胰高血糖素片段(15-29)与牛血清白蛋白缀合而获得的新产品,(c)通过向哺乳动物施用上述产物而产生的对胰高血糖素特异性反应的新型抗体 b)和(d)下式的新型肽:其中R 1和R 2分别表示H或放射性I,R 3是具有至多4个碳原子的烷烃残基,其可任选地具有NH 2或OH R4是与胰高血糖素的19-丙氨酸结合的1至5个氨基酸残基相对应的肽片段,R5是Met或Nle,可有效地用于通过放射免疫测定血液中的胰高血糖素水平与抗体 以上(c)。
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公开(公告)号:US4277394A
公开(公告)日:1981-07-07
申请号:US90021
申请日:1979-10-31
IPC分类号: C07K5/107 , C07C103/52 , A61K37/00 , C07G7/00
CPC分类号: C07K5/1016 , Y10S514/809
摘要: Novel tetrapeptidehydrazide derivatives, inclusive of a pharmacologically acceptable acid addition salt thereof, which has the general formula (I): ##STR1## [wherein R.sub.1 is hydrogen or lower alkyl; R.sub.2 is hydrogen or the side chain of a D-.alpha.-amino acid; R.sub.3 is hydrogen or lower alkyl; R.sub.4 is hydrogen, or a saturated or unsaturated and straight or branched lower aliphatic acyl group which may optionally be substituted by hydroxy, amino, lower alkoxy, halogen, oxo, lower alkylthio or lower alkylthiooxide], are useful as analgesics.
摘要翻译: 具有通式(I)的新型四肽酰肼衍生物,包括其药理学上可接受的酸加成盐:其中R 1是氢或低级烷基; R2是氢或D-α-氨基酸的侧链; R3是氢或低级烷基; R4是氢或可以被羟基,氨基,低级烷氧基,卤素,氧代,低级烷硫基或低级烷硫基氧化物任选取代的饱和或不饱和的直链或支链低级脂族酰基)可用作止痛剂。
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