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1. 发明公开

EP1695718A3 Biodegradable polyester and Ionic molecular conjugates of biodegradable polyesters and bioactive polypeptides 审中-公开
标题翻译： Polylogisch abbaubarer Polyester und Ionische Konjugate dieses Polyester mit bioaktiven Polypeptiden
公开(公告)号：EP1695718A3
公开(公告)日：2007-01-17
申请号：EP06075178.1
申请日：2000-01-26
申请人： Société de Conseils de Recherches et d'Applications Scientifiques, S.A.S. , Poly-Med, Inc.
发明人： Shalaby, Shalaby W. , Moreau, Jacques-Pierre , Jackson, Steven A.
IPC分类号： A61K47/48 , C08G63/02 , C08G63/06 , C08G63/08 , C08L67/04 , C08L67/02
CPC分类号： C07K7/23 , A61K38/00 , A61K47/593 , C07K14/655 , C08G63/06 , C08G63/08 , C08G63/64 , Y10S514/80 , Y10S514/806 , Y10S514/807 , Y10S514/808 , Y10S514/809
摘要： Disclosed is a sustained release pharmaceutical composition. The composition includes a polyester containing a free COOH group ionically conjugated with a bioactive polypeptide comprising at least one effective ionogenic amine, wherein at least 50% by weight of the polypeptide present in the composition is ionically conjugated to the polyester.
摘要翻译：公开了缓释药物组合物。所述组合物包括含有游离COOH基团的聚酯，所述游离COOH基团与包含至少一种有效的离子型胺的生物活性多肽离子地缀合，其中所述组合物中存在的多肽的至少50重量％与所述聚酯离子共轭。

2. 发明公开

EP0136720A3 Enkephalin analogs 有权
标题翻译：脑啡肽类似物
公开(公告)号：EP0136720A3
公开(公告)日：1987-05-06
申请号：EP84111914
申请日：1984-10-04
申请人： G.D. Searle & Co.
发明人： Hansen, Donald Willis, Jr. , Jones, David Ackley, Jr. , Mazur, Robert Henry , Schlatter, James Myron
IPC分类号： C07K05/10 , A61K37/02
CPC分类号： C07K5/1016 , Y10S514/809
摘要： The invention relates to novel enkephalin analogs of the formula:
which are useful as analgesic agents.
摘要翻译：本发明涉及下式的新型脑啡肽类似物：其可用作止痛剂。

3. 发明公开

EP0125469A1 Conformationally constrained cyclic enkephalin analogs with delta receptor specificity 失效
标题翻译：三角洲受体特异性循环Enkephalinanaloge具有刚性构象。
公开(公告)号：EP0125469A1
公开(公告)日：1984-11-21
申请号：EP84103793.0
申请日：1984-04-05
申请人： GIBSON-STEPHENS INSTITUTE
发明人： Hruby, Victor J. , Mosberg, Henry
IPC分类号： C07K7/12 , A61K37/02
CPC分类号： C07K14/702 , A61K38/00 , Y10S514/809 , Y10S930/26
摘要： Novel compounds which are capable of binding with enhanced specificity to the delta receptor are disclosed. The compounds are a series of cyclic, conformationally constrained analogs of enkephalins which display exceptional delta receptor specificity. The compounds of the present invention are polypeptides of the formula:
wherein R' and R 2 , which may be the same or different, are hydrogen, methyl, or lower alkyl having 1 to 5 carbon atoms;

R 3 and R 4 , which may be the same or different, are hydrogen, methyl, or lower alkyl having 1 to 5 carbon atoms, provided, however, that R 1 , R 2 , R 3 , and R 4 may not all be hydrogen when both n and m are zero;
R 5 is hydrogen, L-tyrosine, D-tyrosine, or L-tyrosine or D-tyrosine substituted on the Na-amino with 1 or 2 lower alkyl or alkenyl groups;
R 6 is a substituted or unsubstituted aromatic;
R 7 is hydrogen or methyl;
R 8 is carboxylate, carboxamide or amino acid residue; provided, however, that where m and n are zero; and R' and R 2 are both methyl groups; and R 3 and R 4 are both hydrogen; and R 7 is hydrogen; R 8 is an amino acid residue;
X and Y are hydrogen or methyl; and,
n and m, which may be the same or different, are 0 or 1.

The novel compounds include those which have either agonist or antagonist activity. The compounds may be used to induce pharmacological or therapeutic effects, including analgesia, in humans and other animals.

4. 发明公开

EP0050503A1 Pharmacologically active pentapeptide derivatives 有权
标题翻译：药理学活性的五肽衍生物。
公开(公告)号：EP0050503A1
公开(公告)日：1982-04-28
申请号：EP81304860.0
申请日：1981-10-19
申请人： ELI LILLY AND COMPANY
发明人： Gesellchen, Paul David , Shuman, Robert Theodore
IPC分类号： C07C103/52 , A61K37/02
CPC分类号： C07K14/702 , Y10S514/809
摘要： Compounds of the formula
and pharmaceutically acceptable non-toxic acid addition salts thereof, in which

R is hydrogen, methyl, or ethyl;
A is the residue of a D-amino acid selected from Ala, Abu, Nva, Val, Nle, Leu, Ile, Gly(Al), Gly(Cp), Met, Cys(Me), Met(O), Cys(Me) (0), Ser, Thr, and Hse;
R 1 is hydrogen, C 1 -C 3 primary alkyl, cyclopropylmethyl, allyl, or propargyl;
X is bromo, iodo, chloro, C 1 -C 3 alkyl, trifluoromethyl, or C 1 -C 2 alkoxy;
B is the residue of a D- or L-amino acid lacking its carboxyl moiety and selected from

Gly, Ala, Abu, Nva, Val, Nle, Leu, lie, Pgl, Cys(Me), Cys(Me) (0), Cys(Me) (0 2 ), Cys(Et), Cys(Et) (0), Cys(Et) (0 2 ), Met, Met(O), Met(O 2 ), Eth, Eth(O), Eth(O 2 ), Ser(Me), Ser(Et), Hse(Me), and Hse(Et) as well as any of such residues substituted at the amino nitrogen by a C 1 -C 3 primary alkyl; Z is -CH 2 OR 2 ,
in which R 2 is hydrogen or C 1 -C 3 alkyl; subject to the proviso that, when R 1 is other than hydrogen, B is the residue of an amino acid that lacks substitution at the amino nitrogen; which are useful analgesic agents, are described.

5. 发明公开

EP0034721A2 Polypeptide and its production and use 失效
标题翻译： Polypeptid，dessen Herstellung und Verwendung。
公开(公告)号：EP0034721A2
公开(公告)日：1981-09-02
申请号：EP81100633.7
申请日：1981-01-29
申请人： Takeda Chemical Industries, Ltd.
发明人： Masahiko, Fujino , Mitsuhiro, Wakimasu , Chieko, Kitada
IPC分类号： C07C103/52 , A61K37/02
CPC分类号： C07K14/675 , A61K38/00 , Y02P20/55 , Y10S514/809
摘要： Novel polypeptide of the formula: is useful as an analgesic agent.
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-IIe-Thr-Leu-Leu-Lys- His-Ile-Thr-Leu-Lys-Asn-Glu-Gln-OH可用作止痛剂。

6. 发明授权

EP0001684B1 Tetrapeptides, methods for their preparation and their use in analgesic compositions 失效
标题翻译：制剂及其在组合物中的使用方法
公开(公告)号：EP0001684B1
公开(公告)日：1981-09-02
申请号：EP78300420.3
申请日：1978-09-27
申请人： ELI LILLY AND COMPANY
发明人： Smithwick, Edward Lee, JR , Frederickson, Robert Curtis Arthur , Shuman, Robert Theodore
IPC分类号： C07C103/52
CPC分类号： C07K5/0812 , C07K5/1016 , Y10S514/809

7. 发明公开

EP1937241A4 PHARMACEUTICAL COMPOSITION FOR PREVENTION AND TREATMENT OF DRUG OR ALCOHOL ADDICTION OR BIPOLAR DISORDER USING SODIUM PHENYLBUTYRATE 有权
标题翻译：用于预防的药物组合物和吸毒或酗酒或干扰双极苯丁酸钠治疗
公开(公告)号：EP1937241A4
公开(公告)日：2010-09-29
申请号：EP06798579
申请日：2006-08-30
申请人： SK HOLDINGS CO LTD
发明人： CHO JEONG-WOO , CHOI SANG-RAK , HWANG SUN-GWAN
IPC分类号： A61K31/192 , A61P25/32 , A61P25/36
CPC分类号： A61K31/192 , Y10S514/809 , Y10S514/81 , Y10S514/812

8. 发明公开

EP0181001A3 Polypeptide, a process for preparing the same, a pharmaceutical composition containing said polypeptide as well as the use thereof 有权转让
标题翻译：多肽，其制备方法，含有所述多肽的药物组合物，其使用方法
公开(公告)号：EP0181001A3
公开(公告)日：1989-04-19
申请号：EP85114226.5
申请日：1985-11-08
申请人： Eisai Co., Ltd.
发明人： Yoshino, Hiroshi , Tsuchiya, Yutaka , Kaneko, Takeru , Nakazawa, Takahiro , Ikeda, Masuhiro , Araki, Shin , Yamatsu, Kiyomi , Tachibana, Shinro , Arakawa, Yoshihiro
IPC分类号： C07K14/665 , A61K38/33
CPC分类号： C07K14/665 , A61K38/00 , Y02P20/55 , Y10S514/809 , Y10S930/26
摘要： Polypeptide, a process for preparing the same, a pharmaceutical composition containing said polypeptide as well as the use thereof There is disclosed a novel polypeptide, a process for preparing the same, a pharmaceutical composition containing the same as well as the use thereof. The novel polypeptide which is useful as an analgesic corresponds to the formula given below: wherein the meaning of R 1 and R 2 , A, B, C, D, E, and F is the same as defined in the claims.

9. 发明授权

EP0076557B1 Peptides and pseudopeptides in which the N terminus bears two substituents 有权
标题翻译： N末端携带两种替代物的肽和蛋白酶
公开(公告)号：EP0076557B1
公开(公告)日：1985-11-13
申请号：EP82302471.6
申请日：1982-05-14
申请人： IMPERIAL CHEMICAL INDUSTRIES PLC
发明人： Gormley, James Joseph
IPC分类号： C07K7/06 , A61K37/02
CPC分类号： C07K14/70 , A61K38/00 , C07K5/0207 , C07K5/0212 , C07K5/06078 , C07K5/0812 , C07K5/1016 , Y10S514/809

10. 发明授权

EP0044451B1 Novel pentapeptides, processes for their production, pharmaceutical compositions comprising said pentapeptides and their use 有权
标题翻译：新产品，其生产工艺，含有此类药物的药物组合物及其用途
公开(公告)号：EP0044451B1
公开(公告)日：1984-04-18
申请号：EP81105159.8
申请日：1981-07-03
申请人： SANDOZ AG
发明人： Cardinaux, François , Huguenin, René , Pless, Janos
IPC分类号： A61K37/02 , C07C103/52
CPC分类号： C07K14/702 , A61K38/00 , Y10S514/809

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