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1. 发明申请

US20210145990A1 MINI-GASTRIN ANALOGUE, IN PARTICULAR FOR USE IN CCK2 RECEPTOR POSITIVE TUMOUR DIAGNOSIS AND/OR TREATMENT 有权
公开(公告)号：US20210145990A1
公开(公告)日：2021-05-20
申请号：US17127265
申请日：2020-12-18
申请人： Paul Scherrer Institut
发明人： Martin BEHE , Roger SCHIBLI
IPC分类号： A61K51/08 , A61K38/22 , G01N33/574 , C07K14/575 , C07K14/595 , C07B59/00 , C07K1/13 , C07K7/08
摘要： A gastrin analogue shows high uptake in CCK-2 receptor positive tumors and simultaneously a very low accumulation in the kidneys. This is achieved by a mini-gastrin analogue PP-F11 having the formula: PP-F11-X-DGlu-DGlu-DGlu-DGlu-DGlu-DGlu-Ala-Tyr-Gly-Trp-Y-Asp-Phe-NH2, wherein Y is an amino acid replacing methionine and X is a chemical group attached to the peptide for diagnostic and/or therapeutic intervention at CCK-2 receptor relevant diseases. Very suitable compounds with respect to a high tumor to kidney ratio are mini-gastrin analogues with six D-glutamic acids or six glutamines. These compounds still possess a methionine which can be oxidized easily which is a disadvantage for clinical application under GMP due to the forms which may occur. The elimination of the methionine leads to a lower affinity to oxidation which in general favors the tumor-kidney-ratio. Ideally, the methionine is replaced by norleucine. This PP-F11N mini gastrin exhibits currently the best tumor-kidney-ratio and is the most promising candidate.

2. 发明授权

US10533050B2 Methods and compositions for liver cancer therapy 有权
公开(公告)号：US10533050B2
公开(公告)日：2020-01-14
申请号：US13189403
申请日：2011-07-22
申请人： Leïla Houhou , Anne-Sophie Dumé , Dominique Joubert , Frédéric Hollande
发明人： Leïla Houhou , Anne-Sophie Dumé , Dominique Joubert , Frédéric Hollande
IPC分类号： A61K39/395 , A61K38/22 , A61K39/00 , C07K14/595 , C07K16/26 , A61K45/06
摘要： The present disclosure provides methods of treating liver cancer and preventing liver cancer recurrence with anti-progastrin antibodies, methods of monitoring treatment efficacy of anti-progastrin therapy for liver cancer, and compositions useful therefore.

3. 发明申请

US20180236065A1 COILED-COIL CONNECTOR 审中-公开
公开(公告)号：US20180236065A1
公开(公告)日：2018-08-23
申请号：US15754562
申请日：2016-09-01
申请人： OncoQR ML GmbH
发明人： Geert MUDDE , Jorge SEPULVEDA , Christopher TAUS , Liesbeth MUDDE-BOER
IPC分类号： A61K39/395 , A61K39/00 , C07K7/08 , C07K14/735 , C07K14/595 , C07K16/28 , A61K39/39
CPC分类号： A61K39/3955 , A61K39/00 , A61K39/0011 , A61K39/39 , A61K2039/5158 , A61K2039/55522 , A61K2039/627 , C07K7/08 , C07K14/595 , C07K14/705 , C07K14/70535 , C07K16/00 , C07K16/283 , C07K2317/622 , C07K2317/92 , C07K2317/94 , C07K2319/73
摘要： A connector of a helical coiled coil-type structure connecting a first and a second molecule, wherein the first molecule comprises a peptidic first alpha-helix and the second molecule comprises a peptidic second alpha-helix, which second alpha-helix is coiled to the first alpha-helix. The first alpha-helix comprises a C-terminal region consisting of a repeat of an amino acid motif a-x1 and the C-terminal motif a-x1-x2, or an N-terminal region consisting of a repeat of an amino acid motif x1-a and the N-terminal motif x2-x1-a, where a is a motif sequence of 4-8 amino acids, x1 is Lysin, and x2 is an extension of the motif. The extension consists of 1-10 amino acids and does not comprise more than 4 consecutive amino acids incorporated in said motif a-x1 or x1-a. In a multimeric protein, two polypeptide chains can be connected to each other by such connector.

4. 发明申请

US20120065365A1 Stable Radiopharmaceutical Compositions and Methods for Their Preparation 审中-公开
标题翻译：稳定的放射性药物组合物及其制备方法
公开(公告)号：US20120065365A1
公开(公告)日：2012-03-15
申请号：US13280485
申请日：2011-10-25
申请人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
发明人： Jianqing Chen , Karen E. Linder , Edmund R. Marinelli , Edmund Metcalfe , Adrian D. Nunn , Rolf E. Swenson , Michael F. Tweedle
IPC分类号： C07K7/06 , C07K14/655 , C07K7/18 , C07K14/595 , C07K7/23 , C07K14/68 , C07K7/16 , C07K14/62 , C07K14/545
CPC分类号： A61K51/12 , A61K51/088
摘要： Stabilized radiopharmaceutical formulations are disclosed. Methods of making and using stabilized radiopharmaceutical formulations are also disclosed. The invention relates to stabilizers that improve the radiostability of radiotherapeutic and radiodiagnostic compounds and formulations containing them. In particular, it relates to stabilizers useful in the preparation and stabilization of targeted radiodiagnostic and radiotherapeutic compounds, and, in a preferred embodiment, to the preparation and stabilization of radiodiagnostic and radiotherapeutic compounds that are targeted to the Gastrin Releasing Peptide Receptor (GRP-Receptor).
摘要翻译：公开了稳定的放射性药物制剂。还公开了制备和使用稳定的放射性药物制剂的方法。本发明涉及改善放射治疗和放射性诊断化合物和含有它们的制剂的无线电稳定性的稳定剂。特别地，本发明涉及可用于靶向放射性诊断和放射治疗化合物的制备和稳定化的稳定剂，并且在优选的实施方案中涉及靶向胃泌素释放肽受体（GRP-受体）的放射性诊断和放射治疗化合物的制备和稳定）。

5. 发明授权

US5900237A Catalytic antibodies which hydrolyze primary amides and methods for eliciting such antibodies 失效
标题翻译：水解初级酰胺的催化抗体和引发此类抗体的方法
公开(公告)号：US5900237A
公开(公告)日：1999-05-04
申请号：US362470
申请日：1996-05-04
申请人： Andrew D. Napper , Richard C. Titmas , Mark T. Martin , Wonpyo Hong
发明人： Andrew D. Napper , Richard C. Titmas , Mark T. Martin , Wonpyo Hong
IPC分类号： A61K38/00 , A61K38/43 , A61P37/02 , C07C229/46 , C07C229/48 , C07C235/74 , C07C271/24 , C07C311/06 , C07C311/19 , C07C317/44 , C07D205/085 , C07D207/40 , C07D207/404 , C07F9/24 , C07F9/30 , C07F9/32 , C07F9/40 , C07F9/48 , C07F9/553 , C07F9/6509 , C07F9/6571 , C07H15/252 , C07H19/04 , C07K7/08 , C07K14/55 , C07K14/585 , C07K14/595 , C07K16/00 , C07K16/10 , C07K16/26 , C07K16/42 , C07K16/44 , C07K16/46 , C12N9/00 , C12P1/00 , C12P13/22 , C12P17/10 , C12P19/34 , C12P41/00 , C12Q1/25 , G01N33/50 , G01N33/531 , G01N33/535 , G01N33/542 , G01N33/577 , A61K39/395
CPC分类号： G01N33/5044 , B82Y5/00 , C07C229/46 , C07C229/48 , C07C235/74 , C07C271/24 , C07C311/06 , C07C311/19 , C07C317/44 , C07D205/085 , C07D207/404 , C07F9/2408 , C07F9/2458 , C07F9/301 , C07F9/3211 , C07F9/3241 , C07F9/4006 , C07F9/4075 , C07F9/4816 , C07F9/5537 , C07F9/650958 , C07F9/657181 , C07H15/252 , C07H19/04 , C07K14/55 , C07K14/585 , C07K14/595 , C07K16/00 , C07K16/1063 , C07K16/26 , C07K16/4241 , C07K16/44 , C07K16/468 , C07K7/086 , C12N9/0002 , C12P1/00 , C12P13/227 , C12P17/10 , C12P19/34 , C12P41/004 , C12Q1/25 , G01N33/5008 , G01N33/502 , G01N33/531 , G01N33/535 , G01N33/542 , G01N33/577 , C07C2101/04 , C07C2102/42 , C07K2319/00 , G01N2333/16 , G01N2333/96472 , G01N2500/00
摘要： Described and claimed are compounds of formula (I) wherein Y is a polypeptide, R.sub.1 is bonded to the N-terminus of Y and is hydrogen or a branched or linear, substituted or unsubstituted, C.sub.1-21 alkyl, alkene, or alkyne group, R.sub.2 is a side chain of a naturally occurring amino acid, and X is (a), (b), (c). Such compounds are useful as haptens and immunogens for the elicitation of antibodies which catalytically enhance the rate of formation or hydrolysis of primary amide bonds. Also described and claimed are methods employing the compounds and antibodies.
摘要翻译： PCT No.PCT / US94 / 04437 371日期：1996年5月4日 102（e）日期1996年5月4日PCT 1994年4月22日PCT PCT。公开号WO94 / 25573 日期：1994年11月10日描述和要求保护的是式（I）化合物，其中Y是多肽，R 1与Y的N末端键合，并且是氢或支链或直链，取代或未取代的C 1-11烷基，烯烃或炔基，R2是天然氨基酸的侧链，X是（a），（b），（c）。这样的化合物可用作引发抗体的半抗原和免疫原，所述抗体催化增强初级酰胺键的形成或水解速率。还描述和要求保护的是使用化合物和抗体的方法。

6. 发明授权

US5739106A Appetite regulating compositions 失效
标题翻译：食欲调节组合物
公开(公告)号：US5739106A
公开(公告)日：1998-04-14
申请号：US477727
申请日：1995-06-07
申请人： Timothy J. Rink , Andrew A. Young , Nigel Robert Arnold Beeley , Kathryn S. Prickett
发明人： Timothy J. Rink , Andrew A. Young , Nigel Robert Arnold Beeley , Kathryn S. Prickett
IPC分类号： C12N15/09 , A61K38/00 , A61K38/22 , A61K38/23 , A61K45/06 , A61P3/04 , C07K7/06 , C07K7/08 , C07K14/47 , C07K14/575 , C07K14/595 , A61K38/28 , C07K5/00 , C07K7/00
CPC分类号： C07K14/595 , A61K38/23 , C07K14/575 , A61K38/00 , C07K2319/00
摘要： Compositions and methods for reducing food intake, suppressing appetite and controlling body weight are provided. Such compositions may include an amylin agonist and a CCK agonist or a hybrid peptide.
摘要翻译：提供了减少食物摄取，抑制食欲和控制体重的组合物和方法。这样的组合物可以包括胰岛淀粉样多肽激动剂和CCK激动剂或杂交肽。

7. 发明授权

US5486597A Tetrapeptide derivatives and analogues 失效
标题翻译：四肽衍生物和类似物
公开(公告)号：US5486597A
公开(公告)日：1996-01-23
申请号：US75528
申请日：1993-06-17
申请人： Sarkis B. Kalindjian , Howard B. Broughton , Caroline M. R. Low , Iain M. McDonald , Robert A. D. Hull , Nigel P. Shankley , Ildiko M. Buck , Katherine I. M. Steel , Jonathan M. R. Davies
发明人： Sarkis B. Kalindjian , Howard B. Broughton , Caroline M. R. Low , Iain M. McDonald , Robert A. D. Hull , Nigel P. Shankley , Ildiko M. Buck , Katherine I. M. Steel , Jonathan M. R. Davies
IPC分类号： C07K14/595 , A61K38/00 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K14/595
摘要： The C-terminal tetrapeptide of gastrin, Trp-Met-Asp-Phe-NH.sub.2, possesses gastrin pharmacological activity. Replacement of the methionyl moiety in the gastrin tetrapeptide, or its analogs, with a naphthylalanyl group produces compounds which interact with gastrin and/or cholecystokinin receptors, but have reduced gastrin and/or cholecystokinin agonist activity. Such partial agonists or antagonists of gastrin and/or cholecystokinin provide useful therapeutic agents.
摘要翻译： PCT No.PCT / GB91 / 02249 Sec。 371日期：1993年6月17日 102（e）日期1993年6月17日PCT 1991年12月17日PCT公布。出版物WO92 / 11284 日期：1992年7月9日。胃泌素C末端四肽Trp-Met-Asp-Phe-NH2具有胃泌素的药理活性。用萘丙氨酰基替代胃泌素四肽或其类似物中的甲硫氨酰部分产生与胃泌素和/或胆囊收缩素受体相互作用但具有降低的胃泌素和/或胆囊收缩素激动剂活性的化合物。胃泌素和/或胆囊收缩素的这种部分激动剂或拮抗剂提供有用的治疗剂。

8. 发明授权

US4507235A Method for preparing peptides and intermediate products 失效
标题翻译：制备肽和中间产物的方法
公开(公告)号：US4507235A
公开(公告)日：1985-03-26
申请号：US586187
申请日：1984-03-05
申请人： Erich Wunsch
发明人： Erich Wunsch
IPC分类号： A61K38/00 , C07K1/06 , C07K14/595 , C07C103/52
CPC分类号： C07K14/595 , C07K1/065 , A61K38/00
摘要： Peptides having the carboxyl terminated sequence of the pancreozymin-cholstokinin 25-33 modified such that the amino acid group 25 carries a strongly basic group, the amino acid group 28 exhibits a hydrophilic character similar to that of the hydroxyamino acids and the amino acid group 31 exhibits a strongly hydrophobic character similar to that of amino acids with aliphatic side chains, and in particular nonapeptides having the sequence H--X--Asp--Tyr(SO.sub.3 H)--Y--Gly--Trp--Z--Asp--Phe--NH.sub.2 wherein X is arginine, homoarginine, norarginine, N.sub..epsilon.,N.sub..epsilon. -dialkyllysine, N.sub..delta. or N.sub..delta. -dialkyl-ornithine, Y is threonine, serine or hydroxy-proline and Z is norleucine, leucine, norvaline or .alpha.-amino-butyric acid, possess pronounced pancreozymin activity and can be employed in pharmaceutical preparations for controlling the function of the gall bladder and for controlling the enzyme secretion of the pancreas. Tyrosine-O-sulfate-barium salt and its N-acyl derivatives can be used as intermediate products for the preparation of peptides. For introducing the amino acid group 27 an N-acyltyrosine is reacted with an excess of pyridine--SO.sub.3 in a polar organic solvent, the resulting solution is extracted with water, the barium salt of the N-acyl-tyrosine-O-sulfate is precipitated from the aqueous phase by addition of a soluble barium compound, possibly the acyl group is split off in conventional manner, and the resulting tyrosine-O-sulfate-barium salt or its acyl derivative are processed employing the usual methods of peptide synthesis.
摘要翻译：具有胰蛋白酶 - 缩胆囊素25-33羧基末端序列的肽被修饰，使得氨基酸25携带强碱性基团，氨基酸组28表现出与羟基氨基酸和氨基酸组31相似的亲水性表现出类似于具有脂肪族侧链的氨基酸的强疏水性，特别是具有序列HX-Asp-Tyr（SO3H）-Y-Gly-Trp-Z-Asp-Phe-NH2的非肽，其中X是精氨酸，精氨酸，降血清蛋白，Nε，Nε-二烷基赖氨酸，N或N二烷基鸟氨酸，Y是苏氨酸，丝氨酸或羟基脯氨酸，Z是正亮氨酸，亮氨酸，正缬氨酸或α-氨基丁酸，具有显着的胰酶活性，可用于控制胆囊功能和控制胰腺酶分泌的药物制剂中。酪氨酸-O-硫酸盐钡盐及其N-酰基衍生物可用作制备肽的中间产物。为了引入氨基酸组27，使N-酰基酪氨酸与极性有机溶剂中过量的吡啶-SO 3反应，所得溶液用水萃取，N-酰基 - 酪氨酸-O-硫酸盐的钡盐沉淀通过添加可溶性钡化合物从水相中，可能以常规方式分离出酰基，并且使用通常的肽合成方法处理所得的酪氨酸-O-硫酸盐 - 钡盐或其酰基衍生物。

9. 发明授权

US4400377A Use of polypeptides as analgesic drugs 失效
公开(公告)号：US4400377A
公开(公告)日：1983-08-23
申请号：US355252
申请日：1982-03-05
申请人： Gerhard Zetler , Alessandro Rossi , Chiara De Paolis
发明人： Gerhard Zetler , Alessandro Rossi , Chiara De Paolis
IPC分类号： C07K5/113 , C07K14/595 , A61K37/00
CPC分类号： C07K5/1021 , C07K14/595
摘要： A method of treating pain of whatever origin and nature in human and animal which comprises administering to the patient in need an effective amount of a polypeptide of structure: ##STR1## wherein X is selected from the group consisting of hydrogen, t-butyloxycarbonyl(Boc), Asp, Pyr-Glu, Pyr-Gln-Asp, Pyr-Asn-Asp; Y is selected from the group consisting of Thr, Met, Leu, Nle, Val; W is selected from the group consisting of Met, Nle, Leu.

10. 发明授权

US3723406A Novel peptides having cholecystokinin activity and intermediates therefor 失效
标题翻译：具有CHOLECYSTOKININ活性的新型肽及其中间体
公开(公告)号：US3723406A
公开(公告)日：1973-03-27
申请号：US3723406D
申请日：1969-12-23
申请人： SQUIBB & SONS INC
发明人： ONDETTI M , JORPES J , MUTT V , PLUSCEC J , SHEEHAN J
IPC分类号： A61K38/00 , C07K14/595 , C07C103/52 , C07G7/00
CPC分类号： C07K14/595 , A61K38/00
摘要： Novel peptide amides of the general formula
摘要翻译：通式R-Met-Gly-Trp-Met-Asp-Phe-NH 2的新型肽酰胺，其中R表示L-天冬氨酰基-O-硫酸盐-L-酪氨酰基，L-天冬氨酰基-L-精氨酰-L-天冬氨酰基-O 硫酸盐-L-酪氨酰基或异亮氨酰-L-丝氨酰-L-天冬氨酰-L-精氨酰-L-天冬氨酰基-O-硫酸盐-L-酪氨酰基，以及其生产中的中间体。已经发现本发明的肽酰胺及其药学上可接受的盐具有胆囊收缩素活性。

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