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101. 发明申请

US20050192214A1 Cyclosporine analogue mixtures and their use as immunomodulating agents 有权
标题翻译：环孢霉素类似物混合物及其作为免疫调节剂的用途
公开(公告)号：US20050192214A1
公开(公告)日：2005-09-01
申请号：US11118830
申请日：2005-04-28
申请人： Selvaraj Naicker , Randall Yatscoff , Robert Foster
发明人： Selvaraj Naicker , Randall Yatscoff , Robert Foster
IPC分类号： A61K38/00 , A61K9/00 , A61K9/107 , A61K9/48 , A61K38/13 , A61P19/02 , A61P37/06 , C07K7/00 , C07K7/52 , C07K7/64
CPC分类号： C07K7/645 , A61K9/0095 , A61K9/1075 , A61K9/4858 , A61K38/00 , A61K38/13 , B82Y5/00 , C07K7/64 , Y10S530/806
摘要： The invention is directed to isomeric mixtures of cyclosporine analogues that are structurally similar to cyclosporine A. The mixtures possess enhanced efficacy and reduced toxicity over the individual isomers and over naturally occurring and other presently known cyclosporines and cyclosporine derivatives. Embodiments of the present invention are directed toward cis and trans-isomers of cyclosporin A analogs referred to as ISATX247, and derivatives thereof. Mixtures of ISATX247 isomers exhibit a combination of enhanced potency and reduced toxicity over the naturally occurring and presently known cyclosporins. ISATX247 isomers and alkylated, arylated, and deuterated derivatives are synthesized by stereoselective pathways where the particular conditions of a reaction determine the degree of siereoselectivity. The ratio of isomers in a mixture may range from about 10 to 90 percent by weight of the (E)-isomer to about 90 to 10 percent by weight of the (Z)-isomer, based on the total weight of the mixture.
摘要翻译：本发明涉及结构类似于环孢霉素A的环孢菌素类似物的异构体混合物。该混合物具有比单个异构体和天然存在的和其它目前已知的环孢菌素和环孢菌素衍生物更强的功效和降低的毒性。本发明的实施方案涉及被称为ISA 247的环孢菌素A类似物及其衍生物的顺式和反式异构体。 ISA 247异构体的混合物显示了与天然存在的和目前已知的环孢菌素相比增强的效力和降低的毒性的组合。通过立体选择性途径合成烷基化，芳基化和氘代衍生物，其中反应的特定条件决定了Silectoslectivity的程度。基于混合物的总重量，混合物中异构体的比例可以为（E） - 异构体的约10至90重量％至（Z） - 异构体的约90至10重量％。

102. 发明申请

US20050075480A1 Urotensin-II agonists and antagonists 失效
标题翻译：促肾上腺素Ⅱ激动剂和拮抗剂
公开(公告)号：US20050075480A1
公开(公告)日：2005-04-07
申请号：US10399542
申请日：2001-10-19
申请人： David Coy , Wojciech Rossowski , John Taylor
发明人： David Coy , Wojciech Rossowski , John Taylor
IPC分类号： A61K38/00 , A61K38/12 , A61P1/04 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/14 , A61P25/14 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07K7/06 , C07K7/52 , C07K7/64 , C07K14/575
CPC分类号： C07K7/52 , A61K38/00 , C07K14/57509
摘要： The present invention features a novel class of cyclic polypeptides that have U-II antagonist and agonist activity. The invention also features methods for treating physiological or psychological conditions characterized by an excess or under expression of Ur4otensin-II.
摘要翻译：本发明的特征在于具有U-II拮抗剂和激动剂活性的新一类环状多肽。本发明还具有用于治疗特征在于Ur4otensin-II过量或低表达的生理或心理状态的方法。

103. 发明申请

US20050037951A1 Composition and methods for treatment of sexual dysfunction 审中-公开
标题翻译：治疗性功能障碍的组成和方法
公开(公告)号：US20050037951A1
公开(公告)日：2005-02-17
申请号：US10946969
申请日：2004-09-20
申请人： Christine Blood , Annette Shadiack , Guy Herbert , Joanna Bernstein
发明人： Christine Blood , Annette Shadiack , Guy Herbert , Joanna Bernstein
IPC分类号： A61K38/24 , A61K38/00 , A61P15/00 , A61P15/10 , C07K7/52 , C07K14/685 , A61K38/12
CPC分类号： C07K14/685 , A61K38/00 , Y10S436/811
摘要： Compositions and methods are provided for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction, wherein pharmaceutically sufficient quantities of a linear or cyclic peptide with a carboxyl terminus —OH group or pharmaceutically acceptable salt thereof and a core His-Phe-Arg-Trp (SEQ ID NO:1) or His-D-Phe-Arg-Trp sequence are administered. Methods of administration include injection, oral, nasal and mucosal administration.
摘要翻译：提供用于治疗哺乳动物性功能障碍的组合物和方法，包括男性性功能障碍，例如勃起功能障碍和女性性功能障碍，其中药学上足量的具有羧基末端-OH基团的线性或环状肽或其药学上可接受的盐和核心His-Phe-Arg-Trp（SEQ ID NO：1）或His-D-Phe-Arg-Trp序列。给药方法包括注射，口服，鼻腔和粘膜给药。

104. 发明授权

US5981477A Peptide-metal chelate conjugates 失效
公开(公告)号：US5981477A
公开(公告)日：1999-11-09
申请号：US39116
申请日：1998-03-13
申请人： Richard T. Dean
发明人： Richard T. Dean
IPC分类号： A61K51/00 , A61K38/00 , A61K38/04 , A61K49/00 , A61K51/08 , A61P35/00 , C07B59/00 , C07F13/00 , C07K5/10 , C07K7/06 , C07K7/08 , C07K7/52 , C07K14/00 , C07K14/655 , C07K14/775
CPC分类号： C07B59/008 , A61K51/083 , A61K51/088 , C07K14/655 , C07K14/6555 , C07K14/775 , C07K7/06 , A61K2121/00 , A61K2123/00 , A61K38/00
摘要： This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.

105. 发明授权

US5972308A Peptide-metal chelate conjugates 失效
标题翻译：肽 - 金属螯合物
公开(公告)号：US5972308A
公开(公告)日：1999-10-26
申请号：US042224
申请日：1998-03-13
申请人： Richard T. Dean
发明人： Richard T. Dean
IPC分类号： A61K51/00 , A61K38/00 , A61K38/04 , A61K49/00 , A61K51/08 , A61P35/00 , C07B59/00 , C07F13/00 , C07K5/10 , C07K7/06 , C07K7/08 , C07K7/52 , C07K14/00 , C07K14/655 , C07K14/775 , A61M36/14
CPC分类号： C07B59/008 , A61K51/083 , A61K51/088 , C07K14/655 , C07K14/6555 , C07K14/775 , C07K7/06 , A61K2121/00 , A61K2123/00 , A61K38/00
摘要： This invention relates to diagnostic and radiodiagnostic agents, including radiolabeled scintigraphic imaging agents, and therapeutic and radiotherapeutic agents. The invention provides such agents and reagents for preparing such agents, and methods for producing and using such reagents. Specifically, the invention provides radiolabeled imaging agents and non-radioactively labeled imaging agents for imaging sites in a mammalian body and reagents for preparing these imaging agents. The invention also provides radiolabeled therapeutic agents, as well as non-radioactively labeled therapeutic agents, and reagents and methods for preparing these agents. The agents and reagents provided comprise a specific binding peptide, covalently linked to a metal ion-complexing moiety. Reagents, methods and kits for making such reagents, methods for labeling such reagents, and methods for using such labeled reagents are provided.
摘要翻译：本发明涉及诊断和放射诊断剂，包括放射性标记的闪烁照相成像剂，以及治疗和放射治疗剂。本发明提供了用于制备这种试剂的这种试剂和试剂，以及用于生产和使用这些试剂的方法。具体地，本发明提供放射性标记的成像剂和用于哺乳动物体内成像位点的非放射性标记显像剂和用于制备这些成像剂的试剂。本发明还提供了放射性标记的治疗剂以及非放射性标记的治疗剂，以及用于制备这些试剂的试剂和方法。提供的试剂和试剂包含与金属离子络合部分共价连接的特异性结合肽。提供了用于制备这些试剂的试剂，方法和试剂盒，用于标记这些试剂的方法，以及使用这些标记试剂的方法。

106. 发明授权

US5763397A Glycopeptides, a process for their preparation and their use 失效
标题翻译：糖肽，其制备方法及其用途
公开(公告)号：US5763397A
公开(公告)日：1998-06-09
申请号：US907747
申请日：1992-06-29
申请人： Laszlo Vertesy , Joachim Betz , Hans-Wolfram Fehlhaber , Michael Limbert
发明人： Laszlo Vertesy , Joachim Betz , Hans-Wolfram Fehlhaber , Michael Limbert
IPC分类号： A61K31/33 , A61K31/00 , A61K38/00 , A61K38/12 , A61K38/14 , A61P31/00 , A61P31/04 , C07D519/00 , C07K1/02 , C07K1/113 , C07K1/20 , C07K7/06 , C07K7/52 , C07K9/00 , C07K14/195 , C07K14/41 , C12N1/20 , C12P21/00 , C12P21/02 , C12R1/04 , C12N1/22 , C12P19/60
CPC分类号： C07K7/06 , C07K9/008 , A61K38/00 , Y10S435/822
摘要： Desmethylbalhimycin, a compound of the formula C.sub.65 H.sub.71 Cl.sub.2 N.sub.9 O.sub.24, desmethylleucylbalhimycin, a compound of the formula C.sub.59 H.sub.60 Cl.sub.2 N.sub.8 O.sub.23, desglucobalhimycin, a compound of the formula C.sub.60 H.sub.63 Cl.sub.2 N.sub.9 O.sub.19, ureidobalhimycin, a compound of the formula C.sub.67 H.sub.74 Cl.sub.2 N.sub.10 O.sub.25, desmethyl-desglucobalhimycin, a compound of the formula C.sub.59 H.sub.61 Cl.sub.2 N.sub.9 O.sub.19 and balhimycin V, a compound of the formula C.sub.73 H.sub.84 Cl.sub.2 N.sub.10 I.sub.26, methylbalhimycin, a compound of the formula C.sub.67 H.sub.75 Cl.sub.2 N.sub.9 O.sub.24 and balhimycin R, a compound of the formula C.sub.72 H.sub.83 Cl.sub.2 N.sub.9 O.sub.28, have an antibiotic action.
摘要翻译：去甲基巴马霉素，式C65H71Cl2N9O24的化合物，脱甲基亮氨酰巴马霉素，式C59H60Cl2N8O23的化合物，去环巴豆霉素，式C 60 H 63 Cl 2 N 9 O 19的化合物，脲基巴拉霉素，式C67H74Cl2N10O25的化合物，脱甲基去环糊精霉素，式C59H61Cl2N9O19的化合物和巴利霉素V，式C73H84Cl2N10I26的化合物，甲基巴马霉素，式C67H75Cl2N9O24的化合物和巴尔霉素R，式C72H83Cl2N9O28的化合物具有抗生素作用。

107. 发明授权

US5693612A Cyclopeptides of the formula I 失效
标题翻译：式I的环肽
公开(公告)号：US5693612A
公开(公告)日：1997-12-02
申请号：US430238
申请日：1995-04-28
申请人： Alfred Jonczyk , Gunter Holzemann , Simon Goodman , Horst Kessler , Roland Haubner , Jochen Wermuth
发明人： Alfred Jonczyk , Gunter Holzemann , Simon Goodman , Horst Kessler , Roland Haubner , Jochen Wermuth
IPC分类号： A61K38/00 , A61K38/08 , A61K38/12 , A61P7/02 , A61P9/00 , A61P9/08 , A61P9/10 , A61P19/10 , A61P31/00 , A61P35/00 , A61P43/00 , C07K1/22 , C07K5/02 , C07K5/10 , C07K5/12 , C07K7/52 , C07K7/64 , C07K14/75
CPC分类号： C07K14/75 , C07K5/1019 , C07K7/52 , A61K38/00 , Y10S930/27
摘要： The invention relates to novel cyclopeptides of the formula I cyclo-(Arg-A-Asp-R.sup.1 -R.sup.2) I in which A, R.sup.1 and R.sup.2 have the meaning given in claim 1, and their salts. These compounds act as integrin inhibitors and can be used in particular for the prophylaxis and treatment of disorders of the circulation, bones and in tumour therapy, and as antimicrobial and antiviral active compounds.
摘要翻译：本发明涉及式I环 - （Arg-A-Asp-R1-R2）Iin的新型环肽，其中A，R 1和R 2具有权利要求1中给出的含义及其盐。这些化合物用作整联蛋白抑制剂，特别可用于预防和治疗循环障碍，骨骼和肿瘤治疗以及抗微生物和抗病毒活性化合物。

108. 发明授权

US5569741A Cyclic octapeptide neuromedin B receptor antagonists 失效
标题翻译：循环八肽神经介肽B受体拮抗剂
公开(公告)号：US5569741A
公开(公告)日：1996-10-29
申请号：US352392
申请日：1994-12-08
申请人： David H. Coy , John E. Taylor
发明人： David H. Coy , John E. Taylor
IPC分类号： A61K38/00 , A61K38/31 , A61P43/00 , C07K7/06 , C07K7/52 , C07K14/655 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： A61K38/31 , C07K14/6555
摘要： A cyclic octapeptide of the formula: ##STR1## wherein: A.sup.1 is D-Nal or D-Trp;A.sup.3 is Phe, F.sub.5 -Phe, or X-Phe wherein X is a halogen, NO.sub.2, CH.sub.3, or OH;A.sup.5 is --NH--CH(Y)--CO-- wherein Y is (CH.sub.2).sub.m --R.sub.4 --N(R.sub.5)(R.sub.6) or (CH.sub.2).sub.n --R.sub.4 --NH--C(R.sub.7)--N(R.sub.5) (R.sub.6);A.sup.6 is the D-- or L-- isomer of Thr, Leu, Ile, Nle, Val, and Abu;A.sup.8 is Nal or Trp;m is 1, 2, or 3;n is 1, 2, 3, 4 or 5;each of R.sub.1 and R.sub.2, independently, is H, E, COE, or COOE wherein E is C.sub.1-12 alkyl, C.sub.2-12 alkenyl, C.sub.2-12 alkynyl, phenyl, naphthyl, C.sub.7-12 phenylalkyl or alkylphenyl, C.sub.8-12 phenylalkenyl or alkenylphenyl, C.sub.8-12 phenylalkynyl or alkynylphenyl, C.sub.11-20 naphthylalkyl or alkylnaphthyl, C.sub.12-20 naphthylalkenyl or alkenylnaphthyl, or C.sub.12-20 naphthylalkynyl or alkynylnaphthyl, provided that when one of R.sub.1 or R.sub.2 is COE or COOE, the other must be H;R.sub.4 is C.sub.6 H.sub.4 or absent;R.sub.7 is .dbd.NR.sub.8, .dbd.S, or .dbd.O; andeach of R.sub.3, R.sub.5, R.sub.6, and R.sub.8, independently, is H or E.
摘要翻译：下式的环状八肽：其中：A1为D-Nal或D-Trp; A3是Phe，F5-Phe或X-Phe，其中X是卤素，NO 2，CH 3或OH; A5是-NH-CH（Y）-CO-，其中Y是（CH2）m-R4-N（R5）（R6）或（CH2）n-R4-NH-C（R7）-N（R5））; A6是Thr，Leu，Ile，Nle，Val和Abu的D-或L-异构体; A8是Nal或Trp; m为1,2或3; n为1,2,3,4或5; R 1和R 2各自独立地是H，E，COE或COOE，其中E是C 1-12烷基，C 2-12烯基，C 2-12炔基，苯基，萘基，C 7-12苯基烷基或烷基苯基，C 8-12苯基烯基或烯基苯基，C 8-12苯基炔基或炔基苯基，C 11-20萘基烷基或烷基萘基，C 12-20萘基烯基或链烯基萘基，或C 12-20萘基炔基或炔基萘基，条件是当R 1或R 2中的一个为COE或COOE时，另一个必须为H ; R4为C6H4或不存在; R 7 = NR 8，= S或= O; R 3，R 5，R 6和R 8各自独立地为H或E.

109. 发明授权

US5543496A Cyclic bradykinin antagonist peptides 失效
标题翻译：循环缓激肽拮抗剂肽
公开(公告)号：US5543496A
公开(公告)日：1996-08-06
申请号：US279763
申请日：1994-07-25
申请人： Donald J. Kyle , Sarvajit Chakravarty
发明人： Donald J. Kyle , Sarvajit Chakravarty
IPC分类号： A61K38/00 , C07K7/18 , A61K38/12 , C07K7/52
CPC分类号： C07K7/18 , A61K38/00 , Y10S930/27
摘要： Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at postions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.
摘要翻译：基于修饰的缓激肽序列的环化合物是有效的缓激肽受体拮抗剂。在位置2和5或6处进行氨基酸取代，以通过氨基酸侧链的共价键来促进肽的环化。所产生的类似物可用于治疗其中产生或注射过量的缓激肽或相关激肽的哺乳动物和人的病症和疾病，例如通过昆虫叮咬。

110. 发明授权

US5462926A Neuromedin B receptor antagonists which demonstrate selectivity 失效
标题翻译：证明选择性的神经介肽B受体拮抗剂
公开(公告)号：US5462926A
公开(公告)日：1995-10-31
申请号：US78419
申请日：1993-06-17
申请人： David H. Coy , John E. Taylor
发明人： David H. Coy , John E. Taylor
IPC分类号： A61K38/00 , A61K38/31 , A61P43/00 , C07K7/06 , C07K7/52 , C07K14/655 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： A61K38/31 , C07K14/6555
摘要： A method of selectively inhibiting biochemical activity of cells induced by neuromedin B. The method includes the step of contacting cells which contain neuromedin B receptor with a cyclic octapeptide, D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys-Nal-NH.sub.2, or an analog thereof.
摘要翻译：一种选择性抑制由神经介肽B诱导的细胞生化活性的方法。该方法包括使含有神经介肽B受体的细胞与环状八肽D-Nal-Cys-Tyr-D-Trp-Lys-Val-Cys- Nal-NH 2，或其类似物。

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