公开(公告)号：WO2011063366A1

公开(公告)日：2011-05-26

申请号：PCT/US2010/057699

申请日：2010-11-23

Applicant: PALATIN TECHNOLOGIES, INC. ,  YANG, Wei ,  SHI, Yi-qun

Inventor： YANG, Wei ,  SHI, Yi-qun

IPC: C07K7/50 ,  C07K7/54 ,  C07K7/56

CPC classification number: C07K7/56 ,  A61K31/407 ,  A61K38/00 ,  C07K7/54 ,  C07K14/68

Abstract: Melanocortin receptor-specific cyclic peptides of the formula (I) where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and R 9 are as defined in the specification, compositions and formulations including the peptides of the foregoing formula or salts thereof, and methods of preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.

Abstract translation: 式（I）的黑皮质素受体特异性环肽，其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8和R 9如说明书中所定义，组合物和制剂包括前述式的肽或其盐 以及预防，改善或治疗黑皮质素-1受体介导或反应性疾病，适应症，病症和综合征的方法。

公开(公告)号：WO2010144344A3

公开(公告)日：2010-12-16

申请号：PCT/US2010/037589

申请日：2010-06-07

Applicant: PALATIN TECHNOLOGIES, INC. ,  SHI, Yi-qun ,  SHARMA, Shubh, D. ,  DODD, John, H. ,  YANG, Wei ,  CHEN, Xin

Inventor： SHI, Yi-qun ,  SHARMA, Shubh, D. ,  DODD, John, H. ,  YANG, Wei ,  CHEN, Xin

IPC: A61K38/00 ,  C07K5/00 ,  A61K33/16

Abstract: Melanocortin receptor-specific cyclic peptides of the formula where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and z are as defined in the specification, compositions and formulations including the peptides of the foregoing formula, and methods of preventing, ameliorating or treating melanocortin receptor-mediated diseases, indications, conditions and syndromes.

公开(公告)号：WO2010065801A1

公开(公告)日：2010-06-10

申请号：PCT/US2009/066671

申请日：2009-12-04

Applicant: PALATIN TECHNOLOGIES, INC. ,  BULLINGTON, James ,  METZGER, Axel ,  CHEN, Xin ,  DODD, John, H.

Inventor： BULLINGTON, James ,  METZGER, Axel ,  CHEN, Xin ,  DODD, John, H.

IPC: C07D211/58 ,  C07D295/12 ,  C07D401/12 ,  A61K31/495 ,  A61K31/496 ,  A61P15/00 ,  A61P25/00

CPC classification number: C07D401/12 ,  C07D211/58 ,  C07D295/30

Abstract: A compound of the formula where R1, R 2a , R 2D , R 3 , L 1 , L 2 , Q, J, X, m and n are as defined, or an enantiomer, stereoisomer or diastereoisomer thereof, or a pharmaceutically acceptable salt thereof, and the use thereof in the treatment of diseases, syndromes and conditions modulated by melanocortin receptors.;

Abstract translation: 下式的化合物其中R1，R2a，R2D，R3，L1，L2，Q，J，X，m和n如定义，或其对映体，立体异构体或非对映异构体或其药学上可接受的盐， 用于治疗由黑皮质素受体调节的疾病，综合征和病况;

公开(公告)号：WO2009144432A1

公开(公告)日：2009-12-03

申请号：PCT/GB2008/001847

申请日：2008-05-30

Applicant: PALATIN TECHNOLOGIES, INC. ,  SHARMA, Shubh, D. ,  BURRIS, Kevin ,  RAJPUROHIT, Ramesh

Inventor： SHARMA, Shubh, D. ,  BURRIS, Kevin ,  RAJPUROHIT, Ramesh

IPC: A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  A61P3/04 ,  G01N33/53 ,  G01N33/68

CPC classification number: G01N33/6893 ,  A61K31/495 ,  A61K31/496 ,  A61K31/497 ,  G01N2333/665 ,  G01N2333/68 ,  G01N2333/695 ,  G01N2500/02 ,  G01N2800/044

Abstract: Methods for selection of compounds for treatment of obesity, compounds selected by the disclosed methods, and methods of treatment of obesity, wherein a selective melanocortin-4 receptor compound is identified, which compound is further characterized in that it attenuates the binding of both an agonist, including alpha-melanocyte stimulating hormone, and an inverse agonist, including agouti-related protein, to a melanocortin receptor, including melanocortin-4 receptor.

Abstract translation: 用于选择用于治疗肥胖症的化合物的方法，通过公开的方法选择的化合物和治疗肥胖症的方法，其中鉴定了选择性黑皮质素-4受体化合物，该化合物的特征还在于其减弱激动剂 ，包括α-黑素细胞刺激激素和包括agouti相关蛋白的反向激动剂，包括黑皮质素受体，包括黑皮质素-4受体。

公开(公告)号：WO2007115175A3

公开(公告)日：2008-12-11

申请号：PCT/US2007065645

申请日：2007-03-30

Applicant: PALATIN TECHNOLOGIES INC ,  SHARAMA SHUBH D ,  BASTOS MARGARITA ,  YANG WEI ,  CAI HUI-ZHI

Inventor： SHARAMA SHUBH D ,  BASTOS MARGARITA ,  YANG WEI ,  CAI HUI-ZHI

IPC: A61K38/12

CPC classification number: C07K14/58

Abstract: Cyclic constructs with an N-terminus and a C-terminus which bind to a natriuretic peptide receptor and include a plurality of amino acid residues, at least one amino acid surrogate of formula I: where R, R', Q, Y, W, Z, J, x and n are as defined in the specification, and optionally at least one prosthetic group, pharmaceutical compositions including such cyclic constructs, and methods of treating congestive heart failure or other conditions, syndromes or diseases for which induction of anti hypertensive, cardiovascular, renal or endocrine effects are desired.

Abstract translation: 具有结合利尿钠肽受体并包含多个氨基酸残基的N末端和C末端的至少一个式I的氨基酸替代物的环状构建体：其中R，R'，Q，Y，W， Z，J，x和n如说明书中所定义，以及任选的至少一个假体基团，包括这种环状构建体的药物组合物，以及治疗充血性心力衰竭或其它病症的方法，综合征或疾病，其诱导抗高血压， 需要心血管，肾脏或内分泌效应。

公开(公告)号：WO2008090357A2

公开(公告)日：2008-07-31

申请号：PCT/GB2008000263

申请日：2008-01-24

Applicant: PALATIN TECHNOLOGIES INC ,  SHARMA SHUBH D ,  SHI YI-QUN

Inventor： SHARMA SHUBH D ,  SHI YI-QUN

IPC: C07D401/14 ,  A61K31/495 ,  A61P15/00 ,  A61P25/00 ,  C07D241/04 ,  C07D295/04 ,  C07D401/06 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D407/06 ,  C07D409/06 ,  C07D413/12 ,  C07D417/06 ,  C07D417/12

CPC classification number: C07D241/04 ,  C07D295/10 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D403/14 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

Abstract: Melanocortin receptor-specific piperazine compounds, of the formula (I) wherein the variables are as defined in the specification, and pharmaceutically acceptable salts thereof. Compounds disclosed herein bind to one or more melanocortin receptors and may be an agonist, a partial agonist, an antagonist, an inverse agonist or an antagonist of an inverse agonist as to one or more melanocortin receptors, and may be employed for treatment of one or more melanocortin receptor-associated conditions or disorders, including specifically treatment of obesity and related conditions.

Abstract translation: 式（I）的黑皮质素受体特异性哌嗪化合物，其中变量如说明书中所定义，及其药学上可接受的盐。 本文公开的化合物结合一种或多种黑皮质素受体，并且可以是关于一种或多种黑皮质素受体的反向激动剂的激动剂，部分激动剂，拮抗剂，反向激动剂或拮抗剂，并且可用于治疗一种或多种黑皮质素受体 更多的黑皮质素受体相关病症或障碍，包括特别治疗肥胖症和相关病症。

公开(公告)号：WO2007115164A2

公开(公告)日：2007-10-11

申请号：PCT/US2007/065632

申请日：2007-03-30

Applicant: PALATIN TECHNOLOGIES, INC. ,  SHARMA, Shubh, D. ,  BASTOS, Margarita ,  YANG, Wei ,  CAI, Hui-Zhi

Inventor： SHARMA, Shubh, D. ,  BASTOS, Margarita ,  YANG, Wei ,  CAI, Hui-Zhi

IPC: B23B31/12

CPC classification number: C07K14/58

Abstract: Ring-constrained amino acid surrogates of formula I where R 1 , R 2 , R 3 , R 4 , R 5 , R 6a , R 6b , R 7 , and y are as defined in the specification, methods for synthesizing ring-constrained amino acid surrogates of formula I, methods of use of ring-constrained amino acid surrogates of formula I, including use in linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I and linear or cyclic compounds which include a plurality of amino acid residues and one or more ring-constrained amino acid surrogates of formula I.

Abstract translation: 式I的环受限氨基酸替代物，其中R 1，R 2，R 3，R 4， R 5，R 6a，R 6b，R 7和Y如说明书中所定义，方法 用于合成式I的环受限制的氨基酸替代物，使用式I的环受限氨基酸替代物的方法，包括用于线性或环状化合物的方法，其包括多个氨基酸残基和一个或多个环受限制的氨基酸 式I的替代物和包括多个氨基酸残基和一个或多个式I的环受限氨基酸替代物的线性或环状化合物。

公开(公告)号：WO2004075830A3

公开(公告)日：2006-09-28

申请号：PCT/US2004002933

申请日：2004-02-02

Applicant: PALATIN TECHNOLOGIES INC ,  SHARMA SHUBH D ,  SHI YI-QUN ,  RAJPUROHIT RAMESH ,  BASTOS MARGARITA ,  CAI HUI-ZHI

Inventor： SHARMA SHUBH D ,  SHI YI-QUN ,  RAJPUROHIT RAMESH ,  BASTOS MARGARITA ,  CAI HUI-ZHI

IPC: G01N33/53 ,  A61K20060101 ,  A61K6/00 ,  C07K1/04 ,  C07K5/103 ,  C07K5/107 ,  C07K5/117 ,  G01N33/567 ,  G01N33/68

CPC classification number: C07K5/1008 ,  C07K1/047 ,  C07K5/1016 ,  C07K5/1024 ,  G01N33/6803

Abstract: The invention provides methods for identification and determination of target-specific sites in peptides and proteins, including a method for determining the primary sequence of a secondary structure within a known parent polypeptide that binds to the target of interest. In one embodiment of the invention, a residue or mimetic containing a nitrogen atom and a sulfur atom available for binding to a metal ion is serially substituted for single residues in or inserted between adjacent residues in a known primary sequence of a peptide or protein. The resulting sequence is complexed with a metal ion thereby forming a metallopeptide. The resulting metallopeptides are then used in binding or functional assays related to the target of interest, and the metallopeptide(s) which result in significant or substantially decreased or changed binding or functionality are determined to identify the primary sequence involved in such binding or functionality.

Abstract translation: 本发明提供用于鉴定和确定肽和蛋白质中靶特异性位点的方法，包括确定结合目的靶标的已知亲本多肽内的二级结构的一级序列的方法。 在本发明的一个实施方案中，含有可用于与金属离子结合的氮原子和硫原子的残基或模拟物连续取代肽或蛋白质的已知一级序列中相邻残基之间或插入其中的单个残基。 所得到的序列与金属离子络合，从而形成金属肽。 然后将所得金属肽用于与感兴趣靶标相关的结合或功能测定，并确定导致显着或显着降低或改变的结合或功能的金属肽，以鉴定涉及这种结合或功能的一级序列。

公开(公告)号：WO2005117935A1

公开(公告)日：2005-12-15

申请号：PCT/US2005/018739

申请日：2005-05-27

Applicant: PALATIN TECHNOLOGIES, INC. ,  DIAMOND, Lisa, E. ,  EARLE, Dennis, C. ,  SHADIACK, Annette, M. ,  SHARMA, Shubh, D. ,  SPANA, Carl

Inventor： DIAMOND, Lisa, E. ,  EARLE, Dennis, C. ,  SHADIACK, Annette, M. ,  SHARMA, Shubh, D. ,  SPANA, Carl

IPC: A61K38/12

CPC classification number: C07K14/685 ,  A61K31/519 ,  A61K33/24 ,  A61K38/12 ,  A61K45/06 ,  Y10S436/811 ,  A61K2300/00

Abstract: Multiple agent therapy for treatment of sexual dysfunction, including male erectile dysfunction, with sequential administration a type V phosphodiesterase inhibitor (PDE-5), such as sildenafil, preferably wherein the PDE-5 inhibitor is administered by oral dose means, and a melanocortin 3 and/or 4 receptor agonist, such as Ac-Nle- cyclo (-Asp-His-D-Phe-Arg-Trp-Lys)-OH (PT-141) preferably wherein the PT-141 is formulated for and administered by intranasal means, and further preferably wherein the PDE-5 inhibitor is administered prior to PT-141.

Abstract translation: 用于治疗性功能障碍（包括男性勃起功能障碍）的多药物治疗，连续施用V型磷酸二酯酶抑制剂（PDE-5），例如西地那非，其中PDE-5抑制剂通过口服剂量方式施用，黑皮质素3 和/或4受体激动剂，例如Ac-Nle-cyclo（-Asp-His-D-Phe-Arg-Trp-Lys）-OH（PT-141），优选其中PT-141配制用于鼻内给药 是指，进一步优选其中PDE-5抑制剂在PT-141之前施用。

公开(公告)号：WO2005014617A3

公开(公告)日：2005-02-17

申请号：PCT/US2004/025749

申请日：2004-08-09

Applicant: PALATIN TECHNOLOGIES, INC. ,  SHARMA, Shubh, D. ,  SHADIACK, Annette, M. ,  YANG, Wei ,  RAJPUROHIT, Ramesh

Inventor： SHARMA, Shubh, D. ,  SHADIACK, Annette, M. ,  YANG, Wei ,  RAJPUROHIT, Ramesh

IPC: A61K38/00

Abstract: A cyclic peptide of the structural formula: or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , m and p are as defined. Further provided are compositions and methods for treatment of sexual dysfunction in mammals, including male sexual dysfunction, such as erectile dysfunction, and female sexual dysfunction, by administration of a cyclic peptide including a C-terminus -OH group. Methods of administration include injection, oral, urethral, vaginal, nasal and mucosal administration.