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1. 发明申请

WO2021094626A1 MEDICAL COMPOSITION FOR TREATING CARDIAC WASTING AND CACHEXIA 审中-公开
公开(公告)号：WO2021094626A1
公开(公告)日：2021-05-20
申请号：PCT/EP2020/082308
申请日：2020-11-16
申请人： RELAXERA PHARMAZEUTISCHE GMBH & CO. KG
发明人： DSCHIETZIG, Thomas Bernd
IPC分类号： A61K38/22 , A61P9/04 , C07K14/64
摘要： Human relaxin-2 as active ingredient in a pharmaceutical composition for treating a subject suffering from cachexia syndrome or cardiac wasting or suspected of being at risk of suffering from cardiac wasting or cardiac decompensation. The application also described methods of diagnosis of cachexia and cardiac wasting and patients suspected of being at risk of suffering from cardiac decompensation. Further described is a patch pump for sc. or iv infusion of relaxin or human relaxin-2.

2. 发明申请

WO2018148419A1 MODIFIED RELAXIN POLYPEPTIDES COMPRISING A PHARMACOKINETIC ENHANCER AND USES THEREOF 审中-公开
公开(公告)号：WO2018148419A1
公开(公告)日：2018-08-16
申请号：PCT/US2018/017436
申请日：2018-02-08
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： DUBOWCHIK, Gene, M. , GUDMUNDSSON, Olafur, S. , HAN, Xiaojun , LAWRENCE, R., Michael , LIPOVSEK, Dasa , MADSEN, Cort, S. , MAPELLI, Claudio , MORIN, Paul, E. , MYERS, Michael, C.
IPC分类号： C07K14/64 , A61K38/22
摘要： The present disclosure generally relates to modified relaxin polypeptides, such as modified human relaxin 2 polypeptides, comprising a non-naturally encoded amino acid which is linked to a pharmacokinetic enhancer, and therapeutic uses of such polypeptides, such as for the treatment of cardiovascular conditions (such as heart failure) and/or conditions relating to fibrosis.

3. 发明申请

WO2012024452A3 MODIFIED RELAXIN POLYPEPTIDES AND THEIR USES 审中-公开
公开(公告)号：WO2012024452A3
公开(公告)日：2012-02-23
申请号：PCT/US2011/048157
申请日：2011-08-17
申请人： AMBRX, INC. , KRAYNOV, Vadim , KNUDSEN, Nick , HEWET, Amha , DE DIOS, Kristine , PINKSTAFF, Jason , SULLIVAN, Lorraine
发明人： KRAYNOV, Vadim , KNUDSEN, Nick , HEWET, Amha , DE DIOS, Kristine , PINKSTAFF, Jason , SULLIVAN, Lorraine
IPC分类号： C07K14/64 , A61K38/22
摘要： Modified relaxin polypeptides and their uses thereof are provided.

4. 发明申请

WO2010063604A1 PROCESS FOR PREPARING THERAPEUTIC PEPTIDE 审中-公开
标题翻译：制备治疗肽的方法
公开(公告)号：WO2010063604A1
公开(公告)日：2010-06-10
申请号：PCT/EP2009/065674
申请日：2009-11-24
申请人： F. HOFFMANN-LA ROCHE AG , CHEN, Li
发明人： CHEN, Li
IPC分类号： C07K14/435 , C07K14/575 , C07K14/64
CPC分类号： C07K14/64
摘要： This application discloses processes for synthesizing human relaxin Chain B for treatment of diseases mediated by relaxin. This application in particular discloses processes of synthesizing the Chain B of human relaxin using a solid and solution phase ("hybrid") approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to couple the fragments.
摘要翻译：该申请公开了用于治疗由松弛素介导的疾病的人松弛素B链的方法。本申请特别公开了使用固相和溶液相（“混合”）方法合成人松弛素的链B的方法。通常，该方法包括使用固相化学合成三种不同的肽中间体片段。然后使用溶液相化学来连接片段。

5. 发明申请

WO2007115414A1 MODIFIED H2 RELAXIN FOR TUMOR SUPPRESSION 审中-公开
标题翻译：用于肿瘤抑制的修饰的H2 RELAXIN
公开(公告)号：WO2007115414A1
公开(公告)日：2007-10-18
申请号：PCT/CA2007/000604
申请日：2007-04-11
申请人： UNIVERSITY OF GUELPH , MEDIN, Jeffrey, A. , SILVERTOWN, Joshua, Daniel , SUMMERLEE, Alastair, J.S.
发明人： MEDIN, Jeffrey, A. , SILVERTOWN, Joshua, Daniel , SUMMERLEE, Alastair, J.S.
IPC分类号： C12N15/16 , A61K31/7088 , A61K35/12 , A61K38/22 , A61K48/00 , A61P35/00 , C07K14/64
CPC分类号： C12N15/86 , A61K38/00 , A61K48/00 , C07K14/64 , C12N2740/10043
摘要： Modified H2 relaxms which act as antagonists of the relaxm receptor in cells and tissues, in particular, modified H2 relaxms comprising one or more alterations of the ammo acid sequence at positions B 13, B17 and B20 located in the receptor binding domain The antagonists retain affinity to the receptor, but do not substantially activate the receptor once bound thereto The H2 relaxm antagonists are used in compositions and methods for the treatment of cancers wherein a relaxm receptor is expressed
摘要翻译：充当细胞和组织中松弛受体的拮抗剂的修饰的H2松弛物，特别是包含位于受体结合结构域中位置B13，B17和B20处的氨基酸序列的一个或多个改变的修饰的H2松弛素。拮抗剂保持亲和力但不能基本上活化一旦结合到其上的受体.H 2松弛素拮抗剂用于治疗癌症的组合物和方法，其中松弛受体被表达

6. 发明申请

WO03016487A3 MAMMALIAN RELAXIN RECEPTORS 审中-公开
标题翻译：哺乳动物松弛素受体
公开(公告)号：WO03016487A3
公开(公告)日：2003-10-16
申请号：PCT/US0226185
申请日：2002-08-15
申请人： UNIV LELAND STANFORD JUNIOR , HSU SHEAU YU , HSUEH AARON J W
发明人： HSU SHEAU YU , HSUEH AARON J W
IPC分类号： A61K38/00 , C07K14/72 , C07K14/00 , A61K38/16 , C07K14/64
CPC分类号： C07K14/723 , A61K38/00
摘要： High affinity relaxin receptors, polypeptide compositions related thereto, as well as nucleotide compositions encoding the same, are provided. These proteins, herein termed LGR7 and LGR8, are orphan leucine-repeat-containing, G protein-coupled receptors. These receptors have a wide and a unique tissue expression pattern. The receptors, particularly soluble fragments thereof, are useful as therapeutic agents capable of inhibiting the action of relaxin and InsL3. The receptors and fragments thereof also find use in the screening and design of relaxin agonists and antagonists. Conditions treatable with relaxin agonists or antagonists include prevention or induction of labor, treatment of endometriosis, treatment of skin conditions such as scleroderma that require collagen or extracellular matrix remodelling. Additionally, relaxin has been implicated in the dilation of blood vessels' smooth muscle cells directly and through release of nitric oxide and atrial natriuretic peptide. Relaxin has also been used in the treatment of severe chronic pain, particularly pain arising from stretching, swelling, or dislocation of tissues.
摘要翻译：提供了高亲和力松弛素受体，与其相关的多肽组合物，以及编码其的核苷酸组合物。这些蛋白质，在这里被称为LGR7和LGR8，是孤儿亮氨酸重复，G蛋白偶联受体。这些受体具有广泛且独特的组织表达模式。受体，特别是其可溶性片段可用作能够抑制松弛素和InsL3作用的治疗剂。这些受体及其片段也可用于松弛素激动剂和拮抗剂的筛选和设计。可用松弛素激动剂或拮抗剂治疗的病症包括预防或诱导分娩，治疗子宫内膜异位症，治疗皮肤病如需要胶原蛋白或细胞外基质重塑的硬皮病。此外，松弛素已直接牵涉血管平滑肌细胞的扩张，并通过释放一氧化氮和心房利钠肽。松弛素还用于治疗严重的慢性疼痛，特别是由于伸展，肿胀或组织脱位引起的疼痛。

7. 发明申请

WO0228418B1 METHODS OF MODULATING APOPTOSIS BY ADMINISTRATION OF RELAXIN AGONISTS OR ANTAGONISTS 审中-公开
标题翻译：通过放线松弛激素或拮抗剂调节药物的方法
公开(公告)号：WO0228418B1
公开(公告)日：2002-07-18
申请号：PCT/US0142484
申请日：2001-10-04
申请人： MOLECULAR MEDICINE RES INST , AMENTO EDWARD P , SAMUEL CHRISHAN S
发明人： AMENTO EDWARD P , SAMUEL CHRISHAN S
IPC分类号： A61K48/00 , A61K31/7088 , A61K38/22 , A61K39/395 , A61P15/08 , A61P15/10 , A61P35/00 , A61P43/00 , C07K14/64 , A61K38/17 , A01N63/00 , C07H21/04 , C12N15/63
CPC分类号： C07K14/64 , A01K2217/075 , A61K38/2221
摘要： The present invention relates to the discovery that relaxin is associated with the development or maturation of body tissues. Knockouts of the gene encoding relaxin result in various abnormalities in the development of various tissues. The present invention provides methods of modulating apoptosis by administering a relaxin agonist or antagonist to a subject.
摘要翻译：本发明涉及松弛素与身体组织的发育或成熟有关的发现。编码松弛素的基因的敲除导致各种组织发育的各种异常。本发明提供了通过向受试者施用松弛素激动剂或拮抗剂来调节凋亡的方法。

8. 发明申请

WO99037780A1 EXPRESSION OF THE INSL4 GENE IN HUMAN EMBRYONIC BONE TISSUES AND APPLICATIONS 审中-公开
标题翻译：人类骨骼组织中INSL4基因的表达及应用
公开(公告)号：WO99037780A1
公开(公告)日：1999-07-29
申请号：PCT/FR1999/000137
申请日：1999-01-22
IPC分类号： G01N33/53 , A61K38/00 , A61K39/395 , A61K45/00 , A61K48/00 , A61P19/00 , C07H21/00 , C07K14/64 , C07K16/26 , C12N5/10 , C12N15/09 , C12N15/16 , C12P21/02 , C12Q1/68 , G01N33/569 , G01N33/68 , G01N33/74 , A61K38/28
CPC分类号： G01N33/74 , A61K38/00 , C07K14/64
摘要： The invention concerns the locating of the expression of the insulin-like 4 (ISNL4) gene in the human embryonic bone tissues and ligaments, detection and diagnostic methods, methods for marking and detecting said tissues expressing INSL4 gene expression products as well as methods for selecting compounds capable of modulating the activity of said cells. The invention also concerns medicines for treating pathologies related to the differentiation and/or abnormal proliferation of said tissues, particularly pathologies related to the abnormal development of the cartilage and/or an abnormal ossification of the bone being formed and/or the abnormal development of interarticular ligaments.
摘要翻译：本发明涉及在人胚胎骨组织和韧带中定位胰岛素样4（ISNL4）基因的表达，检测和诊断方法，用于标记和检测表达INSL4基因表达产物的所述组织的方法以及选择方法能够调节所述细胞活性的化合物。本发明还涉及用于治疗与所述组织的分化和/或异常增殖相关的病症的药物，特别是与软骨的异常发育相关的病症和/或正在形成的骨的异常骨化和/或相关的异常发育韧带。

9. 发明申请

WO99009172A1 METHOD FOR IDENTIFYING AND LOCATING EXPRESSED EPIL PEPTIDES, CODED BY THE INSL4 GENE AND THEIR USES 审中-公开
标题翻译：用于识别和定位INSL4基因编码的表达的EPIL肽的方法及其用途
公开(公告)号：WO99009172A1
公开(公告)日：1999-02-25
申请号：PCT/FR1998/001799
申请日：1998-08-12
IPC分类号： A61K38/00 , C07K14/64 , C07K16/26 , C12N15/16 , G01N33/68 , G01N33/74 , A61K38/22 , C12Q1/68 , G01N33/53 , G01N33/574
CPC分类号： G01N33/68 , A61K38/00 , C07K14/64 , C07K16/26 , G01N33/74 , G01N2333/62
摘要： The invention concerns the identification and localisation in the tissue of novel polypeptides expressed by the insulin-like 4 gene (INSL4), their amino acid and nucleic acid sequence, detection and diagnosis methods, methods for marking, selecting and detecting cells expressing said polypeptides or their corresponding nucleic sequence and methods for selecting compounds capable of modulating the activity of said polypeptides. The invention also concerns medicines for treating tumours, such as Kaposi's Sarcoma, for the vascularization of specific tissues, tissue differentiation and/or regeneration, modulating embryonary implantation and treating pathologies related to insulin-like activity such as diabetes and its complications.
摘要翻译：本发明涉及由胰岛素样4基因（INSL4）表达的新型多肽的组织中的鉴定和定位，其氨基酸和核酸序列，检测和诊断方法，标记，选择和检测表达所述多肽的细胞的方法或它们相应的核酸序列和选择能够调节所述多肽活性的化合物的方法。本发明还涉及用于治疗肿瘤的药物，例如卡波西氏肉瘤，用于特异性组织的血管化，组织分化和/或再生，调节胚胎植入和治疗与胰岛素样活性相关的病症如糖尿病及其并发症。

10. 发明申请

WO2019149782A1 MODIFIED LIPIDATED RELAXIN B CHAIN PEPTIDES AND THEIR THERAPEUTIC USE 审中-公开
公开(公告)号：WO2019149782A1
公开(公告)日：2019-08-08
申请号：PCT/EP2019/052298
申请日：2019-01-30
申请人： SANOFI
发明人： DUCLOS, Olivier , ILLIANO, Stéphane , MALLART, Sergio , MINOLETTI-HOCHEPIED, Claire , BIANCHI, Elisabetta , INGENITO, Raffaele , MAGOTTI, Paola , SANTOPRETE, Alessia
IPC分类号： C07K14/64 , A61K38/00
摘要： The present invention relates to a biologically active single chain Relaxin peptide having the following formula (I): N ter -Ac-X 10 -E-G-R-E-X 15 -V-R-X 18 -X 19 -I-X 21 -X 22 -E-G-X 25 -S-X 27 -X 28 -X 29 -X 30 -X 31 -X 32 -X 33 -NH 2 -C ter or a salt or solvate thereof. It also concerns a pharmaceutical composition comprising at least one peptide of the invention, and the peptide or the pharmaceutical composition for its use as a medicament.

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