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1. 发明申请

US20070105759A1 Melanocortin receptor 4 (mc4) agonists and their uses 审中-公开
标题翻译：黑皮质素受体4（mc4）激动剂及其用途
公开(公告)号：US20070105759A1
公开(公告)日：2007-05-10
申请号：US10556689
申请日：2004-06-17
申请人： David Flora , Mark Heiman , JeAnne Hertel , Hansen Hsiung , John Mayer , David Smiley , Liang Yan , Lianshan Zhang
发明人： David Flora , Mark Heiman , JeAnne Hertel , Hansen Hsiung , John Mayer , David Smiley , Liang Yan , Lianshan Zhang
IPC分类号： A61K38/12 , C07K7/64
CPC分类号： C07K14/68 , A61K38/12
摘要： The present invention relates to peptide agonists of the MC4 receptor, and as such are useful in the treatment of disorders responsive to the activation of this receptor, such as obesity, diabetes mellitus and male and/or female sexual dysfunction.
摘要翻译：本发明涉及MC4受体的肽激动剂，因此可用于治疗对该受体的活化有响应的病症，例如肥胖症，糖尿病和男性和/或女性性功能障碍。

2. 发明申请

US20060293223A1 Uses of melanocortin-3 receptor (mc3r) agonist peptides 审中-公开
标题翻译：黑皮质素-3受体（mc3r）激动剂肽的使用
公开(公告)号：US20060293223A1
公开(公告)日：2006-12-28
申请号：US10556690
申请日：2004-06-17
申请人： Robert Gadski , Mark Heiman , Hansen Hsiung , John Mayer , Liang Yan
发明人： Robert Gadski , Mark Heiman , Hansen Hsiung , John Mayer , Liang Yan
IPC分类号： A61K38/12
CPC分类号： A61K38/12
摘要： The present invention provides methods of treating metabolic disorders, including, for example, obesity, diabetes mellitus, cachexia, sarcopenia, and cardiovascular disorders, methods of inducing weight loss and increasing muscle mass in a patient, by administration of MC3R agonist peptides. Furthermore, the present invention provides the use of an MC3R agonist peptide for the manufacture of a medicament for the treatment of metabolic disorders, including, for example, obesity, diabetes mellitus, cachexia, sarcopenia, and cardiovascular disorders, inducing weight loss and increasing muscle mass in a patient.
摘要翻译：本发明提供了通过施用MC3R激动剂肽来治疗代谢紊乱的方法，包括例如肥胖症，糖尿病，恶病质，肌营养不良和心血管疾病，诱导患者体重减轻和增加肌肉质量的方法。此外，本发明提供了MC3R激动剂肽用于制备用于治疗代谢紊乱的药物的用途，所述代谢紊乱包括例如肥胖，糖尿病，恶病质，肌营养不良和心血管疾病，引起体重减轻和增加肌肉在病人身上。

3. 发明申请

US20070123453A1 Uses of melanocortin-4 receptor (mc4r) agonist peptides administered by continuous infusion 审中-公开
标题翻译：通过连续输注施用黑皮质素-4受体（mc4r）激动剂肽的用途
公开(公告)号：US20070123453A1
公开(公告)日：2007-05-31
申请号：US10588667
申请日：2004-06-17
申请人： Mark Heiman , JeAnne Hertel
发明人： Mark Heiman , JeAnne Hertel
IPC分类号： A61K38/12
CPC分类号： A61K38/12
摘要： The present invention provides a method of inducing weight loss in a patient, comprising continuous infusion of an effective amount of an MC4R agonist peptide into the patient. Additionally, the present invention provides a method of treating obesity in a patient, comprising continuous infusion of an effective amount of an MC4R agonist peptide into the patient. Furthermore, the present invention provides the use of an MC4R agonist peptide for the manufacture of a medicament for the treatment of obesity, wherein the medicament is administered by continuous infusion.
摘要翻译：本发明提供了一种诱导患者体重减轻的方法，包括将有效量的MC4R激动剂肽连续输注到患者体内。另外，本发明提供一种治疗患者肥胖症的方法，包括将有效量的MC4R激动剂肽连续输注到患者体内。此外，本发明提供了MC4R激动剂肽在制备用于治疗肥胖症的药物中的用途，其中所述药物通过连续输注施用。

4. 发明申请

US20060269550A1 Anti-ghrelin fab antibodies 审中-公开
标题翻译：抗Ghrelin fab抗体
公开(公告)号：US20060269550A1
公开(公告)日：2006-11-30
申请号：US10558604
申请日：2004-05-28
申请人： Mark Heiman
发明人： Mark Heiman
IPC分类号： A61K39/395 , C07H21/04 , C12P21/06 , C07K16/26 , C12N5/06
CPC分类号： C07K16/26 , A61K2039/505 , C07K2317/34 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/76 , C07K2317/92
摘要： Monoclonal antibodies and antigen-binding portions thereof that preferentially bind acetylated human ghrelin with respect to unacylated human ghrelin are disclosed. These molecules have high affinity for acylated human ghrelin, a slow off rate for acylated human ghrelin dissociation, and neutralize an acylated human ghrelin activity. These antibodies or antigen-binding portions thereof are useful for neutralizing ghrelin activity, e.g., in a human subject suffering from a disorder in which ghrelin activity is detrimental.
摘要翻译：公开了相对于未被抑制的人类生长素释放肽优先结合乙酰化的人生长素释放肽的单克隆抗体及其抗原结合部分。这些分子对酰化的人生长素释放肽具有高亲和力，是酰化人类生长素释放肽解离的缓慢速率，并且中和酰化的人类生长素释放肽活性。这些抗体或其抗原结合部分可用于中和生长素释放肽活性，例如在患有生长素释放肽活性有害的病症的人类受试者中。

5. 发明申请

US20060233788A1 Anti-ghrelin antibodies 审中-公开
标题翻译：抗Ghrelin抗体
公开(公告)号：US20060233788A1
公开(公告)日：2006-10-19
申请号：US10568467
申请日：2004-09-02
申请人： Mark Heiman , Kristine Kikly , Joseph Manetta , Derrick Witcher
发明人： Mark Heiman , Kristine Kikly , Joseph Manetta , Derrick Witcher
IPC分类号： A61K39/395
CPC分类号： C07K16/26 , A61K2039/505 , C07K2317/34 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/92
摘要： Monoclonal antibodies, including humanized and chimeric antibodies, that bind acylated and unacylated human ghrelin are provided. Such monoclonal antibodies can be full-length, or an antigen-binding portion thereof, and are useful for neutralizing ghrelin activity, e.g., in a human subject suffering from a disorder in which ghrelin activity is detrimental.
摘要翻译：提供了结合酰化和未被消化的人类生长素释放肽的单克隆抗体，包括人源化和嵌合抗体。这样的单克隆抗体可以是全长的或其抗原结合部分，并且可用于中和生长素释放肽活性，例如在患有其中生长素释放肽活性是有害的病症的人类受试者中。

6. 发明申请

US20050277677A1 Method for treating emesis with ghrelin agonists 审中-公开
标题翻译：用生长素释放肽激动剂治疗呕吐的方法
公开(公告)号：US20050277677A1
公开(公告)日：2005-12-15
申请号：US11130766
申请日：2005-05-17
申请人： Mark Heiman , Dana Sindelar
发明人： Mark Heiman , Dana Sindelar
IPC分类号： A61K31/4172 , A61K31/4178 , A61K31/454
CPC分类号： A61K31/4172 , A61K31/4178 , A61K31/454
摘要： The present invention relates to a method comprising administering to a patient diagnosed as being in need of treatment for nausea, emesis, or symptoms associated therewith comprising administering to a patient in need thereof a compound of formula (I) wherein: R1 is C6H5CH2OCH2—, C6H5(CH2)3— or indol-3-ylmethyl; Y is pyrrolidinyl, 4-methyl-piperidinyl or NR2R2; R2 are each independently C1-C6 alkyl; R3 is 2-napthyl or phenyl para-substituted by W; W is H, F, CF3, C1-C6 alkoxy or phenyl; and R4 is H or CH3; or a pharmaceutically acceptable salt or solvate thereof, in an amount that is effective in treating nausea, emesis, or symptoms associated therewith in said patient.
摘要翻译：本发明涉及一种方法，其包括向被诊断为需要治疗的患者施用恶心，呕吐或与之相关的症状的方法，包括向有需要的患者施用式（I）化合物，其中：R 1 C 6是C 6 H 5 CH 2 CH 2 CH 2 - ， - C 6 - （CH 2）3 - 或吲哚-3-基甲基; Y是吡咯烷基，4-甲基 - 哌啶基或NR 2 R 2; R 2各自独立地为C 1 -C 6烷基; R 3是2-萘基或被W对位取代的苯基; W是H，F，CF 3，C 1 -C 6烷氧基或苯基; R 4是H或CH 3; 或其药学上可接受的盐或溶剂合物，其量可有效治疗所述患者的恶心，呕吐或与之相关的症状。

7. 发明申请

US20050201938A1 Method for selectively inhibiting ghrelin action 审中-公开
标题翻译：选择性抑制生长素释放肽作用的方法
公开(公告)号：US20050201938A1
公开(公告)日：2005-09-15
申请号：US11106899
申请日：2005-04-15
申请人： Henry Bryant , Mark Heiman
发明人： Henry Bryant , Mark Heiman
IPC分类号： A61K31/00 , A61K38/25 , A61K38/27 , A61K45/06 , A61K49/00 , A61K49/04 , C07K16/18 , G01N33/50 , G01N33/74 , C12Q1/00 , A61K38/17
CPC分类号： A61K31/00 , A61K38/25 , A61K38/27 , A61K45/06 , A61K49/0004 , A61K49/04 , A61K2039/505 , C07K16/18 , G01N33/5008 , G01N33/502 , G01N33/5058 , G01N33/5088 , G01N33/74 , G01N2500/10 , A61K2300/00
摘要： The present invention provides a method selectively inhibiting ghrelin activity to treat a variety of diseases including obesity and related disorders, particularly in individuals who are genetically predisposed. One aspect of the invention comprises administering an agent that effectively neutralizes ghrelin. Another aspect comprises administering a ghrelin receptor (growth hor- mone secretagogue receptor) antagonist.
摘要翻译：本发明提供了选择性抑制生长素释放肽活性以治疗多种疾病的方法，包括肥胖症和相关疾病，特别是在遗传易感患者中。本发明的一个方面包括施用有效中和生长素释放肽的药剂。另一方面包括施用生长素释放肽受体（生长激素促分泌素受体）拮抗剂。

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