-
1.发明申请METHODS OF INHIBITING THE GHRELIN/GROWTH HORMONE SECRETATOGUE RECEPTOR PATHWAY AND USES THEREOF 有权抑制GHRELIN /生长激素分泌受体途径的方法及其用途公开(公告)号：US20170049849A9
公开(公告)日：2017-02-23
申请号：US14505101
申请日：2014-10-02
CPC分类号： A61K38/10 , A61K31/167 , A61K31/404 , A61K31/44 , A61K31/4418 , A61K31/495 , A61K38/08 , A61K38/22 , A61K45/06 , C07K7/06 , C07K7/08 , Y02P20/55 , A61K2300/00
摘要： The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.
摘要翻译： 本发明通过向受试者施用生长素释放肽O-酰基转移酶（GOAT）抑制剂和/或生长素释放肽受体拮抗剂来提供治疗，预防或控制受试者中肥胖症，肥胖相关病症，糖尿病和代谢综合征的方法。 本发明还提供式（VII）的生长素释放肽受体拮抗剂：A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18，其中A11，A12和A13各自独立地不存在， 氨基酸或氨基保护基; A15，A16，A17和A18各自独立地不存在或氨基酸; 并且A14是与-C（O）C1-C20烷基或与-C（O）C1-C20烷基共轭的二氨基丙酸缀合的丝氨酸，条件是存在A11，A12或A13中的至少一种。
-
公开(公告)号：US20190106473A1
公开(公告)日：2019-04-11
申请号：US16087426
申请日：2017-03-23
发明人： Joseph A. FUSELIER , David H. COY
IPC分类号： C07K14/655 , C07K14/765 , A61P37/06 , A61P1/04 , A61P19/02
摘要： Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)) including but not limited to conjugates comprising FK-506 and ascomycin. Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating. Further embodiments include methods for making the inventive compound. Additional embodiments of the invention are also discussed herein.
-
3.发明申请ANALOGS OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND METHODS FOR THEIR USE 审中-公开丙烯酸环化酶活化多肽（PACAP）的模拟物及其使用方法公开(公告)号：US20150104388A1
公开(公告)日：2015-04-16
申请号：US14578818
申请日：2014-12-22
发明人： David H. COY , Jerome L. MADERDRUT , Min LI
CPC分类号： C07K14/57563 , A61K33/24 , A61K38/00 , A61K38/2278 , A61K45/06 , A61K47/64 , A61K51/088 , A61L31/08 , A61L31/16 , A61L2300/252 , A61L2300/40 , A61L2420/00 , C07K2319/50 , A61K2300/00
摘要： This invention relates to novel analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC1, VPAC1 and VPAC2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders, including (but not limited to) cancer and autoimmune disease. These PACAP analogs can be coupled to suitable radionuclides and used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, or coupled to small molecule therapeutics and used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP-like compounds of the invention either alone or in combination with one or more other prophylactic/therapeutic agents.
摘要翻译： 本发明涉及垂体腺苷酸环化酶活化多肽（PACAP）的新型类似物，其是PACAP /血管活性肠肽（VIP）受体的激动剂：PAC1，VPAC1和VPAC2受体。 这些PACAP类似物可以用作广泛的医学疾病的预防/治疗剂，包括（但不限于）癌症和自身免疫性疾病。 这些PACAP类似物可以耦合到合适的放射性核素，并用于弥散性癌症和转移性肿瘤的定位，诊断和治疗，或与小分子治疗剂偶联，并用作靶向药物递送的载体。 本发明还提供单独一种或与一种或多种其它预防/治疗剂组合的本发明的一种或多种PACAP样化合物的药物组合物。
-
4.发明申请ANALOGS OF PITUITARY ADENYLATE CYCLASE-ACTIVATING POLYPEPTIDE (PACAP) AND METHODS FOR THEIR USE 审中-公开丙烯酸环化酶活化多肽（PACAP）的模拟物及其使用方法公开(公告)号：US20160122406A1
公开(公告)日：2016-05-05
申请号：US14896178
申请日：2014-06-09
发明人： David H. COY , Jerome L. MADERDRUT
CPC分类号： C07K14/4705 , A61K38/13 , A61K38/14 , A61K38/1816 , A61K45/06 , A61K47/64 , A61K49/0004 , A61K51/08 , C07K14/57563 , A61K2300/00
摘要： This invention relates to analogs of pituitary adenylate cyclase-activating polypeptide (PACAP), which are agonists for the PACAP/vasoactive intestinal peptide (VIP) receptors: PAC1, VPAC1 and VPAC2 receptors. These PACAP analogs can be used as prophylactic/therapeutic agents for a wide range of medical disorders. These PACAP analogs coupled to suitable radionuclides can be used in the localization, diagnosis and treatment of disseminated cancers and metastatic tumors, and coupled to small molecule therapeutics can be used as vectors for targeted drug delivery. This invention also provides pharmaceutical compositions of one or more PACAP analogs of the invention either alone or in combination with one or more other prophylactic/therapeutic agent.
摘要翻译： 本发明涉及垂体腺苷酸环化酶活化多肽（PACAP）的类似物，其是PACAP /血管活性肠肽（VIP）受体的激动剂：PAC1，VPAC1和VPAC2受体。 这些PACAP类似物可用作广泛的医学疾病的预防/治疗剂。 耦合到合适的放射性核素的这些PACAP类似物可用于弥散性癌症和转移性肿瘤的定位，诊断和治疗，并且与小分子治疗剂相结合可用作靶向药物递送的载体。 本发明还提供单独的或与一种或多种其它预防/治疗剂组合的本发明的一种或多种PACAP类似物的药物组合物。
-
5.发明申请METHODS OF INHIBITING THE GHRELIN/GROWTH HORMONE SECRETATOGUE RECEPTOR PATHWAY AND USES THEREOF 有权抑制GHRELIN /生长激素分泌受体途径的方法及其用途公开(公告)号：US20150031605A1
公开(公告)日：2015-01-29
申请号：US14505101
申请日：2014-10-02
CPC分类号： A61K38/10 , A61K31/167 , A61K31/404 , A61K31/44 , A61K31/4418 , A61K31/495 , A61K38/08 , A61K38/22 , A61K45/06 , C07K7/06 , C07K7/08 , Y02P20/55 , A61K2300/00
摘要： The invention provides methods for treatment, prevention or management of obesity, obesity related disorders, diabetes mellitus, and metabolic syndrome in a subject by administering a ghrelin O-acyltransferase (GOAT) inhibitor and/or a ghrelin receptor antagonist to the subject. The invention also provides ghrelin receptor antagonists of formula (VII): A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18, wherein each of A11, A12, and A13 is independently absent, an amino acid, or an amino protecting group; each of A15, A16, A17, and A18 is independently absent or an amino acid; and A14 is a serine conjugated with a —C(O)C1-C20alky or a diaminopropionic acid conjugated with a —C(O)C1-C20alkyl group, provided that at least one of A11, A12, or A13 is present.
摘要翻译： 本发明通过向受试者施用生长素释放肽O-酰基转移酶（GOAT）抑制剂和/或生长素释放肽受体拮抗剂来提供治疗，预防或控制受试者中肥胖症，肥胖相关病症，糖尿病和代谢综合征的方法。 本发明还提供式（VII）的生长素释放肽受体拮抗剂：A11-A12-A13-Gly-Ser-A14-Phe-Leu-A15-A16-A17-A18，其中A11，A12和A13各自独立地不存在， 氨基酸或氨基保护基; A15，A16，A17和A18各自独立地不存在或氨基酸; 并且A14是与-C（O）C1-C20烷基或与-C（O）C1-C20烷基共轭的二氨基丙酸缀合的丝氨酸，条件是存在A11，A12或A13中的至少一种。
-
-
-
-
搜索结果
5 条记录 (耗时 0.025 秒)
