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公开(公告)号:US08580918B2
公开(公告)日:2013-11-12
申请号:US13503010
申请日:2010-10-21
申请人: Sudarkodi Alagarsamy , Guangcheng Jiang , Pierre Riviere , Claudio Daniel Schteingart , Javier Sueiras-Diaz , Kazimierz Wisniewski
发明人: Sudarkodi Alagarsamy , Guangcheng Jiang , Pierre Riviere , Claudio Daniel Schteingart , Javier Sueiras-Diaz , Kazimierz Wisniewski
CPC分类号: C07K14/605 , A61K38/00
摘要: Novel GLP-2 analogs with improved pharmacokinetic properties are described as well as their use in the treatment of disease.
摘要翻译: 描述了具有改善的药代动力学性质的新型GLP-2类似物以及它们在治疗疾病中的用途。
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公开(公告)号:US20120231999A1
公开(公告)日:2012-09-13
申请号:US13503010
申请日:2010-10-21
申请人: Sudarkodi Alagarsamy , Guangcheng Jiang , Pierre Riviere , Claudio Daniel Schteingart , Javier Sueiras-Diaz
发明人: Sudarkodi Alagarsamy , Guangcheng Jiang , Pierre Riviere , Claudio Daniel Schteingart , Javier Sueiras-Diaz
IPC分类号: A61K38/16 , A61P1/00 , A61P3/04 , A61P3/10 , A61P1/04 , A61P37/08 , A61P29/00 , A61P25/24 , A61P19/10 , A61P25/00 , C07K14/00 , A61P3/00
CPC分类号: C07K14/605 , A61K38/00
摘要: Novel GLP-2 analogs with improved pharmacokinetic properties are described as well as their use in the treatment of disease.
摘要翻译: 描述了具有改善的药代动力学性质的新型GLP-2类似物以及它们在治疗疾病中的用途。
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公开(公告)号:US07713937B2
公开(公告)日:2010-05-11
申请号:US12119311
申请日:2008-05-12
申请人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
IPC分类号: A61K38/07
CPC分类号: C07K5/1016 , C07K7/02
摘要: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.
摘要翻译: 本发明涉及作为κ阿片受体的配体的合成肽酰胺,特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构:其中Xaa是D-氨基酸,G选自以下三组:所述化合物可用于预防和治疗与各种各样的相关的疼痛,瘙痒和炎症 疾病和病症。
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公开(公告)号:US20090156508A1
公开(公告)日:2009-06-18
申请号:US12119311
申请日:2008-05-12
申请人: Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人: Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
CPC分类号: C07K5/1016 , C07K7/02
摘要: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.
摘要翻译: 本发明涉及作为κ阿片受体的配体的合成肽酰胺,特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构:其中Xaa是D-氨基酸,G选自以下三组:所述化合物可用于预防和治疗与各种各样的相关的疼痛,瘙痒和炎症 疾病和病症。
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公开(公告)号:US20130012448A1
公开(公告)日:2013-01-10
申请号:US13543022
申请日:2012-07-06
申请人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
CPC分类号: C07K5/1016 , A61K38/00 , A61K38/07 , C07K5/10 , C07K5/1008 , C07K5/101 , C07K7/02
摘要: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
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公开(公告)号:US20090075907A1
公开(公告)日:2009-03-19
申请号:US12176279
申请日:2008-07-18
申请人: Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人: Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
CPC分类号: C07K5/1016 , A61K38/00 , A61K38/07 , C07K5/10 , C07K5/1008 , C07K5/101 , C07K7/02
摘要: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
摘要翻译: 本发明涉及κ阿片样物质受体的合成肽酰胺配体,特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片受体激动剂。 本发明的合成肽酰胺符合式I的结构:含有这些化合物的药物组合物可用于预防和治疗与多种疾病和病症相关的疼痛和炎症。 这种可治疗的疼痛包括内脏痛,神经性疼痛和痛觉过敏。 与IBD和IBS等条件相关的炎症,眼部和耳部炎症,其他疾病和病症如瘙痒症,水肿,低钠血症,低钾血症,肠梗阻,肠炎和青光眼均可用本发明的药物组合物治疗或预防。
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公开(公告)号:US20140357579A1
公开(公告)日:2014-12-04
申请号:US13959931
申请日:2013-08-06
申请人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
CPC分类号: C07K5/1016 , A61K38/00 , C07K5/1005 , C07K5/1008 , C07K5/1024 , C07K7/06
摘要: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: The compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions.
摘要翻译: 本发明涉及κ阿片样物质受体的合成肽酰胺配体,特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片受体激动剂。 本发明的合成肽酰胺符合以下结构:该化合物可用于预防和治疗与各种疾病和病症相关的疼痛和炎症。
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公开(公告)号:US08486894B2
公开(公告)日:2013-07-16
申请号:US12773992
申请日:2010-05-05
申请人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
IPC分类号: A61K38/07
CPC分类号: C07K5/1016 , C07K7/02
摘要: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.
摘要翻译: 本发明涉及作为κ阿片受体的配体的合成肽酰胺,特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构:其中Xaa是D-氨基酸,G选自以下三组:所述化合物可用于预防和治疗与各种各样的相关的疼痛,瘙痒和炎症 疾病和病症。
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公开(公告)号:US08217007B1
公开(公告)日:2012-07-10
申请号:US12786686
申请日:2010-05-25
申请人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Robert Zhiyong Luo
发明人: Claudio D. Schteingart , Frédérique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Robert Zhiyong Luo
IPC分类号: A61K38/07
CPC分类号: C07K5/1016 , A61K38/00 , A61K38/07 , C07K5/10 , C07K5/1008 , C07K5/101 , C07K7/02
摘要: The invention relates to synthetic peptide amide ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure of formula I: Pharmaceutical compositions containing these compounds are useful in the prophylaxis and treatment of pain and inflammation associated with a variety of diseases and conditions. Such treatable pain includes visceral pain, neuropathic pain and hyperalgesia. Inflammation associated with conditions such as IBD and IBS, ocular and otic inflammation, other disorders and conditions such as pruritis, edema, hyponatremia, hypokalemia, ileus, tussis and glaucoma are treatable or preventable with the pharmaceutical compositions of the invention.
摘要翻译: 本发明涉及κ阿片样物质受体的合成肽酰胺配体,特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片受体激动剂。 本发明的合成肽酰胺符合式I的结构:含有这些化合物的药物组合物可用于预防和治疗与各种疾病和病症相关的疼痛和炎症。 这种可治疗的疼痛包括内脏痛,神经性疼痛和痛觉过敏。 与IBD和IBS等条件相关的炎症,眼部和耳部炎症,其他疾病和病症如瘙痒症,水肿,低钠血症,低钾血症,肠梗阻,肠炎和青光眼均可用本发明的药物组合物治疗或预防。
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公开(公告)号:US20110118186A1
公开(公告)日:2011-05-19
申请号:US12773992
申请日:2010-05-05
申请人: Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
发明人: Claudio D. Schteingart , Frederique Menzaghi , Guangcheng Jiang , Roberta Vezza Alexander , Javier Sueiras-Diaz , Robert H. Spencer , Derek T. Chalmers , Zhiyong Luo
IPC分类号: A61K38/07 , C07K7/06 , A61K38/08 , C07K5/11 , C07K7/56 , A61K38/12 , C07K7/02 , A61P17/04 , A61P27/06 , A61P3/12 , A61P9/10 , A61P29/00 , A61P11/14
CPC分类号: C07K5/1016 , C07K7/02
摘要: The invention relates to synthetic peptide amides that are ligands of the kappa opioid receptor and particularly to agonists of the kappa opioid receptor that exhibit low P450 CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: wherein Xaa is a D-amino acid and G is selected from the following three groups: The compounds are useful in the prophylaxis and treatment of pain, pruritis and inflammation associated with a variety of diseases and conditions.
摘要翻译: 本发明涉及作为κ阿片受体的配体的合成肽酰胺,特别是涉及低P450 CYP抑制和低渗透入脑的κ阿片样物质受体的激动剂。 本发明的合成肽酰胺符合以下结构:其中Xaa是D-氨基酸,G选自以下三组:所述化合物可用于预防和治疗与各种各样的相关的疼痛,瘙痒和炎症 疾病和病症。
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