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1. 发明申请

WO2008057608A3 SYNTHETIC PEPTIDE AMIDES 审中-公开
公开(公告)号：WO2008057608A3
公开(公告)日：2008-05-15
申请号：PCT/US2007/023858
申请日：2007-11-12
申请人： CARA THERAPEUTICS, INC. , SCHTEINGART, Claudio, D. , MENZAGHI, Frederique , JIANG, Guangcheng , ALEXANDER, Roberta, Vezza , SUEIRAS-DIAZ, Javier , SPENCER, Robert, H. , CHALMERS, Derek, T. , LUO, Zhiyong
发明人： SCHTEINGART, Claudio, D. , MENZAGHI, Frederique , JIANG, Guangcheng , ALEXANDER, Roberta, Vezza , SUEIRAS-DIAZ, Javier , SPENCER, Robert, H. , CHALMERS, Derek, T. , LUO, Zhiyong
IPC分类号： C07K5/107 , C07K7/02 , A61K38/07 , A61K38/08
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 P 450 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.

2. 发明申请

WO2007139921A2 N-OXIDES OF KAPPA OPIOID RECEPTOR PEPTIDES 审中-公开
标题翻译： KAPPA阿片受体肽的N-氧化物
公开(公告)号：WO2007139921A2
公开(公告)日：2007-12-06
申请号：PCT/US2007/012463
申请日：2007-05-25
申请人： CARA THERAPEUTICS, INC. , JUNIEN, Jean-Louis , RIVIERE, Pierre, J., M. , SCHTEINGART, Claudio, D. , DIAZ, Javier, S. , TROJNAR, Jerzy, A. , VANDERAH, Todd, W. , LEWIS, Michael, E.
发明人： JUNIEN, Jean-Louis , RIVIERE, Pierre, J., M. , SCHTEINGART, Claudio, D. , DIAZ, Javier, S. , TROJNAR, Jerzy, A. , VANDERAH, Todd, W. , LEWIS, Michael, E.
IPC分类号： C07K5/10 , C07K5/107 , C07K5/117 , A61K38/07 , A61P29/00 , A61P13/10 , A61P1/00 , A61P17/04 , A61P37/00
CPC分类号： C07K5/1016 , A61K38/00
摘要： Certain peptides which exhibit high selectivity for the kappa opioid receptor (KOR) versus the mu opioid receptor and little or no CYP3A4 inhibitory activity including tetrapeptides of four D-isomer amino acid residues having a C-terminus which is an N-oxide-substituted amide such, as H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4- picolyl-N-oxide. A preferred compound, which has an affinity for the KOR at least 1,000 times its affinity for the mu opioid receptor and an IC50 for CYP3 A4 of greater than about 10 micromolar, is H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide
摘要翻译：对于κ阿片样物质受体（KOR）与μ-阿片样物质受体显示出高选择性的某些肽，并且很少或没有CYP3A4抑制活性，包括具有C-末端的四个D-异构体氨基酸残基的四肽，其是N-氧化物取代的酰胺如HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基-N-氧化物。 HD-Phe-D-Phe-D-Nle-D-D对于KOR具有对μ-阿片样物质受体的亲和力至少1000倍的亲和力以及大于约10微摩尔的CYP3A4的IC 50的优选化合物，精氨酸-NH-4-吡啶甲基-N-氧化物

3. 发明申请

WO2007139921A3 N-OXIDES OF KAPPA OPIOID RECEPTOR PEPTIDES 审中-公开
标题翻译： KAPPA阿片受体肽的N-氧化物
公开(公告)号：WO2007139921A3
公开(公告)日：2008-01-24
申请号：PCT/US2007012463
申请日：2007-05-25
申请人： CARA THERAPEUTICS INC , JUNIEN JEAN-LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER S , TROJNAR JERZY A , VANDERAH TODD W , LEWIS MICHAEL E
发明人： JUNIEN JEAN-LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER S , TROJNAR JERZY A , VANDERAH TODD W , LEWIS MICHAEL E
IPC分类号： C07K5/10 , A61K38/07 , A61P1/00 , A61P13/10 , A61P17/04 , A61P29/00 , A61P37/00 , C07K5/107 , C07K5/117
CPC分类号： C07K5/1016 , A61K38/00
摘要： Certain peptides which exhibit high selectivity for the kappa opioid receptor (KOR) versus the mu opioid receptor and little or no CYP3A4 inhibitory activity including tetrapeptides of four D-isomer amino acid residues having a C-terminus which is an N-oxide-substituted amide such, as H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4- picolyl-N-oxide. A preferred compound, which has an affinity for the KOR at least 1,000 times its affinity for the mu opioid receptor and an IC50 for CYP3 A4 of greater than about 10 micromolar, is H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide
摘要翻译：对于κ阿片样物质受体（KOR）与μ-阿片样物质受体显示出高选择性的某些肽，并且很少或没有CYP3A4抑制活性，包括具有C-末端的四个D-异构体氨基酸残基的四肽，其是N-氧化物取代的酰胺如HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基-N-氧化物。 HD-Phe-D-Phe-D-Nle-D-D对于KOR具有对μ-阿片样物质受体的亲和力至少1000倍的亲和力以及大于约10微摩尔的CYP3A4的IC 50的优选化合物，精氨酸-NH-4-吡啶甲基-N-氧化物

4. 发明申请

WO2005037798A3 AMIDE OR THIOMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF PAIN 审中-公开
标题翻译：酰胺或其衍生物及其在治疗疼痛中的应用
公开(公告)号：WO2005037798A3
公开(公告)日：2005-06-16
申请号：PCT/US2004033698
申请日：2004-10-14
申请人： FERRING BV , CHANG CHIA-PING , STALEWSKI JACEK , RIVIERE PIERRE J-M , WISNIEWSKI KAZIMIERZ A , SCHTEINGART CLAUDIO D
发明人： CHANG CHIA-PING , STALEWSKI JACEK , RIVIERE PIERRE J-M , WISNIEWSKI KAZIMIERZ A , SCHTEINGART CLAUDIO D
IPC分类号： C07C237/22 , C07C275/28 , C07C279/28 , A61K31/165 , A61K31/17 , A61P25/04
CPC分类号： C07C275/28 , C07C237/22 , C07C2601/08 , C07C2601/14
摘要： The present invention relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of pain and disorders related thereto as well as a method for treatment of pain and disorders related thereto, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.
摘要翻译：本发明涉及新化合物，包含其的药物组合物，所述化合物在制备用于治疗与其相关的疼痛和病症的药物中的用途以及治疗与其相关的疼痛和病症的方法，其中所述化合物是管理。化合物由通式（I）表示，如说明书中进一步定义的。

5. 发明申请

WO2008060552A3 SYNTHETIC PEPTIDE AMIDES AND DIMERS THEREOF 审中-公开
公开(公告)号：WO2008060552A3
公开(公告)日：2008-05-22
申请号：PCT/US2007/023874
申请日：2007-11-13
申请人： CARA THERAPEUTICS, INC. , SCHTEINGART, Claudio, D. , MENZAGHI, Frederique , JIANG, Guangcheng , ALEXANDER, Roberta, Vezza , SUEIRAS-DIAZ, Javier , SPENCER, Robert, H. , CHALMERS, Derek, T. , LUO, Zhiyong
发明人： SCHTEINGART, Claudio, D. , MENZAGHI, Frederique , JIANG, Guangcheng , ALEXANDER, Roberta, Vezza , SUEIRAS-DIAZ, Javier , SPENCER, Robert, H. , CHALMERS, Derek, T. , LUO, Zhiyong
IPC分类号： C07K5/10 , A61K38/07
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 P 45O CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: 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.

6. 发明申请

WO2005037798A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2005037798A2
公开(公告)日：2005-04-28
申请号：PCT/US2004/033698
申请日：2004-10-14
申请人： FERRING B.V. , CHANG, Chia-Ping , STALEWSKI, Jacek , RIVIERE , Pierre, J-M. , WISNIEWSKI , Kazimierz, A. , SCHTEINGART , Claudio, D.
发明人： CHANG, Chia-Ping , STALEWSKI, Jacek , RIVIERE , Pierre, J-M. , WISNIEWSKI , Kazimierz, A. , SCHTEINGART , Claudio, D.
IPC分类号： C07D233/00
CPC分类号： C07C275/28 , C07C237/22 , C07C2601/08 , C07C2601/14
摘要： The present invention relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of pain and disorders related thereto as well as a method for treatment of pain and disorders related thereto, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.
摘要翻译：本发明涉及新化合物，包含其的药物组合物，所述化合物在制备用于治疗与其相关的疼痛和病症的药物中的用途以及治疗与其相关的疼痛和病症的方法，其中所述化合物是管理。化合物由通式（I）表示，如说明书中进一步定义的。

7. 发明申请

WO9932510A9 KAPPA RECEPTOR OPIOID PEPTIDES 审中-公开
标题翻译： KAPPA受体OPIOID PEPTIDES
公开(公告)号：WO9932510A9
公开(公告)日：1999-09-23
申请号：PCT/US9827282
申请日：1998-12-22
申请人： FERRING BV , JUNIEN JEAN LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER SUEIRAS , TROJNAR JERZY A , VANDERAH TODD W
发明人： JUNIEN JEAN LOUIS , RIVIERE PIERRE J M , SCHTEINGART CLAUDIO D , DIAZ JAVIER SUEIRAS , TROJNAR JERZY A , VANDERAH TODD W
IPC分类号： A61K38/00 , A61K38/07 , A61P1/04 , A61P13/00 , A61P13/10 , A61P25/04 , C07K5/10 , C07K5/107 , C07K5/117
CPC分类号： C07K5/1027 , A61K38/00 , C07K5/1016 , C07K5/1024
摘要： Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono- or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED50 of not greater than about 0.5 mg/kg, include H-D-Phe-D-Phe-D-Nle-D-Arg-NHEt, H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr, H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NEt2, H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe, H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl, H-D-4Fpa-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl, H-D-Ala-(2Thi)-D-3, 4Cpa-D-Leu-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Gmf-morpholinyl, H-D-Phe-D-Phe-D-Leu-D-Orn-NH(Aeb), H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl, and H-D-Phe-D-Phe-D-Nle-D-Arg-NH(Hoh).
摘要翻译：产生对κ阿片样物质受体（KOR）具有高选择性且长时间持续的外周作用但不明显进入脑的肽是具有C末端的四个D-异构体氨基酸残基的序列，其是单或二取代酰胺。对KOR具有至少1,000次对μ阿片受体的亲和力和不大于约0.5mg / kg的ED 50的亲和力的代表性化合物包括HD-Phe-D-Phe-D-Nle-D-Arg -NHEt，HD-Phe-D-Phe-D-Nle-D-Arg-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NH-4-吡啶甲基，HD-Phe-D-Phe -D-Nle-D-Arg-NHPr，HD-Phe-D-Phe-D-Nle-D-Arg-硫代吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-NEt2，HD-Phe -D-Phe-D-Nle-D-Arg-NHMe，HD-Phe-D-Phe-D-Leu-D-Orn-吗啉基，HD-4Fpa-D-Phe-D-Nle-D-Arg-NH 4-吡啶甲基，HD-Phe-D-Phe-D-Nle-D-Arg-NH-环丙基，HD-Ala-（2Thi）-D-3,4cpa-D-Leu-D-Arg-吗啉基，HD -Phe-D-Phe-D-Nle-D-Gmf-吗啉基，HD-Phe-D-Phe-D-Leu-D-Orn-NH（Aeb），HD-Phe-D-Phe-D-Leu- D-Lys-吗啉基，HD-Phe-D-Phe-D-Nle-D-Arg-哌嗪基和HD-Phe-D-Phe-D-Nle-D-Arg-NH（Hoh）。

8. 发明申请

WO2010022171A1 PEPTIDIC PTH RECEPTOR AGONISTS 审中-公开
标题翻译： PEPTIDIC PTH受体激素
公开(公告)号：WO2010022171A1
公开(公告)日：2010-02-25
申请号：PCT/US2009/054342
申请日：2009-08-19
申请人： FERRING INTERNATIONAL CENTER S.A. , SCHTEINGART, Claudio, D. , SUEIRAS-DIAZ, Javier
发明人： SCHTEINGART, Claudio, D. , SUEIRAS-DIAZ, Javier
IPC分类号： A61K38/00
CPC分类号： C07K14/635 , A61K38/00
摘要： Novel peptidic pth receptor agonists and methods of using the same are provided.
摘要翻译：提供新型肽肽受体激动剂及其使用方法。

9. 发明申请

WO2008057608A8 SYNTHETIC PEPTIDE AMIDES 审中-公开
标题翻译：合成肽类
公开(公告)号：WO2008057608A8
公开(公告)日：2008-12-11
申请号：PCT/US2007023858
申请日：2007-11-12
申请人： CARA THERAPEUTICS INC , SCHTEINGART CLAUDIO D , MENZAGHI FREDERIQUE , JIANG GUANGCHENG , ALEXANDER ROBERTA VEZZA , SUEIRAS-DIAZ JAVIER , SPENCER ROBERT H , CHALMERS DEREK T , LUO ZHIYONG
发明人： SCHTEINGART CLAUDIO D , MENZAGHI FREDERIQUE , JIANG GUANGCHENG , ALEXANDER ROBERTA VEZZA , SUEIRAS-DIAZ JAVIER , SPENCER ROBERT H , CHALMERS DEREK T , LUO ZHIYONG
IPC分类号： C07K5/107 , A61K38/07 , A61K38/08 , C07K7/02
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。

10. 发明申请

WO2008060552A2 SYNTHETIC PEPTIDE AMIDES AND DIMERS THEREOF 审中-公开
标题翻译：合成肽类及其类似物
公开(公告)号：WO2008060552A2
公开(公告)日：2008-05-22
申请号：PCT/US2007023874
申请日：2007-11-13
申请人： CARA THERAPEUTICS INC , SCHTEINGART CLAUDIO D , MENZAGHI FREDERIQUE , JIANG GUANGCHENG , ALEXANDER ROBERTA VEZZA , SUEIRAS-DIAZ JAVIER , SPENCER ROBERT H , CHALMERS DEREK T , LUO ZHIYONG
发明人： SCHTEINGART CLAUDIO D , MENZAGHI FREDERIQUE , JIANG GUANGCHENG , ALEXANDER ROBERTA VEZZA , SUEIRAS-DIAZ JAVIER , SPENCER ROBERT H , CHALMERS DEREK T , LUO ZHIYONG
IPC分类号： C07K5/10 , A61K38/07
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 P 45O CYP inhibition and low penetration into the brain. The synthetic peptide amides of the invention conform to the structure: 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，特别涉及表现出低P CYP抑制和低渗透入脑的κ阿片受体的激动剂。本发明的合成肽酰胺符合以下结构：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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