公开(公告)号：US20060270695A1

公开(公告)日：2006-11-30

申请号：US11393133

申请日：2006-03-30

Applicant: Roland Dolle ,  Bertrand Le Bourdonnec ,  Guo-Hua Chu

Inventor： Roland Dolle ,  Bertrand Le Bourdonnec ,  Guo-Hua Chu

IPC: A61K31/4747

CPC classification number: C07D491/10 ,  C07D221/20 ,  C07D223/14 ,  C07D311/96 ,  C07D493/10 ,  C07D495/10

Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.

公开(公告)号：US20060074086A1

公开(公告)日：2006-04-06

申请号：US11242318

申请日：2005-10-03

Applicant: Roland Dolle ,  Karin Worm ,  Q. Jean Zhou

Inventor： Roland Dolle ,  Karin Worm ,  Q. Jean Zhou

IPC: A61K31/537 ,  C07D265/30

CPC classification number: C07D213/82 ,  C07C275/24 ,  C07C275/32 ,  C07C311/04 ,  C07C311/08 ,  C07D207/28 ,  C07D207/34 ,  C07D213/89 ,  C07D231/14 ,  C07D241/24 ,  C07D261/18 ,  C07D285/06 ,  C07D295/096 ,  C07D295/185 ,  C07D307/24 ,  C07D307/68 ,  C07D333/38

Abstract: Novel phenyl compounds, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, genitourinary disorders, inflammation, glaucoma, auto-immune diseases, ischemic conditions, immune-related disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, and as an appetite stimulant.

Abstract translation: 公开了新的苯基化合物，含有这些化合物的药物组合物及其药物用途的方法。 在某些实施方案中，化合物是大麻素受体的激动剂和/或配体，并且可用于治疗和/或预防疼痛，胃肠道疾病，泌尿生殖器疾病，炎症，青光眼，自身免疫疾病，缺血性疾病，免疫 相关疾病和神经变性疾病，用于提供针对缺血和再灌注作用的心脏保护，用于诱导恶性细胞中的细胞凋亡以及作为食欲刺激剂。

公开(公告)号：US20050203123A1

公开(公告)日：2005-09-15

申请号：US10798664

申请日：2004-03-11

Applicant: Roland Dolle ,  Bertrand Le Bourdonnec

Inventor： Roland Dolle ,  Bertrand Le Bourdonnec

IPC: A61K31/445 ,  A61K31/46 ,  C07D211/18 ,  C07D451/02 ,  C07D487/02

CPC classification number: C07D221/22 ,  A61K31/451 ,  A61K31/473 ,  A61K45/06 ,  C07D221/06 ,  A61K2300/00

Abstract: Certain 4-aryl-piperidine compounds, including N-substituted 9β-substituted-5-(3-substituted-phenyl)morphans and N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines, pharmaceutical compositions, and methods of their use, inter alia, as opioid antagonists are disclosed.

Abstract translation: 某些4-芳基哌啶化合物，包括N-取代的9b取代-5-（3-取代苯基）吗啡和N-取代的八氢-4a-（3-羟基苯基）-10a-甲基 - 苯并[g]异喹啉， 药物组合物及其使用方法，特别是作为阿片样物质拮抗剂。

公开(公告)号：US20050113295A1

公开(公告)日：2005-05-26

申请号：US10991785

申请日：2004-11-18

Applicant: Roland Dolle

Inventor： Roland Dolle

IPC: A61K31/4709 ,  A61K38/00 ,  A61K45/06 ,  C07D401/04 ,  C07K5/06 ,  C07K5/103 ,  C07K5/12 ,  C07K7/56 ,  C07K7/60 ,  A61K38/12

CPC classification number: C07D401/04 ,  A61K31/4709 ,  A61K38/00 ,  A61K45/06 ,  C07K5/06008 ,  C07K5/1013 ,  C07K5/123 ,  C07K5/126 ,  C07K7/56 ,  C07K7/60

Abstract: Carboxamide and amino derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the carboxamide derivatives are ligands of the δ opioid receptor and are useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, cancer, and other δ opioid receptor-mediated conditions.

Abstract translation: 公开了酰胺和氨基衍生物，含有这些化合物的药物组合物及其药物用途的方法。 在某些实施方案中，羧酰胺衍生物是δ阿片样物质受体的配体，尤其用于治疗和/或预防疼痛，焦虑，胃肠道疾病，癌症和其他δ阿片受体介导的病症。

公开(公告)号：US20080058302A1

公开(公告)日：2008-03-06

申请号：US11558332

申请日：2006-11-09

Applicant: Roland Dolle ,  Karin Worm

Inventor： Roland Dolle ,  Karin Worm

IPC: A61K31/195 ,  A61K31/34 ,  A61K31/397 ,  A61K31/40 ,  A61K31/445 ,  A61K31/535 ,  A61P25/00 ,  C07C307/02 ,  C07D265/30

CPC classification number: C07D295/26 ,  C07C311/38 ,  C07C311/40 ,  C07C311/42 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/42 ,  C07C2603/74 ,  C07D207/12 ,  C07D209/44 ,  C07D211/42 ,  C07D211/44

Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.

Abstract translation: 公开了新型氨磺酰苯甲酰胺化合物，含有氨磺酰苯甲酰胺化合物的药物组合物及其药物用途的方法。 在某些实施方案中，氨磺酰苯甲酰胺化合物是大麻素受体的激动剂和/或配体，尤其可用于治疗和/或预防疼痛，胃肠道疾病，炎症，自身免疫疾病，缺血性病症，免疫相关疾病 ，高血压，神经系统疾病和神经变性疾病，用于提供针对缺血和再灌注作用的心脏保护，用于诱导恶性细胞凋亡，用于抑制与神经损伤相关的机械痛觉过敏以及作为食欲刺激剂。

公开(公告)号：US20060223840A1

公开(公告)日：2006-10-05

申请号：US11442075

申请日：2006-05-25

Applicant: Roland Dolle ,  Bertrand Le Bourdonnec

Inventor： Roland Dolle ,  Bertrand Le Bourdonnec

IPC: C07D221/06 ,  A61K31/473

CPC classification number: C07D221/22 ,  A61K31/451 ,  A61K31/473 ,  A61K45/06 ,  C07D221/06 ,  A61K2300/00

Abstract: Certain 4-aryl-piperidine compounds, including N-substituted 9β-substituted-5-(3-substituted-phenyl)morphans and N-substituted octahydro-4a-(3-hydroxyphenyl)-10a-methyl-benzo[g]isoquinolines, pharmaceutical compositions, and methods of their use, inter alia, as opioid antagonists are disclosed.

Abstract translation: 某些4-芳基哌啶化合物，包括N-取代的9b取代-5-（3-取代苯基）吗啡和N-取代的八氢-4a-（3-羟基苯基）-10a-甲基 - 苯并[g]异喹啉， 药物组合物及其使用方法，特别是作为阿片样物质拮抗剂。

公开(公告)号：US20060079557A1

公开(公告)日：2006-04-13

申请号：US11251160

申请日：2005-10-13

Applicant: Roland Dolle ,  Karin Worm ,  Q. Zhou

Inventor： Roland Dolle ,  Karin Worm ,  Q. Zhou

IPC: C07D211/06 ,  A61K31/445

CPC classification number: C07D205/04 ,  C07C311/16 ,  C07C311/21 ,  C07C2602/42 ,  C07C2603/74 ,  C07D207/48 ,  C07D209/44 ,  C07D211/46 ,  C07D211/60 ,  C07D211/96 ,  C07D213/40 ,  C07D215/58 ,  C07D295/26

Abstract: Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or modulating ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.

Abstract translation: 公开了新型氨磺酰苯甲酰胺化合物，含有氨磺酰苯甲酰胺化合物的药物组合物及其药物用途的方法。 在某些实施方案中，氨磺酰苯甲酰胺化合物是大麻素受体的激动剂和/或调节配体，并且尤其可用于治疗和/或预防疼痛，胃肠道疾病，炎症，自身免疫疾病，缺血性病症，免疫相关 疾病，高血压，神经系统疾病和神经变性疾病，用于提供针对缺血和再灌注作用的心脏保护，用于诱导恶性细胞凋亡，用于抑制与神经损伤相关的机械痛觉过敏以及作为食欲刺激剂。

公开(公告)号：US20050054630A1

公开(公告)日：2005-03-10

申请号：US10651197

申请日：2003-08-28

Applicant: Roland Dolle ,  Guo-Hua Chu

Inventor： Roland Dolle ,  Guo-Hua Chu

IPC: A61K31/397 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/452 ,  C07D207/12 ,  C07D403/12 ,  C07D405/00 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D45/02

CPC classification number: C07D405/12 ,  C07D207/12 ,  C07D403/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14

Abstract: Fused bicyclic carboxamide derivatives are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.

Abstract translation: 公开了稠合的二环甲酰胺衍生物。 还公开了含有这些化合物的药物组合物及其使用方法。

公开(公告)号：US20080102031A1

公开(公告)日：2008-05-01

申请号：US11960845

申请日：2007-12-20

Applicant: Roland Dolle ,  Bertrand Le Bourdonnec ,  Christopher Ajello ,  Minghua Gu ,  Guo-Hua Chu ,  Paul Tuthill ,  Lara Leister ,  Q. Zhou

Inventor： Roland Dolle ,  Bertrand Le Bourdonnec ,  Christopher Ajello ,  Minghua Gu ,  Guo-Hua Chu ,  Paul Tuthill ,  Lara Leister ,  Q. Zhou

IPC: A61K47/00 ,  A61K31/407 ,  A61K31/4433 ,  A61K31/496 ,  A61P25/00 ,  A61P25/28 ,  A61P27/06 ,  A61P9/06 ,  C07D241/04 ,  C07D491/052 ,  C07D273/01 ,  C07D211/26 ,  A61P41/00 ,  A61P25/30 ,  A61P25/04 ,  A61P15/12 ,  A61K31/5355 ,  A61K31/55

CPC classification number: C07D491/107 ,  C07D221/20 ,  C07D311/96 ,  C07D401/04 ,  C07D493/10 ,  C07D495/10

Abstract: Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions.

Abstract translation: 公开了螺环杂环衍生物，含有这些化合物的药物组合物及其制药方法。 在某些实施方案中，螺环杂环衍生物是δ阿片受体受体的配体，尤其可用于治疗和/或预防疼痛，焦虑，胃肠道疾病和其他δ阿片受体介导的病症。

公开(公告)号：US20060089383A1

公开(公告)日：2006-04-27

申请号：US11217528

申请日：2005-09-01

Applicant: Bertrand Le Bourdonnec ,  Roland Dolle

Inventor： Bertrand Le Bourdonnec ,  Roland Dolle

IPC: A61K31/454 ,  A61K31/445 ,  C07D211/32 ,  C07D401/02

CPC classification number: C07D401/06 ,  C07D211/22 ,  C07D401/12 ,  C07F9/59

Abstract: Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

Abstract translation: 公开了新的3,4-二取代-4-芳基 - 哌啶化合物。 还公开了含有3,4-二取代-4-芳基 - 哌啶化合物的药物组合物及其药物用途的方法。 所公开的化合物尤其可用作阿片受体的拮抗剂。