公开(公告)号：US20120115894A1

公开(公告)日：2012-05-10

申请号：US13254363

申请日：2010-02-22

Applicant: Ping Liu ,  Robert J. DeVita ,  Linus S. Lin ,  Marc D. Chioda ,  Terence G Hamill ,  Wenping Li

Inventor： Ping Liu ,  Robert J. DeVita ,  Linus S. Lin ,  Marc D. Chioda ,  Terence G Hamill ,  Wenping Li

IPC: A61K31/506 ,  A61K31/4439 ,  C07D233/84 ,  A61K31/4164 ,  C07D413/14 ,  C07D401/14 ,  C07D413/10 ,  A61K31/4245 ,  A61P19/02 ,  A61P29/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/20 ,  A61P25/28 ,  A61P25/16 ,  C07D401/12

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D413/10 ,  C07D413/14

Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）和FAAH显像剂的调节剂的某些咪唑衍生物。 本发明还涉及包含这些化合物作为活性成分的药物制剂，以及这些化合物及其制剂在治疗某些疾病，包括骨关节炎，类风湿性关节炎，糖尿病性神经病变，带状疱疹后神经痛，ke肉肌痛和纤维肌痛等方面的用途。 作为急性疼痛，偏头痛，睡眠障碍，阿尔茨海默病和帕金森病。

公开(公告)号：US08106070B2

公开(公告)日：2012-01-31

申请号：US12311541

申请日：2007-10-16

Applicant: David Chen ,  Christopher L. Franklin ,  Peter R. Guzzo ,  Linus S. Lin ,  Jian Liu ,  Michael M. -C. Lo ,  Ravi P. Nargund ,  Iyassu K. Sebhat

Inventor： David Chen ,  Christopher L. Franklin ,  Peter R. Guzzo ,  Linus S. Lin ,  Jian Liu ,  Michael M. -C. Lo ,  Ravi P. Nargund ,  Iyassu K. Sebhat

IPC: A61K31/437 ,  A61K31/44 ,  A61K31/4178 ,  C07D401/10 ,  C07D231/02 ,  C07D471/04

CPC classification number: C07D401/10 ,  C07D233/64 ,  C07D401/14 ,  C07D403/10 ,  C07D417/10 ,  C07D471/04

Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

Abstract translation: 某些新颖的取代的咪唑是人类bombesin受体的配体，特别是人类bombesin受体亚型-3（BRS-3）的选择性配体。 因此，它们可用于治疗，控制或预防对调节BRS-3的疾病和病症，例如肥胖症和糖尿病。

公开(公告)号：US20110269769A1

公开(公告)日：2011-11-03

申请号：US12996429

申请日：2009-06-04

Applicant: Linus S. Lin ,  Marc D. Chioda ,  Ping Liu ,  Ravi P. Nargund

Inventor： Linus S. Lin ,  Marc D. Chioda ,  Ping Liu ,  Ravi P. Nargund

IPC: A61K31/501 ,  C07D417/04 ,  C07D401/04 ,  C07D403/04 ,  C07D405/14 ,  C07D405/04 ,  C07D413/14 ,  C07D401/14 ,  A61K31/4164 ,  A61K31/427 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/4178 ,  A61K31/444 ,  A61K31/513 ,  A61P25/28 ,  A61P25/16 ,  A61P19/08 ,  A61P19/02 ,  A61P25/02 ,  A61P25/00 ,  A61P29/00 ,  A61P25/06 ,  C07D233/84

CPC classification number: A61K31/4174 ,  A61K31/4178 ,  C07D233/84 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D405/14 ,  C07D409/04 ,  C07D413/04 ,  C07D413/10 ,  C07D413/14 ,  C07D417/04 ,  C07D471/14

Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）抑制剂的某些咪唑衍生物。 本发明还涉及包含这些化合物作为活性成分的药物制剂，以及这些化合物及其制剂在治疗某些障碍（包括骨关节炎，类风湿性关节炎，糖尿病性神经病变，带状疱疹后神经痛，ke肉肌痛和纤维肌痛）中的用途以及 作为急性疼痛，偏头痛，睡眠障碍，阿尔茨海默病和帕金森病。

公开(公告)号：US20110021531A1

公开(公告)日：2011-01-27

申请号：US12509542

申请日：2009-07-27

Applicant: Harry CHOBANIAN ,  Linus S. Lin ,  Ping Liu ,  Marc D. Chioda ,  Robert J. DeVita ,  Ravi P. Nargund ,  Yan Guo

Inventor： Harry CHOBANIAN ,  Linus S. Lin ,  Ping Liu ,  Marc D. Chioda ,  Robert J. DeVita ,  Ravi P. Nargund ,  Yan Guo

IPC: A61K31/497 ,  C07D413/14 ,  A61K31/444 ,  A61K31/501 ,  A61P25/00 ,  A61P19/00

CPC classification number: A61K31/444 ,  A61K31/497 ,  A61K31/501 ,  C07D413/14

Abstract: The present invention is directed to certain oxazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）抑制剂的某些恶唑衍生物。 本发明还涉及包含这些化合物作为活性成分的药物制剂，以及这些化合物及其制剂在治疗某些疾病，包括骨关节炎，类风湿性关节炎，糖尿病性神经病变，带状疱疹后神经痛，ke肉肌痛和纤维肌痛等方面的用途。 作为急性疼痛，偏头痛，睡眠障碍，阿尔茨海默病和帕金森病。

公开(公告)号：US20100204236A1

公开(公告)日：2010-08-12

申请号：US12311672

申请日：2007-10-16

Applicant: Peter H. Dobbelaar ,  Christopher L. Franklin ,  Allan Goodman ,  Cheng Guo ,  Peter R. Guzzo ,  Mark Hadden ,  Shuwen He ,  Alan J. Henderson ,  Tianying Jian ,  Linus S. Lin ,  Jian Liu ,  Ravi P. Nargund ,  Megan Ruenz ,  Bruce J. Sargent ,  Iyassu K. Sebhat ,  Larry Yet

Inventor： Peter H. Dobbelaar ,  Christopher L. Franklin ,  Allan Goodman ,  Cheng Guo ,  Peter R. Guzzo ,  Mark Hadden ,  Shuwen He ,  Alan J. Henderson ,  Tianying Jian ,  Linus S. Lin ,  Jian Liu ,  Ravi P. Nargund ,  Megan Ruenz ,  Bruce J. Sargent ,  Iyassu K. Sebhat ,  Larry Yet

IPC: A61K31/4178 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/497 ,  A61K31/506 ,  A61K31/4439 ,  A61K31/427 ,  A61K31/425 ,  A61K31/4196 ,  A61K31/4164 ,  C07D471/04 ,  C07D401/10 ,  C07D417/10 ,  C07D405/10 ,  C07D403/10 ,  C07D409/06 ,  C07D233/64 ,  A61P9/10 ,  A61P3/04

CPC classification number: C07D401/10 ,  C07D233/64 ,  C07D403/10 ,  C07D403/12 ,  C07D405/04 ,  C07D409/10 ,  C07D413/06 ,  C07D417/06 ,  C07D417/10 ,  C07D471/04

Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

公开(公告)号：US07754188B2

公开(公告)日：2010-07-13

申请号：US10559228

申请日：2004-06-25

Applicant: H. Donald Burns ,  Alex M. Chen ,  Raymond E. Gibson ,  Mark T. Goulet ,  William K. Hagmann ,  Terence G. Hamill ,  James P. Jewell ,  Linus S. Lin ,  Ping Liu ,  Andrey V. Peresypkin

Inventor： H. Donald Burns ,  Alex M. Chen ,  Raymond E. Gibson ,  Mark T. Goulet ,  William K. Hagmann ,  Terence G. Hamill ,  James P. Jewell ,  Linus S. Lin ,  Ping Liu ,  Andrey V. Peresypkin

IPC: A61K51/00 ,  A61M36/14

CPC classification number: C07D213/64 ,  A61K51/0406 ,  A61K51/0455 ,  A61K51/0459 ,  C07D239/34

Abstract: The present invention relates to particular radiolabeled Cannabinoid-1 (CB1) receptor modulators, and methods of using these modulators for labeling and diagnostic imaging of Cannabinoid-1 receptors in mammals, particularly humans. In addition, intermediates useful for the synthesis of the radiolabeled Cannabinoid-1 receptor modulators are also disclosed, as well as the processes for synthesizing the radiolabeled Cannabinoid-1 receptor modulators. Still further, formulations of the radiolabeled Cannabinoid-1 receptor compounds are described.

Abstract translation: 本发明涉及特定的放射性标记的大麻素-1（CB1）受体调节剂，以及使用这些调节剂用于哺乳动物，特别是人类中大麻素-1受体的标记和诊断成像的方法。 此外，还公开了可用于合成放射性标记的大麻素-1受体调节剂的中间体，以及合成放射性标记的大麻素-1受体调节剂的方法。 此外，描述了放射性标记的大麻素-1受体化合物的制剂。

公开(公告)号：US07667053B2

公开(公告)日：2010-02-23

申请号：US10509584

申请日：2003-04-08

Applicant: Laurie A. Castonguay ,  William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah

Inventor： Laurie A. Castonguay ,  William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah

IPC: C07D319/14

CPC classification number: C07D405/12 ,  C07C233/59 ,  C07C2602/08 ,  C07C2602/10 ,  C07C2602/12 ,  C07D307/84 ,  C07D311/58 ,  C07D319/20

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract translation: 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：US20100004280A1

公开(公告)日：2010-01-07

申请号：US12311541

申请日：2007-10-16

Applicant: David Chen ,  Christopher L. Franklin ,  Peter R. Guzzo ,  Linus S. Lin ,  Jian Liu ,  Michael M.-C. Lo ,  Ravi P. Nargund ,  Iyassu K. Sebhat

Inventor： David Chen ,  Christopher L. Franklin ,  Peter R. Guzzo ,  Linus S. Lin ,  Jian Liu ,  Michael M.-C. Lo ,  Ravi P. Nargund ,  Iyassu K. Sebhat

IPC: A61K31/437 ,  C07D401/10 ,  C07D231/02 ,  C07D471/04 ,  A61K31/44 ,  A61K31/4178 ,  A61P3/04

CPC classification number: C07D401/10 ,  C07D233/64 ,  C07D401/14 ,  C07D403/10 ,  C07D417/10 ,  C07D471/04

Abstract: Certain novel substituted imidazoles are ligands of the human bombesin receptor and, in particular, are selective ligands of the human bombesin receptor subtype-3 (BRS-3). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of BRS-3, such as obesity, and diabetes.

Abstract translation: 某些新颖的取代的咪唑是人类bombesin受体的配体，特别是人类bombesin受体亚型-3（BRS-3）的选择性配体。 因此，它们可用于治疗，控制或预防对调节BRS-3的疾病和病症，例如肥胖症和糖尿病。

公开(公告)号：US06972295B2

公开(公告)日：2005-12-06

申请号：US10387265

申请日：2003-03-12

Applicant: William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

Inventor： William K. Hagmann ,  Linus S. Lin ,  Shrenik K. Shah ,  Ravindra N. Guthikonda ,  Hongbo Qi ,  Linda L. Chang ,  Ping Liu ,  Helen M. Armstrong ,  James P. Jewell ,  Thomas J. Lanza, Jr.

IPC: A61K31/165 ,  A61K31/27 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/403 ,  A61K31/405 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/423 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4402 ,  A61K31/4409 ,  A61K31/4436 ,  A61K31/445 ,  A61K31/4453 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/553 ,  A61P1/04 ,  A61P1/10 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P5/24 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P9/14 ,  A61P11/06 ,  A61P13/12 ,  A61P15/00 ,  A61P15/10 ,  A61P17/00 ,  A61P19/02 ,  A61P19/06 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  C07C233/12 ,  C07C233/13 ,  C07C235/06 ,  C07C235/18 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C323/41 ,  C07D207/27 ,  C07D209/08 ,  C07D209/34 ,  C07D209/52 ,  C07D209/94 ,  C07D211/34 ,  C07D213/36 ,  C07D213/40 ,  C07D213/56 ,  C07D213/61 ,  C07D213/64 ,  C07D213/65 ,  C07D213/68 ,  C07D213/89 ,  C07D215/06 ,  C07D231/12 ,  C07D233/36 ,  C07D233/70 ,  C07D233/80 ,  C07D237/14 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D249/18 ,  C07D261/08 ,  C07D261/20 ,  C07D263/58 ,  C07D267/14 ,  C07D277/20 ,  C07D277/30 ,  C07D277/36 ,  C07D277/64 ,  C07D277/74 ,  C07D295/12 ,  C07D295/13 ,  C07D295/14 ,  C07D295/15 ,  C07D401/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04 ,  C07D513/04 ,  C07D521/00 ,  A61K31/4412 ,  C07D213/70

CPC classification number: C07D213/64 ,  C07C233/13 ,  C07C235/06 ,  C07C235/20 ,  C07C235/34 ,  C07C235/74 ,  C07C235/78 ,  C07C237/06 ,  C07C255/55 ,  C07C255/60 ,  C07C271/14 ,  C07C271/22 ,  C07C275/30 ,  C07C311/03 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07D209/34 ,  C07D209/94 ,  C07D211/34 ,  C07D213/65 ,  C07D213/68 ,  C07D215/06 ,  C07D231/12 ,  C07D233/56 ,  C07D233/70 ,  C07D237/28 ,  C07D237/32 ,  C07D239/34 ,  C07D249/04 ,  C07D249/08 ,  C07D249/12 ,  C07D263/58 ,  C07D267/14 ,  C07D277/30 ,  C07D277/36 ,  C07D295/13 ,  C07D295/15 ,  C07D513/04

Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.

Abstract translation: 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗物质滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。

公开(公告)号：US08664253B2

公开(公告)日：2014-03-04

申请号：US13254363

申请日：2010-02-22

Applicant: Ping Liu ,  Robert J. DeVita ,  Linus S. Lin ,  Marc D. Chioda ,  Terence G. Hamill ,  Wenping Li

Inventor： Ping Liu ,  Robert J. DeVita ,  Linus S. Lin ,  Marc D. Chioda ,  Terence G. Hamill ,  Wenping Li

IPC: A61K31/4178 ,  A61K31/4439 ,  C07D401/10

CPC classification number: C07D401/12 ,  C07D401/14 ,  C07D413/10 ,  C07D413/14

Abstract: The present invention is directed to certain Inidazole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.

Abstract translation: 本发明涉及可用作脂肪酸酰胺水解酶（FAAH）和FAAH显像剂的调节剂的某些咪唑衍生物。 本发明还涉及包含这些化合物作为活性成分的药物制剂，以及这些化合物及其制剂在治疗某些疾病，包括骨关节炎，类风湿性关节炎，糖尿病性神经病变，带状疱疹后神经痛，ke肉肌痛和纤维肌痛等方面的用途。 作为急性疼痛，偏头痛，睡眠障碍，阿尔茨海默病和帕金森病。