公开(公告)号：US06855708B2

公开(公告)日：2005-02-15

申请号：US10096607

申请日：2002-03-13

Applicant: Linus S. Lin ,  George Doherty ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

Inventor： Linus S. Lin ,  George Doherty ,  Shrenik K. Shah ,  Linda L. Chang ,  William K. Hagmann ,  Richard A. Mumford

IPC: C07D401/12 ,  C07D487/04 ,  C07D498/04 ,  A61K31/55 ,  A61K31/47

CPC classification number: C07D401/12 ,  C07D487/04

Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.

Abstract translation: 式I的化合物是VLA-4和/或α4/β7的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病理学。 这些化合物可以配制成药物组合物，适用于治疗AIDS相关的痴呆，过敏性结膜炎，过敏性鼻炎，阿尔茨海默病，哮喘，动脉粥样硬化，自体骨髓移植，某些类型的毒性和免疫性肾炎， 接触皮肤过敏，包括溃疡性结肠炎和克罗恩病的炎性肠病，炎症性肺病，病毒感染的炎症后遗症，脑膜炎，多发性硬化，多发性骨髓瘤，心肌炎，器官移植，牛皮癣，肺纤维化，再狭窄，视网膜炎，类风湿性关节炎，败血症 关节炎，中风，肿瘤转移，葡萄膜炎和I型糖尿病。

公开(公告)号：US08455528B2

公开(公告)日：2013-06-04

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: A61K31/4174 ,  A61K31/4178 ,  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：US08153626B2

公开(公告)日：2012-04-10

申请号：US12517836

申请日：2007-12-07

Applicant: Robert K. Baker ,  Linda L. Chang ,  Marc Chioda ,  Harry R. Chobanian ,  Ying-Duo Gao ,  Yan Guo ,  Linus S. Lin ,  Ping Liu ,  Ravi P. Nargund ,  Kathleen M. Rupprecht ,  Shouwu Miao

Inventor： Robert K. Baker ,  Linda L. Chang ,  Marc Chioda ,  Harry R. Chobanian ,  Ying-Duo Gao ,  Yan Guo ,  Linus S. Lin ,  Ping Liu ,  Ravi P. Nargund ,  Kathleen M. Rupprecht ,  Shouwu Miao

IPC: A01N43/62 ,  A61K31/55 ,  C07D491/00 ,  C07D513/00 ,  C07D515/00 ,  C07D243/10 ,  C07D487/12

CPC classification number: C07D471/04 ,  C07D471/14

Abstract: Certain novel substituted diazepine sulfonamides 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: 某些新型取代的二氮杂类磺酰胺是人类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：US20110144056A1

公开(公告)日：2011-06-16

申请号：US12996435

申请日：2009-06-01

Applicant: Linus S. Lin ,  Linda L. Chang ,  Harry Chobanian ,  Ravi P. Nargund

Inventor： Linus S. Lin ,  Linda L. Chang ,  Harry Chobanian ,  Ravi P. Nargund

IPC: A61K31/695 ,  C07D231/18 ,  A61K31/415 ,  C07D401/04 ,  C07D403/04 ,  A61K31/4439 ,  A61K31/497 ,  A61K31/506 ,  A61K31/501 ,  C07F7/18 ,  C07D413/10 ,  A61K31/4245 ,  C07D401/14 ,  A61P19/02 ,  A61P3/10 ,  A61P21/00 ,  A61P29/00 ,  A61P25/06 ,  A61P25/28 ,  A61P25/16

CPC classification number: C07D471/04 ,  C07D231/18 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D413/10

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, 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：US20100317645A1

公开(公告)日：2010-12-16

申请号：US12517836

申请日：2007-12-07

Applicant: Robert K. Baker ,  Linda L. Chang ,  Marc Chioda ,  Harry R. Chobanian ,  Ying-Duo Gao ,  Yan Guo ,  Linus S. Lin ,  Ping Liu ,  Ravi P. Nargund ,  Kathleen M. Rupprecht ,  Shouwu Miao

Inventor： Robert K. Baker ,  Linda L. Chang ,  Marc Chioda ,  Harry R. Chobanian ,  Ying-Duo Gao ,  Yan Guo ,  Linus S. Lin ,  Ping Liu ,  Ravi P. Nargund ,  Kathleen M. Rupprecht ,  Shouwu Miao

IPC: A61K31/551 ,  C07D487/04 ,  C07D498/14 ,  C07D487/14 ,  A61P3/10 ,  A61P3/04

CPC classification number: C07D471/04 ,  C07D471/14

Abstract: Certain novel substituted diazepine sulfonamides 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: 某些新型取代的二氮杂类磺酰胺是人类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：US20100022598A1

公开(公告)日：2010-01-28

申请号：US12311487

申请日：2007-10-16

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

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

IPC: A61K31/4178 ,  C07D403/10 ,  A61P3/04 ,  A61P3/10 ,  C07D401/10 ,  A61K31/4439

CPC classification number: C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D409/14 ,  C07D417/10

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：US07514409B2

公开(公告)日：2009-04-07

申请号：US10591820

申请日：2005-03-07

Applicant: William K. Hagmann ,  Linus S. Lin ,  Ping Liu ,  Richard A. Mumford ,  Thomas S. Reger ,  Nicholas D. Smith ,  Nicholas S. Stock ,  Jasmine Zunic

Inventor： William K. Hagmann ,  Linus S. Lin ,  Ping Liu ,  Richard A. Mumford ,  Thomas S. Reger ,  Nicholas D. Smith ,  Nicholas S. Stock ,  Jasmine Zunic

IPC: A61K38/05

CPC classification number: C07K5/06026 ,  C07D401/12 ,  C07D401/14

Abstract: Compounds of Formula I are antagonists of VLA-4, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of inflammatory bowel disease including ulcerative colitis and Crohn's disease, multiple sclerosis, asthma, and rheumatoid arthritis.

Abstract translation: 式I的化合物是VLA-4的拮抗剂，因此可用于抑制或预防细胞粘附和细胞粘附介导的病症。 这些化合物可以配制成药物组合物，并且适用于治疗包括溃疡性结肠炎和克罗恩病，多发性硬化，哮喘和类风湿性关节炎的炎性肠病。

公开(公告)号：US08673941B2

公开(公告)日：2014-03-18

申请号：US13057415

申请日：2009-07-30

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: A01N43/40 ,  A61K31/44

CPC classification number: C07D413/14 ,  C07D263/46 ,  C07D271/06 ,  C07D271/10 ,  C07D413/04 ,  C07D413/10 ,  C07D417/04 ,  C07D417/14

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：US08193228B2

公开(公告)日：2012-06-05

申请号：US12311487

申请日：2007-10-16

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

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

IPC: A61K31/4178 ,  A61K31/4164 ,  C07D471/04 ,  C07D401/10 ,  C07D403/10 ,  C07D233/64

CPC classification number: C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D409/14 ,  C07D417/10

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：US08183275B2

公开(公告)日：2012-05-22

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 ,  A61K31/4164 ,  C07D471/04 ,  C07D401/10 ,  C07D403/10 ,  C07D233/64

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.