公开(公告)号：US20060030604A1

公开(公告)日：2006-02-09

申请号：US11236097

申请日：2005-09-27

申请人： Magdalena Elsinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Elsinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

IPC分类号： C07D285/08 ,  A61K31/433

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D333/16 ,  C07D417/12 ,  C07F9/4018

摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

公开(公告)号：US20060128772A1

公开(公告)日：2006-06-15

申请号：US11344772

申请日：2006-02-01

申请人： Magdalena Eisinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis Fitzpatrick ,  Daniel Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen Reitz ,  Virginia Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  C07D285/08

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D417/12

摘要： The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

公开(公告)号：US08501791B2

公开(公告)日：2013-08-06

申请号：US12835220

申请日：2010-07-13

申请人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  C07D285/08

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D333/16 ,  C07D417/12 ,  C07F9/4018

摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。

公开(公告)号：US20100280079A1

公开(公告)日：2010-11-04

申请号：US12835220

申请日：2010-07-13

申请人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  A61K31/4439 ,  A61P25/00 ,  A61P17/00 ,  A61P3/00 ,  A61P15/00

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D333/16 ,  C07D417/12 ,  C07F9/4018

摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。

公开(公告)号：US07375123B2

公开(公告)日：2008-05-20

申请号：US11344772

申请日：2006-02-01

申请人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  C07D285/08

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D417/12

摘要： The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。

公开(公告)号：US07319107B2

公开(公告)日：2008-01-15

申请号：US10287096

申请日：2002-11-04

申请人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  C07D285/08

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D333/16 ,  C07D417/12 ,  C07F9/4018

摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。

公开(公告)号：US07049331B2

公开(公告)日：2006-05-23

申请号：US10287095

申请日：2002-11-04

申请人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  C07D285/08

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D417/12

摘要： The present invention is directed to novel 1,2,4-thiadiazole derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。

公开(公告)号：US07786311B2

公开(公告)日：2010-08-31

申请号：US12221900

申请日：2008-08-05

申请人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

IPC分类号： C07D285/08

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D333/16 ,  C07D417/12 ,  C07F9/4018

摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。

公开(公告)号：US20090203751A1

公开(公告)日：2009-08-13

申请号：US12221900

申请日：2008-08-05

申请人： Magdalena Eisinger Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

发明人： Magdalena Eisinger Eisinger ,  Louis J. Fitzpatrick ,  Daniel H. Lee ,  Kevin Pan ,  Carlos Plata-Salaman ,  Allen B. Reitz ,  Virginia L. Smith-Swintosky ,  Boyu Zhao

IPC分类号： A61K31/433 ,  A61P3/00 ,  A61P17/00 ,  C07C335/04

CPC分类号： C07D285/08 ,  A61K8/49 ,  A61Q5/006 ,  A61Q19/00 ,  A61Q19/007 ,  C07D333/16 ,  C07D417/12 ,  C07F9/4018

摘要： The present invention is directed to novel 1,2,4-thiadiazol-2-ium derivatives useful as agonists or antagonists of the melanocortin receptor. More particularly, the compounds of the present invention are useful for the treatment of metabolic, CNS and dermatological disorders such as obesity, impaired oral glucose tolerance, elevated blood glucose levels, type II diabetes, Syndrome X, diabetic retinopathy, spinal cord injury, nerve injury, acute neurodegenerative disorders, chronic neurodegenerative disorders, plexopathies, male erectile dysfunction, dry eyes, acne, dry skin, aged skin, seborrheic dermatitis, rosacea, excessive ear wax, meibomian gland disorder, pseudofolliculitis, yeast infections, dandruff, hidradenitis suppurativa, ocular rosacea and eccrine gland disorder.

摘要翻译： 本发明涉及可用作黑皮质素受体的激动剂或拮抗剂的新颖的1,2,4-噻二唑-2-基衍生物。 更具体地，本发明的化合物可用于治疗代谢，CNS和皮肤病学障碍，例如肥胖症，口服葡萄糖耐量降低，血糖水平升高，II型糖尿病，X综合征，糖尿病性视网膜病变，脊髓损伤，神经 伤口，急性神经退行性疾病，慢性神经退行性疾病，性欲症，男性勃起功能障碍，干眼症，痤疮，干性皮肤，老年皮肤，脂溢性皮炎，酒渣鼻，过度耳垢，睑板腺疾病，假性结石炎，酵母菌感染，头皮屑， 眼红斑痤疮和外分泌腺疾病。

公开(公告)号：US20060178390A1

公开(公告)日：2006-08-10

申请号：US11398239

申请日：2006-04-05

申请人： Alfonzo Jordan ,  Allen Reitz ,  Kevin Pan

发明人： Alfonzo Jordan ,  Allen Reitz ,  Kevin Pan

IPC分类号： A61K31/4747 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The present invention is directed to novel 1,3,8-triazaspiro[4.5]decan-4-one derivatives of the general formula wherein all variables are as defined herein, useful in the treatment of disorders and conditions mediated by the ORL-1 G-protein coupled receptor. More particularly, the compounds of the present invention are useful in the treatment of disorders and conditions such as anxiety, depression, substance abuse, neuropathic pain, acute pain, migraine, asthma, cough and for improved cognition.

摘要翻译： 本发明涉及通式的新的1,3,8-三氮杂螺[4.5]癸-4-酮衍生物，其中所有变量如本文所定义，可用于治疗ORL-1 G介导的病症和病症 蛋白偶联受体。 更具体地，本发明的化合物可用于治疗诸如焦虑，抑郁，药物滥用，神经性疼痛，急性疼痛，偏头痛，哮喘，咳嗽和改善认知的病症和病症。