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：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：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：US08497298B2

公开(公告)日：2013-07-30

申请号：US11611961

申请日：2006-12-18

申请人： Virginia L. Smith-Swintosky ,  Allen B. Reitz

发明人： Virginia L. Smith-Swintosky ,  Allen B. Reitz

IPC分类号： A61K31/335 ,  A61K31/16

CPC分类号： A61K31/352 ,  A61K31/353 ,  A61K31/357

摘要： The present invention is a method for the glucose related disorders and lipid related disorders comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) or formula (II) as herein defined. The present invention is further directed to methods of treatment comprising co-therapy with an anti-diabetic agent, and anti-lipid agent and/or an anti-obesity agent.

摘要翻译： 本发明是一种葡萄糖相关疾病和脂质相关病症的方法，包括向有需要的受试者施用治疗有效量的本文所述的一种或多种式（I）或式（II）的新型苯并稠合的杂环磺酰胺衍生物 定义 本发明进一步涉及包括与抗糖尿病药物和抗脂质剂和/或抗肥胖剂的协同治疗的治疗方法。

公开(公告)号：US08691867B2

公开(公告)日：2014-04-08

申请号：US11612202

申请日：2006-12-18

申请人： Virginia L. Smith-Swintosky ,  Allen B. Reitz

发明人： Virginia L. Smith-Swintosky ,  Allen B. Reitz

IPC分类号： A01N43/32 ,  A61K31/335 ,  A01N43/26 ,  A01N43/02 ,  C07D323/00 ,  C07D319/12 ,  C07D317/00 ,  C07D307/00

CPC分类号： A61K31/353 ,  A23V2002/00 ,  A61K31/357 ,  A23V2200/334

摘要： The present invention is a method for the treatment of alcohol abuse and/or addiction comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) and/or formula (II) as herein defined.

摘要翻译： 本发明是用于治疗酒精滥用和/或成瘾的方法，包括向有需要的受试者施用治疗有效量的一种或多种式（I）和/或式（II）的新型苯并稠合的杂环磺酰胺衍生物 ）。

公开(公告)号：US08492431B2

公开(公告)日：2013-07-23

申请号：US11611938

申请日：2006-12-18

申请人： Virginia L. Smith-Swintosky ,  Allen B. Reitz

发明人： Virginia L. Smith-Swintosky ,  Allen B. Reitz

IPC分类号： A61K31/35

CPC分类号： A61K31/353 ,  A61K31/357

摘要： The present invention is a method for the treatment of obesity, for promoting weight loss and/or suppressing appetite comprising administering to a subject in need thereof a therapeutically effective amount of one or more novel benzo-fused heterocycle sulfamide derivatives of formula (I) as herein defined.

摘要翻译： 本发明是一种治疗肥胖症，促进体重减轻和/或抑制食欲的方法，包括向有需要的受试者施用治疗有效量的一种或多种式（I）的新型苯并稠合的杂环磺酰胺衍生物作为 在此定义。