公开(公告)号：US06815464B2

公开(公告)日：2004-11-09

申请号：US10081943

申请日：2002-02-21

申请人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman

发明人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman

IPC分类号： A61K3127

CPC分类号： A61K31/27

摘要： This invention is directed to a method for the treatment of pain comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

摘要翻译： 本发明涉及一种治疗疼痛的方法，包括向有需要的受试者施用治疗有效量的选自式（I）和式（II）的化合物：其中苯基在X与 一至五个选自氟，氯，溴和碘的卤素原子; 并且，R 1，R 2，R 3，R 4，R 5和R 6独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基的取代基取代）。

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：US20090281179A1

公开(公告)日：2009-11-12

申请号：US12505765

申请日：2009-07-20

申请人： Ellen E. CODD ,  Richard P. Shank ,  Katherine E. Rogers ,  Carlos R. Plata-Salaman ,  Boyu Zhao

发明人： Ellen E. CODD ,  Richard P. Shank ,  Katherine E. Rogers ,  Carlos R. Plata-Salaman ,  Boyu Zhao

IPC分类号： A61K31/27 ,  A61P25/00

CPC分类号： A61K31/27

摘要： This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain comprising administering to a subject in need thereof a therapeutically effective amount of an enantiomer of Formula (I) substantially free of other enantiomers or an enantiomeric mixture wherein an enantiomer of Formula (I) predominates: wherein phenyl is substituted at X with one to five halogen atoms independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

摘要翻译： 本发明涉及一种用于预防或治疗神经性疼痛和集束型和偏头痛性头痛相关疼痛的方法，包括向有需要的受试者施用治疗有效量的基本上不含其它对映异构体或对映体混合物的式（I）对映异构体 其中式（I）的对映异构体占主导地位：其中苯基在X上被一至五个独立地选自氟，氯，溴和碘的卤素原子取代; 和; R 1和R 2独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基的取代基取代）。

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：US20060293383A1

公开(公告)日：2006-12-28

申请号：US11194875

申请日：2006-03-30

申请人： Ellen Codd ,  Carlos Plata-Salaman ,  Boyu Zhao

发明人： Ellen Codd ,  Carlos Plata-Salaman ,  Boyu Zhao

IPC分类号： A61K31/325

CPC分类号： A61K31/325 ,  A61K31/27

摘要： This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain comprising administering to a subject in need thereof a therapeutically effective amount of an enantiomer of Formula (I) substantially free of other enantiomers or an enantiomeric mixture wherein an enantiomer of Formula (I) predominates: wherein phenyl is substituted at X with one to five halogen atoms independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

公开(公告)号：US07078436B2

公开(公告)日：2006-07-18

申请号：US10081713

申请日：2002-02-21

申请人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman

发明人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman

IPC分类号： A61K31/27

CPC分类号： A61K31/27

摘要： This invention is directed to a method for preventing or treating anxiety disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

摘要翻译： 本发明涉及一种预防或治疗焦虑症的方法，包括向有需要的受试者施用治疗有效量的选自式（I）和式（II）的化合物：其中苯基在X 具有选自氟，氯，溴和碘的一至五个卤素原子; 和R 1，R 2，R 3，R 4，R 5和/或 和R 6和R 6独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自卤素，C 1 -C 6烷基的取代基取代， C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基）。

公开(公告)号：US20050009905A1

公开(公告)日：2005-01-13

申请号：US10870103

申请日：2004-06-17

申请人： Ellen Codd ,  Carlos Plata-Salaman ,  Boyu Zhao

发明人： Ellen Codd ,  Carlos Plata-Salaman ,  Boyu Zhao

IPC分类号： A61P25/04 ,  A61K31/27 ,  A61K31/325

CPC分类号： A61K31/325 ,  A61K31/27

摘要： This invention is directed to a method for preventing or treating neuropathic pain and cluster and migraine headache-associated pain comprising administering to a subject in need thereof a therapeutically effective amount of an enantiomer of Formula (I) substantially free of other enantiomers or an enantiomeric mixture wherein an enantiomer of Formula (I) predominates: wherein phenyl is substituted at X with one to five halogen atoms independently selected from the group consisting of fluorine, chlorine, bromine and iodine; and; R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

摘要翻译： 本发明涉及一种用于预防或治疗神经性疼痛和集束型和偏头痛性头痛相关疼痛的方法，包括向有需要的受试者施用治疗有效量的基本上不含其它对映异构体或对映体混合物的式（I）对映异构体 其中式（I）的对映异构体占主导地位：其中苯基在X上被一至五个独立地选自氟，氯，溴和碘的卤素原子取代; 和; R 1和R 2独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基的取代基取代）。

公开(公告)号：US06589985B2

公开(公告)日：2003-07-08

申请号：US10081501

申请日：2002-02-21

申请人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman

发明人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman

IPC分类号： A61K3127

CPC分类号： A61K31/27

摘要： This invention is directed to a method for preventing or treating movement disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

摘要翻译： 本发明涉及一种预防或治疗运动障碍的方法，包括向有需要的受试者施用治疗有效量的选自式（I）和式（II）的化合物：其中苯基被X取代 具有选自氟，氯，溴和碘的一至五个卤素原子; 并且，R 1，R 2，R 3，R 4，R 5和R 6独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基的取代基取代）。

公开(公告)号：US06562867B2

公开(公告)日：2003-05-13

申请号：US10081766

申请日：2002-02-21

申请人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman ,  Yong Moon Choi ,  Robert Gordon

发明人： Carlos R. Plata-Salaman ,  Boyu Zhao ,  Roy E. Twyman ,  Yong Moon Choi ,  Robert Gordon

IPC分类号： A61K3127

CPC分类号： A61K31/27

摘要： This invention is directed to a method for preventing or treating bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

摘要翻译： 本发明涉及一种预防或治疗双相情感障碍的方法，包括向有需要的受试者施用治疗有效量的式（I）化合物：其中苯基在X被一至五个选自下列的卤素原子取代： 由氟，氯，溴和碘组成; 并且R 1和R 2独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基的取代基取代）。

公开(公告)号：US20070021500A1

公开(公告)日：2007-01-25

申请号：US11481601

申请日：2006-07-06

申请人： Roy Twyman ,  Boyu Zhao

发明人： Roy Twyman ,  Boyu Zhao

IPC分类号： A61K31/325

CPC分类号： A61K31/325 ,  A61K45/06 ,  A61K2300/00

摘要： This invention is directed to methods for providing neuroprotection comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II), or a pharmaceutically acceptable salt or ester thereof: wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

摘要翻译： 本发明涉及用于提供神经保护作用的方法，包括向有需要的受试者施用治疗有效量的选自式（I）和式（II）的化合物或其药学上可接受的盐或酯：其中 苯基在X上被一至五个选自氟，氯，溴和碘的卤素原子取代; 和R 1，R 2，R 3，R 4，R 5和/或 和R 6和R 6独立地选自氢和C 1 -C 4烷基; 其中C 1 -C 4烷基任选被苯基取代（其中苯基任选被独立地选自卤素，C 1 -C 4烷基的取代基取代， C 1 -C 4烷基，C 1 -C 4烷氧基，氨基，硝基和氰基）。