公开(公告)号：US06380238B1

公开(公告)日：2002-04-30

申请号：US09786154

申请日：2001-03-01

申请人： David Reginald Adams ,  Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  Richard John Hamlyn ,  Suneel Gaur ,  Matthew Alexander James Duncton ,  David Bebbington ,  Nathaniel Julius Monck ,  Claire Elizabeth Dawson ,  Robert Mark Pratt ,  Ashley Roger George

发明人： David Reginald Adams ,  Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  Richard John Hamlyn ,  Suneel Gaur ,  Matthew Alexander James Duncton ,  David Bebbington ,  Nathaniel Julius Monck ,  Claire Elizabeth Dawson ,  Robert Mark Pratt ,  Ashley Roger George

IPC分类号： C07D20908

CPC分类号： C07D401/04 ,  C07D209/08 ,  C07D401/12 ,  C07D409/04 ,  C07D409/12

摘要： For use in therapy a chemical compound of formula (I), wherein R1 to R3 are independently selected from hydrogen and alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, heterocyclyl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, wherein at least one of R4 to R7 is a substituent group other than hydrogen, and pharmaceutically acceptable salts and prodrugs thereof, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes insipidus, and sleep apnea, and especially for the treatment of obesity; chemical compounds of formula (I) other than compounds wherein R7 is hydroxy.

摘要翻译： 用于治疗式（I）化合物，其中R 1至R 3独立地选自氢和烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，杂环基，烷氧基，芳氧基，烷硫基，芳硫基，烷基磺酰基，烷基磺酰基，芳基磺酰基，芳基磺酰基，氨基，单烷基氨基，二烷基氨基，硝基，氰基，甲醛， ，氨基羰基，单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基，其中R4至R7中的至少一个是氢以外的取代基，及其药学上可接受的盐和前药，特别是用于治疗 中枢神经系统; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 尿崩症，睡眠呼吸暂停，特别是治疗肥胖症; 式（I）的化合物，其中R 7是羟基的化合物。

公开(公告)号：US08153651B2

公开(公告)日：2012-04-10

申请号：US12742425

申请日：2008-11-13

申请人： Matthew Cox ,  Donogh John Roger O'Mahony ,  Maria De Los Angeles Estiarte-Martinez ,  Tadashi Kawashima ,  Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Andrew Antony Calabrese

发明人： Matthew Cox ,  Donogh John Roger O'Mahony ,  Maria De Los Angeles Estiarte-Martinez ,  Tadashi Kawashima ,  Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Andrew Antony Calabrese

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D471/02

CPC分类号： C07D215/48 ,  C07C311/08 ,  C07C2602/10 ,  C07D265/36 ,  C07D311/58 ,  C07D311/66 ,  C07D319/20 ,  C07D405/04

摘要： Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

摘要翻译： 公开了具有下列化学式的化合物：化合物可以制备成药物组合物，并且可以用于预防和治疗哺乳动物包括人的多种病症，包括作为非限制性实例的疼痛 ，炎症，创伤性损伤等。

公开(公告)号：US20100267769A1

公开(公告)日：2010-10-21

申请号：US12063159

申请日：2007-11-09

申请人： Koji Ando ,  Andrew Anthony Calabrese ,  Matthew Alexander James Duncton ,  Kentaro Futatsugi ,  Misato Hirano ,  Satochi Nagayama

发明人： Koji Ando ,  Andrew Anthony Calabrese ,  Matthew Alexander James Duncton ,  Kentaro Futatsugi ,  Misato Hirano ,  Satochi Nagayama

IPC分类号： A61K31/415 ,  C07D401/12 ,  C07D231/12 ,  A61K31/4709 ,  A61P25/00 ,  A61P29/00 ,  A61P11/00 ,  A61P1/00

CPC分类号： C07D401/12 ,  C07D231/12

摘要： This invention provides a compound of the formula These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.

摘要翻译： 本发明提供下式的化合物这些化合物可用于治疗哺乳动物VR1受体过度活化（如疼痛等）引起的疾病状况。 本发明还提供了包含上述化合物的药物组合物。

公开(公告)号：US07145009B2

公开(公告)日：2006-12-05

申请号：US10685799

申请日：2003-10-16

申请人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

发明人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

IPC分类号： C07D487/04 ,  A61K31/4985 ,  A61P3/04

CPC分类号： C07D487/04

摘要： Chemical compounds of formula (I): and pharmaceutically acceptable salts and addition compounds and prodrugs thereof are useful in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes inspidus, and sleep apnea.

摘要翻译： 式（I）的化合物及其药学上可接受的盐和加成化合物及其前药可用于治疗，特别是用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 糖尿病，睡眠呼吸暂停。

公开(公告)号：US06800627B1

公开(公告)日：2004-10-05

申请号：US09890186

申请日：2001-10-09

申请人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

发明人： David Reginald Adams ,  Jon Mark Bentley ,  James Davidson ,  Matthew Alexander James Duncton ,  Richard Hugh Phillip Porter

IPC分类号： C07D48704

CPC分类号： C07D487/04

摘要： Chemical compounds of formula (I): and pharmaceutically acceptable salts and addition compounds and prodrugs thereof are useful in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders; diabetes inspidus, and sleep apnea.

摘要翻译： 式（I）的化合物及其药学上可接受的盐和加成化合物及其前药可用于治疗，特别是用于治疗中枢神经系统疾病; 损害中枢神经系统; 心血管疾病; 胃肠道疾病; 糖尿病，睡眠呼吸暂停。

公开(公告)号：US20120088746A1

公开(公告)日：2012-04-12

申请号：US12227197

申请日：2007-05-10

申请人： Yuji Shishido ,  Kazunari Nakao ,  Satoshi Nagayama ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Matthew Cox ,  John Kincaid ,  Kiran Sahasrabudhe ,  Maria de Los Angeles Estiarte-Martinez

发明人： Yuji Shishido ,  Kazunari Nakao ,  Satoshi Nagayama ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Matthew Cox ,  John Kincaid ,  Kiran Sahasrabudhe ,  Maria de Los Angeles Estiarte-Martinez

IPC分类号： A61K31/397 ,  C07D213/76 ,  C07D215/48 ,  C07D215/54 ,  C07D295/155 ,  C07D205/04 ,  A61K31/18 ,  A61K31/44 ,  A61K31/47 ,  A61K31/402 ,  A61K31/5375 ,  A61K31/451 ,  A61P19/02 ,  A61P19/08 ,  A61P1/00 ,  A61P25/16 ,  A61P29/00 ,  A61P25/28 ,  A61P25/18 ,  A61P25/22 ,  A61P25/08 ,  A61P13/00 ,  A61P13/12 ,  A61P13/10 ,  A61P9/12 ,  A61P35/00 ,  A61P3/04 ,  A61P3/00 ,  A61P17/06 ,  A61P17/14 ,  A61P17/04 ,  A61P9/10 ,  A61P11/00 ,  A61P11/06 ,  A61P25/00 ,  C07C311/16

CPC分类号： C07D215/48 ,  C07C311/08 ,  C07C2601/02 ,  C07D205/04 ,  C07D215/54 ,  C07D217/26 ,  C07D231/12 ,  C07D239/94 ,  C07D241/44 ,  C07D295/155 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D405/12 ,  C07D471/04 ,  C07D498/04 ,  C07D498/12

摘要： Compounds are disclosed that have a formula represented by the following: Formula (I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

摘要翻译： 公开了具有由下式表示的式的化合物：式（I）。 化合物可以制备成药物组合物，并且可以用于预防和治疗包括人在内的哺乳动物中的各种病症，包括作为非限制性实例，疼痛，炎症，创伤性损伤等。

公开(公告)号：US07964732B2

公开(公告)日：2011-06-21

申请号：US12063159

申请日：2007-11-09

申请人： Koji Ando ,  Andrew Anthony Calabrese ,  Matthew Alexander James Duncton ,  Kentaro Futatsugi ,  Misato Hirano ,  Satochi Nagayama

发明人： Koji Ando ,  Andrew Anthony Calabrese ,  Matthew Alexander James Duncton ,  Kentaro Futatsugi ,  Misato Hirano ,  Satochi Nagayama

IPC分类号： A61P25/00 ,  A61P29/00 ,  A61P11/00 ,  A61P1/00

CPC分类号： C07D401/12 ,  C07D231/12

摘要： This invention provides a compound of the formula These compounds are useful for the treatment of disease conditions caused by overactivation of the VR1 receptor such as pain, or the like in mammal. This invention also provides a pharmaceutical composition comprising the above compound.

摘要翻译： 本发明提供下式的化合物这些化合物可用于治疗哺乳动物VR1受体过度活化（如疼痛等）引起的疾病状况。 本发明还提供了包含上述化合物的药物组合物。

公开(公告)号：US06433175B1

公开(公告)日：2002-08-13

申请号：US09763889

申请日：2001-02-28

申请人： David Reginald Adams ,  Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  Richard John Hamlyn ,  Suneel Gaur ,  Matthew Alexander James Duncton ,  James Edward Paul Davidson ,  Michael John Bickerdike ,  Ian Anthony Cliffe ,  Howard Langham Mansell

发明人： David Reginald Adams ,  Jonathan Mark Bentley ,  Jonathan Richard Anthony Roffey ,  Richard John Hamlyn ,  Suneel Gaur ,  Matthew Alexander James Duncton ,  James Edward Paul Davidson ,  Michael John Bickerdike ,  Ian Anthony Cliffe ,  Howard Langham Mansell

IPC分类号： C07D48704

CPC分类号： C07D471/04 ,  C07D487/04 ,  C07D491/14

摘要： A chemical compound of formula (I), wherein n is 1, 2 or 3; R1 and R2 are independently selected from hydrogen and alkyl; R3 is alkyl; R4 to R7 are independently selected from hydrogen, halogen, hydroxy, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, alkylsulfoxyl, alkylsulfonyl, arylsulfoxyl, arylsulfonyl, amino, monoalkylamino, dialkylamino, nitro, cyano, carboxaldehyde, alkylcarbonyl, arylcarbonyl, aminocarbonyl, monoalkylaminocarbonyl, dialkylaminocarbonyl, alkoxycarbonylamino, aminocarbonyloxy, monoalkylaminocarbonyloxy, dialkylaminocarbonyloxy, monoalkylaminocarbonylamino and dialkylaminocarbonylamino, or R5 and R6 together form a carbocyclic or heterocyclic ring, and pharmaceutically acceptable salts and prodrugs thereof, and the use thereof in therapy, particularly for the treatment of disorders of the central nervous system; damage to the central nervous system; cardiovascular disorders; gastrointestinal disorders, diabetes insipidus, and sleep apnea, and particularly for the treatment of obesity

摘要翻译： 式（I）的化合物，其中n为1,2或3; R1和R2独立地选自氢和烷基; R3是烷基; R4至R7独立地选自氢，卤素，羟基，烷基，芳基，烷氧基，芳氧基，烷硫基，芳硫基，烷基磺酰基，烷基磺酰基，芳基亚砜基，芳基磺酰基，氨基，单烷基氨基，二烷基氨基，硝基，氰基，甲醛，烷基羰基，芳基羰基，氨基羰基 ，单烷基氨基羰基，二烷基氨基羰基，烷氧基羰基氨基，氨基羰基氧基，单烷基氨基羰基氧基，二烷基氨基羰基氧基，单烷基氨基羰基氨基和二烷基氨基羰基氨基，或R5和R6一起形成碳环或杂环，以及其药学上可接受的盐和前药，以及其用于治疗，特别是治疗疾病 的中枢神经系统; 损害中枢神经系统; 心血管疾病; 胃肠道疾病，尿崩症和睡眠呼吸暂停，特别是用于治疗肥胖症

公开(公告)号：US20110021514A1

公开(公告)日：2011-01-27

申请号：US12742425

申请日：2008-11-13

申请人： Matthew Cox ,  Donogh John Roger O'Mahony ,  Maria De Los Angeles Estiarte-Martinez ,  Tadashi Kawashima ,  Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Andrew Antony Calabrese

发明人： Matthew Cox ,  Donogh John Roger O'Mahony ,  Maria De Los Angeles Estiarte-Martinez ,  Tadashi Kawashima ,  Satoshi Nagayama ,  Yuji Shishido ,  Hirotaka Tanaka ,  Matthew Alexander James Duncton ,  Andrew Antony Calabrese

IPC分类号： A61K31/18 ,  C07D311/66 ,  A61K31/352 ,  C07C311/08 ,  C07D265/36 ,  A61K31/538 ,  C07D215/48 ,  A61K31/47 ,  C07D319/20 ,  A61K31/357 ,  C07D405/04 ,  A61K31/4709 ,  A61P29/00 ,  A61P37/06 ,  A61P13/10 ,  A61P3/00 ,  A61P9/00 ,  A61P35/00 ,  A61P19/00

CPC分类号： C07D215/48 ,  C07C311/08 ,  C07C2602/10 ,  C07D265/36 ,  C07D311/58 ,  C07D311/66 ,  C07D319/20 ,  C07D405/04

摘要： Compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, pain, inflammation, traumatic injury, and others.

摘要翻译： 公开了具有下列化学式的化合物：化合物可以制备成药物组合物，并且可以用于预防和治疗哺乳动物包括人的多种病症，包括作为非限制性实例的疼痛 ，炎症，创伤性损伤等。