公开(公告)号：US06319941B1

公开(公告)日：2001-11-20

申请号：US09655897

申请日：2000-09-06

申请人： Adam Matthew Gilbert ,  Zhen-jia Chen

发明人： Adam Matthew Gilbert ,  Zhen-jia Chen

IPC分类号： A61K31415

CPC分类号： C07D231/38 ,  C07D401/12

摘要： This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及平滑肌痉挛状态或过度肌肉收缩的治疗，例如用糠醛的化合物促进尿失禁：R1和R2分别是1至6个碳原子的直链烷基，3至6个碳原子的支链烷基，或 3至6个碳原子的环烷基，其中R 1和R 2可以被F，Cl，Br，I，OH，NH 2，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，COOH或COOC 1 -C 6烷基取代; R 3是芳基或 任选被0至4个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，F，Cl，Br，C 1 -C 6烷硫基，CO 2 R 1，CONH 2，OH，NH 2和NO 2的基团取代的杂芳基; n 为0或1; R 4为碳原子数为1〜10的直链烷基，碳数为3〜10的支链烷基或碳原子数为3〜10的环烷基;以及所有结晶形式及其药学上可接受的盐。

公开(公告)号：US06313149B1

公开(公告)日：2001-11-06

申请号：US09655891

申请日：2000-09-06

申请人： Adam Matthew Gilbert ,  Zhen-jia Chen

发明人： Adam Matthew Gilbert ,  Zhen-jia Chen

IPC分类号： A61K31415

CPC分类号： C07D231/38 ,  C07D401/12

摘要： This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof

摘要翻译： 本发明涉及平滑肌痉挛状态或过度肌肉收缩的治疗，例如用糠醛的化合物促进尿失禁：R1和R2分别是1至6个碳原子的直链烷基，3至6个碳原子的支链烷基，或 3至6个碳原子的环烷基，其中R 1可被F，Cl，Br，I，OH，NH 2，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，COOH或COOC 1 -C 6烷基取代; R 3是芳基或杂芳基 任选地被0至4个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，F，Cl，Br，C 1 -C 6烷硫基，CO 2 R 1，CONH 2，OH，NH 2和NO 2基团取代的基团取代; n是 0或1; R 4是碳原子数1〜10的直链烷基，碳原子数3〜10的支链烷基或碳原子数3〜10的环烷基;全部结晶形式及其药学上可接受的盐

公开(公告)号：US06172222B2

公开(公告)日：2001-01-09

申请号：US09327065

申请日：1999-06-07

申请人： Adam Matthew Gilbert ,  Zhen-jia Chen

发明人： Adam Matthew Gilbert ,  Zhen-jia Chen

IPC分类号： C07D40112

CPC分类号： C07D231/38 ,  C07D401/12

摘要： This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.

公开(公告)号：US6133273A

公开(公告)日：2000-10-17

申请号：US304180

申请日：1999-05-03

申请人： Adam Matthew Gilbert ,  Zhen-jia Chen ,  Gerardo De La Cruz Francisco ,  Magda Asselin

发明人： Adam Matthew Gilbert ,  Zhen-jia Chen ,  Gerardo De La Cruz Francisco ,  Magda Asselin

IPC分类号： A61K31/519 ,  C07D487/04 ,  A61K31/4162

CPC分类号： C07D487/04 ,  A61K31/519

摘要： A compound of formula (I) ##STR1## wherein: X=N and Y=CH or X=CH and Y=NR.sub.1 and R.sub.2 are independently, straight chain alkyl of 2 to 12 carbon atoms, branched chain alkyl of 3 to 10 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, aryl of 4 to 10 carbon atoms, 4 to 10 membered heteroaryl or a moiety of the formula (CH.sub.2).sub.m -A wherein m is 1 to 9 and A is cycloalkyl of 3 to 7 carbon atoms; and R.sub.3 is a straight chain alkyl of 1 to 12 carbon atoms, branched chain alkyl of 3 to 10 carbon atoms, aryl of 4 to 10 carbon atoms or 4 to 10 membered heteroaryl for use in the treatment of disorders associated with bone loss by increased transcription and elevation of plasma calcitonin levels.

摘要翻译： 式（I）的化合物，其中：X = N，Y = CH或X = CH，Y = N R 1，R 2独立地为2至12个碳原子的直链烷基，3至10个碳原子的支链烷基， 3至10个碳原子的环烷基，4至10个碳原子的芳基，4至10元杂芳基或式（CH2）mA部分，其中m为1至9，A为3至7个碳原子的环烷基; 并且R 3是1至12个碳原子的直链烷基，3至10个碳原子的支链烷基，4至10个碳原子的芳基或4至10元杂芳基，用于治疗与骨丢失相关的疾病增加 血浆降钙素水平的转录和升高。

公开(公告)号：US06458823B1

公开(公告)日：2002-10-01

申请号：US09963254

申请日：2001-09-25

申请人： Adam Matthew Gilbert ,  Zhen-jia Chen

发明人： Adam Matthew Gilbert ,  Zhen-jia Chen

IPC分类号： A61K314155

CPC分类号： C07D231/38 ,  C07D401/12

摘要： This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.

摘要翻译： 本发明涉及平滑肌痉挛状态或过度肌肉收缩的治疗，例如用糠醛的化合物促进尿失禁：R1和R2分别是1至6个碳原子的直链烷基，3至6个碳原子的支链烷基，或 3至6个碳原子的环烷基，其中R 2可以被F，Cl，Br，I，OH，NH 2，氰基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，COOH或COOC 1 -C 6烷基取代; R 3是芳基或杂芳基 任选被0至4个独立地选自C 1 -C 6烷基，C 1 -C 6烷氧基，氰基，F，Cl，Br，C 1 -C 6烷硫基，CO 2 R 1，CONH 2，OH，NH 2和NO 2基团取代的基团取代; n为0 或1; R 4为碳原子数为1〜10的直链烷基，碳原子数为3〜10的支链烷基或碳原子数为3〜10的环烷基;以及所有结晶形式及其药学上可接受的盐。