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公开(公告)号：US20100010227A1
公开(公告)日：2010-01-14
申请号：US12483002
申请日：2009-06-11
IPC分类号： C07D211/34
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention discloses a process for preparing the piperidine derivative compound 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid of formula comprising the sequential steps of: (1) reacting 4-bromo-α,α-dimethyl-α-(4,4-dimethylisoxazolin-2-yl)toluene with 4-chlorobutyryl chloride to provide 4-(4-chloro-1-oxobutyl)-α,α-dimethyl-α-(4,4-dimethylisoxazolin-2-yl)toluene; (2) hydrolyzing said 4-(4-chloro-1-oxobutyl)-α,α-dimethyl-α-(4,4-dimethylisoxazolin-2-yl)toluene to provide 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid; (3) reacting said 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid with methanol to provide methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate; (4) reacting said methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate with 4-(α,α-diphenyl)piperidinemethanol to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate; (5) reducing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate; and (6) hydrolyzing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate to provide said 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid.
摘要翻译： 本发明公开了一种制备下式的哌啶衍生化合物4- [4- [4-羟基联苯甲基）-1-哌啶基] -1-羟基丁基-α-α-二甲基苯基乙酸的方法，包括以下顺序步骤：（1） 使4-溴-α，α-二甲基-α-（4,4-二甲基异恶唑啉-2-基）甲苯与4-氯丁酰氯反应，得到4-（4-氯-1-氧代丁基）-α，α-二甲基 - α-（4,4-二甲基异恶唑啉-2-基）甲苯; （2）水解所述4-（4-氯-1-氧代丁基）-α，α-二甲基-α-（4,4-二甲基异恶唑啉-2-基）甲苯，得到4-（4-氯-1-氧代丁基） α，α-二甲基苯乙酸; （3）使所述4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸与甲醇反应，得到4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸甲酯; （4）使4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸甲酯与4-（α，α-二苯基）哌啶甲醇反应，得到4- [4- [4-（羟基二苯基甲基）-1 - 哌啶基] -1-氧代丁基]-α，α-二甲基苯基乙酸酯; （5）还原所述4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯基乙酸甲酯，得到4- [4- [4-（羟基二苯基甲基）-1- 哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸酯; 和（6）水解所述4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸甲酯，得到所述4- [4- [4-羟基二苯基甲基）-1- 哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸。
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公开(公告)号：US6127414A
公开(公告)日：2000-10-03
申请号：US171779
申请日：1998-10-26
IPC分类号： A61K31/165 , A61P3/04 , A61P3/10 , A61P5/14 , A61P9/02 , A61P9/04 , A61P9/06 , A61P9/10 , A61P9/12 , A61P13/12 , A61P25/06 , A61P31/00 , A61P35/00 , C07C279/14 , A01N37/10 , A01N37/12 , A01N37/44 , A61K31/235 , A61K31/24
CPC分类号： C07C279/14 , C07B2200/07 , C07C2101/02 , C07C2102/08
摘要： There is provided pharmaceutically useful compounds of formula I, ##STR1## wherein Ar.sup.1, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 have meanings given in the description, which are useful as antagonists of neuropeptide Y and in particular in the treatment of cardiovascular diseases, for example vasoconstriction.
摘要翻译： PCT No.PCT / SE98 / 01686 Sec。 371日期：1998年10月26日 102（e）1998年10月26日PCT PCT 1998年9月21日PCT公布。 公开号WO99 / 15498 日期1999年4月1日提供药学上有用的式I化合物，其中Ar1，R1，R2，R3，R4，R5和R6具有描述中给出的含义，其可用作神经肽Y的拮抗剂，特别是在治疗中 的心血管疾病，例如血管收缩。
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公开(公告)号：US20100137605A1
公开(公告)日：2010-06-03
申请号：US12686516
申请日：2010-01-13
IPC分类号： C07D211/34
CPC分类号： C07D211/22 , C07D211/14 , C07D211/20 , C07D211/46
摘要： The present invention is directed to a process for preparing the piperidine derivative compound 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid of formula comprising the sequential steps of: (1) reacting 4-bromo-α,α-dimethyl-α-(4,4-dimethylisoxazolin-2-yl) toluene with N,N-dimethyl cyclopropylcarboxylic acid amide to provide 4-(cyclopropyl-oxo-methyl)-α,α-dimethyl-α-(4,4-dimethyloxozolin-2-yl) toluene; (2) hydrolyzing said 4-(cyclopropyl-oxo-methyl)-α,α-dimethyl-α-(4,4-dimethyloxozolin-2-yl) toluene to provide 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid; (3) reacting said 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetic acid with methanol to provide methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate; (4) reacting said methyl 4-(4-chloro-1-oxobutyl)-α,α-dimethylphenylacetate with 4-(α,α-diphenyl)piperidinemethanol to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate; (5) reducing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-oxobutyl]-α,α-dimethylphenylacetate to provide methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate; and (6) hydrolyzing said methyl 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetate to provide said 4-[4-[4-hydroxydiphenylmethyl)-1-piperidinyl]-1-hydroxybutyl]-α,α-dimethylphenylacetic acid.
摘要翻译： 本发明涉及制备下式的哌啶衍生化合物4- [4- [4-羟基联苯甲基）-1-哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸的方法，其包括以下顺序步骤：（ 1）使4-溴-α，α-二甲基-α-（4,4-二甲基异恶唑啉-2-基）甲苯与N，N-二甲基环丙基羧酸酰胺反应，得到4-（环丙基 - 氧代 - 甲基）-α， α-二甲基-α-（4,4-二甲基恶唑啉-2-基）甲苯; （2）水解所述4-（环丙基 - 氧代甲基）-α，α-二甲基-α-（4,4-二甲基恶唑啉-2-基）甲苯，得到4-（4-氯-1-氧代丁基）-α ，α-二甲基苯乙酸; （3）使所述4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸与甲醇反应，得到4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸甲酯; （4）使4-（4-氯-1-氧代丁基）-α，α-二甲基苯基乙酸甲酯与4-（α，α-二苯基）哌啶甲醇反应，得到4- [4- [4-（羟基二苯基甲基）-1 - 哌啶基] -1-氧代丁基]-α，α-二甲基苯基乙酸酯; （5）还原4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-氧代丁基]-α，α-二甲基苯基乙酸甲酯，得到4- [4- [4-（羟基二苯基甲基）-1- 哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸酯; 和（6）水解所述4- [4- [4-（羟基二苯基甲基）-1-哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸甲酯，得到所述4- [4- [4-羟基二苯基甲基）-1- 哌啶基] -1-羟基丁基]-α，α-二甲基苯基乙酸。
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公开(公告)号：US06448406B1
公开(公告)日：2002-09-10
申请号：US09634775
申请日：2000-08-09
IPC分类号： C07D21122
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is —CG1G2G3; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
摘要翻译： 本发明涉及一种通过用哌啶化合物转化具有下式的区域异构体制备哌啶衍生物化合物的方法：其中Z为-CG1G2G3; G1，G2和G3相同或不同，选自OR8，SR8和NR8R9; X3是卤素，OR15，SR15，NR15R16，OSO2R15或NHSO2R15; R8，R9，R15和R16相同或不同，并且选自氢，烷基部分和芳基部分; 并且A是其环的取代基，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。
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公开(公告)号：US5053405A
公开(公告)日：1991-10-01
申请号：US541662
申请日：1990-06-21
申请人： Garry M. Pilling , John P. Mallamo
发明人： Garry M. Pilling , John P. Mallamo
IPC分类号： C07J71/00
CPC分类号： C07J71/0094
摘要： 2'-Alkylsulfonylsteroido[3,2-d]thiazoles, for example 2'-methylsulfonyl-5.alpha.-pregn-2-en-20-yno[3,2-d]thiazol-17.beta.-ol, which are useful as antiandrogenic agents, and processes for preparation, method of use and compositions thereof are disclosed.
摘要翻译： 2'-烷基磺酰基类似甾族化合物[3,2-d]噻唑，例如2'-甲基磺酰基-5α-孕-2-烯-20-炔[3,2-d]噻唑-17β-醇，其可用作 公开了抗雄激素剂及其制备方法，使用方法及其组合物。
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公开(公告)号：US06974872B2
公开(公告)日：2005-12-13
申请号：US10212854
申请日：2002-08-05
IPC分类号： A61K31/00 , A61K31/42 , A61K31/421 , A61K31/445 , A61P37/00 , A61P37/08 , C07D211/22 , C07D211/54 , C07D261/04 , C07D263/10 , C07D211/14 , C07D419/10
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
摘要翻译： 本发明公开了制备下式的哌啶衍生物化合物的方法：其中n为0或1; R 1是氢或羟基; R 2是氢; 或者当n为0时，R 1和R 2一起形成带有R 1和R 2的碳原子之间的第二个键 > 2 ，条件是当n为1时，R 1和R 2各自为氢; R 3是-COOH或-COOR 4; R 4是烷基或芳基部分; A，B和D是它们的环的取代基，其各自可以不同或相同，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。
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公开(公告)号：US06919458B2
公开(公告)日：2005-07-19
申请号：US10212829
申请日：2002-08-05
IPC分类号： C07D211/22 , A61K31/00 , A61K31/42 , A61K31/421 , A61K31/445 , A61P37/00 , A61P37/08 , C07D211/14 , C07D211/34 , C07D211/44 , C07D211/46 , C07D263/10 , C07D419/10
CPC分类号： C07D211/22 , C07D211/14 , C07D211/20 , C07D211/46
摘要： The present invention relates to a process for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound.
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公开(公告)号：US06452011B1
公开(公告)日：2002-09-17
申请号：US09634169
申请日：2000-08-09
IPC分类号： C07D21134
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
摘要翻译： 本发明涉及通过用哌啶化合物转化具有下式的区域异构体来制备哌啶衍生物化合物的方法：其中Z为异或其中m为1或4-6; Q和Y相同或不同，选自O，S和NR5; R6和R7相同或不同，并且选自氢，烷基部分，芳基部分，OR8，SR8和NR8R9; X3是卤素，OR15，SR15，NR15R16，OSO2R15或NHSO2R15; R5，R8，R9，R15和R16相同或不同，并且选自氢，烷基部分和芳基部分; 并且A是其环的取代基，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。
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公开(公告)号：US06201124B1
公开(公告)日：2001-03-13
申请号：US08575344
申请日：1995-12-21
IPC分类号： C07D21134
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: and where m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.
摘要翻译： 本发明涉及通过用哌啶化合物转化具有下式的区域异构体制备哌啶衍生物化合物的方法：其中m为1至6的整数; Q和Y相同或不同，选自O，S和NR5; G1，G2和G3相同或不同，选自OR8，SR8和NR8R9; R6和R7相同或不同，并且选自氢，烷基部分，芳基部分，OR8，SR8和NR8R9; X3是卤素，OR15，SR15，NR15R16，OSO2R15或NHSO2R15; R5，R8，R9，R15和R16相同或不同，并且选自氢，烷基部分和芳基部分; 并且A是其环的取代基，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。
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公开(公告)号：US20110295014A1
公开(公告)日：2011-12-01
申请号：US13207850
申请日：2011-08-11
IPC分类号： C07D211/46
CPC分类号： C07D211/54 , C07D211/22 , C07D261/04
摘要： The present invention discloses processes for preparing piperidine derivative compounds of the formulae: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents. One process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound. Another process for producing piperidine derivative compounds comprises providing an α,α-disubstituted-methylbenzene derivative having the formula: wherein X1 is a halogen, trialkyl or triaryl tin, trialkyl or triaryl borate, trialkyl silicon, alkylhalo silicon, a substituted sulfonic ester, or substituents useful in organometallic coupling reactions and converting the α,α-disubstituted-methylbenzene derivative to the piperidine derivative compound with a piperidine compound. In yet another process, a 4-(α,α-disubstituted)-toluic acid derivative having the formula: wherein X2 is a halogen; an alkali metal oxide; a moiety having the formula —OR10; a moiety having the formula —SR10; or an amine; and R10 is selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety is provided and converted to the piperidine derivative compound with a piperidine compound.
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