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1. 发明授权

EP0665843B1 SUBSTITUTED QUINUCLIDINES AS SUBSTANCE P ANTAGONISTS 失效
标题翻译：取代奎宁环THAN P物质拮抗剂
公开(公告)号：EP0665843B1
公开(公告)日：2003-08-13
申请号：EP93922406.9
申请日：1993-09-30
申请人： PFIZER INC.
发明人： ITO, Fumitaka , KOKURA, Toshihide , NAKANE, Masami , SATAKE, Kunio , WAKABAYASHI, Hiroaki
IPC分类号： C07D453/02 , A61K31/435
CPC分类号： C07D453/02
摘要： Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having formula (I) wherein Ar?1 and Ar2¿ are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; X is -CONR?3R4, -CO¿2R3, -CH2OR3, -CH2NR3R4 or -CONR?3OR4; R1, R3 and R4¿ are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms; R2 is alkyl having 1 to 4 carbon atoms; Y is alkylsulfonyl having 1 to 4 carbon atoms, N-alkyl-N-alkanoylamino (which may be substituted by halogen in the alkanoyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkanoyl moieties, N-alkyl-N-alkylsulfonylamino (which may be substituted by halogen in the alkylsulfonyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkyl sulfonyl moieties, alkenyl having 2 to 4 carbon atoms, alkynyl having 2 to 4 carbon atoms, halosubstituted alkyl having 1 to 4 carbon atoms, alkylamino having 1 to 4 carbon atoms, alkanoylamino (which may be substituted by halogen) having 1 to 4 carbon atoms or alkylsulfonylamino (which may be substituted by halogen) having 1 to 4 carbon atoms. These compounds are useful in the treatment gastrointestinal or central nervous system disorders and the alleviation of inflammatory diseases, asthma, pain and migraine in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

2. 发明公开

EP0840732A1 SUBSTITUTED BENZOLACTAM COMPOUNDS AS SUBSTANCE P ANTAGONISTS 失效
标题翻译：取代BENZOLAKTAMVERBINDUNGEN THAN P物质拮抗剂
公开(公告)号：EP0840732A1
公开(公告)日：1998-05-13
申请号：EP96911079.0
申请日：1996-05-09
申请人： PFIZER INC.
发明人： WAKABAYASHI, Hiroaki , IKUNAKA, Masaya
IPC分类号： C07D401 , A61K31 , A61P1 , A61P13 , A61P15 , A61P25 , A61P29 , A61P43 , C07D211 , C07D403 , C07D413 , C07D417 , C07D453 , C07D471
CPC分类号： C07D401/12 , C07D211/56 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/08
摘要： This invention provides a compound of general formula (I) and its pharmaceutically acceptable salts, wherein: W is methylene, ethylene, propylene, vinylene, -CH2-O-, -O-CH2-, -CH2-S- or -S-CH2-; R?1, R2 and R3¿ are independently hydrogen, C¿1?-C3 alkyl, C1-C3 alkoxy or halo C1-C3 alkyl, provided that when W is methylene, both R?2 and R3¿ are not hydrogen; X is halo, C¿1?-C3 alkoxy, C1-C3 alkyl, halo C1-C3 alkoxy or C1-C3 alkenyl; Y is imino or oxy; Q is oxygen or sulfur; and T is (2S,3S)-2-diphenylmethylquinuclidin-3-yl, (2S,3S)-2-phenylpiperidin-3-yl or (2S,3S)-2-diphenylmethyl-1-azanorbornan-3-yl. These compounds are useful in the treatment of treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, emesis, urinary incontinence, pain, migraine, angiogensis or the like in a mammaliam subject, especially humans. Also, intermediates of the above compounds are disclosed.

3. 发明公开

EP0665843A1 SUBSTITUTED QUINUCLIDINES AS SUBSTANCE P ANTAGONISTS 失效
标题翻译：取代奎宁环THAN P物质拮抗剂。
公开(公告)号：EP0665843A1
公开(公告)日：1995-08-09
申请号：EP93922406.0
申请日：1993-09-30
申请人： PFIZER INC.
发明人： ITO, Fumitaka , KOKURA, Toshihide , NAKANE, Masami , SATAKE, Kunio , WAKABAYASHI, Hiroaki
IPC分类号： A61K31 , A61P1 , A61P11 , A61P25 , A61P29 , A61P43 , C07D453
CPC分类号： C07D453/02
摘要： Certain novel substituted quinuclidine compounds having the ability to antagonize substance P and having formula (I) wherein Ar?1 and Ar2¿ are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; X is -CONR?3R4, -CO¿2R3, -CH2OR3, -CH2NR3R4 or -CONR?3OR4; R1, R3 and R4¿ are each, independently, hydrogen or alkyl having 1 to 4 carbon atoms; R2 is alkyl having 1 to 4 carbon atoms; Y is alkylsulfonyl having 1 to 4 carbon atoms, N-alkyl-N-alkanoylamino (which may be substituted by halogen in the alkanoyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkanoyl moieties, N-alkyl-N-alkylsulfonylamino (which may be substituted by halogen in the alkylsulfonyl moiety) having 1 to 4 carbon atoms in the alkyl and the alkyl sulfonyl moieties, alkenyl having 2 to 4 carbon atoms, alkynyl having 2 to 4 carbon atoms, halosubstituted alkyl having 1 to 4 carbon atoms, alkylamino having 1 to 4 carbon atoms, alkanoylamino (which may be substituted by halogen) having 1 to 4 carbon atoms or alkylsulfonylamino (which may be substituted by halogen) having 1 to 4 carbon atoms. These compounds are useful in the treatment gastrointestinal or central nervous system disorders and the alleviation of inflammatory diseases, asthma, pain and migraine in mammals and as the active ingredient in pharmaceutical compositions for treating such conditions.

4. 发明授权

EP0632809B1 QUINUCLIDINE DERIVATIVES AS SUBSTANCE P ANTAGONISTS 失效
标题翻译：奎宁环衍生物作为P物质拮抗剂
公开(公告)号：EP0632809B1
公开(公告)日：2001-09-05
申请号：EP93907099.1
申请日：1993-03-05
申请人： PFIZER INC.
发明人： SATAKE, Kunio , WAKABAYASHI, Hiroaki , NAKANE, Masami
IPC分类号： C07D453/02 , A61K31/435
CPC分类号： C07D453/02
摘要： Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof, wherein X1 is alkoxy or halosubstituted alkoxy; X2 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halosubstitued alkyl, halosubstituted alkoxy, alkylamino, dialkylamino, alkylsulfonylamino (which may be substituted), N-alkyl-N-alkylsulfonylamino (which may be substituted), alkanoylamino (which may be substituted) or N-alkyl-N-alkanoylamino (which may be substituted); Ar?1 and Ar2¿ are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; A is Y-(CH¿2?)m-CH(R?2)-(CH¿2)n-NR1-; R1 is hydrogen, alkyl, benzyl or -(CH¿2?)p-Y; R?2¿ is hydrogen, alkyl (which may be substituted), benzyl, 4-hydroxybenzyl, 3-indolylmethyl or -(CH¿2?)p-Y; Y is -CN, -CH2Z or -COZ; Z is hydroxy, amino, alkoxy, alkylamino or dialkylamino; m, n and p are each, independently, 0, 1, 2 or 3; and R?1 and R2¿ may be connected to form a ring.

5. 发明授权

EP0708771B1 BENZYLOXYQUINUCLIDINES AS SUBSTANCE P ANTAGONISTS 失效
标题翻译：作为物质拮抗剂的苄氧基喹啉
公开(公告)号：EP0708771B1
公开(公告)日：1998-10-07
申请号：EP94919851.9
申请日：1994-07-05
申请人： PFIZER INC.
发明人： SATAKE, Kunio , WAKABAYASHI, Hiroaki
IPC分类号： C07D453/02 , A61K31/435
CPC分类号： C07D453/02
摘要： A compound of chemical formula (I) and its pharmaceutically acceptable salt, wherein X and Y are each hydrogen, halogen, C1-C6 alkyl, halosubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl or tri C1-C6 alkylsilyl; Ar?1 and Ar2¿ are each aryl optionally substituted by halogen; A is -CO- or -(CH¿2?)-; Z-A- is at 2 or 3 position on the quinuclidine ring; and Z is hydroxy, C1-C6 alkoxy, NR?1R2¿ or the like. Typical examples are (3S,4R,5S,6S)-5-(3,5-bis(trifluoromethyl)benzyloxy)-N,N-dimethyl-6-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-carboxamide; (3S,4R,5S,6S)-5-(3,5-bis(trifluoromethyl)benzyloxy)-6-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-carboxylic acid. The novel benzyloxyquinuclidines in this invention have substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis, migraine, urinary incontinence or angiogenesis in mammals, especially humans.
摘要翻译：其中X和Y各自为氢，卤素，C 1 -C 6烷基，卤素取代的C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷硫基，C 1 -C 6烷基亚磺酰基， C1-C6烷基磺酰基或三C1-C6烷基甲硅烷基; Ar 1和Ar 2各自为任选被卤素取代的芳基; A是-CO-或 - （CH 2 2） - ; Z-A-在奎宁环的2或3位; Z是羟基，C 1 -C 6烷氧基，NR 1 R 2等。典型的例子是（3S，4R，5S，6S）-5-（3,5-双（三氟甲基）苄氧基）-N，N-二甲基-6-二苯基甲基-1-氮杂二环[2.2.2]辛烷-3-甲酰胺 ; （3S，4R，5S，6S）-5-（3,5-双（三氟甲基）苄氧基）-6-二苯基甲基-1-氮杂双环[2.2.2]辛烷-3-羧酸。本发明中的新型苄氧基奎宁环素具有P物质拮抗活性，因此可用于治疗哺乳动物特别是人的胃肠病症，中枢神经系统病症，变态反应，炎性疾病，哮喘，疼痛，呕吐，偏头痛，尿失禁或血管生成。

6. 发明公开

EP0632809A1 QUINUCLIDINE DERIVATIVES AS SUBSTANCE P ANTAGONISTS 失效
标题翻译： CHINUCHIDINE衍生物作为P物质拮抗剂。
公开(公告)号：EP0632809A1
公开(公告)日：1995-01-11
申请号：EP93907099.0
申请日：1993-03-05
申请人： PFIZER INC.
发明人： SATAKE, Kunio , WAKABAYASHI, Hiroaki , NAKANE, Masami
IPC分类号： A61K31 , A61P1 , A61P11 , A61P25 , A61P29 , C07D453
CPC分类号： C07D453/02
摘要： Compounds useful in the treatment of inflammatory disorders, central nervous system disorders and other disorders of formula (I) and the pharmaceutically-acceptable salts thereof, wherein X1 is alkoxy or halosubstituted alkoxy; X2 is hydrogen, halogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, halosubstitued alkyl, halosubstituted alkoxy, alkylamino, dialkylamino, alkylsulfonylamino (which may be substituted), N-alkyl-N-alkylsulfonylamino (which may be substituted), alkanoylamino (which may be substituted) or N-alkyl-N-alkanoylamino (which may be substituted); Ar?1 and Ar2¿ are each, independently, thienyl, phenyl, fluorophenyl, chlorophenyl or bromophenyl; A is Y-(CH¿2?)m-CH(R?2)-(CH¿2)n-NR1-; R1 is hydrogen, alkyl, benzyl or -(CH¿2?)p-Y; R?2¿ is hydrogen, alkyl (which may be substituted), benzyl, 4-hydroxybenzyl, 3-indolylmethyl or -(CH¿2?)p-Y; Y is -CN, -CH2Z or -COZ; Z is hydroxy, amino, alkoxy, alkylamino or dialkylamino; m, n and p are each, independently, 0, 1, 2 or 3; and R?1 and R2¿ may be connected to form a ring.

7. 发明授权

EP0840732B1 SUBSTITUTED BENZOLACTAM COMPOUNDS AS SUBSTANCE P ANTAGONISTS 失效
标题翻译：取代的苯甲酰胺化合物作为物质拮抗剂
公开(公告)号：EP0840732B1
公开(公告)日：2001-03-07
申请号：EP96911079.0
申请日：1996-05-09
申请人： PFIZER INC.
发明人： WAKABAYASHI, Hiroaki , IKUNAKA, Masaya
IPC分类号： C07D401/12 , A61K31/40 , A61K31/47 , C07D471/08 , C07D453/02 , C07D265/18 , C07D265/28 , C07D279/08 , C07D279/10
CPC分类号： C07D401/12 , C07D211/56 , C07D413/12 , C07D417/12 , C07D453/02 , C07D471/08
摘要： This invention provides a compound of general formula (I) and its pharmaceutically acceptable salts, wherein: W is methylene, ethylene, propylene, vinylene, -CH2-O-, -O-CH2-, -CH2-S- or -S-CH2-; R?1, R2 and R3¿ are independently hydrogen, C¿1?-C3 alkyl, C1-C3 alkoxy or halo C1-C3 alkyl, provided that when W is methylene, both R?2 and R3¿ are not hydrogen; X is halo, C¿1?-C3 alkoxy, C1-C3 alkyl, halo C1-C3 alkoxy or C1-C3 alkenyl; Y is imino or oxy; Q is oxygen or sulfur; and T is (2S,3S)-2-diphenylmethylquinuclidin-3-yl, (2S,3S)-2-phenylpiperidin-3-yl or (2S,3S)-2-diphenylmethyl-1-azanorbornan-3-yl. These compounds are useful in the treatment of treating gastrointestinal disorders, central nervous system disorders, inflammatory diseases, emesis, urinary incontinence, pain, migraine, angiogensis or the like in a mammaliam subject, especially humans. Also, intermediates of the above compounds are disclosed.
摘要翻译：本发明提供了通式（I）的化合物及其药学上可接受的盐，其中：W是亚甲基，亚乙基，亚丙基，亚乙烯基，-CH 2 -O-，-O-CH 2 - ，-CH 2 -S-或-S- CH2-; 条件是当W是亚甲基时，R 2和R 3都不是氢;条件是当W是亚甲基时，R 2和R 3不都是氢。 X是卤素，C 1 -C 3烷氧基，C 1 -C 3烷基，卤代C 1 -C 3烷氧基或C 1 -C 3链烯基; Y是亚氨基或氧基; Q是氧或硫; （2S，3S）-2-二苯基甲基奎宁环-3-基，（2S，3S）-2-苯基哌啶-3-基或（2S，3S）-2-二苯基甲基-1-氮杂降冰片-3-基。这些化合物可用于治疗哺乳动物对象，特别是人的胃肠病症，中枢神经系统病症，炎性疾病，呕吐，尿失禁，疼痛，偏头痛，血管生成等。而且，公开了上述化合物的中间体。

8. 发明公开

EP0861235A1 SUBSTITUTED BENZYLAMINOPIPERIDINE COMPOUNDS 失效
标题翻译：取代的苯甲酰氨基哌啶化合物
公开(公告)号：EP0861235A1
公开(公告)日：1998-09-02
申请号：EP96914375.0
申请日：1996-06-10
申请人： PFIZER INC.
发明人： SATAKE, Kunio , SHISHIDO, Yuji , WAKABAYASHI, Hiroaki
IPC分类号： A61K , C07D , G06F9 , A61K31 , A61P1 , A61P13 , A61P25 , A61P29 , A61P31 , A61P43 , C07D211 , C07D405 , G06F7
CPC分类号： C07D211/56
摘要： This invention provides a compound of formula (I) and its pharmaceutically acceptable salts, wherein R is halo C1-C8 alkyl, halo C2-C8 alkenyl, halo C2-C8 alkynyl or halo C1-C8 alkyl substituted by hydroxy or C1-C8 alkoxy; R1 is hydrogen, halo or C¿1?-C6 alkoxy; or R and R?1¿, together with the two carbon atoms shared between the benzene ring and the R and R1, complete a fused C¿4?-C6 cycloalkyl wherein one carbon atom is optionally replaced by oxygen and wherein one or two of the carbon atoms are optionally substituted by up to five substituents selected from halo, C1-C6 alkyl and halo C1-C6 alkyl; X is C1-C6 alkoxy, halo C1-C6 alkoxy, phenoxy or halo; and Ar is phenyl optionally substituted by halo. These compounds are of use in treating a gastrointestinal disorder, a central nervous system (CNS) disorder, an inflammatory disease, emesis, urinary incontinence, pain, migraine, sunburn, diseases, disorders and adverse conditions caused by Helicobacter pylori, or angiogenesis especially CNS disorders in a mammalian subject, especially humans.
摘要翻译：本发明提供了式（I）化合物及其药学上可接受的盐，其中R为被羟基或C 1 -C 8烷氧基取代的卤代C 1 -C 8烷基，卤代C 2 -C 8烯基，卤代C 2 -C 8炔基或卤代C 1 -C 8烷基 ; R 1是氢，卤素或C 1 -C 6烷氧基; 或者R 1和R 2与苯环与R 1和R 1之间共有的两个碳原子一起形成稠合的C 4 -C 6环烷基，其中一个碳原子任选地被氧代替，并且其中一个或两个碳原子任选被至多五个选自卤素，C 1 -C 6烷基和卤代C 1 -C 6烷基的取代基取代; X是C1-C6烷氧基，卤代C1-C6烷氧基，苯氧基或卤素; Ar是任选被卤素取代的苯基。这些化合物可用于治疗由幽门螺杆菌引起的胃肠疾病，中枢神经系统（CNS）疾病，炎性疾病，呕吐，尿失禁，疼痛，偏头痛，晒伤，疾病，病症和不良疾病或血管生成，特别是CNS 哺乳动物受试者特别是人类的疾病。

9. 发明公开

EP0708771A1 BENZYLOXYQUINUCLIDINES AS SUBSTANCE P ANTAGONISTS 失效
标题翻译： Benzyloxyquinuclidines THAN P物质拮抗剂
公开(公告)号：EP0708771A1
公开(公告)日：1996-05-01
申请号：EP94919851.0
申请日：1994-07-05
申请人： PFIZER INC.
发明人： SATAKE, Kunio , WAKABAYASHI, Hiroaki
IPC分类号： A61K31 , A61P1 , A61P11 , A61P25 , A61P29 , A61P37 , C07D453
CPC分类号： C07D453/02
摘要： A compound of chemical formula (I) and its pharmaceutically acceptable salt, wherein X and Y are each hydrogen, halogen, C1-C6 alkyl, halosubstituted C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, C1-C6 alkylsulfinyl, C1-C6 alkylsulfonyl or tri C1-C6 alkylsilyl; Ar?1 and Ar2¿ are each aryl optionally substituted by halogen; A is -CO- or -(CH¿2?)-; Z-A- is at 2 or 3 position on the quinuclidine ring; and Z is hydroxy, C1-C6 alkoxy, NR?1R2¿ or the like. Typical examples are (3S,4R,5S,6S)-5-(3,5-bis(trifluoromethyl)benzyloxy)-N,N-dimethyl-6-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-carboxamide; (3S,4R,5S,6S)-5-(3,5-bis(trifluoromethyl)benzyloxy)-6-diphenylmethyl-1-azabicyclo[2.2.2]octan-3-carboxylic acid. The novel benzyloxyquinuclidines in this invention have substance P antagonistic activity and are thus useful for the treatment of gastrointestinal disorders, central nervous system disorders, allergy, inflammatory diseases, asthma, pain, emesis, migraine, urinary incontinence or angiogenesis in mammals, especially humans.

10. 发明公开

EP0585328A1 SUBSTITUTED 3-AMINOQUINUCLIDINES 失效
标题翻译：取代的3-氨基喹啉
公开(公告)号：EP0585328A1
公开(公告)日：1994-03-09
申请号：EP92911350.0
申请日：1992-05-19
申请人： PFIZER INC.
发明人： ITO, Fumitaka , KOKURA, Toshihide , NAKANE, Masami , SATAKE, Kunio , WAKABAYASHI, Hiroaki
IPC分类号： A61K31 , C07D453
CPC分类号： C07D453/02
摘要： L'invention se rapporte à des composés représentés par la formule (I), où W, Ar1, Ar2 et Ar3 sont définis ci-dessous; ainsi qu'à des sels pharmaceutiquement acceptables de ces composés. Ces composés sont des antagonistes de la substance P et ils sont utiles dans le traitement des troubles gastro-intestinaux, des troubles inflammatoires, des troubles du système nerveux central et de la douleur.
摘要翻译：本发明涉及由式（I）表示的化合物，其中W，Ar 1，Ar 2和Ar 3如下定义; 以及这些化合物的药学上可接受的盐。这些化合物是P物质拮抗剂，可用于治疗胃肠疾病，炎性疾病，中枢神经系统疾病和疼痛。

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