公开(公告)号：US5576318A

公开(公告)日：1996-11-19

申请号：US216742

申请日：1994-03-23

申请人： Giuseppe Bietti ,  Franco Borsini ,  Marco Turconi ,  Ettore Giraldo ,  Maura Bignotti

发明人： Giuseppe Bietti ,  Franco Borsini ,  Marco Turconi ,  Ettore Giraldo ,  Maura Bignotti

IPC分类号： A61K31/495 ,  A61K31/00 ,  A61K31/397 ,  A61K31/41 ,  A61K31/4184 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/55 ,  A61P9/00 ,  A61P25/00 ,  A61P25/04 ,  A61P43/00 ,  C07D235/26 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D403/00 ,  C07D473/00

CPC分类号： C07D403/06 ,  C07D235/26 ,  C07D403/12 ,  C07D405/12

摘要： Pharmacologically active benzimidazolone derivatives as 5-HT.sub.1A and 5-HT.sub.2 receptors, useful in the treatment of CNS disorders, of formula: ##STR1## wherein the substituents are defined herein.

摘要翻译： 用于治疗CNS病症的5-HT1A和5-HT2受体的药理学活性苯并咪唑酮衍生物，其分子式如下：其中取代基在本文中定义。

公开(公告)号：US4649150A

公开(公告)日：1987-03-10

申请号：US610958

申请日：1984-05-16

申请人： Giuseppe Bietti ,  Enzo Cereda ,  Arturo Donetti ,  Antonio Giachetti ,  Ferdinando Pagani

发明人： Giuseppe Bietti ,  Enzo Cereda ,  Arturo Donetti ,  Antonio Giachetti ,  Ferdinando Pagani

IPC分类号： C07D233/34 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4166 ,  A61P1/04 ,  C07D233/54 ,  C07D233/64 ,  C07D233/66 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88 ,  A61K31/44

CPC分类号： C07D233/64 ,  C07D233/68 ,  C07D233/70 ,  C07D233/84 ,  C07D233/88

摘要： Compounds of the formula ##STR1## wherein R represents substituents of various types;R.sub.1 and R.sub.2 are each independently hydrogen or lower alkyl;R.sub.3 represents substituents of various types; andR.sub.4 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halogen, cyano or carbamoyl;tautomers thereof; and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics.

摘要翻译： 其中R代表各种类型的取代基的式“IMAGE”的化合物; R 1和R 2各自独立地为氢或低级烷基; R3代表各种类型的取代基; R4为氢，1〜3个碳原子的烷基，1〜3个碳原子的烷氧基，卤素，氰基或氨基甲酰基; 互变异构体 和无毒的，药学上可接受的酸加成盐。 化合物及其盐可用作抗溃疡药。

公开(公告)号：US4548944A

公开(公告)日：1985-10-22

申请号：US465572

申请日：1983-02-10

申请人： Giuseppe Bietti ,  Enzo Cereda ,  Arturo Donetti ,  Piero del Soldato ,  Antonio Giachetti ,  Rosamaria Micheletti

发明人： Giuseppe Bietti ,  Enzo Cereda ,  Arturo Donetti ,  Piero del Soldato ,  Antonio Giachetti ,  Rosamaria Micheletti

IPC分类号： C07D277/20 ,  A61K31/155 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/535 ,  A61P1/00 ,  A61P1/04 ,  A61P43/00 ,  C07D263/48 ,  C07D271/06 ,  C07D271/07 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D285/08 ,  C07D285/12 ,  C07D285/125 ,  C07D285/135 ,  C07F9/535 ,  C07F9/54

CPC分类号： C07D271/07 ,  C07D263/48 ,  C07D277/48 ,  C07D285/08 ,  C07D285/135 ,  C07F9/5355 ,  C07F9/5463 ,  Y10S514/925

摘要： Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; orR.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group;R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; andHet is a substituted or unsubstituted heterocycle containing two or three heteroatoms;tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.

摘要翻译： 互变异构体式（I）的化合物其中R，R 1和R 2可以彼此相同或不同，分别为氢或1-4个碳原子的烷基; R3是直链或支链烷基，任选地被杂原子例如氧，硫或氮中断; 直链或支链烯基; 炔基; 氰基; 环烷基或脂环族烷基; 双环组 芳基; 或杂环基; 或R 2和R 3彼此连接并与它们相连的氮原子形成杂环基; R4是氢，卤素，1至4个碳原子的烷基或1至4个碳原子的烷氧基; Het是含有两个或三个杂原子的取代或未取代的杂环; 互变异构体及其无毒的药理学上可接受的酸加成盐。 化合物及其盐可用作抗溃疡发生剂。

公开(公告)号：US4666932A

公开(公告)日：1987-05-19

申请号：US751081

申请日：1985-07-02

申请人： Enzo Cereda ,  Giuseppe Bietti ,  Arturo Donetti ,  Piero del Soldato ,  Antonio Giachetti ,  Ferdinando Pagani

发明人： Enzo Cereda ,  Giuseppe Bietti ,  Arturo Donetti ,  Piero del Soldato ,  Antonio Giachetti ,  Ferdinando Pagani

IPC分类号： A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41 ,  A61K31/4245 ,  A61P1/04 ,  A61P43/00 ,  C07D213/40 ,  C07D231/12 ,  C07D231/38 ,  C07D233/54 ,  C07D233/64 ,  C07D233/68 ,  C07D233/84 ,  C07D233/95 ,  C07D239/26 ,  C07D239/36 ,  C07D239/42 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D271/07 ,  C07D277/28 ,  C07D277/40 ,  C07D277/42 ,  C07D307/38 ,  C07D307/52 ,  C07D333/12 ,  C07D333/16 ,  C07D333/20 ,  C07D405/12 ,  A61K31/415

CPC分类号： C07D213/40 ,  C07D231/12 ,  C07D233/64 ,  C07D233/68 ,  C07D233/84 ,  C07D233/95 ,  C07D239/26 ,  C07D239/36 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D271/07 ,  C07D277/28 ,  C07D277/40 ,  C07D277/42 ,  C07D307/38 ,  C07D307/52 ,  C07D333/12 ,  C07D333/16 ,  C07D333/20 ,  C07D405/12

摘要： Compounds of the formula ##STR1## wherein R is hydrogen or methyl;R.sub.1 is straight or branched alkyl of 1 to 6 carbon atoms, dimethyldioxolylmethyl, hydroxymethyldioxolylmethyl, hydroxy(alkyl of 1 to 6 carbon atoms), mono- or di-(alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms), (alkyl of 1 to 6 carbon atoms)thio- (alkyl of 1 to 6 carbon atoms), (alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms)thio-(alkyl of 1 to 6 carbon atoms), cyano(alkyl of 1 to 6 carbon atoms), di-lower alkyl-amino(alkyl of 1 to 6 carbon atoms), alkenyl, alkynyl, or cycloalkyl;R.sub.2 and R.sub.3 are each independently hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen; andZ is imidazol-2-yl or imidazol-4-yl;provided however that, when R.sub.1 is straight or branched alkyl, alkenyl, alkynyl, cycloalkyl or cyano and R, R.sub.2 and R.sub.3 are hydrogen, Z is other than imidazol-4-yl; tautomers thereof and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics and gastric acid secretion inhibitors.

摘要翻译： 其中R是氢或甲基的式“IMAGE”的化合物; R1是1至6个碳原子的直链或支链烷基，二甲基二恶唑基甲基，羟甲基二恶唑基甲基，羟基（1至6个碳原子的烷基），1或6个碳原子的单 - 或二 - （烷氧基）（1-6个碳原子的烷基） ），（碳原子数1〜6的烷基）硫代（1〜6个碳原子的烷基），（碳原子数为1〜6的烷氧基）（碳原子数1〜6的烷基）硫代 - 原子），氰基（1至6个碳原子的烷基），二低级烷基 - 氨基（1至6个碳原子的烷基），烯基，炔基或环烷基; R2和R3各自独立地为氢，1至3个碳原子的烷基，1至3个碳原子的烷氧基或卤素; 和Z是咪唑-2-基或咪唑-4-基; 但是当R1为直链或支链烷基，烯基，炔基，环烷基或氰基时，R，R2和R3为氢，Z为咪唑-4-基; 其互变异构体和无毒的药学上可接受的酸加成盐。 化合物及其盐可用作抗溃疡药和胃酸分泌抑制剂。

公开(公告)号：US4645841A

公开(公告)日：1987-02-24

申请号：US748309

申请日：1985-06-24

申请人： Giuseppe Bietti ,  Enzo Cereda ,  Arturo Donetti ,  Piero Del Soldato ,  Antonio Giachetti ,  Rosamaria Micheletti

发明人： Giuseppe Bietti ,  Enzo Cereda ,  Arturo Donetti ,  Piero Del Soldato ,  Antonio Giachetti ,  Rosamaria Micheletti

IPC分类号： C07D277/20 ,  A61K31/155 ,  A61K31/42 ,  A61K31/425 ,  A61K31/426 ,  A61K31/535 ,  A61P1/00 ,  A61P1/04 ,  A61P43/00 ,  C07D263/48 ,  C07D271/06 ,  C07D271/07 ,  C07D277/40 ,  C07D277/42 ,  C07D277/48 ,  C07D285/08 ,  C07D285/12 ,  C07D285/125 ,  C07D285/135 ,  C07F9/535 ,  C07F9/54 ,  C07D263/28

CPC分类号： C07D271/07 ,  C07D263/48 ,  C07D277/48 ,  C07D285/08 ,  C07D285/135 ,  C07F9/5355 ,  C07F9/5463 ,  Y10S514/925

摘要： Compounds of the tautomeric formula ##STR1## wherein R, R.sub.1 and R.sub.2, which may be identical to or different from each other, are each hydrogen or alkyl of 1 to 4 carbon atoms;R.sub.3 is straight or branched alkyl, optionally interrupted by heteroatoms such as oxygen, sulfur or nitrogen; straight or branched alkenyl; alkynyl; cyano; cycloalkyl or cycloaliphatic alkyl; a bicyclic group; aryl; or a heterocyclic group; orR.sub.2 and R.sub.3, together with each other and the nitrogen atoms to which they are attached, form a heterocyclic group;R.sub.4 is hydrogen, halogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; andHet is a substituted or unsubstituted heterocycle containing two or three heteroatoms; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics.

公开(公告)号：US5164386A

公开(公告)日：1992-11-17

申请号：US541106

申请日：1990-06-20

申请人： Enzo Cereda ,  Giuseppe Bietti ,  Giovanni B. Schiavi ,  Arturo Donetti ,  Antonio Schiavone ,  Henri N. Doods

发明人： Enzo Cereda ,  Giuseppe Bietti ,  Giovanni B. Schiavi ,  Arturo Donetti ,  Antonio Schiavone ,  Henri N. Doods

IPC分类号： C07D401/12 ,  A61K31/435 ,  A61K31/439 ,  A61K31/445 ,  A61K31/55 ,  A61P1/00 ,  A61P1/04 ,  A61P11/00 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  A61P25/02 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14 ,  C07D453/00 ,  C07D453/02

CPC分类号： C07D453/02

摘要： Pharmacologically active R(-) 3-quinuclidinol derivatives are described which are muscarinic receptor blocking agents useful for the treatment of gastrointestinal and respiratory tract disorders of the following formula (I) ##STR1## wherein R represents a linear or branched lower alkyl group, a cycloalkyl-C.sub.1-2 alkyl or an aralkyl group, or it is absent;X represents the anion of an organic or inorganic acid, or it is absent, when R is absent;R.sub.1 represents H, a linear or branched lower alkyl group or an acyl group of the type R.sub.2 --CO, in which R.sub.2 is H or a linear or branched lower alkyl group;A represents a cycloalkyl, an aromatic ring or a 5- or 6-membered heterocyclic ring;Y and Z may be simultaneously or alternatively present or absent; when they are simultaneously present, they represent oxygen; when only one of them is present, it is oxygen or sulphur;n is 1, 2 or 3;A and the 3-quinuclidinyl ester groups are inserted simultaneously on the same carbon atom of the ring to give rise to a geminal substitution.The process for the preparation of the compounds of formula (I) as well as pharmaceutical compositions containing them are also described.

公开(公告)号：US4699915A

公开(公告)日：1987-10-13

申请号：US751087

申请日：1985-07-02

申请人： Enzo Cereda ,  Giuseppe Bietti ,  Arturo Donetti ,  Piero del Soldato ,  Antonio Giachetti ,  Ferdinando Pagani

发明人： Enzo Cereda ,  Giuseppe Bietti ,  Arturo Donetti ,  Piero del Soldato ,  Antonio Giachetti ,  Ferdinando Pagani

IPC分类号： A61K31/34 ,  A61K31/341 ,  A61K31/38 ,  A61K31/381 ,  A61K31/41 ,  A61K31/4245 ,  A61P1/04 ,  A61P43/00 ,  C07D213/40 ,  C07D231/12 ,  C07D231/38 ,  C07D233/54 ,  C07D233/64 ,  C07D233/68 ,  C07D233/84 ,  C07D233/95 ,  C07D239/26 ,  C07D239/36 ,  C07D239/42 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D271/07 ,  C07D277/28 ,  C07D277/40 ,  C07D277/42 ,  C07D307/38 ,  C07D307/52 ,  C07D333/12 ,  C07D333/16 ,  C07D333/20 ,  C07D405/12 ,  A61K31/415

CPC分类号： C07D213/40 ,  C07D231/12 ,  C07D233/64 ,  C07D233/68 ,  C07D233/84 ,  C07D233/95 ,  C07D239/26 ,  C07D239/36 ,  C07D249/08 ,  C07D263/32 ,  C07D271/06 ,  C07D271/07 ,  C07D277/28 ,  C07D277/40 ,  C07D277/42 ,  C07D307/38 ,  C07D307/52 ,  C07D333/12 ,  C07D333/16 ,  C07D333/20 ,  C07D405/12

摘要： Compounds of the formula ##STR1## wherein R is hydrogen or methyl;R.sub.1 is straight or branched alkyl of 1 to 6 carbon atoms, hydroxy(alkyl of 1 to 6 carbon atoms), mono- or di-(alkoxy of 1 to 6 carbon atoms)(alkyl of 1 to 6 carbon atoms), (alkyl of 1 to 6 cabon atoms)thio(alkyl of 1 to 6 carbon atoms), cyano(alkyl of 1 to 6 carbon atoms), alkenyl, alkynyl, or cycloalkyl;R.sub.2 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halogen; andX is pyrazol-3-yl, 1,2,4-triazol-3-yl, pyridin-2-yl, pyridin-3-yl, thiazol-4-yl, 2-methyl-thiazol-4-yl or 2-methylamino-thiazol-4-yl;tautomers thereof, and non-toxic, pharmacologiically acceptable acid addition salts thereof. The compounds as well as their salts are useful as antiulcerogenics and gastric acid secretion inhibitors.