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：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：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.

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：US4643993A

公开(公告)日：1987-02-17

申请号：US495717

申请日：1983-05-18

申请人： Enzo Cereda ,  Arturo Donetti ,  Antonio Giachetti ,  Piero del Soldato

发明人： Enzo Cereda ,  Arturo Donetti ,  Antonio Giachetti ,  Piero del Soldato

IPC分类号： A61K31/41 ,  A61P1/04 ,  C07D231/12 ,  C07D233/54 ,  C07D233/64 ,  C07D249/08 ,  C07F9/40 ,  C07F9/6503 ,  C07F9/6506 ,  C07F9/6518 ,  A61K31/675 ,  C07F9/65

CPC分类号： C07D231/12 ,  C07D233/64 ,  C07D249/08 ,  C07F9/4006 ,  C07F9/65037 ,  C07F9/65067 ,  C07F9/65187

摘要： Compounds of the formula ##STR1## wherein Het is a heterocycle containing 2 to 3 nitrogen atoms;R is hydrogen, lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen;Y is --SO.sub.3 H or ##STR2## R" is alkyl of 1 to 3 carbon atoms; and R' is straight or branched alkyl which may contain a heteroatom such as sulfur, oxygen or nitrogen; straight or branched alkenyl; cycloalkyl; alkyl-cycloalkyl; aryl; or aralkyl optionally substituted by lower alkyl, alkoxy of 1 to 3 carbon atoms or halogen; tautomers thereof, and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as anti-ulcerogenics and gastric acid secretion inhibitors.

摘要翻译： 其中Het是含有2至3个氮原子的杂环的式“IMAGE”的化合物; R为氢，低级烷基，1〜3个碳原子的烷氧基或卤素; Y是-SO 3 H或R 3是具有1至3个碳原子的烷基; 并且R'是可以含有杂原子如硫，氧或氮的直链或支链烷基; 直链或支链烯基; 环烷基 烷基 - 环烷基 芳基; 或任选被低级烷基，1至3个碳原子的烷氧基或卤素取代的芳烷基; 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和胃酸分泌抑制剂。

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：US5223511A

公开(公告)日：1993-06-29

申请号：US845891

申请日：1992-03-04

申请人： Marco Turconi ,  Arturo Donetti ,  Ernesto Montagna ,  Massimo Nicola ,  Annamaria Uberti ,  Rosamaria Micheletti ,  Antonio Giachetti

发明人： Marco Turconi ,  Arturo Donetti ,  Ernesto Montagna ,  Massimo Nicola ,  Annamaria Uberti ,  Rosamaria Micheletti ,  Antonio Giachetti

IPC分类号： C07D401/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08

CPC分类号： C07D401/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08

摘要： New pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid derivatives which are 5-HT receptor antagonists useful as antiemetic agents and as gastric prokinetic agents of the following formula: ##STR1##wherein R is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl; R.sub.1 is hydrogen; R.sub.2 is hydrogen, halogen or C.sub.1-6 alkoxy; Y is oxygen or N--R.sub.3 in which R.sub.3 is hydrogen; A is a group selected from: ##STR2##wherein p is 1; r is 0, 2 or 3: R.sub.4 is hydrogen; R.sub.5 is hydrogen, C.sub.1-6 alkyl, or R.sub.5 is a group of the formula --CR.sub.6 =N--R.sub.7 wherein R.sub.6 is hydrogen, C.sub.1-4 alkyl or amino and R.sub.7 is hydrogen or C.sub.1-6 alkyl; or a pharmaceutically acceptable acid addition salt thereof.The processes for the preparation of the compounds of formula (I) as well as pharmaceutical compositions contained in them are also described.

摘要翻译： 新的药理学活性苯并咪唑啉-2-氧代-1-羧酸衍生物，其是可用作止吐剂的5-HT受体拮抗剂和作为下式的胃促动力剂：其中R是氢，C 1-6烷基 ，C 2-6烯基或C 2-6炔基; R1是氢; R2是氢，卤素或C1-6烷氧基; Y是氧或N-R3，其中R3是氢; （a）选自下列的组：（a）（b）（c）（d）其中p为1; r为0,2或3：R4为氢; R5是氢，C1-6烷基或R5是式-CR6 = N-R7的基团，其中R6是氢，C1-4烷基或氨基，R7是氢或C1-6烷基; 或其药学上可接受的酸加成盐。 还描述了制备式（I）化合物的方法以及其中所含的药物组合物。

公开(公告)号：US5358954A

公开(公告)日：1994-10-25

申请号：US33675

申请日：1993-03-16

申请人： Marco Turconi ,  Arturo Donetti ,  Ernesto Montagna ,  Massimo Nicola ,  Annamaria Uberti ,  Rosamaria Micheletti ,  Antonio Giachetti

发明人： Marco Turconi ,  Arturo Donetti ,  Ernesto Montagna ,  Massimo Nicola ,  Annamaria Uberti ,  Rosamaria Micheletti ,  Antonio Giachetti

IPC分类号： C07D401/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08 ,  A61K31/46

CPC分类号： C07D401/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08

摘要： Pharmacologically active benzimidazoline-2-oxo-1-carboxylic acid compounds which are useful for treating a human host suffering from anxiety.

摘要翻译： 可用于治疗患有焦虑的人宿主的药理学活性苯并咪唑啉-2-氧代-1-羧酸化合物。

公开(公告)号：US5552408A

公开(公告)日：1996-09-03

申请号：US432338

申请日：1994-05-01

申请人： Marco Turconi ,  Arturo Donetti ,  Ernesto Montagna ,  Massimo Nicola ,  Annamaria Uberti ,  Rosamaria Micheletti ,  Antonio Giachetti

发明人： Marco Turconi ,  Arturo Donetti ,  Ernesto Montagna ,  Massimo Nicola ,  Annamaria Uberti ,  Rosamaria Micheletti ,  Antonio Giachetti

IPC分类号： C07D401/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08 ,  A61K31/46

CPC分类号： C07D401/12 ,  C07D451/12 ,  C07D451/14 ,  C07D453/02 ,  C07D453/06 ,  C07D487/08

摘要： A method for treating a human host suffering from psychosis, which method comprises administering to such host a therapeutically effective amount of a compound of the formula I ##STR1## wherein the radicals are defined in claim 1.

摘要翻译： 用于治疗患有精神病的人宿主的方法，该方法包括向所述宿主施用治疗有效量的式I（I）化合物，其中所述基团如权利要求1所定义。

公开(公告)号：US4724236A

公开(公告)日：1988-02-09

申请号：US944146

申请日：1986-12-19

申请人： Wolfgang Eberlein ,  Gunter Trummlitz ,  Wolfhard Engel ,  Gerhard Mihm ,  Rudolf Hammer ,  Norbert Mayer ,  Antonio Giachetti ,  Adriaan de Jonge

发明人： Wolfgang Eberlein ,  Gunter Trummlitz ,  Wolfhard Engel ,  Gerhard Mihm ,  Rudolf Hammer ,  Norbert Mayer ,  Antonio Giachetti ,  Adriaan de Jonge

IPC分类号： A61K31/55 ,  C07D471/04 ,  C07D403/14

CPC分类号： C07D471/04

摘要： Compounds of general formula I are described, ##STR1## wherein X represents the group .dbd.CHR, .dbd.NR or an oxygen atom andA represents the groups --NR.sup.1 R.sup.2,wherein R.sup.1 and R.sup.2 represent alkyl, cycloalkyl or phenylalkyl groups, n represents the number 0, 1 or 2, R.sup.3 represents a hydrogen atom, a hydroxy or alkyl group or a group --(CH.sub.2).sub.n --N--R.sup.5 R.sup.6 (R.sup.5 and R.sup.6 being lower alkyl groups) and R.sup.4 is an alkyl or phenylalkyl group; two processes for preparing these compounds and the salts thereof are also described.The compounds have favourable effects on heart rate and can be used as vagal pacemakers for treating bradycardia and bradyarrhythmia in human and veterinary medicine. Some of these compounds also have very good antithrombotic effects.

摘要翻译： 描述通式I的化合物，其中X表示基团= CHR，= NR或氧原子，A表示基团-NR1R2，其中R1和R2表示烷基，环烷基或苯基烷基，n表示 数字0,1或2，R3表示氢原子，羟基或烷基或基团 - （CH2）nN-R5R6（R5和R6是低级烷基），R4表示烷基或苯基烷基; 还描述了制备这些化合物及其盐的两种方法。 这些化合物对心率有好的影响，可用作迷走神经心脏起搏器，用于治疗人和兽医学中的心动过缓和缓慢性心律失常。 这些化合物中的一些也具有非常好的抗血栓形成作用。