公开(公告)号：US4927837A

公开(公告)日：1990-05-22

申请号：US292257

申请日：1988-12-30

申请人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

发明人： Giulio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

IPC分类号： A61K31/445 ,  A61K31/451 ,  A61P25/28 ,  C07D211/28 ,  C07D211/94

CPC分类号： C07D211/94 ,  C07D211/28

摘要： Derivatives of 3-piperidine carbaldehyde oxime having the formula ##STR1## process for preparing the same, therapeutic compositions containing the same, and method of use in treating patients suffering from Alzheimer's disease, senile dementia, or memory disorders in the aged.

摘要翻译： 具有式“IMAGE”的3-哌啶甲醛肟的衍生物，其制备方法，含有该组合物的治疗组合物，以及用于治疗患有阿尔茨海默病，老年性痴呆或老年记忆障碍的患者的方法。

公开(公告)号：US4897414A

公开(公告)日：1990-01-30

申请号：US211720

申请日：1988-06-27

申请人： Emilio Toja ,  Carlo Zirotti ,  Fernando Barzaghi ,  Giulio Galliani

发明人： Emilio Toja ,  Carlo Zirotti ,  Fernando Barzaghi ,  Giulio Galliani

IPC分类号： A61K31/40 ,  A61K31/4025 ,  A61K31/42 ,  A61K31/435 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07D207/26 ,  C07D207/273 ,  C07D207/48 ,  C07D409/12 ,  C07D411/12 ,  C07D413/12

CPC分类号： C07D207/273 ,  C07D207/48

摘要： Compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures, senescence or mental strain of the formula (I) ##STR1## in which R' represents hydrogen, linear, branched or cyclic alkyl containing up to 8 carbon atoms, alkenyl containing from 2 to 8 carbon atoms, acyl containing from 1 to 6 carbon atoms or aralkyl containing from 7 to 15 carbon atoms and R represents aryl containing up to 14 carbon atoms, possibly substituted, or a mono- or polycyclic heterocyclic aromatic radical possibly substituted; also process and intermediates for their preparation, therapeutic compositions containing those compounds and method of use.

摘要翻译： 用于治疗患有智力或神经性虚弱，记忆障碍，衰老或精神紧张的患者的化合物（I）其中R'表示氢，直链，支链或环状烷基含有至多8个 碳原子，含有2至8个碳原子的烯基，含有1至6个碳原子的酰基或含有7至15个碳原子的芳烷基，R代表含有至多14个碳原子的芳基，可能被取代，或单环或多环杂环 可能被取代的芳族基团 还包括其制备方法和中间体，含有这些化合物的治疗组合物和使用方法。

公开(公告)号：US4810722A

公开(公告)日：1989-03-07

申请号：US30113

申请日：1987-03-26

申请人： Emilio Toja ,  Carlo Zirotti ,  Giulio Galliani ,  Fernando Barzaghi

发明人： Emilio Toja ,  Carlo Zirotti ,  Giulio Galliani ,  Fernando Barzaghi

IPC分类号： A61K31/40 ,  A61P25/28 ,  C07D207/48

CPC分类号： C07D207/48

摘要： The therapeutic compounds useful in the treatment of patients suffering from intellectual or nervous asthenias, memory failures or old age and excessive intellectual fatigue having the formula (I): ##STR1## in which R.sub.1 represents an alkyl radical, linear or branched, containing up to 8 carbons atoms, an acyl radical containing from 1 to 6 carbon atoms or a cycloalkyl radical containing from 3 to 6 carbon atoms and R represents an aryl radical containing up to 14 carbon atoms, unsubstituted or substituted, or a mono- or polycyclic heterocyclic radical, unsubstituted or substituted. Also, therapeutic compositions containing the compound, method of preparing the compound and method of use.

摘要翻译： 治疗化合物可用于治疗患有智力或神经失调，记忆障碍或老年人和过度智力疲劳的患者，其具有式（I）：其中R 1表示直链或支链的烷基， 含有至多8个碳原子，含有1至6个碳原子的酰基或含有3至6个碳原子的环烷基，R表示含有至多14个碳原子的芳基，未取代或取代的，或单或 多环杂环基团，未取代或取代的。 此外，含有该化合物的治疗组合物，该化合物的制备方法和使用方法。

公开(公告)号：US5532375A

公开(公告)日：1996-07-02

申请号：US313616

申请日：1994-09-30

申请人： Giulio Galliani ,  Fernando Barzashi ,  Alina Butti ,  Carla Bonetti ,  Emilio Toja

发明人： Giulio Galliani ,  Fernando Barzashi ,  Alina Butti ,  Carla Bonetti ,  Emilio Toja

IPC分类号： A61K31/44 ,  A61P25/28 ,  A61P43/00 ,  C07D211/28 ,  C07D211/70 ,  C07D211/82

CPC分类号： C07D211/70

摘要： Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.

摘要翻译： 用于治疗阿尔茨海默病，老年性痴呆或记忆障碍的化合物，其具有式（IMAGE），其中R表示氢原子，含有至多8个碳原子的饱和或不饱和的直链，支链或环状烷基， 可能被游离或酯化的羧基取代，或R表示含有至多10个碳原子的芳烷基，R'表示含有至多8个碳原子的直链或支链，饱和或不饱和的烷基，基团-COalk1或 自由基 - （CH2）2N（alk2）2，alk1和alk2代表含有至多8个碳原子的烷基，以及它们与酸的加成盐。 还含有相同的组合物，制备方法和使用其的处理方法。

公开(公告)号：US5391754A

公开(公告)日：1995-02-21

申请号：US39826

申请日：1993-03-30

申请人： Giulio Galliani ,  Fernando Barzashi ,  Alina Butti ,  Carla Bonetti ,  Emilio Toja

发明人： Giulio Galliani ,  Fernando Barzashi ,  Alina Butti ,  Carla Bonetti ,  Emilio Toja

IPC分类号： A61K31/44 ,  A61P25/28 ,  A61P43/00 ,  C07D211/28 ,  C07D211/70

CPC分类号： C07D211/70

摘要： Compounds useful in the treatment of Alzheimer's disease, senile dementia, or memory disorders which have the formula ##STR1## in which R represents a hydrogen atom, a linear, branched or cyclic alkyl radical, saturated or unsaturated, containing up to 8 carbon atoms, possibly substituted by a free or esterified carboxy radical or R represents an aralkyl radical containing up to 10 carbon atoms and R' represents a linear or branched, saturated or unsaturated, alkyl radical, containing up to 8 carbon atoms, a radical --COalk.sub.1 or a radical --(CH.sub.2).sub.2 N(alk.sub.2).sub.2, alk.sub.1 and alk.sub.2 representing an alkyl radical containing up to 8 carbon atoms, as well as their addition salts with acids. Also compositions containing the same, method of preparation and method of treatment using the same.

摘要翻译： 用于治疗阿尔茨海默病，老年性痴呆或记忆障碍的化合物，其具有式（IMAGE），其中R表示氢原子，含有至多8个碳原子的饱和或不饱和的直链，支链或环状烷基， 可能被游离或酯化的羧基取代，或R表示含有至多10个碳原子的芳烷基，R'表示含有至多8个碳原子的直链或支链，饱和或不饱和的烷基，基团-COalk1或 自由基 - （CH2）2N（alk2）2，alk1和alk2代表含有至多8个碳原子的烷基，以及它们与酸的加成盐。 还含有相同的组合物，制备方法和使用其的处理方法。

公开(公告)号：US5231107A

公开(公告)日：1993-07-27

申请号：US863466

申请日：1992-04-01

申请人： Guilio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

发明人： Guilio Galliani ,  Fernando Barzaghi ,  Carla Bonetti ,  Emilio Toja

IPC分类号： C07D211/70

CPC分类号： C07D211/70

摘要： Compounds useful in the treatment of patients suffering from senile dementia, Alzheimer's disease or memory defects, of the formula ##STR1## in which R' represents hydrogen, a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, and R represents a linear, branched or cyclic alkyl, alkenyl, or alkynyl, containing up to 18 carbon atoms, possibly substituted, aryl containing up to 14 carbon atoms, possibly substituted, aralkyl containing up to 18 carbon atoms, possibly substituted, as well as their addition salts with organic or mineral acids, and to compounds of formula (I) in which R represents phenyl substituted in the 4 position by Br, F, CH.sub.3, NO.sub.2 or C(CH.sub.3).sub.2 C(CH.sub.3).sub.3 and R' represents CH.sub.3.

摘要翻译： 用于治疗患有老年性痴呆，阿尔茨海默病或记忆缺陷的患者的化合物，其中R'代表氢，直链，支链或环状的烷基，烯基或炔基，其含有至多8个 并且R表示含有至多18个碳原子的直链，支链或环状烷基，烯基或炔基，可能被取代的，含有至多14个碳原子的芳基，可能被取代的含有至多18个碳原子的芳烷基，可能被取代 以及它们与有机或无机酸的加成盐，以及式（I）化合物，其中R表示被Br，F，CH 3，NO 2或C（CH 3）2 C（CH 3）3取代的4位的苯基， R'表示CH3。

公开(公告)号：US4435417A

公开(公告)日：1984-03-06

申请号：US391653

申请日：1982-06-24

申请人： Emilio Toja ,  Amedeo Omodei-Sale' ,  Domenica Selva

发明人： Emilio Toja ,  Amedeo Omodei-Sale' ,  Domenica Selva

IPC分类号： C07D235/02 ,  A61K31/415 ,  C07D235/18

CPC分类号： C07D235/02 ,  Y10S514/825

摘要： 3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 stands for hydrogen, hydroxy, methoxy, ethoxy, or mono- or di-methylamino, and R.sub.4 represents hydrogen or (C.sub.1-4)alkyl.Also described and claimed are their use as antiinflammatory agents and the pharmaceutical compositions containing them.

摘要翻译： 其中R代表（C 1-6）烷基，（C 3-6）烯基，（C 3-6）炔基或（C 3-7）环烷基，R 1 并且R 2各自独立地表示氢，卤素，（C 1-4）烷基，（C 1-4）烷硫基，（C 1-4）烷氧基或卤代（C 1-4）烷氧基，R 3代表氢，羟基，甲氧基，乙氧基 ，或单 - 或二 - 甲基氨基，R 4表示氢或（C 1-4）烷基。 还描述和要求保护它们用作抗炎剂和含有它们的药物组合物。

公开(公告)号：US4716159A

公开(公告)日：1987-12-29

申请号：US891815

申请日：1986-07-30

申请人： Emilio Toja

发明人： Emilio Toja

IPC分类号： A61K31/47 ,  A61K31/50 ,  A61P25/20 ,  C07D209/46 ,  C07D237/14 ,  C07D471/04 ,  C07D491/04

CPC分类号： C07D471/04 ,  C07D209/46 ,  C07D237/14 ,  C07D491/04

摘要： The present invention is directed to pyridazino[4,3-c]isoquinolines of Formula I ##STR1## wherein R represents methyl, phenyl or substituted phenyl groups, R.sub.1 represents inter alia amino or substituted amino, alkoxy or cycloalkoxy groups, having pharmacological activity, to process for preparing them and to the pharmaceutical compositions containing them. The compounds of the invention possess anti-anxiety activity.

摘要翻译： 本发明涉及式I的哒嗪并[4,3-c]异喹啉其中R代表甲基，苯基或取代的苯基，R 1代表氨基或取代的氨基，烷氧基或环烷氧基，具有药理活性 ，以制备它们以及含有它们的药物组合物。 本发明化合物具有抗焦虑活性。

公开(公告)号：US4594348A

公开(公告)日：1986-06-10

申请号：US698653

申请日：1985-02-06

申请人： Emilio Toja ,  Domenico Barone ,  Emiliana Baldoli

发明人： Emilio Toja ,  Domenico Barone ,  Emiliana Baldoli

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/495 ,  A61K31/496 ,  A61P9/12 ,  C07D235/02 ,  A61K31/50

CPC分类号： C07D235/02

摘要： The present invention is directed to a new pharmacological use of some known naphthoimidazole derivatives. More particularly, the compounds of the invention are 2-[2-(4-phenyl-1-piperazinyl)ethyl]-1H-naphtho[1,2-d]imidazoles of formula ##STR1## wherein R is selected from methyl and 1-methylethyl and R.sup.1 is selected from hydrogen, chloro, methoxy and trifluoromethyl and the pharmaceutically acceptable acid addition salts thereof and possess antihypertensive activity.

摘要翻译： 本发明涉及一些已知的萘并咪唑衍生物的新的药理学应用。 更具体地说，本发明的化合物是式[IMAGE]的2- [2-（4-苯基-1-哌嗪基）乙基] -1H-萘并[1,2-d]咪唑，其中R选自甲基和 - 甲基乙基，R 1选自氢，氯，甲氧基和三氟甲基及其药学上可接受的酸加成盐，并具有抗高血压活性。

公开(公告)号：US4340607A

公开(公告)日：1982-07-20

申请号：US236468

申请日：1981-02-20

申请人： Emilio Toja ,  Amedeo Omodei-Sale ,  Domenica Selva

发明人： Emilio Toja ,  Amedeo Omodei-Sale ,  Domenica Selva

IPC分类号： A61K31/415 ,  A61K31/4184 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P25/04 ,  A61P29/00 ,  A61P31/04 ,  C07D235/02 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D405/02

CPC分类号： C07D235/02

摘要： 3H-naphtho[1,2-d]imidazole derivatives of formula ##STR1## wherein R stands for (C.sub.1-6)alkyl, (C.sub.3-6)alkenyl, (C.sub.3-6)alkynyl or (C.sub.3-7)cycloalkyl, R.sub.1 and R.sub.2, each independently may represent hydrogen, halogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkylthio, (C.sub.1-4)alkoxy or halo(C.sub.1-4)alkoxy, R.sub.3 and R.sub.4, each independently, represent hydrogen or (C.sub.1-4)alkoxy, R.sub.5 stands for hydrogen, (C.sub.1-4)alkyl, (C.sub.3-4)alkoxy, mono- and di-(C.sub.2-4)alkylamino, (C.sub.2-4)alkanoylamino, carboxymethoxy and [carbo(C.sub.1-4)alkoxy]methoxy and R.sub.6 is hydrogen or R.sub.4 and R.sub.6 taken together may represent a methylenedioxy radical with the proviso that when R.sub.5 is hydrogen at least one of R.sub.3 and R.sub.4 must be different from hydrogen, useful as antimicrobial agents.

摘要翻译： 其中R代表（C 1-6）烷基，（C 3-6）烯基，（C 3-6）炔基或（C 3-7）环烷基，R 1 并且R 2各自独立地表示氢，卤素，（C 1-4）烷基，（C 1-4）烷硫基，（C 1-4）烷氧基或卤代（C 1-4）烷氧基，R 3和R 4各自独立地表示氢或 （C 1-4）烷氧基，R5代表氢，（C1-4）烷基，（C3-4）烷氧基，单 - 和二 - （C2-4）烷基氨基，（C2-4）烷酰基氨基，羧甲氧基和[ C 1-4）烷氧基]甲氧基并且R 6是氢或R 4和R 6一起可以代表亚甲二氧基，条件是当R 5是氢时，R 3和R 4中的至少一个必须不同于氢，可用作抗微生物剂。