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：US5037822A

公开(公告)日：1991-08-06

申请号：US482500

申请日：1990-02-21

申请人： Emilio Toja ,  Fernando Barzaghi ,  Giulio Galliani

发明人： Emilio Toja ,  Fernando Barzaghi ,  Giulio Galliani

IPC分类号： C07D211/72 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/445 ,  A61P25/02 ,  A61P25/08 ,  C07C311/19 ,  C07D207/263 ,  C07D207/48 ,  C07D211/54 ,  C07D211/96 ,  C07F9/38

CPC分类号： C07D211/96 ,  C07D207/48

摘要： The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represent a hydrogen atom or a linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero form, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl radical containing up to 8 carbon atoms or an aryl radical containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with a radical R'.sub.1, R'.sub.1 having one of the definitions stated above for R.sub.1, and n represents the number 1 or number 2, to a process for the preparation thereof, to their application as medicinal products and to compositions containing them.

摘要翻译： 本发明涉及式（I）的产物，其中R表示基团“IMAGE”，其中苯环上任何位置的R 1表示直链，支链或环状的含有至多8个碳的烷基，烯基或炔基 原子或其中可以相同或不同的R 2和R 3表示氢原子或含有至多8个碳原子的直链烷基，烯基或炔基或与其形成氮原子的基团“IMAGE” 或含有至多8个碳原子的直链，支链或环状烷基或含有至多14个碳原子的芳基的基团OR'，R'表示氢，或含有至多14个碳原子的芳基，或 基团SR4或S（O）R5，R4和R5表示直链，支链或环状的含有至多8个碳原子的烷基，烯基或炔基，或R表示任选被R 1'，R' 的定义ab 对于R1，n代表数字1或数2，其制备方法，作为药用产品和含有它们的组合物的应用。

公开(公告)号：US4990531A

公开(公告)日：1991-02-05

申请号：US315170

申请日：1989-02-24

申请人： Giulio Galliani ,  Fernando Barzaghi ,  Michel Fortin ,  Carlo Gorini ,  Emilio Toja

发明人： Giulio Galliani ,  Fernando Barzaghi ,  Michel Fortin ,  Carlo Gorini ,  Emilio Toja

IPC分类号： C07D207/263 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/495 ,  A61K31/535 ,  A61P25/02 ,  C07D207/27 ,  C07D207/48 ,  C07D401/12

CPC分类号： C07D207/48

摘要： Compounds useful for the treatment of patients suffering from muscle spasms of the formula (I) ##STR1## in which R represents the radical ##STR2## in which R.sub.1, in any position on the phenyl nucleus, represents a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, identical or different each represents a hydrogen atom, a linear alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or form together with the nitrogen atom to which they are joined, a heterocyclic radical optionally containing another heteroatom, or NO.sub.2, or OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms, or aryl containing up to 14 carbon atoms, or an SR.sub.4 or S(O)R.sub.5 radical, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl, containing up to 8 carbon atoms, or R represents naphthyl, optionally substituted by an R.sub.1 radical, as defined above; also therapeutic compositions containing the same and method of use.

摘要翻译： 可用于治疗患有式（I）的肌肉痉挛的患者的化合物（I）其中R表示基团“IMAGE”，其中在苯基核上任何位置的R 1表示直链，支链或 含有至多8个碳原子的环烷基，烯基或炔基，或其中R 2和R 3相同或不同各自表示氢原子，直链烷基，烯基或炔基，其含有至多8个碳原子的基团， 或与其连接的氮原子一起形成任选地含有另外的杂原子的杂环基团，或代表氢的NO 2或OR'，R'，含有至多8个碳原子的直链，支链或环状烷基，或含有 至多14个碳原子，或SR4或S（O）R5基团，R4和R5代表含有至多8个碳原子的直链，支链或环状烷基，烯基或炔基，或R代表萘基，任选被R1 如上所述; 还含有相同的治疗组合物和使用方法。

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：US4885307A

公开(公告)日：1989-12-05

申请号：US205958

申请日：1988-06-13

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

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

IPC分类号： A61K31/40 ,  A61P25/18 ,  C07D207/48

CPC分类号： 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, a 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 thereapeutic compositions containing those compounds and method of use.

摘要翻译： 用于治疗患有智力或神经失调，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，其含有至多 8个碳原子，含有2至8个碳原子的链烯基，含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表示可含有至多14个碳原子的芳基，或单环或多环 杂环芳族基团，可能被取代; 还含有这些化合物和使用方法的治疗组合物。

公开(公告)号：US4885306A

公开(公告)日：1989-12-05

申请号：US203740

申请日：1988-06-02

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

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

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

CPC分类号： 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' and R.sub.2, being identical or different, represent hydrogen, a 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, R.sub.1 represents a possibly substituted aryl containing up to 14 carbon atoms, or a possibly substituted mono- or polycyclic heterocyclic aromatic radical; also therapeutic compositions containing those compounds and method of use.

摘要翻译： 用于治疗患有智力或神经失调，记忆障碍，衰老或精神紧张的患者（I）的患者的化合物，其中R 1和R 2相同或不同，代表氢，直链，支链或 含有至多8个碳原子的环状烷基，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 1表示可能被取代的含有至多14个碳原子的芳基，或 可能取代的单环或多环杂环芳族基团; 还含有这些化合物和使用方法的治疗组合物。

公开(公告)号：US5041436A

公开(公告)日：1991-08-20

申请号：US482806

申请日：1990-02-21

申请人： Emilio Toja ,  Fernando Barzaghi ,  Giulio Galliani

发明人： Emilio Toja ,  Fernando Barzaghi ,  Giulio Galliani

IPC分类号： C07D211/76 ,  A61K31/445 ,  A61K31/55 ,  A61P25/02 ,  C07D211/32 ,  C07D211/96

CPC分类号： C07D211/96

摘要： The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represents hydrogen or linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero atom, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms or aryl containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing linear, branched or cyclic alkyl, alkenyl, or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with the radical R'.sub.1, R'.sub.1 being as defined above for R.sub.1, to a process and intermediates for the preparation thereof, to their application as medicinal products and to compositions containing them.

摘要翻译： 本发明涉及式（I）的产物，其中R表示基团，其中苯环上任何位置的R 1表示直链，支链或环烷基，含有至多8个碳原子的烷基，烯基或炔基 或者其中可以相同或不同的R 2和R 3表示氢或含有至多8个碳原子的直链烷基，烯基或炔基或与它们所连接的氮原子一起形成的基团 或任选含有另一个杂原子的碳质杂环基，或代表氢的基团OR'，R'，含有至多8个碳原子的直链，支链或环状烷基或含有至多14个碳原子的芳基，或基团SR4或S（O ）R 5，R 4和R 5表示直链，支链或环状的含有至多8个碳原子的烷基，烯基或炔基，或R表示任选被R 1'，R''如上面对R 1所定义的基团取代的萘基， 过程和中间体 他的准备，作为药用产品和含有它们的组合物的应用。

公开(公告)号：US4948804A

公开(公告)日：1990-08-14

申请号：US211287

申请日：1988-06-24

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

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

IPC分类号： C07D413/06 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/4025 ,  A61K31/42 ,  A61K31/425 ,  A61P25/18 ,  A61P25/28 ,  A61P43/00 ,  C07D207/26 ,  C07D207/273 ,  C07D409/06 ,  C07D411/06

CPC分类号： C07D207/273

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 12 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, optionally substituted, or a mono- or polycryclic heterocyclic aromatic radical, optionally substituted; also therapeutic compositions containing those compounds and method of use.

摘要翻译： 用于治疗患有智力或神经失调，记忆障碍，衰老或精神紧张的患者（I）的患者的化合物：其中R'表示氢，直链，支链或环状烷基，其包含至多 12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表示含有至多14个碳原子的芳基，任选取代的，或单或多个 杂环芳族基，任选取代; 还含有这些化合物和使用方法的治疗组合物。

公开(公告)号：US4829079A

公开(公告)日：1989-05-09

申请号：US947270

申请日：1986-12-29

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

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

IPC分类号： C07D333/00 ,  A61K20060101 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P25/28 ,  C07D207/26 ,  C07D207/273 ,  C07D207/48 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D401/12 ,  C07D207/48 ,  C07D405/12 ,  C07D409/12

摘要： Memory enhancing 1-(benzenesulfonyl)-2-oxo-5-alkoxy-pyrrolidines are prepared by alkylation of the corresponding pyrrolidones or pyrrolidone precursors.

摘要翻译： 通过相应的吡咯烷酮或吡咯烷酮前体的烷基化制备记忆增强1-（苯磺酰基）-2-氧代-5-烷氧基 - 吡咯烷。