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1. 发明授权

US4340607A Antimicrobial 3H-naphtho[1,2-d]imidazoles 失效
标题翻译：抗微生物3H-萘并[1,2-d]咪唑
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。

2. 发明授权

US4435417A Antiinflammatory 3H-naphtho[1,2-d]imidazoles 失效
标题翻译：抗炎3H-萘并[1,2-d]咪唑
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。

3. 发明授权

US5204479A Derivatives of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde oxime 失效
标题翻译： 1,2,5,6-四氢吡啶-3-羧甲醛氧化物的衍生物
公开(公告)号：US5204479A
公开(公告)日：1993-04-20
申请号：US699631
申请日：1991-05-15
申请人： Emilio Toja , Carla Bonetti , Fernando Barzaghi , Giulio Galliani
发明人： Emilio Toja , Carla Bonetti , Fernando Barzaghi , Giulio Galliani
IPC分类号： A61K31/445 , A61K31/00 , A61K31/4465 , A61P25/28 , C07D211/70
CPC分类号： C07D211/70
摘要： The subject of the invention is the compounds of formula (I): ##STR1## in which: R represents a hydrogen atom, a saturated or unsaturated, linear, branched or cyclic alkyl radical containing up to 8 carbon atoms,R' represents an amine-containing moiety of an .alpha.-amino acid or a peptide, containing as an end group an amine-containing moiety of an .alpha.-amino acid as well as their addition salts with organic or mineral acids.The compounds of formula (I) have useful pharmacological properties which justify their use in therapeutics.
摘要翻译：本发明的主题是式（I）的化合物：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，R' 代表α-氨基酸或肽的含胺部分，其含有作为端基的α-氨基酸的含胺部分以及它们与有机或无机酸的加成盐。式（I）化合物具有有用的药理学性质，其证明其在治疗中的用途。

4. 发明授权

US4921868A Carbamate derivatives of the oxime of 1,2,5,6-tetrahydropyridin-3-carboxaldehyde, their use as medicaments and compositions containing them 失效
标题翻译： 1,2,5,6-四氢吡啶-3-甲醛的肟的氨基甲酸酯衍生物，它们作为药物和含有它们的组合物的用途
公开(公告)号：US4921868A
公开(公告)日：1990-05-01
申请号：US234632
申请日：1988-08-22
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 , A61K31/44 , A61K31/4412 , A61P25/02 , A61P25/28 , A61P43/00 , 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.
摘要翻译：用于治疗患有老年性痴呆，阿尔茨海默氏病或记忆缺陷的患者，其中R'代表氢，直链，支链或环状的烷基，烯基或炔基，其中含有至多 8个碳原子，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，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，可能取代的，以及它们与有机或无机酸的加成盐。

5. 发明授权

US4885307A Derivatives of 1-arylsulphonyl-1,5-dihydro-2H-pyrrol-2-one, and compositions containing them 失效
标题翻译： 1-芳基磺酰基-1,5-二氢-2H-吡咯-2-酮的衍生物和含有它们的组合物
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。

6. 发明授权

US4885306A Derivatives of 1-arylsulphonyl-2-oxo-5-alkoxy-pyrrolidine and medical compositions containing them 失效
标题翻译： 1-芳基磺酰基-2-氧代-5-烷氧基 - 吡咯烷的衍生物和含有它们的医药组合物
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。

7. 发明授权

US5204341A 1-arylsulphonyl-2-pyrrolidone derivatives, their preparation process and the new intermediates obtained, their use as medicaments and the pharmaceutical compositions containing them 失效
标题翻译： 1-ARYLSULPHONYL-2-吡咯烷酮衍生物，其制备方法和获得的新的中间体，它们作为药物和含有它们的药物组合物使用
公开(公告)号：US5204341A
公开(公告)日：1993-04-20
申请号：US805694
申请日：1991-12-11
申请人： Emilio Toja , Carla Bonetti , Fernando Barzaghi , Giulio Galliani
发明人： Emilio Toja , Carla Bonetti , Fernando Barzaghi , Giulio Galliani
IPC分类号： A61K31/40 , A61K31/4015 , A61P25/02 , C07C311/39 , C07C311/42 , C07D207/24 , C07D207/273 , C07D207/48 , C07D401/12 , C07F9/572
CPC分类号： C07D401/12 , C07C311/39 , C07D207/48 , C07F9/5725
摘要： 1-arylsulphonyl-2-pyrrolidone derivatives for treating spasmodic disorders in gastro-enterology, in gynaecology, in obstetrics, in urology; intermediates in the preparation of such products; methods for preparing such products and pharmaceutical preparations containing such products.
摘要翻译： 1-芳基磺酰基-2-吡咯烷酮衍生物，用于治疗胃肠学，妇科，妇产科，泌尿科的痉挛性疾病; 中间体在制备此类产品时; 制备此类产品的方法和含有此类产品的药物制剂。

8. 发明授权

US5037822A 1-arylsulphonyl-2-pyrrolidinethione or 1-arylsulphonyl-2-piperidinethione derivatives, process for the preparation thereof their application as medicinal products and compositions containing them 失效
标题翻译： 1-芳基磺酰基-2-吡咯烷硫酮或1-芳基磺酰基-2-哌啶硫酮衍生物，其制备方法作为药用产品和含有它们的组合物
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。

9. 发明授权

US5015655A 1-azabicycloalkane derivatives, their preparation process and their use as medicaments 失效
标题翻译： 1-氮杂双环链烷烃衍生物，其制备方法及其作为药物的用途
公开(公告)号：US5015655A
公开(公告)日：1991-05-14
申请号：US426778
申请日：1989-10-26
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： A61K31/40 , A61K31/435 , A61K31/55 , A61P25/02 , A61P25/28 , C07D453/02 , C07D471/08 , C07D487/08
CPC分类号： C07D487/08 , C07D453/02
摘要： Compounds useful in the treatment of Alzheimers's disease, senile dementia or memory disorders of the aged of the formula ##STR1## in which n represents the number 1, 2 or 3,R.sub.1 and R.sub.2, identical or different, represent hydrogen, a linear, branched or cyclic alkyl, alkenyl, or alkynyl which contain up to 6 carbon atoms, R.sub.1 and R.sub.2 optionally substituted by hydroxy, alkoxy containing up to 6 carbon atoms, aralkyl containing up to 14 carbon atoms, a COOalk.sub.1 radical in which alk.sub.1 represents alkyl containing up to 6 carbon atoms, a --CON(alk.sub.2).sub.2 radical in which alk.sub.2 represents alkyl containing up to 6 carbon the radical --C(R.sub.1).dbd.NOR.sub.2 being in position 2, 3 or 4, in all their isomer forms and their mixture, as well as their addition salts with pharmaceutically acceptable organic or mineral acids. Also therapeutic compositions containing the compounds, method of treatment and method of preparation.
摘要翻译：用于治疗阿尔茨海默病，老年痴呆或老年化记忆障碍的化合物，其中n表示数字1,2或3，R 1和R 2相同或不同，表示氢，a 含有至多6个碳原子的直链，支链或环状烷基，烯基或炔基，任选被羟基取代的R 1和R 2，含有至多6个碳原子的烷氧基，含有至多14个碳原子的芳烷基，其中alk1代表含有至多6个碳原子的烷基，-CON（alk2）2基团，其中alk2表示含有至多6个碳的烷基，基团-C（R 1）= NOR 2位于2,3或4位，全部为其异构体形式，它们的混合物，以及它们与药学上可接受的有机或无机酸的加成盐。还含有该化合物的治疗组合物，治疗方法和制备方法。

10. 发明授权

US4990531A Derivatives of 1-arylsulphonyl-2-pyrrolidinone and their use as medicaments 失效
标题翻译： 1-芳基磺酰基-2-吡咯烷酮的衍生物及其作为药物的用途
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。

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