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。

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：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。

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：US4459302A

公开(公告)日：1984-07-10

申请号：US87375

申请日：1979-10-23

申请人： Amedeo Omodei-Sale ,  Pietro Consonni ,  Giulio Galliani

发明人： Amedeo Omodei-Sale ,  Pietro Consonni ,  Giulio Galliani

IPC分类号： A61K31/41 ,  C07D233/54 ,  C07D249/08 ,  C07D249/12 ,  C07D405/04

CPC分类号： C07D233/64 ,  C07D233/54 ,  C07D249/08 ,  Y10S514/841

摘要： New acyl-1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy;a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenacyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluoromethyl, phenyl, halo and dimethylamino;R.sub.2 may represent a (C.sub.1-4)alkyl radical or the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also represent a methylenedioxy group; with the proviso that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.5 -CO or the group R.sub.6 -SO.sub.2 wherein R.sub.5 and R.sub.6 are as above defined;and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.

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。

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。

公开(公告)号：US4888350A

公开(公告)日：1989-12-19

申请号：US915119

申请日：1986-10-03

申请人： Amedeo Omodei-Sale' ,  Pietro Consonni ,  Giulio Galliani

发明人： Amedeo Omodei-Sale' ,  Pietro Consonni ,  Giulio Galliani

IPC分类号： C07D233/54 ,  C07D249/08

CPC分类号： C07D233/64 ,  C07D233/54 ,  C07D249/08

摘要： New acyl -1H-1,2,4-triazole derivatives of the formula ##STR1## wherein R may be located on one of the two adjacent nitrogen atoms and may represent hydrogen; a group R.sub.5 -CO wherein R.sub.5 is selected from (C.sub.1-4)alkyl, (C.sub.2-4)alkenyl, (C.sub.2-4)alkynyl, phenyl, phenyl substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylenedioxy, benzyl, cinnamyl, amino, (C.sub.1-4)alkylamino, di-(C.sub.1 -C.sub.4)alkylamino, phenylamino, phenylamino wherein the phenyl ring may be substituted by one to three groups independently selected from halo, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, trifluoromethyl, cyano, nitro, amino, di-(C.sub.1-4)alkylamino, (C.sub.2-4)acylamino and methylendioxy, halo(C.sub.1-4)alkyl, (C.sub.1-4)alkoxy and benzyloxy; a group R.sub.6 -SO.sub.2 wherein R.sub.6 may represent (C.sub.1-4)alkyl, phenyl, phenyl substituted by a radical selected from (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy, or phenactyl;R.sub.1 is selected from hydrogen, (C.sub.1-4)alkyl, (C.sub.1-4)alkoxy, allyloxy, propargyloxy, trifluormethyl, phenyl, halo and dimethylamino;R.sub.2 may represent the group ##STR2## wherein R.sub.7 is hydrogen or methyl and R.sub.8 is a (C.sub.1-4)alkyl radical, the group R.sub.5.sup.--CO or the group R.sub.6.sup.-- SO.sub.2 in which R.sub.5 and R.sub.6 are defined as above, or R.sub.7 and R.sub.8 taken together may represent a further bond between the carbon and oxygen atom;R.sub.3 and R.sub.4 are independently selected from hydrogen, halo, (C.sub.1-4)alkyl and (C.sub.1-4)alkoxy;R.sub.1 and R.sub.4 taken together may also repesent a methylenedioxy group; with the provison that, when R represents hydrogen, R.sub.2 must be the group ##STR3## in which R.sub.8 must be the group R.sub.6.sup.--SO.sub.2 wherein R.sub.6 is as above defined; and salts therewith of pharmaceutically acceptable acids. The compounds possess antireproductive utility.

摘要翻译： 式Ⅰ的新的酰基-1H-1,2,4-三唑衍生物，其中R可以位于两个相邻的氮原子之一上并且可以代表氢; 其中R 5选自（C 1-4）烷基，（C 2-4）烯基，（C 2-4）炔基，苯基，被一至三个独立地选自卤素，（C 1-4） 烷基，（C 1-4）烷氧基，三氟甲基，氰基，硝基，氨基，二 - （C 1-4）烷基氨基，（C 2-4）酰氨基和亚甲二氧基，苄基，肉桂基，氨基，（C 1-4）烷基氨基， （C 1 -C 4）烷基氨基，苯基氨基，苯基氨基，其中苯环可以被一至三个独立地选自卤素，（C 1-4）烷基，（C 1-4）烷氧基，三氟甲基，氰基，硝基，氨基，二 - （C 1-4）烷基氨基，（C 2-4）酰氨基和甲基二氧基，卤代（C 1-4）烷基，（C 1-4）烷氧基和苄氧基; 基团R6-SO2，其中R6可以表示（C1-4）烷基，苯基，被选自（C1-4）烷基和（C1-4）烷氧基的基团取代的苯基或苯甲酰基; R 1选自氢，（C 1-4）烷基，（C 1-4）烷氧基，烯丙氧基，炔丙氧基，三氟甲基，苯基，卤素和二甲基氨基; R 2可以表示基团，其中R 7是氢或甲基，R 8是（C 1-4）烷基，R 5 -CO或其中R 5和R 6如上所定义的基团R 6 -SO 2，或R 7和 一起可以代表碳和氧原子之间的另一个键; R 3和R 4独立地选自氢，卤素，（C 1-4）烷基和（C 1-4）烷氧基; R 1和R 4一起也可以代替亚甲二氧基; 当R表示氢时，R2必须是其中R8必须是R6-SO2的基团，其中R6如上所定义; 以及其与药学上可接受的酸的盐。 该化合物具有抗生素效用。

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。