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公开(公告)号:US4407801A
公开(公告)日:1983-10-04
申请号:US306224
申请日:1981-09-28
IPC分类号: A61K9/20 , A61K31/495 , A61K31/70
CPC分类号: A61K9/2018 , A61K31/495 , A61K9/2059
摘要: The subject of the invention is a novel pharmaceutical composition, especially having an anti-ischaemic action, containing, in combination, a high dosage (within the range of from 20 to 80 mg) of the dihydrochloride (or another mineral or organic salt) of 1-(2,3,4-trimethoxybenzyl)piperazine and a disintegrating agent, such as mannitol or sodium carboxymethyl starch, that has the effect of liberating the salt of 1-(2,3,4-trimethoxybenzyl)piperazine virtually instantaneously in the organism, this composition being, furthermore, advantageously enclosed in a thin coating film or held together by a binder that is itself readily disintegrated in situ in the organism in such a manner that it makes possible a "flash" action, that is to say a virtually instantaneous action, of the above-mentioned salt in situ. This composition is administered to the patient at a dosage of from 20 to 80 mg/day.
摘要翻译: 本发明的主题是特别是具有抗缺血作用的新型药物组合物,其组合含有二盐酸盐(或另一种矿物或有机盐)的高剂量(在20至80mg范围内) 1-(2,3,4-三甲氧基苄基)哌嗪和崩解剂,如甘露糖醇或羧甲基淀粉钠,其实际上可以瞬间释放1-(2,3,4-三甲氧基苄基)哌嗪的盐 此外,该组合物还有利地封闭在薄的涂膜中或通过粘合剂保持在一起,所述粘合剂本身容易在生物体中原位分解,使得可能发生“闪光”作用,也就是说 几乎瞬间作用,上述盐原位。 将该组合物以20至80mg /天的剂量施用于患者。
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公开(公告)号:US5332735A
公开(公告)日:1994-07-26
申请号:US792238
申请日:1991-11-14
申请人: Sylvain Rault , Marie P. Foloppe , Max Robba , Michel Boulouard , Pierre Renard , Michelle Devissaguet , Gerard Adam
发明人: Sylvain Rault , Marie P. Foloppe , Max Robba , Michel Boulouard , Pierre Renard , Michelle Devissaguet , Gerard Adam
IPC分类号: A61K31/40 , A61K31/401 , A61P9/00 , A61P9/10 , A61P25/28 , C07D207/08 , C07D207/16 , C07D207/24 , C07D405/06 , C07D491/08 , C07D207/12
CPC分类号: C07D207/08 , C07D207/24 , C07D405/06 , C07D491/08
摘要: Compounds of the general formula (I): ##STR1## where A, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are defined in the description.Medicinal products.
摘要翻译: 通式(I)的化合物:其中A,R 1,R 2,R 3,R 4,R 5和R 6在说明书中定义。 药用产品。
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公开(公告)号:US5190939A
公开(公告)日:1993-03-02
申请号:US665812
申请日:1991-03-07
申请人: Sylvain Rault , Michel Boulouard , Patrick Dallemagne , Max Robba , Beatrice Guardiola , Michelle Devissaguet
发明人: Sylvain Rault , Michel Boulouard , Patrick Dallemagne , Max Robba , Beatrice Guardiola , Michelle Devissaguet
IPC分类号: A61K31/55 , A61P1/00 , A61P1/04 , A61P3/06 , A61P9/10 , A61P25/00 , A61P25/18 , A61P25/28 , C07D495/14 , C07D498/22
CPC分类号: C07D495/14
摘要: The invention relates to compounds of general formula I: ##STR1## in which: R.sub.1 represents a radical of general formula (Z.sub.0), (Z.sub.1), (Z.sub.2), (Z.sub.3) or (Z.sub.4) ##STR2## R.sub.2 represents a methylene radical, a hydroxymethylene radical, a carbonyl radical or a radical of general formula (Y.sub.1), (Y.sub.2), (Y.sub.3) or (Y.sub.4): ##STR3## or, with R.sub.12 and the nitrogen atom to which they are attached, forms a radical of general formula (W): ##STR4## R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10, R.sub.11, R.sub.12 and n being as defined in the description, medicinal products containing the same and a method-of-treating metabolic ailments therewith.
摘要翻译: 本发明涉及通式I的化合物:其中:R1表示通式(ZO),(Z1),(Z2),(Z3)或(Z4)的基团(Z0) (Z 1)(Z 3)(Z 3)(Z 3)(Z 3)(Z 4)R 2表示亚甲基,羟基亚甲基,羰基或通式(Y1) (Y3)或(Y4):(Y1)(Y1)
(Y2) (Y3) (Y4)或与R12及其相连的氮原子形成 通式(W)的基团:其中R 3,R 4,R 5,R 6,R 7,R 8,R 9,R 10,R 11,R 12和n如说明书中所定义, 治疗代谢疾病。 -
公开(公告)号:US5254548A
公开(公告)日:1993-10-19
申请号:US820512
申请日:1992-01-14
申请人: Camille-Georges Wermuth , Jean-Jacques Bourguignon , Isabelle Morin , Pierre Renard , Michelle Devissaguet , Jean-Francois R. de La Faverie , Gerard Adam
发明人: Camille-Georges Wermuth , Jean-Jacques Bourguignon , Isabelle Morin , Pierre Renard , Michelle Devissaguet , Jean-Francois R. de La Faverie , Gerard Adam
IPC分类号: A61K31/53 , A61P25/00 , A61P25/04 , C07D253/06 , C07D253/07 , C07D401/06 , C07D403/04 , C07D487/04 , C07D253/065
CPC分类号: C07D487/04 , C07D253/07 , C07D403/04
摘要: A compound having an aryltriazine structure selected from those of formula (I): ##STR1## for which the meaning of the substituents Ar, R.sub.1, R.sub.5, R.sub.6, and R.sub.6 ' is given in the description.The compound of the invention is useful as medicinal product for disorders associated with a cholinergic dysfunction.
摘要翻译: 具有选自式(I)的芳基三嗪结构的化合物:其中在说明书中给出了取代基Ar,R 1,R 5,R 6和R 6'的含义的式(I)化合物。 本发明的化合物可用作与胆碱能功能障碍相关的疾病的药物产品。
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公开(公告)号:US5147883A
公开(公告)日:1992-09-15
申请号:US708515
申请日:1991-05-31
申请人: Hocine Aichaioui , Daniel Lesieur , Charles Lespagnol , Michelle Devissaguet , Beatrice Guardiola
发明人: Hocine Aichaioui , Daniel Lesieur , Charles Lespagnol , Michelle Devissaguet , Beatrice Guardiola
IPC分类号: A61K31/42 , A61K31/423 , A61K31/44 , A61K31/455 , A61K31/47 , A61P7/02 , A61P9/08 , A61P9/10 , C07D263/52 , C07D263/58 , C07D263/60 , C07D263/62 , C07D413/06
CPC分类号: C07D263/52 , C07D263/58 , C07D263/60 , C07D413/06
摘要: Compounds of general formula (I): ##STR1## in which: R.sub.1 represents a hydrogen atom or a lower alkyl group,A represents a hydrogen atom, and in this case B represents a group CO-G, G being:either a heteroaryl group selected from furan, indole, pyrrole, pyridine, quinoline, isoquinoline and benzofuran, optionally substituted with one or more lower alkyl or lower alkoxy groups or a halogen atoms,or a linear or branched lower alkyl group substituted with a carboxyl group,or a linear or branched lower alkenyl group substituted with a carboxyl group,or a phenyl or naphthyl group substituted with a carboxyl group,or alternatively A forms with B a group CO(CH.sub.2).sub.n CH(CH.sub.3) with n being a integer equal to 1, 2, 3 or 4, the CO group being attached to the aromatic ring of the benzoxazolinone at the 5- or 6-position,as well as, where appropriate, their isomers and, when the compound of formula (I) possesses a carboxylic acid group, their addition salts with a pharmaceutically acceptable base, and, when the compound of formula (I) contains a basic group, their addition salts with a pharmaceutically acceptable acid, it being understood that lower alkyl and lower alkenyl mean linear or branched groups comprising from 1 to 6 carbon atoms.Medicinal products.
摘要翻译: 通式(I)的化合物:其中:R1表示氢原子或低级烷基,A表示氢原子,在这种情况下,B表示CO-G基团,G表示: 选自呋喃,吲哚,吡咯,吡啶,喹啉,异喹啉和苯并呋喃的杂芳基,任选被一个或多个低级烷基或低级烷氧基或卤素原子取代,或被羧基取代的直链或支链低级烷基, 或被羧基取代的直链或支链的低级链烯基或被羧基取代的苯基或萘基,或者与B a基团CO(CH 2)n CH(CH 3)形成A,其中n为等于1的整数 ,2,3或4,所述CO基团在5-或6-位连接于苯并恶唑啉酮的芳环,并且在适当的情况下连接其异构体,并且当式(I)化合物具有羧酸 酸基,它们与药学上可接受的碱的加成盐 并且当式(I)化合物含有碱性基团时,其与药学上可接受的酸的加成盐,应理解为低级烷基和低级烯基表示包含1至6个碳原子的直链或支链基团。 药用产品。
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公开(公告)号:US5130301A
公开(公告)日:1992-07-14
申请号:US675420
申请日:1991-03-26
CPC分类号: C07D495/14
摘要: Novel 4H-pyrrolo[1,2-a]thieno[2,3-f][1,4]diazepine which are usable as a medicinal product and correspond to the general formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and R.sub.4 have the same meaning as given in the specification.These compounds, as well as their physiologically tolerable salts, may be used in therapy, in particular in the treatment of disorders linked to hypoxemia and to certain metabolic disorders.
摘要翻译: 可用作药用产物并对应于通式(I)的新颖的4H-吡咯并[1,2-a]噻吩并[2,3-f] [1,4]二氮杂:其中 :R1,R2,R3和R4与本说明书中的含义相同。 这些化合物及其生理上可耐受的盐可用于治疗,特别是用于治疗与低氧血症和某些代谢紊乱相关的疾病。
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公开(公告)号:US5242923A
公开(公告)日:1993-09-07
申请号:US839819
申请日:1992-02-21
申请人: Gerald Guillaumet , Christine Flouzat , Michelle Devissaguet , Pierre Renard , Daniel H. Caignard , Gerard Adam
发明人: Gerald Guillaumet , Christine Flouzat , Michelle Devissaguet , Pierre Renard , Daniel H. Caignard , Gerard Adam
IPC分类号: C07D213/74 , C07D498/04
CPC分类号: C07D213/74
摘要: The invention relates to the compounds of general formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3, R.sub.4, A, Z and m are as defined in the description, their isomers, epimers and diastereoisomers,their addition salts with a pharmaceutically acceptable acid and, when R1 and R.sub.2 each represent a hydrogen atom, their addition salts with a pharmaceutically acceptable base.
摘要翻译: 本发明涉及通式(I)的化合物:其中:R1,R2,R3,R4,A,Z和m如说明书中所定义,它们的异构体,差向异构体和非对映异构体,其加成盐与 药学上可接受的酸,并且当R 1和R 2各自表示氢原子时,它们与药学上可接受的碱的加成盐。
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公开(公告)号:US5190960A
公开(公告)日:1993-03-02
申请号:US791261
申请日:1991-11-12
申请人: Gerald Guillaumet , Christine Flouzat , Daniel H. Caignard , Pierre Renard , Michelle Devissaguet , Beatrice Guardiola
发明人: Gerald Guillaumet , Christine Flouzat , Daniel H. Caignard , Pierre Renard , Michelle Devissaguet , Beatrice Guardiola
IPC分类号: C07D213/74 , C07D498/04
CPC分类号: C07D213/74
摘要: Compounds of general formula (I): ##STR1## in which: R.sub.1 and R.sub.2 each represent a hydrogen atom or, with the nitrogen and oxygen which bear them, form an --O--CO--N link,W represents a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as trifluoromethyl, and m being between 0 and 3,A is a linear or branched alkyl radical comprising from 1 to 6 carbon atoms,R.sub.3 and R.sub.4 are defined in the description.
摘要翻译: 通式(I)的化合物:其中:R 1和R 2各自表示氢原子,或者与含有它们的氮和氧形成-O-CO-N键,W表示卤素 原子或任选被一个或多个卤素原子取代的低级烷基或烷氧基,例如三氟甲基,m在0和3之间,A是包含1至6个碳原子的直链或支链烷基,R3和R4被定义 在说明中。
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公开(公告)号:US5179091A
公开(公告)日:1993-01-12
申请号:US709613
申请日:1991-06-03
申请人: Daniel Lesieur , Daniel H. Caignard , Isabelle Lesieur , Michelle Devissaguet , Beatrice Guardiola
发明人: Daniel Lesieur , Daniel H. Caignard , Isabelle Lesieur , Michelle Devissaguet , Beatrice Guardiola
IPC分类号: A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/535 , A61K31/536 , A61K31/5377 , A61K31/538 , A61K31/54 , A61K31/5415 , A61P3/06 , A61P3/08 , A61P3/10 , A61P7/02 , A61P29/00 , C07D263/52 , C07D263/58 , C07D263/60 , C07D263/62 , C07D265/18 , C07D265/36 , C07D277/60 , C07D277/68 , C07D279/08 , C07D279/16 , C07D413/04 , C07D417/04
CPC分类号: C07D263/52 , C07D263/58 , C07D263/60 , C07D265/36 , C07D279/16
摘要: Compounds of general formula (I): in which: ##STR1## R.sub.1, X, Y, Z, T, R.sub.2, R.sub.3 and R.sub.4 are defined in the description. Medicinal products.
摘要翻译: 通式(I)的化合物:其中:(I)R 1,X,Y,Z,T,R 2,R 3和R 4在说明书中定义。 药用产品。
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公开(公告)号:US5155116A
公开(公告)日:1992-10-13
申请号:US711297
申请日:1991-06-06
申请人: Gerald Guillaumet , Christine Flouzat , Daniel H. Caignard , Pierre Renard , Michelle Devissaguet , Beatrice Guardiola
发明人: Gerald Guillaumet , Christine Flouzat , Daniel H. Caignard , Pierre Renard , Michelle Devissaguet , Beatrice Guardiola
IPC分类号: A61K31/44 , A61P9/00 , A61P25/04 , A61P25/28 , C07D213/74 , C07D498/04
CPC分类号: C07D213/74
摘要: Compounds of general formula (I): ##STR1## in which: R.sub.1 and R.sub.2 each represent a hydrogen atom or, with the nitrogen and oxygen which bear them, form an --O--CO--N link,W represents a halogen atom or a lower alkyl or alkoxy group optionally substituted with one or more halogen atoms, such as trifluoromethyl, and m being between 0 and 3,A is a linear or branched alkyl radical comprising from 1 to 6 carbon atoms,R.sub.3 and R.sub.4 are defined in the description have medicinal properties.
摘要翻译: 通式(I)的化合物:其中:R 1和R 2各自表示氢原子,或者与含有它们的氮和氧形成-O-CO-N键,W表示卤素 原子或任选被一个或多个卤素原子取代的低级烷基或烷氧基,例如三氟甲基,m在0和3之间,A是包含1至6个碳原子的直链或支链烷基,R3和R4被定义 在说明书中具有药用性质。
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