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    1H, 3H-pyrrolo (1,2-C) thiazole derivatives and pharmaceutical compositions
    2.
    发明授权
    1H, 3H-pyrrolo (1,2-C) thiazole derivatives and pharmaceutical compositions 失效
    1H，3H-吡咯（1,2-C）噻唑衍生物和药物组合物

    公开(公告)号：US4786645A

    公开(公告)日：1988-11-22

    申请号：US69211

    申请日：1987-07-02

    申请人： Jean-Louis Fabre ,  Claude James ,  Daniel Lave

    发明人： Jean-Louis Fabre ,  Claude James ,  Daniel Lave

    IPC分类号： A61K31/50 ,  A61K31/44 ,  A61K31/47 ,  A61P7/02 ,  A61P29/00 ,  C07D513/04 ,  C07D417/14

    CPC分类号： C07D513/04

    摘要： A compound of the general formula I: ##STR1## in which Ar is a pyridyl, quinolinyl, isoquinolinyl, naphthyridinyl, pyrimidyl, quinazolinyl, thiazolyl, benzothiazolyl, imidazolyl, benzimidazolyl, oxazolyl, benzoxazolyl, thienyl, benzothienyl or naphthyl group; optionally substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, alkylcarbonyl, benzoyl, alkyloxycarbonyl, carboxy, phenoxycarbonyl, alkylcabonyloxy, benzoyloxy, alkylcarbonylamino, benzamido, phenyl, benzyl, phenoxy or phenylthio group, provided that (i) when Ar is a pyridyl group, the pyridyl group must be substituted, (ii) an alkyl moiety contains 1 to 4 straight- or branched chain carbon atoms; (iii) a phenyl moiety may be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, phenyl or benzyl groupin separate enantiomeric form or mixtures thereof, or a pharmaceutically acceptable salt thereof is useful in the treatment of all pathological conditions in which PAF-acether may be implicated directly or indirectly.

    摘要翻译： 其中Ar是吡啶基，喹啉基，异喹啉基，萘啶基，嘧啶基，喹唑啉基，噻唑基，苯并噻唑基，咪唑基，苯并咪唑基，恶唑基，苯并恶唑基，噻吩基，苯并噻吩基或萘基的通式I的化合物：其中Ar是吡啶基， 烷基氨基，烷基磺酰基，磺酰氨基，烷基亚磺酰氨基，二烷基磺酰氨基，烷基羰基，苯甲酰基，烷氧基羰基，羧基，苯氧基羰基，烷基羰基氧基，苯甲酰氧基， 烷基羰基氨基，苯甲酰氨基，苯基，苄基，苯氧基或苯硫基，条件是（ⅰ）当Ar是吡啶基时，吡啶基必须被取代，（ii）烷基部分含有1-4个直链或支链碳原子; （iii）苯基部分可以是未取代的或被一个或多个分开的对映体形式或其混合物中的一个或多个卤素或烷基，烷氧基，烷硫基，三氟甲基，氨基，烷基氨基，二烷基氨基，羟基，氰基，苯基或苄基 其可接受的盐可用于治疗PAF-乙酰胆碱可直接或间接牵连的所有病理状况。

    1H,3H-pyrrol[1,2-c]thiazole derivatives and pharmaceutical compositions containing them
    3.
    发明授权
    1H,3H-pyrrol[1,2-c]thiazole derivatives and pharmaceutical compositions containing them 失效

    公开(公告)号：US4783472A

    公开(公告)日：1988-11-08

    申请号：US69520

    申请日：1987-07-02

    申请人： Jean-Louis Fabre ,  Claude James ,  Daniel Lave

    发明人： Jean-Louis Fabre ,  Claude James ,  Daniel Lave

    IPC分类号： A61K31/44 ,  A61P7/02 ,  A61P29/00 ,  C07D513/04 ,  C07D409/00 ,  C07D215/04 ,  C07D217/00 ,  C07D401/00

    CPC分类号： C07D513/04

    摘要： A compound of the general formula I; ##STR1## in which R is hydrogen or a halogen or an alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino, benzamido, phenyl, phenoxy or phenylthio group, X is oxygen or sulphur or an imino, alkylimino, phenylimino, benzylimino, sulphinyl, sulphonyl, carbonyl, carbonylmethylene, methylenecarbonyl, carbonylvinylene or vinylenecarbonyl group, or X represents a valency bond or a straight-chain alkylene group containing 1 to 4 carbon atoms and Ar is a phenyl, naphthyl, pyridyl, quinolinyl, isoquinolinyl, thienyl, benzothienyl, thieno[3,2-b]thien-2-yl or thieno[2,3-b]thien-2-yl group, it being possible for the group Ar to be unsubstituted or substituted with one or more halogen or alkyl, alkyloxy, alkylthio, trifluoromethyl, amino, alkylamino, dialkylamino, hydroxy, cyano, carboxy, alkylsulphinyl, alkylsulphonyl, sulphamido, alkylsulphamido, dialkylsulphamido, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, phenylcarbamoyl, diphenylcarbamoyl, pyridylcarbamoyl, dipyridylcarbamoyl, benzyl, alkylcarbonyl, benzoyl, alkyloxycarbonyl, phenoxycarbonyl, alkylcarbonyloxy, benzoyloxy, alkylcarbonylamino or benzamido group;each alkyl moiety containing 1 to 4 straight- or branched-chain carbon atoms; the compound being in separate enantiomeric form or mixtures thereof or a pharmaceutically acceptable salt thereof is useful in the treatment of all the pathological conditions in which PAF-acether may be directly or indirectly implicated.

    Substituted phenyl piperazinyl pyrrolidin-2-ones and related compounds useful as anti-depressants and their use
    4.
    发明授权
    Substituted phenyl piperazinyl pyrrolidin-2-ones and related compounds useful as anti-depressants and their use 失效
    取代的苯基哌嗪基吡咯烷-2-酮和可用作抗抑郁剂的相关化合物及其用途

    公开(公告)号：US4547504A

    公开(公告)日：1985-10-15

    申请号：US558775

    申请日：1983-12-06

    申请人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    发明人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    IPC分类号： C07D401/04 ,  A61K31/40 ,  A61P25/00 ,  C07D207/24 ,  C07D207/26 ,  C07D207/273 ,  C07D295/135 ,  C07D403/04 ,  A61K31/445 ,  A61K31/495

    CPC分类号： C07D207/273 ,  C07D207/24 ,  C07D295/135

    摘要： Pyrrolidine derivatives of the formula: ##STR1## wherein X represents an oxygen or sulphur atom, R represents a hydrogen atom or an alkyl radical, R.sub.o represents a hydrogen atom, an alkyl radical or a phenyl radical optionally substituted by a halogen atom or by an alkyl, alkoxy, alkylthio or nitro radical, A represents a nitrogen atom or a radical .dbd.CH--, the symbol Y represents a hydrogen or halogen atom or an alkyl, alkoxy, alkylthio, alkylcarbonyl, nitro, amino, alkylcarbonylamino, alkylamino, dialkylamino, alkylsulphinyl, alkylsulphonyl, alkoxycarbonyl, cyano, trifluoromethyl, hydroxy, mercapto, alkylcarbonyloxy or alkylcarbonylthio radical, n represents zero or 1, and p represents 1, 2 or 3, it being understood that the alkyl and alkoxy radicals, and alkyl and alkoxy moieties of any of the aforementioned groups, contain from 1 to 4 carbon atoms are new therapeutically useful compounds, more particularly useful as antidepressants.

    摘要翻译： 下式的吡咯烷衍生物：其中X表示氧或硫原子，R表示氢原子或烷基，Ro表示氢原子，烷基或任选被卤素原子取代的苯基，或由 烷基，烷氧基，烷硫基或硝基，A表示氮原子或基团= CH-，符号Y表示氢或卤素原子或烷基，烷氧基，烷硫基，烷基羰基，硝基，氨基，烷基羰基氨基，烷基氨基，二烷基氨基， 烷基亚磺酰基，烷基磺酰基，烷氧基羰基，氰基，三氟甲基，羟基，巯基，烷基羰基氧基或烷基羰基硫基，n表示0或1，p表示1,2或3，应理解烷基和烷氧基，烷基和烷氧基部分 含有1至4个碳原子的任何上述基团是新的治疗上有用的化合物，更特别可用作抗抑郁药。

    Anti-thrombotic ortho-condensed pyrrole derivatives, compositions, and method of use therefor
    5.
    发明授权
    Anti-thrombotic ortho-condensed pyrrole derivatives, compositions, and method of use therefor 失效

    公开(公告)号：US4684658A

    公开(公告)日：1987-08-04

    申请号：US684061

    申请日：1984-12-20

    申请人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    发明人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    IPC分类号： A61K31/435 ,  A61K31/505 ,  A61P7/02 ,  C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  A61K31/38 ,  C07D417/14

    CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D417/06 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

    摘要： The invention provides novel pyrrole derivatives of formula: ##STR1## in which R'=H, alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, Z=0 or S, p=0 or 1, andeither A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine optionally substituted by OH, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 2,3-dihydropyrrolo[2,1-b]thiazole, 1H,3H-pyrrolo[1,2-c]oxazole, 1,2-dihydro-4H-pyrrolo]1,2-c]-1,3-oxazine or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, n=0 or 1, Het=3-pyridyl or 5-thiazolyl, and(1) either R=H, halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio and Y=alkyl or phenyl optionally substituted by halogen, alkyl, alkyloxy or alkylthio, or Y=--NR.sub.1 R.sub.2 with:either R.sub.1 =H and R.sub.2 =unsubstituted alkyl, cycloalkyl (C.sub.3 -C.sub.6), alkenyl (C.sub.2 -C.sub.4), alkynyl (C.sub.3 -C.sub.4), benzyl or phenyl radicals optionally substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3 or NO.sub.2, or R.sub.2 =adamantyl, pyridyl or pyridylmethyl,or R.sub.1 and R.sub.2 =both unsubstituted alkylor R.sub.1 and R.sub.2 from a 4-phenylpiperazin-1-yl radical the phenyl part of which may be substituted by halogen, alkyl, alkyloxy, alkylthio, CF.sub.3 or NO.sub.2(2) or R=halogen, alkyl or phenyl optionally substituted by halogen, alkyloxy or alkylthio, and Y=NH.sub.2or A is a heterocyclic ring such that it forms, with pyrrole, a 2,3-dihydro-1H-pyrrolizine substituted by OH, 2,3-dihydropyrrolo[2,1-b]thiazole or 2,3-dihydropyrrolo[2,1-b]oxazole ring system, R=H, Y=NH.sub.2, n=0 or 1 or Het=5-thiazolyl or 3-pyridyl,or A is a heterocyclic ring such that it forms, with pyrrole, a 1H,3H-pyrrolo[1,2-c]thiazole, 2,3-dihydro-1H-pyrrolizine, 5,6,7,8-tetrahydroindolizine, 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-thiazine, 1H,3H-pyrrolo[1,2-c]oxazole or 1,2-dihydro-4H-pyrrolo[1,2-c]-1,3-oxazine ring system, R=H, Y=NH.sub.2 andeither Het=5-thiazolyl and n=0 or 1or Het=3-pyridyl and n=1, the alkyl containing 1 to 4 C as a straight or branched chain, and their acid addition salts, pharmaceutical compositions containing the said pyrrole derivatives and process for their preparation. These pyrrole derivatives are useful in prophylactic and therapeutic treatment of thrombotic complaints.

    1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and anti-inflammatory activity
    7.
    发明授权
    1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and anti-inflammatory activity 失效
    1H，具有抗过敏和抗炎活性的3H-吡咯并[1,2-c]噻唑衍生物

    公开(公告)号：US4529728A

    公开(公告)日：1985-07-16

    申请号：US569908

    申请日：1984-01-11

    申请人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    发明人： Jean-Louis Fabre ,  Daniel Farge ,  Claude James ,  Daniel Lave

    IPC分类号： C07D471/04 ,  A61K31/425 ,  A61K31/429 ,  A61K31/435 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/54 ,  A61P7/02 ,  A61P29/00 ,  A61P37/08 ,  C07D213/02 ,  C07D233/60 ,  C07D513/04 ,  C07D521/00 ,  A61K31/445

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D513/04

    摘要： New compounds of the formula ##STR1## in which R.sub.1 and R.sub.2 =H or alkyl and(a) R=CN or alkylcarbonyl, or(b) R=CON(R.sub.3)R.sub.4, in which R.sub.3 =H and R.sub.4 =NH.sub.2, alkylamino, dialkylamino, phenylamino or diphenylamino; or R.sub.3 and R.sub.4 =H, alkyl (1 to 5 C) or substituted phenyl; or R.sub.3 =H and R.sub.4 =pyridyl or alkyl (1 to 5 C) substituted by COOH, NH.sub.2, alkylamino, dialkylamino, morpholino, piperidino, pyrrolidin-1-yl, piperazin-1-yl (optionally substituted by alkyl, pyridyl or optionally substituted phenyl or benzyl), optionally substituted phenyl, pyridyl or imidazolyl; or R.sub.3 and R.sub.4 form an imidazolyl radical or a 5-membered or 6-membered heterocycle which can contain an oxygen, sulphur or nitrogen atom and which is optionally substituted by alkyl, alkoxycarbonyl, hydroxyalkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, pyridyl, pyrimidinyl, pyrazinyl, optionally substituted phenyl or optionally substituted benzyl; or(c) R=--C(.dbd.NOH)NH.sub.2 or --C[.dbd.NN(R'R")NH.sub.2 ], in which R' and R"=alkyl,the said alkyl radicals and alkyl portions being straight-chain or branched-chain and, unless mentioned otherwise, containing 1 to 4 carbon atoms, and the substituted phenyl and benzyl radicals carrying a halogen atom or an alkyl, alkoxy, alkylthio, trifluoromethyl or dialkylamino radical, and their tautomeric forms, addition salts with acids and the metals salts and the addition salts with nitrogen bases, are useful anti-allergic and anti-inflammatory agents. A variety of methods of making them are described.

    摘要翻译： 式（I）的新化合物，其中R 1和R 2 = H或烷基和（a）R = CN或烷基羰基，或（b）R = CON（R3）R4，其中R3 = H和R4 = NH 2，烷基氨基，二烷基氨基，苯基氨基或二苯基氨基; 或R 3和R 4 = H，烷基（1至5 C）或取代的苯基; 或R 3 = H和R 4 =被COOH，NH 2，烷基氨基，二烷基氨基，吗啉代，哌啶子基，吡咯烷-1-基，哌嗪-1-基取代的吡啶基或烷基（1至5 C）（任选地被烷基，吡啶基或任选地 取代的苯基或苄基），任选取代的苯基，吡啶基或咪唑基; 或R3和R4形成咪唑基或可含有氧，硫或氮原子的5元或6元杂环，并且其任选被烷基，烷氧基羰基，羟基烷基，氨基烷基，烷基氨基烷基，二烷基氨基烷基，吡啶基，嘧啶基， 吡嗪基，任选取代的苯基或任选取代的苄基; 或（c）R = -C（= NOH）NH 2或-C [= NN（R'R“）NH 2]，其中R'和R”=烷基，所述烷基和烷基部分为直链， 链或支链，除非另有说明，含有1至4个碳原子，并且取代的苯基和苄基带有卤素原子或烷基，烷氧基，烷硫基，三氟甲基或二烷基氨基，以及它们的互变异构形式，与 酸和金属盐和与氮碱的加成盐是有用的抗过敏和抗炎剂。 描述了制作它们的各种方法。

    1H, 3H-pyrrolo[1,2-c]thiazole-7-carboxamide derivatives and pharmaceutical compositions containing them
    8.
    发明授权
    1H, 3H-pyrrolo[1,2-c]thiazole-7-carboxamide derivatives and pharmaceutical compositions containing them 失效

    公开(公告)号：US5086051A

    公开(公告)日：1992-02-04

    申请号：US493439

    申请日：1990-03-14

    申请人： Claude James ,  Daniel Lave ,  Francoise Soler

    发明人： Claude James ,  Daniel Lave ,  Francoise Soler

    IPC分类号： A61K31/425 ,  A61K31/435 ,  A61K31/44 ,  A61P1/00 ,  A61P1/04 ,  A61P29/00 ,  A61P31/04 ,  C07D513/04 ,  C07D519/00

    CPC分类号： C07D513/04

    摘要： New derivatives of formula (I) in which R.sub.1 =H, halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH, CH, phenyl or phenoxy, Ar=phenyl, naphthyl, pyridyl, quinolyl, isoquinolyl, thienyl, thieno[2,3-b]thienyl or thieno[3,2-b]thienyl (these groups optionally substituted with halogen, alkyl, alkyloxy, CF.sub.3, NH.sub.2, alkylamino, dialkylamino, OH or CN), p=0, 1 or 2, andA--either Z=valency bond and R.sub.2 =HB--or Z=valency bond and R.sub.2 =pyridyl, quinuclidinyl, 3-pyrrolidinyl, 3- or 4-piperidyl (these groups optionally being substituted with alkyl, hydroxyalkyl, phenyl or phenylalkyl)C--or Z=alkylene radical (1 to 4C) and R.sub.2 =2-, 3- or 4-pyridyl, 3-quinuclidinyl, 2- or 3-pyrrolidinyl, 2-, 3- or 4-piperidyl (optionally substituted with alkyl, hydroxyalkyl, phenyl or phenylalkyl) or R.sub.2 =CON(R.sub.3)(R.sub.4) wherea) either R.sub.3 and R.sub.4 form a piperazine optionally substituted with alkyl, hydroxyalkyl, pyridyl, phenyl or phenylalkyl,b) or R.sub.3 =H, alkyl, phenyl or phenylalkyl, or (CH.sub.2).sub.n N(R.sub.5) (R.sub.6) where 1