会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 2. 发明授权
    • 1H, 3H-pyrrolo (1,2-C) thiazole derivatives and pharmaceutical
compositions
    • 1H,3H-吡咯(1,2-C)噻唑衍生物和药物组合物
    • US4786645A
    • 1988-11-22
    • US69211
    • 1987-07-02
    • Jean-Louis FabreClaude JamesDaniel Lave
    • Jean-Louis FabreClaude JamesDaniel Lave
    • A61K31/50A61K31/44A61K31/47A61P7/02A61P29/00C07D513/04C07D417/14
    • C07D513/04
    • 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.
    • 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。
    • 3. 发明授权
    • 1H,3H-pyrrol[1,2-c]thiazole derivatives and pharmaceutical compositions
containing them
    • US4783472A
    • 1988-11-08
    • US69520
    • 1987-07-02
    • Jean-Louis FabreClaude JamesDaniel Lave
    • Jean-Louis FabreClaude JamesDaniel Lave
    • A61K31/44A61P7/02A61P29/00C07D513/04C07D409/00C07D215/04C07D217/00C07D401/00
    • C07D513/04
    • 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.
    • 6. 发明授权
    • Anti-thrombotic ortho-condensed pyrrole derivatives, compositions, and
method of use therefor
    • US4684658A
    • 1987-08-04
    • US684061
    • 1984-12-20
    • Jean-Louis FabreDaniel FargeClaude JamesDaniel Lave
    • Jean-Louis FabreDaniel FargeClaude JamesDaniel Lave
    • A61K31/435A61K31/505A61P7/02C07D401/06C07D401/14C07D417/06C07D471/04C07D487/04C07D498/04C07D513/04A61K31/38C07D417/14
    • C07D401/06C07D401/14C07D417/06C07D471/04C07D487/04C07D513/04
    • 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.
    • 8. 发明授权
    • 1H,3H-pyrrolo[1,2-c]thiazole derivatives having anti-allergic and
anti-inflammatory activity
    • 1H,具有抗过敏和抗炎活性的3H-吡咯并[1,2-c]噻唑衍生物
    • US4529728A
    • 1985-07-16
    • US569908
    • 1984-01-11
    • Jean-Louis FabreDaniel FargeClaude JamesDaniel Lave
    • Jean-Louis FabreDaniel FargeClaude JamesDaniel Lave
    • C07D471/04A61K31/425A61K31/429A61K31/435A61K31/44A61K31/4427A61K31/54A61P7/02A61P29/00A61P37/08C07D213/02C07D233/60C07D513/04C07D521/00A61K31/445
    • C07D231/12C07D233/56C07D249/08C07D513/04
    • 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.
    • 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。
    • 10. 发明授权
    • Thienothienylcarbonyl-phenylalkanoic acids and derivatives thereof
    • 噻吩并噻吩基 - 苯基链烷酸及其衍生物
    • US4183944A
    • 1980-01-15
    • US915241
    • 1978-06-13
    • Jean-Louis FabreDaniel FargeClaude James
    • Jean-Louis FabreDaniel FargeClaude James
    • C07D493/04C07D495/04
    • C07D493/04C07D495/04
    • Compounds of the formula: ##STR1## wherein R represents hydrogen or an alkyl radical, R.sub.1 represents a hydroxy, amino or alkoxy radical or an alkylamino or dialkylamino group, the various alkyl radicals and the alkoxy radical being optionally substituted by a dialkylamino group, the alkyl radicals of the said dialkylamino groups optionally being linked together to form a heterocyclyl radical with 5 or 6 atoms in the ring, and A represents the thieno[2,3-b]thien-2-yl or thieno[3,2-b]thien-2-yl radical, the A--CO-- grouping being attached to the 3- or 4-position of the phenyl ring, have been found to possess useful pharmacological properties and are particularly active as analgesics, antipyretics, agents for inhibiting platelet aggregation and as anti-inflammatory agents.
    • 其中R表示氢或烷基,R1表示羟基,氨基或烷氧基或烷基氨基或二烷基氨基,各种烷基和烷氧基任选被二烷基氨基取代, 所述二烷基氨基的烷基任选地连接在一起形成环中具有5或6个原子的杂环基,A表示噻吩并[2,3-b]噻吩-2-基或噻吩并[3,2-b ]噻吩-2-基自由基,苯环的3-或4-位连接的A-CO-基团已经被发现具有有用的药理学性质,并且作为止痛剂,解热剂,抑制血小板的药剂特别​​有活性 聚集和作为抗炎剂。