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16 条记录 (耗时 0.024 秒)

    Method of reducing cholesterol using certain aromatic keto acids
    2.
    发明授权
    Method of reducing cholesterol using certain aromatic keto acids 失效
    使用某些芳香族酮酸降低胆固醇的方法

    公开(公告)号：US4008323A

    公开(公告)日：1977-02-15

    申请号：US560344

    申请日：1975-03-21

    申请人： Henri Cousse ,  Gilbert Mouzin ,  Jean-Pierre Rieu ,  Andre Delhon

    发明人： Henri Cousse ,  Gilbert Mouzin ,  Jean-Pierre Rieu ,  Andre Delhon

    IPC分类号： C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07D295/185 ,  A61K31/495 ,  A61K31/19 ,  A61K31/205 ,  A61K31/235

    CPC分类号： C07D295/185 ,  C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90

    摘要： This invention relates to new chemical compounds useful as drugs, as well as to pharmaceutical compositions containing the same. This application claims their hypocholesterolemic use.The new products are aromatic keto acid compounds with antiinflammatory as well as analgetic and hypocholesteremic acitvity and having the general formula: ##STR1## wherein R.sub.1 is hydrogen, halogen, phenyl, halophenyl, alkyl, phenoxy, or substituted phenoxy.R.sub.2 is hydrogen or alkoxy. R.sub.1 and R.sub.2 may form a ring, for instance: phenyl or cyclohexyl. R.sub.3 is always other than hydrogen, being either methyl (CH.sub.3) or methylene.When R.sub.3 is CH.sub.3, a double bond is present between the A and B carbons. When R.sub.3 is a methylene connected by a double bond to the B carbon, there can be only a single bond between the A and B carbons. The remaining valences of the A carbon atom are satisfied by hydrogen atoms.R.sub.4 may be OH, alkoxy, ##STR2## The drugs containing these active principles are useful in the prevention and treatment of inflammatory syndromes, pain, and conditions involving excess chloresterol.

    摘要翻译： 本发明涉及可用作药物的新化合物，以及含有该化合物的药物组合物。 本申请要求其低胆固醇血症用途。

    Aromatic keto acids and derivatives having analgetic, antiinflammatory, and hypocholesterolemizing action
    5.
    发明授权
    Aromatic keto acids and derivatives having analgetic, antiinflammatory, and hypocholesterolemizing action 失效
    具有止痛，抗炎和低胆固醇作用的芳香酮酸和衍生物

    公开(公告)号：US4058558A

    公开(公告)日：1977-11-15

    申请号：US560946

    申请日：1975-03-21

    申请人： Henri Cousse ,  Gilbert Mouzin ,  Jean-Pierre Rieu

    发明人： Henri Cousse ,  Gilbert Mouzin ,  Jean-Pierre Rieu

    IPC分类号： C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07D295/185 ,  C07C63/33 ,  A61K31/19

    CPC分类号： C07D295/185 ,  C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90

    摘要： This invention relates to new chemical compounds useful as drugs, as well as to pharmaceutical compositions containing the same.The new products are aromatic keto acid compounds with antiinflammatory as well as analgetic and hypocholesteremic activity and having the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, phenyl, halophenyl, phenoxy, or substituted phenoxy.R.sub.2 is hydrogen or alkoxy.R.sub.1 and R.sub.2 may form a ring, for instance: phenyl or cyclohexyl.R.sub.3 is always other than hydrogen, being either methyl (CH.sub.3) or methylene. When R.sub.3 is CH.sub.3, a double bond is present between the A and B carbons. When R.sub.3 is a methylene connected by a double bond to the B carbon, there can be only a single bond between the A and B carbons. The remaining valences of the A carbon atom are satisfied by hydrogen atoms.R.sub.4 may be OH, alkoxy, ##STR2##The drugs containing these active principles are useful in the prevention and treatment of inflammatory syndromes, pain, and conditions involving excess cholresterol.

    摘要翻译： 本发明涉及可用作药物的新化合物，以及含有该化合物的药物组合物。

    Derivatives of 2H pyridazin-3-ones, their preparation and their use as SCD-1 inhibitors
    7.
    发明授权
    Derivatives of 2H pyridazin-3-ones, their preparation and their use as SCD-1 inhibitors 有权
    2H哒嗪-3-酮的衍生物，其制备及其作为SCD-1抑制剂的用途

    公开(公告)号：US08946225B2

    公开(公告)日：2015-02-03

    申请号：US13388884

    申请日：2010-08-05

    申请人： Elisabeth Dupont-Passelaigue ,  Samuel Mialhe ,  Jean-Pierre Rieu ,  Didier Junquero ,  Karine Valeille

    发明人： Elisabeth Dupont-Passelaigue ,  Samuel Mialhe ,  Jean-Pierre Rieu ,  Didier Junquero ,  Karine Valeille

    IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D237/02

    CPC分类号： C07D237/22 ,  C07D401/12 ,  C07D403/12

    摘要： The present invention concerns compounds of general formula (I) characterized in that (formula 1) wherein, in particular: —R1 represents one or more groups such as: trifluoromethyl, halogen such as F, Cl, —when n=m=1, W represents CH then Y represents oxygen, —U represents: •either —(C═O)CH2NH— and is branched at position 4 of pyridazinone, then R2 represents H, •or —(C═O)NH— and U is branched at positions (4), (5) or (6) of pyridazinone, then R2 represents H, —R3 represents a hydrogen or methyl and the addition salts with pharmaceutically acceptable bases and acids and the different isomers, and their mixtures in any proportion for use as SCD-1 enzyme inhibitors for the treatment of obesity, type-2 diabetes and lipid disorders.

    摘要翻译： 本发明涉及通式（I）的化合物，其特征在于（式1）其中特别地：-R 1表示一个或多个基团，例如三氟甲基，卤素如F，Cl， - 当n = m = 1时， W表示CH，Y表示氧，-U表示：• - （C = O）CH2NH-，并且在哒嗪酮的第4位分支，则R2表示H，•或 - （C = O）NH-，U为支链 在哒嗪酮的位置（4），（5）或（6）中，R 2表示H，-R 3表示氢或甲基，加成盐与药学上可接受的碱和酸和不同的异构体， 用作SCD-1酶抑制剂用于治疗肥胖，2型糖尿病和脂质疾病。

    Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application
    9.
    发明授权
    Substituted 1-(4-piperidyl)-3-(aryl) isothioureas their preparation and their therapeutic application 失效
    取代的1-（4-哌啶基）-3-（芳基）异硫脲的制备及其治疗应用

    公开(公告)号：US06531469B1

    公开(公告)日：2003-03-11

    申请号：US09889805

    申请日：2001-07-20

    申请人： Jean-Pierre Rieu ,  Jean-François Patoiseau ,  Gareth John ,  Bruno Legrand ,  Yvan Verscheure

    发明人： Jean-Pierre Rieu ,  Jean-François Patoiseau ,  Gareth John ,  Bruno Legrand ,  Yvan Verscheure

    IPC分类号： C07D41712

    CPC分类号： C07D413/12 ,  C07D417/12

    摘要： The invention concerns novel substituted N-benzo(thia/oxa)zines-2-yl-1-arylalkyloxyalkyl-4-piperidinamine, their preparation and their therapeutic use. The invention concerns compounds of formula (1) wherein: X represents an oxygen or sulphur atom; Y represents either an alkylene radical, branched or not and containing 2 to 6 carbon atoms or a CH2—CH(OH)—CH2— radical. R represents a hydrogen, an alkyl radical, branched or not and containing 1 to 7 carbon atoms; R1 to R6, identical or different, represent a hydrogen, a saturated or unsaturated alkyl, branched or not and containing 1 to 5 carbon atoms, a saturated or unsaturated alkyloxy, branched or not and containing 1 to 5 carbon atoms, a halogeno, nitro, hydroxy, acyl or acyloxy group comprising 2 to 3 carbon atoms, an alkylamino group containing 1 to 5 carbon atoms, a trifluoro methyl or trifluoro methoxyl group; n is an integer ranging from 1 to 6 inclusively, and their pure, enantiomers or their mixtures, the therapeutically acceptable mineral and organic salts of the compounds of formula (1) and their possible hydrates.

    摘要翻译： 本发明涉及新型取代的N-苯并（噻唑/氧杂）嗪-2-基-1-芳基烷氧基烷基-4-哌啶胺及其制备及其治疗用途。 本发明涉及式（1）的化合物，其中：X表示氧或硫原子; Y表示亚烷基，支链或不支链，含有2-6个碳原子或CH2-CH（OH）-CH2-基。 R表示氢，烷基，支链或不支链，含有1至7个碳原子; R 1至R 6相同或不同，表示氢，饱和或不饱和的烷基，支链或不含并且含有1至5个碳原子，饱和或不饱和烷氧基，支链或不具有1至5个碳原子，卤代，硝基 ，含有2〜3个碳原子的羟基，酰基或酰氧基，含1至5个碳原子的烷基氨基，三氟甲基或三氟甲氧基; n是1至6的整数，以及它们的纯的对映体或它们的混合物，式（1）化合物的治疗上可接受的矿物和有机盐及其可能的水合物。

    Sulfonamides derived from benzocyclic or benzoheterocyclic acids, their preparation and application in therapeutics
    10.
    发明授权
    Sulfonamides derived from benzocyclic or benzoheterocyclic acids, their preparation and application in therapeutics 失效
    衍生自苯环或苯并杂环酸的磺酰胺，其制备和在治疗中的应用

    公开(公告)号：US5385931A

    公开(公告)日：1995-01-31

    申请号：US613842

    申请日：1990-12-28

    申请人： Dennis Bigg ,  Alain Duflos ,  Jean-Pierre Rieu

    发明人： Dennis Bigg ,  Alain Duflos ,  Jean-Pierre Rieu

    IPC分类号： A61K31/19 ,  A61K31/215 ,  A61K31/22 ,  A61K31/335 ,  A61K31/34 ,  A61K31/343 ,  A61K31/35 ,  A61K31/352 ,  A61K31/357 ,  A61K31/38 ,  A61K31/381 ,  A61P7/02 ,  C07C69/757 ,  C07C229/26 ,  C07C311/19 ,  C07D307/85 ,  C07D311/66 ,  C07D317/46 ,  C07D333/70 ,  C07D307/81 ,  C07D333/60

    CPC分类号： C07D311/66 ,  C07C229/26 ,  C07C311/19 ,  C07C69/757 ,  C07D307/85 ,  C07D317/46 ,  C07D333/70 ,  C07C2102/08

    摘要： The invention relates to new sulphonamide derivatives of benzo-cyclic or benzo-heterocyclic acids and their derivatives of general formula I ##STR1## in which: R represents a straight-chain or branched lower alkyl radical having 1 to 9 C;a phenyl radical which is unsubstituted or substituted by one or more groups:straight-chain or branched lower alkyl having 1 to 4 C, halogeno, alkoxy, nitro, amino, dialkylamino or CF.sub.3 ;a substituted or unsubstituted naphthalene;a thiophenyl radical;R.sub.1 represents a hydrogen or a straight-chain or branched lower alkyl or a benzyl;R.sub.2 represents a hydrogen, a straight-chain or branched lower alkyl group, a substituted or unsubstituted phenyl group or an aralkyl group;R.sub.3 represents a hydrogen or a straight-chain or branched lower alkyl (1 to 6 C);--X-- represents a divalent functional radical chosen from the following: --CH.sub.2 --; ##STR2## where R.sub.4 =H or Me; A represents a benzo-cyclic or benzo-heterocyclic divalent radical chosen from the following (a) to (j): ##STR3## and n can assume the values 1 to 4 inclusive; and the therapeutically acceptable organic or inorganic salts (R.sub.3 =H), the pure isomers or diastereoisomers or their mixture and all the pharmaceutical compositions of formula I with other active principles.The invention relates to the application of I as a medicament and the preparation processes.

    摘要翻译： PCT No.PCT / FR90 / 00234 Sec。 371 1990年12月28日第 102（e）1990年12月28日日期PCT提交1990年4月4日PCT公布。 WO90 / 12007 PCT出版物 日本1990年10月18日。本发明涉及苯并环或苯并杂环酸的新磺酰胺衍生物及其通式I的衍生物或具有1〜9个C的支链低级烷基; 未取代或被一个或多个基团取代的苯基：具有1-4个碳原子的直链或支链低级烷基，卤代，烷氧基，硝基，氨基，二烷基氨基或CF 3; 取代或未取代的萘; 硫代苯基; R1表示氢或直链或支链的低级烷基或苄基; R2表示氢，直链或支链的低级烷基，取代或未取代的苯基或芳烷基; R3表示氢或直链或支链的低级烷基（1-6）; -X-表示选自以下的二价官能团：-CH 2 - ; 其中R4 = H或Me; A表示选自以下（a）至（j）的苯并环或苯并杂环二价基团：（a）GE（e）图像（f） （h）（i）（j），n可以取值1〜4， 和治疗上可接受的有机或无机盐（R3 = H），纯异构体或非对映异构体或其混合物以及具有其它活性成分的式I的所有药物组合物。 本发明涉及I作为药物的应用及其制备方法。