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    Chromene compounds, a process for their preparation and pharmaceutical compositions containing them
    1.
    发明授权
    Chromene compounds, a process for their preparation and pharmaceutical compositions containing them 失效
    色烯化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US08247441B2

    公开(公告)日：2012-08-21

    申请号：US12804355

    申请日：2010-07-20

    申请人： Guillaume De Nanteuil ,  Bernard Cimetiere ,  Anne Dekeyne ,  Mark Millan

    发明人： Guillaume De Nanteuil ,  Bernard Cimetiere ,  Anne Dekeyne ,  Mark Millan

    IPC分类号： A61K31/407 ,  C07D209/58

    CPC分类号： C07D491/04

    摘要： The invention relates to compounds of formula (I): wherein R1 and R2 together form the following carbon-containing chain: wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl, aryl, heteroaryl, 3,4-dioxocyclobutenyl, alkylcarbonyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, benzoyl, arylsulphonyl or heteroarylsulphonyl group, each of those groups optionally being substituted, or R3 and R4 together with the nitrogen atom carrying them form a 5- to 8-membered ring, the ring thereby formed optionally being substituted. Medicinal products containing the same which are useful in treating conditions requiring a D3 receptor antagonist.

    摘要翻译： 本发明涉及式（I）化合物：其中R 1和R 2一起形成以下含碳链：其中：R 3表示氢原子或烷基，R 4表示氢原子或烷基，芳基，杂芳基，3 ，4-二氧环戊烯基，烷基羰基，环烷基羰基，杂环烷基羰基，苯甲酰基，芳基磺酰基或杂芳基磺酰基，这些基团任选被取代，或者R3和R4与携带它们的氮原子一起形成5-至8-元环， 形成任选地被取代。 含有该药物的药物可用于治疗需要D3受体拮抗剂的病症。

    4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds
    2.
    发明授权
    4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrazine-6-carboxamide compounds 失效
    4-氧代-4,6,7,8-四氢 - 吡咯并[1,2-a]吡嗪-6-甲酰胺化合物

    公开(公告)号：US07498330B2

    公开(公告)日：2009-03-03

    申请号：US11079638

    申请日：2005-03-14

    申请人： Guillaume De Nanteuil ,  Philippe Gloanec ,  Jean-Gilles Parmentier ,  Alain Benoist ,  Alain Rupin ,  Marie-Odile Vallez ,  Tony Verbeuren

    发明人： Guillaume De Nanteuil ,  Philippe Gloanec ,  Jean-Gilles Parmentier ,  Alain Benoist ,  Alain Rupin ,  Marie-Odile Vallez ,  Tony Verbeuren

    IPC分类号： A01N43/66 ,  A61K31/53 ,  C07D241/36

    CPC分类号： C07D487/04

    摘要： Compound of formula (I): wherein: represents 1-oxidopyridyl substituted by the remainder of the molecule in any one of the positions 2, 3 and 4, m and n, which may be identical or different, each represent an integer of from 1 to 3, R1 represents hydrogen or alkyl, R2 and R3, which may be identical or different, each represent an atom or group selected from hydrogen, halogen, alkyl, hydroxy, acyloxy and alkoxy, or, together with the carbon atom carrying them, form a cycloalkane having from 3 to 6 carbon atoms, R4 and R5 each represent hydrogen, or are adjacent and, together with the carbon atoms carrying them, form a benzo ring, Ar represents aryl or heteroaryl. Medicinal products containing the same which are useful as thrombin inhibitors.

    摘要翻译： 式（I）的化合物：其中：表示由位置2,3和4中的任一个中的分子的其余部分取代的1-氧化吡啶基，m和n可以相同或不同，各自表示1的整数 至3，R 1表示氢或烷基，可以相同或不同的R 2和R 3各自表示选自氢，卤素，烷基，羟基，酰氧基和烷氧基的原子或基团，或者与携带它们的碳原子一起， 形成具有3至6个碳原子的环烷烃，R 4和R 5各自表示氢或邻近，并且与携带它们的碳原子一起形成苯并环，Ar表示芳基或杂芳基。 含有该药物的药物可用作凝血酶抑制剂。

    Pyrrolidine and thiazolidine compounds
    3.
    发明授权
    Pyrrolidine and thiazolidine compounds 失效
    吡咯烷和噻唑烷化合物

    公开(公告)号：US07439263B2

    公开(公告)日：2008-10-21

    申请号：US11131510

    申请日：2005-05-18

    申请人： Guillaume De Nanteuil ,  Alain Benoist ,  Murielle Combettes ,  Elizabeth Harley

    发明人： Guillaume De Nanteuil ,  Alain Benoist ,  Murielle Combettes ,  Elizabeth Harley

    IPC分类号： A61K31/40 ,  C07D207/04

    CPC分类号： C07D405/12 ,  C07D207/10 ,  C07D207/16 ,  C07D277/12 ,  C07D295/185 ,  C07D403/12 ,  C07D409/12 ,  C07D417/12

    摘要： Compounds of formula (I): wherein: X1 represents an atom or group selected from CR4aR4b, O, S(O)q1 and NR5, wherein R4a, R4b, q1 and R5 are as defined in the description, m1 represents zero or an integer from 1 to 4 inclusive, m2 represents an integer from 1 to 4 inclusive, n1 and n2, which may be identical or different, each represent an integer from 1 to 3 inclusive, R1 represents hydrogen or a group selected from carboxy, alkoxycarbonyl, optionally substituted carbamoyl and optionally substituted alkyl, R2 represents hydrogen or alkyl, Ak represents an optionally substituted alkylene chain, p represents zero, 1 or 2, R3 represents hydrogen or cyano, X2 and X3, which may be identical or different, each represent either S(O)q2, or CR6aR6b, wherein q2, R6a and R6b are as defined in the description, its optical isomers, where they exist, and its addition salts with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful as DPP-IV inhibitors.

    摘要翻译： 式（I）的化合物：其中：X 1表示选自CR 4a R 4a，O，S（O） q1和NR5，其中R 4a 4a，R 4b，q 1和...， R 5如描述中所定义，m 1表示0或1至4的整数，其中m 2表示1的整数， 至4个，其中可以相同或不同的n 1和n 2各自表示1至3的整数，包括1和3的整数，R 1， 表示氢或选自羧基，烷氧基羰基，任选取代的氨基甲酰基和任选取代的烷基的基团，R 2表示氢或烷基，Ak表示任选取代的亚烷基链，p表示0,1或2，R 3或3表示氢或氰基，X 2和X 3可以相同或不同，各自表示S（O） q2，或CR 6a R 6b，其中q2

    Alpha-amino-acid compounds
    4.
    发明授权
    Alpha-amino-acid compounds 失效
    α-氨基酸化合物

    公开(公告)号：US06706742B2

    公开(公告)日：2004-03-16

    申请号：US10146272

    申请日：2002-05-15

    申请人： Guillaume De Nanteuil ,  Bernard Portevin ,  Alain Benoist ,  Nigel Levens ,  Olivier Nosjean ,  Bernadette Husson-Robert ,  Michelle Boulanger

    发明人： Guillaume De Nanteuil ,  Bernard Portevin ,  Alain Benoist ,  Nigel Levens ,  Olivier Nosjean ,  Bernadette Husson-Robert ,  Michelle Boulanger

    IPC分类号： C07D27704

    CPC分类号： C07D295/185 ,  C07D207/16 ,  C07D277/04 ,  C07D277/06 ,  Y02P20/55

    摘要： Compound selected from those of formula (I): wherein: represents an optionally substituted 5-membered nitrogen-containing heterocycle, Ak represents an alkylene chain, X represents a single bond or phenylene, R1 and R2, which may be identical or different, each represent hydrogen or alkyl, R3 represents alkyl, nitro or cyano, Y represents NR4 or CHNO2, R4 represents hydrogen or alkyl, its tautomers when they exist, its optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, with the exclusion of compounds wherein, simultaneously, represents an unsubstituted 5-membered nitrogen-containing heterocycle, Ak represents —(CH2)3—, X represents a single bond, Y represents NH and R3 represents nitro. Medicinal products containing the same which are useful as dipeptidyl peptidase IV inhibitors.

    摘要翻译： 选自式（I）的化合物的化合物：其中：表示任选取代的5元含氮杂环，Ak表示亚烷基链，X表示单键或亚苯基，R 1和R 2可以相同或不同，各自相同或不同 代表氢或烷基，R3代表烷基，硝基或氰基，Y代表NR4或CHNO2，R4代表氢或烷基，其互变异构体存在时，其光学异构体及其与药学上可接受的酸的加成盐，排除化合物 其中，同时代表未取代的5元含氮杂环，Ak表示 - （CH2）3-，X表示单键，Y表示NH，R3表示硝基。含有该二价基团的肽酶IV 抑制剂。

    Piperidine compounds
    6.
    发明授权
    Piperidine compounds 失效
    哌啶化合物

    公开(公告)号：US5652246A

    公开(公告)日：1997-07-29

    申请号：US546263

    申请日：1995-10-20

    申请人： Guillaume de Nanteuil ,  Georges Remond ,  Bernard Portevin ,  Jacqueline Bonnet ,  Emmanuel Canet ,  Graham Birrell

    发明人： Guillaume de Nanteuil ,  Georges Remond ,  Bernard Portevin ,  Jacqueline Bonnet ,  Emmanuel Canet ,  Graham Birrell

    IPC分类号： A61K31/4427 ,  A61K31/445 ,  A61P1/00 ,  A61P11/00 ,  A61P13/02 ,  A61P15/00 ,  A61P25/00 ,  A61P25/04 ,  A61P25/06 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D401/06 ,  C07D471/04 ,  C07D471/02 ,  A61K31/415 ,  A61K31/44 ,  C07D235/22

    CPC分类号： C07D401/06 ,  C07D471/04

    摘要： The invention relates to the compounds of formula (I): ##STR1## in which: R.sub.1 represents alkyl, phenyl, naphthyl, pyridyl or thienyl group, each phenyl, naphthyl, pyridyl or thienyl optionally being substituted,R.sub.2 represents a hydrogen atom or a substituted or unsubstituted alkyl, substituted or unsubstituted phenyl, cycloalkyl, piperidino or substituted or unsubstituted amino group,X represents CO or SO.sub.2,R.sub.3 represents hydrogen or alkyl,R.sub.4 represents alkyl, substituted or unsubstituted phenyl or trihalomethyl, or else R.sub.3 and R.sub.4 form, together with the carbon atoms which carry them, cyclo(C.sub.3 -C.sub.7)alkenyl,A represents phenyl, naphthyl or pyridyl ring, each phenyl, naphthyl or pyridyl ring optionally being substituted,their isomers, the corresponding quaternary ammonium salts of the piperidine and their addition salts with a pharmaceutically acceptable acid, an medicinal products containing the same are useful as antagonists of NK.sub.1 receptors.

    摘要翻译： 本发明涉及式（I）化合物：其中：R 1表示烷基，苯基，萘基，吡啶基或噻吩基，每个苯基，萘基，吡啶基或噻吩基任选被取代，R 2表示氢 原子或取代或未取代的烷基，取代或未取代的苯基，环烷基，哌啶子基或取代或未取代的氨基，X表示CO或SO 2，R 3表示氢或烷基，R 4表示烷基，取代或未取代的苯基或三卤甲基， R 4与携带它们的碳原子一起形成环（C 3 -C 7）链烯基，A代表苯基，萘基或吡啶环，每个苯基，萘基或吡啶基任选被取代，它们的异构体是相应的季铵盐 哌啶及其与药学上可接受的酸的加成盐，含有它们的药物可用作NK1受体的拮抗剂。

    4-methyl-5-substituted-1,3-oxazoles having anti-inflammatory activity
    7.
    发明授权
    4-methyl-5-substituted-1,3-oxazoles having anti-inflammatory activity 失效
    具有抗炎活性的4-甲基-5-取代-1,3-恶唑

    公开(公告)号：US5468761A

    公开(公告)日：1995-11-21

    申请号：US164464

    申请日：1993-12-09

    申请人： Guillaume de Nanteuil ,  Michel Vincent ,  Christine Lila ,  Jacqueline Bonnet ,  Armel Fradin

    发明人： Guillaume de Nanteuil ,  Michel Vincent ,  Christine Lila ,  Jacqueline Bonnet ,  Armel Fradin

    IPC分类号： A61K31/42 ,  A61K31/421 ,  A61P29/00 ,  C07D263/32

    CPC分类号： C07D263/32 ,  A61K31/42

    摘要： Compound of formula (I): ##STR1## in which: R.sub.1 represents 1-adamantyl, dicyclopropylmethyl, substituted or unsubstituted (C.sub.3 -C.sub.6) cycloalkyl or substituted or unsubstituted bicyclo[2.2.2]oct-1-yl,R.sub.2 represents: ##STR2## in which: m represents 1, 2 or 3,X represents oxygen or sulfur or N--R,R.sub.3 or R.sub.4, which are identical or different, represent hydrogen, (C.sub.1 -C.sub.6) alkyl or trifluoromethyl, ##STR3## n represents 0, 1 or 2, R.sub.5 represents hydroxy, or (C.sub.1 -C.sub.6) alkoxy, and anti-inflammatory medicinal products containing the same.

    摘要翻译： 式（I）化合物：其中：R1表示1-金刚烷基，二环丙基甲基，取代或未取代的（C3-C6）环烷基或取代或未取代的双环[2.2.2]辛-1-基，R2 表示： 其中：m表示1,2或3，X表示氧或硫或NR，R3或R4相同或不同，表示氢，（C1-C6）烷基或三氟甲基， IMAGE> n表示0,1或2，R 5表示羟基或（C 1 -C 6）烷氧基，和含有它们的抗炎药物。