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31. 发明授权

US07119116B2 Derivatives of dioxane-2-alkyl carbamates, preparation thereof and application thereof in therapeutics 有权
标题翻译：二恶烷-2-烷基氨基甲酸酯的衍生物，其制备及其在治疗中的应用
公开(公告)号：US07119116B2
公开(公告)日：2006-10-10
申请号：US11062541
申请日：2005-02-22
申请人： Ahmed Abouabdellah , Michele Bas , Gihad Dargazanli , Christian Hoornaert , Adrien Tak Li , Florence Medaisko
发明人： Ahmed Abouabdellah , Michele Bas , Gihad Dargazanli , Christian Hoornaert , Adrien Tak Li , Florence Medaisko
IPC分类号： A61K31/36 , C07D319/06
CPC分类号： C07D319/06 , C07C235/06 , C07D405/12
摘要： A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1–C3)alkyl, (C1–C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3–C6)cycloalkyl-O— or (C3–C6)cycloalkyl(C1–C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1–C3)alkyl, (C3–C5)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1–C3)alkyl, (C1–C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.
摘要翻译：对应于通式（I）的化合物：其中R 1表示任选被一个或多个卤素原子或羟基取代的苯基或萘基，氰基，硝基，（C 1）（C 1 -C 3）烷基，（C 1 -C 3 -C 3）烷氧基，三氟甲基，三氟甲氧基，苄氧基，（C 3 H 3） C 1 -C 6环烷基-O-或（C 3 -C 6 -C 6）环烷基（C 1 -C 6） C 1 -C 3烷氧基; R 2表示其中R 3 3表示氢原子的通式为CHR 3 CONHR 4 S的基团，或甲基和R 4代表氢原子或（C 1 -C 3 -C 3）烷基，（C 3 H 3）（C 1 -C 5）环烷基或（吡啶-4-基）甲基; 或2,2,2-三氟乙基; 或（咪唑-2-基）甲基; 或（苯并咪唑-2-基）甲基; 或任选被一个或多个卤素原子取代的苯基或氰基，硝基，（C 1 -C 3 - ）烷基，（C 1 -C 3）烷基， -C 3 -C 3烷氧基，三氟甲基或三氟甲氧基; n表示1〜3的数; 以碱的形式，与酸的加成盐，水合物或溶剂合物的形式。还公开并要求保护的是由其衍生的药物组合物及其治疗各种疾病的治疗用途。

32. 发明申请

US20110071162A1 TRIAZOLOPYRIDINE CARBOXAMIDE DERIVATIVES AND TRIAZOLOPYRIMIDINE CARBOXAMIDE DERIVATIVES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF 审中-公开
标题翻译：三唑酰胺羧酰胺衍生物和三唑基吡啶羧酰胺衍生物，其制备方法及其治疗方法
公开(公告)号：US20110071162A1
公开(公告)日：2011-03-24
申请号：US12956892
申请日：2010-11-30
申请人： Luc Even , Christian Hoornaert
发明人： Luc Even , Christian Hoornaert
IPC分类号： A61K31/496 , A61P25/00 , A61P1/00 , A61P13/10 , A61P11/00 , A61P27/02 , A61P19/10 , A61P29/00 , A61P3/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The disclosure relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
摘要翻译：本公开涉及通式（I）的三唑并吡啶甲酰胺衍生物和三唑并嘧啶甲酰胺衍生物：其中X，A，R 1和R 2如本文所定义。本发明还涉及其制备方法及其治疗用途。

33. 发明授权

US5958924A Quinolein-2 (1H)-one derivatives as serotonin antagonists 失效
标题翻译：喹啉-2（1H） - 酮衍生物作为血清素拮抗剂
公开(公告)号：US5958924A
公开(公告)日：1999-09-28
申请号：US11482
申请日：1998-02-04
申请人： Gary McCort , Christian Hoornaert , Genevieve Dellac , Michel Aletru
发明人： Gary McCort , Christian Hoornaert , Genevieve Dellac , Michel Aletru
IPC分类号： A61K31/00 , A61K31/435 , A61K31/4353 , A61K31/4365 , A61K31/47 , A61K31/4709 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/06 , A61P9/10 , A61P43/00 , C07D401/06 , C07D495/04
CPC分类号： C07D401/06 , C07D495/04
摘要： Compounds of formula (I) ##STR1## in which A represents a 4-(thieno�3,2-c! pyridin-4-yl)-1-piperazinyl or 4-(4-fluorobenzoyl)-1-piperidyl group, R.sub.1 and R.sub.2 each represent, independently of one another, either a hydrogen or halogen atom, or an amino, hydroxyl, nitro, cyano, (C.sub.1 -C.sub.6)alkyl, (C.sub.1 -C.sub.6)alkoxy, trifluoromethyl, trifluoromethoxy or --COOH group, a group --COOR.sub.4, a --CONH.sub.2 group or a group --CONHR.sub.4, --CONR.sub.4 R.sub.5, --SR.sub.4, --SO.sub.2 R.sub.4, --NHCOR.sub.4, --NHS0.sub.2 R.sub.4 or --N(R.sub.4).sub.2, where R.sub.4 and R.sub.5 are each a (C.sub.1 -C.sub.4)alkyl group, R.sub.3 represents either a hydrogen atom, or a (C.sub.1 -C.sub.4)alkyl group, or a group --(CH.sub.2)OH, --(CH.sub.2).sub.p NH.sub.2, --(CH.sub.2).sub.n COOH, --(CH.sub.2).sub.n COOR.sub.4, --(CH.sub.2).sub.n CONH.sub.2, --(CH.sub.2).sub.n CONHOH, --(CH.sub.2).sub.p SH, --(CH.sub.2).sub.n SO.sub.3 H, --(CH.sub.2).sub.n SO.sub.2 NH.sub.2, --(CH.sub.2).sub.n SO.sub.2 NHR.sub.4, --(CH.sub.2).sub.n SO.sub.2 NH.sub.4 R.sub.5, --(CH.sub.2).sub.n CONHR.sub.4, --(CH.sub.2).sub.n CONR.sub.4 R.sub.5, --(CH.sub.2).sub.p NHSO.sub.2 R.sub.4, --(CH.sub.2).sub.p NHCOR.sub.4 or --(CH.sub.2).sub.p OCOR.sub.4, where R.sub.4 and R.sub.5 are each a (C.sub.1 -C.sub.4)alkyl group, n is equal to 1, 2, 3 or 4, p is equal to 2, 3 or 4 and m is equal to 2, 3 or 4. use in therapy.
摘要翻译： PCT No.PCT / FR96 / 01401 Sec。 371日期：1998年2月4日 102（e）1998年2月4日PCT PCT 1996年9月12日PCT公布。公开号WO97 / 10238 日期1997年3月20日，式（I）的化合物，其中A表示4-（噻吩并[3,2-c]吡啶-4-基）-1-哌嗪基或4-（4-氟苯甲酰基）-1-哌啶基，R 1和R 2各自独立地表示氢或卤素原子，或氨基，羟基，硝基，氰基，（C 1 -C 6）烷基，（C 1 -C 6）烷氧基，三氟甲基，三氟甲氧基或-COOH基，-COOR4基团，-CONH 2基团或-CONHR 4基，-CONR 4 R 5，-SR 4，-SO 2 R 4，-NHCOR 4，-NHSO 2 R 4或-N（R 4）2，其中R 4和R 5各自为（C 1 -C 4）烷基，R 3表示氢原子或（C 1 -C 4）烷基，或基团 - （CH 2）OH， - （CH 2）p NH 2， - （CH 2）n COOH， - （CH 2）n COOR 4 - ）nCONH 2， - （CH 2）n CONHOH， - （CH 2）n CONH 4， - （CH 2）n SO 2 NH 2， - （CH 2）n SO 2 NHR 4， - （CH 2）n SO 2 NH 4 R 5 - ， - （CH 2）p NHSO 2 R 4， - （CH 2）p NHCOR 4或 - （CH 2）pOCOR 4，其中R 4和R 5各自为（C 1 -C 4）烷基，n等于1,2,3或4，p等于 2,3或4，m等于2,3或4.用于治疗。

34. 发明授权

US07863279B2 Triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives, preparation thereof and therapeutic use thereof 失效
标题翻译：三唑并吡啶甲酰胺衍生物和三唑并嘧啶甲酰胺衍生物，其制备及其治疗用途
公开(公告)号：US07863279B2
公开(公告)日：2011-01-04
申请号：US12577777
申请日：2009-10-13
申请人： Luc Even , Christian Hoornaert
发明人： Luc Even , Christian Hoornaert
IPC分类号： A61K31/4353 , A61K31/519 , C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The invention relates to the triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
摘要翻译：本发明涉及三唑并吡啶甲酰胺衍生物和通式（I）的三唑并嘧啶甲酰胺衍生物：其中X，A，R 1和R 2如本文所定义。本发明还涉及其制备方法及其治疗用途。

35. 发明授权

US5373023A Tetrahydronaphtalene derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译：四氢萘衍生物，它们的制备和含有它们的药物组合物
公开(公告)号：US5373023A
公开(公告)日：1994-12-13
申请号：US101764
申请日：1993-08-04
申请人： Paul Howard Williams , Christian Hoornaert , Jean Claude Muller
发明人： Paul Howard Williams , Christian Hoornaert , Jean Claude Muller
IPC分类号： A61K31/165 , A61P3/00 , A61P9/10 , A61P25/28 , C07C231/14 , C07C233/66 , C07C233/75 , C07C233/78 , C07C233/88 , C07C253/30 , C07C255/60 , C07D213/38 , C07D319/18 , C07C53/06 , C07C55/07 , C07C233/65
CPC分类号： C07D319/18 , C07C233/66 , C07C233/75 , C07C233/78 , C07C233/88 , C07C255/60 , C07D213/38
摘要： The invention provides compounds which are tetrahydronaphthalene derivatives of the formula (I) ##STR1## wherein R.sub.1 represents a halogen atom, a cyano group, a nitro group, an unbranched (C.sub.1 -C.sub.6) alkoxy group, a (C.sub.1 -C.sub.6 cycloalkyl) (C.sub.1 -C.sub.2 alkoxy) group or an aryl (C.sub.1 -C.sub.2 alkoxy) group,R.sub.2 represents a (C.sub.1 -C.sub.4) alkyl group, an aryl group optionally substituted with at least one methoxy group, a pyridyl group or a benzodioxanyl group,R.sub.3 represents a hydrogen atom or a (C.sub.1 -C.sub.2) alkyl group, and n=0 to 3, or are addition salts with pharmaceutically acceptable acids. The compounds of the invention have anti-ischaemic activity.
摘要翻译：本发明提供化合物，其为式（I）的四氢萘衍生物其中R 1表示卤素原子，氰基，硝基，无支链（C1-C6）烷氧基，（C1-C6）烷氧基环烷基）（C1-C2烷氧基）或芳基（C1-C2烷氧基）基，R2表示（C1-C4）烷基，任选被至少一个甲氧基，吡啶基或苯并二恶烷基取代的芳基，R3表示氢原子或（C1-C2）烷基，n = 0〜3，或与药学上可接受的酸形成的加成盐。本发明的化合物具有抗缺血活性。

36. 发明授权

US5075325A N-aminobutyl-n-phenylarylamide derivatives, their preparation and their application in therapy 失效
标题翻译： N-氨基丁基-N-苯甲酰胺衍生物，其制备及其在治疗中的应用
公开(公告)号：US5075325A
公开(公告)日：1991-12-24
申请号：US540229
申请日：1990-06-19
申请人： Christian Hoornaert , Jean-Claude Muller , Nigel Beeley
发明人： Christian Hoornaert , Jean-Claude Muller , Nigel Beeley
IPC分类号： A61K31/165 , A61K31/357 , A61K31/36 , A61K31/435 , A61K31/47 , A61K31/472 , A61K31/535 , A61K31/5375 , A61K31/54 , A61P1/04 , A61P9/00 , A61P11/08 , A61P25/08 , C07C67/00 , C07C231/00 , C07C231/02 , C07C231/08 , C07C231/12 , C07C233/88 , C07C235/68 , C07D211/14 , C07D213/38 , C07D213/74 , C07D213/82 , C07D215/50 , C07D217/04 , C07D217/26 , C07D295/12 , C07D295/13 , C07D317/58
CPC分类号： C07D213/74 , C07D211/14 , C07D213/82 , C07D215/50 , C07D217/04 , C07D217/26 , C07D295/13
摘要： A compound of formula (I) ##STR1## in which: X denotes hydrogen, a halogen, a trifluoromethyl group, a C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.4 alkoxy group;R.sub.1 denotes a linear or branched C.sub.2 -C.sub.8 alkyl group, a C.sub.3 -C.sub.5 cycloalkyl group or a cycloalkylmethyl group in which the cycloalkyl moiety has from 3 to 5 carbon atoms;R.sub.2 denotes hydrogen or a C.sub.1 -C.sub.4 alkyl group;R.sub.3 denotes a pyridylalkyl group; andAr denotes a phenyl group, optionally having from one to three substituents, each of which is, independently, a halogen or a C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, trifluoromethyl; nitro or cyano group, or Ar denotes a naphthyl group;or a pharmacologically acceptable acid addition salt thereof.

37. 发明授权

US08080547B2 Triazolopyridine carboxamide derivatives and triazolopyrimidine carboxamide derivatives, preparation thereof and therapeutic use thereof 失效
标题翻译：三唑并吡啶甲酰胺衍生物和三唑并嘧啶甲酰胺衍生物，其制备及其治疗用途
公开(公告)号：US08080547B2
公开(公告)日：2011-12-20
申请号：US12573959
申请日：2009-10-06
申请人： Luc Even , Christian Hoornaert
发明人： Luc Even , Christian Hoornaert
IPC分类号： A61K31/4353 , A61K31/519 , C07D471/04
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention relates to the triazolopyridine carboxamide derivative and trizolopyrimidine carboxamide derivative of general Formula (I): Wherein X, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
摘要翻译：本发明涉及三唑并吡啶甲酰胺衍生物和通式（I）的三唑并嘧啶甲酰胺衍生物：其中X，R 1和R 2如本文所定义。本发明还涉及其制备方法及其治疗用途。

38. 发明授权

US07868007B2 Triazolopyridine carboxamide derivatives, preparation thereof and therapeutic use thereof 失效
标题翻译：三唑并吡啶甲酰胺衍生物，其制备及其治疗用途
公开(公告)号：US07868007B2
公开(公告)日：2011-01-11
申请号：US12573961
申请日：2009-10-06
申请人： Christian Hoornaert
发明人： Christian Hoornaert
IPC分类号： A61K31/4353 , A61K31/496 , C07D471/04
CPC分类号： C07D471/04
摘要： The invention relates to the triazolopyridine carboxamide derivatives of general formula (I): Wherein X, A, R1 and R2 are as defined herein. The invention further relates to preparation methods and therapeutic use thereof.
摘要翻译：本发明涉及通式（I）的三唑并吡啶甲酰胺衍生物：其中X，A，R 1和R 2如本文所定义。本发明还涉及其制备方法及其治疗用途。

39. 发明授权

US5472967A 4-pyrimidinone derivatives their preparation and their application in therapy 失效
标题翻译： 4-嘧啶酮衍生物的制备及其在治疗中的应用
公开(公告)号：US5472967A
公开(公告)日：1995-12-05
申请号：US294023
申请日：1994-08-24
申请人： Christian Hoornaert , Marc Daumas , Michel Aletru , Jean-Claude Muller
发明人： Christian Hoornaert , Marc Daumas , Michel Aletru , Jean-Claude Muller
IPC分类号： C07D239/36 , C07D239/52 , C07D403/10 , A61K31/505
CPC分类号： C07D239/36 , C07D239/52 , C07D403/10
摘要： Compounds which can be expressed as tautomeric forms and having the formulas (I), (I') and (I") ##STR1## wherein R.sub.1 =a straight or branched (C.sub.1-7) alkyl group or a straight or branched (C.sub.3-9) alkenyl group or a cyclo(C.sub.3-7)alkyl(C.sub.1-6) alkyl group, R.sub.2 =an atom of hydrogen, or a straight or branched (C.sub.1-7)alkyl group, or a cyclo(C.sub.3-7)alkyl(C.sub.1-3)alkyl group, or an aryl(C.sub.1-3)alkyl group optionally substituted on the ring, or an aryloxy(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylthio(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylsulfonyl(C.sub.1-3)alkyl group optionally substituted on the ring, or a heteroaryl(C.sub.1-3)alkyl group optionally substituted on the ring, R.sub.3 =CO.sub.2 H, 1H-tetrazol-5-yl, NHCOR.sub.11, NHSO.sub.2 R.sub.11, CONHSO.sub.2 R.sub.11 or CONHOR.sub.12 group where R.sub.11 =a methyl, trifluoromethyl, or phenyl group optionally substituted, R.sub.12 =a hydrogen atom, or a methyl or a phenyl group optionally substituted. The compounds are useful for antagonizing angiotensin II.
摘要翻译：可以表示为互变异构形式并具有式（I），（I'）和（I“）的化合物其中R 1 =直链或支链（C 1-7）烷基基团或直链或支链（C3-9）烯基或环（C3-7）烷基（C1-6）烷基，R2 =氢原子或直链或支链（C1-7）烷基，或环（C 3-7）烷基（C 1-3）烷基或任选在环上取代的芳基（C 1-3）烷基或任意在环上取代的芳氧基（C 1-3）烷基，或或环上任选取代的芳基磺酰基（C 1-3）烷基或环上任选取代的杂芳基（C 1-3）烷基，R 3 = CO 2 H ，1H-四唑-5-基，NHCOR 11，NHSO 2 R 11，CONHSO 2 R 11或CONHOR 12基团，其中R 11 =任选取代的甲基，三氟甲基或苯基，R 12 =氢原子或任选取代的甲基或苯基。该化合物可用于拮抗血管紧张素II。

40. 发明授权

US5371233A 2-(tetrazol-5-yl)-1,1'-biphenyl derivatives, their preparation and their use as synthetic intermediates 失效
标题翻译： 2-（四唑-5-基）-1,1'-联苯衍生物，其制备及其作为合成中间体的用途
公开(公告)号：US5371233A
公开(公告)日：1994-12-06
申请号：US998055
申请日：1992-12-29
申请人： Marc Daumas , Christian Hoornaert , Isaac Chekroun , Manuel Bedoya-Zurita , Jose Ruiz-Montes , Guy Rossey , Helene Greciet
发明人： Marc Daumas , Christian Hoornaert , Isaac Chekroun , Manuel Bedoya-Zurita , Jose Ruiz-Montes , Guy Rossey , Helene Greciet
IPC分类号： C07D257/04 , C07D403/10
CPC分类号： C07D257/04
摘要： Compounds corresponding to the formula (I) ##STR1## in which X represents dibromomethyl, formyl, (C.sub.1-4)alkyl, or a group CH(OR.sub.5).sub.2 or CH(OH)OR.sub.5, wherein the or each R.sub.5 is hydrogen (C.sub.1-3)alkyl or the two R.sub.5 's in the case of CH(OR.sub.5).sub.2 are linked to provide a 1,3-dioxolane or 1,3-dioxane ring, and Y represents hydrogen, 1,1-dimethylethyl, triphenylmethyl, trimethylstannyl, tributylstannyl, (1,1-dimethylethyl)dimethylsilyl, (1,1-dimethylethyl)diphenylsilyl, 2-cyanoethyl, or a group CH.sub.2 OR.sub.6 wherein R.sub.6 is methyl, phenylmethyl, 1,1-dimethylethyl, 2,2,2-trichloroethyl, benzyloxycarbonyl or 2,2,2-trichloroethyloxycarbonyl, Y being in position 1 or 2 on the tetrazole ring. The compounds of formula (I) are useful as intermediates in the synthesis of compounds possessing therapeutic activity.
摘要翻译：对应于式（I）的化合物其中X表示二溴甲基，甲酰基，（C 1-4）烷基或CH（OR 5）2或CH（OH）OR 5基团，其中每个R 5为氢（C 1-3）烷基或在CH（OR 5）2的情况下的两个R 5连接，得到1,3-二氧戊环或1,3-二恶烷环，Y代表氢，1,1-二甲基乙基，三苯基甲基，三甲基甲锡烷基，三丁基甲锡烷基，（1,1-二甲基乙基）二甲基甲硅烷基，（1,1-二甲基乙基）二苯基甲硅烷基，2-氰乙基或CH 2 OR 6，其中R 6是甲基，苯甲基，1,1-二甲基乙基，三氯乙基，苄氧基羰基或2,2,2-三氯乙氧基羰基，Y在四唑环上位于1或2位。式（I）的化合物可用作合成具有治疗活性的化合物的中间体。

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