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1. 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。

2. 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。

3. 发明授权

US07973042B2 Derivatives of alkylpiperazine- and alkylhomopiperazine-carboxylates, preparation method thereof and use of same as fatty acid amido hydrolase enzyme inhibitors 失效
标题翻译：烷基哌嗪和烷基高哌嗪羧酸衍生物的制备方法及其与脂肪酸酰氨基水解酶抑制剂的应用
公开(公告)号：US07973042B2
公开(公告)日：2011-07-05
申请号：US12334798
申请日：2008-12-15
申请人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Tak Adrien Li
发明人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Tak Adrien Li
IPC分类号： C07D241/04 , C07D295/00 , A61K31/4965
CPC分类号： C07D295/185 , C07D209/16 , C07D215/20 , C07D215/26 , C07D231/12 , C07D239/26 , C07D243/08 , C07D295/205
摘要： The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
摘要翻译：本发明包括烷基哌嗪和烷基高哌嗪羧酸盐及其衍生物，其制备方法及其作为脂肪酸酰氨基水解酶（FAAH）酶抑制剂的治疗用途。这些衍生物通过与大麻素和香草素受体的相互作用发挥各种药理活性。通过抑制FAAH酶的代谢活性，不会产生常常引起疾病发病和其他病理状况的化合物，并且疾病的发病率大大降低。

4. 发明申请

US20100279998A1 PIPERIDINYLALKYLCARBAMATE DERIVATIVES, METHODS FOR THEIR PREPARATION AND THE THERAPEUTIC USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 审中-公开
标题翻译：哌啶二甲酰胺衍生物，其制备方法及其作为脂肪酸酰胺酶水解酶抑制剂的治疗方法
公开(公告)号：US20100279998A1
公开(公告)日：2010-11-04
申请号：US12834267
申请日：2010-07-12
申请人： Ahmed ABOUABDELLAH , Antonio Almario Garcia , Christian Hoornaert , Jean Jeunesse
发明人： Ahmed ABOUABDELLAH , Antonio Almario Garcia , Christian Hoornaert , Jean Jeunesse
IPC分类号： A61K31/397 , C07D211/62 , A61K31/4468 , C07D401/06 , A61K31/4545 , C07D401/12 , A61K31/4709 , A61K31/506 , A61P25/06 , A61P31/22 , A61P3/10 , A61P29/00 , A61P19/02 , A61P19/06 , A61P1/00
CPC分类号： C07D207/09 , C07D205/04 , C07D211/26 , C07D211/58
摘要： The present invention relates to piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
摘要翻译：本发明涉及哌啶基烷基氨基甲酸酯衍生物，其制备方法及其作为脂肪酸酰氨基水解酶（FAAH）酶抑制剂的治疗用途。这些衍生物通过与大麻素和香草素受体的相互作用发挥各种药理活性。通过抑制FAAH酶的代谢活性，不会产生常常负责多种疾病和其他病理状况发生的化合物，并且疾病的发病率大大降低。

5. 发明申请

US20090088470A1 ALKYL-, ALKENYL- AND ALKYNYLCARBAMATE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS 审中-公开
标题翻译：阿尔茨基，亚苄基和烷基氨基甲酸酯衍生物，其制备及其在治疗中的应用
公开(公告)号：US20090088470A1
公开(公告)日：2009-04-02
申请号：US12328386
申请日：2008-12-04
申请人： Antonio ALMARIO-GARCIA , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
发明人： Antonio ALMARIO-GARCIA , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
IPC分类号： A61K31/27 , A61P25/24 , A61P25/22 , A61P25/28 , A61P25/08 , A61P25/14 , A61P25/16
CPC分类号： C07C271/12 , C07C271/24 , C07C2601/18
摘要： The invention relates to a compound of formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to methods of preparation of compounds of formula (I) as well as to their therapeutic application.
摘要翻译：本发明涉及式（I）化合物：其中R1，R2，R3和R4如本文所定义。本发明还涉及式（I）化合物的制备方法及其治疗应用。

6. 发明授权

US07476756B2 Alkyl-, alkenyl- and alkynylcarbamate derivatives, their preparation and their application in therapeutics 失效
标题翻译：烷基，链烯基和炔基氨基甲酸酯衍生物，其制备及其在治疗中的应用
公开(公告)号：US07476756B2
公开(公告)日：2009-01-13
申请号：US11874959
申请日：2007-10-19
申请人： Antonio Almario-Garcia , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
发明人： Antonio Almario-Garcia , Pascal George , Christian Hoornaert , Adrien Tak Li , Frederic Puech
IPC分类号： C07C269/04 , C07C271/08 , A61K31/27
CPC分类号： C07C271/12 , C07C271/24 , C07C2601/18
摘要： The invention relates to a compound of formula (I): Wherein R1, R2, R3 and R4 are as defined herein. The invention also relates to methods of preparation of compounds of formula (I) as well as to their therapeutic application.
摘要翻译：本发明涉及式（I）化合物：其中R1，R2，R3和R4如本文所定义。本发明还涉及式（I）化合物的制备方法及其治疗应用。

7. 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。

8. 发明申请

US20100120845A1 ARYLOXYALKYLCARBAMATE-TYPE DERIVATIVES, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS 有权
标题翻译： ARYLOXYALKYLCARBAMATE-TYPE衍生物，其制备方法及其在治疗中的应用
公开(公告)号：US20100120845A1
公开(公告)日：2010-05-13
申请号：US12691384
申请日：2010-01-21
申请人： Ahmed ABOUABDELLAH , Antonio Almario Garcia , Jacques Froissant , Christian Hoornaert
发明人： Ahmed ABOUABDELLAH , Antonio Almario Garcia , Jacques Froissant , Christian Hoornaert
IPC分类号： A61K31/4725 , A61K31/27 , A61K31/40 , A61K31/445
CPC分类号： C07D207/08 , C07C271/16 , C07D211/22 , C07D211/46 , C07D213/65 , C07D215/20 , C07D215/28 , C07D217/24 , C07D401/12
摘要： The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
摘要翻译：本发明涉及式（I）化合物：其中m，n，X，Y，R 1，R 2，R 3和R 4如本文所定义。本发明还涉及其在治疗中的用途。

9. 发明申请

US20100069405A1 DERIVATIVES OF HETEROARYL-ALKYLCARBAMATES, METHODS FOR THEIR PREPARATION AND USE THEREOF AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 审中-公开
标题翻译：异喹啉酮的衍生物，其制备方法及其作为脂肪酸氨基水解酶酶抑制剂的用途
公开(公告)号：US20100069405A1
公开(公告)日：2010-03-18
申请号：US12625125
申请日：2009-11-24
申请人： Ahmed Abouabdellah , Regine Bartsch-Li , Christian Hoornaert , Antoine Ravet
发明人： Ahmed Abouabdellah , Regine Bartsch-Li , Christian Hoornaert , Antoine Ravet
IPC分类号： A61K31/27 , C07D213/56 , C07D209/08 , C07C271/12 , C07D261/08 , C07D239/26 , C07D271/06 , C07D215/00 , C07D217/00 , A61K31/4418 , A61K31/404 , A61K31/42 , A61K31/505 , A61K31/47 , A61P25/00
CPC分类号： C07D213/54 , C07C271/12 , C07D209/08 , C07D213/40 , C07D215/04 , C07D215/12 , C07D215/227 , C07D217/14 , C07D231/12 , C07D233/64 , C07D235/06 , C07D239/26 , C07D239/42 , C07D261/14 , C07D273/02 , C07D413/04 , C07D471/04
摘要： The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ischaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula (I): wherein A, n, R1, R7 and R8 are as defined herein.
摘要翻译：本发明涉及用于治疗神经系统疾病的化合物和组合物，其引起神经源性和神经性疼痛，炎症性疾病，肾缺血，心血管疾病和由内源性大麻素及其代谢活性产生的其它底物引起的其它病症脂肪酸酰胺水解酶（FAAH）。这些化合物由式（I）表示：其中A，n，R 1，R 7和R 8如本文所定义。

10. 发明申请

US20070027141A1 DERIVATIVES OF ALKYLPIPERAZINE AND ALKYLHOMOPIPERAZINE-CARBOXYLATES, PREPARATION METHOD THEREOF AND USE OF SAME AS FATTY ACID AMIDO HYDROLASE ENZYME INHIBITORS 失效
标题翻译：烷基哌嗪和烷基二磷杂环己烷羧酸的衍生物，其制备方法及其作为脂肪酸氨基水解酶酶抑制剂的用途
公开(公告)号：US20070027141A1
公开(公告)日：2007-02-01
申请号：US11466192
申请日：2006-08-22
申请人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Tak Li
发明人： Ahmed Abouabdellah , Antonio Almario Garcia , Christian Hoornaert , Tak Li
IPC分类号： A61K31/551 , A61K31/506 , A61K31/496 , A61K31/495 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号： C07D295/185 , C07D209/16 , C07D215/20 , C07D215/26 , C07D231/12 , C07D239/26 , C07D243/08 , C07D295/205
摘要： The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.
摘要翻译：本发明包括烷基哌嗪和烷基高哌嗪羧酸盐及其衍生物，其制备方法及其作为脂肪酸酰氨基水解酶（FAAH）酶抑制剂的治疗用途。这些衍生物通过与大麻素和香草素受体的相互作用发挥各种药理活性。通过抑制FAAH酶的代谢活性，不会产生常常引起疾病发病和其他病理状况的化合物，并且疾病的发病率大大降低。

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