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1. 发明申请

US20050245747A1 Thio-substituted biaryl-methanesulfinyl derivatives 有权
标题翻译：硫取代的联芳基 - 甲亚磺酰基衍生物
公开(公告)号：US20050245747A1
公开(公告)日：2005-11-03
申请号：US11104091
申请日：2005-04-12
申请人： Edward Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
发明人： Edward Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07D205/04 , C07D207/16 , C07D207/325 , C07D207/333 , C07D209/10 , C07D209/48 , C07D211/74 , C07D213/34 , C07D213/40 , C07D215/12 , C07D261/08 , C07D295/185 , C07D307/38 , C07D307/79 , C07D317/56 , C07D319/18 , C07D319/20 , C07D321/10 , C07D327/08 , C07D333/18 , C07D333/28 , C07D333/54 , C07D345/00 , C07D405/12 , C07D409/12 , C07D249/16 , C07D209/18 , C07D235/04 , C07D249/08 , C07D403/02
CPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07D207/325 , C07D207/333 , C07D209/48 , C07D213/40 , C07D295/185 , C07D307/38 , C07D307/79 , C07D333/54
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
摘要翻译：本发明涉及化学组成，其制备方法和组合物的用途。特别地，本发明涉及包含式（I）的取代的联芳基 - 甲亚磺酰基乙酰胺的组合物：其中Ar，Y，R 1，R 2，R 2， 4，R 5，q和x如本文所定义; 及其用于治疗疾病的用途，包括治疗与发作性睡眠相关的嗜睡，阻塞性睡眠呼吸暂停或转移工作障碍; 帕金森病阿尔茨海默氏病; 注意力缺陷障碍注意缺陷多动障碍; 萧条; 或与神经系统疾病相关的疲劳; 以及促进觉醒。

2. 发明授权

US07981907B2 Thio-substituted biarylmethanesulfinyl derivatives 有权
标题翻译：硫取代的联芳基甲亚磺酰基衍生物
公开(公告)号：US07981907B2
公开(公告)日：2011-07-19
申请号：US12199167
申请日：2008-08-27
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： A61K31/445
CPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07D207/325 , C07D207/333 , C07D209/48 , C07D213/40 , C07D295/185 , C07D307/38 , C07D307/79 , C07D333/54
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
摘要翻译：本发明涉及化学组成，其制备方法和组合物的用途。特别地，本发明涉及包含式（I）的取代的联芳基 - 甲亚磺酰基乙酰胺的组合物：其中Ar，Y，R 1，R 2，R 4，R 5，q和x如本文所定义; 及其用于治疗疾病的用途，包括治疗与发作性睡眠相关的嗜睡，阻塞性睡眠呼吸暂停或转移工作障碍; 帕金森病阿尔茨海默氏病; 注意力缺陷障碍注意缺陷多动障碍; 萧条; 或与神经系统疾病相关的疲劳; 以及促进觉醒。

3. 发明授权

US07449481B2 Thio-substituted biaryl-methanesulfinyl derivatives 有权
标题翻译：硫取代的联芳基 - 甲亚磺酰基衍生物
公开(公告)号：US07449481B2
公开(公告)日：2008-11-11
申请号：US11104091
申请日：2005-04-12
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： A61K31/445 , C07D333/02
CPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07D207/325 , C07D207/333 , C07D209/48 , C07D213/40 , C07D295/185 , C07D307/38 , C07D307/79 , C07D333/54
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
摘要翻译：本发明涉及化学组成，其制备方法和组合物的用途。特别地，本发明涉及包含式（I）的取代的联芳基 - 甲亚磺酰基乙酰胺的组合物：其中Ar，Y，R 1，R 2，R 2， 4，R 5，q和x如本文所定义; 及其用于治疗疾病的用途，包括治疗与发作性睡眠相关的嗜睡，阻塞性睡眠呼吸暂停或转移工作障碍; 帕金森病阿尔茨海默氏病; 注意力缺陷障碍注意缺陷多动障碍; 萧条; 或与神经系统疾病相关的疲劳; 以及促进觉醒。

4. 发明申请

US20090062284A1 Thio-Substituted Biarylmethanesulfinyl Derivatives 有权
标题翻译：硫取代的二芳基甲亚磺酰基衍生物
公开(公告)号：US20090062284A1
公开(公告)日：2009-03-05
申请号：US12199167
申请日：2008-08-27
申请人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg A. Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
发明人： Edward R. Bacon , Sankar Chatterjee , Derek Dunn , Marie-Edith Gourdel , Greg A. Hostetler , Mohamed Iqbal , Brigitte Lesur , Philippe Louvet , Eric Riguet , Dominique Schweizer , Christophe Yue
IPC分类号： A61K31/381 , C07D333/24 , C07D307/54 , C07D409/12 , C07D405/12 , C07D401/12 , C07D413/12 , C07D209/44 , C07C235/72 , A61K31/496 , A61K31/40 , A61K31/4025 , A61K31/5377 , A61P25/00
CPC分类号： C07C317/10 , C07C317/44 , C07C323/65 , C07C2601/04 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2601/18 , C07D207/325 , C07D207/333 , C07D209/48 , C07D213/40 , C07D295/185 , C07D307/38 , C07D307/79 , C07D333/54
摘要： The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions that include substituted biaryl-methanesulfinyl acetamides of Formula (I): wherein Ar, Y, R1, R2, R4, R5, q and x are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness associated with narcolepsy, obstructive sleep apnea, or shift work disorder; Parkinson's disease; Alzheimer's disease; attention deficit disorder; attention deficit hyperactivity disorder; depression; or fatigue associated with a neurological disease; as well as the promotion of wakefulness.
摘要翻译：本发明涉及化学组成，其制备方法和组合物的用途。特别地，本发明涉及包含式（I）的取代的联芳基 - 甲亚磺酰基乙酰胺的组合物：其中Ar，Y，R 1，R 2，R 4，R 5，q和x如本文所定义; 及其用于治疗疾病的用途，包括治疗与发作性睡眠相关的嗜睡，阻塞性睡眠呼吸暂停或转移工作障碍; 帕金森病阿尔茨海默氏病; 注意力缺陷障碍注意缺陷多动障碍; 萧条; 或与神经系统疾病相关的疲劳; 以及促进觉醒。

5. 发明授权

US09546150B2 Substituted quinazolin-4-ones for inhibiting ubiquitin specific protease 7 有权
标题翻译：用于抑制泛素特异性蛋白酶的取代喹唑啉-4-酮7
公开(公告)号：US09546150B2
公开(公告)日：2017-01-17
申请号：US14241923
申请日：2012-08-29
申请人： Frédéric Colland , Marie-Edith Gourdel
发明人： Frédéric Colland , Marie-Edith Gourdel
IPC分类号： A61K31/517 , C07D239/88 , C07D401/06 , C07D409/14 , C07D239/91 , A61K45/06
CPC分类号： C07D401/06 , A61K31/517 , A61K45/06 , C07D239/88 , C07D239/91 , C07D409/14
摘要： The present invention relates to quinazolin-4-one compounds of formula (I′), their process of preparation and uses thereof. These compounds are useful as selective and reversible inhibitors of ubiquitin specific proteases, particularly USP7, for treating e.g. cancer, neurodegenerative diseases, inflammatory disorders and viral infections.
摘要翻译：本发明涉及式（I）化合物及其制备方法及用途。这些化合物可用作泛素特异性蛋白酶的选择性和可逆抑制剂，特别是USP7，用于治疗例如。癌症，神经变性疾病，炎性疾病和病毒感染。

6. 发明申请

US20100093784A1 NOVEL HETEROCYCLIC NITROGENOUS COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL MEDICAMENTS 失效
标题翻译：新型杂环化合物，其制备及其作为抗菌药物使用
公开(公告)号：US20100093784A1
公开(公告)日：2010-04-15
申请号：US12536034
申请日：2009-08-05
申请人： Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
发明人： Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
IPC分类号： A61K31/439 , C07D471/02 , A61P31/04
CPC分类号： C07D487/18
摘要： The invention relates to nitrogenous heterocyclic compounds of formula in which: R1 represents hydrogen, —(CH2)m—NH2, —(CH2)m—NH(C1-C6)alk, —(CH2)m—N(C1-C6)alk2, —(CH2)m—NH—C(NH)NH2 or —(CH2)m—NH—CH═NH, m is equal to 1 or 2; R2 and R3 together form a nitrogenous heterocycle of aromatic character with 5 vertices containing 1, 2 or 3 nitrogen atoms, substituted on a nitrogen atom by R4; R4 represents hydrogen, C1-C6)alk or a chain of formula: -(A)n-(NH)o—(CH2)p—(CHR′)qR″ A represents C═O, C═NH or SO2; R′ represents hydrogen or carboxy.
摘要翻译：本发明涉及下式的含氮杂环化合物，其中：R1表示氢， - （CH2）m -NH2， - （CH2）m-NH（C1-C6）烷基， - （CH2）m-N（C1-C6）烷基， - （CH2）m-NH-C（NH）NH2或 - （CH2）m-NH-CH = NH，m等于1或2; R2和R3一起形成芳族字符的含氮杂环，其中5个顶点含有1,2或3个氮原子，在氮原子上被R4取代; R 4表示氢，C 1 -C 6烷基或下式的链： - （A）n-（NH）o-（CH 2）p - （CHR'）q R“A表示C = O，C = NH或SO 2; R'表示氢或羧基。

7. 发明申请

US20100087648A1 NOVEL NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS, THEIR PREPARATION AND THEIR USE AS ANTIBACTERIAL DRUGS 失效
标题翻译：新型含氮杂环化合物，其制备及其作为抗菌药物使用
公开(公告)号：US20100087648A1
公开(公告)日：2010-04-08
申请号：US12536096
申请日：2009-08-05
申请人： Maxime Lampilas , David Rowlands , Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
发明人： Maxime Lampilas , David Rowlands , Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
IPC分类号： C07D471/06
CPC分类号： C07D471/18
摘要： The invention relates to nitrogen-containing heterocyclic compounds of general formula (I) wherein: R1 represents a (CH2)n—NH2 radical, n being equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 form together a nitrogen-containing heterocycle with aromaticity with 5 apices containing 1, 2 or 3 nitrogen atoms, substituted on this nitrogen atom or one of these nitrogen atoms with a (CH2)m—(C(O))p—R5 group, m being equal to 0, 1, 2 or 3, p being equal to 0 or 1 and R5 representing a hydroxy group, in which case p is equal to 1, or an amino, (C1-C6)alkyl or di-(C1-C6)alkyl amino, a nitrogen-containing heterocycle with aromaticity with 5 or 6 apices containing 1 or 2 nitrogen atoms and if necessary, an oxygen or sulfur atom; it being understood that when the sub-group (C(O))p—R5 forms a carboxy, amino, (C1-C6) alkyl or di-(C1-C6) alkyl amino, group, m is different from 0 or 1; in free form or as zwitterions and salts with pharmaceutically acceptable mineral or organic bases and acids, to their preparation and to their use as antibacterial drugs.
摘要翻译：本发明涉及通式（I）的含氮杂环化合物，其中：R1表示（CH2）n-NH2基，n等于1或2; R2表示氢原子; R3和R4一起形成具有芳香性的含氮杂环，其中含有1,2或3个氮原子的5个顶点，在该氮原子上被这些氮原子取代，或者与（CH 2）m - （C（O） R5基团，m等于0,1,2或3，p等于0或1，R5表示羟基，在这种情况下p等于1，或氨基，（C 1 -C 6）烷基或二 - （C1-C6）烷基氨基，具有芳香性的含有5或6个含有1或2个氮原子的顶点的含氮杂环，如果需要，含氧或硫原子; 应理解，当亚组（C（O））p -R 5形成羧基，氨基，（C 1 -C 6）烷基或二 - （C 1 -C 6）烷基氨基时，m不同于0或1 ; 游离形式或与药学上可接受的矿物或有机碱和酸的两性离子和盐与其制备和作为抗菌药物的用途。

8. 发明申请

US20140371247A1 Selective and Reversible Inhibitors of Ubiquitin Specific Protease 7 有权
标题翻译：泛素特异性蛋白酶的选择性和可逆抑制剂7
公开(公告)号：US20140371247A1
公开(公告)日：2014-12-18
申请号：US14241923
申请日：2012-08-29
申请人： Frédéric Colland , Marie-Edith Gourdel
发明人： Frédéric Colland , Marie-Edith Gourdel
IPC分类号： C07D401/06 , A61K45/06 , C07D409/14 , A61K31/517
CPC分类号： C07D401/06 , A61K31/517 , A61K45/06 , C07D239/88 , C07D239/91 , C07D409/14
摘要： The present invention relates to quinazolin-4-one compounds of formula (I′), their process of preparation and uses thereof. These compounds are useful as selective and reversible inhibitors of ubiquitin specific proteases, particularly USP7, for treating e.g. cancer, neurodegenerative diseases, inflammatory disorders and viral infections.
摘要翻译：本发明涉及式（I'）的喹唑啉-4-酮化合物，其制备方法及用途。这些化合物可用作泛素特异性蛋白酶的选择性和可逆抑制剂，特别是USP7，用于治疗例如。癌症，神经变性疾病，炎性疾病和病毒感染。

9. 发明授权

US08148366B2 Substituted pyrazolo[3,4-E][diazepin-6-5(H)ones and analogues thereof, their preparation and their use as antibacterial medicaments 失效
标题翻译：取代的吡唑并[3,4-E] [二氮杂-6-5（H））及其类似物，其制备及其作为抗菌药物的用途
公开(公告)号：US08148366B2
公开(公告)日：2012-04-03
申请号：US12536034
申请日：2009-08-05
申请人： Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
发明人： Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
IPC分类号： A61K31/55
CPC分类号： C07D487/18
摘要： The invention relates to nitrogenous heterocyclic compounds of formula (I): in which: R1 represents hydrogen, —(CH2)m—NH2, —(CH2)m—NH(C1-C6)alk, —(CH2)m—N(C1-C6)alk2, —(CH2)m—NH—C(NH)NH2 or —(CH2)m—NH—CH═NH, m is equal to 1 or 2; R2 and R3 together form a nitrogenous heterocycle of aromatic character with 5 vertices containing 1, 2 or 3 nitrogen atoms, substituted on a nitrogen atom by R4; R4 represents hydrogen, C1-C6)alk or a chain of formula: -(A)n-(NH)o—(CH2)p—(CHR′)qR″ A represents C═O, C═NH or SO2; R′ represents hydrogen or carboxy.
摘要翻译：本发明涉及式（I）的含氮杂环化合物：其中：R1表示氢， - （CH2）m -NH2， - （CH2）m-NH（C1-C6）烷基， - （CH2）m-N C1-C6）烷基， - （CH2）m-NH-C（NH）NH2或 - （CH2）m-NH-CH = NH，m等于1或2; R2和R3一起形成芳族字符的含氮杂环，其中5个顶点含有1,2或3个氮原子，在氮原子上被R4取代; R 4表示氢，C 1 -C 6烷基或下式的链： - （A）n-（NH）o-（CH 2）p - （CHR'）q R“A表示C = O，C = NH或SO 2; R'表示氢或羧基。

10. 发明授权

US08067435B2 Nitrogen-containing heterocyclic compounds, their preparation and their use as antibacterial drugs 失效
标题翻译：含氮杂环化合物，其制备及其用作抗菌药物
公开(公告)号：US08067435B2
公开(公告)日：2011-11-29
申请号：US12536096
申请日：2009-08-05
申请人： Maxime Lampilas , David Rowlands , Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
发明人： Maxime Lampilas , David Rowlands , Benoit Ledoussal , Marie-Edith Gourdel , Emilie Renaud , Camille Pierres , Adel Kebsi
IPC分类号： C07D471/06
CPC分类号： C07D471/18
摘要： The invention relates to nitrogen-containing heterocyclic compounds of general formula (I) wherein: R1 represents a (CH2)n—NH2 radical, n being equal to 1 or 2; R2 represents a hydrogen atom; R3 and R4 form together a nitrogen-containing heterocycle with aromaticity with 5 apices containing 1, 2 or 3 nitrogen atoms, substituted on this nitrogen atom or one of these nitrogen atoms with a (CH2)m—(C(O))p—R5 group, m being equal to 0, 1, 2 or 3, p being equal to 0 or 1 and R5 representing a hydroxy group, in which case p is equal to 1, or an amino, (C1-C6)alkyl or di-(C1-C6)alkyl amino, a nitrogen-containing heterocycle with aromaticity with 5 or 6 apices containing 1 or 2 nitrogen atoms and if necessary, an oxygen or sulfur atom; it being understood that when the sub-group (C(O))p—R5 forms a carboxy, amino, (C1-C6) alkyl or di-(C1-C6) alkyl amino, group, m is different from 0 or 1; in free form or as zwitterions and salts with pharmaceutically acceptable mineral or organic bases and acids, to their preparation and to their use as antibacterial drugs.
摘要翻译：本发明涉及通式（I）的含氮杂环化合物，其中：R1表示（CH2）n-NH2基，n等于1或2; R2表示氢原子; R3和R4一起形成具有芳香性的含氮杂环，其中含有1,2或3个氮原子的5个顶点，在该氮原子上被这些氮原子取代，或者与（CH 2）m - （C（O） R5基团，m等于0,1,2或3，p等于0或1，R5表示羟基，在这种情况下p等于1，或氨基，（C 1 -C 6）烷基或二 - （C1-C6）烷基氨基，具有芳香性的含有5或6个含有1或2个氮原子的顶点的含氮杂环，如果需要，含氧或硫原子; 应理解，当亚组（C（O））p -R 5形成羧基，氨基，（C 1 -C 6）烷基或二 - （C 1 -C 6）烷基氨基时，m不同于0或1 ; 游离形式或与药学上可接受的矿物或有机碱和酸的两性离子和盐与其制备和作为抗菌药物的用途。

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