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1.发明授权Derivatives of heterocycles with 5 members, their preparation and their use as medicaments 有权具有5个成员的杂环衍生物，其制备及其作为药物的用途公开(公告)号：US07956075B2
公开(公告)日：2011-06-07
申请号：US12001439
申请日：2007-12-11
申请人： Pierre-Etienne Chabrier De Lassauniere , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
发明人： Pierre-Etienne Chabrier De Lassauniere , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
IPC分类号： A61K31/425 , C07D277/28
CPC分类号： C07D277/28 , A61K31/417 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , C07D233/64 , C07D261/04 , C07D263/32 , C07D277/24 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/04 , C07D417/06
摘要： The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl and Ω is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl. These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.
摘要翻译： 本发明涉及噻唑，恶唑，咪唑，异恶唑和其中Het为噻唑，恶唑，咪唑，异恶唑或异恶唑啉的通式（I）的异恶唑啉衍生物，n为0至6的整数，A特别选自各种任选取代的 芳基，B特别是氢，烷基或苯基，R 1和R 2特别独立地是氢，烷基或环烷基，和OHgr; 是-NR46R47或-OR48，R46和R47独特地是氢，烷基，环烷基或 - （CH2）k-COOR51，R51尤其是烷基或卤代烷基，R48特别是氢或烷基。 这些化合物具有有利的药理学性质，其允许其用于治疗学，特别是用于治疗神经变性疾病或疼痛。
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公开(公告)号：US20050234118A1
公开(公告)日：2005-10-20
申请号：US10517267
申请日：2003-07-24
IPC分类号： C07D233/64 , A61K31/4164 , A61K31/4178 , A61P1/04 , A61P1/14 , A61P3/04 , A61P3/10 , A61P9/00 , A61P9/06 , A61P9/10 , A61P11/00 , A61P11/02 , A61P11/06 , A61P15/00 , A61P15/10 , A61P15/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/32 , A61P25/36 , A61P27/02 , A61P27/16 , A61P29/00 , A61P29/02 , A61P31/12 , A61P31/18 , A61P31/22 , A61P33/00 , A61P35/00 , A61P37/06 , A61P37/08 , A61P39/02 , A61P43/00 , C07D409/12 , C07D409/14 , C07D49/02
CPC分类号： C07D409/12 , C07D409/14
摘要： The invention concerns compounds of general formula (1) wherein R1 represents H, alkyl,cycloalkyl or cycloalkylalkyl and R2 represents H or alkyl; R3 represents H, alkyl or aralkyl; X represents a bond or a linear or branched alkylene radical (II); Y represents H, cycloalkyl, OR14, SR15, NR4R5 or A represents a bond or phenyl; B and B′ are independently selected among alkyl, NR6R7, SR8 and carbocyclic aryl orheterocyclic aryl radicals with five or six members optionally substituted; R4 represents H, alkyl, aryl, cycloalkyl, cycloalkylalkyl, aralkyl, C(O)R9, C(O)OR9, —C(O)NHR9 or —SO2R9, or further aryl or aralkyl whereof the aromatic ring is optionally substituted and R5 represents in particular H or alkyl, or further R, and R5 form with the nitrogen atom bearing them a non-aromatic hetcrocycle of five to seven members optionally substituted; R6 represents (in particular) II or alkyl and R7 represents (in particular) II or alkyl; R8 represents an alkyl radical optionally substituted; R9 represents alkyl, haloakyl, cycloalkyl or cycloalkylalkyl, or further one of the aralkyl or aryl or heteroaryl radicals optionally substituted; R14 and R15 independently represent (in particular) alkyl, phenyl or aralkyl. The compounds of general formula (I) can be used as NO synthase inhibitors and as modulators of sodium channels (for treating pains, multiple sclerosis, the central nervous system or the peripheral nervous system and the like).
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3.发明申请New analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them 有权喜树碱的新类似物，它们作为药物的用途和含有他们的药物组合物公开(公告)号：US20050038064A1
公开(公告)日：2005-02-17
申请号：US10930622
申请日：2004-08-31
申请人： Dennis Bigg , Olivier Lavergne , Francesc Rodas , Jacques Pommier , Gerard Ulibarri , Jerry Harnett , Alain Rolland , Anne-Marie Liberatore , Christophe Lanco , Jean-Bernard Cazaux , Christine Le Breton , Eric Manginot
发明人： Dennis Bigg , Olivier Lavergne , Francesc Rodas , Jacques Pommier , Gerard Ulibarri , Jerry Harnett , Alain Rolland , Anne-Marie Liberatore , Christophe Lanco , Jean-Bernard Cazaux , Christine Le Breton , Eric Manginot
IPC分类号： C07D213/61 , C07D213/64 , C07D471/14 , C07D491/04 , C07D491/22 , C07D498/22
CPC分类号： C07D213/64 , C07D213/61 , C07D471/14 , C07D491/04
摘要： A compound of the formula wherein the substituents are defined as in the specification which compounds are useful in the treatment of cancer.
摘要翻译： 下式的化合物，其中取代基如本说明书中所定义，其中该化合物可用于治疗癌症。
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4.发明申请DERIVATIVES OF HETEROCYCLES WITH 5 MEMBERS, THEIR PREPARATION AND THEIR USE AS MEDICAMENTS 有权具有5个成员的杂环化合物的衍生物，其制备及其作为药物的用途公开(公告)号：US20110172434A1
公开(公告)日：2011-07-14
申请号：US13053092
申请日：2011-03-21
申请人： Pierre-Etienne CHABRIER DE LASSAUNIERE , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
发明人： Pierre-Etienne CHABRIER DE LASSAUNIERE , Jeremiah Harnett , Dennis Bigg , Anne-Marie Liberatore , Jacques Pommier , Jacques Lannoy , Christophe Thurieau
IPC分类号： C07D277/28
CPC分类号： C07D277/28 , A61K31/417 , A61K31/4178 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , C07D233/64 , C07D261/04 , C07D263/32 , C07D277/24 , C07D403/04 , C07D403/06 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/04 , C07D417/06
摘要： The invention relates to thiazole, oxazole, imidazole, isoxazole and isoxazoline derivatives of general formula (I) wherein Het is thiazole, oxazole, imidazole, isoxazole or isoxazoline, n is an integer from 0 to 6, A is notably selected from various optionally substituted aromatic radicals, B is notably hydrogen, alkyl or phenyl, R1 and R2 are notably independently hydrogen, alkyl or cycloalkyl and Ω is —NR46R47 or —OR48, R46 and R47 are notably independently hydrogen, alkyl, cycloalkyl or —(CH2)k—COOR51, R51 is notably alkyl or haloalkyl and R48 is notably hydrogen or alkyl.These compounds have advantageous pharmacological properties which allow their use in therapeutics, notably for treating neurodegenerative disorders or pain.
摘要翻译： 本发明涉及噻唑，恶唑，咪唑，异恶唑和其中Het为噻唑，恶唑，咪唑，异恶唑或异恶唑啉的通式（I）的异恶唑啉衍生物，n为0至6的整数，A特别选自各种任选取代的 芳基，B特别是氢，烷基或苯基，R 1和R 2特别独立地是氢，烷基或环烷基，和OHgr; 是-NR46R47或-OR48，R46和R47独特地是氢，烷基，环烷基或 - （CH2）k-COOR51，R51尤其是烷基或卤代烷基，R48特别是氢或烷基。 这些化合物具有有利的药理学性质，其允许其用于治疗学，特别是用于治疗神经变性疾病或疼痛。
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5.发明申请公开(公告)号：US20100137275A1
公开(公告)日：2010-06-03
申请号：US12598842
申请日：2008-04-30
IPC分类号： A61K31/506 , C07D403/14 , C07D413/14 , C07D405/14 , C07D417/14 , C07D401/14 , A61K31/5377 , C07D239/42 , A61K31/505 , A61K31/498 , A61P35/00 , A61P35/02 , A61P33/00 , A61P31/00 , A61P29/00 , A61P25/28 , A61P17/14 , A61P37/06 , A61P37/08
CPC分类号： C07D239/50 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to the novel triaminopyrimidine derivatives of formula (I) in which R1, R2, W, R3, R4, and R5 are variable groups. These products have a Cdc25-phosphatase-inhibiting activity. The invention also relates to a process for synthesizing these compounds and also to therapeutic compositions containing these products and to the use thereof as medicaments.
摘要翻译： 本发明涉及式（I）的新颖的三氨基嘧啶衍生物，其中R1，R2，W，R3，R4和R5是可变基团。 这些产品具有Cdc25-磷酸酶抑制活性。 本发明还涉及一种合成这些化合物的方法，还涉及含有这些产物的治疗组合物及其作为药物的用途。
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公开(公告)号：US20090186930A1
公开(公告)日：2009-07-23
申请号：US12298757
申请日：2007-04-26
IPC分类号： A61K31/4164 , C07D233/58 , A61P35/00
CPC分类号： C07D233/64
摘要： The invention concerns novel imidazole derivatives of general formula (I), wherein Z′ and Z represent different variable groups. Said products have an antitumoral activity. The invention also concerns pharmaceutical compositions containing said products and their use for preparing antitumoral medicine.
摘要翻译： 本发明涉及通式（I）的新型咪唑衍生物，其中Z'和Z代表不同的可变基团。 所述产品具有抗肿瘤活性。 本发明还涉及含有所述产品的药物组合物及其用于制备抗肿瘤药物的用途。
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7.发明授权Analogues of camptothecin, their use as medicaments and the pharmaceutical compositions containing them 失效喜树碱的类似物，它们作为药物的用途以及含有他们的药物组合物公开(公告)号：US07053102B2
公开(公告)日：2006-05-30
申请号：US10862245
申请日：2004-06-07
申请人： Dennis Bigg , Olivier Lavergne , Francesc Pla Rodas , Jacques Pommier , Gerard Ulibarri , Jerry Harnett , Alain Rolland , Anne-Marie Liberatore , Christophe Lanco , Jean-Bernard Cazaux , Christine Le Breton , Eric Manginot
发明人： Dennis Bigg , Olivier Lavergne , Francesc Pla Rodas , Jacques Pommier , Gerard Ulibarri , Jerry Harnett , Alain Rolland , Anne-Marie Liberatore , Christophe Lanco , Jean-Bernard Cazaux , Christine Le Breton , Eric Manginot
IPC分类号： A61K31/47
CPC分类号： C07D213/64 , C07D213/61 , C07D471/14 , C07D491/04
摘要： Compositions for treating cancer comprising an amount of a camptothecin with a 7-ring β-hydroxy lactone ring of the formula wherein the substituents are defined as in the specification sufficient to treat cancer.
摘要翻译： 用于治疗癌症的组合物，其包含一定量的具有下式的7-环β-羟基内酯环的喜树碱，其中取代基如本说明书中所定义，足以治疗癌症。
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公开(公告)号：US20060069146A1
公开(公告)日：2006-03-30
申请号：US11281864
申请日：2005-11-17
IPC分类号： A61K31/4164
CPC分类号： C07D233/64 , A61K31/00 , A61K31/4164 , A61K31/4174
摘要： A method of treating cardiac rhythm disorders linked with neurodegenerating depression, bipolar disorders and irritable bowel disorders in warm-blooded animals in need thereof by administering a compound of the formula wherein the substituents are defined as in the specification.
摘要翻译： 一种在有需要的温血动物中治疗与神经退行性抑郁症，双相性精神障碍和肠易激综合障碍有关的心律紊乱的方法，其通过给予式
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9.发明授权Use of diazepines for preparing medicines for treating pathological conditions or diseases involving one of the growth hormone release inhibiting factor receptors 失效二氮杂用于制备用于治疗涉及生长激素释放抑制因子受体之一的病理状况或疾病的药物公开(公告)号：US07015213B1
公开(公告)日：2006-03-21
申请号：US09701893
申请日：1999-06-15
IPC分类号： A61K31/55 , C07D243/22 , C07D243/24 , C07D495/04 , C07D495/14
CPC分类号： C07D495/22
摘要： The invention concerns the use of pyrido-thieno-triazolo-diazepins for preparing a medicine for treating pathological conditions or diseases involving one of the growth hormone release inhibiting factor receptors. The invention also concerns novel pyrido-thieno-triazolo-diazepins and therapeutic compositions containing them.
摘要翻译： 本发明涉及吡啶并噻吩并三唑并二氮杂用于制备用于治疗涉及生长激素释放抑制因子受体之一的病理状况或疾病的药物。 本发明还涉及新颖的吡啶并噻吩并三氮唑并和含有它们的治疗组合物。
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10.发明申请TRIAMINOPYRIMIDINE CYCLOBUTENEDIONE DERIVATIVES USED AS PHOSPHATASE CDC25 INHIBITORS 审中-公开用作磷酸酶CDC25抑制剂的三亚氨基嘧啶环化酶衍生物公开(公告)号：US20100173910A1
公开(公告)日：2010-07-08
申请号：US12668999
申请日：2008-07-10
申请人： Anne-Marie Liberatore , Dominique Pons , Dennis Bigg , Grégorie Prevost , Marie-Christine Brezak Pannetier
发明人： Anne-Marie Liberatore , Dominique Pons , Dennis Bigg , Grégorie Prevost , Marie-Christine Brezak Pannetier
IPC分类号： A61K31/5377 , A61P35/00 , C07D403/12 , A61K31/506 , C07D413/12
CPC分类号： C07D239/50 , C07D213/74 , C07D257/04 , C07D317/66 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to triaminopyrimidine derivatives of formula (I) where Y, R3, W, R4a, R5a, R4b, R5b, n and m are variable. These compounds have CDC25 phosphatase-inhibiting activity and can therefore be used as drugs in diseases in which CDC25 phosphatases are involved. The invention also relates to pharmaceutical compositions containing said products and methods of using the drug.
摘要翻译： 本发明涉及式（I）的三氨基嘧啶衍生物，其中Y，R3，W，R4a，R5a，R4b，R5b，n和m是可变的。 这些化合物具有CDC25磷酸酶抑制活性，因此可用作涉及CDC25磷酸酶的疾病中的药物。 本发明还涉及含有所述产品的药物组合物和使用该药物的方法。
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