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1. 发明申请

WO2009127609A1 SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：螺旋体脱乙酰酶抑制剂的螺环衍生物
公开(公告)号：WO2009127609A1
公开(公告)日：2009-10-22
申请号：PCT/EP2009/054376
申请日：2009-04-14
申请人： DAC S.R.L. , VARASI, Mario , THALER, Florian , ABATE, Agnese , CARENZI, Giacomo , MERCURIO, Ciro , MINUCCI, Saverio
发明人： VARASI, Mario , THALER, Florian , ABATE, Agnese , CARENZI, Giacomo , MINUCCI, Saverio
IPC分类号： C07D471/10 , C07D491/107 , A61K31/527 , A61K31/438 , A61P35/00
CPC分类号： C07D498/10 , A61K31/438 , C07D471/10 , C07D491/107 , Y02A50/409 , Y02A50/411
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: the dotted line is an optional additional bond; n is zero or an integer from 1 to 4; R 1 is hydrogen; C 1 -C 6 alkyl, optionally substituted by cycloalkyl, aryl or by heteroaryl; (CO)R 3 ; (SO 2 )R 4 ; cycloalkyl; aryl; or heteroaryl; R 2 is C 1 -C 6 alkyl, optionally substituted by aryl or by heteroaryl; aryl; heteroaryl; or (CO)R 5 ; X is CH 2 , oxygen or NR 6 ; Y is a bond, CHR 7 or NR 8 ; Z is oxygen, CR 9 R 10 or C=R 11 ; and R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译：本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：虚线是任选的附加键; n为0或1至4的整数; R1是氢; 任选被环烷基，芳基或杂芳基取代的C 1 -C 6烷基; （CO）R 3; （SO 2）R 4; 环烷基; 芳基; 或杂芳基; R2是任选被芳基或杂芳基取代的C 1 -C 6烷基; 芳基; 杂; 或（CO）R5; X是CH 2，氧或NR 6; Y是一个键，CHR7或NR8; Z是氧，CR9R10或C = R11; R3，R4，R5，R6，R7，R8，R9，R10和R11在说明书中进一步定义; 及其药学上可接受的盐。

2. 发明申请

WO2009027395A1 A NEW CLASS OF HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：一类新型脱乙酰壳多糖酶抑制剂
公开(公告)号：WO2009027395A1
公开(公告)日：2009-03-05
申请号：PCT/EP2008/061140
申请日：2008-08-26
申请人： DAC S.R.L. , THALER, Florian , VARASI, Mario , MERCURIO, Ciro , MINUCCI, Saverio , COLOMBO, Andrea , GAGLIARDI, Stefania
发明人： THALER, Florian , VARASI, Mario , MERCURIO, Ciro , MINUCCI, Saverio , COLOMBO, Andrea , GAGLIARDI, Stefania
IPC分类号： C07D241/04 , C07D401/10 , C07D413/10 , A61K31/435 , A61P35/00
CPC分类号： C07D241/04 , C07D401/10 , C07D413/10
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH 2 , NR 5 or oxygen, X is CH or nitrogen, Y is a bond, CH 2 , oxygen or NR, Z is CH or nitrogen, R 1 , R 2 are, independently, hydrogen or C 1 -C 6 alkyl, R 3 , R 4 are, independently, hydrogen, halogen, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkyl or C 1 -C 6 haloalkoxy, and R 5 and R 6 are as further defined in the specification, and pharmaceutical acceptable salts thereof.
摘要翻译：本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：Q为键，CH2，NR5或氧，X为CH或氮，Y为键，CH2，氧或NR，Z为CH 或氮，R 1，R 2独立地为氢或C 1 -C 6烷基，R 3，R 4独立地为氢，卤素，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6卤代烷基或C 1 -C 6卤代烷氧基，和R6在说明书中进一步定义，及其药学上可接受的盐。

3. 发明申请

WO2004014374A1 BICYCLO-PYRAZOLES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：作为激酶抑制剂的双羟基磷酸酯，其制备和包含它们的药物组合物的方法
公开(公告)号：WO2004014374A1
公开(公告)日：2004-02-19
申请号：PCT/EP2003/007000
申请日：2003-07-01
申请人： PHARMACIA ITALIA S.P.A. , VILLA, Manuela , ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VULPETTI, Anna
发明人： VILLA, Manuela , ABRATE, Francesca , FANCELLI, Daniele , VARASI, Mario , VULPETTI, Anna
IPC分类号： A61K31/437
CPC分类号： C07D471/04
摘要： The present invention provides a method for treating diseases caused by and/or associated with an altered protein kinase activity which comprises administering to a mammal in need thereof an effective amount of a pyrazole-tetrahydro pyridine derivative. The invention also provides specific pyrazole-tetrahydro pyridines, a library comprising at least two of them, a process for their preparation and the pharmaceutical compositions containing them, which are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, viral infections, autoimmune diseases and neurodegenerative disorders.
摘要翻译：本发明提供了治疗由变化的蛋白激酶活性引起和/或与其相关的疾病的方法，其包括向有需要的哺乳动物施用有效量的吡唑 - 四氢吡啶衍生物。本发明还提供特异性的吡唑 - 四氢吡啶，其中包含其中至少两个的文库，其制备方法和含有它们的药物组合物，其可用于治疗由改变的蛋白激酶引起的和/或与其相关的疾病活动如癌症，细胞增殖性疾病，病毒感染，自身免疫性疾病和神经变性疾病。

4. 发明申请

WO0112189A8 3(5)-AMINO-PYRAZOLE DERIVATIVES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS ANTITUMOR AGENTS 审中-公开
标题翻译： 3（5） - 氨基吡唑衍生物及其制备方法及其作为抗菌剂的用途
公开(公告)号：WO0112189A8
公开(公告)日：2001-08-02
申请号：PCT/US0006699
申请日：2000-05-05
申请人： PHARMACIA & UPJOHN SPA , UPJOHN CO , PEVARELLO PAOLO , ORSINI PAOLO , TRAQUANDI GABRIELLA , VARASI MARIO , FRITZEN EDWARD L , WARPEHOSKI MARTHA A , PIERCE BETSY S , BRASCA MARIA GRABRIELLA
发明人： PEVARELLO PAOLO , ORSINI PAOLO , TRAQUANDI GABRIELLA , VARASI MARIO , FRITZEN EDWARD L , WARPEHOSKI MARTHA A , PIERCE BETSY S , BRASCA MARIA GRABRIELLA
IPC分类号： A61K31/415 , A61K31/4155 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/506 , A61K45/06 , A61P9/10 , A61P11/00 , A61P13/08 , A61P13/12 , A61P17/06 , A61P17/14 , A61P19/02 , A61P25/28 , A61P31/12 , A61P35/00 , A61P37/02 , A61P43/00 , C07D231/16 , C07D231/40 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D417/12
CPC分类号： C07D403/12 , A61K31/415 , A61K31/4155 , A61K45/06 , C07D231/16 , C07D231/40 , C07D405/12 , C07D409/12
摘要： Compounds which are 3-amino-pyrazole derivatives represented by formula (I) wherein R is C3-C6 cycloalkyl group optionally substituted by a straight or branched C1-C6 alkyl or arylalkyl group; R1 is a straight or branched C1-C6 alkyl, C2-C4 alkenyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, arylalkyl, arylcarbonyl, aryloxyalkyl or arylalkenyl group, each of which may be optionally further substituted as indicated in the description; or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer, cell proliferative disorders, Alzheimer's disease, viral infections, auto-immune diseases or neurodegenerative diseases.
摘要翻译：由式（I）表示的3-氨基 - 吡唑衍生物的化合物，其中R是任选被直链或支链C 1 -C 6烷基或芳烷基取代的C 3 -C 6环烷基; R1是直链或支链C 1 -C 6烷基，C 2 -C 4烯基，环烷基，环烯基，杂环基，芳基，芳基烷基，芳基羰基，芳氧基烷基或芳基烯基，其各自可以任选地进一步被取代，如说明书所述; 或其药学上可接受的盐。该化合物可用于治疗癌症，细胞增殖性疾病，阿尔茨海默病，病毒感染，自身免疫疾病或神经变性疾病。

5. 发明申请

WO9916753A3 TRICYCLIC 3-OXO-PROPANENITRILE COMPOUNDS 审中-公开
标题翻译：三聚3-氧代丙酰化合物
公开(公告)号：WO9916753A3
公开(公告)日：1999-05-20
申请号：PCT/EP9806051
申请日：1998-09-23
申请人： PHARMACIA & UPJOHN SPA , PEVARELLO PAOLO , VARASI MARIO , AMICI RAFFAELLA , TOMA SALVATORE , SPECIALE CARMELA
发明人： PEVARELLO PAOLO , VARASI MARIO , AMICI RAFFAELLA , TOMA SALVATORE , SPECIALE CARMELA
IPC分类号： C07D231/54 , A61K31/416 , A61K31/423 , A61K31/4738 , A61K31/4745 , A61P9/02 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/28 , A61P31/18 , A61P43/00 , C07D231/56 , C07D261/20 , C07D471/04 , C07D498/04 , A61K31/415 , A61K31/42 , A61K31/47
CPC分类号： C07D471/04 , C07D231/56 , C07D261/20
摘要： Tricyclic 3-oxo-propanenitrile compounds of formula (I), wherein Y represents a nitrogen atom or a CH or N-oxide group; X represents an oxygen atom or NR2 wherein R2 represents C1-C6 alkyl, benzyl, pyridyl or phenyl, the phenyl being unsubstituted or substituted by one or two substituents chosen independently from halogen, trifluoromethyl, C1-C6 alkyl, C1-C6 alkoxy, nitro, amino, formylamino and C2-C8 alkanoylamino; each of R and R1 is independently hydrogen, halogen, CF3, C1-C6 alkyl, hydroxy, C1-C6 alkoxy, C3-C4 alkenyloxy, nitro, amino, formylamino, C2-C8 alkanoylamino or C2-C8 alkanoyloxy; m is zero or an integer of 1 to 6; Q is C1-C14 alkyl, phenyl or unsaturated pentatomic heteromonocylic ring containing two or three heteroatoms chosen from oxygen, sulphur and nitrogen, wherein the phenyl ring and the heteromonocylic ring are unsubstituted or substituted by one or two substituents chosen independently from halogen, CF3, C1-C6 alkyl, hydroxy, C1-C6 alkoxy, nitro, amino, formylamino, C2-C8 alkanoylamino or C2-C8 alkanoyloxy; and W represents a -CONH- or -SO2- or -CO- group; and pharmaceutically acceptable salt thereof having kynurenine-3-hydroxylase enzyme inhibitor activity are provided.
摘要翻译：式（I）的三环3-氧代 - 丙腈化合物，其中Y表示氮原子或CH或N-氧化物基团; X表示氧原子或NR 2，其中R2表示C1-C6烷基，苄基，吡啶基或苯基，苯基未取代或被一个或两个独立地选自卤素，三氟甲基，C 1 -C 6烷基，C 1 -C 6烷氧基，硝基，氨基，甲酰氨基和C 2 -C 8烷酰基氨基; R 1和R 2各自独立地为氢，卤素，CF 3，C 1 -C 6烷基，羟基，C 1 -C 6烷氧基，C 3 -C 4烯氧基，硝基，氨基，甲酰氨基，C 2 -C 8烷酰基氨基或C 2 -C 8烷酰氧基。 m为0或1〜6的整数; Q是含有选自氧，硫和氮的两个或三个杂原子的C 1 -C 14烷基，苯基或不饱和五原子异单环，其中苯环和异单环是未取代的或被一个或两个独立地选自卤素，CF 3， C 1 -C 6烷基，羟基，C 1 -C 6烷氧基，硝基，氨基，甲酰氨基，C 2 -C 8烷酰基氨基或C 2 -C 8烷酰氧基; W表示-CONH-或-SO 2 - 或-CO-基团; 及其药学上可接受的盐具有犬尿苷-3-羟化酶抑制剂活性。

6. 发明申请

WO1998009938A1 N-SUBSTITUTED-2-AMINO-4-PHENYL-4-OXO-BUTANOIC ACID DERIVATIVES WITH KYNURENINE-3-HYDROXYLASE INHIBITORY ACTIVITY 审中-公开
标题翻译： N-取代-2-氨基-4-苯基-4-氧代 - 丁酸衍生物与奎宁尼-3-羟基酶抑制活性
公开(公告)号：WO1998009938A1
公开(公告)日：1998-03-12
申请号：PCT/EP1997004271
申请日：1997-07-31
申请人： PHARMACIA & UPJOHN S.P.A. , VARASI, Mario , GIORDANI, Antonio , CINI, Massimo , SPECIALE, Carmela , BIANCHETTI, Alberto
发明人： PHARMACIA & UPJOHN S.P.A.
IPC分类号： C07C229/36
CPC分类号： C07C233/47 , C07C311/06
摘要： N-substituted-2-amino-4-phenyl-4-oxo-butanoic acid compound of formula (I), wherein each of the groups X and Y is, independently, hydrogen; halogen; nitro; C1-C6 alkyl; C2-C4 alkenyl; C2-C4 alkynyl; C1-C6 alkoxy; C1-C6 alkylthio; SOR2 or SO2R2 in which R2 is C1-C6 alkyl, phenyl or benzyl; or SO2N(R3)2 in which each of the groups R3 is, independently, hydrogen, C1-C6 alkyl, C2-C4 alkenyl, C2-C4 alkynyl, phenyl or benzyl; R is hydroxy, -OR5 in which R5 is C1-C6 alkyl, C2-C4 alkenyl, C2-C4 alkynyl or benzyl; -N(R3)2 or -N(R3)OR3 in which each of R3 is as defined above; W is -COOR4, -COR4 or -SO2R4 in which R4 is C1-C6 alkyl, an optionally substituted C2-C4 alkenyl, an optionally substituted phenyl or benzyl; -CONHR5 or -CSNHR5 in which R5 is as defined above; trichloroacetyl; or trifluoroacetyl; or a pharmaceutically acceptable salts thereof, for use as a medicament, in particular as Kynurenine 3-hydroxylase inhibitor is disclosed.
摘要翻译：式（I）的N-取代-2-氨基-4-苯基-4-氧代 - 丁酸化合物，其中基团X和Y各自独立地为氢; 卤素; 硝基; C1-C6烷基; C 2 -C 4烯基; C2-C4炔基; C1-C6烷氧基; C1-C6烷硫基; SOR2或SO2R2，其中R2是C1-C6烷基，苯基或苄基; 或SO 2 N（R 3）2，其中基团R 3各自独立地为氢，C 1 -C 6烷基，C 2 -C 4烯基，C 2 -C 4炔基，苯基或苄基; R是羟基，-OR 5，其中R 5是C 1 -C 6烷基，C 2 -C 4烯基，C 2 -C 4炔基或苄基; -N（R3）2或-N（R3）OR3，其中R3各自如上所定义; W是-COOR 4，-COR 4或-SO 2 R 4，其中R 4是C 1 -C 6烷基，任选取代的C 2 -C 4烯基，任选取代的苯基或苄基; -CONHR 5或-CSNHR 5，其中R 5如上所定义; 三氯; 或三氟乙酰基; 或其药学上可接受的盐，用作药物，特别是Kynurenine 3-羟化酶抑制剂。

7. 发明申请

WO2013064919A9 QUINAZOLINE DERIVATIVES WITH HSP90 INHIBITORY ACTIVITY 审中-公开
标题翻译：具有HSP90抑制活性的喹唑啉衍生物
公开(公告)号：WO2013064919A9
公开(公告)日：2013-06-27
申请号：PCT/IB2012054649
申请日：2012-09-07
申请人： DAC SRL , AMICI RAFFAELLA , COLOMBO ANDREA , COURTNEY STEPHEN MARTIN , MERCURIO CIRO , MONTALBETTI CHRISTIAN ALDO GEORGES NAPOLEON , MORTONI ANNALISA , VARASI MARIO
发明人： AMICI RAFFAELLA , COLOMBO ANDREA , COURTNEY STEPHEN MARTIN , MERCURIO CIRO , MONTALBETTI CHRISTIAN ALDO GEORGES NAPOLEON , MORTONI ANNALISA , VARASI MARIO
IPC分类号： C07D401/10 , A61K31/517 , A61P35/00 , C07D401/14 , C07D451/06
CPC分类号： C07D401/10 , C07D401/14 , C07D451/06
摘要： Compounds of general formula (I): or a stereoisomer, tautomer, polymorph, hydrate, solvate, or a pharmaceutically acceptable salt thereof, wherein R is as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as proliferative diseases, e.g. cancers, viral and fungal infections, neurodegenerative or inflammatory diseases or conditions. The invention also relates to the preparation of these compounds as well as to pharmaceutical compositions comprising them.
摘要翻译：通式（I）的化合物：或其立体异构体，互变异构体，多晶型物，水合物，溶剂合物或其药学上可接受的盐，其中R如本文所定义，可用于治疗由过量或不适当介导的疾病和病症 Hsp90活性如增殖性疾病，例如癌症，病毒和真菌感染，神经变性或炎性疾病或病症。本发明还涉及这些化合物的制备以及包含它们的药物组合物。

8. 发明申请

WO2011067145A1 TRICYCLOPYRAZOLE DERIVATIVES 审中-公开
标题翻译：三羟甲基吡唑衍生物
公开(公告)号：WO2011067145A1
公开(公告)日：2011-06-09
申请号：PCT/EP2010/068129
申请日：2010-11-24
申请人： NERVIANO MEDICAL SCIENCES S.R.L. , DISINGRINI, Teresa , MANTEGANI, Sergio , VARASI, Mario
发明人： DISINGRINI, Teresa , MANTEGANI, Sergio , VARASI, Mario
IPC分类号： C07D487/14 , A61K31/435
CPC分类号： C07D487/14 , C07D207/34 , C07D471/14
摘要： Compounds which are tricyclopyrazole derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.
摘要翻译：公开了作为三环吡唑衍生物或其药学上可接受的盐的化合物，其制备方法和包含它们的药物组合物; 这些化合物可用于治疗由改变的蛋白激酶活性引起的和/或与其相关的疾病，例如癌症，病毒感染，HIV感染个体中的AIDS发展的预防，细胞增殖性疾病，自身免疫和神经变性疾病; 还公开了用于制备本发明化合物的固相合成条件和包含多个化合物的化学文库的方法。

9. 发明申请

WO2011045265A2 SPIROCYCLIC DERIVATIVES AS HISTONE DEACETYLASE INHIBITORS 审中-公开
标题翻译：螺旋体脱乙酰酶抑制剂的螺环衍生物
公开(公告)号：WO2011045265A2
公开(公告)日：2011-04-21
申请号：PCT/EP2010/065176
申请日：2010-10-11
申请人： DAC S.R.L. , VARASI, Mario , THALER, Florian , AMICI, Raffaella , ABATE, Agnese , FULCO, Maria Carmela , MINUCCI, Saverio , MERCURIO, Ciro
发明人： VARASI, Mario , THALER, Florian , AMICI, Raffaella , ABATE, Agnese , FULCO, Maria Carmela , MINUCCI, Saverio , MERCURIO, Ciro
IPC分类号： C07D491/10 , C07D498/10 , A61K31/35 , A61K31/407 , A61K31/438 , A61K31/537 , A61K31/55
CPC分类号： C07D491/10 , C07D498/10
摘要： This invention is related to new histone deacetylase inhibitors according to the general formula (I), wherein: m and n are independently zero or an integer from 1 to 4; p is zero or an integer from 1 to 3, with the proviso that when p is zero, n and m cannot be both 1; R is hydrogen; C 1 -C 6 alkyl, optionally substituted by C 3 -C 8 cycloalkyl, C 6 -C 10 aryl or hetero(C 2 -C 9 )aryl; (CO)R 2 ; (SO 2 )R 3 ; C 3 -C 8 cycloalkyl; C 6 -C 10 aryl; or hetero(C 2 -C 9 )aryl; R 1 is halogen, C 1 -C 6 alkyl, C 1 -C 6 haloalkyl, C 1 -C 6 alkoxy, C 1 -C 6 haloalkoxy; Y is CH 2 or NR 4 ; Z is C=R 5 ; and R 2 , R 3 , R 4 , and R 5 are as further defined in the specification; and pharmaceutical acceptable salts thereof.
摘要翻译：本发明涉及根据通式（I）的新的组蛋白脱乙酰酶抑制剂，其中：m和n独立地为0或1至4的整数; p为0或1至3的整数，条件是当p为零时，n和m不能同时为1; R是氢; 任选被C 3 -C 8环烷基，C 6 -C 10芳基或杂（C 2 -C 9）芳基取代的C 1 -C 6烷基; （CO）R 2; （SO 2）R 3; C3-C8环烷基; C6-C10芳基; 或杂（C 2 -C 9）芳基; R1是卤素，C1-C6烷基，C1-C6卤代烷基，C1-C6烷氧基，C1-C6卤代烷氧基; Y是CH 2或NR 4; Z为C = R5; R2，R3，R4和R5如说明书中进一步定义; 及其药学上可接受的盐。

10. 发明申请

WO2007068728A3 N-SUBSTITUTED PYRROLOPYRIDINONES ACTIVE AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的N-取代的吡咯烷酮
公开(公告)号：WO2007068728A3
公开(公告)日：2007-09-27
申请号：PCT/EP2006069690
申请日：2006-12-13
申请人： PFIZER ITALIA SRL , VANOTTI ERMES , MENICHINCHERI MARIA , ORSINI PAOLO , SCOLARO ALESSANDRA , VARASI MARIO
发明人： VANOTTI ERMES , MENICHINCHERI MARIA , ORSINI PAOLO , SCOLARO ALESSANDRA , VARASI MARIO
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： Compounds represented by formula (I) wherein A, R1, R2, R3. R4, R5, and R6 are as defined in the specification, pharmaceutical compositions thereof, and methods of use thereof.
摘要翻译：由式（I）表示的化合物，其中A，R1，R2，R3。 R4，R5和R6如本说明书中所定义，其药物组合物及其使用方法。

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