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2. 发明申请

WO2009016132A1 PYRROLOPYRIMIDINES 审中-公开
标题翻译：的吡咯
公开(公告)号：WO2009016132A1
公开(公告)日：2009-02-05
申请号：PCT/EP2008/059833
申请日：2008-07-25
申请人： JANSSEN PHARMACEUTICA NV , DIELS, Gaston Stanislas Marcella , TEN HOLTE, Peter , FREYNE, Eddy Jean Edgard , GRAND-PERRET, Thierry Andre Regis , VAN EMELEN, Kristof , EMBRECHTS, Werner Constant Johan , BONNET, Pascal Ghislain André
发明人： DIELS, Gaston Stanislas Marcella , TEN HOLTE, Peter , FREYNE, Eddy Jean Edgard , GRAND-PERRET, Thierry Andre Regis , VAN EMELEN, Kristof , EMBRECHTS, Werner Constant Johan , BONNET, Pascal Ghislain André
IPC分类号： C07D487/08 , C07D498/08 , A61K31/529 , A61P35/02
CPC分类号： C07D498/08 , C07D487/08
摘要： The present invention relates to compounds or pharmaceutically-acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to compounds that are polo-like kinase (PLKs) inhibitors useful for the treatment of disease states mediated by PLK, especially PLK4, in particular such compounds that are useful in the treatment of pathological processes which involve an aberrant cellular proliferation, such as tumour growth, rheumatoid arthritis, restenosis and atherosclerosis.
摘要翻译：本发明涉及其化合物或药学上可接受的盐，其制备方法，含有它们的药物组合物及其在治疗中的用途。本发明特别涉及可用于治疗由PLK，特别是PLK4介导的疾病状态的polo样激酶（PLK）抑制剂的化合物，特别是可用于治疗涉及异常细胞增殖的病理过程的此类化合物，如肿瘤生长，类风湿关节炎，再狭窄和动脉粥样硬化。

3. 发明申请

WO2006061417A3 MACROCYCLIC QUINAZOLE DERIVATIVES AND THEIR USE AS MTKI 审中-公开
标题翻译：大分子喹唑啉衍生物及其作为MTKI的用途
公开(公告)号：WO2006061417A3
公开(公告)日：2006-08-03
申请号：PCT/EP2005056609
申请日：2005-12-08
申请人： JANSSEN PHARMACEUTICA NV , FREYNE EDDY JEAN EDGARD , WILLEMS MARC , TEN HOLTE PETER , PAPANIKOS ALEXANDRA , EMBRECHTS WERNER CONSTANT JOHA , STORCK PIERRE HENRI , PONCELET VIRGINIE SOPHIE
发明人： FREYNE EDDY JEAN EDGARD , WILLEMS MARC , TEN HOLTE PETER , PAPANIKOS ALEXANDRA , EMBRECHTS WERNER CONSTANT JOHA , STORCK PIERRE HENRI , PONCELET VIRGINIE SOPHIE
IPC分类号： C07D498/08 , A61K31/529 , A61P35/00 , C07D239/00 , C07D273/00
CPC分类号： C07D498/06 , C07D498/08
摘要： The present invention concerns kinase inhibitors formula, formula (I), the N-oxide forms, the pharmaceutically isomeric forms thereof, wherein Z represents NH and the other substituents are defined as in the claims.
摘要翻译：本发明涉及激酶抑制剂式（I），N-氧化物形式及其药学上异构体形式，其中Z表示NH且其它取代基如权利要求中所定义。

4. 发明申请

WO2006074984A1 PYRAZOLOPYRIMIDINES AS CELL CYCLE KINASE INHIBITORS 审中-公开
标题翻译：作为细胞周期激酶抑制剂的吡唑并嘧啶
公开(公告)号：WO2006074984A1
公开(公告)日：2006-07-20
申请号：PCT/EP2006/050096
申请日：2006-01-09
申请人： JANSSEN PHARMACEUTICA N.V. , FREYNE, Eddy, Jean, Edgard , LACRAMPE, Jean, Fernand, Armand , PERERA, Timothy, Pietro, Suren , TEN HOLTE, Peter , LIGNY, Yannick, Aimé, Eddy , LARDEAU, Delphine, Yvonne, Raymonde , LAVRIJSSEN, Tom
发明人： FREYNE, Eddy, Jean, Edgard , LACRAMPE, Jean, Fernand, Armand , PERERA, Timothy, Pietro, Suren , TEN HOLTE, Peter , LIGNY, Yannick, Aimé, Eddy , LARDEAU, Delphine, Yvonne, Raymonde , LAVRIJSSEN, Tom
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： This invention comprises the novel compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, X1 and X2 have defined meanings, having cell cycle kinase inhibiting enzymatic activity, their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明包括式（I）的新化合物，其中R 1，R 2，R 3，R 4，R 5，R 6，X 1和X 2具有定义的含义，具有抑制细胞周期激酶的酶活性，其制备方法，含有它们的组合物及其作为医学。

5. 发明申请

WO2004007498A2 3-PHENYL ANALOGS OF TOXOFLAVINE AS KINASE INHIBITORS 审中-公开
标题翻译：吡喹酮作为激酶抑制剂的3-苯基类似物
公开(公告)号：WO2004007498A2
公开(公告)日：2004-01-22
申请号：PCT/EP0350292
申请日：2003-07-08
申请人： JANSSEN PHARMACEUTICA NV , LACRAMPE JEAN FERNAND ARMAND , CONNORS RICHARD WILLIAM , HO CHIH YUNG , RICHARDSON ALAN , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , BAKKER ANNETTE CORNELIA
发明人： LACRAMPE JEAN FERNAND ARMAND , CONNORS RICHARD WILLIAM , HO CHIH YUNG , RICHARDSON ALAN , FREYNE EDDY JEAN EDGARD , BUIJNSTERS PETER JACOBUS JOHAN , BAKKER ANNETTE CORNELIA
IPC分类号： A61K31/53 , A61K31/5377 , A61P9/10 , A61P35/00 , A61P43/00 , C07D487/04 , C07D519/00
CPC分类号： C07D487/04
摘要： The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 0, 1 or 2; m represents an integer being 0 or 1; R represents C I -4alkyl; R represents C I -4alkyl; R represents CI-4alkyl; or R and R taken together with the carbon atom to which they are attached form a C3-8cycloalkyl or Het wherein said C3-8cycloalkyl or Het each independently may optionally be substituted with C1-4alkyloxycarbonyl; R represents halo or C I -4alkyloxy; R represents C 1-4alkyloxycarbonyl, -O-(mono- or di(C1-4alkyl)aminosulfonyl), CI-4alkyl substituted with one or where possible more substituent being selected from Het or NR R , C1-4alkyloxy substituted with one or where possible more substituents being selected from amino, Het or NR R ; R and R are each independently selected from hydrogen, C I-4alkyl, C I-4alkyloxyC1-4alkyl, -Het or CI-4alkyl substituted with one or where possible more substituents being selected from hydroxy, or Het ; R and R are each independently selected from hydrogen, C,1-4alkyl, -Het or mono- or di(C 1-4alkyl)aminosulphonyl; Het represents a heterocycle selected from piperidinyl, or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from hydroxy, aminosulfonyl, amino, mono-or di(C 1-4 alkyl)aminosulfonyl, hydroxyC 1-4alkyloxyC1-4alkyl or C1-4alkyloxy; Het represents a heterocycle selected from morpholinyl, piperidinyl or piperazinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from C1-4alkyl, C1-4alkyloxycarbonyl or mono- or di(C1-4alkyl)aminosulfonyl; Het represents a heterocycle selected from pyridinyl or piperidinyl wherein said monocyclic heterocycles each independently may optionally be substituted with one, or where possible two or three substituents each independently selected from aminosulfonyl, or mono- or di(Cl4alkyl)aminosulfonyl; Het represents piperidinyl.
摘要翻译：本发明涉及式（I）化合物的N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n表示0,1或2的整数; m表示0或1的整数; R 1表示C 1-4烷基; R 2表示C 1-4烷基; R 3表示C 1-4烷基; 或R 2和R 3与它们所连接的碳原子一起形成C 3-8环烷基或Het 1，其中所述C 3-8环烷基或Het 1各自独立地可以被C1- 4alkyloxycarbonyl; R 4表示卤素或C 1-4烷氧基; R 5表示C 1-4烷氧基羰基，-O-（单或二（C 1-4烷基）氨基磺酰基），被一个或多个可能的更多取代基取代的C 1-4烷基选自Het 3或NR 6 R 被一个或多个可能的更多取代基取代的C 1-4烷氧基选自氨基，Het 4或NR 8 R 9; R 6和R 7各自独立地选自氢，C 1-4烷基，C 1-4烷氧基C 1-4烷基，-Het 5或被一个或多个可能的更多取代基取代的C 1-4烷基，所述取代基选自羟基，或Het <5>; R 8和R 9各自独立地选自氢，C 1-4烷基，-Het 7或单或二（C 1-4烷基）氨基磺酰基; Het 3表示选自哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自羟基，氨基磺酰基，氨基，单或二（C 1 -4烷基）氨基磺酰基，羟基C 1-4烷氧基C 1-4烷基或C 1-4烷氧基; Het 4表示选自吗啉基，哌啶基或哌嗪基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者如果可能的话，两个或三个取代基各自独立地选自C 1-4烷基，C 1-4烷氧基羰基或一或二（C 1-4烷基）氨基磺酰基; Het 5表示选自吡啶基或哌啶基的杂环，其中所述单环杂环各自独立地可以任选地被一个取代，或者两个或三个取代基各自独立地选自氨基磺酰基或单或二（C 1-4烷基）氨基磺酰基; Het 7表示哌啶基。

6. 发明申请

WO1990010630A1 [5(6)-(BENZISOXA-, BENZISOTHIA- OR INDAZOL-3-YL)-1H-BENZIMIDAZOL-2-YL] CARBAMATES 审中-公开
标题翻译： [5（6） - （苯并咪唑，苯并噻唑或吲哚-3-基）-1H-苯并咪唑-2-基]碳酸酯
公开(公告)号：WO1990010630A1
公开(公告)日：1990-09-20
申请号：PCT/EP1990000373
申请日：1990-03-07
申请人： JANSSEN PHARMACEUTICA N.V. , RAEYMAEKERS, Alfons, Herman, Margaretha , FREYNE, Eddy, Jean, Edgard , BOECKX, Gustaaf, Maria
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D413/04
CPC分类号： C07D403/04 , C07D231/56 , C07D261/20 , C07D275/04 , C07D413/04 , C07D417/04
摘要： [5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl] carbamates of formula (I) wherein R is hydrogen, C 1-4alkyl, halo, hydroxy or C1-4alkyloxy; R is C1-4alkyl; and X is O, S, SO, SO2 or NR , said R being hydrogen, C1-4alkyl, aryl or arylC1-4alkyl. The compounds of formula (I) have anthelminthic properties. Compositions containing said compounds as active ingredient, a method of combating helminths, and a process for preparing said compounds and compositions.
摘要翻译：式（I）的[5（6） - （苯并异恶唑，苯并异噻唑或吲唑-3-基）-1H-苯并咪唑-2-基]氨基甲酸酯其中R 1是氢，C 1-4烷基，卤素，羟基或C 1-4烷氧基; R 2是C 1-4烷基; 并且X是O，S，SO，SO 2或NR 3，所述R 3是氢，C 1-4烷基，芳基或芳基C 1-4烷基。式（I）的化合物具有anthelminthic性质。含有所述化合物作为活性成分的组合物，对抗蠕虫的方法，以及制备所述化合物和组合物的方法。

7. 发明申请

WO2010119285A1 IMIDAZO [1,2-A]PYRIDINE DERIVATIVES AS FGFR KINASE INHIBITORS FOR USE IN THERAPY 审中-公开
标题翻译：作为用于治疗的FGFR激酶抑制剂的咪唑并[1,2-A]吡啶衍生物
公开(公告)号：WO2010119285A1
公开(公告)日：2010-10-21
申请号：PCT/GB2010/050618
申请日：2010-04-15
申请人： ASTEX THERAPEUTICS LIMITED , SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher William , FREYNE, Eddy Jean Edgard , LIGNY, Yannick Aimé Eddy , BONNET, Pascal Ghislain André , WROBLOWSKI, Berthold , PAPANIKOS, Alexandra
发明人： SAXTY, Gordon , BERDINI, Valerio , MURRAY, Christopher William , FREYNE, Eddy Jean Edgard , LIGNY, Yannick Aimé Eddy , BONNET, Pascal Ghislain André , WROBLOWSKI, Berthold , PAPANIKOS, Alexandra
IPC分类号： C07D471/04 , A61K31/437 , A61P35/00
CPC分类号： C07D471/04
摘要： The invention relates to new bicyclic heterocyclyl derivatives of formula (I), to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译：本发明涉及式（I）的新的双环杂环基衍生物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途，例如，癌症。

8. 发明申请

WO2008107478A8 QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PARP和油墨抑制剂
公开(公告)号：WO2008107478A8
公开(公告)日：2008-10-23
申请号：PCT/EP2008052764
申请日：2008-03-07
申请人： JANSSEN PHARMACEUTICA NV , VIALARD JORGE EDUARDO , ANGIBAUD PATRICK RENE , MEVELLEC LAURENCE ANNE , MEYER CHRISTOPHE , FREYNE EDDY JEAN EDGARD , PILATTE ISABELLE NOELLE CONSTANCE , ROUX BRUNO , PASQUIER ELISABETH THERESE JEANNE , BOURDREZ XAVIER MARC , ADELINET CHRISTOPHE DENIS , MARCONNET-DECRANE LAURENCE FRANCOISE BERNADETTE , MACRITCHIE JACQUELINE ANNE , DUFFY JAMES EDWARD STEWART , OWENS ANDREW PATE , STORCK PIERRE-HENRI , PONCELET VIRGINIE SOPHIE
发明人： VIALARD JORGE EDUARDO , ANGIBAUD PATRICK RENE , MEVELLEC LAURENCE ANNE , MEYER CHRISTOPHE , FREYNE EDDY JEAN EDGARD , PILATTE ISABELLE NOELLE CONSTANCE , ROUX BRUNO , PASQUIER ELISABETH THERESE JEANNE , BOURDREZ XAVIER MARC , ADELINET CHRISTOPHE DENIS , MARCONNET-DECRANE LAURENCE FRACOISE BERNADETTE , MACRITCHIE JACQUELINE ANNE , DUFFY JAMES EDWARD STEWART , OWENS ANDREW PATE , STORCK PIERRE-HENRI , PONCELET VIRGINIE SOPHIE
IPC分类号： C07D215/22 , A61K31/4704
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of Formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , n, m and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为PARP抑制剂的用途以及包含所述化合物的药物组合物，其中R 1，R 2，R 2， R 4，R 4，R 5，R 6，R 7，n，m和 X已经定义了含义。

9. 发明申请

WO2008049901A1 USE OF A MT KINASE INHIBITOR FOR TREATING OR PREVENTING BRAIN CANCER 审中-公开
标题翻译：使用MT激酶抑制剂治疗或预防脑癌
公开(公告)号：WO2008049901A1
公开(公告)日：2008-05-02
申请号：PCT/EP2007/061498
申请日：2007-10-25
申请人： JANSSEN PHARMACEUTICA NV , PERERA, Timothy Pietro Suren , PAGE, Martin John , JANICOT, Michel Marie François , FREYNE, Eddy Jean Edgard
发明人： PERERA, Timothy Pietro Suren , PAGE, Martin John , JANICOT, Michel Marie François , FREYNE, Eddy Jean Edgard
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： A61K31/519
摘要： The present invention is concerned with the finding that some the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5- b ][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13,14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication WO2004/105765, is useful in the manufacture of a medicament for the treatment or prevention of a primary brain cancer or brain metastasis. It accordingly provides methods for treating, preventing, delaying or mitigating brain cancer, or for preventing or slowing proliferation of cells of brain origin.
摘要翻译：本发明涉及一些大环喹唑啉衍生物4,6-乙二亚甲基嘧啶并[4,5-b] [6,1,12]苯并二氮杂环十五碳烯，17-溴-8,9,10,11,12 在PCT公开WO2004 / 105765中描述为化合物22的13,14,19-八氢-20-甲氧基-13-甲基，可用于制备用于治疗或预防原发性脑癌或脑转移的药物。因此，它提供了治疗，预防，延迟或减轻脑癌或预防或减缓脑源性细胞增殖的方法。

10. 发明申请

WO2005012304A3 TRIAZOLOPYRIMIDINE DERIVATIVES AS GLYCOGEN SYNTHASE KINASE 3 INHIBITORS 审中-公开
标题翻译：三氮唑嘧啶衍生物作为GLYCOGEN SYNTHASE激酶3抑制剂
公开(公告)号：WO2005012304A3
公开(公告)日：2007-04-26
申请号：PCT/EP2004051457
申请日：2004-07-12
申请人： JANSSEN PHARMACEUTICA NV , FREYNE EDDY JEAN EDGARD , LOVE CHRISTOPHER JOHN , COOYMANS LUDWIG PAUL , VANDERMAESEN NELE , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA
发明人： FREYNE EDDY JEAN EDGARD , LOVE CHRISTOPHER JOHN , COOYMANS LUDWIG PAUL , VANDERMAESEN NELE , BUIJNSTERS PETER JACOBUS JOHAN , WILLEMS MARC , EMBRECHTS WERNER CONSTANT JOHA
IPC分类号： C07D487/04 , A61K31/519 , A61P3/10 , A61P25/24 , C07D235/00 , C07D249/00
CPC分类号： C07D487/04
摘要： This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochernically isomeric form thereof, wherein ring A represents phenyl, pyridyl, pyrimidinyl, pyridazinyl or pyrazinyl; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 a]kyl; C 1-6 alkyloxycarbonyl; C 1-6 alkyl substituted with formyl, C 1-6 alkylcarbonyl, C 1-6 alkyloxycarbonyl, C 1-6 alkylcarbonytoxy; or optionally substituted C 1-6 alkyloxyCl-6alkylcarbonyl; X 1 represents a direct bond; -(CH 2 ) n3 - or -(CH 2 ) n4 -X 1a -X 1b -; R 2 represents optionally substituted C 3-7 CYCloalkyl; phenyl; a 4, 5, 6- or 7-membered monocyclic heterocycle containing at least one heteroatorn selected from 0, S or N; benzoxazolyl or a radical of formula (a-1); X 2 represents a direct bond; -NR 1 -NR 1 -(CH 2 ) N3 -; -0-; -0-(CH 2 ) n3 -; -C(=O)-; -C(=O)- (CH 2 ) n3 -; -C(=O)-NR 5 -(CH 2 ) n3 -; -C(=S)-; -S-; -S(=O) n1 -; -(CH 2 ) n3 -; -(CH 2 ) n4 -X 1a -X 1b -; -X 1a .-X 1b -(CH 2 ) n4 -; -S(=O) n1 -NR 5 -(CH 2 ) n3 -NR 5 _ or -S(=O) n1 ,-NR 5 -(CH 2 ) n3 -; R 3 represents an optionally substituted 5-or 6-membered monocyclic heterocycle containing at least one heteroatom selected from 0, S or N, or a 9-or 10-membered bicyclic heterocycle containing at least one heteroatom selected from 0, S or N; R 4 represents hydrogen; halo; hydroxy; optionally substituted C 1-4 alkyl; optionally substituted C 2-4 alkenyl or C 2-4 alkynyl; polyhaloC 1-3 alkyl; optionally substituted C 1-4 alkyloxy; polyhaloC 1-3 alkyloxy; C 1-4 alkylthio; polyhaloC 1-3 alkylthio; C 1-4 alkyloxycarbonyl; C 1-4 alkylcarbonyloxy; C 1-4 alkylcarbonyl; polyhaloC 1-4 alkylcarbonyl; nitro; cyano; carboxyl; NR 9 R 10 ; C(=O)NR 9 R 10 ;-NR 5_ C(=O)-NR 9 R 10 ; -NR 5 -C(=O)-R 5 ; -S(=O) n1 ,-R 11 -NR 5 -S(=O) n1 ,-R 11 -S-CN; -NR 5 -CN; their use, pharmaceutical compositions comprising them and processes for their preparation.
摘要翻译：本发明涉及式（I）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体异构体形式，其中环A表示苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; R 1表示氢; 芳基; 甲酰基; C 1-6烷基羰基; C 1-6 a] kyl; C 1-6烷氧基羰基; 被甲酰基，C 1-6烷基羰基，C 1-6烷氧基羰基，C 1-6烷基羰基取代的C 1-6烷基， / SUB> alkylcarbonytoxy; 或任选取代的C 1-6烷氧基C 1-6烷基羰基; X 1表示直接键; - （CH 2 2）n3 - 或 - （CH 2）n4 - - - - - SUB> -X _{图1b - ; R 2表示任选取代的C 3-7环烷基; 苯基; 含有至少一个选自0，S或N的杂化子的4,5,6-或7-元单环杂环; 苯并恶唑基或式（a-1）基团; X 2代表直接键; -NR 1 - （CH 2）N 3 - ;（CH 2）N 3 - 。 -0-; -O-（CH _{2 ）_{N3 - ; -C（= O） - ; -C（= O） - （CH 2）n3 - ; -C（= O）-NR ^{5 - （CH _{2 ）_{N3 - ; -C（= S） - ; -S-; -S（= O）_{N1 - ; - （CH _{2 ）_{N3 - ; - （CH _{2 ）_{N4 -X _{1A -X _{图1b - ; -X _{1A .- X _{图1b - （CH _{2 ）_{N4 - ; -S（= O）_{N1 -NR ^{5 - （CH _{2 ）_{N3 -NR ^{5 n =（CH 2）n或-S（= O）n1， - NR 5 - （CH 2）n 3 - ; R 3表示含有至少一个选自O，S或N的杂原子或含有至少一个杂原子的9元或10元双环杂环的任选取代的5元或6元单环杂环从0，S或N; R 4表示氢; 光环; 羟基; 任选取代的C 1-4烷基; 任选取代的C 2-4 - 烯基或C 2-4 - 炔基; 多卤代_{1-3 烷基; 任选取代的C 1-4烷氧基; 多卤代_{1-3 烷氧基; ç_{1-4 烷硫基; 多卤代_{1-3 烷硫基; ç_{1-4 烷氧基羰基; ç_{1-4 烷基羰基氧基; ç_{1-4 烷基羰基; 多卤代_{1-4 烷基羰基; 硝基; 氰基; 羧基; NR ^{9 - [R ^{10 ; C（= O）NR ^{9 - [R ^{10 ; - NR ^{5 _ C（= O）-NR ^{9 ř ^{10 ; -NR ^{5 C（= O）-R ^{5 ; -S（= O）n1， - R 11 -NR 5 -S（= O）n1， -R 11 -S-CN; -NR 5 -CN; 其用途，包含它们的药物组合物及其制备方法。}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}}

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