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1. 发明申请

WO2006007468A1 PYRROLOTRIAZINE COMPOUNDS 审中-公开
标题翻译：吡咯烷酮化合物
公开(公告)号：WO2006007468A1
公开(公告)日：2006-01-19
申请号：PCT/US2005/022059
申请日：2005-06-22
申请人： BRISTOL-MYERS SQUIBB COMPANY , GAVAI, Ashvinikumar, V. , MASTALERZ, Harold , DARIS, Jean-Paul , DEXTRAZE, Pierre , LAPOINTE, Philippe , RUEDIGER, Edward, H. , VYAS, Dolatrai, M. , ZHANG, Guifen
发明人： GAVAI, Ashvinikumar, V. , MASTALERZ, Harold , DARIS, Jean-Paul , DEXTRAZE, Pierre , LAPOINTE, Philippe , RUEDIGER, Edward, H. , VYAS, Dolatrai, M. , ZHANG, Guifen
IPC分类号： C07D253/10
CPC分类号： C07D487/04
摘要： The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of the invention inhibit tyrosine kinase activity of growth factor receptors such as HER1, HER2 and HER4 thereby making them useful as antiproliferative agents. The compounds are also useful for the treatment of other diseases associated with signal transduction pathways operating through growth factor receptors.
摘要翻译：本发明提供式（I）化合物及其药学上可接受的盐。本发明的化合物抑制生长因子受体如HER1，HER2和HER4的酪氨酸激酶活性，从而使它们用作抗增殖剂。所述化合物还可用于治疗与通过生长因子受体作用的信号转导途径相关的其它疾病。

2. 发明申请

WO2005082867A1 NOVEL 1,2,4-BENZOTRIAZINE-1,4-DIOXIDES 审中-公开
标题翻译：新的1,2,4-苯并噻唑-1,4-二氧化物
公开(公告)号：WO2005082867A1
公开(公告)日：2005-09-09
申请号：PCT/NZ2005/000034
申请日：2005-03-01
申请人： AUCKLAND UNISERVICES LIMITED , DENNY, William, Alexander , HAY, Michael, Patrick , HICKS, Kevin, Owen , PRUIJN, Frederik, Bastiaan , WILSON, William, Robert , PCHALEK, Karin
发明人： DENNY, William, Alexander , HAY, Michael, Patrick , HICKS, Kevin, Owen , PRUIJN, Frederik, Bastiaan , WILSON, William, Robert , PCHALEK, Karin
IPC分类号： C07D253/10
CPC分类号： C07D253/10 , C07D253/08 , C07D401/12
摘要： The present invention provides a simplified set of characteristics that can be used to select 1,2,4 benzotriazine 1,4 dioxide compounds (TPZ analogues) with therapeutic activity against hypoxic cells in human tumour xenografts, and to further provide a novel class of 1,2,4-benzotriazine-1,4-dioxides (TPZ analogues) with predicted in vivo activity against tumours, to their preparation, and to their use as hypoxia-selective cytotoxic drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本发明提供了可用于选择具有针对人肿瘤异种移植物中缺氧细胞的治疗活性的1,2,4苯并三嗪二氧化物化合物（TPZ类似物）的简化的特征集，并进一步提供新的1类，具有预测的肿瘤体内活性的2,4-苯并三嗪-1,4-二氧化物（TPZ类似物），其制备及其作为用于癌症治疗的缺氧选择性细胞毒性药物和放射增敏剂的用途，单独或与辐射和/或其他抗癌药物。

3. 发明申请

WO01095856A2 UREA DERIVATIVE USEFUL AS AN ANTI-CANCER AGENT AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：尿素衍生物作为抗癌剂及其制备方法有用
公开(公告)号：WO01095856A2
公开(公告)日：2001-12-20
申请号：PCT/KR2001/001017
申请日：2001-06-13
IPC分类号： C07D211/16 , C07D211/64 , C07D211/70 , C07D213/75 , C07D223/16 , C07D241/44 , C07D251/54 , C07D253/10 , C07D295/215 , C07D319/18 , C07D401/12 , C07D403/12 , C07D491/10 , C07D521/00 , A61K
CPC分类号： C07D213/75 , C07D211/16 , C07D211/64 , C07D211/70 , C07D223/16 , C07D231/12 , C07D233/56 , C07D241/44 , C07D249/08 , C07D251/54 , C07D253/10 , C07D295/215 , C07D319/18 , C07D401/12 , C07D403/12 , C07D491/10
摘要： The present invention relates to a novel urea derivative which is useful as an anti-cancer agent, its pharmaceutically acceptable acid addition salt or stereoisomer, and to a process for preparing the urea derivative and an anti-cancer composition comprising same as an active ingredient.
摘要翻译：本发明涉及可用作抗癌剂，其药学上可接受的酸加成盐或立体异构体的新型尿素衍生物，以及制备该尿素衍生物的方法和含有作为活性成分的抗癌组合物。

4. 发明申请

WO01072696A1 ARTHROPODICIDAL CARBOXANILIDES 审中-公开
标题翻译：抗坏血酸羧甲基纤维素
公开(公告)号：WO01072696A1
公开(公告)日：2001-10-04
申请号：PCT/US2001/009716
申请日：2001-03-26
IPC分类号： C07D253/08 , A01N25/30 , A01N43/54 , A01N43/707 , A01N43/88 , A01N43/90 , A01N47/02 , A01N47/16 , C07D239/20 , C07D239/70 , C07D253/06 , C07D253/10 , C07D273/00 , C07D273/04 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D498/04 , C07C253/08
CPC分类号： C07D253/06 , A01N43/707 , A01N43/90 , A01N47/02 , A01N47/16 , C07D239/20 , C07D239/70 , C07D253/10 , C07D273/00 , C07D273/04 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04
摘要： Compounds of Formula (I), and their N -oxides and agriculturally suitable salts, are disclosed which are useful as arthropodicides wherein A is H; E is H or C1-C3 alkyl; or A and E can be taken together to form -CH2-, -CH2CH2-, -O-, -S-, -S(O)-, -S(O)2-, -NR -, -OCH2-, -SCH2-, -N(R )CH2-, substituted -CH2- and substituted -CH2CH2-, the substituents independently selected from 1-2 halogen and 1-2 methyl; W is N or CR ;X is CR R , O, S, NR or a direct bond, provided that when W is N, then X is other than a direct bond; Y is H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C1-C3 alkylsulfonyl, C3-C6 cycloalkyl, C3-C6 cycloalkylalkyl, NR R , N=CR R , OR , COR , CO2R or C1-C6 alkyl substituted by at least one group selected from halogen, C1-C3 alkoxy, CN, NO2, S(O)rR , COR , CO2R and optionally substituted phenyl; Z is O or S; and R , R , R , R , R , R , R , R , R , R , R , R , R , R , G, n and r are as defined in the disclosure.Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling arthropods which involves contacting the arthropods or their environment with an effective amount of a compound of Formula (I).
摘要翻译：公开了式（I）化合物及其N，N-氧化物和农业上合适的盐，其可用作其中A为H的节肢动物剂; E是H或C 1 -C 3烷基; 或A和E可以一起形成-CH 2 - ， - CH 2 CH 2 - ， - O - ， - S - ， - S（O） - ， - S（O）2 - ， - NR 8 - ， - OCH 2 - ， - CH 2 - ， - N（R 8）CH 2 - ，取代的-CH 2 - 和取代的-CH 2 CH 2 - ，独立地选自1-2个卤素和1-2个甲基的取代基; W是N或CR 4; X是CR 5 R 6，O，S，NR 7或直接键，条件是当W是N时，X不是直接键; Y是H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，C 1 -C 3烷基磺酰基，C 3 -C 6环烷基，C 3 -C 6环烷基烷基，NR 9 R 10，N = CR 11 C 12，OR 7，COR 13，CO 2 R 14或被至少一个选自卤素，C 1 -C 3烷氧基，CN，NO 2，S（O）r R 15基团取代的C 1 -C 6烷基， COR 13，CO 2 R 14和任选取代的苯基; Z是O或S; R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10，R 11， R 12，R 13，R 14，R 15，G，n和r如本公开所定义。还公开了含有式（I）化合物和控制方法的组合物其包括将节肢动物或其环境与有效量的式（I）化合物接触的节肢动物。

5. 发明申请

WO2022026285A1 POLYCYCLIC CAP-DEPENDENT ENDONUCLEASE INHIBITORS FOR TREATING OR PREVENTING INFLUENZA 审中-公开
公开(公告)号：WO2022026285A1
公开(公告)日：2022-02-03
申请号：PCT/US2021/042711
申请日：2021-07-22
申请人： MERCK SHARP & DOHME CORP. , ZHANG, Yonglian , MCCAULEY, John A. , LO, Michael Man-Chu , GUO, Liangqin , ZHAO, Kake , BENNETT, Frank , KIM, Ronald M. , DEJESUS, Reynalda Keh , SHURTLEFF, Valerie W. , DE LERA RUIZ, Manuel , PLOTKIN, Michael A. , SU, Hua , FELLS, James , CROWLEY, Brendan M. , CHOBANIAN, Harry R.
发明人： ZHANG, Yonglian , MCCAULEY, John A. , LO, Michael Man-Chu , GUO, Liangqin , ZHAO, Kake , BENNETT, Frank , KIM, Ronald M. , DEJESUS, Reynalda Keh , SHURTLEFF, Valerie W. , DE LERA RUIZ, Manuel , PLOTKIN, Michael A. , SU, Hua , FELLS, James , CROWLEY, Brendan M. , CHOBANIAN, Harry R.
IPC分类号： A61K31/4738 , A61K31/53 , C07D253/10 , C07D471/04
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing influenza. The compounds are cap-dependent endonuclease inhibitors.

6. 发明申请

WO2004026846A8 DNA-TARGETED BENZOTRIAZINE 1,4-DIOXIDES AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译： DNA靶向苯扎他嗪1,4-二氧化物及其在癌症治疗中的应用
公开(公告)号：WO2004026846A8
公开(公告)日：2007-03-08
申请号：PCT/NZ0300210
申请日：2003-09-17
申请人： AUCKLAND UNISERVICES LTD , UNIV LELAND STANFORD JUNIOR , BROWN J MARTIN , DENNY WILLIAM ALEXANDER , HAY MICHAEL PATRICK , HICKS KEVIN OWEN , GAMAGE SWARNALATHA AKURATIYA , PRUIJIN FREDERIK BASTIAAN , WILSON WILLIAM ROBERT
发明人： BROWN J MARTIN , DENNY WILLIAM ALEXANDER , HAY MICHAEL PATRICK , HICKS KEVIN OWEN , GAMAGE SWARNALATHA AKURATIYA , PRUIJIN FREDERIK BASTIAAN , WILSON WILLIAM ROBERT
IPC分类号： C07D253/10 , A61P35/00 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D253/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
摘要： The present invention relates to DNA-targeted 1,2,4-benzotriazine- 1,4-dioxides and related analogues, to their preparation, and to their use as hypoxia-selective drugs and radiosensitizers for cancer therapy, both alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本发明涉及DNA靶向的1,2,4-苯并三嗪-1,4-二氧化物及其相关类似物及其制备方法，并且涉及它们作为用于癌症治疗的缺氧选择性药物和放射增敏剂，它们单独或与辐射和/或其他抗癌药物。

7. 发明申请

WO2006004833A3 PYRROLOTRIAZINE KINASE INHIBITORS 审中-公开
公开(公告)号：WO2006004833A3
公开(公告)日：2006-01-12
申请号：PCT/US2005/023099
申请日：2005-06-28
申请人： BRISTOL-MYERS SQUIBB COMPANY , BORZILLERI, Robert, M. , CHEN, Zhong , HUNT, John, T. , HUYNH, Tram, N. , POSS, Michael, A. , SCHROEDER, Gretchen, M. , VACCARO, Wayne , WONG, Tai, W. , CHEN, Xiao Tao , KIM, Kyoung, S.
发明人： BORZILLERI, Robert, M. , CHEN, Zhong , HUNT, John, T. , HUYNH, Tram, N. , POSS, Michael, A. , SCHROEDER, Gretchen, M. , VACCARO, Wayne , WONG, Tai, W. , CHEN, Xiao Tao , KIM, Kyoung, S.
IPC分类号： A61K31/53 , C07D487/04 , C07D253/10 , A61P19/02 , A61P35/00
摘要： In general, the instant invention comprises compounds of Formulas I and II including pharmaceutically acceptable salts thereof. The compounds of the invention are useful as protein kinase inhibitors and therefore are useful for treating cancer and other protein kinase mediated diseases.

8. 发明申请

WO03090912A9 PYRROLO-TRIAZINE ANILINE COMPOUNDS USEFUL AS KINASE INHIBITORS 审中-公开
标题翻译：吡咯啉 - 三嗪化合物作为激酶抑制剂有用
公开(公告)号：WO03090912A9
公开(公告)日：2004-01-08
申请号：PCT/US0312426
申请日：2003-04-15
申请人： SQUIBB BRISTOL MYERS CO , DYCKMAN ALARIC , HYNES JOHN , LEFTHERIS KATHERINA , LIU CHUNJIAN , WROBLESKI STEPHEN T
发明人： DYCKMAN ALARIC , HYNES JOHN , LEFTHERIS KATHERINA , LIU CHUNJIAN , WROBLESKI STEPHEN T
IPC分类号： B01F3/12 , A61K31/53 , A61P1/04 , A61P3/10 , A61P9/10 , A61P11/00 , A61P11/06 , A61P17/06 , A61P19/02 , A61P19/08 , A61P19/10 , A61P29/00 , A61P37/06 , A61P43/00 , C07D253/10 , C07D401/06 , C07D403/06 , C07D487/04
CPC分类号： C07D487/04
摘要： Compounds having the formula (I), and pharmaceutically acceptable salts, prodrugs, and solvates thereof, are useful as kinase inhibitors, wherein R1, R2, R3, R4, R5, R6, X and Z are as described in the specification.
摘要翻译：具有式（I）的化合物及其药学上可接受的盐，前药和溶剂合物可用作激酶抑制剂，其中R1，R2，R3，R4，R5，R6，X和Z如说明书中所述。

9. 发明申请

WO0195856A3 UREA DERIVATIVE USEFUL AS AN ANTI-CANCER AGENT AND PROCESS FOR PREPARING SAME 审中-公开
标题翻译：尿素衍生物作为抗癌剂及其制备方法有用
公开(公告)号：WO0195856A3
公开(公告)日：2002-06-27
申请号：PCT/KR0101017
申请日：2001-06-13
申请人： CHACONNE NSI CO LTD , KIM JOONG YOUNG , YOON BYUNG HOON , HWANG SUN KYUNG , OH CHUL MIN , PARK MEE SEON , SONG KYOUNG OK , OH SEONG SOO
发明人： KIM JOONG YOUNG , YOON BYUNG HOON , HWANG SUN KYUNG , OH CHUL MIN , PARK MEE SEON , SONG KYOUNG OK , OH SEONG SOO
IPC分类号： C07D211/16 , C07D211/64 , C07D211/70 , C07D213/75 , C07D223/16 , C07D241/44 , C07D251/54 , C07D253/10 , C07D295/215 , C07D319/18 , C07D401/12 , C07D403/12 , C07D491/10 , C07D521/00
CPC分类号： C07D213/75 , C07D211/16 , C07D211/64 , C07D211/70 , C07D223/16 , C07D231/12 , C07D233/56 , C07D241/44 , C07D249/08 , C07D251/54 , C07D253/10 , C07D295/215 , C07D319/18 , C07D401/12 , C07D403/12 , C07D491/10
摘要： The present invention relates to a novel urea derivative which is useful as an anti-cancer agent, its pharmaceutically acceptable acid addition salt or stereoisomer, and to a process for preparing the urea derivative and an anti-cancer composition comprising same as an active ingredient.
摘要翻译：本发明涉及可用作抗癌剂，其药学上可接受的酸加成盐或立体异构体的新型尿素衍生物，以及制备该尿素衍生物的方法和含有作为活性成分的抗癌组合物。

10. 发明申请

WO2023063906A1 SYNTHESIS AND IN VITRO ANTITUMOR ACTIVITIES OF NOVEL THIOAMIDE SUBSTITUTED PIPERAZINYL-1,2,4-TRIAZINES 审中-公开
公开(公告)号：WO2023063906A1
公开(公告)日：2023-04-20
申请号：PCT/TR2022/051044
申请日：2022-09-27
申请人： ISTANBUL MEDIPOL UNIVERSITESI
发明人： BİLTEKİN KALELİ, Sevde Nur , DEMİRAYAK, Şeref , ŞAHİN, Zafer , BERK, Barkin
IPC分类号： A61P35/00 , C07D253/10
摘要： This invention is directed to novel thioamide substituted piperazinyl-1,2,4-triazines and their potential for use in treatment of malignant diseases, such as cancer.

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