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1. 发明申请

WO2012028332A8 PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS 审中-公开
标题翻译：药物活性化合物作为AXL抑制剂
公开(公告)号：WO2012028332A8
公开(公告)日：2013-03-07
申请号：PCT/EP2011004451
申请日：2011-08-26
申请人： LEAD DISCOVERY CENTER GMBH , MAX PLANCK GESELLSCHAFT , SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D401/12 , A61K31/47 , A61K31/495 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及通式（I）的1-氮杂环-2-甲酰胺：和/或其药学上可接受的盐，这些衍生物作为药物活性剂的用途，特别是用于治疗和/或预防Ax1受体酪氨酸激酶亚家族诱导的疾病，包括癌症和原发性肿瘤转移，以及含有至少一种所述1-氮杂环-2-甲酰胺衍生物和/或其药学上可接受的盐的药物组合物。

3. 发明专利

ZA201300533B PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS 未知
公开(公告)号：ZA201300533B
公开(公告)日：2014-03-26
申请号：ZA201300533
申请日：2013-01-21
申请人： LEAD DISCOVERY CENTER GMBH , MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

4. 发明专利

SG187597A1 PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS 未知
公开(公告)号：SG187597A1
公开(公告)日：2013-03-28
申请号：SG2013005541
申请日：2011-08-26
申请人： LEAD DISCOVERY CENTER GMBH , MAX PLANCK GESELLSCHAFT
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

5. 发明专利

CA2807620A1 PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS 未知
公开(公告)号：CA2807620A1
公开(公告)日：2012-03-08
申请号：CA2807620
申请日：2011-08-26
申请人： MAX PLANCK GESELLSCHAFT , LEAD DISCOVERY CENTER GMBH
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

6. 发明专利

CA2807620C PHARMACEUTICALLY ACTIVE COMPOUNDS AS AXL INHIBITORS 未知
公开(公告)号：CA2807620C
公开(公告)日：2016-05-17
申请号：CA2807620
申请日：2011-08-26
申请人： MAX-PLANCK-GESELLSCHAFT ZUR FORDERUNG DER WSS E V , LEAD DISCOVERY CENTER GMBH
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

7. 发明专利

AU2011297889A8 Pharmaceutically active compounds as Axl inhibitors 未知
公开(公告)号：AU2011297889A8
公开(公告)日：2013-06-06
申请号：AU2011297889
申请日：2011-08-26
申请人： LEAD DISCOVERY CENTER GMBH , MAX PLANCK GESELLSCHAFT
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

8. 发明专利

AU2011297889B2 Pharmaceutically active compounds as Axl inhibitors 未知
公开(公告)号：AU2011297889B2
公开(公告)日：2015-12-24
申请号：AU2011297889
申请日：2011-08-26
申请人： LEAD DISCOVERY CENTER GMBH , MAX PLANCK GESELLSCHAFT
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides of general formula (I): and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.

9. 发明专利

ES2530492T3 Compuestos farmacéuticamente activos como inhibidores AXL 未知
公开(公告)号：ES2530492T3
公开(公告)日：2015-03-03
申请号：ES11754617
申请日：2011-08-26
申请人： LEAD DISCOVERY CENTER GMBH , MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER , ULLRICH AXEL
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： Los compuestos que tienen la fórmula general (I)**fórmula** donde A representa C-R10, N; B representa C-R11, N; D representa uno de los siguientes heterociclos**Fórmula** R1, R4, R88, R92, R100 se seleccionan de forma mutuamente independiente a partir de -H, -F, -Cl, -Br, -I, -OH, -NH2, - NHR19, -NR19R20, -OCH3, -OC2H5, -OC3H7, -OCH(CH3)2, -OC(CH3)3, -OC4H9, -NO2, -CHO, -COCH3, - COC2H5, -Ociclo-C3H5, -OCH2-ciclo-C3H5, -O-C2H4-ciclo-C3H5, -OPh, -COC3H7, -COCH(CH3)2, -COC(CH3)3, - COOH, -COOCH3, -COOC2H5, -COOC3H7, -COOCH(CH3)2, -COOC(CH3)3, -OOC-CH3, -OOC-C2H5, -OOCC3H7, -OOC-CH(CH3)2, -OOC-C(CH3)3, -NHCH3, -NHC2H5, -NHC3H7, -NHCH(CH3)2, -NHC(CH3)3, -N(CH3)2, - N(C2H5)2, -N(C3H7)2, -N[CH(CH3)2]2, -N[C(CH3)3]2, -OCF3, -OC2F5, -CH2F, -CHF2, -CF3, -CH2Cl, -CH2Br, - CH2I, -CH2-CH2F, -CH2-CHF2, -CH2-CF3, -CH2-CH2Cl, -CH2-CH2Br, -CH2-CH2I, ciclo-C3H5, -CH2-ciclo-C3H5, - CH3, -C2H5, -C3H7, -CH(CH3)2, -C4H9, -CH2-CH(CH3)2, -CH(CH3)-C2H5, -C(CH3)3, -C5H11, -CH(CH3)-C3H7, - CH2-CH(CH3)-C2H5, -CH(CH3)-CH(CH3)2, -C(CH3)2-C2H5, -CH2-C(CH3)3, -CH(C2H5)2, -C2H4-CH(CH3)2, - C6H13, -C3H6-CH(CH3)2, -C2H4-CH(CH3)-C2H5, -CH(CH3)-C4H9, -CH2-CH(CH3)-C3H7, -CH(CH3)-CH2- CH(CH3)2, -CH(CH3)-CH(CH3)-C2H5, -CH2-CH(CH3)-CH(CH3)2, -CH2-C(CH3)2-C2H5, -C(CH3)2-C3H7, - C(CH3)2-CH(CH3)2, -C2H4-C(CH3)3, -CH(CH3)-C(CH3)3, -CH>=CH2, -CH2-CH>=CH2, -C(CH3)>=CH2, -CH>=CH-CH3, -C2H4-CH>=CH2, -CH2-CH>=CH-CH3, -CH>=CH-C2H5, -CH2-C(CH3)>=CH2, -CH(CH3)-CH>=CH, -CH>=C(CH3)2, - C(CH3)>=CH-CH3, -CH>=CH-CH>=CH2, -C3H6-CH>=CH2, -C2H4-CH>=CH-CH3, -CH2-CH>=CH-C2H5, -CH>=CH-C3H7, - CH2-CH>=CH-CH>=CH2, -CH>=CH-CH>=CH-CH3, -CH>=CH-CH2-CH>=CH2, -C(CH3)>=CH-CH>=CH2, -CH>=C(CH3)- CH>=CH2, -CH>=CH-C(CH3)>=CH2, -C2H4-C(CH3)>=CH2, -CH2-CH(CH3)-CH>=CH2, -CH(CH3)-CH2-CH>=CH2, -CH2- CH>=C(CH3)2, -CH2-C(CH3)>=CH-CH3, -CH(CH3)-CH>=CH-CH3, -CH>=CH-CH(CH3)2, -CH>=C(CH3)-C2H5, - C(CH3)>=CH-C2H5, -C(CH3)>=C(CH3)2, -C(CH3)2-CH>=CH2, -CH(CH3)-C(CH3)>=CH2, -C(CH3)>=CH-CH>=CH2, - CH>=C(CH3)-CH>=CH2,- CH>=CHC(CH3)>=CH2, -C4H8-CH>=CH2, -C3H6-CH>=CH-CH3, -C2H4-CH>=CH-C2H5, -CH2- CH>=CH-C3H7, -CH>=CH-C4H9, -C3H6-C(CH3)>=CH2, -C2H4-CH(CH3)-CH>=CH2, -CH2-CH(CH3)-CH2-CH>=CH2, - CH(CH3)-C2H4-CH>=CH2, -C2H4-CH>=C(CH3)2, -C2H4-C(CH3)>=CH-CH3, -CH2-CH(CH3)-CH>=CH-CH3, -CH(CH3)- CH2-CH>=CH-CH3, -CH2-CH>=CH-CH(CH3)2, -CH2-CH>=C(CH3)-C2H5, -CH2-C(CH3)>=CH-C2H5, -CH(CH3)- CH>=CH-C2H5, -CH>=CH-CH2-CH(CH3)2, -CH>=CH-CH(CH3)-C2H5, -CH>=C(CH3)-C3H7, -C(CH3)>=CH-C3H7, -CH2- CH(CH3)-C(CH3)>=CH2, -CH(CH3)-CH2-C(CH3)>=CH2, -CH(CH3)-CH(CH3)-CH>=CH2, -CH2-C(CH3)2-CH>=CH2, - C(CH3)2-CH2-CH>=CH2, -CH2-C(CH3)>=C(CH3)2, -CH(CH3)-CH>=C(CH3)2, -C(CH3)2-CH>=CH-CH3, -CH(CH3)- C(CH3)>=CH-CH3, -CH>=C(CH3)-CH(CH3)2, -C(CH3)>=CH-CH(CH3)2, -C(CH3)>=C(CH3)-C2H5, -CH>=CH-C(CH3)3, - C(CH3)2-C(CH3)>=CH2, -CH(C2H5)-C(CH3)>=CH2, -C(CH3)(C2H5)-CH>=CH2, -CH(CH3)-C(C2H5)>=CH2, -CH2- C(C3H7)>=CH2, -CH2-C(C2H5)>=CH-CH3, -CH(C2H5)-CH>=CH-CH3, -C(C4H9)>=CH2, -C(C3H7)>=CH-CH3, - C(C2H5)>=CH-C2H5, -C(C2H5)>=C(CH3)2, -C[C(CH3)3]>=CH2, -C[CH(CH3)(C2H5)]>=CH2, -C[CH2-CH(CH3)2]>=CH2, - C2H4-CH>=CH-CH>=CH2, -CH2-CH>=CHCH2- CH>=CH2, -CH>=CH-C2H4-CH>=CH2, -CH2-CH>=CH-CH>=CH-CH3, - CH>=CH-CH2-CH>=CH-CH3, -CH>=CH CH>=CH-C2H5, -CH2-CH>=CH-C(CH3)>=CH2, -CH2-CH>=C(CH3)-CH>=CH2, - CH2-C(CH3)>=CH-CH>=CH2, -CH(CH3)-CH>=CH-CH>=CH2, -CH>=CH-CH2-C(CH3)>=CH2, -CH>=CH-CH(CH3)-CH>=CH2, -CH>=C(CH3)-CH2-CH>=CH2, -C(CH3)>=CH-CH2-CH>=CH2, -CH>=CH-CH>=C(CH3)2, -CH>=CH-C(CH3)>=CH-CH3, - CH>=C(CH3)-CH>=CH-CH3, -C(CH3)>=CH-CH>=CH-CH3, -CH>=C(CH3)-C(CH3)>=CH2, -C(CH3)>=CH-C(CH3)>=CH2, - C(CH3)>=C(CH3)-CH>=CH2, -CH>=CH-CH>=CH-CH>=CH2, -C≡CH, -C≡C-CH3, -CH2-C≡-CH, -C2H4-C≡CH, -CH2-C≡CCH3, -C≡C-C2H5, -C3H6-C≡CH, -C2H4-C≡C-CH3, -CH2-C≡C-C2H5, -C≡C-C3H7, -CH(CH3)-C≡CH, -CH2- CH(CH3)-C≡CH, -CH(CH3)-CH2-C≡CH, -CH(CH3)-C≡C-CH3, -C4H8-C≡CH, -C3H6-C≡C-CH3, -C2H4-C≡C-C2H5, - CH2-C≡C-C3H7, -C≡C-C4H9, -C2H4-CH(CH3)-C≡CH, -CH2-CH(CH3)-CH2-C≡CH, -CH(CH3)-C2H4-C≡CH, -CH2- CH(CH3)-C≡C-CH3, -CH(CH3)-CH2-C≡C-CH3, -CH(CH3)-C≡C-C2H5, -CH2-C≡CCH(CH3)2, -C≡C-CH(CH3)-C2H5, -C≡C-CH2-CH(CH3)2, -C≡C-C(CH3)3, -CH(C2H5)-C≡C-CH3,- C(CH3)2-C≡CCH3, -CH(C2H5)-CH2-C≡CH, -CH2- CH(C2H5)-C≡CH, -C(CH3)2-CH2-C≡CH, -CH2-C(CH3)2-C≡CH, -CH(CH3)-CH(CH3)-C≡CH, -CH(C3H7)-C≡CH, - C(CH3)(C2H5)-C≡CH, -C≡C-C≡CH, -CH2-C≡C-C≡CH, -C≡CC≡C-CH3, -CH(C≡CH)2, -C2H4-C≡C-C≡CH, -CH2- C≡C-CH2-C≡CH, -C≡C-C2H4-C≡CH, -CH2-C≡C-C≡C-CH3, -C≡C-CH2-C≡C-CH3, -C≡C-C≡C-C2H5, -C≡CCH( CH3)-C≡CH, -CH(CH3)-C≡C-C≡CH, -CH(C≡CH)-CH2-C≡CH, -C(C≡CH)2-CH3, -CH2-CH(C≡CH)2, -CH(C≡CH)- C≡C-CH3;, R21, R35, R36.

10. 发明专利

DK2609091T3 Farmaceutisk aktive forbindelser som AXL-inhibitorer 未知
公开(公告)号：DK2609091T3
公开(公告)日：2015-01-12
申请号：DK11754617
申请日：2011-08-26
申请人： LEAD DISCOVERY CENTER GMBH , MAX PLANCK GES ZUR FÖRDERUNG DER WISSENSCHAFTEN E V
发明人： SCHULTZ-FADEMRECHT CARSTEN , KLEBL BERT , ULLRICH AXEL , CHOIDAS AXEL , KOCH UWE , EICKHOFF JAN , WOLF ALEXANDER
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , C07D215/233 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14

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