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1. 发明申请

WO2004013633A3 METHOD FOR ISOLATING ATP BINDING PROTEINS BY MEANS OF IMMOBOLIZED PROTEIN INHIBITORS 审中-公开
标题翻译：通过免疫蛋白抑制剂分离ATP结合蛋白的方法
公开(公告)号：WO2004013633A3
公开(公告)日：2004-10-28
申请号：PCT/EP0308375
申请日：2003-07-29
申请人： AXXIMA PHARMACEUTICALS AG , GODL KLAUS , MISSIO ANDREA , DAUB HENRIK , STEIN-GERLACH MATTHIAS , GREFF ZOLTAN , KLEBL BERT , ORFI LASZLO , KERI GYOERGY , VARGA ZOLTAN
发明人： GODL KLAUS , MISSIO ANDREA , DAUB HENRIK , STEIN-GERLACH MATTHIAS , GREFF ZOLTAN , KLEBL BERT , ORFI LASZLO , KERI GYOERGY , VARGA ZOLTAN
IPC分类号： A61K38/00 , C07D239/72 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/573 , G01N33/68
CPC分类号： G01N33/573 , A61K38/00 , C07D401/04 , C07D401/14 , C07K1/22 , G01N33/6803 , G01N2333/91205
摘要： The present invention relates to a medium and a method for enriching ATP binding proteins, e.g. proteinkinases, from a pool of proteins, like a proteome. The medium of the present invention comprises specific inhibitors, e.g. at least one of the compounds 4-[4-(4-fluoro-phenyl)-5-pyridine-4-yl-lH-imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)- phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3-aminopropyl)-1H-indole-3-yl)maleimide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-3-(1H-indol 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1H-indol-3-yl]-4-(1-methyl-lH-indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2-a]-indol-10-yl)-4-(1-methyl-lH-indol -3-y1)-maleinmide, [6-(3-Amino-propoxy)-methoxy-quinazolin-4-yl]-(3-chloro-phenyl)-amine, 6-(3-Amino-propoxy)-7-methoxy-quinazolin-4-yl-(3-chloro-4-fluoro-phenyl)-amine, 6-(3Amino-propoxy)-7-methoxy-quinazolin-4-yl]-(3-bromo-phenyl)-amine and 4-[4-(4-Amino-butyl)-piperazin-l-yl-methyl]-N-[4-methyl-3-(4-pyridin-3-yl-pyrimidin-2-ylamino)-phenyl]-benzamide immobilized on a support material. According to the method of the present invention the above-mentioned immobilized compounds are used to selectively bind protein kinases (e.g. p38, JNK1, JNK2, CK18, RICK, GAK) from a pool of heterogeneous proteins.
摘要翻译：本发明涉及一种培养基和一种富含ATP结合蛋白的方法，蛋白质蛋白酶，来自蛋白质库，如蛋白质组。本发明的培养基包含特异性抑制剂，例如， 4- [4-（4-氟 - 苯基）-5-吡啶-4-基-1H-咪唑-2-基] - 苄胺中的至少一种化合物，2- [4-（2-氨基 - 乙氧基） - 苯基氨基] -6-（2,6-二氯 - 苯基）-8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮，2- [1-（3-氨基丙基）-1H-吲哚 -3-基）马来酰亚胺，3- [1-（3-氨基丙基）-1H-吲哚-3-基] -3-（1H-吲哚-3-基） - 马来酰亚胺，3- [1-（3-氨基丙基） -1H-吲哚-3-基] -4-（1-甲基-1H-吲哚-3-基）马来酰亚胺，3-（8-氨基甲基-6,7,8,9-四氢吡啶并[1,2-a ] - （1-甲基-1H-吲哚-3-基） - 马来酰胺，[6-（3-氨基 - 丙氧基） - 甲氧基 - 喹唑啉-4-基] - （3- 苯基） - 胺，6-（3-氨基 - 丙氧基）-7-甲氧基 - 喹唑啉-4-基 - （3-氯-4-氟 - 苯基） - 胺，6-（3Amino-丙氧基） - -7-甲氧基 - 喹唑啉-4-基] - （3-溴 - 苯基） - 胺和4- [4-（4-氨基 - 丁基） - 哌嗪-1-基 - 甲基] -N- [4-甲基 - 3-（4-吡啶-3-基 - 嘧啶-2-基氨基） - 苯基] - 苯甲酰胺固定在载体材料上。根据本发明的方法，上述固定化化合物用于选择性地结合蛋白激酶（例如p38，JNK1，JNK2，CK18，RICK，GAK）从异源蛋白质库中。

2. 发明申请

WO2006021458A3 PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡嗪衍生物
公开(公告)号：WO2006021458A3
公开(公告)日：2007-04-12
申请号：PCT/EP2005009291
申请日：2005-08-29
申请人： GPC BIOTECH AG , KLEBL BERT , BAUMANN MATTHIAS , HOPPE EDMUND , BREHMER DIRK , DAUB HENRIK , KERI GYOERGY , VARGA ZOLTAN , MAROSFALVI JENOE , OERFI LASZLO
发明人： KLEBL BERT , BAUMANN MATTHIAS , HOPPE EDMUND , BREHMER DIRK , DAUB HENRIK , KERI GYOERGY , VARGA ZOLTAN , MAROSFALVI JENOE , OERFI LASZLO
IPC分类号： C07D239/42 , A61K31/506 , A61P37/08 , C07D401/04 , C07D401/10 , C07D401/14
CPC分类号： C07D239/42 , C07D401/04 , C07D401/10 , C07D401/14
摘要： The present invention relates to pyrimidine derivatives, methods for their synthesis, and the use of said pyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of cell proliferation disorders, cancer, leukemia, erectile dysfunction, cardiovascular diseases and disorders, inflammatory diseases, transplant rejection, immunological diseases, neuroimmunological diseases, autoimmune diseases, infective diseases including opportunistic infections, prion diseases and/or neuro-degeneration. Furthermore, the present invention relates to pharmaceutical compositions containing at least one pyrimidine derivative and/or pharmaceutically acceptable salts thereof as an active ingredient together with at least one pharmaceutically acceptable carrier, excipient or diluents as well as to methods for prophylaxis and/or treatment of the above-mentioned diseases and disorders.
摘要翻译：本发明涉及嘧啶衍生物，其合成方法和所述嘧啶衍生物作为药物活性剂的用途，特别是用于预防和/或治疗细胞增殖障碍，癌症，白血病，勃起功能障碍，心血管疾病和病症，炎症性疾病，移植排斥反应，免疫疾病，神经免疫疾病，自身免疫疾病，感染性疾病，包括机会性感染，朊病毒疾病和/或神经变性。此外，本发明涉及含有至少一种嘧啶衍生物和/或其药学上可接受的盐作为活性成分以及至少一种药学上可接受的载体，赋形剂或稀释剂的药物组合物，以及用于预防和/或治疗上述疾病和障碍。

3. 发明申请

WO2005105097A2 PYRIDOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：吡啶衍生物衍生物
公开(公告)号：WO2005105097A2
公开(公告)日：2005-11-10
申请号：PCT/EP2005051892
申请日：2005-04-27
申请人： GPC BIOTECH AG , DAUB HENRIK , WISSING JOSEF , MISSIO ANDREA , KLEBL BERT
发明人： DAUB HENRIK , WISSING JOSEF , MISSIO ANDREA , KLEBL BERT
IPC分类号： A61K31/513 , A61P29/00 , A61P37/00
CPC分类号： A61K31/513
摘要： The present invention relates to the use of pyridopyrimidine derivatives having the general formula (I) wherein X represents =NH, =N-Acyl, =O, or =S; R represents -NR R , -SR , -SO-R , -SO2-R , -OR ; R , R , and R are independently of each other hydrogen, -(CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR R , phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R and R are independently of each other hydrogen, (CH2)nPh*, heteroaryl, C3-C7-cycloalkyl, C1-C6-alkyl, C1-C6-alkanoyl, C2-C6-alkenyl, C2-C6-alkynyl; R and R can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ph* represents phenyl or substituted phenyl; n is 0, 1, 2, or 3; R can optionally be -CO-R , -CO-OR , -SO2-R , -SO2-NR R , -CO-NR R , -CS-NR R , -C(=NH)-R , -C(=NH)-NR R ; R and R can be taken together with the nitrogen to which they are attached to complete a ring having 3 to 7 carbon atoms, optionally containing 1, 2, or 3 heteroatoms selected from nitrogen, oxygen, and sulfur; Ar represents phenyl, substituted phenyl, or heteroaryl; and pharmaceutically acceptable salts thereof for prophylaxis and/or treatment of inflammatory diseases, neurodegenerative disorders, immunological diseases, neuroimmunological diseases, autoimmune diseases, diabetes, transplant rejection, infective diseases, prion diseases, cardiovascular diseases and disorders.
摘要翻译：本发明涉及具有通式（I）的吡啶并嘧啶衍生物的用途，其中X表示= NH，= N-酰基，= O或= S; R 1表示-NR 3 R 4，-SR 3，-SO-R 3，-SO 2 -R 3，-OR 3; R 2，R 3和R 4彼此独立地为氢， - （CH 2）n Ph *，杂芳基，C 3 -C 7 - 环烷基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷酰基，C 2 C 1-6 - 烯基，C 2 -C 6 - 炔基; 其中环烷基，烷基，烷酰基，烯基，炔基残基可以任选被一个或多个下列基团取代：-NR 5 R 6，苯基，取代的苯基，硫代烷基，烷氧基，羟基，羧基，卤素，环烷基 ; R 5和R 6彼此独立地为氢，（CH 2）n Ph *，杂芳基，C 3 -C 7 - 环烷基，C 1 -C 6 - 烷基，C 1 -C 6 - 烷酰基，C 2 -C 6 - 烯基， C6炔基; R 5和R 6可以与它们所连接的氮一起连接，以形成具有3至7个碳原子的环，任选地含有1,2或3个选自氮，氧和硫的杂原子; Ph *表示苯基或取代的苯基; n为0,1,2或3; R 4可以任选地是-CO-R 3，-CO-OR 3，-SO 2 -R 3，-SO 2 -NR 5 R 6，-CO-NR 5， R 6，-C 6 -NR 5 R 6，-C（= NH）-R 3，-C（= NH）-NR 5 R 6; R 3和R 4可以与它们所连接的氮一起连接，以形成具有3-7个碳原子的环，任选地含有1,2或3个选自氮，氧和硫的杂原子; Ar表示苯基，取代的苯基或杂芳基; 用于预防和/或治疗炎性疾病，神经变性疾病，免疫疾病，神经免疫疾病，自身免疫疾病，糖尿病，移植排斥，感染性疾病，朊病毒疾病，心血管疾病和病症的药学上可接受的盐。

4. 发明申请

WO2004050101A3 FORMULATIONS USEFUL AGAINST HEPATITIS C VIRUS INFECTIONS 审中-公开
标题翻译：有效的抗生素C病毒感染的配方
公开(公告)号：WO2004050101A3
公开(公告)日：2004-09-10
申请号：PCT/EP0313514
申请日：2003-12-01
申请人： AXXIMA PHARMACEUTICALS AG , HERGET THOMAS , KLEBL BERT
发明人： HERGET THOMAS , KLEBL BERT
IPC分类号： A61K31/00 , A61K38/21 , A61P31/14 , A61K33/04
CPC分类号： A61K38/212 , A61K9/0014 , A61K9/2866 , A61K31/00 , A61K31/203 , A61K31/593 , A61K33/04 , A61K38/215 , A61K38/217 , A61K45/06 , A61K2300/00
摘要： The present invention relates generally to chemical compounds and substances which are effective against Hepatitis C virus (HCV) infections. Moreover, the present invention relates to compositions comprising said compounds and/or substances, to methods for preventing HCV infections as well use of the compounds and/or substances for the preparation of compositions useful for the prophylaxis and/or treatment of HCV infections. Useful compounds and substances according to the invention are selenium, selenium salts, Vitamin D3 and retinoids, like all trans retinoic acid and salts thereof, C1 - C alkyl amide of all trans retinoic acid and salts thereof, C1 - C10 alkyl esters of all trans retinoic acid and salts thereof, 9-cis retinoic acid and salts thereof, C1 - C10 alkyl amide of 9-cis retinoic acid and salts thereof, C1 - C10 alkyl esters of 9-cis retinoic acid and salts thereof, (E)-4-[2 (5,6,7,8-tetrahydro-5,5,8,8-tetra methyl-2-naphthalenyl-1-propenyl) benzoic acid (TTNPB), (4-[5,6,7,8-tetrahydro5,5,8,8-tetramethyl-2-naphtalenyl) carboxamido] benzoic acid (AM-580), N-(4-hydroxyphenyl) retinamide (4-HPR), and 6-[3-(1- adamantyl) -4-hydroxyphenyl]-2-naphthalene carboxylic acid (AHPN).
摘要翻译：本发明一般涉及对丙型肝炎病毒（HCV）感染有效的化合物和物质。此外，本发明涉及包含所述化合物和/或物质的组合物，用于预防HCV感染的方法以及化合物和/或物质用于制备用于预防和/或治疗HCV感染的组合物的用途。根据本发明的有用的化合物和物质是硒，硒盐，维生素D3和类视色素，如所有反式视黄酸及其盐，全反式视黄酸及其盐的C1-C烷基酰胺，全反式的C1-C10烷基酯视黄酸及其盐，9-顺式视黄酸及其盐，9-顺式视黄酸的C1-C10烷基酰胺及其盐，9-顺式视黄酸的C1-C10烷基酯及其盐，（E）-4 - [2（5,6,7,8-四氢-5,5,8,8-四甲基-2-萘基-1-丙烯基）苯甲酸（TTNPB）），（4- [5,6,7,8 四氢-5,5,8,8-四甲基-2-萘基）甲酰胺基]苯甲酸（AM-580），N-（4-羟基苯基）视黄酰胺（4-HPR）和6- [3-（1-金刚烷基） -4-羟基苯基] -2-萘甲酸（AHPN）。

5. 发明申请

WO2005023818A3 HETEROBICYCLIC COMPOUNDS AS PHARMACEUTICALLY ACTIVE AGENTS 审中-公开
标题翻译：异种化合物作为药物活性剂
公开(公告)号：WO2005023818A3
公开(公告)日：2005-08-25
申请号：PCT/EP2004010161
申请日：2004-09-10
申请人： AXXIMA PHARMACEUTICALS AG , KOUL ANIL , KLEBL BERT , MUELLER GERHARD
发明人： KOUL ANIL , KLEBL BERT , MUELLER GERHARD
IPC分类号： A61K31/381 , C07D209/42 , C07D333/66 , C07D333/68 , C07D409/12 , C07D491/04 , C07D493/04 , C07D495/04 , C07D495/10 , A61P31/04
CPC分类号： C07D409/12 , C07D209/42 , C07D333/66 , C07D333/68 , C07D491/04 , C07D493/04 , C07D495/04 , C07D495/10
摘要： Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.
摘要翻译：描述的是杂双环化合物，例如4,5,6,7-四氢苯并[b]噻吩-3-羧酸酰胺，4,7-二氢-5H-噻吩并[2,3-c]噻喃-3-羧酸酰胺，4 ，7-二氢-5H-噻吩并[2,3-c]吡喃-3-羧酸酰胺或苯并[b]噻吩-3-羧酸酰胺及其药学上可接受的盐，这些衍生物用于预防和 /或治疗诸如感染性疾病，包括分泌细菌感染和机会性疾病，朊病毒疾病，免疫疾病，自身免疫疾病，双相和临床病症，心血管疾病，细胞增殖性疾病，糖尿病，炎症，移植排斥，勃起功能障碍，神经变性疾病和中风，以及含有至少一种杂双环化合物和/或其药学上可接受的盐的组合物。此外，公开了用于合成杂双环化合物的反应程序。

6. 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。

7. 发明申请

WO2008132138A9 DERIVATIVES OF 4,6-DISUBSTITUTED AMINOPYRIMIDINES 审中-公开
标题翻译： 4,6-取代氨基亚氨基嘧啶的衍生物
公开(公告)号：WO2008132138A9
公开(公告)日：2008-12-31
申请号：PCT/EP2008055015
申请日：2008-04-24
申请人： INGENIUM PHARMACEUTICALS GMBH , CHOIDAS AXEL , KLEBL BERT , MUELLER GERHARD , SCHWAB WILFRIED
发明人： CHOIDAS AXEL , KLEBL BERT , MUELLER GERHARD , SCHWAB WILFRIED
IPC分类号： C07D239/42 , A61K31/505 , A61P35/00
CPC分类号： C07D239/42
摘要： The present invention relates to methylenesulfone and methylenesulfonamide derivatives of 4,6-disubstituted aminopyrimidines having the general formula (II) as given below and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or the treatment of cell proliferative diseases, inflammation, cardiac hypertrophy and infectious diseases, especially viral infections such as HIV. Furthermore, the present invention is directed towards pharmaceutical composition containing at least one of the methylenesulfone or methylenesulfonamide derivatives of 4,6-disubstituted aminopyrimidines and/or pharmaceutically acceptable salts thereof.
摘要翻译：本发明涉及具有下述通式（II）的4,6-二取代氨基嘧啶的亚甲基砜和亚甲基磺酰胺衍生物和/或其药学上可接受的盐，这些衍生物用作药物活性剂，特别是用于预防和/ 或治疗细胞增殖性疾病，炎症，心脏肥大和感染性疾病，特别是病毒感染如HIV。此外，本发明涉及含有4,6-二取代氨基嘧啶的亚甲基砜或亚甲基磺酰胺衍生物和/或其药学上可接受的盐中的至少一种的药物组合物。

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