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    • 2. 发明申请
    • PYRIDOPYRIMIDINES FOR TREATING INFLAMMATORY AND OTHER DISEASES
    • WO2005105097A3
    • 2005-11-10
    • PCT/EP2005/051892
    • 2005-04-27
    • GPC BIOTECH AGDAUB, HenrikWISSING, JosefMISSIO, AndreaKLEBL, Bert
    • DAUB, HenrikWISSING, JosefMISSIO, AndreaKLEBL, Bert
    • A61K31/513A61P29/00A61P37/00
    • 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 1 represents -NR 3 R 4 , -SR 3 , -SO-R 3 , -SO 2 -R 3 , -OR 3 ; R 2 , R 3 , and R 4 are independently of each other hydrogen, -(CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; wherein the cycloalkyl, alkyl, alkanoyl, alkenyl, alkynyl residues can optionally substituted by one or more of the following groups: -NR 5 R 6 , phenyl, substituted phenyl, thioalkyl, alkyloxy, hydroxy, carboxy, halogen, cycloalkyl; R 5 and R 6 are independently of each other hydrogen, (CH 2 ) n Ph*, heteroaryl, C 3 -C 7 -cycloalkyl, C 1 -C 6 -alkyl, C 1 -C 6 -alkanoyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl; R 5 and R 6 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 4 can optionally be -CO-R 3 , -CO-OR 3 , -SO 2 -R 3 , -SO 2 -NR 5 R 6 , -CO-NR 5 R 6 , -CS-NR 5 R 6 , -C(=NH)-R 3 , -C(=NH)-NR 5 R 6 ; R 3 and R 4 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.
    • 3. 发明申请
    • PYRIDOPYRIMIDINE DERIVATIVES
    • 吡啶衍生物衍生物
    • WO2005105097A2
    • 2005-11-10
    • PCT/EP2005051892
    • 2005-04-27
    • GPC BIOTECH AGDAUB HENRIKWISSING JOSEFMISSIO ANDREAKLEBL BERT
    • DAUB HENRIKWISSING JOSEFMISSIO ANDREAKLEBL BERT
    • A61K31/513A61P29/00A61P37/00
    • A61K31/513
    • 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.
    • 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。
    • 6. 发明申请
    • MEDIUM AND METHOD FOR ENRICHING, PURIFYING OR DEPLETING ATP BINDING PROTEINS FROM A POOL OF PROTEINS
    • 从蛋白质池中增殖,净化或减少ATP结合蛋白的培养基和方法
    • WO2004013633A2
    • 2004-02-12
    • PCT/EP2003/008375
    • 2003-07-29
    • AXXIMA PHARMACEUTICALS AGGODL, KlausMISSIO, AndreaDAUB, HenrikSTEIN-GERLACH, MatthiasGREFF, Zoltan
    • GODL, KlausMISSIO, AndreaDAUB, HenrikSTEIN-GERLACH, MatthiasGREFF, Zoltan
    • G01N33/68
    • G01N33/573A61K38/00C07D401/04C07D401/14C07K1/22G01N33/6803G01N2333/91205
    • 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-l H -imidazole-2-yl]-benzylamine, 2-[4-(2-Amino-ethoxy)­- phenylamino]-6-(2,6-dichloro-phenyl)-8-methyl-8 H -pyrido[2,3-d]pyrimidine-7-one, 2-[1-(3­-aminopropyl)-1 H -indole-3-yl)maleimide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-3-(1 H -indol­ 3-yl)-maleinmide, 3-[1-(3-Aminopropyl)-1 H -indol-3-yl]-4-(1-methyl-l H -indol-3-yl) maleinimide, 3-(8-Aminomethyl-6,7,8,9-tetrahydropyrido-[1,2- a ]-indol-10-yl)-4-(1-methyl-l H -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 from a pool of heterogeneous proteins.
    • 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来自异质蛋白库的蛋白激酶。
    • 9. 发明申请
    • METHOD FOR ISOLATING ATP BINDING PROTEINS BY MEANS OF IMMOBOLIZED PROTEIN INHIBITORS
    • 通过免疫蛋白抑制剂分离ATP结合蛋白的方法
    • WO2004013633A3
    • 2004-10-28
    • PCT/EP0308375
    • 2003-07-29
    • AXXIMA PHARMACEUTICALS AGGODL KLAUSMISSIO ANDREADAUB HENRIKSTEIN-GERLACH MATTHIASGREFF ZOLTANKLEBL BERTORFI LASZLOKERI GYOERGYVARGA ZOLTAN
    • GODL KLAUSMISSIO ANDREADAUB HENRIKSTEIN-GERLACH MATTHIASGREFF ZOLTANKLEBL BERTORFI LASZLOKERI GYOERGYVARGA ZOLTAN
    • A61K38/00C07D239/72C07D401/04C07D401/14C07K1/22G01N33/573G01N33/68
    • G01N33/573A61K38/00C07D401/04C07D401/14C07K1/22G01N33/6803G01N2333/91205
    • 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.
    • 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。