Abstract:
다양한 질환 또는 병인의 치료용 인다졸 화합물들이 공개된다. 더 구체적으로, 본 발명은 Wnt 경로 신호생성의 활성화를 특징으로 하는 장애 (예를 들면, 암, 비정상적 세포 증식, 혈관신생, 알츠하이머 질환, 폐 질환 및 골관절염)의 치료, Wnt 경로 신호생성에 의해 매개된 세포 이벤트의 조절, 뿐만 아니라 상기 Wnt 경로의 돌연변이 또는 조절이상 및/또는 하나 또는 그 이상의 Wnt 신호생성 성분들의 돌연변이 또는 조절이상으로 인한 유전 질환들 및신경의 상태/장애/질환에 인다졸 화합물 또는 이의 유사체들의 사용에 관계된다. 또한 Wnt-관련된 질환 상태를 치료하는 방법들이 또한 제공된다.
Abstract:
PURPOSE: A tyrosine kinase compound is provided to suppress the tyrosine kinase activation of DDR1 and DDR2 and to prevent or treat cancer, arteriosclerosis, rheumatoid arthritis, and osteoarthritis. CONSTITUTION: A tyrosine kinase suppression compound is denoted by chemical formula 1. A pharmaceutical composition for anti-cancer contains a compound of chemical formula 1, isomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutically acceptable salt is hydrochloride or trifluoroacetic acid salt. A pharmaceutical composition for preventing or treating rheumatism or osteoarthritis contains the compound of chemical formula 1, the isomer, and the salt as active ingredients.
Abstract:
R = H, C1-11 alkyl, cyclopropyl, CF3 ; R1 = H, Br, C1, F ; R2 , R3 = H, C1-3 alkl, C1-3 alkoxy, Br, C1, F, CF3), useful as fungicides, were prepd. by reaction of the acylhydrazine (II) with equi. mol. O-halophenyl-isocyanate (III; X = Br, Cl, F) at 60-100≦̸C for 24hr, followed by reac- tion of equi. mol. base at 60-200≦̸C in anhydrous amide solvent to give I.
Abstract:
Title compds. (I; R = H, C1-12 alkyl, cyclopropyl, CF3; R1 = H, Br, C1, F ; R2, R3 = H, C1-3 alkyl, C1-3 alkoxy, Br, C1, F, CF3), useful as fungicides and bactericides (no data), were prepd. by the reaction of II and same mole base at 60-200≦̸C, in amide anhydride. Thus, 4-(2,4-dichloro- phenyl)-5-methyl-1,2,4-triazole-3-thiol in DMF was refluxed for 24hr adding NaOH followed by extrating with ethylacetate using liq-liq extractor to give 7-chloro-3-methyl-S-triazolo [3,4-b benzothiazole.
Abstract:
PURPOSE: A CK2 inhibitor compound and a composition containing the same for suppressing CK2 are provided to treat CK2 inhibition-associated diseases. CONSTITUTION: A compound with activity of suppressing CK2 is denoted by chemical formula I. The compound of chemical formula I is prepared by reacting a compound of chemical formula II with a compound of chemical formula III and acid under the presence of an organic solvent. The acid is X-Y-Z, wherein X is halogen, Y is alkenyl, and Z is carboxyl. A composition for suppressing CK2 contains the compound of chemical formula I, pharmaceutically acceptable salt or solvate thereof as active ingredients. The composition is used for treating cancer or viral infection.
Abstract:
하기 화학식 (I)의 화합물, 이들의 이성질체, 및 이들의 부가염: (I), 상기 식에서: R 1 은 수소, 할로겐 또는 알킬을 나타내며, R 1a 는 수소 또는 알킬을 나타내며, R 2 는 수소, 할로겐 또는 히드록시를 나타내며, A는 CR 4 R 5 또는 NR 4 를 나타내며, R 3 는 수소, 알킬 또는 시클로알킬을 나타내며, R 4 는 수소 또는 알킬을 나타내거나, A는 질소를 나타내며, 인접한 -CHR 3 -와 함께 고리 (여기에서, m은 1, 2 또는 3임)를 형성하며, R 5 는 수소 또는 할로겐를 나타내며, X는 발명의 상세한 설명에서 정의한 바와 같다.
Abstract:
PURPOSE: Benzothiazine and benzothiadiazine compounds, a preparation process thereof and pharmaceutical compositions containing the same are provided. The compounds have higher pharmacological activity on AMPA current than that of conventional compounds having similar structures, and are useful as AMPA modulators for treatment or prevention of the memory and recognition disorders associated with aging, the anxious or depressive syndromes, progressive neurodegenerative diseases, Alzheimer's disease, Pick's disease, Huntington's chorea, schizophrenia, after-effects of acute neurodegenerative diseases, after-effects of ischemia and after-effects of epilepsy. CONSTITUTION: The benzothiazine and benzothiadiazine compounds represented by the formula(I), enantiomers or partial stereoisomers thereof, or pharmaceutically acceptable addition salts with acid or base are provided, wherein R1 is hydrogen, halogen or linear or branched C1-C6 alkyl; R1a is hydrogen or linear or branched C1-C6 alkyl; R2 is hydrogen, halogen or hydroxy; A is CR4R5 group or NR4 group or is nitrogen and forms a N-containing ring with -CHR3- group in which m is 1, 2 or 3; R3 is hydrogen, linear or branched C1-C6 alkyl or C3-C7 cycloalkyl; R4 is hydrogen or linear or branched C1-C6 alkyl; R5 is hydrogen or halogen; X is NR6R7, S(O)nR8 or OR'8 or heterocyclic; R6 is hydrogen, linear or branched C1-C6 alkyl, S(O)pR9, COR9 or P(O)OR9OR10; R7 is hydrogen, or linear or branched C1-C6 alkyl; R6 and R7 form heterocyclic with nitrogen; R8, R9 and R10 are the same or different, and hydrogen, linear or branched C1-C6 alkyl optionally substituted with one or more halogen, aryl C1-C6 alkyl wherein aryl is linear or branched, or aryl; R'8 is linear or branched C1-C6 alkyl, or linear or branched C1-C6 acyl; and n and p is the same or different, and 1 or 2.
Abstract translation:目的:提供苯并噻嗪和苯并噻二嗪化合物及其制备方法和含有它们的药物组合物。 该化合物对具有相似结构的常规化合物具有较高的AMPA电流的药理学活性,并且可用作用于治疗或预防与老化,焦虑或抑郁综合征,进行性神经变性疾病,阿尔茨海默氏病相关的记忆和识别障碍的AMPA调节剂 ,皮克病,亨廷顿舞蹈病,精神分裂症,急性神经退行性疾病的后遗症,缺血后遗症和癫痫后期作用。 构成:提供由式(I)表示的苯并噻嗪和苯并噻二唑化合物,其对映异构体或部分立体异构体,或与酸或碱的药学上可接受的加成盐,其中R 1是氢,卤素或直链或支链C 1 -C 6烷基; R 1a是氢或直链或支链C 1 -C 6烷基; R2是氢,卤素或羟基; A是CR4R5基或NR4基,或是氮,并形成具有-CHR3-基团的含N环,其中m是1,2或3; R3是氢,直链或支链C1-C6烷基或C3-C7环烷基; R4是氢或直链或支链C1-C6烷基; R5是氢或卤素; X是NR 6 R 7,S(O)n R 8或OR 8或杂环; R 6是氢,直链或支链C 1 -C 6烷基,S(O)p R 9,COR 9或P(O)OR 9 OR 10; R 7是氢或直链或支链C 1 -C 6烷基; R6和R7与氮形成杂环; R 8,R 9和R 10相同或不同,氢,任选被一个或多个卤素取代的直链或支链C 1 -C 6烷基,芳基为直链或支链的芳基C 1 -C 6烷基或芳基; R '8是直链或支链C 1 -C 6烷基,或直链或支链C 1 -C 6酰基; 并且n和p相同或不同,和1或2。
Abstract:
본 발명은 일반식 (I)의 1N치환된 피라지노[2,3-c]-1,2,6-티아디아진 2,2-디옥사이드 및 이의 제조방법에 관한 것이다.
상기식에서, R l 및 R 2 는 동일하거나 상이할 수 있으며, 수소, 직쇄 또는 측쇄 알킬, 아릴, 트리플로오로메틸, 할로겐, 옥소, 아미노. 카복스아미도 및 알콕시카보닐로 이루어진 그룹의 원이고, R 3 은 직쇄 또는 측쇄 알킬, 디알킬아미노에틸, 아르알킬. 알코시카보닐메틸, 카복시메틸 및 하이드록시에틸로 이루어진 그룹의 원이며, R 4 및 R 5 는 동일하거나 상이할 수 있고. 수소, 직쇄 또는 측쇄 알킬 및 아르알킬, 하이드록시알킬. 아미노, 아미노 알킬 및 알킬아미노알킬로 이루어진 그룹의 원이다.