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    • 6. 发明申请
    • SUBSTITUTED 5-PHENYL PYRIMIDINES I IN THERAPY
    • 取代的5-苯基吡啶在治疗中
    • WO2006079556A2
    • 2006-08-03
    • PCT/EP2006000774
    • 2006-01-30
    • BASF AGRHEINHEIMER JOACHIMGROTE THOMASMUELLER BERNDNAVE BARBARASCHIEWECK FRANKSCHWOEGLER ANJAJABS THORSTENBLETTNER CARSTEN
    • RHEINHEIMER JOACHIMGROTE THOMASMUELLER BERNDNAVE BARBARASCHIEWECK FRANKSCHWOEGLER ANJAJABS THORSTENBLETTNER CARSTEN
    • A61K31/506A61K31/505C07D239/42C07D239/48C07D401/04C07D403/04C07D417/04
    • C07D239/48C07D239/42C07D401/04C07D403/04C07D417/04
    • The present invention relates to substituted 5-phenyl pyrimidines I, which carry a radical X in the 4-position of the pyrimidine ring, a radical Y in the 6-position of the pyrimidine ring, the radical X denoting a group of the formula NR 1 R 2 , OR 1a or SR 1a , in which R 1 , R 2 , independently of each other, denote hydrogen, C 1 -C 10 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 10 -haloalkyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -halocycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing 1, 2, 3 or 4 nitrogen atoms or 1, 2 or 3 nitrogen atoms and one sulfur or oxygen atom as ring members, which radicals may be unsubstituted or may carry 1, 2, 3 or 4 radicals R a1 ; or the radical NR 1 R 2 may also form a 5- or 6-membered optionally substituted heterocyclic ring, containing 1, 2, 3 or 4 nitrogen atoms or 1, 2 or 3 nitrogen atoms and one sulfur or oxygen atom as ring members, which are non-adjacent to the nitrogen of NR 1 R 2 , in which two adjacent C atoms or one N atom and one adjacent C atom can be linked by a C 1 -C 4 -alkylene chain and wherein the heterocyclic ring may be unsubstituted or may carry 1, 2, 3 or 4 radicals R a1 as defined in claim 1, R 1a has one of the meanings given for R 1 except for hydrogen; the radical Y being selected from the group consisting of halogen, cyano, C 1 -C 4 -alkyl, C 2 -C 4 -alkenyl, C 2 -C 4 -alkynyl, C 3 -C 6 -cycloalkyl, C 1 -C 4 -alkoxy, C 3 -C 4 -alkenyloxy, C 3 -C 4 -alkynyloxy, C 1 -C 6 -alkylthio, di-(C 1 -C 6 -alkyl)amino or C 1 -C 6 -alkylamino, where the alkyl, alkenyl and alkynyl radicals of Y may be substituted by halogen, cyano, nitro, C 1 -C 2 -alkoxy or C 1 -C 4 -alkoxycarbonyl; and wherein the pyrimidine radical may also carry a radical different from hydrogen in the 2-position and wherein the phenyl ring in the 5-position of the pyrimidine ring may be unsubstituted or carry 1, 2, 3, 4 or 5 radicals L which are different from hydrogen, and the pharmaceutically acceptable salts substituted 5-phenyl pyrimidines for use in therapy, in particular in therapy or treatment of cancerous diseases.
    • 本发明涉及取代的5-苯基嘧啶I,其在嘧啶环的4-位上携带基团X,嘧啶环的6-位的基团Y,基团X表示式NR的基团 其中R 1,R 2,R 2,R 1,R 2, R 2彼此独立地表示氢,C 1 -C 10 - 烷基,C 2 - C 6 - 烯基,C 2 -C 6 - 炔基,C 1 -C 10 - C 1 -C 3烷基,C 3 -C 8 - 环烷基,C 3 -C 8 - 卤代烷基,C 3 -C 8 - 苯基或含有1,2,3或4个氮原子或1,2或3个氮原子和一个硫或氧原子作为环成员的5-或6-元杂芳基或5-或6-元杂环基,该基团可以 未被取代或可以携带1,2,3或4个基团R a1a; 或自由基NR 1 R 2还可以形成含有1,2,3或4个氮原子或1,2或2个氮原子的5或6元任选取代的杂环 或3个氮原子和一个硫或氧原子作为环成员,其与NR 1 R 2 O 2的氮不相邻,其中两个相邻的C原子或一个 N原子和一个相邻的C原子可以通过C 1 -C 4 - 亚烷基链连接,并且其中杂环可以是未取代的或可以携带1,2,3 或如权利要求1所定义的4个基团R a1,其中R 1a除了氢之外具有R 1给出的含义之一; 基团Y选自卤素,氰基,C 1 -C 4 - 亚烷基,C 2 -C 3 - 烷基, 4 - 烯基,C 2 -C 4 - 炔基,C 3 -C 6 - 环烷基,C 1 -C 4 - 烷氧基,C 3 -C 4 - 炔基氧基,C 1 -C 4 - 3-C 4 - 炔基氧基,C 1 -C 6 - 烷硫基,二 - (C 1 -C 6) C 1 -C 6 - 烷基)氨基或C 1 -C 6 - 烷基氨基,其中Y的烷基,烯基和炔基可以 被卤素,氰基,硝基取代,C 1 -C 2 - 烷氧基或C 1 -C 4 - - 烷氧基; 并且其中嘧啶基团还可以携带2-位上与氢不同的基团,其中嘧啶环的5-位上的苯环可以是未取代的或携带1,2,3,4或5个基团L,其为 不同于氢,以及用于治疗,特别是治疗或治疗癌性疾病的药学上可接受的盐取代的5-苯基嘧啶。
    • 7. 发明申请
    • 7-AMINO-6-HETARYL-1,2,4-TRIAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AND THE USE THEREOF FOR CONTROLLING PATHOGENIC FUNGI
    • 7-氨基-6-杂芳基-1,2,4-三唑并[1,5-a]嘧啶化合物和它们在防治有害真菌中的用途
    • WO2006066818A3
    • 2006-11-02
    • PCT/EP2005013577
    • 2005-12-16
    • BASF AGWAGNER OLIVERGROTE THOMASRHEINHEIMER JOACHIMNAVE BARBARASTIERL REINHARD
    • WAGNER OLIVERGROTE THOMASRHEINHEIMER JOACHIMNAVE BARBARASTIERL REINHARD
    • C07D487/04A01N43/90
    • A01N43/90C07D213/55C07D237/14C07D487/04
    • The invention relates to novel 7-amino-6-hetaryl-1,2,4-triazolo[1,5-a]pyrimidine compounds and the salts thereof that can be used in agriculture, the use of the same for controlling pathogenic fungi, and plant protection agents containing at least one such compound as an active constituent. Said novel 7-amino-6-hetaryl-1,2,4-triazolo[1,5-a]pyrimidine compounds correspond to general formula (I) wherein the substituents R 1 , R 2 , Het, X and Y have the following designations: Het represents a six-membered heteroaromatic radical selected from pyridinyl, pyridazinyl, pyrazinyl, 1,2,4-triazinyl and 1,3,5-triazinyl, the six-membered heteroaromatic radical comprising 1, 2 or 3 substituents L which are the same or different, R 1 , R 2 independently represent hydrogen, C 1 -C 8 alkyl, C 1 -C 8 halogenalkyl, C 1 -C 8 alkoxy, C 3 -C 8 cycloalkyl, C 3 -C 8 cycloalkoxy, C 5 -C 10 bicycloalkyl, C 3 -C 8 halogencycloalkyl, C 2 -C 8 alkenyl, C 2 -C 8 alkenyloxy, C 4 -C 10 alkadienyl, C 2 -C 8 halogenalkenyl, C 3 -C 8 cycloalkenyl, C 3 -C 8 halogencycloalkenyl, C 2 -C 8 alkinyl, C 2 -C 8 alkinyloxy, C 2 -C 8 halogenalkinyl, NH 2, C 1 -C 8 alkylamino, Di-C 1 -C 8 -alkylamino, phenyl, naphthyl, or a five-membered or six-membered saturated, partially unsaturated or aromatic heterocycle, X represents hydrogen, halogen, OH, cyano, C 1 -C 4 alkyl and the like, and Y represents hydrogen, halogen, cyano, C 1 -C 4 alkyl, and the like.
    • 本发明涉及新颖的7-氨基-6-杂芳基-1,2,4-三唑并[1,5-a]嘧啶化合物及其农业上可接受的盐,以及它们在防治有害真菌中的用途,以及植物保护剂,这些化合物的至少一种作为 含有活性成分。 新的7-氨基-6-杂芳基-1,2,4-三唑并[1,5-a]嘧啶化合物可通过通式(I)所示,其中取代基R 1 来表示 ,R 2 ,(I)的Het,X和Y在式具有以下含义:Het是其选自吡啶基,哒嗪基,吡嗪基的6元杂芳基,1,2,4- 三嗪基和1,3,5-三嗪基,其中所述6元杂芳基1,2或3个相同或不同的取代基L可以包括,R 1 ,R 2 独立地 另一个氢,C 1 -C 8 烷基,C 1 -C 8 卤代烷基,C 1 -C 8 烷氧基,C 3 -C 8 环烷基,C 3 -C 8 环烷氧基,C 5 -C 10 双环,C 3 -C 8 卤代环烷基,C 2 -C 8 烯基,C 2 -C 8 烯 ,C 4 -C 10 链二烯基,C 2 -C 8 卤代,C 3 -C 8 环烯基,C 3 -C 8 卤代环,C 2 -C 8 炔基,C 2 -C 8 炔氧基,C 2 -C 8 卤代炔基,NH 2 C 1 -C 8 烷基氨基,二-C 1 -C 8 烷基氨基,苯基,萘基或五 - 或六元饱和,部分不饱和或芳族的杂环,X是氢,卤素,OH,氰基,C < SUB> 1 -C 4 烷基等,Y是氢,卤素,氰基,C 1 -C 4 烷基, 等等。