会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 3. 发明授权
    • Substituted heteroaryl- and aryl-cyclopropylamine acetamides and their use
    • 取代的杂芳基 - 和芳基 - 环丙胺乙酰胺及其用途
    • US08946296B2
    • 2015-02-03
    • US13500687
    • 2010-04-19
    • Alberto Ortega MuñozJulio Castro-Palomino LariaMatthew Colin Thor Fyfe
    • Alberto Ortega MuñozJulio Castro-Palomino LariaMatthew Colin Thor Fyfe
    • A61K31/165C07C237/20C07C237/06C07C255/54C07D213/36
    • C07C237/06C07C255/54C07C2601/02C07D213/36
    • The invention relates to compounds of Formula (I): (A′)x-(A)-(B)—(Z)-(L)-C(═O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A′), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
    • 本发明涉及式(I)化合物:(A')x-(A) - (B) - (Z) - (L)-C(= O)NH 2或其药学上可接受的盐或溶剂合物,其中: A)是杂芳基或芳基; 每个(A')如果存在,独立地选自芳基,芳基烷氧基,芳基烷基,杂环基,芳氧基,卤素,烷氧基,卤代烷基,环烷基,卤代烷氧基和氰基,其中每个(A')被0,1,2 或3个独立地选自卤素,卤代烷基,芳基,芳基烷氧基,烷基,烷氧基,氰基,磺酰基,亚磺酰基和羧酰胺的取代基; X为0,1,2或3; (B)是环丙基环,其中(A)和(Z)与(B)的不同碳原子共价结合; (Z)为-NH-; 和(L)是 - (CH 2)m CR 1,R 2 - ,其中m是0,1,2,3,4,5或6,并且其中R 1和R 2各自独立地是氢或C 1 -C 6烷基; 条件是,如果(L)是-CH 2 - 或-CH(CH 3) - ,则X不为0.本发明的化合物可用于治疗疾病如癌症和神经变性疾病。
    • 4. 发明申请
    • SUBSTITUTED HETEROARYL- AND ARYL-CYCLOPROPYLAMINE ACETAMIDES AND THEIR USE
    • 取代的杂芳基和芳基环丙基氨基甲酸酯及其用途
    • US20120264823A1
    • 2012-10-18
    • US13500687
    • 2010-04-19
    • Alberto Ortega MuñozJulio Castro-Palomino LariaMatthew Colin Thor Fyfe
    • Alberto Ortega MuñozJulio Castro-Palomino LariaMatthew Colin Thor Fyfe
    • A61K31/165A61K31/277C07C237/20A61P25/28A61P25/16C07C255/60A61P35/00
    • C07C237/06C07C255/54C07C2601/02C07D213/36
    • The invention relates to compounds of Formula (I): (A′)x-(A)-(B)—(Z)-(L)-C(═O)NH2 or pharmaceutically acceptable salts or solvates thereof, wherein: (A) is heteroaryl or aryl; each (A′), if present, is indepedently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2 or 3 substituents independently chosen from halo, haloalkyl, aryl, arylalkoxy, alkyl, alkoxy, cyano, sulfonyl, sulfinyl, and carboxamide; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; and (L) is —(CH2)mCR1,R2—, wherein m is 0, 1, 2, 3, 4, 5, or 6, and wherein R1 and R2 are each independently hydrogen or C1-C6 alkyl; provided that, if (L) is —CH2— or —CH(CH3)—, then X is not 0. The compounds of the invention are useful in the treatment of diseases such as cancer and neurodegenerative diseases.
    • 本发明涉及式(I)化合物:(A')x-(A) - (B) - (Z) - (L)-C(= O)NH 2或其药学上可接受的盐或溶剂合物,其中: A)是杂芳基或芳基; 每个(A')如果存在,独立地选自芳基,芳基烷氧基,芳烷基,杂环基,芳氧基,卤素,烷氧基,卤代烷基,环烷基,卤代烷氧基和氰基,其中每个(A')被0,1,2 或3个独立地选自卤素,卤代烷基,芳基,芳基烷氧基,烷基,烷氧基,氰基,磺酰基,亚磺酰基和羧酰胺的取代基; X为0,1,2或3; (B)是环丙基环,其中(A)和(Z)与(B)的不同碳原子共价结合; (Z)为-NH-; 和(L)是 - (CH 2)m CR 1,R 2 - ,其中m是0,1,2,3,4,5或6,并且其中R 1和R 2各自独立地是氢或C 1 -C 6烷基; 条件是,如果(L)是-CH 2 - 或-CH(CH 3) - ,则X不为0.本发明的化合物可用于治疗疾病如癌症和神经变性疾病。
    • 8. 发明授权
    • Lysine specific demethylase-1 inhibitors and their use
    • 赖氨酸特异性脱甲基酶-1抑制剂及其用途
    • US08722743B2
    • 2014-05-13
    • US13641916
    • 2011-04-19
    • Alberto Ortega MunozJulio Castro-Palomino LariaMatthew Colin Thor Fyfe
    • Alberto Ortega MunozJulio Castro-Palomino LariaMatthew Colin Thor Fyfe
    • A61K31/165C07C211/00
    • C07C217/74A61K31/135A61K31/165A61K45/06A61N5/10C07C211/35C07C211/40C07C211/42C07C217/52C07C237/24C07C2101/02C07C2101/14C07C2101/18C07C2102/08C07C2102/10C07C2601/02C07C2601/14C07C2601/18C07C2602/08C07C2602/10
    • The present invention relates to a compound of Formula 1, wherein: (A) is heteroaryl or aryl; each (A′), if present, is independently chosen from aryl, arylalkoxy, arylalkyl, heterocyclyl, aryloxy, halo, alkoxy, haloalkyl, cycloalkyl, haloalkoxy, and cyano, wherein each (A′) is substituted with 0, 1, 2, or 3 substituents independently chosen from halo, haloalkyl, haloalkoxy, aryl, arylalkoxy, alkyl, alkoxy, amido, —CH2C(=0)NH2, heteroaryl, cyano, sulfonyl, and sulfinyl; X is 0, 1, 2, or 3; (B) is a cyclopropyl ring, wherein (A) and (Z) are covalently bonded to different carbon atoms of (B); (Z) is —NH—; (L) is chosen from a single bond, —CH2—, —CH2CH2—, —CH2CH2CH2—, and —CH2CH2CH2CH2—; and (D) is an aliphatic carbocyclic group or benzocycloalkyl, wherein said aliphatic carbocyclic group or said benzocycloalkyl has 0, 1, 2, or 3 substituents independently chosen from —NH2, —NH(C1-C6 alkyl), —N(C1-C6 alkyl)(C1-C6 alkyl), alkyl, halo, amido, cyano, alkoxy, haloalkyl, and haloalkoxy. (A′)X-(A)-(B)—(Z)-(L)-(D) formula (I) The compounds of the invention show activity for inhibiting LSD1, which makes them useful in the treatment or prevention of diseases such as cancer.
    • 本发明涉及式1的化合物,其中:(A)是杂芳基或芳基; 每个(A')如果存在,独立地选自芳基,芳基烷氧基,芳基烷基,杂环基,芳氧基,卤素,烷氧基,卤代烷基,环烷基,卤代烷氧基和氰基,其中每个(A')被0,1,2 ,或3个独立地选自卤素,卤代烷基,卤代烷氧基,芳基,芳基烷氧基,烷基,烷氧基,酰氨基,-CH 2 C(= O)NH 2,杂芳基,氰基,磺酰基和亚磺酰基的取代基。 X为0,1,2或3; (B)是环丙基环,其中(A)和(Z)与(B)的不同碳原子共价结合; (Z)为-NH-; (L)选自单键-CH 2 - , - CH 2 CH 2 - , - CH 2 CH 2 CH 2 - 和-CH 2 CH 2 CH 2 CH 2 - ; - 和(D)是脂族碳环基或苯并环烷基,其中所述脂族碳环基或所述苯并环烷基具有0,1,2或3个独立地选自-NH 2,-NH(C 1 -C 6烷基), - N(C1- C6烷基)(C1-C6烷基),烷基,卤素,酰胺基,氰基,烷氧基,卤代烷基和卤代烷氧基。 (A')X-(A) - (B) - (Z) - (L) - (D)式(I)本发明化合物显示出抑制LSD1的活性,使其可用于治疗或预防 疾病如癌症。