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
    • Compounds having CRTH2 antagonist activity
    • 具有CRTH2拮抗活性的化合物
    • US08563536B2
    • 2013-10-22
    • US13017860
    • 2011-01-31
    • Richard Edward ArmerEric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • Richard Edward ArmerEric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • A61K31/70A61K31/56A61K31/50A61K31/47A61K31/44
    • A61K31/4439A61K31/47A61K45/06C07D401/06
    • Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    • 通式(II)的化合物,其中W是氯或氟; R 1是任选被一个或多个选自卤素,-CN,-C 1 -C 6烷基,-SOR 3,-SO 2 R 3,-SO 2 N(R 2)2,-N(R 2)2,-NR 2 C(O)R 3 ,-CO 2 R 2,-CONR 2 R 3,-NO 2,-OR 2,-SR 2,-O(CH 2)pOR 2或-O(CH 2)p O(CH 2)q OR 2,其中每个R 2独立地是氢,-C 1 -C 6烷基, C8环烷基,芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基,-C 3 -C 8环烷基,芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基,(CH2)mOC(= O)C1-C6烷基,((CH2)mO)nCH2CH2X,(CH2)mN(R5)2或CH ((CH 2)m O(C = O)R 6)2; m为1或2; n为1-4; X为OR 5或N(R 5)2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐,水合物,溶剂合物,复合物或前药可用于口服给药的组合物中,用于治疗过敏性疾病如哮喘,过敏性鼻炎和特应性皮炎。
    • 4. 发明授权
    • Compounds having CRTH2 antagonist activity
    • 具有CRTH2拮抗活性的化合物
    • US08536158B2
    • 2013-09-17
    • US13014314
    • 2011-01-26
    • Richard Edward ArmerEric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • Richard Edward ArmerEric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • A61K31/70A61K31/56A61K31/50A61K31/47A61K31/44
    • A61K31/4439A61K31/47A61K45/06C07D401/06
    • Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    • 通式(I)的化合物,其中W是氯或氟; R 1是任选被一个或多个选自卤素,-CN,-C 1 -C 6烷基,-SOR 3,-SO 2 R 3,-SO 2 N(R 2)2,-N(R 2)2,-NR 2 C(O)R 3 ,-CO 2 R 2,-CONR 2 R 3,-NO 2,-OR 2,-SR 2,-O(CH 2)pOR 2或-O(CH 2)p O(CH 2)q OR 2,其中每个R 2独立地是氢,-C 1 -C 6烷基, C8环烷基,芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基,-C 3 -C 8环烷基,芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基,(CH2)mOC(= O)C1-C6烷基,((CH2)mO)nCH2CH2X,(CH2)mN(R5)2或CH ((CH 2)m O(C = O)R 6)2; m为1或2; n为1-4; X为OR 5或N(R 5)2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐,水合物,溶剂合物,复合物或前药可用于口服给药的组合物中,用于治疗过敏性疾病如哮喘,过敏性鼻炎和特应性皮炎。
    • 6. 发明申请
    • Compounds Having CRTH2 Antagonist Activity
    • 具有CRTH2拮抗作用的化合物
    • US20100063103A1
    • 2010-03-11
    • US12625497
    • 2009-11-24
    • Richard Edward ARMEREric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • Richard Edward ARMEREric Roy PettipherMark WhittakerGraham Michael WynneJulia VileFrank Schroer
    • A61K31/4439C07D401/06A61P37/08
    • A61K31/4439A61K31/47A61K45/06C07D401/06
    • Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
    • 通式(I)的化合物,其中W是氯或氟; R 1是任选被一个或多个选自卤素,-CN,-C 1 -C 6烷基,-SOR 3,-SO 2 R 3,-SO 2 N(R 2)2,-N(R 2)2,-NR 2 C(O)R 3 ,-CO 2 R 2,-CONR 2 R 3,-NO 2,-OR 2,-SR 2,-O(CH 2)pOR 2或-O(CH 2)p O(CH 2)q OR 2,其中每个R 2独立地是氢,-C 1 -C 6烷基, C8环烷基,芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基,-C 3 -C 8环烷基,芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基,(CH2)mOC(= O)C1-C6烷基,((CH2)mO)nCH2CH2X,(CH2)mN(R5)2或CH ((CH 2)m O(C = O)R 6)2; m为1或2; n为1-4; X为OR 5或N(R 5)2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐,水合物,溶剂合物,复合物或前药可用于口服给药的组合物中,用于治疗过敏性疾病如哮喘,过敏性鼻炎和特应性皮炎。
    • 7. 发明申请
    • Glyoxalase inhibitors
    • 乙二醛酶抑制剂
    • US20070015799A1
    • 2007-01-18
    • US10556901
    • 2004-05-14
    • Mark AshtonAlan DavidsonRussell ThomasMark Whittaker
    • Mark AshtonAlan DavidsonRussell ThomasMark Whittaker
    • A61K31/4436A61K31/44A61K31/381
    • C07D405/04A61K31/10A61K31/381A61K31/44A61K31/4436C07C323/62C07D213/85C07D217/26C07D409/04C07D409/14
    • This invention relates to compounds of formula (I) which are glyoxalase I inhibitors, pharmaceutical salts or compositions comprising such compounds, and the use of such compositions and compounds to treat various conditions alleviated by the inhibition of glyoxalase 1. Wherein X is N or CH. R2 is H, CF3; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. R3 is H; or optionally substituted C5-6 aryl, C3-7 cycloalkyl, C5-7 heterocyclyl. Alternatively R2 and R3 together form an optionally substituted C3-4alkylene group wherein L3 and L4 are single bonds thus forming a C5-6 ring fused with the aromatic ring to which L3 and L4 are attached. L3 and L4 are independently selected from a single bond, optionally substituted C1-4 alkylene, -L9YN(OH)C(═O)L10- and -L9C(═O)N(OH)YL10-, wherein L9 and L10 are independently selected from optionally substituted C1-4 alkylene, C5-6 arylene, C1-4 alkylene-C5-6arylene and a single bond, wherein Y is NH or a single bond.
    • 本发明涉及作为乙二醛酶I抑制剂的式(I)化合物,包含这些化合物的药物盐或组合物,以及这些组合物和化合物用于治疗通过抑制乙二醛酶1减轻的各种病症的用途。其中X是N或CH 。 R 2是H,CF 3 N; 或任选取代的C 5-6芳基,C 3-7环烷基,C 5-7杂环基。 R 3是H; 或任选取代的C 5-6芳基,C 3-7环烷基,C 5-7杂环基。 或者R 2和R 3一起形成任选取代的C 3-4亚烷基,其中L 3和L 3 因此形成与L 3和L 4的芳环稠合的C 5〜6环, SUP>连接。 L 3和L 4独立地选自单键,任选取代的C 1-4亚烷基,-L 9, SUP-YN(OH)C(-O)L 10 - 和-L 9 C( - )N(OH)Y L 10 - ,其中L 9和L 10独立地选自任选取代的C 1-4 - 亚烷基,C 5-6 - 亚芳基,C 1-4亚烷基-C 5-6亚芳基和单键,其中Y是NH或单键。