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    • 6. 发明授权
    • Pyrazolopyridine compound and pharmaceutical use thereof
    • 吡唑并吡啶化合物及其药物用途
    • US6124456A
    • 2000-09-26
    • US147543
    • 1999-01-19
    • Atsushi AkahaneSatoru KurodaHiromichi ItaniYasuyo Shimizu
    • Atsushi AkahaneSatoru KurodaHiromichi ItaniYasuyo Shimizu
    • A61K31/501A61P1/04A61P3/10A61P9/00A61P11/06A61P13/12A61P25/00A61P37/06A61P43/00C07D471/04A61K31/497
    • C07D471/04
    • A pyrazolopyridine compound of formula (I) wherein R.sup.1 is aryl, and R.sup.2 is lower alkyl substituted with unsaturated 3 to 8-membered heteromonocyclic group containing 1 or 2 sulfur atom(s) and 1 to 3 nitrogen atom(s) which may have one or more substituent(s); a group of formula (1) wherein R.sup.3 is hydrogen, lower alkyl, ar(lower)alkyl or acyl, R.sup.4 is hydrogen or hydroxy, A is lower alkylene, m is an integer of 0 or 1, and n is an integer of 1 or 2; a group of formula (2) wherein R.sup.5 and R.sup.6 are each lower alkyl; or quinuclidinyl, or a salt the The pyrazolopyridine compound (I) and a salt thereof of the present invention are adenosine antagonists and are useful for the prevention and/or treatment of depression, dementia (e.g. Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, etc.), anxiety, pain, cerebrovascular disease (e.g. stroke, etc.), heart failure, and the like.
    • PCT No.PCT / JP97 / 02493 Sec。 371日期1999年1月19日 102(e)1999年1月19日PCT PCT 1997年7月17日PCT公布。 第WO98 / 03507号公报 日本1998年1月29日,式(I)的吡唑并吡啶化合物,其中R1为芳基,R2为被1或2个硫原子和1〜3个氮原子(s)的不饱和3〜8元杂单环取代的低级烷基 ),其可以具有一个或多个取代基; 式(1)的基团,其中R 3是氢,低级烷基,芳基(低级)烷基或酰基,R 4是氢或羟基,A是低级亚烷基,m是0或1的整数,n是整数1 或2; 式(2)的基团,其中R 5和R 6各自为低级烷基; 或奎宁环基或其盐本发明的吡唑并吡啶化合物(I)及其盐是腺苷拮抗剂,可用于预防和/或治疗抑郁症,痴呆(例如阿尔茨海默病,脑血管性痴呆,帕金森病等) ),焦虑,疼痛,脑血管疾病(例如中风等),心力衰竭等。
    • 7. 发明授权
    • 1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds
    • 1-氮杂双环[3.2.0]庚-2-烯-2-羧酸化合物
    • US5286721A
    • 1994-02-15
    • US853746
    • 1992-06-12
    • Masayoshi MurataToshiyuki ChibaHideo TsutsumiKohji HattoriSatoru KurodaHiroaki OhtakeFumiyuki Shirai
    • Masayoshi MurataToshiyuki ChibaHideo TsutsumiKohji HattoriSatoru KurodaHiroaki OhtakeFumiyuki Shirai
    • C07D477/14C07D477/00
    • C07D477/14
    • 1-Azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid compounds of the formula: ##STR1## in which R.sup.1 is carboxy, COO.sup.-- or protected carboxy,R.sup.2 is hydroxy(lower)alkyl or protected hydroxy(lower)alkyl,R.sup.8 is hydrogen or lower alkyl,Z is a group of the formula: ##STR2## wherein R.sup.3 is hydrogen; lower alkyl or lower alkenyl, each of which is optionally substituted by the group consisting of lower alkoxy, carbamoyl, hydroxy, halogen, mono(or di)(lower)alkylcarbamoyl, mono(or di)(lower)alkenylcarbamoyl, mono(or bis)[hydroxy(lower)alkyl]carbamoyl, optionally substituted cyclic-aminocarbonyl, acylamino, ureido, optionally substituted heterocyclic-carbonylamino, carbamoyloxy, mono(or di)(lower)alkylcarbamoyloxy, lower alkylthio, halo(lower)alkylthio, optionally substituted heterocyclicthio, optionally substituted heterocyclic group, optionally substituted aryl, and acyl;R.sup.9 is hydrogen or lower alkyl, andR.sup.10 is lower alkyl,or pharmaceutically acceptable salts thereof, which is useful as an antimicrobial agent.
    • PCT No.PCT / JP91 / 01394 Sec。 371日期:1992年6月12日 102(e)日期1992年6月12日PCT 1991年10月14日PCT PCT。 出版物WO92 / 06978 日期:4月30日,1992.1-氮杂双环(3.2.0)庚-2-烯-2-羧酸化合物,其结构式如下:(*化学结构*)其中R 1为羧基,COO-或被保护的羧基,R 2为羟基( 低级)烷基或被保护的羟基(低级)烷基,R 8是氢或低级烷基,Z是下列基团:(*化学结构*)其中R 3是氢; 羟基,卤素,单(或二)(低级)烷基氨基甲酰基,单(或二)(低级)烯基氨基甲酰基,单(或双(低级))链烯基氨基甲酰基, )(羟基(低级)烷基)氨基甲酰基,任选取代的环氨基羰基,酰氨基,脲基,任选取代的杂环羰基氨基,氨基甲酰氧基,单(或二)(低级)烷基氨基甲酰氧基,低级烷硫基,卤(低级)烷硫基, ,任选取代的杂环基,任选取代的芳基和酰基; R9为氢或低级烷基,R10为低级烷基,或其药学上可接受的盐,可用作抗微生物剂。