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    • 33. 发明授权
    • Neurotrophic factor secretion promoters
    • 神经营养因子分泌促进剂
    • US06433019B1
    • 2002-08-13
    • US09601186
    • 2000-07-28
    • Hiroyuki Nawa
    • Hiroyuki Nawa
    • A61K3141
    • A61K31/5377A61K31/00A61K31/15A61K31/16A61K31/198A61K31/21A61K31/34
    • The present invention relates to a neurotrophic factor secretagogue, in particular, to a BDNF (brain-derived neurotrophic factor) secretagogue, which comprises as an active ingredient an NO donor. The medicament of the present invention promotes the secretion of neurotrophic factors from mammalian central neural cells. Thus, the medicament of the present invention, i.e., NO donor, is possibly applicable to the treatment of diseases caused by neutrotrophic factors, for example, neurodegenerative diseases, and is expected to exhibit the efficacious effects thereon. Also, the present invention provides a novel medication for neurodegenerative diseases.
    • 本发明涉及神经营养因子促分泌素,特别涉及BDNF(脑源性神经营养因子)促分泌素,其包含作为活性成分的NO供体。 本发明的药物促进哺乳动物中枢神经细胞分泌神经营养因子。 因此,本发明的药物即NO供体可能适用于治疗由中性营养因子引起的疾病,例如神经变性疾病,并且预期其对其有显着的效果。 另外,本发明提供了用于神经变性疾病的新型药物。
    • 38. 发明授权
    • Aqueous agents for combating parasitic insects and acarina in human beings
    • 用于防治人类寄生昆虫和螨虫的水剂
    • US06369054B1
    • 2002-04-09
    • US09601572
    • 2000-08-03
    • Kirkor SirinyanKarin HornRonald Helmut StöckerRainer Sonneck
    • Kirkor SirinyanKarin HornRonald Helmut StöckerRainer Sonneck
    • A61K3141
    • A01N51/00A01N61/00A01N43/08A01N31/02A01N25/02A01N2300/00
    • The present invention relates to water-containing formulations for the dermal control of parasitic insects and mites on humans, said formulations having the following composition: a—agonists or antagonists of the nicotinic acetylcholine receptors of insects in a concentration of from 0.0001 to 7.5% by weight, based on the overall weight of the formulation; b—water in a concentration of from 20 to 50% by weight, based on the overall weight of the formulation; c—acyclic alcohols in a concentration of from 20 to 50% by weight, based on the overall weight of the formulation; d—solvents from the group consisting of cyclic carbonates and lactones in a concentration of from 2.5 up to 20.0% by weight, based on the overall weight of the formulation; e—optionally further auxiliaries from the group consisting of thickeners, spreading agents, colorants, antioxidants, propellants, preservatives, tackifiers, emulsifiers, in a concentration of from 0 up to 30% by weight, based on the overall weight of the formulation.
    • 本发明涉及用于真皮控制人类寄生昆虫和螨虫的含水制剂,所述制剂具有以下组成:昆虫的烟碱乙酰胆碱受体的α-激动剂或拮抗剂,其浓度为0.0001至7.5%,浓度为 重量,基于制剂的总重量;基于制剂的总重量,浓度为20至50重量%的b-水;浓度为20至50重量%的c-无环醇 ,基于制剂的总重量;基于制剂总重量的2.5重量%至20.0重量%的来自环状碳酸酯和内酯的d-溶剂; e-任选的另外的辅助剂 基于总重量的浓度为0至30重量%的增稠剂,铺展剂,着色剂,抗氧化剂,推进剂,防腐剂,增粘剂,乳化剂组成的组 公式。
    • 39. 发明授权
    • Benzofuroxan derivatives, their therapeutic uses and pharmaceutical compositions
    • 苯并呋喃衍生物,其治疗用途和药物组合物
    • US06232331B1
    • 2001-05-15
    • US09690805
    • 2000-10-18
    • Alangudi Sankaranarayanan
    • Alangudi Sankaranarayanan
    • A61K3141
    • A61K31/4245C07D271/12
    • The invention discloses use of a compound of the benzofuroxan series for treatment of cardiovascular disorders represented by the general formula (I) and pharmaceutically acceptable salts thereof wherein: R is halogen, acetoxy, —X—R′, —C(O)NR″R′″, or —C(O)Cl; X is oxygen, sulfur, —C(O)—, or —C(O)O—; R′ is hydrogen, straight chain or branched lower alkyl (C1-C8); R″ and R′″ are independently hydrogen, straight chain or branched lower alkyl (C1-C8) or R″ and R′″ are linked together with or without a heteroatom selected from the group consisting of oxygen and nitrogen wherein substitution on nitrogen is with hydrogen or lower alkyl. The invention further discloses pharmaceutical compositions containing compounds of general formula I as active ingredients. The invention also discloses a method of treatment of mammal, including man, of coronary heart disease by administration of an effective amount of a compound of formula I as defined above.
    • 本发明公开了苯并呋喃酮系列化合物用于治疗由通式(I)表示的心血管疾病及其药学上可接受的盐的用途,其中:R为卤素,乙酰氧基,-X-R',-C(O)NR' R'是-C(O)Cl; X是氧,硫,-C(O) - 或-C(O)O-; R'是氢,直链或支链的低级烷基(C1- C8); R“和R”'独立地是氢,直链或支链的低级烷基(C1-C8)或R“和R”'与或不具有选自氧的杂原子连接在一起 和氮,其中在氮上取代为氢或低级烷基。本发明还公开了含有通式I化合物作为活性成分的药物组合物。本发明还公开了一种通过给药治疗冠状动脉心脏病的哺乳动物(包括人)的方法 有效量的如上定义的式I化合物。
    • 40. 发明授权
    • Method of inhibiting connective tissue degradation
    • 抑制结缔组织降解的方法
    • US06211209B1
    • 2001-04-03
    • US09130215
    • 1998-08-06
    • Vijaykumar BaragiDiane Harris BoschelliDavid Thomas ConnorRichard Raymond RenkiewiczHoward Glenn Welgus
    • Vijaykumar BaragiDiane Harris BoschelliDavid Thomas ConnorRichard Raymond RenkiewiczHoward Glenn Welgus
    • A61K3141
    • A61K31/433A61K31/341A61K31/4196A61K31/4245A61K31/426
    • The present invention provides a method of inhibiting connective tissue degradation that comprises administering to a patient having a condition in which connective tissue is degraded a therapeutically effective amount of a compound having the formula where R1, R2, R3, and R4 are independently hydrogen, hydroxy, halo, amino, nitro, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, CF3, CN, S(O)n—, R6 and R7 are independently hydrogen, C1-C6 alkyl, or acyl; n is 0 to 2; R8 is hydrogen or C1-C6 alkyl; W is S or O; Z is C1-C6 alkyl, C1-C6 alkoxy, or NR9R10; R9 and R10 are independently hydrogen or C1-C6 alkyl; and R5 is where Y is hydroxy, thiol, amino, or NHCN; X is sulfur or oxygen; and Q is sulfur, oxygen, NH, or NCN, and the pharmaceutically acceptable salts and prodrugs thereof. Also provided is a method of inhibiting the production of matrix metalloproteinases comprising administering to a patient having a condition associated with matrix metalloproteinase-mediated tissue degradation a therapeutically effective amount of a compound having the formula where R1, R2, R3, and R4 are independently hydrogen, hydroxy, halo, amino, nitro, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C6 alkoxy, CF3, CN, S(O)n—, R6 and R7 are independently hydrogen, C1-C6 alkyl or acyl; n is 0 to 2; R8 is hydrogen or C1-C6 alkyl; W is S or O; Z is C1-C6 alkyl, C1-C6 alkoxy, or NR9R10; R9 and R10 are independently hydrogen or C1-C6 alkyl; and R5 is where Y is hydroxy, thiol, amino, or NHCN; X is sulfur or oxygen; and Q is sulfur, oxygen, NH, or NCN, and the pharmaceutically acceptable salts and prodrugs thereof.
    • 本发明提供了一种抑制结缔组织降解的方法,其包括对患有结缔组织降解的病症的患者施用治疗有效量的具有下式的化合物:R 1,R 2,R 3和R 4独立地为氢,羟基, 卤素,氨基,硝基,C 1 -C 6烷基,C 3 -C 6环烷基,C 1 -C 6烷氧基,CF 3,CN,S(O)n - ,R 6和R 7独立地是氢,C 1 -C 6烷基或酰基; n是0 R 2是氢或C 1 -C 6烷基; W是S或O; Z是C 1 -C 6烷基,C 1 -C 6烷氧基或NR 9 R 10; R 9和R 10独立地是氢或C 1 -C 6烷基; 和R 5是其中Y是羟基,硫醇,氨基或NHCN; X是硫或氧; 和Q是硫,氧,NH或NCN,及其药学上可接受的盐和前药。 还提供了抑制基质金属蛋白酶产生的方法,包括对具有与基质金属蛋白酶介导的组织降解有关的病症的患者施用治疗有效量的具有下式的化合物:R1,R2,R3和R4独立地是氢, 羟基,卤素,氨基,硝基,C1-C6烷基,C3-C6环烷基,C1-C6烷氧基,CF3,CN,S(O)n,R6和R7独立地是氢,C1-C6烷基或酰基; n是 0至2; R 8是氢或C 1 -C 6烷基; W是S或O; Z是C 1 -C 6烷基,C 1 -C 6烷氧基或NR 9 R 10; R 9和R 10独立地是氢或C 1 -C 6烷基; 和R 5是其中Y是羟基,硫醇,氨基或NHCN; X是硫或氧; 和Q是硫,氧,NH或NCN,及其药学上可接受的盐和前药。