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    • 2. 发明申请
    • TRIAZOLOPYRIDINES AS PHOSPHODIESTERASE INHIBITORS FOR TREATMENT OF DERMAL DISEASES
    • 作为磷酸二酯酶抑制剂治疗牙齿疾病的三唑吡啶
    • US20100113442A1
    • 2010-05-06
    • US12595922
    • 2008-04-16
    • Jakob FeldingMorten Dahl Sornesen
    • Jakob FeldingMorten Dahl Sornesen
    • A61K31/437C07D471/04A61K31/5377A61K31/497A61P35/00A61P17/02A61P17/10
    • C07D471/04A61K31/437
    • The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH2, CH2—CH2, CH2—NH, or NH; R1 is halogen, or R1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkyl, alkoxycarbonyl, aryl, all of which are optionally substituted; R2 is hydrogen, or R2 is alkyl, cycloalkyl, alkoxy, heterocycloalkyl, aryl, heteroaryl, alkoxycarbonyl, aminocarbonyl, amino, all of which are optionally substituted; A is aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocycloalkyl or heterocycloalkenyl, all of which are optionally substituted; and pharmaceutically acceptable salts, hydrates, or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments, in particular for the treatment of dermal diseases.
    • 本发明涉及式(I)化合物,其中X和Y为C和N或N和C; Z是CH 2,CH 2 -CH 2,CH 2 -NH或NH; R1是卤素,或R1是烷基,烯基,炔基,卤代烷基,烷氧基,环烷基,烷氧基羰基,芳基,它们都是任选被取代的; R2是氢,或R2是烷基,环烷基,烷氧基,杂环烷基,芳基,杂芳基,烷氧基羰基,氨基羰基,氨基,它们都是任选被取代的; A是芳基,环烷基,环烯基,杂芳基,杂环烷基或杂环烯基,它们都是任选被取代的; 和其药学上可接受的盐,水合物或溶剂合物。 本发明还涉及用于治疗的所述化合物,包含所述化合物的药物组合物,治疗疾病的方法,例如, 所述化合物的皮肤病,以及所述化合物在制备药物中的用途,特别是用于治疗真皮疾病。
    • 5. 发明授权
    • Matrix metalloproteinase inhibitors
    • 基质金属蛋白酶抑制剂
    • US06521606B2
    • 2003-02-18
    • US09899017
    • 2001-07-06
    • Morten Dahl SørensenLars Kristian Albert BlæhrMette Knak Christensen
    • Morten Dahl SørensenLars Kristian Albert BlæhrMette Knak Christensen
    • A61K3166
    • A61K31/675C07F9/65842
    • A compound of the general formula I wherein Y is O or S; n is 1, 2, 3 or 4; X represents hydroxamic acid, carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R1 is wherein E, when present represents, a bond or optionally substituted methylene or ethylene; s and t are independently 0, 1, 2 or 3; A and A′ independently represent a bond, or a saturated or unsaturated, optionally substituted cyclic or heterocyclic hydrocarbon di- or triradical; Z represents a bond, O, S, C(O), C(O)NR7, NR7C(O) or NR7, wherein R7 is hydrogen, hydroxy, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R5 represents a bond, alkane or alkene diradical, one or more ether diradicals (R—O—R′) or amine diradicals (R—N—R′), wherein R and R′ independently represent alkane or alkene diradicals with a C-content from 0 to 3; R6 represents hydrogen, hydroxy, halogen, cyano, nitro, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical, unsaturated optionally substituted cyclic or heterocyclic hydrocarbon radical, NR8R9, C(O)NR8R9, C(O)R8, CO(O)R8, S(O)2R9, wherein each R8 and R9 independently represent hydrogen, halogen, a branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R2 represents hydrogen, (C1-8)alkyl, (C2-6)alkenyl, (C3-8)cycloalkyl, aryl(C0-6)alkyl or heteroaryl(C0-6)alkyl; provided that if A, A′, Z and R5 are all bonds, and s and t are both 0 (zero), then R6 is different from hydrogen; or a salt, hydrate or solvate thereof. The compounds are valuable for human and veterinary therapy.
    • 通式I的化合物,其中Y为O或S; n为1,2,3或4; X为异羟肟酸,羧酸,膦酸,乙酰硫代甲基或巯基甲基; R1为E时,当存在时为 键或任选取代的亚甲基或亚乙基; s和t独立地为0,1,2或3; A和A'独立地表示键,或饱和或不饱和的任选取代的环状或杂环烃二取代或杂芳基; Z表示 键,O,S,C(O),C(O)NR7,NR7C(O)或NR7,其中R7是氢,羟基,支链或直链,饱和或不饱和的任选取代的烃基; R 5表示键, 或二烯基双基,一个或多个醚双基(RO-R')或胺二基(RN-R'),其中R和R'独立地表示C含量为0至3的烷烃或烯烃双基; R 6表示氢, 羟基,卤素,氰基,硝基,支链或直链,饱和或不饱和的,任选取代的氢化物 芳基,不饱和的任选取代的环状或杂环烃基,NR 8 R 9,C(O)NR 8 R 9,C(O)R 8,CO(O)R 8,S(O)2 R 9,其中各R 8和R 9分别代表氢,卤素, 分支或直链,饱和或不饱和的任选取代的烃基; R 2表示氢,(C 1-8)烷基,(C 2-6)烯基,(C 3-8)环烷基,芳基(C 0-6)烷基或杂芳基 6)烷基;条件是如果A,A',Z和R5都是键,并且s和t均为0(零),则R6不同于氢;或其盐,水合物或溶剂化物。化合物是有价值的 用于人类和兽医治疗。
    • 8. 发明授权
    • Triazolopyridines as phosphodiesterase inhibitors for treatment of dermal diseases
    • 三唑并吡啶类作为治疗皮肤疾病的磷酸二酯酶抑制剂
    • US08829190B2
    • 2014-09-09
    • US12595922
    • 2008-04-16
    • Jakob FeldingMorten Dahl Sørensen
    • Jakob FeldingMorten Dahl Sørensen
    • C07D471/04A61K31/437
    • C07D471/04A61K31/437
    • The present invention relates to a compound according to formula (I), wherein X and Y are either C and N or N and C; Z is CH2, CH2—CH2, CH2—NH, or NH; R1 is halogen, or R1 is alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, cycloalkyl, alkoxycarbonyl, aryl, all of which are optionally substituted; R2 is hydrogen, or R2 is alkyl, cycloalkyl, alkoxy, heterocycloalkyl, aryl, heteroaryl, alkoxycarbonyl, aminocarbonyl, amino, all of which are optionally substituted; A is aryl, cycloalkyl, cycloalkenyl, heteroaryl, heterocycloalkyl or heterocycloalkenyl, all of which are optionally substituted; and pharmaceutically acceptable salts, hydrates, or solvates hereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments, in particular for the treatment of dermal diseases.
    • 本发明涉及式(I)化合物,其中X和Y为C和N或N和C; Z是CH 2,CH 2 -CH 2,CH 2 -NH或NH; R1是卤素,或R1是烷基,烯基,炔基,卤代烷基,烷氧基,环烷基,烷氧基羰基,芳基,它们都是任选被取代的; R2是氢,或R2是烷基,环烷基,烷氧基,杂环烷基,芳基,杂芳基,烷氧基羰基,氨基羰基,氨基,它们都是任选被取代的; A是芳基,环烷基,环烯基,杂芳基,杂环烷基或杂环烯基,它们都是任选被取代的; 和其药学上可接受的盐,水合物或溶剂合物。 本发明还涉及用于治疗的所述化合物,包含所述化合物的药物组合物,治疗疾病的方法,例如, 所述化合物的皮肤病,以及所述化合物在制备药物中的用途,特别是用于治疗真皮疾病。