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    • 1. 发明授权
    • Peptidyl derivatives
    • 肽基衍生物
    • US5889058A
    • 1999-03-30
    • US335957
    • 1994-11-03
    • John Robert PorterThomas Andrew MillicanJohn Richard MorphyNigel Robert Arnold Beeley
    • John Robert PorterThomas Andrew MillicanJohn Richard MorphyNigel Robert Arnold Beeley
    • A61K31/19A61K31/195C07C229/04C07C229/24C07C229/28C07C233/05C07C233/08C07C237/06
    • A61K31/195
    • Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastases. ##STR1##
    • 其中R代表-CON​​HOH,羧基(-CO 2 H)或酯化的羧基;式(I)化合物的使用方法; R 1表示氢原子或任选取代的烷基,烯基,芳基,芳烷基,杂芳烷基或杂芳硫基烷基; R2表示任选取代的苯乙基,苯基丙基或苯基丁基; R3表示氢原子或烷基; R4表示氢原子或烷基; R5表示任选被一个或多个-O-或-S-原子或-N(R 7) - 基团(其中R 7是氢原子或C 1-6烷基)间隔的任选取代的烷基或烯基; X表示氨基(-NH 2)或取代的氨基,羟基或取代的羟基; 及其盐,溶剂化物和水合物。 化合物是金属蛋白酶抑制剂,特别是具有选择性明胶酶作用,并且可用于治疗癌症以控制肿瘤转移的发展。 (一)
    • 3. 发明授权
    • N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives
    • N - [(1-二甲基氨基环烷基)甲基]苯甲酰胺衍生物
    • US07126027B2
    • 2006-10-24
    • US10484410
    • 2002-07-11
    • John Richard MorphyZoran Rankovoc
    • John Richard MorphyZoran Rankovoc
    • C07C233/65A61K31/165
    • C07D333/16C07C235/50C07C2601/04C07C2601/08C07C2601/14C07C2601/18
    • The present invention relates to N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives having the general formula I wherein n is 0, 1, 2 or 3; R1 and R2 are independently H, (C1-4)alkyl or (C1-4)alkyloxy; R3 is (C3-8)alkyl, (C4-7)cycloalkyl, (C4-7)cycloalkyl (C1-3)alkyl, (C6-12)aryl(C1-3)alkyl (wherein the aryl moiety is optionally substituted with 1–3 substituents selected from (C1-4)alkyl, (C1-4)alkyloxy, halogen, trifluoromethyl and methoxycarbonyl), or (C4-9)heteroaryl(C1-3)alkyl; or a pharmaceutically acceptable salt thereof. The invention also relates to pharmaceutical compositions comprising said derivatives, and to the use of these N-[(1-dimethylaminocycloalkyl)methyl]benzamide derivatives in the treatment of disorders or conditions which are responsive to inhibition of the GlyT-2 transporter, such as muscle spasticity, epilepsy and, particularly, acute, chronic and neuropathic pain.
    • 本发明涉及具有通式I的N - [(1-二甲基氨基环烷基)甲基]苯甲酰胺衍生物,其中n为0,1,2或3; R 1和R 2独立地是H,(C 1-4烷基)烷基或(C 1-4) )烷氧基; R 3是(C 3-8)烷基,(C 1-4-7)环烷基,(C 1-4 - (C 1-3)烷基,(C 6-12)芳基(C 1-3-2烷基)烷基(其中 芳基部分任选被1-3个选自(C 1-4烷基)烷基,(C 1-4 - 烷基)烷氧基,卤素,三氟甲基和甲氧基羰基的取代基取代)或 (C 1-4 - )杂芳基(C 1-3-3烷基)烷基; 或其药学上可接受的盐。 本发明还涉及包含所述衍生物的药物组合物,以及这些N - [(1-二甲基氨基环烷基)甲基]苯甲酰胺衍生物用于治疗对抑制GlyT-2转运蛋白有反应的病症或病症的用途,例如 肌肉痉挛,癫痫,特别是急性,慢性和神经性疼痛。
    • 10. 发明授权
    • 6-substituted isoquinoline derivatives
    • 6-取代的异喹啉衍生物
    • US07893088B2
    • 2011-02-22
    • US11839703
    • 2007-08-16
    • Peter Christopher RaySteven LaatsJohn Richard MorphyBrad Sherborne
    • Peter Christopher RaySteven LaatsJohn Richard MorphyBrad Sherborne
    • C07D217/00A61K31/47
    • C07D217/22C07D217/24
    • The present invention relates to 6-substituted isoquinoline derivatives having the general Formula I wherein X is O, S or NH; Y is OH or NH2; m is 0, 1 or 2; n is 0 or 1; o is 0 or 1; R1 is H, when Y is NH2; or R1 is H, (C1-4)alkyl or halogen, when Y is OH; R2 and R3 are independently H, (C1-4)alkyl or halogen; R4 is H or (C1-6)alkyl, optionally substituted with halogen, (C3-7)cycloalkyl, (C6-10)aryl or a saturated 5- or 6-membered heterocyclic ring comprising 1-3 heteroatoms independently selected from O, S and N, the (C6-10)aryl and heterocyclic ring being optionally substituted with (C1-4)alkyl, (C1-4)alkyloxy or halogen; R5 is H or (C1-4)alkyl; or a pharmaceutically acceptable salt thereof, with the proviso that the compounds of Formula I wherein X is O, Y is OH , n is 0 and m+o=2 are excluded, to pharmaceutical compositions comprising the same, as well as to the use of said 6-substituted isoquinoline derivatives for the preparation of a medicament for the treatment of ROCK-I related disorders such as glaucoma, hypertension and atherosclerosis.
    • 本发明涉及具有通式I的6-取代的异喹啉衍生物,其中X是O,S或NH; Y是OH或NH 2; m为0,1或2; n为0或1; o为0或1; 当Y为NH 2时,R 1为H; 或者当Y为OH时,R 1为H,(C 1-4)烷基或卤素; R2和R3独立地是H,(C1-4)烷基或卤素; R4是H或(C 1-6)烷基,任选地被卤素,(C 3-7)环烷基,(C 6-10)芳基或饱和的5-或6-元杂环包含1-3个独立地选自O, S和N,(C 6-10)芳基和杂环任选被(C 1-4)烷基,(C 1-4)烷氧基或卤素取代; R5是H或(C1-4)烷基; 或其药学上可接受的盐,条件是其中X为O,Y为OH,n为0且m + o = 2的式I化合物排除于包含该化合物的药物组合物中,以及使用 的所述6-取代的异喹啉衍生物用于制备用于治疗ROCK-1相关疾病如青光眼,高血压和动脉粥样硬化的药物。