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    • 1. 发明授权
    • Use of isoxazolin-3-one derivatives as antidepressants
    • 使用ISOXAZOLIN-3-ONE衍生物作为抗病毒剂
    • US5116839A
    • 1992-05-26
    • US537517
    • 1990-06-13
    • Nobuyoshi IwataKenji YoshimiMitsuo Nagano
    • Nobuyoshi IwataKenji YoshimiMitsuo Nagano
    • A61K9/48A61K31/41A61K31/42A61K31/535A61K38/01
    • A61K31/535A61K31/42
    • A method of treating depression comprising administering to a patient an effective antidepressive amount of a compound of the formula (I) ##STR1## wherein the endocyclic dotted line ##STR2## is a single bond; the exocyclic dotted line ##STR3## is a double bond; A is oxygen; B is a group of the formula (II) ##STR4## wherein m is 0 and n is 0 or 1; R.sup.3, R.sup.4 and the nitrogen to which they are attached together represent an alicyclic amino having a total of 5 or 6 ring atoms, of which one ring atom is the nitrogen and one ring atom is optionally an additional heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, the alicyclic amino being unsubstituted or, where there is an additional nitrogen heteroatom, the alicyclic amino having as a substituent a C.sub.1 -C.sub.3 alkyl on the additional nitrogen heteroatom; R.sup.1 is hydrogen or halogen; and R.sup.2 is an unsubstituted phenyl, a substituted phenyl having a substituent selected from the group consisting of C.sub.1-3 alkyl, C.sub.1-3 alkoxy, halogen and nitro, an unsubstituted 5- or 6-membered heterocyclic group having one or more of oxygen, sulfur or a nitrogen as heteroatoms, or a substituted 5- or 6-membered heterocyclic group having one or more of oxygen, sulfur or a nitrogen as heteroatoms and having at least one substituent selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1-3 alkoxy, halogen and nitro; or a pharmaceutically acceptable acid addition salt thereof.
    • 2. 发明授权
    • Use of isoxazolin-3-one derivatives as antidepressants
    • 异恶唑啉-3-酮衍生物作为抗抑郁药的使用
    • US5262413A
    • 1993-11-16
    • US11208
    • 1993-01-29
    • Nobuyoshi IwataKenji YoshimiMitsuo Nagano
    • Nobuyoshi IwataKenji YoshimiMitsuo Nagano
    • A61K31/42A61K31/535A61K31/41A61K31/54
    • A61K31/535A61K31/42
    • A method of treating depression comprising administering to a patient an effective amount of a compound of the formula (Ib): ##STR1## wherein R.sup.1b is hydrogen, halogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, an unsubstituted benzyl group, a substituted benzyl having at least one substitutent (b) selected from the group consisting of C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, hydroxy, halogen, nitro, amino and C.sub.2 -C.sub.4 aliphatic carboxylic acylamino; unsubstituted phenyl or a substituted phenyl having at least one substitutent (b); R.sup.2b is hydrogen, C.sub.1 -C.sub.4 alkyl, unsubstituted phenyl, substituted phenyl having at least one substitutent (b), unsubstituted 5- or 6- membered heterocyclic having an oxygen, sulfur or nitrogen as a heteroatom, or substituted 5- or 6- membered heterocyclic having an oxygen, sulfur or nitrogen as a heteroatom and having at least one substitutent (b); and R.sup.3b and R.sup.4b are the same or different and each is hydrogen, C.sub.1 -C.sub.4 alkyl, unsubstituted benzyl, substituted benzyl having at least one substituent (b), unsubstituted phenyl, or substituted phenyl having at least one substitutent (b); or R.sup.3b, R.sup.4b and the nitrogen atom to which they are attached together represent an alicyclic amino group having a total of 5 or 6 ring atoms, or which one ring atom is the nitrogen atom and one ring atom is optionally an additional heteroatom selected from the group consisting of nitrogen, oxygen and sulfur, the alicyclic amino group being unsubstituted or, where there is an additional nitrogen heteroatom, the alicyclic amino group having a C.sub.1 -C.sub.3 alkyl substitutent on the additional nitrogen heteroatom; or a pharmacologically acceptable acid addition salt thereof.
    • 治疗抑郁症的方法包括向患者施用有效量的式(Ib)化合物:其中R 1b是氢,卤素,C 1 -C 4烷基,C 2 -C 4烯基,C 2 -C 4炔基 ,未取代的苄基,具有至少一个选自C 1 -C 3烷基,C 1 -C 3烷氧基,羟基,卤素,硝基,氨基和C 2 -C 4脂族羧酸酰基氨基的取代基(b)的取代苄基; 未取代的苯基或具有至少一个取代基(b)的取代苯基; R2b是氢,C1-C4烷基,未取代的苯基,具有至少一个取代基(b)的取代苯基,具有氧,硫或氮作为杂原子的未取代的5-或6-元杂环,或取代的5-或6-元 具有氧,硫或氮作为杂原子且具有至少一个取代基(b)的杂环基; 并且R 3b和R 4b相同或不同,各自为氢,C 1 -C 4烷基,未取代的苄基,具有至少一个取代基的取代苄基(b),未取代的苯基或具有至少一个取代基(b)的取代的苯基。 或R 3b,R 4b和它们所连接的氮原子一起表示具有总共5或6个环原子的脂环族氨基,或者一个环原子是氮原子,一个环原子任选地是选自以下的杂原子: 由氮,氧和硫组成的组,脂环族氨基是未取代的,或者在另外的氮杂原子上,在另外的氮杂原子上具有C1-C3烷基取代基的脂环族氨基; 或其药理学上可接受的酸加成盐。
    • 3. 发明授权
    • Use of isoxazolin-3-one derivatives as antidepressants
    • 异恶唑啉-3-酮衍生物作为抗抑郁药的使用
    • US5217970A
    • 1993-06-08
    • US856494
    • 1992-03-24
    • Nobuyoshi IwataKenji YoshimiMitsuo Nagano
    • Nobuyoshi IwataKenji YoshimiMitsuo Nagano
    • A61K31/42A61K31/535
    • A61K31/535A61K31/42
    • A method of treating depression comprising administering to a patient an effective antidepressive amount of a compound of the formula ##STR1## wherein either (i) the endocyclic dotted line ( ) is a double bond; the exoxyclic dotted line ( ) is a single bond;A is ##STR2## m is 1; n is 0; R.sup.3 and R.sup.4 are hydrogen, C.sub.1 -C.sub.4 alkyl, benzyl or phenyl or R.sup.3, R.sup.4 and the nitrogen to which they are attached represent an alicyclic amino having 5 or 6 ring atoms, of which one ring atom is nitrogen and one ring atom is optionally an additional nitrogen, oxygen or sulfur heteroatom; R.sup.1 is hydrogen, halogen C.sub.1 -C.sub.4 alkyl C.sub.2 -C.sub.4 alkenyl, C.sub.2 -C.sub.4 alkynyl, benzyl or phenyl; and R.sup.2 is hydrogen, C.sub.1 -C.sub.4 alkyl phenyl or a 5- or 6- membered heterocyclic; or(ii) the endocyclic dotted line ( ) is a single bond; the exocyclic dotted line ( ) is a double bond;A is oxygen;B is ##STR3## m is 0; n is 1; R.sup.3, R.sup.4 and the nitrogen to which they are attached together represent an alicyclic amino group having 5 or 6 ring atoms, of which one ring atom is nitrogen and one ring atom is optionally an additional nitrogen, oxygen or sulfur heteroatom; and R.sup.1 and R.sup.2, together with the carbon to which they are attached, represent phenyl fused to the isoxazole ring.
    • 一种治疗抑郁症的方法,包括向患者施用有效的抗抑郁量的下式化合物,其中(i)内环虚线()是双键; 外消旋虚线()是单键; A是 m是1; n为0; R3和R4是氢,C1-C4烷基,苄基或苯基或R3,R4,它们所连接的氮代表具有5或6个环原子的脂环族氨基,其中一个环原子是氮,一个环原子是任选的 另外的氮,氧或硫杂原子; R1是氢,卤素C1-C4烷基C2-C4烯基,C2-C4炔基,苄基或苯基; 和R 2是氢,C 1 -C 4烷基苯基或5-或6-元杂环; 或(ii)内环虚线()是单键; 环外虚线()是双键; A是氧气; B是 m是0; n为1; R3,R4和它们所连接的氮一起表示具有5或6个环原子的脂环族氨基,其中一个环原子是氮,一个环原子任选地是另外的氮,氧或硫杂原子; 并且R 1和R 2与它们所连接的碳一起表示与异恶唑环稠合的苯基。
    • 8. 发明授权
    • Amino-acid derivatives, their preparation and their use as
pharmaceuticals
    • 氨基酸衍生物,其制备及其作为药物的用途
    • US4545942A
    • 1985-10-08
    • US597817
    • 1984-04-09
    • Mitsuo NaganoKoichi HiraiKouichi KitamuraKenkichi ShinkaiHiroshi Yasuda
    • Mitsuo NaganoKoichi HiraiKouichi KitamuraKenkichi ShinkaiHiroshi Yasuda
    • A61K31/275A61K20060101A61K31/165A61K31/19A61K31/195A61K31/215A61P35/00A61P37/04C07C20060101C07C67/00C07C253/00C07C255/24C07C255/26C07C255/29C07C255/32C07C255/44C07C255/56C07C255/66C07D317/68C07C121/78
    • C07C255/00
    • New compounds useful as immunoregulatory and antineoplastic agents are amino-acid derivatives of formula: ##STR1## wherein: n is an integer from 1 to 5;R.sup.1 is a hydrogen atom, an alkyl group, a haloalkyl group, a halogen atom, a mercapto group, an alkylmercapto group, a hydroxy group, an alkoxy group, an acyloxy group, a carboxyl group, an alkoxycarbonyl group, an amino group, an alkyl-substituted amino group, an aryl-substituted amino group, an acylamino group, a haloalkoxycarbonylamino group, an alkanesulphonyl group, a nitro group or a cyano group (and, when n is an integer from 2 to 5, the radicals R.sup.1 may be the same or different);R.sup.2 and R.sup.3 may be the same or different and each is a hydrogen atom or an alkyl group;R.sup.4 is a hydrogen atom, an alkyl group, a cyano group, a cyanoalkyl group, a hydroxyalkyl group, an alkoxycarbonyl group, a carboxyl group, an aryl group, an aralkyl group, a mercaptoalkyl group, an alkylthioalkyl group, or a thioalkyl group (the free bond of the sulphur in said thioalkyl group being joined to the sulphur of another moiety of the same formula); andA is a hydroxy group, an alkoxy group, an amino group, an alkyl-substituted amino group (optionally halogen- or carbamoyl- substituted in the alkyl moiety), a hydrazino group, an alkyl- or aryl- substituted hydrazino group, a hydroxylamino group, an alkoxyamino group or an aralkyloxyamino group;and the pharmaceutically acceptable salts thereof.
    • 可用作免疫调节和抗肿瘤剂的新化合物是下式的氨基酸衍生物:其中:n是1至5的整数; R1是氢原子,烷基,卤代烷基,卤素原子,巯基,烷基巯基,羟基,烷氧基,酰氧基,羧基,烷氧基羰基,氨基, 烷基取代的氨基,芳基取代的氨基,酰氨基,卤代烷氧基羰基氨基,链烷磺酰基,硝基或氰基(当n为2至5的整数时,基团R 1可以 相同或不同); R2和R3可以相同或不同,各自为氢原子或烷基; R4是氢原子,烷基,氰基,氰基烷基,羟基烷基,烷氧基羰基,羧基,芳基,芳烷基,巯基烷基,烷硫基烷基或硫代烷基 (所述硫代烷基中的硫的游离键与相同式的另一部分的硫连接); 并且A是羟基,烷氧基,氨基,烷基取代的氨基(在烷基部分中任选被卤素取代或氨基甲酰基取代),肼基,烷基或芳基取代的肼基, 羟基氨基,烷氧基氨基或芳烷氧基氨基; 及其药学上可接受的盐。