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    • 2. 发明申请
    • TRITERPENE DERIVATIVES AND REMEDY FOR LIVER DISEASES
    • TRAILRPENE DIVIVATIVES AND REMEDY FOR LIVER DISEASES
    • WO1997003088A1
    • 1997-01-30
    • PCT/JP1996001891
    • 1996-07-08
    • MEIJI SEIKA KABUSHIKI KAISHASASAKI, KazueMINOWA, NobutoNISHIYAMA, ShojiKUZUHARA, Hiroyuki
    • MEIJI SEIKA KABUSHIKI KAISHA
    • C07J63/00
    • C07J63/008C07J71/0005
    • A remedy for liver diseases which comprises a triterpene derivative represented by following general formula (I) or a pharmaceutically acceptable salt thereof wherein R represents hydroxy, alkoxy, alkylcarbonyloxy or aralkyloxy; R represents alkyl, -CH2O (wherein R represents hydrogen, alkyl, aralkyl or akylcarbonyl), formyl, -COOR (wherein R represents hydrogen or alkyl) or -CH2N(R )R , or R and R are bonded to each other to form -O-CR (R )-OCH2- (wherein R and R are the same or different and each represents hydrogen, alkyl or aryl); R and R are the same or different and each represents hydrogen, hydroxy, alkyl, hydroxyalkyl, formyl, -COOR (wherein R represents hydrogen or alkyl) or -OR (wherein R represents alkyl, aralkyl, C1-6 alkylcarbonyl, arylcarbonyl, alkenyl, alkenylcarbonyl or optionally substituted arylalkenylcarbonyl, or R and R together form methylene; and - - - represents a single or double bond, provided that when - - - is a double bond, then R is not present.
    • 一种肝病的治疗方法,其包含由以下通式(I)表示的三萜衍生物或其药学上可接受的盐,其中R 1表示羟基,烷氧基,烷基羰氧基或芳烷氧基; R 2表示烷基,-CH 2 O(其中R 5表示氢,烷基,芳烷基或烷基羰基),甲酰基,-COOR 6(其中R 6表示氢或烷基)或-CH 2 N(R 7 )R 8或R 1和R 2彼此键合以形成-O-CR 9(R 10)-O 2 2-(其中R 9和R 10 >相同或不同,各自表示氢,烷基或芳基); R 3和R 4相同或不同,各自表示氢,羟基,烷基,羟烷基,甲酰基,-COOR 11(其中R 11表示氢或烷基)或-OR 12( 其中R 12表示烷基,芳烷基,C 1-6烷基羰基,芳基羰基,烯基,烯基羰基或任选取代的芳基烯基羰基,或R 3和R 4一起形成亚甲基;和 - 表示单键或双键,条件是当< - - - - 双键时,则不存在R 4。
    • 3. 发明申请
    • NOVEL CEPHEM DERIVATIVES
    • 新的CEPHEM衍生物
    • WO1996037499A1
    • 1996-11-28
    • PCT/JP1996001406
    • 1996-05-24
    • MEIJI SEIKA KABUSHIKI KAISHAUMEMURA, EijiroATSUMI, KunioIWAMATSU, KatsuyoshiTAMURA, Atsushi
    • MEIJI SEIKA KABUSHIKI KAISHA
    • C07D519/00
    • C07D501/00Y02P20/55
    • Compounds represented by general formula (I) and having a beta -(optionally substituted imidazo[5,1-b]thiazolyl)vinyl group at the 3-position of the cephem ring, and salts and esters thereof. These compounds have an extremely broad antimicrobial spectrum and exerts potent antimicrobial effects on Gram-positive bacteria, Gram-negative bacteria and even resistant bacteria. In formula (I) X represents CH or N; R represents hydrogen or an amino protecting group; R represents hydrogen, C1-6 alkyl, C3-7 cycloalkyl or a hydroxy protecting group; R is not present or represents hydrogen, a cation forming a salt or a carboxy protecting group; R , R and R may be the same or different and each represents hydrogen or C1-6 alkyl; R is not present or represents a cation of C1-6 alkyl; and n is an integer of 0 or 1.
    • 由通式(I)表示并在头孢烯环的3位具有β-(任选取代的咪唑并[5,1-b]噻唑基)乙烯基的化合物及其盐和酯。 这些化合物具有非常宽的抗菌谱,对革兰氏阳性菌,革兰氏阴性细菌甚至抗性细菌都发挥有力的抗菌作用。 在式(I)中,X表示CH或N; R 1表示氢或氨基保护基; R 2表示氢,C 1-6烷基,C 3-7环烷基或羟基保护基; R 3不存在或表示氢,形成盐或羧基保护基的阳离子; R 4,R 5和R 6可以相同或不同,各自表示氢或C 1-6烷基; R 7+不存在或表示C 1-6烷基的阳离子; n为0或1的整数。
    • 4. 发明申请
    • BICYCLIC THIAZOLE COMPOUND
    • 双环噻唑化合物
    • WO1996016968A1
    • 1996-06-06
    • PCT/JP1995002412
    • 1995-11-27
    • MEIJI SEIKA KABUSHIKI KAISHAFUKUDA, YoshimasaHASEGAWA, ToshifumiNAKATANI, YuukoMURASE, KenshiFUJI, Kazuyuki
    • MEIJI SEIKA KABUSHIKI KAISHA
    • C07D519/00
    • C07D513/04
    • A compound having a psychotropic effect and represented by general formula (I) and a pharmaceutically acceptable salt thereof, wherein one of R and R represents W-(CH2)m-, wherein m is an integer of from 1 to 4, and another represents hydrogen or optionally substituted lower alkyl; W represents a group represented by formula (i) (wherein R represents hydrogen or halogeno; A represents oxygen or sulfur; B represents nitrogen or CH and Y represents CH or nitrogen); and the cyclic structure -D- represents one member selected from among those represented by formulae (a) to (d), wherein n represents an integer of 0 to 2; R independently represent hydrogen, lower alkyl, hydroxy, alkoxy, alkoxycarbonyl or aminocarbonyl; and the solid line accompanied by the dotted line represents either a single bond or a double bond.
    • 具有精神作用并由通式(I)表示的化合物及其药学上可接受的盐,其中R 1和R 2之一表示W-(CH 2)m - ,其中m为1的整数 至4,另一个表示氢或任选取代的低级烷基; W表示由式(i)表示的基团(其中R 3表示氢或卤素; A表示氧或硫; B表示氮或CH,Y表示CH或氮); 环状结构-D-表示选自由式(a)〜(d)表示的那些,其中,n表示0〜2的整数。 [R <4? 和R 5>独立地表示氢,低级烷基,羟基,烷氧基,烷氧基羰基或氨基羰基; 伴随虚线的实线表示单键或双键。
    • 10. 发明申请
    • NOVEL TETRAHYDRONAPHTHOFURANONE DERIVATIVES AND PROCESS FOR PRODUCING THE SAME
    • 新的四氢呋喃酮衍生物及其制备方法
    • WO1997030040A1
    • 1997-08-21
    • PCT/JP1997000451
    • 1997-02-19
    • MEIJI SEIKA KABUSHIKI KAISHAKURIHARA, KenichiSHINEI, RieTANABE, KiyoshiYAMAMOTO, YasuoAJITO, KeiichiMIYAJIMA, KaoriTABATA, YujiYASUDA, ShoheiTATSUTA, KuniakiOKONOGI, Tsuneo
    • MEIJI SEIKA KABUSHIKI KAISHA
    • C07D307/92
    • C07D307/92C07D407/12C07D407/14C07D409/12C07D417/12
    • Compounds represented by general formula (I) and pharmaceutically acceptable salts thereof, which have progesterone receptor binding inhibitory activities and so are used as remedies and preventives for diseases in which progesterone participates, more particularly, as anticancer agents against mammary and ovarian cancers, remedies for uterine myoma, endometriosis, meningioma and myeloma, abortifacient, peroral contraceptive, and remedies and preventives for osteoporosis and climacteric disturbance, wherein R and R represent each hydroxy, alkyloxy, alkenyloxy, alkynyloxy, cycloalkyloxy, alkoxyalkyloxy, oxygenous cycloalkyloxy, aralkyloxy, alkylcarbonyloxy, alkenylcarbonyloxy, alkynylcarbonyloxy, cycloalkylcarbonyloxy, alkoxycarbonyloxy, aryloxycarbonyloxy, aralkylcarbonyloxy, aromatic acyloxy, heteroaromatic acyloxy, saturated heterocyclic carbonyloxy, alkylsulfonyloxy, aromatic sulfonyloxy, alkylcarbamoyloxy, or aromatic carbamoyloxy, the R optionally representing hydrogen alkyl, alkenyl, or alkynyl; and R , R , and R represent each independently hydrogen, alkyl, or alkenyl.
    • 具有孕酮受体结合抑制活性的由通式(I)表示的化合物及其药学上可接受的盐等用作对孕激素参与的疾病的补救措施和预防药物,更特别地,作为抗乳腺癌和卵巢癌的抗癌剂, 子宫肌瘤,子宫内膜异位症,脑膜瘤和骨髓瘤,流产,口服避孕药,以及骨质疏松症和更年期障碍的治疗和预防药物,其中R 1和R 2代表各羟基,烷氧基,烯氧基,炔氧基,环烷氧基,烷氧基烷氧基, 芳烷氧基,烷基羰基氧基,链烯基羰基氧基,炔基羰基氧基,环烷基羰基氧基,烷氧基羰基氧基,芳氧基羰基氧基,芳烷基羰基氧基,芳香族酰氧基,杂芳基酰氧基,饱和杂环羰基氧基,烷基磺酰氧基,芳香族磺酰氧基,烷基氨基甲酰氧基或芳族氨基甲酰氧基,R 1任选代表氢 烷基,烯基或炔基; R 3,R 4和R 5各自独立地表示氢,烷基或链烯基。