首页 / 专利分类库 / 有机化学 / 杂环化合物 / 杂环化合物,含小于五元的环,有1个硫原子作为仅有的杂环原子
序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
101 Tetrazole-containing rapamycin analogs with shortened half-lives HK01100137 2001-01-05 HK1030771A1 2001-05-18 MOLLISON KARL W
102 PYRIDINE AND PYRIMIDINE DERIVATIVES AND THEIR USE AS INHIBITORS OF CYTOKINE MEDIATED DISEASE CA2367866 2000-03-17 CA2367866A1 2000-09-28 CUMMING JOHN GRAHAM
This invention concerns a bicyclic compound of Formula (I), wherein: G is N, CH or C(CN); ring X is a 5- or 6-membered fused heteroaryl ring which contai ns 1, 2, or 3 heteroatoms selected from oxygen, sulphur and nitrogen; m is 0 - 2; R1 is a group such as hydroxy, halo, trifluoromethyl, cyano, mercapto, nitro , amino, carboxy and carbamoyl; each of R2 and R3 is hydrogen, halo, C1-6alkyl , C2-6alkenyl or C2-6alkynyl; R4 is a group such as hydrogen, hydroxy, C1- 6alkyl, C1-6alkoxy, amino and N-C1-6alkylamino; R5 is a group such as hydrogen, halo, trifluoromethyl, cyano, nitro, amino and hydroxy, and q is 0 - 4; or a pharmaceutically acceptable salt or an in vivo cleavable ester thereof; processes for its preparation, a pharmaceutical composition containing it and its use in the treatment of diseases or medical conditions mediated by cytokines.
103 BR9812305 1998-09-24 BR9812305A 2000-09-05 MOLLISON KARL W
104 NO20001438 2000-03-20 NO20001438D0 2000-03-20 MOLLISON KARL W
105 NAALADASE INHIBITORS USEFUL AS PHARMACEUTICAL COMPOUNDS AND COMPOSITIONS CA2658200 1999-07-02 CA2658200A1 2000-01-13 MACLIN KEITH M; WANG ERIC; SLUSHER BARBARA S; MAJER PAVEL; JACKSON PAUL F; LAPIDUS RENA S
The present invention relates to N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) inhibitors enzyme activity, pharmaceutical compositions comprising such inhibitors, and methods of their use to inhibit NAALADase enzyme activity, thereby effecting neuronal activities, inhibiting angiogenesis, and treating glutamate abnormalities, compulsive disorders, prostate diseases, pain and diabetic neuropathy.
106 Tetrazole-containing rapamycin analogs with shortened half-lives AU9581998 1998-09-24 AU9581998A 1999-04-12 MOLLISON KARL W
107 TETRAZOLE-CONTAINING RAPAMYCIN ANALOGS WITH SHORTENED HALF-LIVES CA2303934 1998-09-24 CA2303934A1 1999-04-01 MOLLISON KARL W
A compound having formula (I) or a pharmaceutically acceptable salt or prodrug thereof, is an immunomodulatory agent and is useful in the treatment of restenosis and immune and autoimmune diseases. Also disclosed are cancer-, fungal growth-, restenosis-, post- transplant tissue rejection- and immuneand autoimmune disease-inhibiting compositions and a method of inhibiting cancer, fungal growth, restenosis, post- transplant tissue rejection, and immune and autoimmune disease in a mammal, with minimized side-effects due to shortened half-lives.
108 NUEVOS TAXOIDES, SU PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LES CONTIENEN ECSP961990 1996-12-20 ECSP961990A 1997-12-23
La presente invención se refiere a nuevos taxoides de fórmula general (gráfico), a su preparación y las composiciones farmacéuticas que los contienen en la fórmula general (I) Z represente un átomo de hidrógeno o un radical de fórmula general (gráfico), en la que R1 representa un radical bencilo eventualmente substituido, furilo o tenilo o un radical R2 -O-CO- en la que R2 representa un radical alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, bicicloalquilo, fenilo eventualmente substituido o heterociclilo. R3 representa un radical alquilo, alquenilo, alquenilo, alquinilo, cicloalquilo, cicloalquenilo, fenilo naftilo o heterociclico aromático o bien R4 representa un átomo de hidrógeno, R6 y R7 forman un conjunto un enlace, o bien R4 representa un átomo de hidrógheno o un radical hidroxi, o un radical alcoxi, alqueniloxi, alquiniloxi eventualmente substituido alcanoiloxi, ariloxi, alqueniloxi, alquiniloxi, cicloalcanoiloxi, alcoxiacetilo, alquiltioacetilo, alquiloxicarboniloxi, cicloalquiiloxi, cicloalqueniloxi, carbamoiloxi, alcoilcarbamoiloxi, dialcoicarbamoiloxi. R5 representa un átomo de hidrógeno, o R4 y R5 forman en conjunto una función cetona, R6 representa un átomo de hidrógeno y R y R7 forman en conjunto un enlace. Los nuevos productos de fórmula general (1) en la cual Z representa un radical de fórmula general (II), presentan propiedades antitumorales y antileucémicas notables.
109 Thioether compounds for use in preparing bifunctional chelating agents for therapeutic radiopharmaceuticals ZA953448 1995-04-28 ZA953448B 1996-01-12 VENKATESH MEERA; JURISSON SILVIA; SCHLEMPER ELMER; KETRING ALAN R; VOLKERT WYNN A
110 SUBSTITUTED THAICYCLOALKENO(3,2-B)PYRIDINES,METHODS OF PREPARATION,COMPOSITIONS AND METHOD OF USE ZA872535 1987-04-08 ZA872535B 1988-11-30 SCHWENDER CHARLES F; CHARLES F SCHWENDER; DODD JOHN H; JOHN H DODD
111 BICYCLIC SULFONAMIDE DERIVATIVES IE300286 1986-11-13 IE863002L 1987-05-18
112 Oxetane and thietanderivater with pesticidal properties DK430386 1986-09-09 DK430386A 1987-03-10 FRANKE HEINRICH; JOPPIEN HARTMUT; FRANKE HELGA
113 DIHYDROPYRIDINES,PROCESSES AND INTERMEDIATES FOR THEIR PRODUCTION AND PHARMACEUTICAL FORMULATIONS CONTAINING THEM ZA856626 1985-08-29 ZA856626B 1986-05-28 BAXTER ANDREW JOHN GILBY; GOULD KENNETH JOHN; DIXON JOHN; TINKER ALAN CHARLES
114 1,3-DITHIOLAN-2-YL(1,3-DITHIAN-2-YL)DERIVATIVES PH20012 1974-07-19 PH19393A 1986-04-07 RAMUZ HENRI DR
115 NITROGEN HETEROCYCLIC COMPOUNDS GB8529301 1985-11-28 GB8529301D0 1986-01-02
116 SULPHIDE COMPOUNDS,PHARMACEUTICAL COMPOSITION AND METHOD OF USE PH18702 1976-07-19 PH15375A 1982-12-10 MEHTA NARIMAN BOMANSHAW; BRIEADDY LAWRENCE EDWARD
117 HYPOLIPIDEMIC AGENTS AND METHOD OF USING THEM PH18526 1976-06-04 PH14090A 1981-02-10 PARKER R
118 SUBSTITUTED ALKYL,PHENONE COMPOUND DERIVATIVE AND PROCESS OF PREPARATION THEREOF PH20013 1977-07-19 PH13396A 1980-03-28 RAMUZ H
119 Preparation of cyclic sulphides GB1543062 1962-04-24 GB998606A 1965-07-14
The compound is prepared by pyrolysing a compound of for mula RCOACH2CH(R1)BH in which R1 in which R1 is H, -CH2OH or a C1-C8 alkyl, A and B respec tively are -O- and -S- or -S- and -O-, and R is a C1-C8 alkoxy group, an aryloxy group or an arylamino group; and the com pound is prepared by pyrolysing HOCH2CH2CH2S-CO-OR or HS-CH2-CH2-CH2-O-CO-OR1 in which R1 is an alkyl or an aryl group. For example ethylene sulphide may be prepared by pyrolysing n-hexyl, ethyl or phenyl 2-hydroxy ethylthiol carbonate or 2-mercaptoethylcarbonate; or by pyrolysing 2-mercaptoethyl phenyl carbamate or 2-hydroxyethyl phenyl thiol carbamate; methylethylene sulphide may be prepared by pyrolysing ethyl-2 mercapto-3-carbonate or 2-hydroxypropyl thiol carbonate; and hydroxymethylethylene sulphide by pyrolysing ethyl-2-mercapto-3-hydroxypropyl carbonate or 2,3-dihydroxy propyl thiolcarbonate. Trimethylene sulphide may be prepared, for example, by heating ethyl-3-hydroxypropyl thiol carbonate. The pyroly sis is preferably carried out in the presence of basic catalyst, for example, an alkali metal hydroxide, sodium methoxide, sodium ethoxide or a tertiary amine. The starting materials are prepared as follows:-(a) compounds of formula RCOSCH2CH(R1)OH in which R is C1-C8 alkoxy or aryloxy and R1 is H, hydroxymethyl or C1-C8 alkyl are prepared by reacting an alkyl or aryl chloroformate with 2-mercapto ethanols, such as 2-mercaptoethanol, 3-mercap to 1,2 - propanediol, 1 - mercapto - 2 - propanol, 1 - mercapto - 2 - butanol, 1 - mercapto - 2 1 - mercapto - 2 - heptanol or 1 - mercapto - 2 - decanol in the presence of a base, e.g. sodium hydroxide, potassium hy droxide or lithium hydroxide; (b) compounds of the formula RCOSCH2CH(R1)OH, in which R is acylamino and R1 is hydrogen, hydroxy methyl or C1-C8 alkyl are prepared by the base catalysed reaction of an aryl isocyanate, e.g. phenyl or tolyl isocyanate, with a 2-mercapto ethanol as exemplified above; (c) compounds of formula RCOOCH2CH(R1)SH, in which R is C1-C8 alkoxy or aryloxy and R1 is hydrogen, hydroxymethyl or C1-C8 alkyl are prepared by isomerization of the corresponding 2-hydroxy ethyl thiocarbonates prepared as in (a) above, by distilling under vacuum in the presence of uranyl acetate; and (d) the compounds of formula RCOOCH2CH(R1)SH, in which R is arylamino and R1 is hydrogen, hydroxymethyl or C1-C8 alkyl, are prepared by the non catalysed reaction of an arylisocyanate with 2-mercaptoethanols as specified above.
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