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. |