Abstract:
PROBLEM TO BE SOLVED: To provide a method for preparing quinoline-substituted carbonate and carbamate compounds which are important intermediates in the synthesis of a 6-O-substituted macrolide antibiotic material. SOLUTION: The carbonate or carbamate derivative expressed by the formula: R 1 -CH=CHCH 2 OC(O)-X-R 2 (I) is obtained by coupling a haloquinoline with propargyl alcohol in the presence of a base and a palladium-based catalyst to form an alkynol, reducing it to make an alkenol and then reacting it with an acylation reagent. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
PROBLEM TO BE SOLVED: To provide pharmaceutical compositions useful in treating conditions or disorders which are prevented or ameliorated by histamine-3 receptor ligands, a method of using such compounds and compositions, and a preparation process therefor. SOLUTION: There are provided a compound of formula (I), pharmaceutically acceptable salts, esters, amides or prodrugs thereof. Pharmaceutical compositions, usage and preparation process therefor are also provided. In the formula, each symbol is defined specifically. COPYRIGHT: (C)2011,JPO&INPIT
Abstract:
Disclosed herein is a process for the preparation of erythromycin derivatives, or pharmaceutically acceptable salts thereof, which contain an optionally substituted propargyl group at the 6-O-position.
Abstract:
Octahydro-pyrrolo[3,4-b]pyrrole derivatives are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Octahydro-pyrrolo[3,4-b]pyrrole compounds, methods for using such compounds, compositions for making them, and processes for preparing such compounds are disclosed herein.
Abstract:
Methods and novel intermediates for the preparation of acyclic nucleoside derivatives of formula (I) where one of R1 and R2 is an amino acid acyl group and the other of R1 and R2 is a -C(O)C3-C21 saturated or monounsaturated, optionally substituted alkyl and R3 is OH or H; or a pharmaceutically acceptable salt thereof.
Abstract:
The invention relates to a process for preparing carbonate and carbamate compounds, which are important intermediates in the synthesis of 6-O-substituted macrolide antibiotics. The process employs metal-catalyzed coupling reactions to provide a carbonate or carbamate of formula (I) or a substrate that can be reduced to obtain the same. €ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒ€ƒR 1 -CH=CHCH 2 OC(O)-X-R 2 €ƒ€ƒ€ƒ€ƒ€ƒ(I)
Abstract:
Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions comprising the histamine-3 receptor ligands, methods for using such compounds and compositions, and a process for preparing compounds within the scope of formula (I).
Abstract:
Un compuesto de formula: o una de sus sales, esteres, amidas, farmaceuticamente aceptables, donde: X es O, S, NH, o N(alquilo); Y, e Y' se seleccionan cada uno independientemente del grupo que consiste en CH, CF, y N; Z es N, uno de R1 y R2 se selecciona del grupo que consiste en arilo, heteroarilo, y heterociclo; el otro de R1 y R2 se selecciona del grupo que consiste en hidrogeno, alquilo, alcoxi, arilo, cicloalquilo, halo, ciano, y tioalcoxi; R3 esta ausente; R4 y R5 se seleccionan cada uno independientemente del grupo que consiste en alquilo, haloalquilo, hidroxialquilo, alcoxialquilo, cicloalquilo, y cicloalquilalquilo, o R4 y R5 tomados junto con el atomo de nitrogeno al que estan unidos cada uno forman un anillo no aromatico de estructura (a): R7, R8, R9, y R10 se seleccionan cada uno independientemente del grupo que consiste en hidrogeno, hidroxialquilo, fluoroalquilo, y alquilo; o uno del par R7 y R6 o el par R9 y R10 se toman juntos para formar un anillo C3-C6, donde 0, 1, o 2 heteroatomos seleccionados entre O, N, o S remplazan a un atomo de carbono en el anillo; R11 y R12 se seleccionan cada uno independientemente del grupo que consiste en hidrogeno, hidroxi, hidroxialquilo, alquilo, y fluor; R13 y R14 en cada aparicion se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo, y fluor; L es -[C(R15)(R16)]n-; R15 y R16 en cada aparicion se seleccionan independientemente del grupo que consiste en hidrogeno, alquilo, alcoxi, y fluor; m es un numero entero de 0-3; y n es un numero entero de 2-3.