摘要:
A chiral resolution process is described for the purification of a substituted chiral quinazoline, by salt formation with a resolving agent, followed by crystallization.
摘要:
A compound of the formula: ##STR1## wherein R.sup.1 is lower alkyl, lower alkanoyl, aryl, ar(lower)alkyl or a heterocyclic group, each of which may have suitable substituent(s),R.sup.2 is carboxy or protected carboxy,R.sup.3 is hydrogen, halogen, hydroxy, lower alkoxy, acyloxy, lower alkylthio, lower alkenyl, lower alkenylthio, lower alkynyl, heterocyclicthio or a heterocyclic group, in which lower alkylthio, lower alkenyl, lower alkenylthio, heterocyclicthio and a heterocyclic group may have suitable substituent(s),R.sup.4 and R.sup.5 are each hydrogen, halogen or arylthio,A is lower alkylene, andn is an integer of 0 or 1,and a pharmaceutically acceptable salt thereof, processes for preparation thereof and pharmaceutical composition comprising the same.
摘要:
This invention relates to novel cephem compounds of high antimicrobial activity of the formula ##STR1## wherein R.sup.1 is amino;R.sup.2 is carboxy or a protected carboxy group;A is hydroxy (lower) alkylene, amino (lower) alkylene, protected amino (lower) alkylene, lower alkenylene, hydroxyimino (lower) alkylene, lower alkoxyimino (lower) alkylene, or lower alkenyloxyimino (lower) alkylene; andR.sup.3 is carboxy or a protected carboxy group,and pharmaceutically acceptable salts thereof.
摘要:
This invention relates to novel cephem compounds of high antimicrobial activity, said compounds being of the formula: ##STR1## wherein R.sup.1 is a group of the formula: ##STR2## in which R.sup.5 is amino or a protected amino group; and R.sup.6 is lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cyclo(lower)alkenyl, aryl, ar(lower)alkyl, or halogen-substituted ar(lower)alkyl;R.sup.2 is carboxy or a protected carboxy group;A is hydroxy(lower)alkylene, amino(lower)alkylene, protected amino(lower)alkylene, lower alkenylene, hydroxyimino(lower)alkylene, lower alkoxyimino(lower)alkylene, or lower alkenyloxyimino(lower)alkylene; andR.sup.3 is carboxy or a protected carboxy group, and pharmaceutically acceptable salts thereof.
摘要:
This invention is related to a method for producing 3-{4-[3-(1-pyrrolidinyl)propoxy]phenyl}-5-trifluoromethyl-4(3H)-quinazolinone comprising a step for reacting 2-methyl-5-trifluoromethyl-4H-3,1-benzoxazin-4-one with 4-[3-(1-pyrrolidinyl)propoxy]aniline or an acid-addition salt thereof, or 4-(1-cyclobutyl-4-piperidinoy9oxyaniline or acid addition salt thereof in the presence of an acid catalyst.
摘要:
The present invention relates to synthetic processes useful in the preparation of fluorinated 4-azasteroid derivatives that modulate androgen receptors and have application in the treatment of conditions caused by androgen deficiency or androgen receptor hyperactivity, such as osteoporosis, periodontal disease, bone fracture, frailty, erectile dysfunction, loss of libido, androgen-dependent cancers and sarcopenia. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation.
摘要:
Amine salts of 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3-(6-methoxy-pyridin-3-yl)propionic acid are potent antagonists of the integrin αvβ3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts.
摘要:
A process for preparation of a compound of formula I: wherein: R1 represents CH3 or H; and P represents a protecting group; comprising reacting a compound of formula IV: wherein R1 and P and are defined above and R4 represents triflate or SO2F; in the presence of a catalyst and (R3)3SnCH2OP″, wherein each R3 represents C1-4 lower alkyl, and P″ represents H or a protecting group, to yield the compound of formula I.
摘要:
A process of synthesizing a carbapenem compound of formula 6: is disclosed using a compound of formula 4′: The intermediate compounds that are described herein are also included in the present invention.
摘要:
A process of synthesizing a carbapenem compound of formula 6: ##STR1## is disclosed using a compound of formula 4': ##STR2## The intermediate compounds that are described herein are also included in the present invention.