Abstract: A compound having the formula ##STR1## wherein Z is CH.sub.2 --N(CH.sub.3), N(CH.sub.3)--CH.sub.2, or ##STR2## R.sup.1 and R.sup.2 are selected from 1) one of R.sup.1 and R.sup.2 is OH and the other of R.sup.1 and R.sup.2 is (C.sub.1 -C.sub.6)alkyl, (C.sub.2 -C.sub.6)alkenyl, or phenyl, with the proviso that Z is not CO;2) one of R.sup.1 and R.sup.2 is H and the other of R.sup.1 and R.sup.2 is NR.sup.5 R.sup.6 wherein R.sup.5 and R.sup.6 are independently selected from H and (C.sub.1 -C.sub.6)alkyl, or is OR.sup.7 wherein R.sup.7 is H or (C.sub.1 -C.sub.6)alkyl; and3) R.sup.1 and R.sup.2 together form an oxo or oxime group;R.sup.3 and R.sup.4 are each hydroxyl or together form a carbonate or thiocarbonate group; and pharmaceutically acceptable salts thereof.
Abstract: Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein: Y is a direct link, --CH.sub.2 --, --(CH.sub.2).sub.2 --, --CH.sub.2 O-- or --CH.sub.2 S--; R is --CN or --CONH.sub.2 ; and R.sup.1 is ##STR2## where X and X.sup.1 are each independently O or CH.sub.2 ; and m is 1, 2 or 3, are muscarinic receptor antagonists useful in the treatment of diseases and conditions associated with the altered motility and/or tone of smooth muscle, such as irritable bowel syndrome.
Abstract: A solid phase coupling reagent for amide formation, comprising insoluble polymer bearing pendant side chains, said side chains each comprising a terminal portion having the formula ##STR1## wherein Y.sup.- is a counteranion and n is independently an integer from 2 to 6; and a method of making amides employing the coupling reagent.
Abstract: This invention relates to novel acidic polycyclic ether antibiotics CP-91,243 and CP-91,244 of the formula ##STR1## wherein R is H in CP-91,243 and R is CH.sub.3 in CP-91,244. The invention also relates to novel Actinomadura roseorufa microorganisms; processes for producing the novel antibiotics and the known antibiotic UK-58,852; methods for controlling coccidial infections in poultry, enteritis in livestock and swine dysentery; methods for promoting growth and/or improving efficiency of feed utilization in ruminant or monogastric animals; and nutrient feed compositions.This is a National filing under 35 U.S.C. 371 based on PCT/US89/02400 filed Jun. 1, 1989.
Abstract: A method of lowering blood lipid levels, comprising administering to a patient in need of such treatment an effective amount of a compound of formula I ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.1 is hydroxy or a group capable of being removed in vivo to produce a compound of formula I wherein R.sup.1 is OH; andX and Y are the same or different and are selected from hydrogen, trifluoromethyl, fluoro, and chloro.
Abstract: Compounds of general formula I, ##STR1## and pharmaceutically acceptable salts thereof, in which R.sup.1 has any of the meanings given in the specification, pharmaceutical compositions comprising them and their use in the treatment of urinary incontinence.
Type:
Grant
Filed:
October 20, 1992
Date of Patent:
August 23, 1994
Assignee:
Imperial Chemical Industries plc
Inventors:
Cyrus J. Ohnmacht, Robert J. Harris, Diane A. Trainor
Abstract: Process for the preparation of a dialkyl trans-piperidine-2,5-dicarboxylate from a corresponding dialkyl cis-piperidine-2,5-dicarboxylate via a transsubstituted pyridine derivative of the formula ##STR1## wherein R is a (C.sub.1 -C.sub.3)alkyl group.
Abstract: Amides having formula I: ##STR1## wherein E, X, R.sup.2 and R.sup.3 have the meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable in vivo hydrolysable esters thereof, which are useful in the treatment of urinary incontinence. Further provided are processes for preparing the amides and pharmaceutical compositions containing them.
Type:
Grant
Filed:
July 23, 1992
Date of Patent:
December 21, 1993
Assignees:
Imperial Chemical Industries PLC, Imperial Chemical House
Inventors:
Keith Russell, Cyrus J. Ohnmacht, Keith H. Gibson
Abstract: Compounds of formula I, Ia or Ib and pharmaceutically acceptable salts thereof, useful in the treatment of neuropsychiatric disorders such as psychoses; pharmaceutical compositions comprising a compound of formula I and a pharmaceutically acceptable diluent or carrier; and methods of treating neuropschiatric disorders comprising administering to a mammal (including man) in need of such treatment an effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof; ##STR1##
Type:
Grant
Filed:
August 6, 1992
Date of Patent:
November 30, 1993
Assignee:
Imperial Chemical Industries PLC
Inventors:
Ying K. Yee, Cyrus J. Ohnmacht, Diane A. Trainor, Joseph J. Lewis
Abstract: The invention provides the novel compound, 9-(3-cyanophenyl)-3,4,6,7,9,10-hexahydro-1,8-(2H,5H)-acridinedione and pharmaceutically acceptable acid addition salts thereof, pharmaceutical compositions containing the compound, and the use of the compound in the treatment of urinary incontinence.
Abstract: The present invention relates to spiroisoindolines that are antagonists at the phencyclidine receptor of the N-methyl-D-aspartate receptor complex and which are useful when such antagonism is desired such as in the treatment of neurological disorders. The invention further provides processes for preparing the spiroisoindolines, intermediates useful for their synthesis, pharmaceutical compositions containing them, and methods for their use.
Abstract: Certain gem-dimethyl substituted bicyclic phenolic pyrazines of formula III possess eukalemic diuretic properties. They are of value in treating those diseases and conditions in which a eukalemic diuretic effect is required, for example in treating edema, hypertension and/or related conditions.
Abstract: Certain amine containing phenolic pyrazines of formula III possess eukalemic diuretic properties and are of value in treating diseases and conditions in which a eukalemic diuretic effect is required, for example in treating edema, hypertension and/or related conditions.