Abstract: Methods of controlling fecal output and of appetite control, and compositions therefor, employing a fiber-containing mixture of cellulose with CMC, are described.
Abstract: A method for treating menopausal symptoms and a pharmaceutical package for effecting the method are disclosed. The method comprises a three phase sequence of estrogen and progestogen administration and an additional drug-free fourth phase during at least one menstrual cycle as follows:(a) as phase one, 0.2 mg to 1.5 mg of estrone, (or of other natural estrogen in an amount sufficient to result in an effect equivalent to the selected amount of estrone within the aforegiven range) for 4-9 days, followed by(b) as phase two, 0.2 mg to 1.5 mg of estrone, (or of other natural estrogen in an amount sufficient to result in an effect equivalent to the selected amount of estrone within the aforegiven range), plus 0.2 to 1.
Abstract: Compounds useful in treating cardiovascular disorders are the carboxylic acids depicted in formulas (1) and (2) ##STR1## as well as their pharmaceutically acceptable, non-toxic salts and esters, wherein:n is an integer from one to four;R.sub.1 is hydroxy;R.sub.2 is hydrogen; orR.sub.1 and R.sub.2 together are an oxo group;R.sub.3 is ##STR2## wherein A is --CH.sub.2 --CH.sub.2 --; trans-CH.dbd.CH--; --C.tbd.C--; andR.sub.4 is linear or branched alkyl of one to twelve carbons, cycloalkyl of three to eight carbons; phenyl optionally substituted with one or two identical substituents selected from the group consisting of lower alkyl, lower alkoxy, hydroxy, trifluoromethyl, and halo; or optionally substituted phenylalkyl.
Abstract: Compounds of the formula: ##STR1## and the pharmaceutically acceptable, non-toxic salts and esters (alkyl, 1-6C) thereof, wherein:X is O or S;R.sup.1 is selected from the group consisting of:(a) alkyl or cycloalkyl of 3-8 carbons, ##STR2## R.sup.2 is hydrogen or methyl; exhibit prostaglandin-like activity and are, thus, useful as platelet aggregation inhibitors.
Abstract: Novel 3-substituted-5,6,7,8-tetrahydropyrrolo[1,2-a]pyridine-8-carboxylic acid and 3-substituted-6,7,8,9-tetrahydro[1,2-a]azepine-9-carboxylic acid compounds represented by the formula ##STR1## and the pharmaceutically acceptable, non-toxic esters and salts thereof, wherein R is hydrogen or a lower alkyl group containing from 1 to 4 carbon atoms, n is the integer selected from the integers 1 or 2 and Ar is a 6- or 5-member ring. These compounds are useful as anti-inflammatory, analgesic and antipyretic agents, platelet aggregation inhibitors, and as smooth muscle relaxants.
Abstract: .alpha.-substituted derivatives of valproic acid are provided for conjugation to antigenic compositions, particularly poly(amino acids), and enzymes. The antigenic conjugates are employed for the production of antibodies, which find particular use in immunoassays for the determination of valproate, while the enzyme conjugate finds use in a homogeneous enzyme immunoassay for the determination of valproate. The compounds are synthesized by alkylating valproate at the tertiary carbon atom by an aliphatic chain with a terminal double bond which is cleaved to provide an acid or aldehyde group.
Abstract: Novel [1-(1,4-benzodioxan-2-yl)-4-(4-aminopyrimidin-2-yl]piperazines having the general formula ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen and lower alkyl;X and Y are independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy or halogen; and n is either 0, 1 or 2 and the pharmaceutically acceptable acid addition salts thereof are useful as anti-depressants.
Abstract: Methods of and compositions for lowering intraocular pressure using compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently selected from the group consisting of hydrogen, lower alkyl, optionally substituted phenyl, and optionally substituted phenyl lower alkyl; or wherein R.sup.1 and R.sup.2 taken together form an optionally substituted benzo;R.sup.3 is hydrogen, alkyl, or optionally substituted phenyl lower alkyl;n is an integer equal to 0, 1 or 2; and the pharmaceutically acceptable acid addition salts thereof, are disclosed.
Abstract: New compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein M is selected from the group consisting of hydrogen, morpholino, benzylamino, di-n-lower alkylamine, n-lower alkylamine, and aryl piperazino;Z.sub.1 and Z.sub.2 are each independently selected from the group consisting of CH.sub.2, CHOB and C.dbd.O, wherein B is selected from the group consisting of hydrogen and alkanoyl;Y is oxygen or sulfur;n is an integer from 0-4 but cannot be zero when Z.sub.1 is CHOB;m is an integer from 0-4 but cannot be zero when Z.sub.2 is CHOB, or when m is hydrogen;R.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy; andR.sub.4 and R.sub.5 are each independently lower alkyl, with the proviso that both R.sub.4 and R.sub.5 cannot be methyl when M is hydrogen;are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold.
Type:
Grant
Filed:
July 31, 1981
Date of Patent:
August 23, 1983
Assignee:
Laroche-Navarron, S.A.
Inventors:
Colette Favier, Henri Pinhas, Serge Beranger, Jean-Claude Pascal
Abstract: Compounds of the formula:R'--CH.sub.2 --S--Awherein:R' is hydrogen, alkyl, --COOH or its pharmaceutically acceptable salts, --alkylene--COOH or its pharmaceutically acceptable salts, --alkylene-SO.sub.2 H or its pharmaceutically acceptable salts, --alkylene-SO.sub.3 H or its pharmaceutically acceptable salts, or --alkylene CH.sub.2 OH; andA is the acyl moiety of a pharmaceutically acceptable carboxylic acid, said acid having antiinflammatory properties;are gastrointestinal tract sparing drugs for antiinflammatory pharmaceuticals.
Abstract: A method of contraception and a pharmaceutical package for effecting the method are disclosed. The method comprises a three phase sequence of estrogen/progestogen administration which is a daily sequence of unit dosages over a repeating cycle, which dosage sequence comprises, for one cycle:(a) administering, as phase one, about 20-40 .mu.g of ethinyl estradiol, (or of other estrogen in an amount sufficient to result in an equivalent effect) and about 0.3-0.8 mg of norethindrone (or of other progestogen in an amount sufficient to result in an equivalent effect) each day for 5-8 days, followed by;(b) administering, as phase two, the same dosage of estrogen and twice the dosage of progestogen each day as was administered each day in phase one, for 7-11 days, followed by;(c) administering, as phase three, the same dosage of estrogen and the same dosage of progestogen each day as was administered each day in phase one, for 3-7 days, followed by;(d) administering, as phase four, no therapeutically active dosage, i.
Type:
Grant
Filed:
August 10, 1981
Date of Patent:
June 28, 1983
Assignee:
Syntex Pharmaceuticals International Ltd.
Abstract: New compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Z.sub.1 and Z.sub.2 are each independently selected from the group consisting of CH.sub.2, CHOB and C.dbd.O, wherein B is selected from the group consisting of hydrogen and alkanoyl;Y is oxygen or sulfur;n is an integer from 0-4 but cannot be zero when Z.sub.1 is CHOB;m is an integer from 0-4 but cannot be zero when Z.sub.2 is CHOB; andR.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy;are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold.
Type:
Grant
Filed:
July 31, 1981
Date of Patent:
February 22, 1983
Assignee:
Laroche Navarron, S.A.
Inventors:
Colette Favier, Henri Pinhas, Serge Beranger, Jean-Claude Pascal
Abstract: New compounds of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein Z.sub.1 and Z.sub.2 are each independently selected from the group consisting of CH.sub.2, CHOB and C.dbd.O, wherein B is selected from the group consisting of hydrogen and alkanoyl;Y is oxygen or sulfur;n is an integer from 0-4 but cannot be zero when Z.sub.1 is CHOB;m is an integer from 0-4 but cannot be zero when Z.sub.2 is CHOB; andR.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, hydroxy, trifluoromethyl, alkyl or alkoxy;are antihistamines and are therefore useful in the treatment of respiratory diseases including asthma, hay fever, allergies and the common cold.
Type:
Grant
Filed:
January 12, 1981
Date of Patent:
February 22, 1983
Assignee:
Laroche-Navarron, S.A.
Inventors:
Colette Favier, Henri Pinhas, Serge Beranger, Jean-Claude Pascal
Abstract: A gel formulation, which is inherently spermicidal and which provides an efficient delivery system for spermicidal and other contraceptively effective compounds intravaginally is disclosed. Said formulation is useful in methods of intravaginal contraception.
Type:
Grant
Filed:
May 7, 1981
Date of Patent:
January 11, 1983
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Brian H. Vickery, Shabbir Anik, Richard E. Jones
Abstract: Degradation of prostaglandins in anhydrous or aqueous pharmaceutically acceptable, water-miscible alcohol solutions is prevented by adding a stabilizing amount of a pharmaceutically acceptable acetal.
Abstract: Inflammation is prevented, reduced or inhibited by administering muramyl and desmethylmuramyl dipeptides of the general formula: ##STR1## wherein each of R.sup.1 through R.sup.5 can independently be hydrogen or a variety of substituted or unsubstituted acyl, alkyl, aryl, or arylalkyl substituents. Pharmaceutical compositions containing such compounds useful for reducing inflammation are described.
Type:
Grant
Filed:
July 29, 1980
Date of Patent:
November 2, 1982
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Wendell H. Rooks, II, Neil R. Ackerman, Albert J. Tomolonis
Abstract: Compounds of the formula ##STR1## wherein the serrated lines denote both endo and exo forms; R.sub.1 and R.sub.2 are the same or different and are C.sub.1 to C.sub.6 alkyl, C.sub.5 or C.sub.6 cycloalkyl, C.sub.5 or C.sub.6 cycloalkenyl, phenyl optionally substituted with C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy or halo, or 5 or 6 membered heterocyclic aryl wherein the heteroatom is oxygen, nitrogen or sulfur; R.sub.3 is a C.sub.1 to C.sub.6 alkyl radical; R.sub.4 and X are optionally present, and when present R.sub.4 is a C.sub.1 to C.sub.6 alkyl radical or hydrogen and X is an inorganic or organic anion which forms a pharmaceutically acceptable salt. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.
Abstract: An improved process for 5-aroylation of 1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic esters and nitriles and for subsequent hydrolysis thereof is disclosed. In the improved process, an aroyl morpholide is reacted with the pyrrolo pyrrole system and the resultant decomposed with base.
Abstract: Contact lenses are fabricated from a copolymer of a polysiloxanylalkyl acrylic ester and an alkyl acrylic ester. The copolymer has increased oxygen permeability.