Abstract: This invention concerns the novel use of certain known thiazoles, particularly acylaminothiazoles and thiazolecarboxamides, as intraocular pressure lowering agents. When administered topically to the eye with increased intraocular pressure the compounds are effective in decreasing intraocular pressure, in preventing development of acute or chronic ocular hypertension including glaucoma, in inhibiting the further deterioration of the eye due to intraocular hypertension, or in relieving the symptoms of already existing ophthalmic disease.
Type:
Grant
Filed:
October 19, 1982
Date of Patent:
October 16, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
L. David Waterbury, A. Peter Roszkowski
Abstract: Disclosed herein are nasal spray compositions and methods for enhancing polypeptide absorption across nasal membranes comprising a chelating agent and a polypeptide in a pharmaceutically acceptable excipient.
Abstract: An implanting device for implanting pellets and like subcutaneously or intramuscularly in animals is described which utilizes means for indexing an implant magazine having a plurality of pellet-containing stations therein and means for automatically retracting a needle from about an implant charge to deposit the pellets in an animal. The implant magazine is indexed for sequential applications automatically as the retraction mechanism is cocked. Additionally, means for automatically ejecting a spent or empty implant cartridge are provided to prevent false deposition of implants. An implant cartridge having open channels containing implants can be utilized with the implanting device, the channels having means thereon for increasing the size of the channel during the implanting step to substantially eliminate the crushing or breaking of pellets as they are expelled from the cartridge. Alignment and stabilization means for the implant magazine and the implanting device also are provided.
Type:
Grant
Filed:
May 5, 1983
Date of Patent:
October 2, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Allen D. McNaughton, Stephen B. Albert, Gerard A. Furbershaw
Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy or lower alkylthio;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms.
Type:
Grant
Filed:
October 27, 1982
Date of Patent:
August 21, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
Gordon H. Jones, Michael C. Venuti, Young, John M.
Abstract: The present invention concerns a new use of certain pyrrolo-pyrrole compounds of chemical formulas (A), (B), (C), and (D): ##STR1## for the treatment of microvascular complications associated with diabetes such as, for example, diabetic retinopathy, diabetic nephropathy and diabetic neuropathy. Pyrrolo-pyrrole compounds prevent development, restrain further progress and relieve symptoms of already developed microvascular complications of diabetes.
Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen or lower alkyl; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.
Abstract: 5-benzoyl-7-halo-1,2-dihydro-3H-pyrrolo[1,2-a]-pyrrole-1-carboxylic acids, represented by the formula ##STR1## and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein:R is hydrogen or lower alkyl;X is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, carboxyl, lower alkylcarbonyl, sulfonic acid, sulfonic acid alkyl ester, fluoro, chloro, or bromo; and Y is chloro or bromo, which are novel, and 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids which are represented by the formula ##STR2## wherein X and R are as above defined except that X cannot be chloro or bromo, are prepared by decarboxylation of the corresponding 1,1 dicarboxylates. Intermediates in said preparation are also disclosed.
Abstract: Certain known pyrroles have been found to be useful in the topical treatment of various ophthalmic diseases in mammals; especially those originating from or associated with inflammation such as, for example, cystoid macular edema, glaucoma, conjunctivitis, uveitis, diabetic retinopathy and eye surgery or trauma.
Abstract: 5-Substituted-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acids of the formula ##STR1## wherein: X is hydrogen, lower alkyl, chloro or bromo; Ar is a moiety selected from the group consisting of ##STR2## in which: Y is oxygen or sulfur;R is hydrogen, methyl, chloro, or bromo, the R substitution being at the 3, 4 or 5 position of the ring;R.sup.1 is hydrogen, lower alkyl, lower alkoxyl, lower alkoxycarbonyl, lower alkylcarbonyl, fluoro, chloro or bromo, the R.sup.1 substitution being at any available position in the ring;R.sup.2 is hydrogen or lower alkyl;are prepared by .beta.-decarboxylation of the corresponding dialkyl-1,1-dicarboxylates. Certain substituted pyrroles are useful as intermediates for preparing the compounds of formula I.
Abstract: Delivery systems for releasing macromolecular active agents to a body site at a controlled rate for a prolonged period of time, comprising a cholesteric matrix permeable to passage of the macromolecular active agent by diffusion, are disclosed. The cholesteric matrix comprises cholesterol powder and cholesterol prills optionally in combination with a binding agent and a lubricating agent. The macromolecular active agent is dispersed throughout the matrix; macromolecules suitable for release from this delivery system have molecular weights of about 1300 to about 75,000 and are at least very slightly soluble in water.
Abstract: A pinch valve assembly is described for location between the manifold assembly and the flow adjustment valves of a dental handpiece system. The pinch valve assembly of the present invention comprises a housing having a plurality of passageways extending therethrough for receiving a plurality of resilient tubes therein. A plurality of transverse slots extending from each of the passageways to the bottom of the housing are provided and are adapted to receive a plurality of slide elements in each of the slots such that the slide elements can move reciprocally within the slots. The housing is supported on a base and a flexible diaphragm is located between the housing and the base. A rigid disc rests on the diaphragm and supports the slide elements in the slots. A chamber is provided in the base beneath the diaphragm and connected to a source of pressurized fluid.
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: Psoriasis in mammals is relieved by topically administering naphthoquinones of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy; andR.sup.3 is halo or cyano.
Abstract: 1-Substituted imidazole derivatives exhibit spermatostatic and spermatocidal activity and are useful for contraceptive purposes both in male and female mammals.
Type:
Grant
Filed:
July 19, 1982
Date of Patent:
March 27, 1984
Assignee:
SYNTEX (U.S.A.) Inc.
Inventors:
Duane W. Hallesy, Richard E. Jones, Brian H. Vickery, Keith A. M. Walker
Abstract: Compounds represented by the formula ##STR1## wherein R.sup.1 is an aliphatic or alicyclic hydrocarbon acyl group of two to eighteen carbon atoms and R.sup.2 is an alkali metal cation or hydrogen are useful for increasing the feed efficiency of ruminants and for treating coccidiosis in domestic animals, especially chickens.
Abstract: An operatory stool having an arcuate, body support arm positioned above the level of the stool seat is described. The body support arm is reversible for right- or left-handed use of the stool. The stool structure permits rapid interchange between the right- and the left-handed configurations by means of a rotatable mechanism between the body support arm and a connecting member between the body support arm and the seat, which permits rotation of the body support arm through a 180.degree. upwardly extending arc from one side of the connecting member to the other. Means are provided for locking the body support arm at dependent positions on either side of the connecting member. Additionally, a reversible locking mechanism for resisting rotation of the body support arm about the connecting member in a predetermined direction in a horizontal plane is provided.
Type:
Grant
Filed:
November 12, 1982
Date of Patent:
February 7, 1984
Assignee:
Syntex (U.S.A.) Inc.
Inventors:
James D. Alsup, Jr., Kenneth L. Barrett, Arden F. Jenkins
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 of the formula ##STR1## wherein m is the integer 1, 2 or 3; R is independently selected from the group C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, halo, trifluoromethyl and hydroxy when m is the integer 1, 2 or 3 and methylenedioxy when m is the integer 2; Z is hydroxymethylene, esterified hydroxymethylene, alkoxymethylene, alkylthiomethylene, carbonyl, or ketal-, thioketal- or hemithioketal-protected carbonyl, and the pharmaceutically acceptable acid addition salts thereof, are useful as anticonvulsants, anti-secretory agents and spermatocides.