Abstract: Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.
Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## where Y is H or OH;j is an integer from 0 to 4;k is an integer from 0 to 4, and whereinm is an integer from 1 to 4;n is an integer from 1 to 4;p is an integer from 1 to 4; andX may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof, but when X is nonexistent the terminal group in which both the n-chain and the p-chain is a methyl group. ##STR2## The reaction was performed under reflux condensation. Following the reaction, which was usually complete within a few hours, the acid chlorides were vacuum distilled and reacted with a thiol compound as described above.The compounds of this invention are anti-muscarinic agents (cholinergic-muscarinic receptor antagonists) which inhibit the actions of acetylcholine on autonomic effectors innervated by postganglionic cholinergic nerves as well as on smooth muscle that lacks cholinergic innervation.
Abstract: Ammonia and/or an alkyleneamine is reacted with an alkanolamine by using a miobium-containing substance as a catalyst to obtain an alkyleneamine having an increased number of alkylene units. The niobium-containing substance has a high activity and a high heat resistance, and is not or only slightly soluble in the water-containing reaction liquid.
Abstract: The invention relates primarily to quaternized polycyclic compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.2 together with the quaternary nitrogen, forms a 5 to 14 membered heterocyclic ring, said ring containing from 1 to 2 hetero atoms selected from the group of nitrogen, sulfur and oxygen; R.sub.1 forms a double bond in the heterocyclic ring of the quaternized nitrogen or is alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, alkylamidoalkyl and X.sup.- is a chloride, bromide or iodide anion. The invention also relates to the preparation and use of said quaternized polycyclic compounds.
Type:
Grant
Filed:
August 28, 1987
Date of Patent:
November 28, 1989
Assignee:
GAF Corporation
Inventors:
Robert B. Login, Ratan K. Chaudhuri, David J. Tracy, Michael W. Helioff
Abstract: Thio-bis-(hydrocarbyl substituted diacid materials), such as thio-bis-(polyalkyl lactone acid) and/or their precursors, the adducts of sulfur chloride and unsaturated diacid materials, e.g., 4,8-bis-polyalkyl-4, 8-dichloro-6-thiaundecane-1,2,10,11-tetracarboxylic acid bis-anhydride and especially their dehydrochlorinated analogs, when treated with an amine preferably polyalkylene polyamines such as tetraethylene pentamine, directly or in the presence of a metal template reagent, yield aminated thio-bis-(alkyl lactone acid) and thio-bis-(hydrocarbyl diacid) materials or their metal complexes which can be characterized in part, as macrocyclic and/or macrocyclic-like amide and/or imide structures, are useful as stable additives in lubricating compositions, e.g., as varnish inhibiting dispersants and/or inhibitors for lubricating oils and fuels.
Abstract: A compound of the formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or halogen;R.sub.2 and R.sub.3 are both hydrogen or together represent a bond;R.sub.4 is hydrogen and R.sub.5 is hydrogen or R.sub.4 and R.sub.5 together represent an oxo group;R.sub.6 is C.sub.1-7 alkyl substituted by NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen or C.sub.1-4 alkyl or together are C.sub.3-7 polymethylene optionally containing a further hetereoatom which is oxygen, sulphur or nitrogen substituted by R.sub.10 where R.sub.10 is hydrogen, C.sub.1-4 alkyl or benzyl, and optionally substituted by one or two C.sub.1-4 alkyl, C.sub.2-5 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminocarbonyl optionally substituted by one or two C.sub.1-6 alkyl groups or by a benzyl group, cyano, phenyl or benzyl and wherein any phenyl or benzyl group is optionally substituted in the phenyl ring by one or two halo, CF.sub.3, C.sub.1-4 alkyl, C.sub.
Abstract: Compounds of the formula: ##STR1## in which m is one of the integers 1, 2 or 3; n is one of the integers 0, 1 or 2; o is one of the integers 0, 1 or 2; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, halo, or, when taken together, 3,4-methylenedioxy; R.sub.3 is alkyl, ##STR2## where R.sub.4 and R.sub.5 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, halo or trifluoromethyl; and R.sub.6 is hydrogen or halo; or a pharmaceutically acceptable salt thereof.
Abstract: A compound of the formula (1) or a salt or solvate thereof: ##STR1## in which: R.sub.0 is hydrogen or C.sub.1-6 alkyl;R.sub.1 and R.sub.2 are both hydrogen; orR.sub.1 is hydrogen, C.sub.1-6 alkyl; and R.sub.2 is CN; CR.sub.5 R.sub.6 Y where R.sub.5 and R.sub.6 are independently selected from hydrogen and C.sub.1-4 alkyl and Y is selected from hydrogen, OR.sub.7 or SR.sub.7 where R.sub.7 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkanoyl, and NR.sub.8 R.sub.9 where R.sub.8 and R.sub.9 are independently hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl or C.sub.2-4 alkanoyl or together are C.sub.4-6 polymethylene; or COR.sub.10 is OH or C.sub.1-4 alkyl, or COR.sub.10 is a pharmaceutically acceptable ester or amide; orR.sub.2 is hydrogen, C.sub.1-6 alkyl, or phenyl optionally substituted by halogen, CF.sub.3, C.sub.1-4 alkoxy or C.sub.1-4 alkyl; and R.sub.1 is CN, CR.sub.5 R.sub.6 Y or COR.sub.10 as defined for R.sub.2 above; orR.sub.1 and R.sub.2 together form C.sub.3 -C.sub.
Type:
Grant
Filed:
April 16, 1987
Date of Patent:
April 4, 1989
Assignee:
Beecham Group p.l.c. of Beecham House
Inventors:
Robert W. Ward, Roger E. Markwell, Ian Hughes
Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.
Type:
Grant
Filed:
November 21, 1985
Date of Patent:
October 4, 1988
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
Abstract: Compounds of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Y have the indicated meanings, their physiologically tolerated acid addition salts, and a process for the preparation of these compounds, are described. The compounds inhibit thromboxane synthetase and can thus be used as medicaments.
Type:
Grant
Filed:
March 11, 1986
Date of Patent:
March 29, 1988
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Hans-Hermann Lau, Wilhelm Bartmann, Gerhard Beck, Gunther Wess
Abstract: Novel pyrimidine compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.1 ' are each hydrogen atom, a lower alkyl, benzyl, an alkali metal, or ammonium; R.sub.2 is hydrogen atom, a halogen atom, a lower alkyl, a lower alkoxy, an aryl, a group of the formula: ##STR2## (wherein R.sub.3 and R.sub.4 are each hydrogen atom, a lower alkyl, or an aryl), or a group of the formula: ##STR3## [wherein R.sub.5 and R.sub.6 are each an alkylene having 1 to 3 carbon atoms, and X is oxygen atom, methylene, or a group of the formula: >N-Y (wherein Y is hydrogen atom, a lower alkyl, benzyl, or an aryl)], which have excellent antiallergic activities and are useful for the prophylaxis and treatment of various allergic diseases, and a pharmaceutical composition containing said pyrimidine compound as an active ingredient.
Abstract: This invention relates to novel isoquinolinesulfonamide derivatives of Formula (I): ##STR1## wherein A is a C.sub.0-10 alkylene group or a C.sub.0-10 alkylene group having a C.sub.1-10 alkyl group, a phenyl group, a substituted phenyl group or a phenylalkyl group; R.sub.1 and R.sub.2 each is a hydrogen atom; or R.sub.1 and R.sub.2 are linked directly to form an ethylene group unsubstituted or substituted with a C.sub.1-4 alkyl group;R.sub.3 and R.sub.4 each is a hydrogen atom, a C.sub.1-6 alkyl group or linked directly to form a C.sub.2-6 alkylene group; and the pharmaceutically acceptable acid addition salt thereof, and to a process for preparing them. The isoquinoline derivatives possess a relaxatory action for vascular smooth muscle and action for increasing blood flow and are useful as a vasodilator and a hypotensor.
Abstract: An isoquinolinesulfonyl compound represented by the formula (I): ##STR1## wherein R.sup.1 : H, Cl, OHA : unsubstituted or substituted ethylene or alkyleneR.sup.2, R.sup.3 : H, alkyl, jointly forming unsubstituted or substituted ethylene or trimethyleneR.sup.4 : H, alkyl, amidinoor an acid salt thereof.They can be prepared, for example, by converting 1-R.sup.1 substituted-5-isoquinolinesulfonic acid to the corresponding sulfonyl chloride and subsequently reacting the chloride with a compound of formula ##STR2## They can be advantageously utilized as vasodilator, cerebral circulation ameliorator, antihypertensive agent and drugs for prevention and treatment of various circulatory organ diseases.
Abstract: Novel 3-amino-tetrahydro-1,3-thiazine-2,4-diones as well as skin treating compositions on the basis of a physiologically compatible carrier and customary additions containing these novel 3-amino-tetrahydro-1,3-thiazin-2,4-dione derivatives as active ingredients for thickening the epidermis. The skin treating compositions are applied 1-2 times daily on the skin for about 3 to 4 weeks. Due to the thickening of the epidermis they cause a strengthening of the skin protection, in particular against sun rays, cold and the contact with harmful environmental substances of all kinds. Moreover, the skin treating compositions are suitable for prophylactically fighting the so-called ageing of skin.
Type:
Grant
Filed:
October 9, 1984
Date of Patent:
March 31, 1987
Assignee:
Wella Aktiengesellschaft
Inventors:
Wolfgang Hanefeld, Rudi Rothlisberger, Friedrich Noser
Abstract: A new class of anti-spasmodic compounds having two branch chains is provided. The compounds have the general formula: ##STR1## wherein the substituents are defined hereinbelow.
Abstract: A new class of anti-spasmodic compounds having three branch chains is provided. These compounds have the general formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are saturated straight chain or branched alkyl groups contained from 1 to 8 carbon atoms, and are separated or linked to one another to form an aliphatic ring system. k is an integer from 0 to 5, and the total number of carbon atoms in R.sub.1 plus R.sub.2 plus R.sub.3 plus k are equal to or less than 12. Furthermore, l is an integer from 1 to 3, m is an integer from 1 to 3, n is an integer from 1 to 3, and X may be nonexistent or may be O, S, NH or CH.sub.2 or salts thereof. However, when X is nonexistent the terminal group in both the m chain and the n chain is a methyl group.
Abstract: New 3-carbamoyl- and 3-thiocarbamoyl-tetrahydro-1,3-thiazine-2-thiones are disclosed as skin treatment compositions based upon physiologically-compatible carriers and a content of these compounds as active substance for increasing the skin protection, in particular against sun radiation and contact with environmental substances of all types. The skin treatment compositions are also suitable for prophylactic control of so-called aging skin. The compositions are applied to the skin one or two times daily for about 3-4 weeks.
Type:
Grant
Filed:
January 24, 1985
Date of Patent:
February 17, 1987
Assignee:
Wella Aktiengesellschaft
Inventors:
Wolfgang Hanefeld, Rudi Rothlisberger, Friedrich Noser