Chalcogen Or Nitrogen Attached Directly To The Hetero Ring By Nonionic Bonding Patents (Class 540/482)
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Patent number: 5215980Abstract: Compounds of the formula: ##STR1## where R is hydrogen, C.sub.1 -C.sub.10 alkylcarbonyl, or C.sub.1 -C.sub.10 alkyl which can be substituted by amino or cyano, R.sup.1 and R.sup.2 are independently hydrogen, hydroxyl or amino, and the pharmaceutically aceptable salts and esters thereof. Pharmaceutical compositions and methods of their use are also provided for.Type: GrantFiled: January 17, 1992Date of Patent: June 1, 1993Assignee: Merck & Co., Inc.Inventor: Anthony B. Jones
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Patent number: 5136053Abstract: A method for producing a cyclic alkyleneimine, which comprises reacting a cyclic ether with a compound of the formula NH.sub.2 R wherein R is a hydrogen atom or an alkyl group, in a vapor phase in the presence of a solid acid catalyst, wherein the reaction is conducted under a pressure of at least 0.5 kg/cm.sup.2 G as the total pressure of partial pressures of the reactants and the reaction product.Type: GrantFiled: March 2, 1990Date of Patent: August 4, 1992Assignee: Mitsubishi Kasei CorporationInventors: Hitoshi Sugiyama, Tomoyuki Mori
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Patent number: 5098916Abstract: Certain propanobicyclic amine compounds are described for treatment of CNS disorders such as psychotic disorders, convulsions, dystonia and cerebral ischemia. Compounds of particular interest are of the formula ##STR1## wherein each R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y and Z is independently selected from hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, phenalkyl, phenyl, alkoxy, phenoxy, phenalkoxy, alkoxyalkyl, halo, haloalkyl and hydroxyalkyl; wherein R.sup.3 and R.sup.4 may be taken together to form oxo;wherein each of R.sup.9, R.sup.10, R.sup.11, R.sup.12, R.sup.13 and R.sup.14 is independently selected from hydrido, alkyl, cycloalkyl, hydroxyalkyl, fluoroalkyl, cycloalkylalkyl, alkoxyalkyl, henalkyl and phenyl; wherein G within the nitrogen-containing cyclohetero moiety is selected from ##STR2## wherein R.sup.15 is selected from hydrido, alkyl, cycloalkyl, cycloalkylalkyl, phenyl, phenalkyl, alkoxyalkyl and hydroxyalkyl; wherein each of R.sup.16 and R.sup.Type: GrantFiled: March 29, 1990Date of Patent: March 24, 1992Assignee: G. D. Searle & Co.Inventors: Nancy M. Gray, Brian K. Cheng
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Patent number: 5089471Abstract: Non-peptidyl compounds characterized generally as .beta.-aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: February 18, 1992Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 5041545Abstract: Hydrazide functionalized 2-hydroxybenzophenone ultraviolet light and heat stabilizers and derivatives are disclosed having the general formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, X, Y, Z, all substituents thereof, and n are set forth in the Summary of the Invention. Y--N(R.sup.6)--Z is the hydrazide or derivative group and --X--R.sup.5 -- links the hydrazide group to an aromatic nucleus of the optionally substituted benzophenone group. Derivatives are, for example, acyl hydrazides, diacyl hydrazides (including imides), hydrazones and alkyl hydrazides. The compounds are useful as ultraviolet light absorbers and heat stabilizers for plastics.Type: GrantFiled: April 6, 1989Date of Patent: August 20, 1991Assignee: Atochem North America, Inc.Inventor: Terry N. Myers
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Patent number: 4994612Abstract: Dihydropyridine derivatives of the formula ##STR1## wherein the symbols R and R.sup.1 to R.sup.6 have the significance given in claim 1, have a pronounced calcium-antagonist activity and can accordingly be used as medicaments, especially in the control or prevention of angina pectoris, ischemia, high blood pressure and/or migraine.Type: GrantFiled: April 11, 1989Date of Patent: February 19, 1991Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jaunin, Henri Ramuz
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Patent number: 4977141Abstract: Non-peptidyl compounds characterized generally as aminoacyl aminodiol carbamates are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: December 11, 1990Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4889849Abstract: The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is phenyl, or a 5- or 6-membered aromatic group containing 1 or 2 of the following hetero atoms: oxygen and/or sulphur and/or nitrogen;R.sub.1 and R.sub.2 may be equal or different and are hydrogen or substituents;R.sub.3 is a hydrogen atom or, together with R.sub.4, may form a ring consisting of 6 or 7 carbon atoms;R.sub.4 is a hydrogen atom or alkyl group having 1-3 carbon atoms;R.sub.5 is a straight, branched or cyclic alkyl group having 1-4 carbon atoms;R.sub.6 is a straight or branched, saturated or unsaturated alkylene group having a chain length of 2-6 carbon atoms;Z is the group NR.sub.12, wherein R.sub.12 is a hydrogen atom or an alkyl group having 1-3 carbon atoms, or Z is an oxygen atom;n has the value 0 or 1;X is a carbonyl group, thiocarbonyl group or SO.sub.2 group;R.sub.7 and R.sub.Type: GrantFiled: January 9, 1989Date of Patent: December 26, 1989Assignee: Duphar International Research B.V.Inventors: Ineke Van Wijngaarden, Johannes M. A. Zwagemakers, Jan Van Dijk
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Patent number: 4880821Abstract: A compound of the formula ##STR1## wherein: R.sub.1 and R.sub.2 are defined as follows:R.sub.1 is hydrogen, an alkyl group, or an alkyl group having one or more hydroxy groups;R.sub.2 is an alkyl group having one or more hydroxy groups, or an alkyl group containing an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups same or different, or two alkyl groups which together form a cyclic amine, e.g. piperidine;R.sub.3 is hydrogen or an alkyl group; andR.sub.4 is hydrogen or an alkyl group.The compounds have high radiosensitizing activity and selectivity for hypoxic cells.Type: GrantFiled: August 17, 1988Date of Patent: November 14, 1989Assignee: Merck & Co., Inc.Inventor: Walfred S. Saari
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Patent number: 4663435Abstract: Somatostatin analogs are prepared wherein a cyclic hexapeptide contains a bridged grouping which replaces eight of the ring amino acids of somatostatin. The bridged cyclic hexapeptides are easier to synthesize, have a longer duration of activity, and many have a greater level of activity than somatostatin. The compounds have the properties of selectively inhibiting the release of glucagon, growth hormone and insulin. Certain of the compounds also are capable of inhibiting the release of gastric acid secretions. The compounds are particularly useful in the treatment of acromegaly, diabetes, diabetic retinopathy and peptic ulcers. These bridged cyclic hexapeptides are prepared by the solid phase method.Type: GrantFiled: June 24, 1985Date of Patent: May 5, 1987Assignee: Merck & Co., Inc.Inventor: Stephen F. Brady
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Patent number: 4628085Abstract: A process for selective preparation of lactams which comprises contacting, in the vapor phase, an aliphatic or aromatic aminonitrile having the formula HR.sub.1 N--D--CN wherein D is a divalent organic moiety and wherein R.sub.1 is (C.sub.1 -C.sub.4) alkyl or hydrogen with an effective amount of a silica catalyst, in the form of substantially spherical beads having a BET surface area greater than about 250 m.sup.2 /g, preferably between 300 and 500 m.sup.2 /g, and an average pore diameter less than about 20 nanometers preferably 8-10 nanometers at a temperature in the range of about 200.degree. to about 400.degree. C. and at a hydrogen or inert gas flow with a pressure in the range of about 0 to about 300 kPa, in the presence of: (a) ammonia in an amount equal to from 0 to about 50 mole percent of the molar amount of aliphatic or aromatic aminonitrile present; and (b) water in an amount from at least about 1.Type: GrantFiled: September 3, 1985Date of Patent: December 9, 1986Assignee: Allied CorporationInventors: Frank Mares, Reginald T-H. Tang, James E. Galle, Rose M. Federici
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Patent number: 4626537Abstract: The invention relates to novel guanidine derivatives, particularly to substituted guanidines of the formula ##STR1## having hypoglycaemic activity, for the oral treatment of hyperglycaemia in mammals, especially for the oral treatment of Diabetes mellitus.Type: GrantFiled: February 28, 1986Date of Patent: December 2, 1986Assignee: Ciba-Geigy CorporationInventors: Krishna G. Dave, Thomas George
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Patent number: 4625023Abstract: Process for the selective conversion of dinitriles into the corresponding lactam by treating the dinitrile with an effective amount of a hydrogenation catalyst such as copper chromite in combination with a co-catalyst, such as titania, at a temperature in the range of from about 200.degree. C. to about 400.degree. C. and at a pressure of at least 50 kPa in the presence of water and hydrogen.Type: GrantFiled: September 3, 1985Date of Patent: November 25, 1986Assignee: Allied CorporationInventors: Frank Mares, Reginald Y. Tang, James E. Galle, Rose M. Federici