Double Bonded Divalent Chalcogen Containing Patents (Class 544/52)
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Patent number: 5389653Abstract: Catechol derivatives of the formula ##STR1## wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adenosylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuronal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure.Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.Type: GrantFiled: April 16, 1993Date of Patent: February 14, 1995Assignee: Hoffman-La Roche Inc.Inventors: Karl Bernauer, Janos Borgulya, Hans Bruderer, Mose Da Prada, Gerhard Zurcher
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Patent number: 5382590Abstract: Compounds of formula: ##STR1## in which R.sub.1 represents a hydrogen atom or an alkyl, alkoxycarbonyl or an unsubstituted or substituted phenyl radical,R.sub.2 represents a hydrogen atom or an unsubstituted or substituted alkyl radical,R.sub.3 represents an alkyl, phenylalkyl, indanyl, cycloalkylalkyl or an unsubstituted or substituted phenyl radical, orR.sub.2 and R.sub.3 form a heterocycle together with the nitrogen atom to which they are attached, andR.sub.4 represents an unsubstituted or substituted phenyl radical, a naphthyl, indolyl or quinolyl radical or a phenylamino radical in which the phenyl ring is unsubstituted or substituted, their preparation and medicaments containing them.Type: GrantFiled: July 8, 1992Date of Patent: January 17, 1995Assignee: Rhone-Poulenc Rorer S.A.Inventors: Jean-Dominique Bourzat, Marc Capet, Claude Cotrel, Claude Guyon, Franco Manfre, Gerard Roussel
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Patent number: 5362706Abstract: Hydantoin for the control of weeds are disclosed.Type: GrantFiled: November 9, 1992Date of Patent: November 8, 1994Assignee: Sandoz Ltd.Inventors: Karl Seckinger, Fred Kuhnen
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Patent number: 5342824Abstract: N-aryltetrahydrophthalimide compounds of the general formula I ##STR1## where is --S--C(R).sub.2 --, and a method for controlling undesirble plant growth.Type: GrantFiled: September 30, 1992Date of Patent: August 30, 1994Assignee: BASF AktiengesellschaftInventors: Lothar Rueb, Karl Eicken, Peter Plath, Barbara Schwalge, Karl-Otto Westphalen, Bruno Wuerzer, Norbert Meyer
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Patent number: 5338734Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: November 25, 1992Date of Patent: August 16, 1994Assignee: Zeneca Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying K. Yee
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Patent number: 5332733Abstract: Pharmacologically active compounds corresponding to the general formula I ##STR1## which are optionally substituted in the benzene ring and in which X denotes oxygen or sulfur,Y denotes oxygen or sulfur,R.sup.1 denotes hydrogen or lower alkyl,n is an integer from 0 to 4, andR.sup.4 is an optionally substituted 6-membered unsaturated heterocycle containing 1 or 2 nitrogen atoms not directly bonded to the piperazine ring,and physiologically acceptable acid addition salts thereof.Type: GrantFiled: November 17, 1992Date of Patent: July 26, 1994Assignee: Kali-Chemie Pharma GmbHInventors: Daniel Jasserand, Francois Floc'h, Richard White
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Patent number: 5322835Abstract: A compound of the formula: ##STR1## wherein X is an oxygen atom or a sulfur atom, Y is a hydrogen atom or a fluorine atom, Z is a methylene group or a group of the formula: N--R.sub.5 (in which R.sub.5 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.7 alkenyl group, a C.sub.3 -C.sub.7 alkynyl group, a halo(C.sub.2 -C.sub.6)alkyl group or a C.sub.1 -C.sub.6 alkoxycarbonylmethyl group), R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, a C.sub.3 -C.sub.7 alkenyl group, a C.sub.3 -C.sub.7 alkynyl group, a halo(C.sub.2 -C.sub.6)alkyl group, a halo(C.sub.3 -C.sub.7)alkenyl group, a cyano(C.sub.1 -C.sub.6)alkyl group, a C.sub.1 -C.sub.6 alkoxy(C.sub.1 -C.sub.6)alkyl group or a C.sub.1 -C.sub.6 alkoxycarbonylmethyl group, R.sub.2 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sub.3 and R.sub.4 are, the same or different, each is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; n is an integer of 0 or 1, which is useful as a herbicide.Type: GrantFiled: April 13, 1989Date of Patent: June 21, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Junya Takahashi, Masayuki Enomoto, Toru Haga, Masaharu Sakaki, Ryo Sato
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Patent number: 5321025Abstract: The invention concerns a bicyclic heterocyclic compound of the formula I ##STR1## wherein Q is an optionally substituted 10-membered bicyclic heterocyclic moiety containing 1 or 2 N's and a further O or S heteroatom;A.sup.1 is a direct link to X.sup.1 or (1-3C)alkylene;X.sup.1 is oxy, thio, sulphinyl, sulphonyl or imino;Ar is optionally substituted phenylene or pyridylene;R.sup.1 is (1-4C)alkyl, (3-4C)alkenyl or (3-4C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula -A.sup.2 -X.sup.2 -A.sup.3 - which, together with the carbon atom to which A.sup.2 and A.sup.3 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.2 and A.sup.3 is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl or sulphonyl;or a pharmaceutically-acceptable salt thereof.The compounds of the invention are inhibitors of the enzyme 5-lipoxygenase.Type: GrantFiled: March 1, 1993Date of Patent: June 14, 1994Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: Pierre A. R. Bruneau, Graham C. Crawley
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Patent number: 5312820Abstract: Carbamoyl and oxycarbonyl derivatives of biphenylmethylamines of structure I are angiotensin-II antagonists with balanced AT.sub.1 and AT.sub.2 activity useful in the treatment of hypertension and related disorders and ocular hypertension. ##STR1## where X is --O-- or --N(R.sup.7)--.Type: GrantFiled: July 17, 1992Date of Patent: May 17, 1994Assignee: Merck & Co., Inc.Inventors: Wallace T. Ashton, Linda L. Chang, William J. Greenlee, Steven M. Hutchins, Ralph A. Rivero
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Patent number: 5296477Abstract: Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description.Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.Type: GrantFiled: December 1, 1992Date of Patent: March 22, 1994Assignee: Adir et CompagnieInventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5288749Abstract: The present invention provides tertiary and secondary amine compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof which are antagonists for alpha-2 adrenoreceptors and which inhibit serotonin (5-hydroxytryptamine, 5-HT) uptake.Type: GrantFiled: December 20, 1991Date of Patent: February 22, 1994Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, John F. DeBernardis, Rajnandan Prasad, Kevin B. Sippy, Karin R. Tietje
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Patent number: 5284841Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams ##STR1## which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: February 4, 1993Date of Patent: February 8, 1994Assignee: Merck & Co., Inc.Inventors: Lin Chu, Michael H. Fisher, Helmut Mrozik, William R. Schoen
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Patent number: 5283243Abstract: Pharmacologically active compounds corresponding to the formula I ##STR1## which are optionally substituted in the benzene ring and in which X denotes oxygen or sulfur,Y denotes oxygen or sulfur,R.sup.1 denotes hydrogen or lower alkyl,n is an integer from 0 to 4,R.sup.4 denotes hydrogen, andR.sup.5 denotes hydrogen, hydroxy or cyano, orR.sup.4 and R.sup.5 together form a bond,R.sup.6 denotes an A--R.sup.7 group in which R.sup.7 denotes an optionally substituted phenyl group, and A denotes a --CH.sub.2 -- group, a CO group or a bond, orR.sup.6 is a halogen-substituted 1-phenylmethyl-1H-benzimidazol-2-ylamino group,and physiologically acceptable acid addition salts thereof.Type: GrantFiled: November 15, 1991Date of Patent: February 1, 1994Assignee: Kali-Chemie Pharma GmbHInventors: Daniel Jasserand, Francois Floc', Richard White
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Patent number: 5283241Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. The compounds are prepared by substitution of an amino-lactam with a substituted amide function. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: August 28, 1992Date of Patent: February 1, 1994Assignee: Merck & Co., Inc.Inventors: Richard J. Bochis, Matthew J. Wyvratt, William R. Schoen
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Patent number: 5281592Abstract: Thiazine derivatives of the formula [I]: ##STR1## wherein R.sup.1 and R.sup.2 are both H or form a naphthalene ring together with the benzene ring; R.sup.3 and R.sup.4 are both H, or one of them is halogen and another is H; X is S or O; R.sup.5 and R.sup.6 are each i) H, ii) lower alkyl, iii) cycloalkyl, iv) substituted phenyl, v) naphthyl, vi) lower alkyl which is substituted by substituted or unsubstituted phenyl, or vii) S-containing heterocyclic group; one of Z.sup.1 and Z.sup.2 is O and another is H.sub.2 ; A is lower alkylene; R.sup.7 and R.sup.8 are each i) H, ii) lower alkyl, iii) lower alkenyl, iv) lower alkynyl, or v) lower alkyl which is substituted by substituted or unsubstituted phenyl, or both form together N-containing heterocyclic group; provided that when both of R.sup.1 and R.sup.2 are H, Z.sup.2 is O and either one of R.sup.5 and R.sup.Type: GrantFiled: September 23, 1992Date of Patent: January 25, 1994Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Masakatsu Ozeki, Shin-ichi Kodato, Kousuke Yasuda, Yukitsuka Kudo, Kayoko Maeda
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Patent number: 5281571Abstract: The invention herein relates to titled compounds having the structure ##STR1## wherein the R.sub.1 -(R.sub.4).sub.n members are as defined in the claims. Characteristic features of these compounds are the haloalkyl R.sub.2 radical and cyclization of two R.sub.4 members at the meta and para positions of the phenyl ring to form a substituted benzoxazinone ring fused to the phenyl or benzthiazinone ring. Such compounds are useful as active ingredients in herbicidal compositions to control undesirable weeds in various crops.Type: GrantFiled: September 25, 1991Date of Patent: January 25, 1994Assignee: Monsanto CompanyInventors: Scott S. Woodard, Bruce C. Hamper, Kurt Moedritzer, Michael D. Rogers, Deborah A. Mischke, Gerard A. Dutra
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Patent number: 5268381Abstract: Compounds of general formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, n, X and A are defined in the description. Medicinal products containing the same are useful as antidepressives or anxiolytics due to their 5-HT1A receptor agonist activity.Type: GrantFiled: September 16, 1992Date of Patent: December 7, 1993Assignee: Adir et CompagnieInventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5252571Abstract: 1,4-Benzothiazine-2-acetic acid derivatives having an excellent aldose reductase inhibitory activity which are useful for the prevention and treatment of diabetic complications, such as diabetic cataract, retinopathy, nephropathy and neuropathy.Type: GrantFiled: December 24, 1991Date of Patent: October 12, 1993Assignee: Sapporo Breweries LimitedInventors: Tomoji Aotsuka, Hiroshi Hosono, Toshio Kurihara, Yoshiyuki Nakamura, Tetsuo Matsui, Fujio Kobayashi
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Patent number: 5240919Abstract: Compounds of general formula (I): ##STR1## where R, X, A, B and p are defined in the description. Medicinal products useful for treating sleep disorders comprising the same.Type: GrantFiled: March 9, 1992Date of Patent: August 31, 1993Assignee: Adir et CompagnieInventors: Said Yous, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5234924Abstract: Compound of general formula (I): ##STR1## where R.sub.1, R.sub.2, R.sub.3, n and X are defined in the description. Medicinal products.Type: GrantFiled: December 5, 1991Date of Patent: August 10, 1993Assignee: Adir et CompagnieInventors: Thierry Taverne, Isabelle Lesieur, Patrick Depreux, Daniel H. Caignard, Beatrice Guardiola, Gerard Adam, Pierre Renard
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Patent number: 5232898Abstract: The invention is concerned with compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, n and X have the significances given in the description, as well as enol ethers and salts thereof and their manufacture. The compounds have herbicidal properties and are accordingly suitable as active ingredients of weed control compositions. The invention is also concerned with weed control compositions containing one or more of such substances as well as the use of the substances or compositions for the control of weeds. Certain starting materials, which also have herbicidal activity, and their production are also described.Type: GrantFiled: December 9, 1991Date of Patent: August 3, 1993Assignee: Ciba-Geigy CorporationInventors: Milos Suchy, Paul Winternitz, Martin Zeller
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Patent number: 5232930Abstract: The invention concerns a benzodioxole derivative of the formula I ##STR1## wherein Ar.sup.1 is an optionally substituted 9- or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen heteroatoms and optionally containing a further heteroatom selected from nitrogen, oxygen and sulphur;R.sup.1 is (1-6C)alkyl, (3-6C)alkenyl or (3-6C)alkynyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X--A.sup.2 -- which, together with the carbon atom to which A.sup.1 and A.sup.2 are attached, defines a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X is oxy, thio, sulphinyl or sulphonyl, and which ring may bear one or two substituents;or a pharmaceutically-acceptable salt thereof;which compounds are inhibitors of 5-lipoxygenase and are useful in the treatment of inflammatory or allergic disease.Type: GrantFiled: January 9, 1992Date of Patent: August 3, 1993Assignees: Imperial Chemical Industries PLC, ICI PharmaInventors: John F. Kingston, David Waterson
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Patent number: 5221744Abstract: Arylaminocarbonyl compounds of the formula (I) ##STR1## wherein R.sub.2-6, X.sub.1, A and m are as defined in the disclosure, intermediates therefore, synthesis thereof, and the use of said compounds for the control of weeds are described.Type: GrantFiled: August 17, 1992Date of Patent: June 22, 1993Assignee: Sandoz Ltd.Inventors: Karl Seckinger, Karlheinz Milzner, Fred Kuhnen, Sasank S. Mohanty
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Patent number: 5206235Abstract: There are disclosed certain novel compounds identified as benzo-fused lactams which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to increase the stature of those afflicted with a lack of a normal secretion of natural growth hormone. Growth promoting compositions containing such benzo-fused lactams as the active ingredient thereof are also disclosed.Type: GrantFiled: February 28, 1992Date of Patent: April 27, 1993Assignee: Merck & Co., Inc.Inventors: Michael H. Fisher, William R. Schoen, Matthew J. Wyvratt, Robert J. DeVita
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Patent number: 5185333Abstract: A benzazine compound, a geometrical isomer of said benzazine compound, an optical isomer of said benzazine compound, and a pharmaceutically acceptable salt of said benzazine compound, said benzazine compound being represented by formula (I): ##STR1## wherein each symbol is as defined in the specification. Said benzazine compounds exhibit 5-HT.sub.3 receptor antagonistic activity, and 5-HT.sub.1A receptor and/or 5-HT.sub.2 receptor and/or dopamine D.sub.2 receptor blocking activity so that they are useful as drugs for the prophylaxis or treatment of various digestive diseases vomiting and disturbances in central nervous systems and the like. The intermediates for said benzazine compounds are also disclosed.Type: GrantFiled: June 26, 1991Date of Patent: February 9, 1993Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Takeshi Kawakita, Takanobu Kuroita, Takemi Fukuda, Ryuhei Iezawa
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Patent number: 5182276Abstract: The present invention relates to a nootropic agent which comprises a derivative of 2-phenyl-3-oxo-2H-1,4-benzothiazine. This nootropic agent is effective for treating diseases accompanied by a lowering of cerebral functions, for instance, cerebral infarction disorders due to ischemia such as transitory cerebral ischemia, brain edema, cerebral disorders due to the after-effect such as cerebral hemorrhage, cerebral disorders due to traumatic injury such as bruise, central nervous degeneration and degenerative diseases such as dementia, mental disorders, neurosis and Alzheimer's diseases.Type: GrantFiled: December 27, 1990Date of Patent: January 26, 1993Assignees: Santen Pharmaceutical Co., Ltd., Daiichi Pharmaceutical Co., Ltd.Inventors: Yasufumi Shirasaki, Shinichiro Ashida
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Patent number: 5141935Abstract: A compound represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom, a halogen atom, a nitro group, a lower alkyl group or a trifluoromethyl group; R.sup.3 represents a hydrogen atom, a lower alkyl group, a phenyl group or a lower alkoxy-carbonyl group; R.sup.4 and R.sup.5 each represent a hydrogen atom or a lower alkyl group; R.sup.6 represents a halogen atom; and X represents an oxygen atom or a sulfur atom,and a microorganism control agent, comprising the above compound as an active ingredient.Type: GrantFiled: September 25, 1989Date of Patent: August 25, 1992Assignee: Ube Industries, Ltd.Inventors: Mitsuaki Takenaka, Masanori Watanabe
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Patent number: 5109006Abstract: This invention relates to novel derivatives of 1,7'-[imidazo-[1,2-a]pyridine]5'-(6'H)ones, to the method for their preparation and to their use as anti-hypertensive, anxiety, anti-depressant and anti-migraine agents, and to their use as appetite regulators useful for the treatment of anorexia and obesity.Type: GrantFiled: August 22, 1991Date of Patent: April 28, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventor: Marcel Hibert
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Patent number: 5096918Abstract: The invention concerns pharmaceutially useful heterocyclic nitromethane compounds of the formula I: ##STR1## in which ring Q is a heterocycle of 4 to 7 ring atoms, the fragment completing the ring Q having 2 to 5 atoms, one of which is carbon, oxygen, sulphur or a group of the formula --NRa--, and the remainder are carbon; Ra is hydrogen, (1-6C)alkyl, (2-6C)alkanoyl, trifluoroacetyl, phenyl, benzoyl, or phenyl(1-4C)alkyl, the latter three optionally substituted; and R.sup.1 R.sup.2 and R.sup.3 are independently hydrogen, hydroxy, (1-6C)alkyl, (1-6C)alkoxy, phenyl, phenoxy or phenyl(1-4C)alkyl, the last three optionally substituted, or two of R.sup.1, R.sup.2 and R.sup.3 situated on adjacent ring carbon atoms and together with said carbon atoms form a benzene ring fused to ring Q, the benzene ring itself optionally substituted, provided that when the fragment completion ring Q is of 3 atoms then at least one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen; and salts thereof.Type: GrantFiled: February 5, 1990Date of Patent: March 17, 1992Assignee: Imperial Chemical Industries PLCInventor: Keith B. Mallion
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Patent number: 5081242Abstract: The synthesis of benzoxazinyl- and benzothiazinylpyridazinone compounds is described. The novel compounds are cardiotonic agents and inhibitors of phosphodiesterase. In addition, the compounds are useful as smooth muscle relaxants and bronchodilators.Type: GrantFiled: February 15, 1991Date of Patent: January 14, 1992Assignee: Ortho Pharmaceutical CorporationInventor: Donald W. Combs
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Patent number: 5077401Abstract: Herbicidal benzo-fused cyclic compounds of the formula ##STR1## wherein Q is ##STR2## Y is O or S, W is ##STR3## T is O, S, --NH-- or ##STR4## and R.sup.4 may represent, together with T, chlorine,Z is O or S,X is hydrogen or halogen,n is 0 or 1 andR is C.sub.3-6 cycloalkyl, and optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms,and salts thereof.Type: GrantFiled: October 6, 1989Date of Patent: December 31, 1991Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi, Katsuhiko Shibuya
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Patent number: 5047529Abstract: Phenylsulfones of the formula ##STR1## in which R.sup. is hydrogen, halogen, C.sub.1 -C.sub.4 -alkyl, nitro, hydroxysulfonyl, carboxyl,the radical --NR.sup.3 R.sup.4,in which R.sup.3 and R.sup.4 are the same or different and denote hydrogen or C.sub.1 -C.sub.4 alkyl, which may or not be substituted,or the radical S(O).sub.n R.sup.5,in which n is 0 or 2 and R.sup.5 denotes C.sub.1 -C.sub.4 -alky which may or may not be substituted,R.sup.2 is hydroxy, mercapto or the radical R.sup.1,X is the radical ##STR2## or, with R.sup.2 in the ortho-position relative to the group SO.sub.2 --X,R.sup.2 and X together denote the radial ##STR3## in which Z.sup.1 is hydroxy, chlorine, C.sub.1 -alkanoyloxy- C.sub.1 -C.sub.4 -alkylsulfonyloxy penylsulfonyloxy, o- or p-tolylsulfonyloxy or sulfato andZ.sup.2 is oxygen, sulfur, imino or optionally substituted C.sub.1 -C.sub.4 -alkylimino, andY denotes amino, C.sub.1 -C.sub.4 -alkanoylamino or nitro, and a process for the preparation thereof.Type: GrantFiled: March 13, 1990Date of Patent: September 10, 1991Assignee: BASF AktiengesellschaftInventors: Manfred Patsch, Klaus Pandl, Martin Fischer
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Patent number: 5041454Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.Type: GrantFiled: April 19, 1990Date of Patent: August 20, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn
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Patent number: 5025010Abstract: A description is given of compounds I ##STR1## with R(1) equal to H, alkyl, alkoxy, Hal, NO.sub.2, OH, acetamido or amino; R(2) equal to H, alk(en)yl or phenylalkyl; R(3) equal to H, (cyclo)alk(en)yl(alkyl), phenyl or phenylalkyl; R(4) equal to H, alkyl, alkoxy, Hal CF.sub.3, NO.sub.2, OH, acetamido or amino; A equal to --C.tbd.C-- or --CH.dbd.CH--; R(5) equal to various amines; m and n equal to 1-3; and their salts. Preparation processes are also described. Compounds I are excellent calcium agonists or calcium antagonists. They also act to regulate the blood glucose.Type: GrantFiled: October 17, 1989Date of Patent: June 18, 1991Assignee: Hoechst AktiengesellschaftInventors: Raymond Oekonomopulos, Rainer Henning, Ulrich Lerch, Bernward Scholkens, Wolfgang Linz
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Patent number: 5015642Abstract: Compounds I ##STR1## in which R(1) and R(4) equal H, alkyl, alkoxy, Hal, CF.sub.3, NO.sub.2, OH, acetamido or amino;R(2) equals H, alk(en)yl or phenylalkyl (optionally substituted);R(3) equals H, (cyclo)alk(en)yl-(alkyl), phenyl or phenylalkyl (optionally substituted);A equal CHOH, CO, CH.dbd.CH, C.tbd.C, CH.sub.2, O or S;m equals 1 or 2;n equals 1 to 3;p equals 0 to 4;R(5) equals some amino groups, and their salts, exhibit excellent calcium-antagonistic activity.Processes for their preparation are described.Type: GrantFiled: August 10, 1988Date of Patent: May 14, 1991Assignee: Hoechst AktiengesellschaftInventors: Ulrich Lerch, Rainer Henning, Hansjorg Urbach, Joachim Kaiser
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Patent number: 4975439Abstract: Substituted N-(1-alkyl-3-hydroxy-4-piperidinyl)benzamides, their N-oxide forms, their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms having gastrointestinal motility stimulating properties, compositions containing the same, and methods of treating warm-blooded animals suffering from motility disorders of the gastrointestinal system.Type: GrantFiled: September 2, 1988Date of Patent: December 4, 1990Assignee: Janssen Pharmaceutical N.V.Inventors: Georges H. P. Van Daele, Freddy F. Vlaeminck, Michel A. J. De Cleyn
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Patent number: 4929269Abstract: Compounds of the formula ##STR1## and salts thereof, W and W, being independently O and S, A being a nitrogen-containing heterocyclic ring system, E being O, S(O)m or NR.sub.3 where m is 0-2, R.sub.1, R.sub.2 and R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 alkenyl or alkynyl and E.sub.1 being hydrogen, halogen or one of a variety of organic substituents.The compounds are effective herbicides.Type: GrantFiled: October 19, 1988Date of Patent: May 29, 1990Assignee: ICI Australia Operations Proprietary LimitedInventors: Keith G. Watson, Peter Drygala, Stephen Bell
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Patent number: 4908453Abstract: Reagents useful in the preparation of 5'-biotinylated oligonucleotides are disclosed.Type: GrantFiled: January 23, 1989Date of Patent: March 13, 1990Assignee: E. I. Du Pont De Nemours and CompanyInventor: Anthony J. Cocuzza
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Patent number: 4902335Abstract: Herbicidal benzo-fused cyclic compounds of the formula ##STR1## wherein Q is ##STR2## Y is O or S, W is ##STR3## T is O, S, --NH-- or ##STR4## and R.sup.4 may represent, together with T, chlorine,Z is O or S,X is hydrogen or halogen,n is 0 or 1 andR is C.sub.3-6 cycloalkyl, an optionally substituted 5-membered heterocyclic group or an optionally substituted 6-membered heteroaromatic group which contains one to three nitrogen atoms,and salts thereof.Type: GrantFiled: June 17, 1988Date of Patent: February 20, 1990Assignee: Nihon Tokushu Noyaku Seizo K.K.Inventors: Toyohiko Kume, Toshio Goto, Atsumi Kamochi, Akihiko Yanagi, Shigeki Yagi, Hiroshi Miyauchi, Katsuhiko Shibuya
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Patent number: 4877785Abstract: Non-peptidyl compounds characterized generally as .beta.-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.Type: GrantFiled: October 1, 1987Date of Patent: October 31, 1989Assignee: G. D. Searle & Co.Inventors: Gunnar J. Hanson, John S. Baran
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Patent number: 4863949Abstract: The present invention provides compounds of the general formula: ##STR1## wherein Ar is a substituted or unsubstituted aromatic or heteroaromatic radical, A is a straight-chained or branched alkylene chain containing up to 8 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms, B is a straight-chained mono- or bicyclic, optionally branched, saturated or unsaturated alkylene chain containing up to 12 carbon atoms, a --CH.sub.2 -- group of which can be replaced by a cycloalkylene radical containing 3 to 7 carbon atoms and/or up to two --CH.sub.2 -- groups of which can be replaced by an oxygen or a sulphur atom or by an --S(.dbd.O) or --S(.dbd.O).sub.2 group, X is a valency bond, an oxygen atom or an --NR.sup.1 group, in which R.sup.1 is a hydrogen atom or a straight-chained or branched, saturated or unsaturated alkyl or nitroxyalkyl radical containing up to 6 carbon atoms or R.sup.1, together with the nitrogen atom of the --NR.sup.Type: GrantFiled: September 21, 1987Date of Patent: September 5, 1989Assignee: Boehringer Mannheim GmbHInventors: Herbert Simon, Helmut Michel, Wolfgang Bartsch, Klaus Strein
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Patent number: 4859692Abstract: The invention concerns novel, pharmaceutically useful, amide derivatives of certain benzoheterocyclylalkanoic acids (and related tetrazoles and acylsulphonamides) of the formula I and salts thereof, wherein the radicals R.sup.1, R.sup.2, L, X, Y, Z, A.sup.1, Q, A.sup.2 and M have the meanings set out in the specification. The invention also includes pharmaceutical compositions incorporating a formula I compound or a salt thereof, a process for the manufacture of the said compound, together with intermediates for use in the latter process.Type: GrantFiled: April 16, 1986Date of Patent: August 22, 1989Assignee: ICI Americas Inc.Inventors: Peter R. Bernstein, Frederick J. Brown, Victor G. Matassa, Ying Kwong Yee
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Patent number: 4831028Abstract: Benzothiazinone derivatives I ##STR1## with R.sup.1 and R.sup.4 being H, alkyl, alkoxy, Hal, CF.sub.3, NO.sub.2, OH, acetamido or amino,R.sup.2 being H, (cyclo)alk(en)yl, cycloalkylakyl, phenyl or phenylalkyl,A being (CH.sub.2).sub.m O(CH.sub.2).sub.n, (CH.sub.2).sub.p --CH(OH)--CH.sub.2).sub.q, (CH.sub.2).sub.p --CH(OCH.sub.3)--(CH.sub.2).sub.q, or (CH.sub.2).sub.r OCH.sub.2 --CO-- and (CH.sub.2).sub.s --CO--,R.sup.5 being NR(6)R(7) or certain cyclic amines, show a calcium-antagonistic action.They are obtained, inter alia, from II ##STR2## by reaction with III ##STR3## A and B are same or different and are lower alkylene having 1 to 6 carbon atoms; and n is 3 to 4.Type: GrantFiled: April 24, 1987Date of Patent: May 16, 1989Assignee: Hoechst AktiengesellschaftInventors: Ulrich Lerch, Rainer Henning
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Patent number: 4786635Abstract: This invention relates to novel benzothizine derivatives of the formula [I], processes for preparing them and therapeutic agents for circulatory diseases containing them as an active ingredient, ##STR1## wherein R.sup.1 is one or more groups selected from those consisting of hydrogen, lower alkyl, halogen, nitro, hydroxy, lower alkoxy, lower alkanoyloxy, amino, lower alkylamino and lower alkoxycarbonyloxy;R.sup.2 is hydrogen, lower alkyl or (C.sub.3 -C.sub.6)cycloalkyl;R.sup.3 is one or more groups selected from those consisting of hydrogen, lower alkyl, hydroxy, lower alkoxy, halogen, nitro, lower alkylenedioxy, lower alkanoyloxy, lower alkanoyl, amino, lower alkylamino, lower alkanoylamino and lower alkoxycarbonyloxy or ##STR2## R.sup.4 is hydrogen or lower alkyl.Type: GrantFiled: March 10, 1987Date of Patent: November 22, 1988Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Jun-ichi Iwao, Tadashi Iso, Masayuki Oya
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Patent number: 4774331Abstract: A process for ortho-cyanation of phenols or phenylamines which comprises reacting a phenyl compound having hydroxy or optionally substituted amino or cyclic amino, of which ortho position is vacant, with trichloroacetonitrile, C.sub.1 -C.sub.5 alkyl thiocyanate or C.sub.6 -C.sub.12 aryl thiocyanate in the presence of a boron trihalide and treating the resultant product with an alkali is provided, and said process is useful in the synthesis of intermediates for medicinals or pesticides.Type: GrantFiled: August 21, 1987Date of Patent: September 27, 1988Assignee: Shionogi & Co., Ltd.Inventors: Makoto Adachi, Hiromu Matsumura, Tsutomu Sugasawa
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Patent number: 4771050Abstract: Compounds of the general formula: ##STR1## wherein, R.sup.1 and R.sup.2 are, the same or different, hydrogen, a halogen, a lower alkyl, a cycloalkyl, a lower alkoxy, trifluoromethyl or a phenylalkyloxy whose phenyl ring may be substituted by one to three substituents selected from the group consisting of a halogen, a lower alkyl, a lower alkoxy, methylenedioxy and trifluoromethyl; R.sup.3 is hydrogen or methyl; R.sup.4 is carboxyl or an esterified carboxyl; and X is oxygen or sulfur, or a salt thereof. These compounds possess aldose reductase inhibitory and platelet aggregation inhibitory activities, and are of use as drugs for prevention and treatment of diabetic complications such as diabetic cataract, retinophathy, nephropathy, and neuropathy.Type: GrantFiled: April 13, 1987Date of Patent: September 13, 1988Assignees: Takeda Chemical Industries, Ltd., Senju Pharmaceutical Co., Ltd.Inventors: Kanji Meguro, Hitoshi Ikeda, Yujiro Yamamoto
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Patent number: 4766118Abstract: The synthesis of benzoxazinyl- and benzothiazinylpyridazinone compounds is described. The novel compounds are cardiotonic agents and inhibitors of phosphodiesterase. In addition, the compounds are useful as smooth muscle relaxants and bronchodilators.Type: GrantFiled: June 22, 1987Date of Patent: August 23, 1988Assignee: Ortho Pharmaceutical CorporationInventor: Donald W. Combs
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Patent number: 4755509Abstract: The invention relates to new compounds of the formula: ##STR1## Aldose reductase inhibitors. Treatment of certain complications of diabetes.Type: GrantFiled: May 14, 1985Date of Patent: July 5, 1988Assignee: CarbipemInventor: Jean-Marie Teulon
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Patent number: 4739050Abstract: This invention relates to 2-arylbenzothiazine derivatives of the formula[I] and salts thereof, process of preparation and therapeutic drug comprising them for circulatory diseases, ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and are hydrogen, lower alkyl, hydroxy, lower alkoxy, acyloxy, tetrahydropyranyloxy, halogen, nitro, amino, lower alkylamino or ##STR2## and the lower alkoxy group may be substituted by halogen, formyl, lower alkoxy or epoxy;R.sup.3 is hydrogen or lower alkyl;R.sup.4 is hydrogen, lower alkyl, cycloalkyl, hydroxy, lower alkoxy, mercapto, lower alkylthio, arylthio, halogen, cyano, formyl-lower alkyl, lower alkoxy-lower alkyl or ##STR3## R.sup.5,R.sup.6,R.sup.7 and R.sup.Type: GrantFiled: November 4, 1986Date of Patent: April 19, 1988Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Iwao Jun-ichi, Iso Tadashi, Oya Masayuki
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Patent number: 4732898Abstract: The present invention are 2-(2-aryl-2-oxo-alkylidene) analogs of 1,2,3,4-tetrahydropyridine-3,5-pyridinecarboxylic acids and particularly esters thereof having valuable calcium antagonist and positive inotropic activity useful in the treatment of cardiovascular disorders, pharmaceutical compositions and methods of use therefor.Type: GrantFiled: March 3, 1987Date of Patent: March 22, 1988Assignee: Warner-Lambert CompanyInventors: Edward W. Badger, Michael D. Taylor