Patents Examined by James H. Turnipseed
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Patent number: 5051418Abstract: Antibacterial 8-cyano-1-cyclopropyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid derivatives of the formula ##STR1## in which Y represents a carboxyl group, a nitrile group, an ester group --COOR.sup.1 or an acid amide group --CONR.sup.2 R.sup.3,X.sup.1 represents hydrogen nitro, alkyl or halogenX.sup.4 can be hydrogen or halogen, or alkyl,R.sup.4 and R.sup.5, together with the nitrogen atom to which they are bonded, form a 5- or 6-membered heterocyclic ring which can additionally contain the atoms or groups --O--, --S--, --SO--, --SO.sub.2 --, ##STR2## as ring members or the group ##STR3## can also represent a ring system of the structure ##STR4## which can optionally be substituted on the ring carbons by methyl and pharmaceutically usable hydrates, salts or esters thereof.These compounds have a high antibacterial activity and are therefore suitable as active compounds for human and veterinary medicine.Type: GrantFiled: November 13, 1989Date of Patent: September 24, 1991Assignee: Bayer AktiengesellschaftInventors: Michael Schriewer, Klaus Grohe, Uwe Petersen, Ingo Haller, Karl G. Metzger, Rainer Endermann, Hans-Joachim Zeiler
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Patent number: 5043450Abstract: Quinolonecarboxylic acid derivatives of the following formula, ##STR1## wherein R indicates a hydrogen atom or lower alkyl group, R.sup.1 indicates a lower alkyl group, R.sup.2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, ##STR2## (here, n is 0 or 1, R.sup.3 indicates a hydrogen atom or lower alkyl group, R.sup.4 indicates a hydrogen atom, lower alkyl group or substituted lower alkyl group and R.sup.5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.Type: GrantFiled: October 22, 1990Date of Patent: August 27, 1991Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Kuniyoshi Masuzawa, Seigo Suzue, Keiji Hirai, Takayoshi Ishizaki
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Patent number: 5039681Abstract: A novel piperidine derivative is defined by the formula (I), including a salt thereof, ##STR1## wherein R.sup.1 denotes a univalent group derived from one selected among substituted or unsubstituted benzene, pyridine, pyrazine, indole, anthraquinone, quinoline, substituted or unsubstituted phthalimide, homophthalimide, pyridinecarboxylic acid imide, pyridine N-oxide, pyrazinedicarboxylic acid imide, naphthalenedicarboxylic acid imide, substituted or unsubstituted quinazolinedione, 1,8-naphthalimide, bicyclo [2.2.2] oct-5-ene-2,3-dicarboxylic acid imide and pyromerylimide,X denotes a group of the formula --(CH.sub.2).sub.n --, a group of the formula --O(CH.sub.2).sub.n --, a group of the formula --S(CH.sub.2).sub.n --, a group of the formula --NH(CH.sub.2).sub.n --, a group of the formula --SO.sub.2 NH(CH.sub.2).sub.n --, a group of the formula ##STR2## a group of the formula ##STR3## a group of the formula ##STR4## a group of the formula --CH.sub.2 NH(CH.sub.2).sub.Type: GrantFiled: February 14, 1990Date of Patent: August 13, 1991Assignee: Eisai Co., Ltd.Inventors: Hachiro Sugimoto, Takaharu Nakamura, Yutaka Tsuchiya, Hiroyuki Sugumi, Kunizou Higurashi, Norio Karibe, Yoshiharu Yamanishi, Hiroo Ogura, Shin Araki, Atsuhiko Kubota, Michiko Ohtake, Kiyomi Tamatsu
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Patent number: 5037835Abstract: There are described compounds of the formula, ##STR1## where R is hydrogen, loweralkyl, arylloweralkyl or loweralkylcarbonyl;k is 0 or 1;m is 1, 2 or 3;k+m is 2 or 3; andn is 0 or 1;which compounds are useful as topical antiinflammatory agents for the treatment of various dermatoses.Type: GrantFiled: September 27, 1990Date of Patent: August 6, 1991Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: Richard C. Effland, Joseph T. Klein, Gordon E. Olsen, Larry Davis
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Patent number: 5037829Abstract: (1H-azol-1-ylmethyl)substituted quinazoline derivatives, compositions containing the same, and methods of treating mammals suffering from disorders which are characterized by an increased proliferation and/or abnormal differentiation of epithelial tissues.Type: GrantFiled: November 13, 1989Date of Patent: August 6, 1991Assignee: Janssen Pharmaceutica N.V.Inventors: Eddy J. E. Freyne, Alfons H. M. Raeymaekers, Gerard C. Sanz, Marc G. Venet
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Patent number: 5032600Abstract: The invention refers to new diamines of the Formula I ##STR1## wherein R stands for ##STR2## or --NH--COA.sup.1 --R.sup.4 or ##STR3## wherein A stands for C.sub.1-5 alkylene which can be substituted by hydroxyl,X stands for a single or double bond,R.sup.2 stands for aryl or heteroaryl optionally substituted by halogen, C.sub.1-4 alkoxy or acylamino,R.sup.3 stands for hydrogen or C.sub.1-4 alkyl,A.sup.1 stands for a single bond or C.sub.1-5 alkyl optionally substituted by hydroxyl or thioalkylene or oxyalkylene,R.sup.4 stands for a 5- or 6- membered aromatic or heteroaromatic ring which can be substituted by one or more hydroxyl, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy and/or halogen or methylenedioxy and the alkyl group can be unsaturated as well,Q stands for a 6-membered ring which can be partially hydrogenated, andR.sup.1 stands for C.sub.1-4 alkyl.The new compounds are antiarrhythmic agents.Type: GrantFiled: October 31, 1990Date of Patent: July 16, 1991Assignee: Alkaloida Vegyeszeti GyarInventors: Kalman Hideg, Olga H. Hankovszky, Laszlo Frank, Ilona Bodi, Jozsef Csak
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Patent number: 5030635Abstract: Novel 6,7-dimethoxy-1,2-dihydro-2-arylquinazoline-3-oxides and their synthesis are described. These novel compounds are cardiotonic agents and bronchodilating agents, and as such are useful for the treatment of heart failure and asthma.Type: GrantFiled: August 8, 1990Date of Patent: July 9, 1991Assignee: Ortho Pharmaceutical CorporationInventors: Donald W. Combs, Robert Falotico, David M. Ritchie
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Patent number: 5028609Abstract: The invention refers to new diamines of the Formula I ##STR1## wherein R stands for ##STR2## wherein A stands for C.sub.1-5 alkylene which can be substituted by hydroxyl,X stands for a single or double bond,R.sup.2 stands for aryl or heteroaryl optionally substituted by halogen, C.sub.1-4 alkoxy or acylamino,R.sup.3 stands for hydrogen or C.sub.1-4 alkyl,A.sup.1 stands for a single bond or C.sub.1-5 alkyl optionally substituted by hydroxyl or thioalkylene or oxyalkylene,R.sup.4 stands for a 5- or 6- membered aromatic or heteroaromatic ring which can be substituted by one or more hydroxyl, C.sub.1-4 alkyl and/or C.sub.1-4 alkoxy and/or halogen or methylenedioxy and the alkyl group can be unsaturated as well,Q stands for a 6-membered ring which can be partially hydrogenated, andR.sup.1 stands for C.sub.1-4 alkyl.The new compounds are antiarrhythmic agents.Type: GrantFiled: November 27, 1989Date of Patent: July 2, 1991Assignee: Alkaloida Vegyeszeti GyarInventors: Kalman Hideg, Olga H. Hankovszky, Laszlo Frank, Ilona Bodi, Jozsef Csak
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Patent number: 5028610Abstract: Compounds of formula (I):A--M--B-- (I)(in which: M represents a saturated heterocyclic group having from 5 to 7 ring atoms of which 2 are nitrogen atoms, said group being unsubstituted or being substituted at any of its carbon atoms by C.sub.1 -C.sub.6 alkyl and/or oxo substituents: A represents a halo-substituted benzhydryl substituent; and B represents certain specific substituted alkyl groups) and salts thereof are valuable for the treatment and prophylaxis of disorders arising from circulatory problems, especially those affecting the brain. They may be prepared by reacting a compound of formula A--M--H with a halo or acyloxy derivative corresponding to the alkyl substituent B which it is desired to introduce.Type: GrantFiled: March 14, 1988Date of Patent: July 2, 1991Assignee: Sankyo Company LimitedInventors: Koichi Hirai, Yuji Iwano, Katsumi Fujimoto, Yoshiki Matsui
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Patent number: 5019576Abstract: This invention relates to piperazine derivatives of the general formula I ##STR1## wherein --(CH.sub.2).sub.n -- represents a straight or branched chain alkyl group having from n=1 to n=20 carbon atoms, and R represents a hydrogen atom, a branched alkyl group, a cycloalkyl group having from 5 to 10 carbon atoms, a phenyl group, optionally substituted by one or several chlorine atoms, methyl or methoxy groups, or straight or branched chain alkenyl groups having from 3 to 11 carbon atoms, to a preparation process of said compounds and to therapeutic compositions containing them as an active ingredient.Type: GrantFiled: April 9, 1990Date of Patent: May 28, 1991Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Braquet, Eduardo Pirotzky, Jean-Jacques Godfroid, Francoise Heymans
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Patent number: 5008266Abstract: 4(3H)-Quinazolinone derivative of formula (I) are provided. ##STR1## wherein R.sub.1 is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group, an aryl group, a substituted aryl group, or an aralkyl group; R.sub.2 is a C.sub.1 -C.sub.6 alkylamino group, a phenyl group, a substituted phenyl group, or a 5- or 6-membered heterocyclic group containing one or more N, O or S as a hetero atom or atoms, said heterocyclic group optionally being substituted or fused with a benzene ring; n is 1 or 2; or R.sub.2 represents a geranyl group or a dipyridylmethyl group together with the group --(CH.sub.2).sub.n --; and X is a hydrogen atom, a C.sub.1 -C.sub.6 alkyl group or a halogen atom, and pharmaceutically acceptable acid addition salts thereof. They are useful as antiucler agents.Type: GrantFiled: July 26, 1989Date of Patent: April 16, 1991Assignee: Nisshin Flour Milling Co., Ltd.Inventors: Toshihiro Takahashi, Tatsuo Horaguchi, Koichi Nakamaru, Yoshikuni Suzuki
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Patent number: 5008400Abstract: Disclosed are cis, exo- and trans-compounds of the formula I ##STR1## in which n denotes 0,1 or 2, R.sub.1 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl which can optionally by substituted by amino, (C.sub.1 -C.sub.4)-acyl- or bezoylamino, (C.sub.2 -C.sub.6)-alkenyl, (C.sub.5 -C.sub.9)-cycloalkyl, (C.sub.5 -C.sub.9)-cycloalkenyl, (C.sub.5 -C.sub.7)-cycloalkyl-(C.sub.1 -C.sub.4)-alkyl, aryl or partially hydrogenated aryl, which can, in each case, be substituted by (C.sub.1 -C.sub.2)-alkyl, (C.sub.2 -C.sub.2)-alkoxy or halogen, aryl-(C.sub.1 -C.sub.4)-alkyl, /which can be substituted as defined previously in the aryl radical/, a monocyclic or bicyclic sulfur or nitrogen and/or nitrogen heterocyclic radical, or a side chain of naturally occurring aminoacid, R.sub.2 denotes hydrogen, (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.6)-alkenyl or aryl-(C.sub.1 -C.sub.4)-alkyl, Y denotes hydrogen or hydroxyl, Z denotes hydrogen or Y and Z together denote oxygen, X denotes (C.sub.1 -C.sub.6)-alkyl, (C.sub.2 -C.sub.Type: GrantFiled: November 21, 1984Date of Patent: April 16, 1991Assignee: Hoechst AktiengesellschaftInventors: Hansjorg Urbach, Rainer Henning, Volker Teetz, Rolf Geiger, Reinhard Becker, Holger Gaul
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Patent number: 5006528Abstract: A novel carbostyril derivative and salt thereof represented by the formula (1) ##STR1## (wherein R is a group of the formula ##STR2## ((wherein R.sup.1 is a C.sub.1- C.sub.3 alkoxy group)), a group of the formula ##STR3## ((wherein R.sup.2 and R .sup.3 are each, at the same time, a chlorine atom, a bromine atom; and R.sup.4 is a hydrogen atom or a chlorine atom)), 2-methyl-3-nitrophenyl group, 3,5-dichlorophenyl group, or a group of the formula ##STR4## ((wherein R.sup.5 is a chlorine atom or a bromine atom; and R.sup.6 is a methyl group)); the carbon-carbon bond between 3- and 4-position in the carbostyril skeleton is a single or double bond).Type: GrantFiled: October 20, 1989Date of Patent: April 9, 1991Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Yasuo Oshiro, Seiji Sato, Nobuyuki Kurahashi
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Patent number: 5004747Abstract: Therapeutically useful isoquinolinone derivatives of the formula A--X--R.sup.3, wherein A represents a group of the formula: ##STR1## wherein R.sup.1 and R.sup.2 represents cycloalkyl, alkyl, alkenyl or alkynyl optionally substituted by halogen or cycloalkyl, or represents optionally substituted aryl or heteroaryl, R.sup.4 represents hydrogen, halogen, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or heteroaryl, or a group R.sup.6 O-- wherein R.sup.6 represents alkyl, aryl or arylalkyl, X represents ethylene or vinylene, R.sup.3 represents a group of the formula:--Y.sup.1 --CH.sub.2 --CH(OH)--CH.sub.2 --COOR.sup.5wherein Y.sup.1 represents carbonyl, hydroxymethylene or --C(OR).sub.2 -- wherein R represents alkyl or the two R symbols together represent alkylene and R.sup.5 represents hydrogen or optionally substituted alkyl or R.sup.Type: GrantFiled: March 15, 1990Date of Patent: April 2, 1991Assignee: May & Baker LimitedInventors: Michael J. Ashton, Andrew W. Bridge, Robert K. Chambers, Donald I. Dron, Garry Fenton, Neil V. Harris, David J. Lythgoe, Ian M. McFarlane, Christopher G. Newton, David Riddell, Christopher Smith, Keith A. J. Stuttle, Malcolm P. Toft
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Patent number: 4999046Abstract: The present invention relates to novel N-(2-nitrophenyl)-N-pyrimidin-2-ylureas having a herbicidal and plant growth-regulating activity, to agrochemical compositions containing those substances as active ingredients, to the use of the novel ureas for controlling weeds or for regulating plant growth, and to processes for the preparation of the novel compounds. The invention also relates to novel intermediates and to processes for the preparation thereof.The novel compounds correspond to formula I ##STR1## in which R.sup.1 is hydrogen, methyl, fluorine, chlorine or bromine,R.sup.2 is C.sub.1 -C.sub.2 haloalkyl having at least 2 fluorine atoms, andR.sup.3 is C.sub.1 -C.sub.4 alkyl,with the proviso that R.sup.2 is not trifluoromethyl when R.sup.3 is methyl.Type: GrantFiled: April 5, 1989Date of Patent: March 12, 1991Assignee: Ciba-Geigy CorporationInventor: Hermann Rempfler
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Patent number: 4997943Abstract: Compounds of formula (I): ##STR1## (in which R.sup.1 is alkoxy, R is alkyl, haloalkyl, alkylamino, cycloalkyl or optionally substituted phenyl, X is chlorine or fluorine and Y is selected from certain specific heterocycles) have excellent antibacterial activity. They may be prepared by introducing the group represented by Y into the corresponding compound in which Y is replaced by a halogen atom.Type: GrantFiled: March 31, 1987Date of Patent: March 5, 1991Assignees: Sankyo Company Limited, Ube Industries LimitedInventors: Masayuki Iwata, Tomio Kimura, Yoshimi Fujihara, Tetsushi Katsube
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Patent number: 4994463Abstract: Novel tricyclic compounds having a TXA.sub.2 antagonizing activity represented by formula (I): ##STR1## possess a potent antagonizing action against thromboxane A.sub.2 and also an antiallergic and/or antihistaminic activity, and are expected to have preventive and therapeutic effects on ischemic diseases, cerebro-vascular diseases, etc.Type: GrantFiled: December 8, 1988Date of Patent: February 19, 1991Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Etsuo Oshima, Hiroyuki Obase, Akira Karasawa, Kazuhiro Kubo, Ichiro Miki, Akio Ishii, Hidee Ishii, Kenji Ohmori
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Patent number: 4994460Abstract: A series of 5-halopyrimidin-2-ylpiperazinylalkyl derivatives having useful anti-ischemic properties for treatment and prevention of dirorders resulting from brain and/or spinal cord anoxia.Type: GrantFiled: March 30, 1990Date of Patent: February 19, 1991Assignee: Bristol-Myers Squibb Co.Inventors: Pierre Dextraze, Joseph P. Yevich
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Patent number: 4994459Abstract: This invention relates to certain substituted piperazines possessing anti-arrhythmic activity, to pharmaceutical compositions and to methods for production thereof.Type: GrantFiled: December 11, 1989Date of Patent: February 19, 1991Assignee: American Home Products CorporationInventors: John A. Butera, Jehan F. Bagli
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Patent number: 4992552Abstract: Disclosed is a process for preparation of an amino acid, such as phenylalanine, with a high degree of optical purity. The process makes use of the same amino acid as a chiral template.Type: GrantFiled: September 14, 1989Date of Patent: February 12, 1991Assignee: Eastman Kodak CompanyInventors: John C. Hubbs, Charles H. Foster