Chalcogen And -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To Ring Carbons Of The Bicyclo Ring System (e.g., 4-oxo-naphthyridine -3-carboxylic Acid, Etc.) Patents (Class 546/123)
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Patent number: 6277993Abstract: A 5-substituted-3-oxadiazolyl-1,6-naphthyridin-2(1H)-one derivative of the formula (I): wherein Het is oxadiazolyl, R1 is H, lower alkyl, cyclo-lower alkyl, trifluoromethyl, lower alkenyl, lower alkynyl, lower alkoxy, lower alkoxy-lower alkyl, hydroxy-lower alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaromatic group, and R2 is H, lower alkyl, cyclo-lower alkyl, cyclo-lower alkylmethyl, lower alkenyl, cyclo-lower alkenyl, lower alkynyl, substituted or unsubstituted aryl, or substituted or unsubstituted hetero-aromatic group, or a pharmaceutically acceptable acid addition salt thereof, which has high selective affinity to benzodiazepine receptor and is useful particularly as a benzodiazepine inverse agonist, for example, as psychoanaleptic drug or a drug for the treatment of dysmnesia in senile dementia or Alzheimer's disease.Type: GrantFiled: September 1, 2000Date of Patent: August 21, 2001Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Kazunori Ohno, Osamu Odai, Kaoru Masumoto, Kiyoshi Furukawa, Makoto Oka
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Patent number: 6265406Abstract: This invention relates generally to quinolin-2(1H)-ones and derivatives thereof of Formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, pharmaceutical compositions and diagnostic kits comprising the same, methods of using the same for treating viral infection or as assay standards or reagents, and intermediates and processes for making the same.Type: GrantFiled: June 13, 2000Date of Patent: July 24, 2001Assignee: DuPont Pharmaceuticals CompanyInventors: Mona Patel, James D. Rodgers
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Patent number: 6239141Abstract: This invention relates to suspensions for oral administration comprising novel trovafloxacin zwitterionic crystals, and processes for preparing such crystals. This invention further relates to other pharmaceutical compositions comprising these novel crystals, and to methods of using these suspensions, and these novel crystals in such other dosage forms, for treating bacterial infections in mammals.Type: GrantFiled: May 5, 2000Date of Patent: May 29, 2001Assignee: Pfizer Inc.Inventors: Douglas J. M. Allen, Daniel R. Arenson, S. Sonja Sekulic
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Patent number: 6229017Abstract: An improved process for preparing quinolone- and naphthyridonecarboxylic acids and esters thereof from benzoyl chlorides and nicotinoyl chlorides, respectively, in which the reaction carried out in the presence of a non-polar to slightly polar solvent without separation of intermediaries that form during the process.Type: GrantFiled: June 11, 1999Date of Patent: May 8, 2001Assignee: Bayer AktiengesellschaftInventors: Norbert Lui, Hans Panskus, Herbert Müller
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Patent number: 6200971Abstract: The bicyclic heterocyclic compounds are prepared by reaction of correspondingly substituted carboxylic acids with amines, in particular with phenylglycinolamine. The bicyclic heterocyclic compounds according to the invention are suitable as active compounds in medicaments, in particular in medicaments having an antiatherosclerotic action.Type: GrantFiled: October 18, 1999Date of Patent: March 13, 2001Assignee: Bayer AktiengesellschaftInventors: Richard Connell, Siegfried Goldmann, Ulrich Müller, Stefan Lohmer, Hilmar Bischoff, Dirk Denzer, Rudi Gr{umlaut over (u )}tzmann, Stefan Wohlfeil
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Patent number: 6194429Abstract: The present invention relates to alatrofloxacin mesylate substantially free of less polar impurities, to parenteral compositions of alatrofloxacin mesylate and to processes for purifying alatrofloxacin mesylate.Type: GrantFiled: October 27, 1999Date of Patent: February 27, 2001Assignee: Pfizer IncInventors: Robert Mark Guinn, John Francis Lambert, Subramanian Sam Guhan, Stanley Walter Walinsky
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Patent number: 6184380Abstract: A process for preparing a naphthyridone carboxylic acid and its derivatives makes use of side chain intermediates of formulae I and IV herein.Type: GrantFiled: January 25, 1999Date of Patent: February 6, 2001Assignee: Pfizer Inc.Inventors: Charles K. Chiu, Lewin T. Wint
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Patent number: 6174895Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are as defined above, useful in the treatment of respiratory, allergic, rheumatoid, body weight regulation, inflammatory and central nervous system disorders such as asthma, chronic obstructive pulmonary disease, adult respiratory diseases syndrome, toxic shock, fibrosis, pulmonary hypersensitivity, allergic rhinitis, atopic dermatitis, psoriasis, weight control, rheumatoid arthritis, cachexia, Crohn's disease, ulcerative colitis, arthritic conditions and other inflammatory diseases, depression, multi-infarct dementia and AIDS.Type: GrantFiled: August 11, 1999Date of Patent: January 16, 2001Assignee: Pfizer Inc.Inventor: Edward Fox Kleinman
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Patent number: 6143760Abstract: The present invention encompasses structures of the Formula ##STR1## or the pharmaceutically acceptable non-toxic salts thereof wherein: x is hydrogen, halogen, (un)substituted alkyl, (un)substituted alkoxy or amino; andY is (un)substituted alkyl, aryl, or heteroaryl,which compounds are highly selective agonists, antagonists or inverse agonists for GABAa brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAa brain receptors. These compounds are useful in the diagnosis and treatment of anxiety, Down Syndrome, sleep, cognitive and seizure disorders, and overdose with benzodiazepine drugs and for enhancement of alertness.Type: GrantFiled: August 25, 1998Date of Patent: November 7, 2000Assignee: Neurogen CorporationInventors: Pamela A. Albaugh, Robert W. DeSimone, Gang Liu
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Patent number: 6133259Abstract: Amyloid binding compounds which are non-azo derivatives of Chrysamine G, pharmaceutical compositions containing, and methods using such compounds to identify Alzheimer's brain in vivo and to diagnose other pathological conditions characterized by amyloidosis, such as Down's Syndrome are described. Pharmaceutical compositions containing non-azo derivatives of Chrysamine G and methods using such compositions to prevent cell degeneration and amyloid-induced toxicity in amyloidosis associated conditions are also described. Methods using non-azo Chrysamine G derivatives to stain or detect amyloid deposits in biopsy or post-mortem tissue are also described. Methods using non-azo Chrysamine G derivatives to quantify amyloid deposits in homogenates of biopsy and post-mortem tissue are also described.Type: GrantFiled: November 9, 1998Date of Patent: October 17, 2000Assignee: University of PittsburghInventors: William E. Klunk, Jay W. Pettegrew, Chester A. Mathis, Jr.
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Patent number: 6121285Abstract: An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone-derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted with various substituents, represented by formula (I), its salts and hydrates thereof: ##STR1## wherein Q is represented by formula (II) or (IV). ##STR2## Also disclosed is a quinolone derivative where R.sup.Type: GrantFiled: May 21, 1998Date of Patent: September 19, 2000Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Makoto Takemura, Youichi Kimura, Hisashi Takahashi, Kenichi Kimura, Satoru Miyauchi, Hitoshi Ohki, Kazuyuki Sugita, Rie Miyauchi
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Patent number: 6117885Abstract: Compounds of the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, A, B, D and E are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.Type: GrantFiled: February 24, 1994Date of Patent: September 12, 2000Assignee: E. R. Squibb & Sons, Inc.Inventors: Denis Evan Ryono, John Lloyd
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Patent number: 6080756Abstract: The invention relates to a monohydrate polymorph PII.M of a compound of the formula ##STR1## exhibiting the following X-ray powder diffraction pattern______________________________________ Peak No. 1 2 3 4 5 6 7 8 ______________________________________ 2.sub.-- .theta..sub.-- (.degree.) Cu 3.6 7.3 13.7 14.5 17.1 21.) 23.6 26.7 d space 24.2 12.2 6.5 6.1 5.2 4.2 3.8 3.3 ______________________________________The invention also relates to methods of preparing the above compound, pharmaceutical compositions containing the above compound, and methods of treating bacterial infections by administering the above compound.Type: GrantFiled: January 30, 1998Date of Patent: June 27, 2000Assignee: Pfizer Inc.Inventors: Timothy Norris, James J. McGarry, Douglas J. M. Allen
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Patent number: 6071930Abstract: The present invention provides compounds of Formula I: ##STR1## wherein A and R.sub.1 -R.sub.8 are defined herein. The compounds of Formula I inhibit the polymerization of tubulin and possess antimitotic activity. The compounds of Formula I may be useful for the treatment of psoriasis, gout, papiloma, warts, and a variety of tumors.Type: GrantFiled: July 29, 1999Date of Patent: June 6, 2000Assignee: The University of North Carolina at Chapel HillInventors: Kuo-Hsiung Lee, Ke Chen, Sheng-Chu Kuo
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Patent number: 6066647Abstract: The invention relates to a non-hygroscopic polymorph of the following compound ##STR1## and to pharmaceutical compositions containing the above compound, methods of treating bacterial infections by administering the above compound, and to methods of preparing the above compound and related compounds.Type: GrantFiled: January 29, 1998Date of Patent: May 23, 2000Assignee: Pfizer Inc.Inventors: Allen J. M. Douglas, David B. Joseph, Timothy Norris
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Patent number: 6048861Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors .alpha.v.beta.3, .alpha.v.beta.5, and/or .alpha.v.beta.6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.Type: GrantFiled: December 15, 1998Date of Patent: April 11, 2000Assignee: Merck & Co., Inc.Inventors: Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
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Patent number: 6048854Abstract: The present invention relates to a 2,3-diaminopropionic acid derivative of the formula (1): ##STR1## or a pharmaceutically acceptable salt thereof. The compounds of the present invention are useful as a platelet aggregation inhibitor, a cancer metastasis inhibitor, a wound healing agent or a bone resorption inhibitor.Type: GrantFiled: September 25, 1997Date of Patent: April 11, 2000Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Yoshiharu Ikeda, Yasuyuki Ueki, Hisakazu Kishimoto, Toshio Nishihara, Yumiko Kamikawa
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Patent number: 6031102Abstract: N.sub.1 -(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: ##STR1## These compounds have patent antibacterial activities against a wide variety of infectious bacteria and are useful as antibacterial agents by oral or parenteral administration.Type: GrantFiled: April 6, 1998Date of Patent: February 29, 2000Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Isao Hayakawa, Youichi Kimura
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Patent number: 6018054Abstract: The invention relates to intermediate compounds for preparing novel quinolone derivatives- and naphthyridone derivatives which are substituted in the 7-position by a partially hydrogenated isoindolinyl ring, to processes for their preparation and to antibacterial agents and feed additives containing them.Type: GrantFiled: November 26, 1997Date of Patent: January 25, 2000Assignee: Bayer AktiengesellschaftInventors: Thomas Philipps, Stephan Bartel, Andreas Krebs, Uwe Petersen, Thomas Schenke, Klaus-Dieter Bremm, Rainer Endermann, Karl Georg Metzger, Burkhard Mielke
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Patent number: 6017911Abstract: This invention relates to pyridonecarboxylic acid derivatives of the following general formula, esters thereof and salts thereof, as well as pharmaceutical preparations containing them. ##STR1## wherein: R is cycloalkyl which may be substituted by halogen, or the like;X is hydrogen, lower alkyl, amino or the like;Y is hydrogen or halogen;A is nitrogen or a group of the formula C--Z in which Z is lower alkoxy that may be substituted by halogen, or the like;R.sub.1 and R.sub.2 may be the same or different and are each hydrogen or the like;R.sub.3 is hydrogen or lower alkyl;R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8 and R.sub.9 may be the same or different and are each hydrogen, halogen or lower alkyl;m is 0 or 1; andn and p may be the same or different and are each 0 or 1.This invention also relates to bicyclic amine compounds useful as direct intermediates for the synthesis of the above-described pyridonecarboxylic acid derivatives.Type: GrantFiled: August 25, 1998Date of Patent: January 25, 2000Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Nobuhiko Horiuchi, Takenori Yonezawa, Katsumi Chiba, Hiroaki Yoshida
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Patent number: 5998436Abstract: A pyridonecarboxylic acid derivative represented by the following general formula (1): ##STR1## [wherein R.sup.1 represents hydrogen atom or a carboxyl protective group; R.sup.2 represents hydroxyl group, a lower alkoxy group, or a substituted or unsubstituted amino group; R.sup.3 represents hydrogen atom or a halogen atom; R.sup.4 represents hydrogen atom or a halogen atom; R.sup.5 represents a halogen atom or an optionally substituted saturated cyclic amino group; R.sup.6 represents hydrogen atom, a halogen atom, nitro group, or an optionally protected amino group; X, Y and Z may be the same or different and respectively represent nitrogen atom, --CH.dbd. or --CR.sup.7 .dbd. (wherein R.sup.7 represents a lower alkyl group, a halogen atom, or cyano group) (with the proviso that at least one of X, Y and Z represent the nitrogen atom), and W represents nitrogen atom or --CR.sup.8 .dbd. (wherein R.sup.Type: GrantFiled: March 20, 1998Date of Patent: December 7, 1999Assignee: Wakunaga Pharmaceuticals Co., Ltd.Inventors: Akira Yazaki, Yoshiko Niino, Yoshihiro Ohshita, Yuzo Hirao, Hirotaka Amano, Norihiro Hayashi, Yasuhiro Kuramoto
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Patent number: 5990106Abstract: This invention relates to bicyclic amino group-substituted pyridonecarboxylic acid derivatives of the general formulaA--Priesters thereof and salts thereof, wherein: Pri is a pyridonecarboxylic acid residue, and A is a bicyclic amino group represented by the following formula and joined to the 7-position of the pyridonecarboxylic acid or a position equivalent to the 7-position thereof. ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represents a hydrogen atom, a lower alkyl group or an amino-protecting group; R.sub.3 and R.sub.4 may be the same or different and each represents a hydrogen atom, a halogen atom, a cyano group, a hydroxyl group, an oxo group, a lower alkoxy group or a lower alkyl group; and n is an integer of 0 or 1.The above-described pyridonecarboxylic acid derivatives, esters thereof and salts thereof are useful as antibacterial agents.Type: GrantFiled: August 4, 1997Date of Patent: November 23, 1999Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Masato Sakamoto, Katsumi Chiba, Yukio Tominaga, Akira Minami
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Patent number: 5952504Abstract: Novel 4-amino-3-acylnaphthyridine derivatives represented by formula (I), wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 lower alkyl group, C.sub.1 -C.sub.6 lower alkoxy group, C.sub.1 -C.sub.6 lower alkoxyalkyl group, C.sub.3 -C.sub.6 cycloalkyl group, C.sub.3 -C.sub.6 cycloalkyl C.sub.1 -C.sub.6 alkyl group, a or phenyl group which maybe substituted with C.sub.1 -C.sub.6 alkyl group; R.sub.2 is hydrogen, C.sub.1 -C.sub.6 lower alkyl group, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.6 alkylthio group, or a group of the formula: NR.sub.6 R.sub.7 wherein R.sub.6 and R.sub.7, identical to or different from each other, are independently hydrogen or C.sub.1 -C.sub.6 lower alkyl group, or R.sub.6 and R.sub.7 may form together 5-membered or 6-membered cycloalkyl group; R.sub.3 is hydrogen, C.sub.1 -C.sub.6 lower alkyl group, C.sub.1 -C.sub.6 alkoxy group, C.sub.1 -C.sub.6 alkylthio group, an amino group substituted with one or two C.sub.1 -C.sub.6 alkyl groups, halogen, cyano group, C.sub.1 -C.sub.Type: GrantFiled: July 3, 1997Date of Patent: September 14, 1999Assignee: Yungjin Pharmaceutical Company, Ltd.Inventors: Han Yong Yoo, Kae Jong Chung, Man Sik Chang, Sung Gyu Kim, Wahn Soo Choi, Dae Pil Kang, Young Hun Kim, Jang Hoon Paek, Sang Kwon Sohn, Bog Goo Kang, Young Heui Kim, Kwi Hyon Seo
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Patent number: 5945431Abstract: The present invention relates to heterocyclic compounds having antiviral activity. In particular, compounds of formula (I): wherein B, W, X, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and n are as defined herein, are useful in the therapy and prophylaxis of cytomegalovirus (CMV) infection in mammals.Type: GrantFiled: September 4, 1997Date of Patent: August 31, 1999Assignee: Biochem Therapeutics IncorporatedInventors: Haolun Jin, Laval C. Chan, Wei Wang, Tomislav Stefanac, Tarek S. Mansour, Paul Nguyen-Ba, Jean-Francois Lavallee, Guy Falardeau
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Process for preparing derivatives of azabicyclo naphthyridine carboxylic acid comprising a dipeptide
Patent number: 5939550Abstract: A multi-step process for preparing a dipeptide derivative of 7-(6-amino-3-azabicyclo?3.1.0.!hex-3-yl)-6-fluoro-1-(2,4-difluorophenyl)-1 ,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, in the form of a pharmaceutically acceptable acid addition salt is disclosed.Type: GrantFiled: March 11, 1998Date of Patent: August 17, 1999Assignee: Pfizer Inc.Inventors: Tamim F. Braish, Michael J. Castaldi, Harry A. Watson, Jr. -
Patent number: 5935952Abstract: This invention relates to a novel quinolone- or naphthyridone-carboxylic acid derivative or its salt useful as an antibacterial agent, said derivative has a substituent represented by the following formula at the 7 position: ##STR1## wherein preferably R.sup.3 represents at least one member selected from the group consisting of a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl, lower alkoxy or lower alkylthio group, a nitro group, a cyano group, a protected or unprotected hydroxyl group and a protected or unprotected amino group; R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group, a lower alkylidene group and a group forming a cycloalkane ring together with the carbon atom to which R.sup.4 is bonded; and R.sup.5 represents a hydrogen atom or a substituted or unsubstituted lower alkyl or cycloalkyl group.Type: GrantFiled: February 12, 1997Date of Patent: August 10, 1999Assignee: Toyama Chemical Co., LTD.Inventors: Yozo Todo, Kazuya Hayashi, Masahiro Tadahata, Yasuo Watanabe, Hirokazu Narita
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Patent number: 5932587Abstract: The heterocyclic-fused pyridines are prepared by reaction of the corresponding heterocyclic-fused pyridine aldehydes with appropriately substituted Grignard or Wittig reagents. The heterocyclic-fused pyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of dislipidaemia and arteriosclerosis.Type: GrantFiled: June 27, 1997Date of Patent: August 3, 1999Assignee: Bayer AktiengesellschaftInventors: Carsten Schmeck, Matthias Muller-Gliemann, Gunter Schmidt, Arndt Brandes, Rolf Angerbauer, Michael Logers, Klaus-Dieter Bremm, Hilmar Bischoff, Delf Schmidt, Joachim Schuhmacher
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Patent number: 5929240Abstract: This invention relates to novel processes and intermediates for the preparation of pharmaceutically acceptable acid salts, of the formulaType: GrantFiled: October 7, 1996Date of Patent: July 27, 1999Assignee: Pfizer Inc.Inventors: Tamim F. Braish, Darrell E. Fox, Timothy Norris, Peter R. Rose
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Patent number: 5925653Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH or S(O).sub.q where q=0, 1 of 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.Type: GrantFiled: September 6, 1996Date of Patent: July 20, 1999Assignee: Hoechst Schering AgrEvo GmbHInventors: Rainer Preuss, Wolfgang Schaper, Martin Markl, Harald Jakobi, Peter Braun, Werner Knauf, Burkhard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen, Werner Bonin
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Patent number: 5919792Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are .alpha.v.beta.3 antagonists, .alpha.v.beta.5 antagonists or dual .alpha.v.beta.3/.alpha.v.beta.5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.Type: GrantFiled: October 28, 1997Date of Patent: July 6, 1999Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, George D. Hartman, William F. Hoffman, Nathan C. Ihle
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Patent number: 5910498Abstract: The invention provides a pyridonecarboxylic acid derivative of the following general formula (1): ##STR1## wherein R.sup.1 is a hydrogen atom or carboxy protecting group, R.sup.2 is a nitro or substituted or unsubstituted amino group, R.sup.3 is a halogen atom, each of R.sup.4 and R.sup.5, which may be the same or different, is a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group, A is a nitrogen atom or --CX.dbd. wherein X is a hydrogen atom, halogen atom, lower alkyl group or lower alkoxy group, and Z is a halogen atom or a saturated cyclic amino group which may have a substituent, or a salt thereof and an antibacterial agent comprising the same.Type: GrantFiled: July 8, 1997Date of Patent: June 8, 1999Assignee: Wakunaga Seiyaku Kabushiki KaishaInventors: Akira Yazaki, Jiro Yoshida, Yoshiko Niino, Yoshihiro Ohshita, Norihiro Hayashi, Hirotaka Amano, Yuzo Hirao, Yasuhiro Kuramoto
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Patent number: 5869670Abstract: The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to 7-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4 -oxo-1,4-dihydro-1,8-naphthyridine -3-carboxylic acid represent by the following formula: ##STR1## or its isomer.Type: GrantFiled: March 27, 1998Date of Patent: February 9, 1999Assignee: LG Chemical Ltd.Inventors: Chang Yong Hong, Young Kwan Kim, Se Ho Kim, Jay Hyok Chang, Hoon Choi, Do Hyun Nam, Ae Ri Kim, Jin Hwa Lee, Ki Sook Park
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Patent number: 5866587Abstract: Compound of formula (I): ##STR1## in which: m, n, which are identical or different, represent 0, 1 or 2,R.sub.1, R.sub.2, which are identical or different, represent hydrogen, optionally substituted alkyl, aryl, or form with the carbon atom carrying them carbonyl or (C.sub.3 -C.sub.7)cycloalkyl,R.sub.3 represents hydrogen, alkyl, hydroxyl or aryl,R.sub.4 represents any of the groups as defined in the description,X represents --SO.sub.2 --, --CO-- or --SO.sub.2 NH--,R.sub.5 represents optionally substituted alkyl, (C.sub.3 -C.sub.7)cycloalkyl, aryl or heterocyclic,A represents an aryl ring or a heterocycle,its isomers as well as its addition salts with a pharmaceutically acceptable acid or base and medicinal products containing the same are useful as metalloprotease inhibitors.Type: GrantFiled: April 25, 1997Date of Patent: February 2, 1999Assignee: Adir Et CompagnieInventors: Guillaume de Nanteuil, Joseph Paladino, Georges Remond, Ghanem Atassi, Alain Pierre, Gordon Tucker, Jacqueline Bonnet, Massimo Sabatini
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Patent number: 5854257Abstract: Compounds of formula I ##STR1## including pharmaceutically acceptable salts thereof in which R.sub.1 represents a phenyl C.sub.1-6 alkyl group (in which the phenyl ring is optionally substituted by one or more of the following: halo, a C.sub.1-4 alkyl group, a C.sub.1-4 alkoxy group, hydroxy or trifluoromethyl) and the alkyl chain is optionally substituted by one or more C.sub.1-2 alkyl groups; R.sub.2 represents a C.sub.2-6 alkoxycarbonyl group; and R.sub.3 represents hydrogen or halo are disclosed, which are antirheumatic agents and are useful as modulators of cytokine synthesis, immunomodulatory agents, antiinflammatory agents and anti-allergic agents. Compositions containing these compounds and processes to make these compounds are also disclosed.Type: GrantFiled: April 24, 1997Date of Patent: December 29, 1998Assignee: Knoll AktiengesellschaftInventors: Bernard John Armitage, Bruce William Leslie
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Patent number: 5837705Abstract: The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2" or R2"' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2" is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2"' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.Type: GrantFiled: April 1, 1996Date of Patent: November 17, 1998Assignee: Zeneca LimitedInventors: Thomas Michael Bare, James Roy Empfield, Janet Marie Forst, Keith John Herzog, Richard Bruce Sparks
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Patent number: 5817670Abstract: 1,8-Naphthyridine derivatives represented by the following general formula (I), salts thereof, hydrates thereof and solvates thereof. ##STR1## They have an activity to inhibit type IV phosphodiesterase and are useful as agents for the prevention and treatment of respiratory diseases, inflammatory diseases accompanying organ transplantation, systemic or local arthropathy, proliferative diseases, micturition-related diseases and diseases in which tumor necrosis factor (TNF) and other cytokine (IL-1, IL-6 or the like) are concerned.Type: GrantFiled: January 30, 1997Date of Patent: October 6, 1998Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kazuhisa Takayama, Masahiro Iwata, Yoshinori Okamoto, Motonori Aoki, Akira Niwa, Yasuo Isomura
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Patent number: 5817669Abstract: This invention relates to pyridone-carboxylic acid derivatives of the following formula or salts thereof: ##STR1## wherein R.sub.1 is a hydrogen atom, a halogen atom, etc.,R.sub.2 is a carboxyl group etc.,R.sub.3 is a hydrogen atom etc.,A is a nitrogen atom or CH,m is 1 or 2, andY is an eliminable group or a group having the following formula: ##STR2## wherein R.sub.4 is a hydrogen atom or a lower alkyl group,Z is a hydrogen atom, a lower alkyl group, etc.,R.sub.5 is a hydrogen atom, a lower alkyl group, etc.,n is 0 or 1, andp is 1, 2, 3 or 4and to processes for the preparation of these compounds, and further to anti-tumor agents which contain the above compounds as effective ingredients.Type: GrantFiled: December 13, 1996Date of Patent: October 6, 1998Assignee: Dainippon Pharmaceutical Co., Ltd.Inventors: Kyoji Tomita, Katsumi Chiba, Shigeki Kashimoto, Koh-ichiro Shibamori, Yasunori Tsuzuki
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Patent number: 5817820Abstract: The present invention relates to optical isomers of quinoline compounds of Formula (IA) or Formula (IA'), their pharmaceutically acceptable salts and their intermediates: ##STR1## In the above formulae, A represent nitrogen or ##STR2## in which Y represents hydrogen, halogen such as fluorine or chlorine, lower alkyl or lower alkoxy such as methoxy, or together with R.sub.1 forms --CH.sub.2 CH.sub.2 CH.sub.2 --, CH.sub.2 CH.sub.2 CH(CH.sub.3)--, --OCH.sub.2 CH.sub.2 --, --OCH.sub.2 CH(CH.sub.3)--, --SCH.sub.2 CH.sub.2 -- or --SCH.sub.2 CH(CH.sub.3)--; R.sub.1 is as defined above or represents straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms, a straight chain or cyclic lower alkyl group having 1 to 3 carbon atoms which is substituted with a halogen atom, a phenyl group or a phenyl group substituted with one or two halogen atoms, such as ethyl, cyclopropyl or 2,4-difluorophenyl; R.sub.Type: GrantFiled: July 20, 1994Date of Patent: October 6, 1998Assignee: Korea Research Institute of Chemical TechnologyInventors: Wan Joo Kim, Tae Ho Park, Moon Hwan Kim, Jewn Giew Park, Bong Jin Kim
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Patent number: 5811433Abstract: The invention relates to novel 1,6-naphthyridonecarboxylic acid derivatives, to processes for their preparation, to antibacterial compositions and feed additives in which they are present, and to novel intermediates for the preparation of these active compounds.Type: GrantFiled: June 19, 1997Date of Patent: September 22, 1998Assignee: Bayer AktiengesellschaftInventors: Stephan Bartel, Klaus Grohe, Hermann Hagemann, Klaus-Dieter Bremm, Rainer Endermann
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Patent number: 5807853Abstract: A method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells is disclosed. The method comprises the administration of a compound of Formula 1.0: ##STR1## to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Novel compounds of formulas 5.0, 5.1 and 5.2, wherein R is --C(R.sup.20)(R.sup.21)(R.sup.46), and 5.3, 5.3A and 5.3B, wherein R is --N(R.sup.25)(R.sup.48), are disclosed. Also disclosed are processes for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3. Further disclosed are novel compounds which are intermediates in the process for making 3-substituted compounds of Formulas 5.0, 5.1, 5.2 and 5.3.Type: GrantFiled: May 25, 1995Date of Patent: September 15, 1998Assignee: Schering CorporationInventors: W. Robert Bishop, Ronald J. Doll, Alan K. Mallams, F. George Njoroge, Joanne M. Petrin, John J. Piwinski, Ronald L. Wolin, Arthur G. Taveras, Stacy W. Remiszewski
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Patent number: 5808076Abstract: The present invention relates to the preparation of orally administrable formulations of quinolone- or naphthyridonecarboxylic acids by mixing quinolone- or naphthyridonecarboxylic acids as such or in the form of their water-soluble salts or derivatives, preferably in the form of their aqueous salt solutions, with embonic acid as such or in the form of its water-soluble salts or derivatives, preferably in the form of its aqueous salt solutions, in the presence of an excipient, optionally in the presence of auxiliaries, when using dry mixtures in the presence of water, and optionally converting the mixture obtained into further ready-to-use forms.Type: GrantFiled: December 6, 1996Date of Patent: September 15, 1998Assignee: Bayer AktiengesellschaftInventors: Oliver Vetter, Reinhold Lohr, Matthias Kuhn, Hubert Rast, Martin Scheer, Ernst Heinen, Francisco Cabrera
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Patent number: 5801183Abstract: Methods of treating or preventing neuronal loss associated with stroke, ischemia, CNS trauma, hypoglycemia and surgery, as well as treating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's syndrome, treating or preventing adverse consequences of the hyperactivity of the excitatory amino acids, as well as treating anxiety, chronic pain, convulsions, inducing anesthesia, and treating or preventing opiate tolerance are disclosed by administering to an animal in need of such treatment or prevention a substituted or unsubstituted pyridine and pyridine (N-oxide) analogs of 4-hydroxydihydroquinolones, tetrahydroquinoline-trione-oximes and quinoxalones, tautomers and pharmaceutically acceptable salts thereof, which have high binding to the glycine receptor.Type: GrantFiled: June 6, 1995Date of Patent: September 1, 1998Assignees: State of Oregon, Acting by and Through the Oregon State Board of Higher Education, Acting for and on Behalf of the Oregon Health Sciences University and the University of Oregon, Cocensys, Inc.Inventors: John F. W. Keana, Sui Xiong Cai, Zhang-Lin Zhou, James M. Navratil
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Patent number: 5783708Abstract: The invention relates to new intermediate compounds for preparation of new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by an unsatured bicyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.Type: GrantFiled: August 18, 1997Date of Patent: July 21, 1998Assignee: Bayer AktiengesellschaftInventors: Uwe Petersen, Michael Ruther, Thomas Schenke, Klaus Dieter Bremm, Rainer Endermann
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Patent number: 5776944Abstract: The present invention relates to a novel quinolone compound having an excellent antibacterial activity. More specifically, the present invention relates to 7-(4-aminomethyl-3-methyloxyiminopyrrolidin-1-yl)-1-cyclopropyl-6-fluoro-4 -oxo-1, 4-dihydro-1,8-naphthyridine-3-carboxylic acid represent by the following formula: ##STR1## or its isomer.Type: GrantFiled: April 4, 1997Date of Patent: July 7, 1998Assignee: LG Chemical Ltd.Inventors: Chang Yong Hong, Young Kwan Kim, Se Ho Kim, Jay Hyok Chang, Hoon Choi, Do Hyun Nam, Ae Ri Kim, Jin Hwa Lee, Ki Sook Park
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Patent number: 5770597Abstract: The present invention relates to quinoline derivatives substituted in the 7-position by a trans-2,8-diazabicyclo?4.3.0!nonan-8-yl group having a broad antibacterial spectrum and to processes for preparing the same.Type: GrantFiled: October 11, 1995Date of Patent: June 23, 1998Assignees: Korea Research Institute of Chemical Technology, Smithkline Beecham P.L.C.Inventors: Wan Joo Kim, Tae Ho Park, Moon Hwan Kim, Bong Jin Kim, Neil D. Pearson
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Patent number: 5767127Abstract: N.sub.1 -(1,2-cis-2-halogenocydopropyl)-substituted pyridonecarboxylic acid derivatives represented by formula (I) and the salts thereof are disclosed. These compounds have patent antibacterial activities against a wide variety of infectious bacteria, and are useful as antibacterial agents by oral or parenteral administration.Type: GrantFiled: June 7, 1995Date of Patent: June 16, 1998Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Isao Hayakawa, Youichi Kimura
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Patent number: 5763454Abstract: The anhydrate of 7-(?1.alpha.,5.alpha.,6.alpha.!-6-amino-3-azabicyclo?3.1.0!hex-3-yl)-6-flu oro-1-(2,4-difluorophenyl)-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid, methanesulfonic acid salt has advantageous stability for formulation as an antibacterial agent.Type: GrantFiled: May 21, 1997Date of Patent: June 9, 1998Assignee: Pfizer, Inc.Inventors: Lynne A. Handanyan, Thomas A. Morris, Robert L. Hendrickson, Phillip J. Johnson, Timothy Norris
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Patent number: 5753669Abstract: The invention relates to new quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in the 7-position by a tricyclic amine radical, their salts, processes for their preparation and antibacterial compositions comprising these compounds.Type: GrantFiled: December 12, 1996Date of Patent: May 19, 1998Assignee: Bayer AktiengesellschaftInventors: Uwe Peterson, Thomas Schenke, Thomas Jaetsch, Stephan Bartel, Klaus Dieter Bremm, Rainer Endermann, Karl Georg Metzger
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Patent number: 5750532Abstract: The disclosed invention is compounds represented by the formula ##STR1## and pharmacetically acceptable acid salts thereof, wherein each Z is independently tetiary butyl, phenyl, naphthyl or adamantyl; substituted phenyl, wherein the substituents are one or more of halogen, lower alkoxy, phenoxy, nitrile, nitro, phenylsulfonyl, loweralkyl-sulfonyl, oxazol-2-yl, lower alkanoyl, benzoyl, lower alkoxycarbonyl, lower alkyl, lower alkylthio, phenyl, phenylaminothiocarbonyl, or lower alkylaminothiocarbonyl, hydroxyiminoloweralkyl hydroxyloweralkyl or carbonyl; or 4 or 6 membered unsubstituted or substituted heterocyclic ring containing at least one nitrogen with the remaining member of the ring being at least one carbon, and optionally sulfur or oxygen,X and Y are each independently a bond, ##STR2## each Q is independently a divalent substituted or unsubstituted, straight or branched chain lower alkanediyl, lower alkanediyl-cycloalkanediyl-lower alkanediyl, lower alkenediyl, lower alkynediyl, phenylene, dihydrofuraType: GrantFiled: May 30, 1995Date of Patent: May 12, 1998Assignee: Schering CorporationInventors: Viyyoor M. Girijavallabhan, Ashit K. Ganguly, Patrick A. Pinto, Richard W. Versace
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Patent number: RE37029Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.Type: GrantFiled: November 5, 1998Date of Patent: January 23, 2001Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Edward J. Glamkowski, Yulin Chiang, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegler