Nitrogen Attached Directly Or Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/550)
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Patent number: 5696273Abstract: The invention relates to the use of cucurbitine or extracts of Cucurbitaceae pips for the preparation of a cosmetic or pharmaceutical, in particular dermatological, composition having antiallergic activity, or for the preparation of cosmetic or pharmaceutical compositions having a reduced risk of being allergenic.Type: GrantFiled: June 7, 1995Date of Patent: December 9, 1997Assignee: Parfums Christian DiorInventors: Patrice Andre, Valerie Thiery, Gerald Guillaumet
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Patent number: 5693630Abstract: Compounds of the general formula ##STR1## or pharmaceutically acceptable salts thereof, wherein Z is a saturated or unsaturated 3 to 6 carbon chain,m is 2 or 3,R.sub.1 is a hydrogen atom, or a straight or branched C.sub.1-4 alkyl group,R.sub.2, R.sub.3 and R.sub.13 are situated in the ortho, meta, or para position of the phenyl ring and are the same or different and selected from the following groups: H, OH, OR.sub.14, halogen, CO.sub.2 R.sub.9, CN, CF.sub.3, NO.sub.2, NH.sub.2, COCH.sub.3,OSO.sub.2 CF.sub.3,OSO.sub.2 CH.sub.3,CONR.sub.10 R.sub.11, OCOR.sub.12, whereinR.sub.9, R.sub.12 and R.sub.14 is a straight or branched C.sub.1-4 alkyl group,R.sub.10 and R.sub.11 are the same or different and represents hydrogen or a straight or branched C.sub.1-6 alkyl group,R is 1) ##STR2## processes for their preparation, pharmaceutical preparations containing them and the use of the compounds in the treatment psychiatric disorders.Type: GrantFiled: October 26, 1994Date of Patent: December 2, 1997Assignee: Astra AktiebolagInventors: Stefan Bengtsson, Sven Hellberg, Nina Mohell, Lian Zhang, Gerd Hallnemo, David Jackson, Bengt Ulff
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Patent number: 5674894Abstract: The current invention discloses novel amidine derivatives with nitric oxide donating property that can inhibit platelet aggregation and promote vasodilation in a single compound.Type: GrantFiled: May 15, 1995Date of Patent: October 7, 1997Assignee: G.D. Searle & Co.Inventors: Mark G. Currie, Foe S. Tjoeng, Mark E. Zupec
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Patent number: 5672598Abstract: The present invention relates to compounds that exhibit inhibitory activity against matrix metalloproteases ("MMPs"). Because MMPs are known to play a role in tissue degradation, the compounds of the present invention may be useful in preventing or treating diseases associated with excess MMP activity. In particular, the compounds have a structure according to Formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are various substituents as described in the specification; and Q is an alkyl chain, an alkenyl chain, a heteroalkyl chain, or a heteroalkenyl chain, wherein said chain has 2, 3, or 4 chain atoms and is unsubstituted or substituted with one or more alkyl moieties; or a pharmaceutically-acceptable salt, or biohydrolyzable alkoxyamide, acyloxyamide, or imide thereof. Preferred are those compounds where Q is an alkyl chain having 2, 3 or 4 chain atoms.Type: GrantFiled: March 21, 1995Date of Patent: September 30, 1997Assignee: The Procter & Gamble CompanyInventors: Biswanath De, Christopher Thomas Wahl, Michael George Natchus, Menyan Cheng
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Patent number: 5660598Abstract: A dye of Formula (1): ##STR1## wherein: D is a group of Formula (2): ##STR2## or a group of Formula (3): ##STR3## or a group of Formula (4): ##STR4## The variables are defined in the specification. The dyes and dye mixtures produce blue to green shades on synthetic textile materials such as polyester which have good build up and good light- and wet-fastness.Type: GrantFiled: May 3, 1995Date of Patent: August 26, 1997Assignee: Zeneca LimitedInventors: Denise Cavanagh, Mark Robert James, Barry Huston Meyrick, Paul Wight
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Patent number: 5637731Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.Type: GrantFiled: April 30, 1996Date of Patent: June 10, 1997Assignee: American Home Products CorporationInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
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Patent number: 5627182Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.Type: GrantFiled: July 25, 1996Date of Patent: May 6, 1997Assignee: Ciba Geigy CorporationInventors: Richard G oschke, J urgen K. Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim C. Cohen, Peter Herold
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Patent number: 5618945Abstract: The invention relates to a novel process for the sulfinylation of heterocyclic compounds, which comprises reacting:a compound of the formula RS(O)X, in which R is a linear or branched alkyl group having from 1 to 4 carbon atoms, which is substituted with one or more identical or different halogen atoms and X is a halogen atom, the hydroxyl group or one of the salts thereof, a group --NR.sub.2 R.sub.3, R.sub.2 and R.sub.Type: GrantFiled: February 22, 1995Date of Patent: April 8, 1997Assignee: Rhone-Poulenc AgrochimieInventors: Michel Casado, Pierre Le Roy, Virginie Pevfre
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Patent number: 5605925Abstract: There are disclosed 1-aminoacetamidopyrroles and 1-amino-2-(substituted)pyrroles and related compounds of the formula ##STR1## wherein all substituents are defined herein, which are useful as glycine partial agonists and for the enhancement of learning and memory and for the treatment of memory dysfunctions associated with neurodegenerative disorders and are thus indicated in the treatment of Alzheimer's disease and other senile dementias.Type: GrantFiled: November 7, 1994Date of Patent: February 25, 1997Assignee: Hoechst Marion Roussel, Inc.Inventors: Lawrence L. Martin, Raymond W. Kosley, Jr., Denise M. Flanagan, Gert U. Kuerzel, Peter A. Nemoto, David G. Wettlaufer
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Patent number: 5599994Abstract: The present invention relates to a method of forming a 1,3-diamino-3-substituted-2-propanol chemical intermediate from which various chemicals, such as selected protease-inhibitors and other drugs, as well as polymers, can be synthesized.The method includes contacting a nitromethyl amino acid compound with at least one reducing agent to form the 1,3-diamino-3-substituted-2-propanol chemical intermediate.Type: GrantFiled: June 7, 1995Date of Patent: February 4, 1997Assignee: Pharm-Eco Laboratories, Inc.Inventors: Biman Pal, Siya Ram, Yesh P. Sachdeva, Jaechul Shim, Salah A. Zahr, Emile Al-Farhan, Richard L. Gabriel
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Patent number: 5591769Abstract: The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.Type: GrantFiled: June 1, 1995Date of Patent: January 7, 1997Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Volkhard Austel, Helmut Pieper, Wolfgang Eisert, Thomas Mueller, Johannes Weisenberger, Guenter Linz, Gerd Krueger
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Patent number: 5591856Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.Type: GrantFiled: January 10, 1995Date of Patent: January 7, 1997Assignee: Hoechst Roussel Pharmaceuticals Inc.Inventors: David G. Wettlaufer, Peter A. Nemoto
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Patent number: 5591846Abstract: New nonionic radiographic contrast agents having the formula ##STR1## wherein Y is a single bond, ##STR2## R.sub.1, R.sub.1 ' and R.sub.2 are the same or different and are hydrogen, alkyl or hydroxyalkyl.Hydroxyalkyl refers to such alkyl groups having 1 or more hydroxy groups. Preferred hydroxyalkyl groups include: ##STR3## R.sub.3 and R.sub.4 are the same or different and are hydrogen, methyl or --CH.sub.2 CH.sub.2 OH; R.sub.5 is hydrogen, alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH or OH and R.sub.6 is alkyl, --CH.sub.2 CH.sub.2 OH, CH.sub.2 OH, OH or hydrogen and may be the same or different than R.sub.5 and m is zero or one, with the proviso that no methylene or methine carbon atom of the heterocyclic ring is attached to both a nitrogen and an oxygen atom with the additional proviso that when Y is a single bond, m is not zero. These new contrast agents are water soluble and have desirable low osmolality and anticoagulant properties.Type: GrantFiled: October 27, 1993Date of Patent: January 7, 1997Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Thangavel Arunchalam, Edmund R. Marinelli, Radhakrishna K. Pillai
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Patent number: 5576447Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.Type: GrantFiled: June 5, 1995Date of Patent: November 19, 1996Assignee: G. D. Searle & Co.Inventors: Norman A. Abood, Daniel L. Flynn, Scott A. Laneman, Roger Nosal, Lori A. Schretzman
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Patent number: 5576293Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 29, 1994Date of Patent: November 19, 1996Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Victor M. Garsky, Elizabeth A. Giuliani, Robert P. Gomez, Samuel L. Graham, Gerald E. Stokker, Catherine M. Wiscount
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Patent number: 5571832Abstract: Compounds comprising a pyrrolidinyl ring are disclosed for use in the treatment of cerebral ischemia.Type: GrantFiled: June 20, 1994Date of Patent: November 5, 1996Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Brian R. de Costa, Wayne D. Bowen, Xiao-Shu He, Lilian Radesca, Kenner C. Rice
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Patent number: 5563168Abstract: O-Benzyloxime ethers of the formula I ##STR1## where 5 X is substituted or unsubstituted CH.sub.2, NOalkylY isO, S, NR.sup.5R.sup.1, R.sup.2, R.sup.5 are H, alkylZ.sup.1, Z.sup.2 are H, halogen, methyl, methoxy, cyanoR.sup.3, R.sup.4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl,N(R.sup.6).sub.2, where R.sup.6 is H, alkyl, substituted or unsubstituted phenyl,--CO--N(R.sup.7).sub.2, where R.sup.Type: GrantFiled: June 16, 1995Date of Patent: October 8, 1996Assignee: BASF AktiengesellschaftInventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 5563250Abstract: The present invention provides cleavable conjugates whose linkers contain a labile bond that is cleavable under a variety of mild conditions, including weakly acidic. Since the agent may be bonded directly to the linker, cleavage can result in release of native agent. The invention also provides methods for producing cleavable conjugates. Preferred agents include drugs, toxins, biological response modifiers, radiodiagnostic compounds, radiotherapeutic compounds, and derivatives thereof. The targeting molecule employed in the invention may be an intact molecule, a fragment thereof, or a functional equivalent thereof. In a particularly preferred embodiment, the targeting molecule is a monoclonal antibody directed towards a tumor-associated antigen in man. The invention further provides methods for delivering to the cytoplasm of a target cell an agent free of its targeting molecule carrier.Type: GrantFiled: May 13, 1994Date of Patent: October 8, 1996Assignee: NeoRx CorporationInventors: Mark D. Hylarides, Ananthachari Srinivasan, Jeffrey N. Fitzner, Vivekananda M. Vrudhula
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Patent number: 5559111Abstract: .delta.-Amino-.gamma.-hydroxy-.omega.-aryl-alkanoic acid amides of formula I ##STR1## and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive medicinal active ingredients.Type: GrantFiled: April 4, 1995Date of Patent: September 24, 1996Assignee: Ciba-Geigy CorporationInventors: Richard G oschke, J urgen K. Maibaum, Walter Schilling, Stefan Stutz, Pascal Rigollier, Yasuchika Yamaguchi, Nissim C. Cohen, Peter Herold
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Patent number: 5554768Abstract: The present invention relates to succinimides of the formula I ##STR1## in which R.sup.1 and R.sup.2, independently of one another, are hydrogen, C.sub.1 -C.sub.24 -alkyl, C.sub.2 -C.sub.24 -alkenyl, C.sub.6 -C.sub.12 -cycloalkyl, C.sub.6 -C.sub.12 -cycloalkenyl, C.sub.6 -C.sub.12 -aryl, C.sub.1 -C.sub.24 -alkoxy, C.sub.1 -C.sub.24 -acyl, C.sub.1 -C.sub.24 -acyloxy, a hydroxyl, amino or sulfo group or a C.sub.1 -C.sub.24 -dialkylamino, C.sub.1 -C.sub.24 -acylamino, C.sub.1 -C.sub.24 -alkylsulfato, C.sub.1 -C.sub.24 -alkylsulfonato, C.sub.1 -C.sub.24 -alkylsulfito, C.sub.1 -C.sub.24 -alkylsulfinyl or C.sub.1 -C.sub.24 -alkoxycarbonyl radical, andR.sup.3 is a polyhydroxyalkyl radical of the formula ##STR2## in which R.sup.4 is --(CHOR.sup.7).sub.n --H,R.sup.5 is --(CHOR.sup.7).sub.m --H,R.sup.6 is --(CHOR.sup.7).sub.o --H where n+m+o is 2-6, andR.sup.7 is H or a carbohydrate attached in the form of a glycoside from the series comprising reducing sugars, a process for their preparation and their use.Type: GrantFiled: May 25, 1994Date of Patent: September 10, 1996Assignee: Hoechst AktiengesellschaftInventors: Reinhard D onges, Rudolf Ehrler, Rainer Helwerth
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Patent number: 5550257Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.Type: GrantFiled: February 22, 1995Date of Patent: August 27, 1996Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
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Patent number: 5547979Abstract: Derivatives of 2-pyrrolidinones are described which inhibit the production of TNF and are useful in the treatment of disease states mediated or exacerbated by TNF production.Type: GrantFiled: April 19, 1995Date of Patent: August 20, 1996Assignee: SmithKline BeechamInventors: Siegfried B. Christensen, IV, Klaus M. Esser, Philip L. Simon
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Patent number: 5541343Abstract: The invention relates to cyclic imino compounds which have, inter alia, valuable pharmacological properties, especially inhibitory effects on cell aggregation, pharmaceutical compositions which contain these compounds and processes for preparing them.Type: GrantFiled: December 28, 1994Date of Patent: July 30, 1996Assignee: Karl Thomae GmbHInventors: Frank Himmelsbach, Volkhard Austel, Helmut Pieper, Wolfgang Eisert, Thomas Mueller, Johannes Weisenberger, Guenter Linz, Gerd Krueger
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Patent number: 5527926Abstract: In accordance with the present invention a novel method and composition for using nonionic contrast media to reduce the risk of clot formation in a diagnostic procedure is disclosed. Novel compositions for such method are also disclosed. The present method comprises employing a triiodinated phenyl contrast agent having a heterocyclic group or a dimeric triiodinated phenyl contrast agent having one or more heterocyclic groups.Type: GrantFiled: June 6, 1995Date of Patent: June 18, 1996Assignee: Bracco International B.V.Inventors: Ramachandran S. Ranganathan, Radhakrishna K. Pillai
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Patent number: 5523415Abstract: An antibacterial aminooxypyrrolidinylthiocarbapenem I, its production from the corresponding carbapenem V and thiol VI, its pharmaceutical formulation, and its use for combating bacteria are presented. ##STR1## (wherein R is optionally substituted amino; R.sup.1 is hydrogen or 1C to 5C alkyl; R.sup.2 is hydrogen or a conventional hydroxy protective group; R.sup.3 is hydrogen or an imino protective group or imino substituent; R.sup.4 is 1C to 5C alkylene; and R.sup.5 is hydrogen or a conventional carboxy protective group; X is a leaving group; R.sup.6 is hydrogen or a thiol protective group; and wavy lines each shows a bond in R or S configuration).Type: GrantFiled: July 12, 1994Date of Patent: June 4, 1996Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Yuji Sendo, Makoto Kii
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Patent number: 5523315Abstract: Disclosed herein are compounds of the formula:A--N(R.sup.1)C(O)CH.sub.2 CHR.sup.2 C(O)--Bwherein A is various oxygen-bearing radicals; for example, HO--CH(R.sup.3)CH.sub.2 wherein R.sup.3 is, inter alia, hydrogen, lower alkyl, lower cycloalkyl or phenyl; or HO--CR.sup.5 (R.sup.6)CH.sub.2 wherein each of R.sup.5 and R.sup.6 is lower alkyl, or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form a 1,1-(lower cycloalkanediyl); R.sup.1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R.sup.2 is, for example, cyclo-alkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state mimic, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.Type: GrantFiled: September 20, 1993Date of Patent: June 4, 1996Assignee: Bio-Mega/Boehringer Ingelheim Research Inc.Inventors: Paul C. Anderson, Teddy Halmos, Grace L. Jung, Marc-Andre Poupart, Bruno Simoneau
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Patent number: 5514694Abstract: A novel class of peptide .alpha.-ketoamides useful for selectively inhibiting serine proteases, selectively inhibiting cysteine proteases, generally inhibiting all serine proteases, and generally inhibiting all cysteine proteases, having the formula Y--CO--AA.sup.2 --AA.sup.1 --CO--NH--X. Processes for the synthesis of peptidyl .alpha.-ketoamide derivatives.Type: GrantFiled: June 24, 1993Date of Patent: May 7, 1996Assignee: Georgia Tech Research CorpInventors: James C. Powers, Zhaozhao Li, Girish S. Patil, Der-Lun Chu
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Patent number: 5510379Abstract: .beta.-Carboxy sulfonates of the formula ##STR1## wherein R.sub.1 is aryl, R.sub.3 and R.sub.4 are hydrogen or alkyl, Y is -O-, -S-, or -NR.sub.2 -, and R.sub.5 is alkyl or aryl are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT) and are thus useful for treating hypercholesterolemia and atherosclerosis.Type: GrantFiled: December 19, 1994Date of Patent: April 23, 1996Assignee: Warner-Lambert CompanyInventors: Helen T. Lee, Joseph A. Picard, Drago R. Sliskovic
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Patent number: 5489693Abstract: Cyclic imino derivatives of the formula ##STR1## wherein X and R.sub.a to R.sub.g are as defined herein, useful for their inhibitory effects on aggregation, pharmaceutical compositions containing the compounds and processes for preparing them.Type: GrantFiled: April 26, 1993Date of Patent: February 6, 1996Inventors: Guenter Linz, Volkhard Austel, Frank Himmelsbach, Johannes Weisenberger, Thomas Mueller, Helmut Pieper, Elke Seewaldt-Becker
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Patent number: 5468733Abstract: The present invention comprises analogs of the CAAX motif of the protein Ras that is modified by farnesylation in vivo. These CAAX analogs inhibit the farnesylation of Ras. Furthermore, these CAAX analogues differ from those previously described as inhibitors of Ras farnesyl transferase in that they do not have a thiol moiety. The lack of the thiol offers unique advantages in terms of improved pharmacokinetic behavior in animals, prevention of thiol-dependent chemical reactions, such as rapid autoxidation and disulfide formation with endogenous thiols, and reduced systemic toxicity. Further contained in this invention are chemotherapeutic compositions containing these farnesyl transferase inhibitors and methods for their production.Type: GrantFiled: September 30, 1993Date of Patent: November 21, 1995Assignee: Merck & Co., Inc.Inventors: S. Jane deSolms, Elizabeth A. Giuliani, Samuel L. Graham
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Patent number: 5461157Abstract: A process for preparing a 2-(1-pyrrolidinyl)acetamide derivative useful as a cerebral function improving agent is disclosed, comprising reacting a halogenoacetamide derivative with substituted or unsubstituted 2-pyrrolidinone, the halogenoacetamide derivative being prepared by reacting an amine and a halogenoacetyl chloride. High yields of the intermediate compound as well as the final product are attained at low cost.Type: GrantFiled: December 15, 1994Date of Patent: October 24, 1995Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Shinji Kamihara, Tohru Kaneuchi, Keiji Uchiyama, Tatsuya Terada
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Patent number: 5457122Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.Type: GrantFiled: July 13, 1993Date of Patent: October 10, 1995Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Mitoshi Konno, Takahiko Nakae, Nobuyuki Hamanaka
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Patent number: 5451685Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.Type: GrantFiled: July 13, 1994Date of Patent: September 19, 1995Assignee: American Cyanamid CompanyInventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander
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Patent number: 5420293Abstract: The new N-substituted .alpha.-fluoroalkyl-lactams of the general formula ##STR1## in which the substituents and indices have the meaning indicated in the description, exhibit a strong action against pests and can be employed in particular for combating unwanted fungi.Type: GrantFiled: January 11, 1994Date of Patent: May 30, 1995Assignee: Bayer AktiengesellschaftInventors: Michael Negele, Norbert Lui, Bernd Baasner, Gerd Hanssler
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Patent number: 5405845Abstract: Novel (pyrrolidinyl)phenyl carbamates and related compounds, intermediates and processes for the preparation thereof, and methods of relieving memory dysfunction utilizing the carbamates and related compounds, or compositions thereof are disclosed.Type: GrantFiled: May 25, 1994Date of Patent: April 11, 1995Assignee: Hoechst-Roussel Pharmaceuticals Inc.Inventors: David G. Wettlaufer, Peter A. Nemoto
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Patent number: 5378724Abstract: Pesticidal substituted 2-arylpyrroles of the formula ##STR1## in which n represents 0, 1 or 2,Ar represents optionally substituted aryl,R.sup.1 and R.sup.2 independently of one another represent hydrogen or halogen, but at least one of the two radicals R.sup.1 or R.sup.2 represents halogen,R.sup.3 represents hydrogen, halogen or optionally substituted alkyl,X.sup.1 and X.sup.2 independently represent hydrogen or halogen andR.sup.4 represents hydrogen or ##STR2## (R.sup.5 and R.sup.6 having various meanings). The compounds of the formulas ##STR3## are also new.Type: GrantFiled: October 1, 1993Date of Patent: January 3, 1995Assignee: Bayer AktiengesellschaftInventors: Hermann Uhr, Albrecht Marhold, Stefan Bohm, Christoph Erdelen, Ulrike Wachendorff-Neumann, Wilhelm Stendel
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Patent number: 5344940Abstract: Individual stereoisomers of 7-[3-(1-aminoalkyl)-1-pyrrolidinyl]-quinolones and naphthyridones are described, their therapeutic advantages as antibacterial agents, as well as a novel method for the preparation and isolation of such stereoisomers.Type: GrantFiled: June 28, 1993Date of Patent: September 6, 1994Assignee: Warner-Lambert CompanyInventors: John M. Domagala, John S. Kiely, Mel C. Schroeder
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Patent number: 5338860Abstract: The invention relates to new 4-(substituted)amino-3-arylpyrrolinone derivatives of the general formula (I) ##STR1## in which X, Y, Z, n, B, M, L and A are as defined in the description, to a process and new intermediates for their preparation, and to their use as herbicides.Type: GrantFiled: December 4, 1992Date of Patent: August 16, 1994Assignee: Bayer AktiengesellschaftInventors: Bernd Baasner, Reiner Fischer, Arno Widdig, Klaus Lurssen, Hans-Joachim Santel, Robert R. Schmidt
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Patent number: 5314886Abstract: This invention relates to novel N-substituted lactams having the following formula ##STR1## useful in the treatment and prevention of Cholecystokinin (CCK) related disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals.Type: GrantFiled: October 29, 1992Date of Patent: May 24, 1994Assignee: G. D. Searle & Co.Inventors: Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
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Patent number: 5312929Abstract: A herbicidal 2-oxo-3-pyrroline derivative having the formula: ##STR1## wherein X is a hydrogen atom or a halogen atom, Z is an oxygen atom or a group of the formula .dbd.N--OR.sup.1 (wherein R.sup.1 is a hydrogen atom, an alkyl group, a benzyl group or a phenyl group which is substituted by halogen atoms); and R is a hydrogen atom, an alkyl group, a benzyl group, a chloro-substituted benzyl group, a benzylidene methyl group, a group of the formula ##STR2## wherein Y is a hydrogen atom, a halogen atom, an alkyl group, a haloalkyl group or an alkoxy group, and n is an integer of from 1 to 3, or a group of the formula ER.sup.2 wherein E is an oxygen atom, a sulfur atom or a group of the formula >N--R.sup.3, wherein R.sup.3 is a hydrogen atom, an alkyl group or an alkenyl group, and R.sup.Type: GrantFiled: December 23, 1992Date of Patent: May 17, 1994Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Nobuyuki Ohba, Toshihiro Nagata, Akira Takeuchi, Shigehiko Tachikawa, Yasunori Ogawa
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Patent number: 5310902Abstract: Novel alkylenediamine derivatives effectively employable glutamate blockers have the formula (I) or (II): ##STR1## wherein each of R.sup.1 and R.sup.6 is an aliphatic hydrocarbon group, an alicyclic hydrocarbon group, an aryl group, or an aralkyl group; each of R.sup.2 and R.sup.7 is an aliphatic hydrocarbon group, an alkoxy group, an aliphatic hydrocarbon group containing an ester bonding, an aliphatic hydrocarbon group containing an ether bonding, or an aryloxy group; each of R.sup.3, R.sup.4, R.sup.5 R.sup.8, R.sup.9 and R.sup.10 is hydrogen, an alkyl group, an alkoxy group, an acyloxy group, an aryl group, an aralkyl group, hydroxyl, a hydroxylalkyl group, halogen, nitrile, nitro, amino, carbamoyl or alkoxycarbonyl; and each of m and n is an integer of 0-3 (m+n does not exceed 3); k is an integer of 1-4; each of p and i is an integer of 2-13; and each of q and j is an integer of 4-7.Type: GrantFiled: August 7, 1991Date of Patent: May 10, 1994Assignee: Nippon Chemiphar Co., Ltd.Inventors: Mitsuo Masaki, Masaru Satoh, Naoya Moritoh, Koichi Hashimoto, Toshiro Kamishiro, Haruhiko Shinozaki
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Patent number: 5298659Abstract: Azomethines can be prepared by the condensation of cycloalkanones and anilines in the presence of acid homogeneous catalysts while the water of reaction is removed azeotropically, the condensation being carried out in a continuous reaction in a column-like reactor to which a temperature profile is applied, the starting materials being fed in in the low-temperature region, and, of the reaction products, the water of reaction to be removed azeotropically being discharged also in the low-temperature region and the azomethine produced being discharged in the high-temperature region.Type: GrantFiled: January 14, 1993Date of Patent: March 29, 1994Assignee: Bayer AktiengesellschaftInventors: Reinhard Langer, Hans-Josef Buysch, Paul Wagner
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Patent number: 5272170Abstract: The present invention relates to new tetralones having the formula I: ##STR1## wherein: R.sup.1 and R.sup.2 represent hydrogen, halogen, cyano, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, pentafluoroethyl, ethynyl, trimethylsilylethynyl, C.sub.1-4 alkylcarbonylamino being the amino optionally substituted by a C.sub.1-4 alkyl group; R.sup.3 is hydrogen or C.sub.1-4 alkyl, and R.sup.4 is C.sub.1-4 alkyl, or R.sup.3 and R.sup.4 together form a C.sub.2-5 polymethylene chain; either R.sup.5 represents hydroxyl, acetoxy or formyloxy and R.sup.6 and R.sup.7 are both hydrogen, or R.sup.5 together with R.sup.6 form a carbonyl group and R.sup.7 is hydrogen, or R.sup.5 and R.sup.7 together form a bond and R.sup.6 is hydrogen; R.sup.8 is, among others, 1,2-dihydro-2-oxo-1-pyridyl, 2,3-dihydro-1-oxo-1H-isoindol-2-yl, 2-oxo-1-pyrrolidinyl, 2-oxo-1-pyperidinyl. The invention also relates to a procedure for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 22, 1993Date of Patent: December 21, 1993Assignee: J. Uriach & Cia., S.A.Inventors: Carmen Almansa, Carmen Torres, Concepcion Gonzalez, Elena Carceller, Javier Bartroli
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Patent number: 5270339Abstract: There are described a phenoxybenzene derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom; an alkyl group having 1 to 3 carbon atoms; --OR.sup.6 or a halogen atom,R.sup.2 is hydrogen atom, nitro group or amino group,R.sup.3 is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 5 carbon atoms, allyl group, vinyl group or --(CH.sub.2)n.sup.1 R.sup.7R.sup.4 is hydrogen atom, an alkyl group having 1 to 3 carbon atoms or --(CH.sub.2)n.sup.3 R.sup.25R.sup.5 hydrogen atom; an alkyl group having 1 to 3 carbon atoms; or phenyl group,X is ##STR2## wherein Y is oxygen atom or sulfur atom; or --CHR.sup.27 -- and line means a single bond or a double bond provided that n is 2 in case that the line means a single bond and n is 1 in case that the line means a double bond, ora pharmacologically acceptable salt thereof,a cognition enhancer comprising the same as an effective ingredient andan antidepressant comprising the same as an effective ingredient.Type: GrantFiled: December 3, 1992Date of Patent: December 14, 1993Assignee: Kanagafuchi Kagaku Kogyo Kabushiki KaishaInventors: Kozo Yamamoto, Yoshihide Fuse, Hideyuki Kishida, Naoko Yasuhara, Toshiaki Miwa, Ikuo Katsumi, Takayoshi Hidaka
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Patent number: 5256795Abstract: Novel pyrrolidinone derivatives of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, X and m have the meanings defined in the specification, useful as herbicides and nematicides.Type: GrantFiled: July 22, 1992Date of Patent: October 26, 1993Assignee: Bayer AktiengesellschaftInventors: Michael Negele, Bernd Baasner, Heinz-Jurgen Bertram, Jurgen Hartwig
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Patent number: 5256657Abstract: Compounds having the structural formula ##STR1## wherein X is HONH or HO and especially wherein the carbon atom bearing CH.sub.2 R.sup.1 has the R-configuration, the carbon atom bearing CH.sub.2 R.sup.2 has the S-configuration, R.sup.1 is isopropyl, R.sup.2 is 3-indolyl, m is 2, n is 0, p is 2 and R.sup.3 and R.sup.4 taken alone are each methyl or R.sup.3 and R.sup.4 taken together with N are morpholino and pharmaceutically acceptable acid addition salts or solvates or acid addition salts-solvates thereof, which are matrix-metalloprotease inhibitors useful in treatment of disease in which matrix-metalloprotease promoted connective tissue remodelling is a causative factor, for example, rheumatoid arthritis and cancer, and a method of preparation and method of use thereof and methods of preparation of intermediates therefor are disclosed.Type: GrantFiled: August 19, 1991Date of Patent: October 26, 1993Assignee: Sterling Winthrop, Inc.Inventors: Jasbir Singh, Barry A. Morgan, James A. Gainor, Thomas D. Gordon, Robert C. Wahl
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Patent number: 5247084Abstract: Compounds presented by the general formula: ##STR1## [wherein when Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH=CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --OCONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --CONH--SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each of R.sup.2 may be the same group or the different group.Type: GrantFiled: September 26, 1991Date of Patent: September 21, 1993Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Katsuhiro Imaki, Yoshinobu Arai, Hiroyuki Ohno
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Patent number: 5232978Abstract: Novel 1-(2-arylethyl)-pyrrolidines of the formula ##STR1## in which, Ar is a phenyl group which is unsubstituted or monosubstituted by OH, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA or NH--SO.sub.2 --A,R.sup.1 is A,R.sup.2 is a phenyl, naphthyl, thienyl, benzothienyl or pyridyl group which is unsubstituted or mono- or disubstituted by A, Hal, CF.sub.3, OH, OA, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NO.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA, --NH--SO.sub.2 A, --CO--A, --CONH.sub.2, --CONHA, --CONA.sub.2, --CH.sub.2 --CONH.sub.2 and/or --O--CH.sub.2 --CONH.sub.2,R.sup.3 is OH or CH.sub.2 OH,A is alkyl with 1-4 C atoms andHal is F, Cl, Br or I,or a pharmaceutically acceptable salt thereof for use as an analgesic in humans and veterinary medicine.Type: GrantFiled: November 1, 1991Date of Patent: August 3, 1993Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Andrew Barbar, Anton Haase, Hartmut Greiner, Gerd Bartoszyk
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Patent number: 5218124Abstract: There are disclosed compounds of the formulaA(CH.sub.2).sub.n O--BwhereinA is a group having the formula ##STR1## wherein X is --N-- or ##STR2## Z is ##STR3## R.sup.1 is hydrogen, lower alkyl or phenyl; R.sup.2 is hydrogen or lower alkyl; orR.sup.1 and R.sup.2 taken together form a benzene ring, with the proviso that when X is --N--, Z is other than ##STR4## R.sup.3 is hydrogen or lower alkyl; n is 1-2;B is ##STR5## wherein Y is OR.sup.5 or N(OH)R.sup.8 ;R.sup.4 and R.sup.5 are each, independently, hydrogen or lower alkyl;R.sup.6 is hydrogen, halo or nitro;R.sup.7 is ##STR6## R.sup.Type: GrantFiled: June 1, 1992Date of Patent: June 8, 1993Assignee: American Home Products CorporationInventors: Amedeo A. Failli, Anthony F. Kreft, III, John H. Musser, Annette L. Banker, James A. Nelson, Uresh S. Shah, Dennis M. Kubrak
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Patent number: 5214063Abstract: A compound of formula (I): ##STR1## in which R, R.sub.1 and R.sub.2 are as defined in the description. Medicinal product, which is useful in treating disorders related to a dysfunction of GABA.sub.B receptors.Type: GrantFiled: July 28, 1992Date of Patent: May 25, 1993Assignee: Adir et CompagnieInventors: Michel Debaert, Pascal Berthelot, Claude Vaccher