At Least Five Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/254)
-
Patent number: 6156756Abstract: The invention provides new triazolo[4,5-d]pyrimidine compounds, their use as medicaments, compositions containing them and processes for their preparation.Type: GrantFiled: September 30, 1998Date of Patent: December 5, 2000Assignee: AstraZeneca UK LimitedInventors: David Hardern, Brian Springthorpe
-
Patent number: 6156766Abstract: Benzamide compounds of the formula ##STR1## wherein each symbol is defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of this compound and a pharamaceutically acceptable additive, and therapeutic agents for hypertension, therapeutic agents for angina pectoris, therapeutic agent for asthma, therapeutic agents for renal and peripheral circulatory disturbances and inhibitor of cerebral vasospasm, which comprise this compound. The compound of the present invention has strong smooth muscle relaxing action, and shows hypertensive action and cerebral.cndot.coronary vasodilating action like conventional calcium antagonists, as well as long-lasting renal and peripheral circulation improving action.Type: GrantFiled: February 18, 1999Date of Patent: December 5, 2000Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Masafumi Arita, Tadamasa Saitoh, Masanori Minoguchi, Keiji Yamagami, Hiroyuki Satoh
-
Patent number: 6124300Abstract: Novel compounds and pharmaceutical compositions thereof, and methods of using same in treating anxiety, depression, and other psychiatric and neurological disorders. The novel compounds provided by this invention are those of the following formulae: ##STR1## wherein R.sup.1, R.sup.13, X, Y, Z, G and Q are as defined herein.Type: GrantFiled: March 20, 1997Date of Patent: September 26, 2000Assignee: DuPont PharmaceuticalsInventors: Parthasarathi Rajagopalan, Robert John Chorvat, Rajagopal Bakthavatchalam, James Peter Beck, Paul Joseph Gilligan, Richard Eric Olson
-
Patent number: 6110931Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: March 25, 1999Date of Patent: August 29, 2000Assignee: Merck & Co., Inc.Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Jonathan R. Young
-
Patent number: 6107300Abstract: Corticotropin releasing factor (CRF) antagonists of formula I or formula II: ##STR1## and their use in treating anxiety, depression, and other psychiatric and neurological disorders.Type: GrantFiled: March 21, 1997Date of Patent: August 22, 2000Assignee: Dupont PharmaceuticalsInventors: Rajagopal Bakthavatchalam, Argyrios Georgios Arvanitis, James Peter Beck, Gary Avonn Cain, Robert John Chorvat, Paul Joseph Gilligan, Richard Eric Olson
-
Patent number: 6107301Abstract: The present invention provides novel compounds, compounds and pharmaceutical compositions thereof, and methods of using same in the treatment of affective disorders, anxiety, depression, post-traumatic stress disorders, eating disorders, supranuclear palsy, irritable bowel syndrome, immune suppression, Alzheimer's disease, gastrointestinal diseases, anorexia nervosa, drug and alcohol withdrawal symptoms, drug addiction, inflammatory disorders, or fertility problems. The novel compounds provided by this invention are those of formula: ##STR1## wherein R.sup.1, R.sup.3, R.sup.4, R.sup.5, Z, Y, V, X, X', J, K, L, and M are as defined herein.Type: GrantFiled: August 5, 1997Date of Patent: August 22, 2000Assignee: Dupont Pharmaceuticals CompanyInventors: Paul Edward Aldrich, Argyrios Georgios Arvanitis, Rajagopal Bakthavatchalam, James Peter Beck, Robert Scott Cheeseman, Robert John Chorvat, Paul Joseph Gilligan, Carl Nicholas Hodge, Zelda Rakowitz Wasserman
-
Patent number: 6046207Abstract: The present invention relates to a compound of the formula and the pharmaceutically acceptable salts thereof wherein W is a bicyclic heterocyclic ring system. The compounds are .alpha.-1 adrenergic antagonists and are useful in the treatment of BPH; also disclosed are .alpha.-1 antagonist compositions and a method for antagonizing .alpha.-1 adrenoreceptors and treating BPH.Type: GrantFiled: November 26, 1997Date of Patent: April 4, 2000Inventors: Michael D. Meyer, Robert J. Altenbach, Fatima Z. Basha, William A. Carroll, Irene Drizin, James F. Kerwin, Jr., Michael D. Wendt, Anthony R. Haight, Weijiang Zhang
-
Patent number: 6030973Abstract: The present invention relates to novel antidiabetic compounds, their tautomeric forms, their derivatives, their analogues, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. This invention particularly relates to novel azolidinediones of the general formula (I), their analogues, their derivatives, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them.Type: GrantFiled: August 17, 1998Date of Patent: February 29, 2000Assignees: Dr. Reddy's Research Foundation, Reddy-Cheminor, Inc.Inventors: Vidya Bhushan Lohray, Braj Bhushan Lohray, Rao Bheema Paraselli, Rajagopalan Ramanujam, Ranjan Chakrabarti
-
Patent number: 6025366Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.Type: GrantFiled: March 25, 1999Date of Patent: February 15, 2000Assignee: Merck & Co., Inc.Inventors: Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Jonathan R. Young
-
Patent number: 5962684Abstract: A therapeutic method is provided, employing an antiviral compound of the general formula: ##STR1## wherein Z is H, OR' or N(R).sub.2, wherein R' is H, (C.sub.1 -C.sub.4)alkyl, aryl, CHO, (C.sub.1 -C.sub.16)alkanoyl or O.dbd.P(OH).sub.2, Y is CH or N, and X is selected from the group consisting of H, N(R).sub.2, SR, OR' or halogen, wherein R is H, lower(C.sub.1 -C.sub.4)alkyl, aryl or mixtures thereof, and the pharmaceutically acceptable salts thereof.Type: GrantFiled: October 27, 1998Date of Patent: October 5, 1999Assignee: Regents of the University of MinnesotaInventors: Robert Vince, Mei Hua
-
Patent number: 5958926Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NO.sub.n -PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO.sub.2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i.e., nitrosonium (NO.sup.+) or nitroxyl (NO.sup.-), or as the neutral species, nitric oxide (NO.cndot.) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.Type: GrantFiled: September 1, 1998Date of Patent: September 28, 1999Assignee: NitroMed, Inc.Inventors: David S. Garvey, Inigo Saenz de Tejada
-
Patent number: 5929079Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: November 20, 1997Date of Patent: July 27, 1999Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5889006Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula with acetylcholinesterase inhibitors.Type: GrantFiled: August 8, 1996Date of Patent: March 30, 1999Assignee: Schering CorporationInventors: Derek B. Lowe, Wei K. Chang, Joseph A. Kozlowski, Joel G. Berger, Robert McQuade, Allen Barnett, Margaret Sherlock, Wing Tom, Sundeep Dugar, Lian-Yong Chen, John W. Clader, Samuel Chackalamannil, Yuguang Wang, Stuart W. McCombie, Jayaram R. Tagat, Susan F. Vice, Wayne Vaccaro, Michael J. Green, Margaret E. Browne, Theodros Asberom, Craig D. Boyle
-
Patent number: 5880129Abstract: A discovery underlying this invention is the concordance between particular cellular signaling mechanisms and cancer cell growth and metastasis. It has now been discovered that certain compounds inhibit the signal transduction required for the maintenance and driving of the malignant process. These compounds are also effective for the in vivo treatment of solid tumors and related disease states. This invention provides a method for the use of these compounds to inhibit the invasion and metastasis of malignant solid tumors in mammals. This invention further provides a method for using related compounds to treat diseases involving aberrant signal transduction pathways. Some of the compounds used in the methods of the present invention are novel and constitute another aspect of this invention.Type: GrantFiled: August 5, 1997Date of Patent: March 9, 1999Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Elise C. Kohn, Lance A. Liotta, Christian C. Felder
-
Patent number: 5869659Abstract: The present invention relates to heteroatom-containing cyclopentanopyridyl-oxazolidinones, processes for their preparation and their use as medicaments, in particular as antibacterial medicaments.Type: GrantFiled: January 13, 1997Date of Patent: February 9, 1999Assignee: Bayer AktiengesellschaftInventors: Andreas Stolle, Dieter Habich, Bernd Riedl, Martin Ruppelt, Stephen Bartel, Walter Guarnieri, Hanno Wild, Rainer Endermann, Hein-Peter Kroll
-
Patent number: 5817661Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5 Y.sub.7, Y.sub.9 are each nitrogen and Y.sub.8 is a CH group,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: June 7, 1995Date of Patent: October 6, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5817672Abstract: This invention relates to novel Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent, Y.sub.3 and Y.sub.8 are CH, Y.sub.5, Y.sub.7 and Y.sub.9 are each independently nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: June 7, 1995Date of Patent: October 6, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5817660Abstract: This invention relates to Trans cyclopentanyl purine analogs of the formula (1) ##STR1## wherein the substituent in the 3-position on the cyclopentanyl ring is in the Trans configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.5, Y.sub.7, Y.sub.8 and Y.sub.9 are each nitrogen,R is a hydrogen, a C.sub.1 -C.sub.7 alkyl acyl or aryl acyl,Q is NH.sub.2, halogen or hydrogen,Z is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: June 7, 1995Date of Patent: October 6, 1998Assignee: Hoechst Marion Roussel, Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5807854Abstract: Compounds of general formula I and their salts and solvates are antifungal agents and as such are useful in the treatment of various fungal infections. Pharmaceutical compositions including these compounds and processes for their preparation are also provided.Type: GrantFiled: March 31, 1997Date of Patent: September 15, 1998Assignee: J. Uriah & Cia. S.A.Inventors: Javier Bartroli, Enric Turmo, Manuel Anguita
-
Patent number: 5763608Abstract: The present invention provides a process for preparing a 5,6-dihydro-3H-pyrimidin-4-one derivatives which comprises the steps of (a) dehydrating a N-acyl beta amino acid in the presence of a dehydration agent and an organic solvent for a sufficient period of time and under suitable temperature and pressure conditions to form an oxazone (b) adding a carboxylic acid and a primary amine salt of a carboxylic acid to said oxazone to form a mixture, (c) distilling azeotropically said mixture for a suitable period of time and under suitable temperature and pressure conditions to substantially remove said dehydration agent and said organic solvent, and (d) heating the product of step (c) for a sufficient period of time and under suitable temperature and pressure conditions to form said pyrimidin derivatives.Type: GrantFiled: February 5, 1996Date of Patent: June 9, 1998Assignee: Hoechst Celanese CorporationInventors: Apurba Bhattacharya, Diane E. Allen
-
Patent number: 5747496Abstract: Compounds of the formula (I) ##STR1## wherein B is O or CH.sub.2 ;X is selected from NR.sup.1 R.sup.2, SR.sup.1, and C.sub.1 -C.sub.7 alkyl;Y is selected SR.sup.1, NR.sup.1 R.sup.2, and C.sub.1 -C.sub.7 alkyl;R.sup.1 and R.sup.2 is each and independently selected from H, or C.sub.1 -C.sub.7 alkyl optionally substituted upon or within the alkyl chain by one or more of O, S, N or halogen;R.sup.3 and R.sup.4 are both H, or R.sup.3 and R.sup.4 together form a bond;A is COOH, C(O)NH(CH.sub.2).sub.p COOH, C(O)N?(CH.sub.2).sub.q COOH!.sub.2, C(O)NHCH(COOH)(CH.sub.2).sub.r COOH, or 5-tetrazolyl, wherein p, q and r is each and independently 1, 2 or 3;as well as pharmaceutically acceptable salts and prodrugs thereof, pharmaceutical compositions comprising the novel compounds and use of the compounds in therapy. Also within the scope of the invention are novel intermediates to the novel compounds. The novel compounds are in particular useful in the prevention of platelet aggregation.Type: GrantFiled: October 31, 1996Date of Patent: May 5, 1998Assignee: Astra Pharmaceuticals LimitedInventors: David Cox, Anthony Ingall, Paul Willis
-
Patent number: 5723609Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## wherein R.sub.2 is hydrogen, methyl, fluoro, chloro, bromo, iodo, hydroxy or amino; or trifluoromethyl; R.sub.5 is alkyl; R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.Type: GrantFiled: March 13, 1989Date of Patent: March 3, 1998Assignee: E. R. Squibb & Sons, Inc.Inventors: William A. Slusarchyk, Robert Zahler
-
Patent number: 5693771Abstract: In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.Type: GrantFiled: March 13, 1996Date of Patent: December 2, 1997Assignee: Gilead Sciences, Inc.Inventors: Petr Alexander, Ernest J. Prisbe
-
Patent number: 5674998Abstract: This invention relates to adenosine kinase inhibitors and to nucleoside analogs, C-4' modified pyrrolo?2,3-d!pyrimidine and pyrazolo?3,4-d!pyrimidine nucleoside analogs having activity as adenosine kinase inhibitors. The invention relates to nucleoside analogs of this kind, having zero substitutions or two substitutions at the C-4' position of the furanose (sugar) moiety. The invention also relates to the preparation and use of these adenosine kinase inhibitors in the treatment of cardiovascular, and cerebrovascular diseases, inflammation and other diseases which can be regulated by increasing the local concentration of adenosine.Type: GrantFiled: June 7, 1995Date of Patent: October 7, 1997Assignee: Gensia Inc.Inventors: Serge H. Boyer, Mark D. Erion, Bheemarao G. Ugarkar
-
Patent number: 5641783Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocycle. R.sub.3 may be either hydrogen or C.sub.1-3. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.Type: GrantFiled: September 8, 1994Date of Patent: June 24, 1997Assignee: Cell Therapeutics, Inc.Inventors: J. Peter Klein, Gail E. Underiner, Anil M. Kumar
-
Patent number: 5641889Abstract: The present invention relates to certain purine nucleoside analogues containing a carbocyclic ring in place of the sugar residue, salts, esters and pharmaceutically acceptable derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and to the use of such compounds in therapy, particularly the treatment or prophylaxis of certain vital infections.Type: GrantFiled: September 12, 1994Date of Patent: June 24, 1997Assignee: Glaxo Wellcome Inc.Inventors: Susan Mary Daluge, Douglas Alan Livingston
-
Patent number: 5622961Abstract: A series of benzoquinolin-3-ones are pharmaceuticals effective in treating conditions consequent on both Type I and Type II 5.alpha.-reductase.Type: GrantFiled: May 11, 1995Date of Patent: April 22, 1997Assignee: Eli Lilly and CompanyInventors: James E. Audia, Loretta A. McQuaid, Blake L. Neubauer, Vincent P. Rocco
-
Patent number: 5576432Abstract: A process of preparing a dihydropyrimidine compound of the structure (I): ##STR1## wherein R.sup.1 and R.sup.2 are bonded together to form an aromatic or heterocyclic ring, which may be substituted or unsubstituted, or are individually selected from the group consisting of hydrogen, or a substituted or unsubstituted aliphatic, carbocyclic, or heterocyclic group;R.sup.3, R.sup.4 and R.sup.5 are individually selected from the group consisting of hydrogen or a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; andX represents the atoms necessary to form a 5 or 6 membered heterocyclic ring, and is selected from the group consisting of oxygen, sulfur, selenium, ##STR2## wherein R.sup.6, R.sup.7, and R.sup.8 are individually selected from the group consisting of a substituted or unsubstituted aliphatic, carbocyclic or heterocyclic group; comprising combining a compound (A) of the structure: ##STR3## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, and R.sup.Type: GrantFiled: December 23, 1994Date of Patent: November 19, 1996Assignee: Eastman Kodak CompanyInventors: Roger Lok, Antony J. Williams
-
Patent number: 5559081Abstract: Herbicidal sulfonamides of the formula: ##STR1## and salts thereof, where: A represents a substituted or unsubstituted benzene ring, or a 5- or 6-membered substituted or unsubstituted heteroaromatic ring; Q is --O--, --S-- or a group --CXX'--; X and X', which may be the same or different, are each hydrogen, halogen, cyano, an optionally-substituted alkyl group, or a group --OR.sup.a, --SR.sup.a, or --COR.sup.b ; or one of X and X' represents hydroxy and the other is as defined above; or X and X' together represent .dbd.O or .dbd.S; R.sup.a is an optionally-substituted alkyl, aryl or acyl group; R.sup.b is an optionally-substituted alkyl or aryl group, or a group --OR.sup.c or --NR.sup.c R.sup.d ; R.sup.c and R.sup.d, which may be the same or different, are each hydrogen, or an optionally-substituted alkyl or aryl group; Y is nitrogen or a group CR.sup.9 ; R.sup.1 is an optionally-substituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heterocyclyl, benzoheterocyclyl or amino group; R.sup.Type: GrantFiled: May 6, 1994Date of Patent: September 24, 1996Assignee: Agrevo UK LimitedInventors: Peter S. Gates, Graham P. Jones, David E. Saunders
-
Patent number: 5543433Abstract: Compounds of the formula I ##STR1## where X is hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, cyano or nitro,Y is an amino, methylamino or dimethylamino group,Z is a group CHCH.sub.3, CHOCH.sub.3 or NOCH.sub.3,R is hydrogen or alkyl,A is hydrogen, alkyl, haloalkyl or cycloalkyl,B is unsubstituted or substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, heterocyclyl, aryl, heteroaryl, arylalkyl, heteroarylalkyl or the group ##STR2## where W is hydrogen, alkyl, alkoxy, alkylthio, alkylamino or dialkylamino, unsubstituted or substituted aryl or heteroaryl, unsubstituted or substituted aryloxy, arylthio, arylamino or aryl-N-(C.sub.1 -C.sub.6 -alkyl)amino, heteroaryloxy, heteroarylthio, heteroarylamino or heteroaryl-N-(alkyl)amino orA and B, together with the C atom whose substituents they are, are an isocyclic or heterocyclic ring which can also be quinonoid,and fungicides containing these compounds.Type: GrantFiled: June 3, 1994Date of Patent: August 6, 1996Assignee: BASF AktiengesellschaftInventors: Reinhard Doetzer, Hubert Sauter, Herbert Bayer, Franz Roehl, Gisela Lorenz, Eberhard Ammermann, Horst Wingert
-
Patent number: 5508277Abstract: Novel bicyclic pyrimidine compounds for use as drugs and having formula (I). Said novel compounds and physiologically tolerable salts thereof may be used in therapeutics, particularly for suppressing tumour cell resistance to antineoplastic agents.Type: GrantFiled: August 10, 1994Date of Patent: April 16, 1996Assignee: Adir Et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre
-
Patent number: 5506347Abstract: Novel lyxose derivatives which selectively inhibit adenosine kinase and methods of preparing these compounds are provided. These compounds are useful in treating certain conditions in vivo which may be ameliorated by increased local concentrations of adenosine.Type: GrantFiled: February 3, 1994Date of Patent: April 9, 1996Assignee: Gensia, Inc.Inventors: Mark D. Erion, Bheemarao G. Ugarkar, Angelo J. Castellino
-
Patent number: 5470878Abstract: Therapeutic compounds have the formula:(X)j-(non-cyclic core moiety),j being an integer from one to three, the core moiety is non-cyclic and X is a racemic mixture, R or S enantiomer, solvate, hydrate, or salt of: ##STR1## *C is a chiral carbon atom, n is an integer from one to four (preferably from one to three), one or more carbon atoms of (CH.sub.2).sub.n may be substituted by a keto or hydroxy group, and m is an integer from one to fourteen. Independently, R.sub.1 and R.sub.2 may be a hydrogen, a straight or branched chain alkane or alkene of up to twelve carbon atoms in length, or --(CH.sub.2).sub.w R.sub.5, w being an integer from two to fourteen and R.sub.5 being a mono-, di- or tri-substituted or unsubstituted aryl group, substituents on R.sub.5 being hydroxy, chloro, fluoro, bromo, or C.sub.1-6 alkoxy. Or jointly, R.sub.1 and R.sub.2 form a substituted or unsubstituted, saturated or unsaturated heterocyclic group having from four to eight carbon atoms, N being a hetero atom. R.sub.Type: GrantFiled: December 8, 1993Date of Patent: November 28, 1995Assignee: Cell Therapeutics, Inc.Inventors: John Michnick, Gail E. Underiner, J. Peter Klein, Glenn C. Rice
-
Patent number: 5470837Abstract: The present invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering to said patient an effective immunosuppressive amount of certain 5'-vinylhalo-aristeromycin/adenosine analogs.Type: GrantFiled: June 16, 1994Date of Patent: November 28, 1995Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jeffrey A. Wolos, Niall S. Doherty, Esa T. Jarvi, James R. McCarthy
-
Patent number: 5470857Abstract: This invention relates to a method of effecting immunosuppression in a patient in need thereof comprising administering an effective amount of a compound of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentenyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof.Type: GrantFiled: November 8, 1994Date of Patent: November 28, 1995Assignee: Marion Merrell Dow Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5457091Abstract: N1-Substituted 1H-1,2,3-triazolo[4,5-d]pyrimidine compounds of the formula I ##STR1## in which the substituents X, Y, R.sup.1, R.sup.2 and R.sup.3 have the meanings recited in the specification, are described as pharmaceutical compositions containing them and processes for their preparation. The compounds are effective antiviral agents.Type: GrantFiled: September 23, 1993Date of Patent: October 10, 1995Assignee: Hoechst AktiengesellschaftInventors: Gerhard Jaehne, Matthias Helsberg, Irvin Winkler, Gerhard Gross, Thomas Scholl
-
Patent number: 5457200Abstract: The present invention is concerned with the use of certain 3-aminopyrazolo-heterocyclic compounds for the colorimetric determination of hydrogen peroxide, hydrogen peroxide-forming systems, peroxidase, peroxidate-active substances and electron-rich aromatic compounds. The present invention is also concerned with corresponding processes of determination and with agents appropriate therefor. Furthermore, the present invention is concerned with new 3-aminopyrazolo-heterocyclic compounds.Type: GrantFiled: May 25, 1993Date of Patent: October 10, 1995Assignee: Boehringer MannheimInventors: Gerd Zimmermann, Joachim Siedel, Gunter Frey
-
Patent number: 5440040Abstract: The present invention is directed to compounds of formula (I), ##STR1## wherein R.sup.1 is OH, NH.sub.2 ; R.sup.2 is a heteroaromatic or aromatic substituent; R.sup.3 is H, OH, F, OCH.sub.3 ; R.sup.4 is H, F, OH or an ether or ester residue thereof, OCH.sub.3, CN, C.dbd.CH, N.sub.3 ; R.sup.5 is OH or an ether or ester residue thereof including mono, di- and triphosphate esters (.alpha.), wherein n is 0 or 1 and M is hydrogen or a pharmaceutically acceptable counterion such as sodium, potassium, ammonium or alkylammonium; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising said compounds can be used for therapeutic treatment of virus infections. The present invention is also directed to compounds of formula (I'), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, as intermediates.Type: GrantFiled: January 18, 1991Date of Patent: August 8, 1995Assignee: Medivir ABInventor: Salo Gronowitz
-
Patent number: 5434152Abstract: An asymmetric synthesis of (S)-(-)-6-chloro-4-cyclopropyl-3,4-dihydro-4-[(2-pyridyl)ethynyl]-2(1H)-qu inazolinone comprises the chiral addition of 2-pyridylacetylide to N.sup.1 -protected 6-chloro-4-cyclopropyl-2-quinazolinone followed by removal of the protecting group.Type: GrantFiled: November 8, 1993Date of Patent: July 18, 1995Assignee: Merck & Co., Inc.Inventors: Mark A. Huffman, Nobuyoshi Yasuda, Ann E. DeCamp, Edward J. J. Grabowski
-
Patent number: 5414096Type: GrantFiled: February 22, 1994Date of Patent: May 9, 1995Assignee: Bristol-Myers Squibb Co.Inventors: Joseph A. Tino, Gregory S. Bisacchi, Saleem Ahmad
-
Patent number: 5414000Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is a substituted purinyl group including pharmaceutically acceptable salts are useful as antiviral agents.Type: GrantFiled: February 22, 1994Date of Patent: May 9, 1995Assignee: Bristol-Myers Squibb Co.Inventors: Joseph A. Tino, Gregory S. Bisacchi, Saleem Ahmad
-
Patent number: 5382585Abstract: The present invention relates to pyrimidofuroxans of the general formula I ##STR1## in which A denotes ##STR2## where in each case the nitrogen atom is bonded via the C-4 and the carbon atom via the C-3 of the furoxan ring and the R radicals are defined as indicated in Claim 1, processes for their preparation and their use for the control and prevention of disorders of the cardiovascular system, in particular for the control and prevention of angina pectoris, and for the treatment of erectile dysfunctions.Type: GrantFiled: May 25, 1993Date of Patent: January 17, 1995Assignee: Cassella AGInventors: Joachim Brendel, Karl Schonafinger, Helmut Bohn
-
Patent number: 5369098Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and their pharmaceutically acceptable salts. R.sub.1 is ##STR2## R.sub.2 is hydrogen, --PO.sub.3 H.sub.2, ##STR3## wherein R.sub.3 is hydrogen, alkyl, substituted alkyl, or aryl, and R.sub.4 is alkyl.Type: GrantFiled: June 16, 1989Date of Patent: November 29, 1994Assignee: E. R. Squibb & Sons, Inc.Inventor: William A. Slusarchyk
-
Patent number: 5359078Abstract: A compound having the formula:Y--(CH.sub.2).sub.p --Ar.sup.11 --X--Ar.sup.12wherein:p is an integer of from 0 to 4;Ar.sup.11 and Ar.sup.12 are each aromatic moieties independently selected from the group consisting of phenyl, naphthyl, and substituted versions thereof in which the substituents are members selected from the group consisting of halogen, nitro, carboxyl and alkoxy;X is a linking moiety selected from the group consisting of O, S, SO.sub.2, CO, CHCN, straight chain alkyl, alkoxy, and alkoxyalkyl; andY is a nitrogen-containing heterocyclic moiety.Type: GrantFiled: December 4, 1992Date of Patent: October 25, 1994Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Elise C. Kohn, Lance A. Liotta, Christian C. Felder
-
Patent number: 5332814Abstract: Process for the preparation of racemic compounds of the formula I ##STR1## or enantiomers thereof, in which B is the radical of a nucleic base from the series comprising purine, a purine analogue or a pyridine analogue, and R is H or a protective group R.sub.1, by reactinga) a compound of the formula II or enantiomer thereof ##STR2## with a compound of the formulae X--CO--X, X--CS--X, X--SO--X, X--SO.sub.2 --X, R.sub.2 --NCO, R.sub.3 R.sub.4 N--C(O)--R.sub.5, X.sub.2 P--R.sub.6 or X.sub.2 P(O)--R.sub.6, in which X is a leaving group, R.sub.2 is, for example, C.sub.1 -C.sub.18 alkyl, R.sub.3 and R.sub.4 are, for example, H or C.sub.1 -C.sub.18 alkyl, R.sub.5 is, for example, H or C.sub.1 -C.sub.12 alkyl, and R.sub.6 is, for example, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy, to give a compound of the formula III or enantiomers thereof ##STR3## in which Y is the groups --C(O)--, --C(S)--, --SO--, --SO.sub.2 --, R.sub.2 NH--CH.dbd., R.sub.3 R.sub.4 N--CR.sub.5 .dbd., R.sub.6 P.dbd. and R.sub.6 (O)P.Type: GrantFiled: October 30, 1992Date of Patent: July 26, 1994Assignee: Ciba-Geigy CorporationInventor: Heinz Moser
-
Patent number: 5322845Abstract: An acrylic acid compound useful for fungicides is provided. The compound has the following formula (I) ##STR1## wherein X represents a phenyl group which may be substituted, or a methylene group, n represents 0 or 1, Y represents an oxygen atom or a sulfur atom, Z represents a phenyl group, an aralkyl group, an aromatic heterocyclyl group or an aromatic heterocyclylmethylene group and Z may be substituted.Type: GrantFiled: October 1, 1992Date of Patent: June 21, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Tsuguhiro Katoh, Atsuo Mizuguchi, Hirotaka Takano
-
Patent number: 5314893Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is an amino substituted pyrimidinone or a pyrimidinedione including pharmaceutically acceptable salts are useful as antiviral agents.Type: GrantFiled: January 25, 1993Date of Patent: May 24, 1994Assignee: Bristol-Myers Squibb Co.Inventors: Joseph A. Tino, Gregory S. Bisacchi, Saleem Ahmad
-
Patent number: 5246931Abstract: A compound of the formula: ##STR1## wherein A is a purin-9-yl group, a heterocyclic isostere of a purin-9-yl group, a pyrimidin-1-yl group or a heterocyclic isostere of a pyrimidin-1-yl group; E is hydrogen, --CH.sub.2 OH or --OH; and G and D are independently selected from hydrogen, C.sub.1 to C.sub.10 alkyl, --OH, --CH.sub.2 OH, --CH.sub.2 OR.sub.20 wherein R.sub.20 is C.sub.1 to C.sub.6 alkyl, --CH.sub.2 OC(O)R.sub.21 wherein R.sub.21 is C.sub.1 to C.sub.10 alkyl, --CH.sub.2 OC(O)CH(R.sub.22)(NHR.sub.23) wherein R.sub.22 is the side chain of any of the naturally occurring amino acids and R.sub.23 is hydrogen or --C(O)CH(R.sub.24)(NH.sub.2) wherein a R.sub.24 is the side chain of any of the naturally occurring amino acids, --CH.sub.2 SH, --CH.sub.2 Cl, --CH.sub.2 F, --CH.sub.2 Br, --CH.sub.2 I, --C(O)H, --CH.sub.2 CN, --CH.sub.2 N.sub.3, --CH.sub.2 NR.sub.1 R.sub.2, --CO.sub.2 R.sub.1, --CH.sub.2 CH.sub.2 OH, --CH.sub.2 CH.sub.2 OR.sub.20 wherein R.sub.20 is as defined above, --CH.sub.2 CH.sub.2 OC(O)R.sub.Type: GrantFiled: May 1, 1991Date of Patent: September 21, 1993Assignee: Bristol-Myers Squibb CompanyInventors: Daniel W. Norbeck, Jacob J. Plattner, Terry J. Rosen, David L. Garmaise, Richard J. Pariza, Steven M. Hannick, Thomas J. Sowin
-
Patent number: 5244896Abstract: This invention relates to novel carbocyclic adenosine compounds of the formula (1) ##STR1## wherein the hydroxy substituent on the cyclopentanyl ring is in the CIS configuration relative to the bicyclic substituent,Y.sub.3, Y.sub.7, Y.sub.8 and Y.sub.9 are each independently nitrogen or a CH group,Q is NH.sub.2, halogen or hydrogen, andZ is hydrogen, halogen, or NH.sub.2 ;or a pharmaceutically-acceptable salt thereof, and to their use as immunosuppressants.Type: GrantFiled: January 23, 1992Date of Patent: September 14, 1993Assignee: Marion Merrell Dow Inc.Inventors: David R. Borcherding, Carl K. Edwards, III, Ronald E. Esser, Douglas L. Cole
-
Patent number: 5225550Abstract: It is possible, by using symmetrical formaldehyde acetals of the formula ##STR1## in which the substituents R.sup.1 -R.sup.3 have the specified meanings, advantageously to introduce the substituent ##STR2## into nitrogen-containing heterocyclic systems to form acyclic nucleoside analogs.Type: GrantFiled: June 25, 1991Date of Patent: July 6, 1993Assignee: Hoechst AktiengesellschaftInventor: Gerhard Jahne