Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/318)
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Publication number: 20030216575Abstract: This invention is directed to novel pyranosyl cytosine compounds depicted graphically as structure I. This invention is further directed to a unique methodology for their preparation using solid-phase methodology. These hexopyranosyl cytosine derived natural product analogs share their parent compounds broad-spectrum antimicrobial and anti-fungal profile and represent a vast, novel compound class of 50S rRNA directed inhibitors of protein translation.Type: ApplicationFiled: February 4, 2002Publication date: November 20, 2003Inventors: Michael T. Migawa, Eric E. Swayze, Richard H. Griffey
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Patent number: 6649622Abstract: aP2 inhibiting compounds are provided having the formula wherein A, B, X, and Y are as described herein. A method is also provided for treating diabetes and related diseases, especially Type II diabetes, employing such aP2 inhibitor or a combination of such aP2 inhibitor and another antidiabetic agent such as metformin, glyburide, troglitazone and/or insulin.Type: GrantFiled: January 26, 2001Date of Patent: November 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: Richard Sulsky, Jeffrey A. Robl
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Patent number: 6620932Abstract: Novel 2-alkoxy-5-methoxypyrimidines and tautomeric forms thereof and also processes for preparing them are described. The 2-alkoxy-5-methoxypyrimidines according to the invention can be synthesized in few reaction steps and in high yields from simple precursors.Type: GrantFiled: August 15, 2002Date of Patent: September 16, 2003Assignee: Degussa AGInventors: Thomas Güthner, Karl-Heinz Neuhauser
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Patent number: 6613773Abstract: The invention provides fungicidal compounds of formula (I) or stereoisomers thereof: wherein X is CH2O; A is hydrogen; E is hydrogen; q is 1; any two of K, L and M are nitrogen and the other is CH; T is oxygen or sulfur; and Z is an optionally substituted phenyl group or an optionally substituted heterocyclyl group.Type: GrantFiled: March 5, 2002Date of Patent: September 2, 2003Assignee: Syngenta LimitedInventors: John Martin Clough, Christopher Richard Ayles Godfrey, Ian Thomas Streeting, Rex Cheetham, Paul John de Fraine, David Bartholomew, James John Eshelby
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Patent number: 6610691Abstract: The invention relates to carboxylic acid derivatives of the formula where the radicals have the meanings defined in the description, to the preparation of these compounds and to their use as drugs.Type: GrantFiled: October 8, 1998Date of Patent: August 26, 2003Assignee: BASF AktiengesellschaftInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Heinz Hillen, Liliane Unger, Bernd Elger
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Patent number: 6600044Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.Type: GrantFiled: June 18, 2001Date of Patent: July 29, 2003Assignee: Brantford Chemicals Inc.Inventors: K. S. Keshava Murthy, Gurijala V. Reddy, Zhi-xian Wang, Chandrawansha B. W. Senanayake
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Patent number: 6586594Abstract: A process for the preparation of a compound of the formula: or an acid addition or base salt thereof, wherein R is phenyl optionally substituted by 1 to 3 substituents each independently selected from halo and trifluoromethyl; R1 is C1-C6 alkyl; and “Het” is pyrimidinyl optionally substituted by 1 to 3 substituents each independently selected from C1-C4 alkyl, C1-C4 alkoxy, halo, oxo, benzyl and benzyloxy, comprising reacting a compound of the formula: with a compound of the formula wherein X is chloro, bromo or iodo, the reaction taking place in the presence of zinc; at least one of iodine or a Lewis acid; and an aprotic organic solvent: optionally further reacting the resulting compound with an acid or base to form the corresponding acid addition or base salt thereof.Type: GrantFiled: February 4, 1998Date of Patent: July 1, 2003Assignee: Pfizer, Inc.Inventors: Michael Butters, Alan John Pettman, Julie Ann Harrison
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Patent number: 6570015Abstract: There is disclosed a process for producing a 2-substituted thiopyrimidine-4-carboxylate represented by the formula (3): wherein R2 represents a substituted or unsubstituted hydrocarbon group and R3 represents a hydrocarbon group, which comprises reacting-an &agr;-keto ester compound represented by the formula (1): R1OCH═CHCOCO2R2 (1) wherein R1 represents a substituted or unsubstituted hydrocarbon group, and R has the same meaning as defined above, with an isothiourea compound represented by the formula (2): wherein R3 has the same meaning as defined above.Type: GrantFiled: September 17, 2002Date of Patent: May 27, 2003Assignee: Ube Industries, Ltd.Inventors: Akio Matsushita, Kiyotaka Yoshii, Masayoshi Oue, Taku Nakamura, Shuji Yamada
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Patent number: 6552028Abstract: This invention relates to certain 2,4-substituted pyrrolidine derivatives that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: December 19, 2001Date of Patent: April 22, 2003Assignee: Syntex (U.S.A.) LLCInventors: Denis John Kertesz, Michael Garret Roepel
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Patent number: 6451738Abstract: The invention relates to novel substituted thienyl(amino)sulphonyl(thio)ureas of the formula (I) in which A represents nitrogen or a CH grouping, E represents a single bond or an NH grouping, Q represents oxygen or sulphur, R1 and R2 independently of one another represent hydrogen, halogen or in each case optionally substituted alkyl, alkoxy, alkylthio, alkylamino, dialkylamino, cycloalkyl, cycloalkyloxy, aryloxy or heterocyclyloxy, R3 represents hydrogen or optionally substituted alkyl, R4 and R5 independently of one another each represent cyano, halogen or represent in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and R6 represents hydrogen, cyano, halogen or represents in each case optionally substituted alkyl, alkoxy, alkenyl, alkenyloxy, alkinyl or alkinyloxy, and to salts of compounds of the formula (I), to processes for preparing the novel compounds and to their use as herbicides.Type: GrantFiled: August 9, 2001Date of Patent: September 17, 2002Assignee: Bayer AktiengesellschaftInventors: Ernst Rudolf F. Gesing, Johannes Rudolf Jansen, Klaus-Helmut Müller, Ulrich Philipp, Markus Dollinger
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Patent number: 6440899Abstract: Cyclohexenonedioxothiochromanoyl derivatives of the formula I where X is oxygen, sulfur, S═O, S(═O)2, CR4R5, C═O or C═NR6, the other substituents are as defined in the specification, and and agriculturally useful salts thereof; processes for preparing the cyclohexenonedioxotheiochromanoyl derivatives; compositions comprising them, and the use of these derivatives or of compositions comprising them for controling undesirable piants.Type: GrantFiled: October 30, 2000Date of Patent: August 27, 2002Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Klaus Langemann, Wolfgang von Deyn, Ulf Misslitz, Ernst Baumann, Stefan Engel, Guido Mayer, Ulf Neidlein, Oliver Wagner, Roland Götz, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6403582Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g.Type: GrantFiled: January 12, 2001Date of Patent: June 11, 2002Assignee: Schering CorporationInventors: Gregory A. Reichard, Neng-Yang Shih, Dasong Wang
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Patent number: 6399620Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: June 29, 2000Date of Patent: June 4, 2002Assignee: Aventis Pharma S.A.Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
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Patent number: 6399776Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.Type: GrantFiled: June 11, 2001Date of Patent: June 4, 2002Assignee: Pfizer INCInventors: Thomas G. LaCour, Charles William Murtiashaw, III
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Patent number: 6387893Abstract: Spirotricyclic azacycloalkyl compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds is also described. One application of these compounds, which are alpha 1a adrenergic receptor antagonists, is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.Type: GrantFiled: September 27, 2000Date of Patent: May 14, 2002Assignee: Merck & Co., Inc.Inventors: Ben E. Evans, Jacob M. Hoffman, Kevin F. Gilbert, Kenneth E. Rittle
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Patent number: 6362183Abstract: An aromatic sulfonyl alpha-hydroxy hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 4, 1999Date of Patent: March 26, 2002Assignee: G. D. Searle & CompanyInventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
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Patent number: 6358976Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the &agr;v&bgr;3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.Type: GrantFiled: February 22, 2000Date of Patent: March 19, 2002Inventors: John Wityak, Aleksandra Ewa Tobin
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Patent number: 6352997Abstract: The present invention provides for a method of treating polycystic ovary syndrome in a subject in need of such treatment comprising the administration of a therapeutically effective amount of a compound of structural formula I: to the subject. The present invention further provides for a method for improving fertility and the response to in vitro fertilization (I.V.F.), comprising administration of therapeutically effective amount of compound of structural formula I to the subject. Further, the present invention provides for compositions useful in the methods of the present invention, as well as a method of manufacture of a medicament useful for treating polycystic ovary syndrome or for improving fertility or the response to in vitro fertilization (I.V.F.).Type: GrantFiled: May 3, 1999Date of Patent: March 5, 2002Assignee: Merck & Co., Inc.Inventors: Joanne Waldstreicher, Georgianna S. Harris
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Patent number: 6348594Abstract: Urea derivatives of formula 1 for the hardening of hydroxyl group-containing polymers, wherein each of R1-R7 is a hydrogen atom or a linear or branched C1-C4-alkyl group, preferably methyl, ethyl, n-propyl, isopropyl, n-butyl or isobutyl, R1-R7 being identical or different, and R8 is a linear or branched C1-C6-alkyl group, preferably methyl, ethyl, n-propyl, isopropyl, n-butyl or isobutyl. The compounds 1 are prepared by reacting a compound 2 wherein R9 is a member selected from the group consisting of —CHO, —CH(OH)—OR8 and —CH(OH)2 with a urea derivative 3 optionally followed by etherification of the reaction product with an alcohol X—OH, wherein X is a linear or branched C1-C4-alkyl group.Type: GrantFiled: July 30, 1999Date of Patent: February 19, 2002Assignee: Dainippon Ink and Chemicals, Inc.Inventors: Kai-Uwe Gaudl, Artur Lachowicz, Gerwald Grahe
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Publication number: 20020004599Abstract: Urea derivatives of formula 1 for the hardening of hydroxyl group-containing polymers.Type: ApplicationFiled: July 30, 1999Publication date: January 10, 2002Inventors: KAI-UWE GAUDL, ARTUR LACHOWICZ, GERWALD GRAHE
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Patent number: 6329522Abstract: The invention relates to a diastereoselective process for the preparation of compounds of formula (1), wherein W is S, S═O, SO2 or O; X is S, S═O, SO2 or O; R1 is hydrogen or acyl, and R2 is a purine or pyrimidine base or an analogue or derivative thereof.Type: GrantFiled: June 23, 1999Date of Patent: December 11, 2001Assignee: Glaxo Group LimitedInventors: Malcolm Leithead Hill, Andrew Jonathan Whitehead, Roy Hornby, Peter Hallett, Michael David Goodyear, P. Owen Dwyer
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Publication number: 20010041798Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.Type: ApplicationFiled: June 11, 2001Publication date: November 15, 2001Inventors: Thomas G. LaCour, Charles William Murtiashaw,
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Publication number: 20010041797Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: 1Type: ApplicationFiled: January 16, 2001Publication date: November 15, 2001Applicant: BioChem Pharma Inc.Inventors: Bernard Belleau, Tarek Mansour, Allan Tse, Colleen A. Evans, Haolun Jin, Boulos Zacharie, Nghe Nguyen-Ba
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Publication number: 20010041707Abstract: This invention is directed to dihydropyrimidines which are selective antagonists for human &agr;1a receptors. This invention is also related to uses of these compounds for relaxing lower urinary tract tissue, treating benign prostatic hyperplasia and for the treatment of any disease where the antagonism of the &agr;1a receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: ApplicationFiled: June 4, 2001Publication date: November 15, 2001Applicant: Merck and Co., IncInventors: Donghui Cui, Margaret R. Davis, Michael Dunn, Ben E. Evans, Hanumath P. Kari, Bharat Lagu, Dhanapalan Nagarathnam, Kamlesh P. Vyas, Kanyin Zhang
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Patent number: 6313296Abstract: A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: GrantFiled: February 23, 2000Date of Patent: November 6, 2001Assignee: Abbott LaboratoriesInventors: Hing Leung Sham, Daniel W. Norbeck, Xiaoqi Chen, David A. Betebenner, Dale J. Kempf, Thomas R. Herrin, Gondi N. Kumar, Stephen L. Condon, Arthur J. Cooper, Daniel A. Dickman, Steven M. Hannick, Lawrence Kolaczkowski, Patricia A. Oliver, Daniel J. Plata, Peter J. Stengel, Eric J. Stoner, Jieh-Heh J. Tien, Jih-Hua Liu, Ketan M. Patel
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Patent number: 6313072Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.Type: GrantFiled: February 18, 1999Date of Patent: November 6, 2001Assignee: American Cyanamid CompanyInventors: Stephen Scheiblich, Thomas Maier, Axel Kleemann, Helmut Siegfried Baltruschat
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Patent number: 6310178Abstract: Ureins are obtained by reaction, in basic medium, between an N&ohgr;-(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.Type: GrantFiled: February 11, 2000Date of Patent: October 30, 2001Assignee: Solvay, S.A.Inventors: Roland Callens, Georges Blondeel, Marc Anteunis, Frank Becu
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Patent number: 6306866Abstract: There are provided compositions and methods comprising compounds of formula I: wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.Type: GrantFiled: March 6, 1998Date of Patent: October 23, 2001Assignee: American Cyanamid CompanyInventors: William Wakefield Wood, Linda Fleming, Salvatore John Cuccia
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Patent number: 6288071Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.Type: GrantFiled: December 10, 1998Date of Patent: September 11, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Publication number: 20010020026Abstract: Disclosed are compounds of the formulaType: ApplicationFiled: October 15, 1998Publication date: September 6, 2001Inventors: BERNARD BELLEAU, PIERETTE BELLEAU, NGHE NGUYEN-BA
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Patent number: 6281219Abstract: The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.Type: GrantFiled: July 12, 1999Date of Patent: August 28, 2001Assignee: American Cyanamid Co.Inventors: Salvatore John Cuccia, William Wakefield Wood, Brian Lee Buckwalter, John Francis Chiarello, Linda Barbara Fleming
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Patent number: 6274733Abstract: This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.Type: GrantFiled: October 28, 1999Date of Patent: August 14, 2001Assignee: Pfizer Inc.Inventors: Thomas G. LaCour, Charles William Murtiashaw, III
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Patent number: 6265398Abstract: The present invention relates to novel substituted pyridines/pyrimidines of the formula I where A is CH or N; X is NH, O or S(O)q where q is 0, 1 or 2; Y1, Y2 and Y3 independently of one another are a group of the formula —O—, —CO—, —CNR6—, —S(O)r— or —N(O)lR6— where l is 0 or 1 and where r is 0, 1 or 2, or a group of the formula CR7R8, or Y1 or Y3 replace a direct bond; Z is a direct bond, NR9, O, S(O)s where s is 0, 1 or 2, OSO2, SO2O, NR10SO2, SO2NR11, SiR12R13 or where U is a direct bond, NR14 or O; W is oxygen or sulfur; V is a direct bond, NR15 or oxygen; m and n and 0, 1, 2, 3 or 4; where the radicals R1 to R15 have the meaning given in the description, to processes for their preparation, to their use as pesticides, fungicides and ovicides and to their use as veterinary medicaments.Type: GrantFiled: October 23, 1998Date of Patent: July 24, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Ralf Braun, Wolfgang Schaper, Herbert Stark, Rainer Preuss, Werner Knauf, Ulrich Sanft, Manfred Kern, Werner Bonin
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Patent number: 6254669Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.Type: GrantFiled: August 5, 1999Date of Patent: July 3, 2001Assignee: Zeneca LimitedInventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
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Patent number: 6248770Abstract: The present invention relates to new benzimidazoles of general formula wherein Ra to Rc, A, Ar and B are defined as in claim 1, the tautomers, the stereoisomers, the mixtures thereof the prodrugs, the derivatives thereof which contain a group which is negatively charged under physiological conditions, instead of a carboxy group, and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties. The compounds of the above general formula I wherein Rc denotes a cyano group are valuable intermediates for preparing the other compounds of general formula I, and the compounds of the above general formula I wherein Rc denotes one of the amidino groups mentioned in claim 1 which have valuable pharmacological properties, particularly an antithrombotic activity.Type: GrantFiled: June 24, 1999Date of Patent: June 19, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Uwe Ries, Iris Kauffmann, Norbert Hauel, Henning Priepke, Herbert Nar, Jean Marie Stassen, Wolfgang Wienen
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Patent number: 6245773Abstract: This invention is directed to dihydropyrimidine compounds of the following formula: which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 16, 1997Date of Patent: June 12, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Wai C. Wong, Bharat Lagu, Dhanapalan Nagarathnam, Mohammad R. Marzabadi, Charles Gluchowski
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Patent number: 6235903Abstract: A process for preparing endothelin receptor antagonists of the sulfanyl type of the general formula I by nucleophilic reaction of a carboxylic acid derivative of the formula II with a sulfide of the formula III to give endothelin receptor antagonists of the formula I.Type: GrantFiled: August 23, 2000Date of Patent: May 22, 2001Assignee: BASF AktiengesellschaftInventors: Wilhelm Amberg, Rolf Jansen, Dagmar Klinge
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Patent number: 6228861Abstract: This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: November 10, 1998Date of Patent: May 8, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, Wai C. Wong, Shou Wu Miao, Charles Gluchowski, Michael A. Patane
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Patent number: 6222036Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: February 11, 2000Date of Patent: April 24, 2001Assignee: SmithKline Beecham CorporationInventor: Zhi-Qiang Peng
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Patent number: 6211190Abstract: Pyrimidine compounds I wherein X is C(CO2CH3)═NOCH3, C(CONHCH3)═NOCH3, C(CO2CH3)═CHOCH3, C(CO2CH3)═CHCH3 or N(CO2CH3)—OCH3; R1, R2 are hydrogen, alkyl, haloalkyl or alkoxy; A is R3 is hydrogen, alkyl, haloalkyl, phenoxyalkyl, cycloalkyl, cyano, alkoxy, hydroxyl or halogen; R4 is hydrogen, optionally substituted alkyl, alkenyl, alkynyl, haloalkenyl, haloalkynyl, cycloalkyl or alkoxy; Y is hydrogen, hydroxyl, halogen, optionally substituted aryl, hetaryl, cycloalkyl, cycloalkenyl, heterocyclyl, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, aryloxy, arylthio, hetaryloxy, hetarylthio, cycloalkyloxy or alkylthio, or their salt, their synthesis and intermediates therefore, and their activity against fungi or animal pests.Type: GrantFiled: August 4, 1998Date of Patent: April 3, 2001Assignee: BASF AktiengesellschaftInventors: Wassilios Grammenos, Herbert Bayer, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Klaus Oberdorf, Arne Ptock, Hubert Sauter, Franz Röhl, Michael Rack, Gisela Lorenz, Eberhard Ammermann, Siegfried Strathmann, Volker Harries
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Patent number: 6204265Abstract: Compound represented by the structural formula or a pharmaceutically acceptable salt thereof, wherein: a is 0-3; b, d and e are 0-2; R is H, alkyl, F or —OR6; A is an optionally substituted oxime or hydrazone; d is not 0 and X is a bond, —C(O)—, —O—, —NR9—, —S(O)e—, —N(R6)C(O)—, —C(O)N(R6)—, —OC(O)NR6—, —OC(═S)NR6—, —N(R6)C(═S)O—, —S(O)2N(R6)—, —N(R6)S(O)2—, —N(R6)C(O)O—, —OC(O)— or —N(R6)C(O)NR7—; or d is 0 and X is a bond or —NR6—; T is H, aryl, heterocycloalkyl or heteroaryl; Q is phenyl, naphthyl or heteroaryl; R6 is H, alkyl, hydroxyalkyl, alkoxyalkyl, phenyl, and benzyl; R9 is R6 or —OR6 R6a, R7a, R8a and R9a are H or alkyl; Z is a nitrogen-containing heterocyclo group, e.g.Type: GrantFiled: December 21, 1999Date of Patent: March 20, 2001Assignee: Schering CorporationInventors: Gregory A. Reichard, Neng-Yang Shih, Dasong Wang
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Patent number: 6175008Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.Type: GrantFiled: June 6, 1995Date of Patent: January 16, 2001Assignee: BioChem Pharma Inc.Inventors: Bernard Belleau, Tarek Mansour, Allan Tse, Colleen A. Evans, Haolun Jin, Boulos Zacharie, Nghe Nguyen-Ba
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Patent number: 6166014Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 19, 1999Date of Patent: December 26, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6153752Abstract: Process for the preparation of heterocycles by reacting 2-substituted acetals of malondialdehyde with a reactant selected from hydroxylamines and their salts, hydrazines and their salts, formamid, amidines and their salts, guanidines and their salts, aminoguanidines and their salts, nitroguanidine and their salts, O-alkyl-isoureas and their salts, O-cycloalkyl-isoureas and their salts, O-aralkyl-isoureas and their salts, O-aryl-isoureas and their salts, S-alkyl-isothioureas, S-cycloalkyl-isothioureas, S-aralkyl-isothioureas, S-arylisothioureas, S-alkyl-isothiouronium salts, S-cycloalkyl-isothiouronium salts, S-aralkyl-isothiouronium salts, S-aryl-isothiuronium salts, thiourea and urea.Type: GrantFiled: January 28, 2000Date of Patent: November 28, 2000Assignee: Creanova, Inc.Inventors: Frank Bauer, Chitoor Subramaniam
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Patent number: 6150382Abstract: This invention is directed to monocyclic N-heterocyclics which are substituted by acyclic or cyclic thio derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.Type: GrantFiled: May 21, 1999Date of Patent: November 21, 2000Assignee: Berlex Laboratories, Inc.Inventors: Monica J. Kochanny, Michael M. Morrissey, Howard P. Ng
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Patent number: 6136976Abstract: Perylene-3,4-dicarboximides I ##STR1## (R.sup.1 is hydrogen; C.sub.1 -C.sub.8 -alkyl; C.sub.5 -C.sub.8 -cycloalkyl; substituted or unsubstituted phenyl or naphthyl;R.sup.2 independently at each occurrence is hydrogen; C.sub.1 -C.sub.18 -alkyl, substituted or unsubstituted aryloxy, arylthio, hetaryloxy or hetarylthio)are prepared by reacting the corresponding perylene-3,4,9,10-tetracarboxylic acid or its anhydride (II) with an amide IIIR.sup.3 --CO--NHR.sup.1 III(R.sup.3 : C.sub.1 -C.sub.4 -alkyl or --NR.sup.4 R.sup.5 where R.sup.4 and R.sup.5 independently are hydrogen or one of the R.sup.1 alkyls, cycloalkyls, phenyls or naphthyls and where if two or more of R.sup.1, R.sup.4 and R.sup.5 are other than hydrogen they are identical)under superatmospheric pressure in the presence of an inert diluent and a transition metal catalyst.Type: GrantFiled: December 7, 1998Date of Patent: October 24, 2000Assignee: BASF AktiengesellschaftInventors: Arno Boehm, Harald Arms, Willi Helfer, Georg Henning
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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
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Patent number: RE37314Abstract: The compounds of the present invention inhibit the HMG-CoA reductase, and subsequently suppress the biosynthesis of cholesterol. And they are useful in the treatment of hypercholesterolemia, hyperlipoproteinemia, and atherosclerosis.Type: GrantFiled: August 27, 1998Date of Patent: August 7, 2001Assignee: Shionogi Seiyaku Kabushiki KaishaInventors: Kentaro Hirai, Teruyuki Ishiba, Haruo Koike, Masamichi Watanabe
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Patent number: RE37729Abstract: 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: February 3, 1999Date of Patent: June 4, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Edward J. Glamkowski, Yulin Chiang, Joseph T. Strupczewski, Kenneth J. Bordeau, Peter A. Nemoto, John J. Tegeler