Nitrogen Attached Directly At 2-position By Nonionic Bonding Patents (Class 544/320)
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Publication number: 20030187004Abstract: A pyrimidone derivative represented by formula (I) or a salt thereof: 1Type: ApplicationFiled: December 2, 2002Publication date: October 2, 2003Inventors: Antonio Almario Garcia, Ryoichi Ando, Keiichi Arimoto, Fumiaki Uehara, Adrien Tak Li, Aya Shoda, Jonathan Reid Frost, Kazutoshi Watanabe
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Patent number: 6617332Abstract: The invention relates to novel natural product derivatives of the formula (I), to processes for their preparation, to pharmaceutical compositions comprising them and to their use in the treatment of disorders in humans or animals: in which R1, D, X, Y and Z are defined as in claim 1.Type: GrantFiled: April 11, 2001Date of Patent: September 9, 2003Assignee: Bayer AktiengesellschaftInventors: Michael Brands, Mazen Es-Sayed, Dieter Häbich, Siegfried Raddatz, Joachim Krüger, Rainer Endermann, Reinhold Gahlmann, Hein-Peter Kroll, Frank-Ulrich Geschke, Armin de Meijere, Vladimir N. Belov, Victor Sokolov, Sergej Kozhushkov, Markus Kordes
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Publication number: 20030162802Abstract: Pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula 1Type: ApplicationFiled: June 17, 2002Publication date: August 28, 2003Inventors: Junqing Guo, Joseph Barbosa, William John Pitts, Marianne Carlsen, Claude Quesnelle, Marco Dodier
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Patent number: 6610698Abstract: Selected novel substituted pyrimidine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: April 3, 2002Date of Patent: August 26, 2003Assignee: Amgen, Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
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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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Publication number: 20030139403Abstract: This invention features pyrimidine compounds of formula (I): 1 2Type: ApplicationFiled: November 30, 2001Publication date: July 24, 2003Inventors: M. Ono, Lijun Sun, Teresa Przewloka, Shijie Zhang, Elena Kostic, Weiwen Ying, Yumiko Wada, K. Koya
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Patent number: 6596719Abstract: The present invention relates to novel bis-sulfonamides represented, for example, by formula I below and a pure diastereomer, a mixture of diastereomers, a diastereomeric racemate, a mixture of diastereomeric racemates and meso-forms and a pharmaceutically acceptable salt thereof, wherein R1 represents aryl; aryl-lower alkyl; aryl-lower alkenyl; heteroaryl; or heteroaryl-lower alkyl; and R2 represents lower alkyl; trifluoromethyl; lower alkoxy-lower alkyl; lower alkenyl; lower alkynyl; aryl; aryl-lower alkyl; aryl-lower alkenyl; heterocyclyl; heterocyclyl-lower alkyl; heteroaryl; heteroaryl-lower alkyl; cycloalkyl; or cycloalkyl-lower alkyl. The present invention also relates to a process for manufacturing those compounds, pharmaceutical compositions containing one or more of those compounds as endothelin antagonists, and a method of treating a subject having a disorder involving endothelin with the compounds of the invention.Type: GrantFiled: August 16, 2001Date of Patent: July 22, 2003Assignee: Actelio Pharmaceuticals Ltd.Inventors: Martin Bolli, Christoph Boss, Martine Clozel, Walter Fischli
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Publication number: 20030135048Abstract: A process for producing predominantly cis nucleosides or nucleoside analogues and derivatives of formula (A): 1Type: ApplicationFiled: June 14, 2002Publication date: July 17, 2003Applicant: Shire BioChem Inc.Inventor: Qing Yu
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Patent number: 6586441Abstract: The invention relates to cyclic heteroaromatic compounds, containing at least one nitrogen atom, and to their use in the manufacture of medicaments for the treatment of diseases, related to adenosine receptor modulators, such as Alzheimer's disease, Parkinson's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, asthma, allergic responses, hypoxia, ischaemia, seizure, substance abuse, sedation and they may be active as muscle relaxants, antipsychotics, anti epileptics, anticonvulsants and cardiaprotective agents.Type: GrantFiled: February 20, 2001Date of Patent: July 1, 2003Assignee: Hoffman-La Roche Inc.Inventors: Edilio Maurizio Borroni, Gerda Huber-Trottmann, Gavin John Kilpatrick, Roger David Norcross
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Publication number: 20030114446Abstract: This invention features pyrimidine compounds of formula (I): 1Type: ApplicationFiled: July 10, 2002Publication date: June 19, 2003Inventors: Lijun Sun, Mitsunori Ono, Teresa Przewloka, Elena Kostic, Yumiko Wada
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Patent number: 6548512Abstract: The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: January 27, 2000Date of Patent: April 15, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Donald Joseph Phillip Pinto, James Russell Pruitt, Joseph Cacciola, John Matthew Fevig, Qi Han, Michael James Orwat, Mimi Lifen Quan, Karen Anita Rossi
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Patent number: 6544997Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula —Alk—R6—, Alk—X—R7, —Alk—Y—C(═O)—R9, or —Alk—Y—C(═O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-Type: GrantFiled: June 8, 2001Date of Patent: April 8, 2003Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie André Bosmans, Ann Louise Gabriëlle Meulemans, Michel Anna Jozef De Cleyn, Henricus Jacobus Maria Gijsen
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Publication number: 20030064996Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.Type: ApplicationFiled: February 1, 2002Publication date: April 3, 2003Inventors: Mark T. Bilodeau, George D. Hartman, Peter J. Manley, Randall W. Hungate, Leonard Rodman
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Publication number: 20030060476Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about −10° C.Type: ApplicationFiled: October 2, 2002Publication date: March 27, 2003Applicant: Biochem Pharma Inc.Inventors: Tarek Mansour, Alex Cimpoia, Krzysztof Bednarski
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Publication number: 20030040524Abstract: This invention discloses compounds, and pharmaceutically acceptable salts, solvates and prodrugs thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii, Toxoplasma gondii, Mycobacterium tuberculosis, and Mycobacterium avium. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed. The compounds include 5-thiapyrimidines.Type: ApplicationFiled: June 27, 2002Publication date: February 27, 2003Inventor: Aleem Gangjee
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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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Publication number: 20030004347Abstract: The invention relates to compounds of the general formula 1Type: ApplicationFiled: November 5, 2001Publication date: January 2, 2003Inventors: Martin Eberle, Andre Jeanguenat, Werner Zambach, Arthur Steiger, Saleem Farooq
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Patent number: 6495555Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; n is 1 or 2; X1 is —O—, —S—, —S(═O)— or —S(═O)2—; each R1 is independently hydrogen, halogen, C1-6alkyl, nitro, hydroxy or C1-4alkyloxy; D is an optionally substituted mono, bi- or tricyclic nitrogen containing heterocycle, a 2H-benzopyranone, a benzamide, a benzophenone or a phenoxyphenyl having central &agr;2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.Type: GrantFiled: March 30, 2001Date of Patent: December 17, 2002Assignee: Janssen Pharmaceutica N.V.Inventors: Ludo Edmond Josephine Kennis, Frans Maria Alfons Van den Keybus, Josephus Carolus Mertens
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Publication number: 20020182625Abstract: Nucleic acid labeling compounds are disclosed. The compounds are synthesized by condensing a heterocyclic derivative with a cyclic group (e.g. a ribofuranose derivative). The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.Type: ApplicationFiled: March 12, 2002Publication date: December 5, 2002Inventors: Glenn McGall, Anthony D. Barone
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Patent number: 6489333Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein 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: April 9, 2001Date of Patent: December 3, 2002Assignee: Bristol - Meyers Squibb Pharma CompanyInventors: William J. Pitts, Prabhakar K. Jadhav
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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: 6440986Abstract: This invention concerns the use of the compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein A is CH, CR4 or N; n is 0 to 4; Q is hydrogen or —NR1R2; R1 and R2 are selected from hydrogen, hydroxy, C1-12alkyl, C1-12alkyloxy, C1-12alkylcarbonyl, C1-12alkyloxycarbonyl, aryl, amino, mono- or di(C1-12alkyl)amino, mono- or di(C1-12alkyl)aminocarbonyl wherein each C1-12alkyl may optionally be substituted; or R1 and R2 taken together may form pyrrolidinyl, piperidinyl, morpholinyl, azido or mono- or di(C1-12alkyl)aminoC1-4alkylidene; R3 is hydrogen, aryl, C1-6alkylcarbonyl, optionally substituted C1-6alkyl, C1-6alkyloxycarbonyl,; and R4 is hydroxy, halo, optionally substituted C1-6alkyl, C1-6alkyloxy, cyano, aminocarbonyl, nitro, amino, trihalomethyl, trihalomethyloxy; R5 is hydrogen or C1-4alkyl; L is optionally substituted C1-10alkyl, C3-10alkenyl, C3-10alkynyl, C3-7cycloalkyl; or L is —X1—R6 orType: GrantFiled: December 27, 2000Date of Patent: August 27, 2002Assignee: Janssen Pharmaceutica, N.V.Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc René De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Patent number: 6432963Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].Type: GrantFiled: June 15, 2000Date of Patent: August 13, 2002Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hiroyuki Hisamichi, Ryo Naito, Souichirou Kawazoe, Akira Toyoshima, Kazuhito Tanabe, Eiichi Nakai, Atsushi Ichikawa, Akiko Orita, Makoto Takeuchi
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Patent number: 6432947Abstract: N-Heterocyclic derivatives of the formula (I): are described herein, as well as other N-heterocycles, as inhibitors of nitric oxide synthase. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of nitric oxide synthase and processes for synthesizing these compounds are also described herein.Type: GrantFiled: August 26, 1999Date of Patent: August 13, 2002Assignees: Berlex Laboratories, Inc., Pharmacopeia, Inc.Inventors: Damian O. Arnaiz, John J. Baldwin, David D. Davey, James J. Devlin, Roland Ellwood Dolle, III, Shawn David Erickson, Kirk McMillan, Michael M. Morrissey, Michael H. J. Ohlmeyer, Gonghua Pan, Vidyadhar Madhav Paradkar, John Parkinson, Gary B. Phillips, Bin Ye, Zuchun Zhao
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Patent number: 6423720Abstract: This invention discloses compounds, and pharmaceutically acceptable salts, solvates and prodrugs thereof, useful in therapeutically and/or prophylactically treating patients with an illness. Such illnesses include cancer, and secondary infections caused by Pneumocystis carinii, Toxoplasma gondii, Mycobacterium tuberculosis, and Mycobacterium avium. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed. The compounds include 5-thiapyrimidines.Type: GrantFiled: February 1, 2001Date of Patent: July 23, 2002Assignee: Duquesne University of the Holy GhostInventor: Aleem Gangjee
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Patent number: 6410482Abstract: (Het)Arylsulfonylureas having an imino function, their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) and salts thereof in which A is a (hetero)aromatic or heterocyclic bridge linked to the group SO2 by a direct bond, or via O, S, NH, CH2 or via alkylated NH or alkylated methylene, B is a group having an imino-containing fragment N═C—N, N═C—S, N═C—O or N═C—C which is linked to A by one of the nitrogen atoms of the fragment, R═H or an aliphatic radical, W═O or S and X, Y and Z are as defined in claim 1 are suitable as herbicides and plant growth regulators. The preparation is carried out for example similarly to known processes via novel intermediates of the formula (XII) (cf.Type: GrantFiled: May 13, 1997Date of Patent: June 25, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer, Christopher Rosinger
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Patent number: 6410730Abstract: Compounds of formula 1, wherein R1 is CO2CH3, CON(CH3)2, OCH2CF3, N(CH3)COCH3, N(CH3)SO2CH3, CF3 or SO2C2H5; R2 is hydrogen or CF3; and M is sodium or potassium are prepared by reacting a compound of formula IV in an aprotic, organic solvent either with a compound of formula V or with NH3 in an aprotic, organic solvent to form a compound of formula III reacting this with a hydride, hydroxide, alcoholate, hydrogen carbonate or carbonate of sodium or potassium in an aprotic, organic solvent to form a compound of formula II and then with a compound of formula VI wherein R1 and R2 are as defined under formula I.Type: GrantFiled: February 9, 2001Date of Patent: June 25, 2002Assignee: Syngenta Crop Protection, Inc.Inventor: Andrea Rolf Sting
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Patent number: 6410729Abstract: Selected novel substituted pyrimidine compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: June 21, 2000Date of Patent: June 25, 2002Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo
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Patent number: 6387914Abstract: The subject invention concerns novel compounds that are useful as ultrashort acting hypnotic barbiturates. Specifically exemplified are derivatives of barbituric and thiobarbituric acids. They are rapidly metabolized by blood and tissue enzymes to form polar metabolites with no hypnotic activity and which are rapidly eliminated.Type: GrantFiled: April 24, 2001Date of Patent: May 14, 2002Assignee: ARYx TherapeuticsInventors: Pascal Druzgala, Peter G. Milner
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Publication number: 20020052495Abstract: Carboxylic acid derivatives 1Type: ApplicationFiled: December 27, 2000Publication date: May 2, 2002Inventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Publication number: 20020045635Abstract: The invention relates to nitro- and cyano-1,2,4,5-tetrahydro-heterocycloazepinyl pyrimidine derivatives as well as their pharmaceutically acceptable salts. The invention further relates to medicaments containing such compounds and a process for the preparation of such compounds. The compounds of the invention are group I mGluR antagonists and are therefore useful for the control or prevention of acute and/or chronic neurological disorders.Type: ApplicationFiled: July 11, 2001Publication date: April 18, 2002Inventors: Alfred Binggeli, Hans-Peter Maerki, Vincent Mutel, Maurice Wilhelm, Wolfgang Wostl
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Patent number: 6365739Abstract: Isocyanates of the formula (I) in which X and Y are defined as in formula (I) of claim 1 can be prepared by reacting a compound of the formula (II) or its salts in which X and Y are defined as in formula (I), with 1 to 6 mol of phosgene per mole of compound of the formula (II), in the presence of 2 to 3.5 molar equivalents of a base per mole of compound of the formula (II) and in the presence of an aprotic organic solvent at a reaction temperature in the range from −30 to +60° C. to give the compound of the formula (I). The compounds (I) can be converted by reaction with nucleophiles to give addition products, such as carbamates, ureas and sulfonylureas and corresponding products, e.g. herbicidal sulfonylureas.Type: GrantFiled: July 21, 1999Date of Patent: April 2, 2002Assignee: Hoechst Schering AgrEvo GmbHInventors: Mark James Ford, Stephen Lachhein
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Patent number: 6352993Abstract: The present invention relates to novel pyrimidine derivatives of formula (I) or pharmaceutically acceptable salts thereof which possess an excellent anti-secretory activity, pharmaceutical compositions containing the same as an active ingredient, their novel intermediates, and processes for the preparation thereof wherein: when A is piperidin-1-yl or —NH—B, wherein B is C3-C4 alkyl, C3-C4 alkenyl, C3-C7 cycloalkyl, C1-C3 alkoxyethyl, phenylethl which may be substituted or unsubstituted, 3-trifluoromethylphenylmethyl, 1-naphthylmethyl, 4-methylthiazol-2-yl or 4-phenylthiazol-2-yl, R1 is hydrogen or methyl; and R2, R3, R4 and R5 are hydrogen; or when A is a group of formula (II); when R1 is hydroxymethyl or C1-C3 alkoxymethyl, R2, R3, R4, R5 and R6 are hydrogen; and R7 is hydrogen or halogen; or when R1 is hydrogen or methyl, R7 is hydrogen or halogen; and one or two of R2, R3, R4, R5 and R6 is hydroxy, methoxy, or a group of formula (III) wherein Z is C1-C4 alkyl, substituted or unsubstituted C1-C4Type: GrantFiled: September 24, 1999Date of Patent: March 5, 2002Assignee: Yuhan CorporationInventors: Jong Wook Lee, Bong Yong Lee, Chang Seop Kim, Seung Kyu Lee, Keun Seog Song, Song Jin Lee, Woo Jeon Shim, Man Soon Hwang
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Publication number: 20020016297Abstract: The present invention relates to compounds of the formula 1 1Type: ApplicationFiled: December 20, 2000Publication date: February 7, 2002Inventors: Robert G. Linde, Matthew Merrill Hayward, Takushi Kaneko
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Patent number: 6342504Abstract: The present invention discloses peptide aldehydes which are potent and specific inhibitors of thrombin, their pharmaceutically acceptable salts, pharmaceutically acceptable compositions thereof, and methods of using them as therapeutic agents for disease states in mammals characterized by abnormal thrombosis.Type: GrantFiled: December 21, 1999Date of Patent: January 29, 2002Assignee: Corvas International, Inc.Inventors: Terence Kevin Brunck, Susan Y. Tamura, Joseph Edward Semple, Robert John Ardecky, Yu Ge, William Charles Ripka
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Patent number: 6329383Abstract: The present invention relates to new benzimidazole compounds with the following general structure (I): in which Y—X is >C═X when X is NR8, O, or S and R2 is H, alkyl, substituted alkylaryl or substituted aryl; or Y—X is >C—X when X is H, alkyl, substituted alkyl, aryl, substituted aryl, OR9 or NHR9 and R2 is a bond to Y; Z is O, S or NR12; R1 is H, alkyl, substituted alkyl, aryl or substituted aryl; R3 is H, alkyl, substituted alkyl, aryl or substituted aryl, OR9 or NHR9; R4, R5, R6 and R7 are H, halogen, OR10, NR10, R11, NO2, CF3, CN, COR8, COOR8, CONHR8 and/or N3 in any combination and/or two adjacent R4, R5, R6 or R7 form a carbocyclic or heterocyclic ring; and R8, R9, R10, R11, R12 and R13 are H, alkyl, substituted alkylaryl, aryl and/or substituted aryl in any combination. These compounds are useful as a human Growth Hormone (hGH) mimetic, which trigger GH agonist effects in animals and especially as an orally available human Growth Hormone (hGH).Type: GrantFiled: January 24, 2000Date of Patent: December 11, 2001Assignee: Pharmacia ABInventors: Charles Hedgecock, Eric Desarbre, Guido Kurz, Martin Norin, Marguerite Luthman, Cathrin Widerståhl
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Patent number: 6323210Abstract: Novel derivatives of 5-thia- and 5-selenopyrimidinone are sound to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.Type: GrantFiled: February 14, 2001Date of Patent: November 27, 2001Assignee: Agouron Pharmaceuticals, Inc.Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
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Publication number: 20010044444Abstract: Hair growth-/hair loss-affecting cosmetic/therapeutic compositions contain an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide having the structural formula (I): 1Type: ApplicationFiled: June 6, 2001Publication date: November 22, 2001Inventors: Yann Mahe, Jean-Francois Michelet, Patrick Pichaud, Jean-Baptiste Galey
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Publication number: 20010044535Abstract: This invention relates to novel heterocycles which are useful as antagonists of the &agr;v&bgr;3 integrin, the &agr;2b&bgr;3 integrin, and related cell surface adhesive protein 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: ApplicationFiled: April 9, 2001Publication date: November 22, 2001Inventors: William J. Pitts, Prabhakar K. Jadhav
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Patent number: 6316388Abstract: N-Heteroaryl-N′-(pyrid-2-yl-sulfonyl)ureas, processes for their preparation, and their use as herbicides and plant growth regulators Compounds of the formula (I) in which R1—R4, A, n, m and w are as defined in claim 1, are suitable as herbicides for controlling harmful plants and can be prepared, inter alia, from the sulfonamides of the formula (II) by reacting them with carbamates R*O—CO—NR4—A.Type: GrantFiled: November 3, 1994Date of Patent: November 13, 2001Assignee: Hoechst Schering AgrEvo GmbHInventors: Rainer Schütze, Heinz Kehne, Klaus Bauer, Hermann Bieringer
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Patent number: 6291468Abstract: Hair growth-/hair loss-affecting cosmetic/therapeutic compositions contain an effective amount of at least one 2-amino-4-alkylaminopyrimidine 3-oxide having the structural formula (I): in which R1 is an alkyl radical having from 5 to 20 carbon atoms, and Z is either a hydrogen atom or a radical —OR2, wherein R2 is an alkyl radical having from 1 to 12 carbon atoms, or an acyl derivative or acid addition salt thereof.Type: GrantFiled: July 23, 1999Date of Patent: September 18, 2001Assignee: Societe L'Oreal S.A.Inventors: Yann Mahe, Jean-Fran{tilde under (c)}ois Michelet, Patrick Pichaud, Jean-Baptiste Galey
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Publication number: 20010018443Abstract: Novel derivatives of 5-thia- and 5-selenopyrimidinone are found to inhibit the enzyme glycinamide ribonucleotide formyl transferase (GARFT) and amino imidazole carboxamide ribonucleotide formyl transferase (AICARFT). Novel intermediates of these compounds are also disclosed. A novel method of preparing such compounds is also disclosed, as well as methods and compositions for employing the compounds as antiproliferative agents.Type: ApplicationFiled: February 14, 2001Publication date: August 30, 2001Inventors: Michael D. Varney, William H. Romines, Cynthia L. Palmer, Judith G. Deal
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Patent number: 6274734Abstract: The present invention provides a process for the manufacture of pyrimidines of formula I: wherein R1, R2, R3 each independently represent hydrogen, C1-7-alkyl, or C1-7-alkoxy, A signifies —CN, a carbanionic R4-alkynyl residue, in which R4 is hydrogen or C1-7-alkyl, or a carbanionic residue of the malonic acid derivative of formula III in which B and B′ independently represent —CN, —COOR5, or —C(O)R5, wherein R5 is alkyl or aryl.Type: GrantFiled: March 16, 2000Date of Patent: August 14, 2001Assignee: Hoffman-La Roche Inc.Inventor: Wolfgang Göhring
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Patent number: 6274580Abstract: Compounds selected from the group consisting of formulae I, II, III, IV, VI, VII, and VIII wherein R is H or NH2, and pharmacologically acceptable salts thereof, are suitable for use in methods for treating non-insulin-dependent diabetes mellitus (NIDDM) or obesity in a patient susceptible to or experiencing NIDDM or obesity by the systemic administration of such a compound in an amount effective to treat the NIDDM or obesity.Type: GrantFiled: August 29, 2000Date of Patent: August 14, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Scott D. Larsen, Martin D. Meglasson, Valerie A. Vaillancourt, Paul D. May
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Patent number: 6271376Abstract: A process for the preparation of N-(amino-4,6-dihalopyrimidine)formamides of the formula: in which X is a halogen atom, starting from 2,5-diamino-4,6-dihalopyrimidine of the formula: in which X has the meaning afore-mentioned, by reaction with formic acid.Type: GrantFiled: December 16, 1999Date of Patent: August 7, 2001Assignee: Lonza AGInventors: Elie Saikali, Walter Brieden
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Publication number: 20010011094Abstract: This invention concerns the use of the compounds of formula 1Type: ApplicationFiled: December 27, 2000Publication date: August 2, 2001Inventors: Koenraad Jozef Lodewijk Marcel Andries, Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Marcel August Constant Janssen, Paul Adriaan Jan Janssen, Lucien Maria Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken
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Publication number: 20010008938Abstract: Compounds of formula 1, 1Type: ApplicationFiled: February 9, 2001Publication date: July 19, 2001Inventor: Andrea Rolf Sting
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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: 6235904Abstract: Abstract of the Disclosure: 2-Amino-(fluoroalkoxy)pyrimidines of the formula I where R1 is hydrogen, alkyl, alkenyl or alkynyl, R2 is hydrogen, halogen or haloalkyl, or else trifluoromethoxy or chlorodifluoromethoxy, R3 is hydrogen, halogen or C1-C4-haloalkyl and n is 0 or 1, are prepared as described.Type: GrantFiled: September 13, 1993Date of Patent: May 22, 2001Assignee: BASF AktiengesellschaftInventor: Gerhard Hamprecht