Pteridines (including Hydrogenated) Patents (Class 544/257)
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Patent number: 7626019Abstract: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.Type: GrantFiled: May 16, 2007Date of Patent: December 1, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Adil Duran, Guenter Linz
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Publication number: 20090270619Abstract: A method for selectively producing stable alpha form crystals of sapropterin hydrochloride is provided. In this method, the alpha form crystal of sapropterin hydrochloride is produced by dissolving sapropterin hydrochloride with hydrochloric acid at a concentration of not less than 4 mol/L at not less than 70 degrees C.; adding heated ethanol to the solution; and cooling the solution at a cooling rate of not faster than 3 degrees C./min to a temperature of 40 to 55 degrees C. to precipitate the crystals.Type: ApplicationFiled: April 13, 2006Publication date: October 29, 2009Applicant: Shiratori Pharmaceutical Co., Ltd.Inventors: Katsumi Hotoda, Hiroomi Kiyono, Shinnosuke Tazawa
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Patent number: 7550472Abstract: The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: November 18, 2005Date of Patent: June 23, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Horst Dollinger, Juergen Mack, Domnic Martyres, Birgit Jung, Peter Nickolaus
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Patent number: 7547780Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: December 18, 2007Date of Patent: June 16, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Matthias Hoffman, Christian Eickmeier
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Publication number: 20090131444Abstract: The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm blooded animals such as humans.Type: ApplicationFiled: May 23, 2006Publication date: May 21, 2009Applicant: ASTRAZENECA ABInventors: Folkert Reck, Marshall Morningstar, Hajnalka Hartl
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Publication number: 20090124628Abstract: The present invention relates to new 2-benzylaminodihydropteridinones of general formula (I) wherein the groups R1 to R7, R10 and R11 have the meanings given in the claims and specification, the isomers thereof, methods of preparing these dihydropteridinones and their use as medicaments.Type: ApplicationFiled: January 22, 2009Publication date: May 14, 2009Applicant: Boehringer Ingelheim International GmbHInventors: Matthias HOFFMANN, Matthias GRAUERT, Thorsten LEHMANN-LINTZ, Martin STEEGMAIER, Flavio SOLCA, Norbert REDEMANN
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Publication number: 20090088439Abstract: The present invention relates to novel compounds of the general formula (I) wherein R1, R2, R3 and R4 are as defined, having a positive allosteric GABAB receptor (GBR) modulator effect, methods for the preparation of said compounds and to their use, optionally in combination with a GABAB agonist, for the inhibition of transient lower esophageal sphincter relaxations, for the treatment of gastroesophageal reflux disease, as well as for the treatment of functional gastrointestinal disorders and irritable bowel syndrome (IBS).Type: ApplicationFiled: September 26, 2008Publication date: April 2, 2009Inventors: Leifeng Cheng, Maria Jonforsen, Peter Schell
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Publication number: 20090081145Abstract: The present invention relates to an improved method of formation of disulfide bridges in substances bearing SH groups, in particular peptides, for example by formation of intramolecular disulfide bridges, in which a heterocyclic compound having at least one nitrogen atom (e.g. caffeine or a caffeine-like substance) is used for catalysis of the reaction. It was found, surprisingly, that addition of the heterocyclic substance increases both the yield and the purity of the product bearing disulfide bridges.Type: ApplicationFiled: December 23, 2006Publication date: March 26, 2009Applicant: AplaGen GmbHInventors: Karsten Knorr, Marco Emgenbroich, Carsten Bungener
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Publication number: 20090042890Abstract: Provided herein are Heteroaryl Compounds having the following structure: wherein R1, R3, R4, L, X, Y, A and B are as defined herein, compositions comprising an effective amount of a Heteroaryl Compound and methods for treating or preventing cancer, inflammatory conditions, immunological conditions, metabolic conditions and conditions treatable or preventable by inhibition of a kinase pathway comprising administering an effective amount of a Heteroaryl Compound to a patient in need thereof.Type: ApplicationFiled: October 18, 2007Publication date: February 12, 2009Inventors: Deborah Sue Mortensen, Maria Mercedes Delgado Mederos, John Joseph Sapienza, Ronald J. Albers, Steven Spencer Clareen, Kimberly Lyn Schwarz, Jason Simon Parnes, Jennifer R. Riggs, Patrick William Papa, Sayee Gajanan Hegde, Jeffrey Mark McKenna
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Publication number: 20080319192Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: ApplicationFiled: August 15, 2008Publication date: December 25, 2008Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Matthias GRAUERT, Matthias HOFFMANN, Martin STEEGMAIER, Flavio SOLCA, Jens Juergen QUANT
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Patent number: 7439358Abstract: The present invention relates to a specific salt of a dihydropteridione derivative, namely the trihydrochloride salt of the compound N-[trans-4-[4-(cyclopropylmethyl)-1-piperazinyl]cyclohexyl]-4-[[(7R)-7-ethyl-5,6,7,8-tetrahydro-5-methyl-8-(1-methylethyl)-6-oxo-2-pteridinyl]amino]-3-methoxy-benzamide, to its crystallisation in the form of an hydrate with water, to a process for the manufacture thereof, and to the use thereof in a pharmaceutical composition.Type: GrantFiled: January 30, 2007Date of Patent: October 21, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Guenter Linz, Peter Sieger, Matthias Grauert, Rolf Schmid
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Patent number: 7429581Abstract: The present invention is directed to a compound of formula I, in which R0; R1; R2; R3; R4; Q; V, G and M have the meanings indicated below. The compound of formula I is a pharmacologically active compound. It exhibits a strong anti-thrombotic effect and is suitable, for example, for the therapy and prophylaxis of a cardio-vascular disorder like a thromboembolic disease or restenosis. It is a reversible inhibitor of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is intended. The invention furthermore is directed to a process for the preparation of the compound of formula I, and pharmaceutical preparation comprising it.Type: GrantFiled: December 23, 2003Date of Patent: September 30, 2008Assignee: Sanofi-Aventis Deutschland GmbHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20080234277Abstract: The invention is concerned with novel aza-pyridopyrimidinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, X1, X2, X3, Y, Z, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds are HM74A agonists and can be used in treating or preventing diseases which are modulated by HM74A agonists.Type: ApplicationFiled: March 17, 2008Publication date: September 25, 2008Inventors: Aurelia Conte, Henrietta Dehmlow, Uwe Grether, Nicole A. Kratochwil, Holger Kuehne, Robert Narquizian, Constantinos G. Panousis, Jens-Uwe Peters, Fabienne Ricklin
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Patent number: 7414053Abstract: Disclosed are new dihydropteridinones of the formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings provided herein, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: August 19, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Flavio Solca, Jens Juergen Quant
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Publication number: 20080171747Abstract: Disclosed are new dihydropteridinones of general formula (I) wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, intermediates and processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.Type: ApplicationFiled: November 16, 2007Publication date: July 17, 2008Inventors: Matthias Hoffman, Matthias Grauert, Trixi Brandl, Steffen Breitfelder, Christian Eickmeier, Martin Steegmaier, Gisela Schnapp, Anke Baum, Jens Juergen Quant, Flavio Solca, Florian Colbatzky
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Publication number: 20080153833Abstract: The invention relates to new pteridines which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: ApplicationFiled: February 14, 2008Publication date: June 26, 2008Inventors: Horst Dollinger, Juergen Mack, Domnic Martyres, Birgit Jung, Peter Nickolaus
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Publication number: 20080146579Abstract: The invention pertains to a method and compositions for treatment or prevention of chronic pulmonary dysfunction in a patient.Type: ApplicationFiled: December 15, 2006Publication date: June 19, 2008Inventors: Erwin Peke MEIJER, George Verlaan, Maarteen Anne Hoijer
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Patent number: 7332491Abstract: Disclosed are new dihydropteridinones of general formula (I) whereby the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and their use as pharmaceutical compositions.Type: GrantFiled: August 24, 2005Date of Patent: February 19, 2008Assignee: Boehringer Ingelheim International, GmbHInventors: Matthias Grauert, Matthias Hoffmann, Martin Steegmaier, Christian Eickmeier, Gisela Schnapp, Norbert Redemann, Flavio Solca, Jens Juergen Quant
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Patent number: 7238807Abstract: Disclosed are processes for the preparation of fused piperazin-2-one derivatives of general formula (I) wherein the groups R1 to R5, A1 and A2 have the meanings given in the claims and in the description, particularly the preparation of 7,8-dihydro-5H-pteridin-6-one derivatives and intermediates thereof.Type: GrantFiled: November 22, 2005Date of Patent: July 3, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Adil Duran, Guenter Linz
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Patent number: 7169778Abstract: Disclosed are compounds of Formulae (Ia), (Ib), (Ic), (Id) wherein: W is NH, S, SO, or SO2; R2 is (un)substituted aryl, (un)substituted heteroaryl, or (un)substituted carbocycle or heterocycle; Q is hydrogen or lower alkyl; R4 and R6 are the same or different and represent hydrogen, halogen, lower alkyl, lower alkoxy, (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl; and R8 is hydrogen, lower alkyl or an (un)substituted carbocyclic group containing from 3–7 members, up to two of which members are optionally hetero atoms selected from oxygen and nitrogen; or R8 is (un)substituted aryl, (un)substituted heteroaryl, (un)substituted arylalkyl or (un)substituted heteroarylalkyl. These compounds are useful for treating cell proliferative disorders, such as cancer and restenosis. These compounds are potent inhibitors of cyclin-dependent kinases (cdks) and growth factor-mediated kinases.Type: GrantFiled: June 21, 2000Date of Patent: January 30, 2007Assignee: Warner-Lambert CompanyInventors: William Alexander Denny, Gordon William Rewcastle, Ellen Dobrusin, James Bernard Kramer, Dennis Joseph McNamara, Howard Daniel Hollis Showalter, Peter Laurence Toogood
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Patent number: 7148224Abstract: The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1, is H or optionally substituted lower alkyl, etc., R2 is H, etc., R3 and R4 are the same or different and are each H, etc., R5 and R6 are the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.Type: GrantFiled: April 14, 2005Date of Patent: December 12, 2006Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
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Patent number: 7074929Abstract: This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y.Type: GrantFiled: November 10, 2003Date of Patent: July 11, 2006Assignees: Neurogen Corp., Pfizer, Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Patent number: 7067658Abstract: The present invention provides compounds of Formula I: wherein the variables A, B, Ar, R1, R2, and R3 are as defined herein. The compounds of Formula (I) can function as corticotropin releasing factor (CRF) receptor antagonists and can be useful, for example, in the treatment of disorders characterized by abnormal levels of CRF such as anxiety and depression.Type: GrantFiled: September 26, 2003Date of Patent: June 27, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Thais Motria Sielecki-Dzurdz, Argyrios George Arvanitis, Carolyn Diane Dzierba
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Patent number: 6989446Abstract: Process for the preparation of compounds of formula I wherein the general symbols are as defined in claim 1, which process comprises reacting a compound of formula V wherein the general symbols are as defined in claim 1, with carbon monoxide in the presence of a catalyst.Type: GrantFiled: June 12, 2002Date of Patent: January 24, 2006Assignee: Ciba Specialty Chemicals Corp.Inventors: Michael Tinkl, Samuel Evans, Peter Nesvadba
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Patent number: 6946465Abstract: Novel poly-substituted pteridinediones (lumazines), and mono- or polysubstituted 2-thiolumazines, 4-thiolumazines or 2,4-dithiolumazines, having disclosed substituents in positions 1, 3, 6 and 7 of the pteridine ring, and pharmaceutically acceptable salts thereof, being represented by the general formula (I). are useful as biologically active ingredients in preparing pharmaceutical compositions especially for the treatment or prevention of a CNS disorder, a cell proliferative disorder, a viral infection, an immune or auto-immune disorder or a transplant rejection. Combinations of the pteridine derivatives of the invention with an immunosuppressant or immunomodulator drug, an antineoplastic drug or an antiviral agent, providing potential synergistic effects, are also disclosed.Type: GrantFiled: May 23, 2003Date of Patent: September 20, 2005Assignee: 4 AZA Bioscience NVInventors: Mark Jozef Albert Waer, Piet André Maurits Maria Herdewijn, Wolfgang Eugen Pfleiderer
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Patent number: 6914062Abstract: The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1 is H or optionally substituted lower alkyl, etc., R2 is H, etc., R3 and R4 are the same or different and are each H, etc., R5 and R6 are the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.Type: GrantFiled: June 28, 2001Date of Patent: July 5, 2005Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Takashi Hayama, Nobuhiko Kawanishi, Tooru Takaki
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Patent number: 6894173Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl-and heteroaryl-substituted urea compounds of the formula(I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.Type: GrantFiled: February 10, 2003Date of Patent: May 17, 2005Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Lin-Hua Zhang, Lei Zhu
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Patent number: 6894041Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; —G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recitType: GrantFiled: November 20, 2002Date of Patent: May 17, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6869945Abstract: This application is directed to compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where Y is ?C(R1a)— or —[N?(O)k]— where k is 0 or 1; G1 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G1 is not a discontinuous or restricted biaryl moiety as defined under G2; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G2 is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic; or that is a 7- to 12-membered, fused polycyclic; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems reType: GrantFiled: November 20, 2002Date of Patent: March 22, 2005Assignee: Pfizer IncInventors: Anthony Marfat, Michael William McKechney
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Patent number: 6861422Abstract: The present invention relates to new dihydropteridinones of general formula (I): wherein the groups L and R1-R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropteridinones and the use thereof as pharmaceutical compositions.Type: GrantFiled: February 26, 2003Date of Patent: March 1, 2005Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Matthias Hoffmann, Matthias Grauert, Trixi Brandl, Steffen Breitfelder, Christian Eickmeier, Martin Steegmaier, Gisela Schnapp, Anke Baum, Jens Juergen Quant, Flavio Solca, Florian Colbatzky
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Publication number: 20040242582Abstract: A cell population expressing folate receptors is selectively targeted with a folate mimetic. The folate mimetic is conjugated to a diagnostic or therapeutic agent to enable selective delivery of the agent to the targeted cell population.Type: ApplicationFiled: June 21, 2004Publication date: December 2, 2004Inventors: Mark A Green, Chun-Yen Ke, Christophe P Leamon
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Publication number: 20040229870Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor.Type: ApplicationFiled: November 10, 2003Publication date: November 18, 2004Applicants: NEUROGEN CORPORATION, PFIZER INC.Inventors: Raymond F. Horvath, Jennifer N. Tran, Stephane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Publication number: 20040220404Abstract: A compound of formula (Ia) comprising a pharmaceutically acceptable salt or solvate thereof, formulations, processes of preparing, and methods of administering to mammals are provided 1Type: ApplicationFiled: April 14, 2004Publication date: November 4, 2004Inventors: Andrew J Carpenter, Joel P Cooper, Anthony L Handlon, Donald L Hertzog, Clifton E Hyman, Yu C Guo, Jason E Speake, David Richard Witty
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Patent number: 6806272Abstract: The present invention relates to new dihydropteridinones of the formula (I) wherein the groups X, R1, R2, R3, R4, R5 and R7 have the meanings given in the claims and the specification, the isomers thereof, processes and intermediates for preparing these dihydropteridinones as well as the use thereof as pharmaceutical compositions.Type: GrantFiled: August 23, 2002Date of Patent: October 19, 2004Assignee: Boehringer Ingelheim Pharma KGInventors: Eckhart Bauer, Steffen Breitfelder, Christian Eickmeier, Matthias Grauert, Matthias Hoffmann, Thorsten Lehmann-Lintz, Gerald Pohl, Jens Quant, Norbert Redemann, Gisela Schnapp, Martin Steegmaier
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Publication number: 20040204406Abstract: The present invention is directed to a compound of formula I, 1Type: ApplicationFiled: December 23, 2003Publication date: October 14, 2004Applicant: AVENTIS PHARMA DEUTSCHLAND GMBHInventors: Marc Nazare, Volkmar Wehner, David W. Will, Hans Matter
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Publication number: 20040152704Abstract: Compounds of formula (I) 1Type: ApplicationFiled: October 22, 2003Publication date: August 5, 2004Inventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-Yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani, Michael P. Curtis
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Publication number: 20040138219Abstract: Piperidine derivatives of formula (I) and pharmaceutically derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.Type: ApplicationFiled: January 26, 2004Publication date: July 15, 2004Inventors: David Thomas Davies, Graham Elgin Jones, Roger Edward Markwell, William Miller, Neil David Pearson
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Patent number: 6762188Abstract: Compounds of formula (I) or salts thereof, wherein the dotted Line represents a single or double bond, R1 is alkyl or amino optionally substituted by alkyl, alkanoyl or benzyl group; R2, R3, R4 and R5 are the same or different and each is selected from hydrogen, phenyl, halo, nitro, a group S(O)nR8 wherein n is the integer 0, 1 or 2 and R8 is halo or alkyl or a group NR9R10 wherein R9 and R10 are both hydrogen, a group NR11R12 wherein R11 and R12 are the same or different and each is hydrogen or alkyl, a group OR13 wherein R13 is hydrogen or C1-4 of alkyl optionally substituted by halo; a C1-4 aliphatic group optionally substituted by a group OR14 or NR14R15 wherein R14 and R15 are the same or different and each is hydrogen or alkyl; or two of R2 to R5 are linked together to form a benzo group, or one of R2 to R5 is a group X—Y—R16 wherein X is CH2, NR17, CO or S(O)m and Y is CH2, NR17, O or S(O)m, or X—Y is O, NR17, —CH═CH— or N═N—, are disclosed as pharmacologicType: GrantFiled: September 12, 2001Date of Patent: July 13, 2004Assignee: SmithKline Beecham CorporationInventors: William Pendergast, Scott Howard Dickerson, Julius Vass Johnson, Robert Ferone
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Publication number: 20040116438Abstract: Compounds, compositions and methods useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.Type: ApplicationFiled: May 22, 2003Publication date: June 17, 2004Inventors: Pu-Ping Lu, David J. Morgans, Bing Yao, Dashyant Dhanak, Steven David Knight
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Publication number: 20040110692Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstituted propanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: ApplicationFiled: October 28, 2003Publication date: June 10, 2004Applicant: Magnesium Diagnostics, Inc.Inventor: Ibert Clifton Wells
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Patent number: 6740654Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the saltType: GrantFiled: July 5, 2001Date of Patent: May 25, 2004Assignee: Celltech R & D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Publication number: 20040092521Abstract: Compounds of formula (I) 1Type: ApplicationFiled: November 12, 2002Publication date: May 13, 2004Inventors: Robert J. Altenbach, Lawrence A. Black, Sou-Jen Chang, Marlon D. Cowart, Ramin Faghih, Gregory A. Gfesser, Yi-yin Ku, Huaqing Liu, Kirill A. Lukin, Diana L. Nersesian, Yu-ming Pu, Padam N. Sharma, Youssef L. Bennani
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Publication number: 20040092739Abstract: This invention relates to a process for synthesizing certain folic acid analogues, which are useful in treating cancer, inflammatory diseases, autoimmune diseases, and are commonly referred to as antifolates. The process employs improved steps for annulation, derivatization and addition reactions to produce the described antifolates from commonly available starting materials.Type: ApplicationFiled: July 25, 2003Publication date: May 13, 2004Inventors: Zejun Xiao, Harry Kochat
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Publication number: 20040082784Abstract: The present invention provides compounds of Formula I: 1Type: ApplicationFiled: September 26, 2003Publication date: April 29, 2004Inventors: Thais Motria Sielecki-Dzurdz, Argyrios George Arvanitis, Carolyn Diane Dzierba
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Publication number: 20040077859Abstract: This invention relates to a group of trisubstituted and tetrasubstituted pteridine derivatives, their pharmaceutically acceptable salts, N-oxides, solvates, dihydro- and tetrahydroderivatives and enantiomers, possessing unexpectedly desirable pharmaceutical properties, in particular which are highly active immunosuppressive agents, and as such are useful in the treatment in transplant rejection and/or in the treatment of certain inflammatory diseases. These compounds are also useful in preventing or treating cardiovascular disorders, allergic conditions, disorders of the central nervous system and cell proliferative disorders.Type: ApplicationFiled: August 29, 2003Publication date: April 22, 2004Inventors: Mark Jozef Albert Waer, Piet Andre Maurits Maria Herdewijn, Wolfgang Eugen Pfleiderer
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Publication number: 20040043984Abstract: This invention provides compounds defined by Formula I 1Type: ApplicationFiled: August 5, 2003Publication date: March 4, 2004Inventor: Patrick Michael O'Brien
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Patent number: 6696443Abstract: Certain compounds which contain a piperidine moiety flanked by aryl groups are inhibitors of p38-&agr; kinase and thus useful in the treatment of a variety of conditions characterized by inappropriate p38-&agr; kinase activity.Type: GrantFiled: November 20, 2001Date of Patent: February 24, 2004Assignee: Scios, Inc.Inventors: Babu Mavunkel, Sundeep Dugar, Gregory Luedtke, Xuefei Tan, Glenn McEnroe
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Publication number: 20040019210Abstract: This invention provides phenyl-substituted pyrimidopyrimidines, dihydropyrimido-pyrimidines, pyridopyrimidines, naphthyridines, and pyridopyrazines of the general formula: 1Type: ApplicationFiled: July 17, 2003Publication date: January 29, 2004Inventors: Cleo J. Chivikas Connolly, Christopher James Deur, James Marino Hamby, Denton Wade Hoyer, Chris Limberakis, Jessica Elizabeth Reed, Mel Conrad Schroeder, Clarke Taylor
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Patent number: RE39198Abstract: 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 amounts of one 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 15, 2000Date of Patent: July 18, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: Joseph T. Strupczewski, Grover C. Helsley, Yulin Chiang, Kenneth J. Bordeau, Edward J. Glamkowski