Phthalazines (including Hydrogenated) Patents (Class 544/237)
-
Patent number: 7432263Abstract: Compounds which are amino-phthalazinone derivatives according to formula 1 and pharmaceutically acceptable salts thereof, together with pharmaceutical compositions comprising them are disclosed; these compounds or compostions are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, cell proliferative disorders, Alzheimer's disease, viral infections, autoimmune diseases and neurodegenerative disorders.Type: GrantFiled: July 30, 2002Date of Patent: October 7, 2008Assignee: Pfizer Italia, S.r.l.Inventor: Maurizio Pulici
-
Publication number: 20080234278Abstract: The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.Type: ApplicationFiled: May 1, 2008Publication date: September 25, 2008Inventors: Thomas Trieselmann, Bradford S. Hamilton
-
Publication number: 20080233601Abstract: Disclosed are compounds having the formula: wherein R1 is selected from the group consisting of hydrogen, C1-C6 alkyl, amino, N-C1-C6-alkylamino, and N,N—C1-C6-dialkylamino; and ring “A” is selected from the group consisting of unsubstituted or substituted C4-C8-cycloalkenyl, unsubstituted or substituted bicyclo [2,2,1]alkenyl, and unsubstituted or substituted bicyclo [2,2,2]alkenyl, unsubstituted phenyl, and phenyl substituted with a moiety selected from the group consisting of C3-C6-alkenyl, acryl, acryl-C1-C6 alkyl, acrylamido, and acrylamido-C1-C6 alkyl; polymers made from these compounds, and ELISAs that use the compounds and polymers as a chemiluminescent detection label.Type: ApplicationFiled: March 24, 2008Publication date: September 25, 2008Inventors: Joseph Thomas Ippoliti, Joshua Cole Speros
-
Patent number: 7423030Abstract: A 1-amino-phthalazine derivative of general formula (I) wherein the substituents are as defined herein. Also disclosed are a method for preparing such compounds, intermediates for use in such method and medical treatments using the compounds of formula (I).Type: GrantFiled: October 11, 2006Date of Patent: September 9, 2008Assignee: Sanofi-AventisInventors: Jean Michel Augereau, Michel Geslin, Gilles Courtemanche
-
Publication number: 20080200469Abstract: Compounds of the formula (I): wherein A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are both hydrogen, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R1 is selected from H and halo.Type: ApplicationFiled: April 24, 2008Publication date: August 21, 2008Inventors: Niall Morrison Barr Martin, Graeme Cameron Smith, Stephen Philip Jackson, Vincent Junior M Loh, Xiao-Ling Fan Cockcroft, Ian Timothy Williams Matthews, Keith Allan Menear, Frank Kerrigan, Alan Ashworth
-
Publication number: 20080194569Abstract: Compounds of the formula I, in which R, R1, R2, R3, R4, R5, R6, R7, R8, Z1, Z2, Z3 and Y1 have the meanings indicated in claim 1, can be employed, inter alia, for the treatment of tumoursType: ApplicationFiled: February 21, 2006Publication date: August 14, 2008Inventors: Hans-Peter Buchstaller, Dirk Finsinger, Kai Schiemann, Ulrich Emde, Frank Zenke, Christiane Amendt
-
Patent number: 7407957Abstract: A compound of formula (I): for use in treating cancer or other diseases ameliorated by the inhibition of PARP, wherein: A and B together represent an optionally substituted, fused aromatic ring; X can be NRX or CRXRY; if X=NRX then n is 1 or 2 and if X=CRXRY then n is 1; RX is selected from the group consisting of H, optionally substituted C1-20 alkyl, C5-20 aryl, C3-20 heterocyclyl, amido, thioamido, ester, acyl, and sulfonyl groups; RY is selected from H, hydroxy, amino; or RX and RY may together form a spiro-C3-7 cycloalkyl or heterocyclyl group; RC1 and RC2 are independently selected from the group consisting of hydrogen and C1-4 alkyl, or when X is CRXRY, RC1, RC2, RX and RY, together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; R1 is selected from H and halo; and Het is selected from: where Y1 is selected from CH and N, Y2 is selected from CH and N, Y3 is selected from CH, CF and N, where only one or two of Y1, Y2 and Y3 can be N; andType: GrantFiled: August 26, 2005Date of Patent: August 5, 2008Assignees: Maybridge Limited, Kudos Pharmaceuticals LimitedInventors: Muhammad Hashim Javaid, Graeme Cameron Murray Smith, Naill Morrison Barr Martin, Sylvie Gomez, Vincent Junior Ming-lai Loh, Xiao-Ling Fan Cockcroft, Stefano Forte, Keith Allan Menear, Ian Timothy William Matthews, Frank Kerrigan
-
Patent number: 7407955Abstract: The present invention relates to substituted xanthines of general formula wherein R1 to R3 are defined as in claims 1 to 16, the tautomers, the stereoisomers, the mixtures, the prodrugs thereof and the salts thereof which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: August 12, 2003Date of Patent: August 5, 2008Assignee: Boehringer Ingelheim Pharma GmbH & Co., KGInventors: Frank Himmelsbach, Elke Langkopf, Matthias Eckhardt, Michael Mark, Roland Maier, Ralf R. H. Lotz, Mohammad Tadayyon
-
Patent number: 7405215Abstract: The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.Type: GrantFiled: September 21, 2005Date of Patent: July 29, 2008Assignee: WyethInventors: Youssef L. Bennani, Lawrence Nathan Tumey, Elizabeth Ann Gleason, Michael Joseph Robarge
-
Patent number: 7402580Abstract: Fused pyridazine derivatives represented by formula (I) or pharmaceutically acceptable salts thereof (wherein each symbol has the meaning as defined in the specification.). Because of inhibiting poly(ADP-ribose)polymerase, the compounds represented by formula (I) are useful as preventives and/or remedies for various ischemic diseases (in brain, cord, heart, digestive tract, skeletal muscle, retina, etc.), inflammatory diseases (inflammatory bowel disease, multiple cerebrosclerosis, arthritis, etc.), neurodegenerative diseases (extrapyramidal disorder, Alzheimer's disease, muscular dystrophy, lumbar spinal canal stenosis, etc.), diabetes, shock, head trauma, renal failure, hyperalgesia, etc. Moreover, these compounds are useful as agents against retroviruses (HIV etc.), sensitizers in treating cancer and immunosuppressants.Type: GrantFiled: February 18, 2003Date of Patent: July 22, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Takuya Seko, Jun Takeuchi, Shinya Takahashi, Yoshihisa Kamanaka, Wataru Kamoshima
-
Publication number: 20080161280Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.Type: ApplicationFiled: December 27, 2007Publication date: July 3, 2008Applicant: Abbott LaboratoriesInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
-
Publication number: 20080146576Abstract: The present invention relates to phthalazin-1-ylpiperidin-4-ylamides of the general formula I, to processes for their preparation and to their use for producing pharmaceutical compositions for treatment of disorders and indications connected to the EP2 receptor.Type: ApplicationFiled: September 6, 2007Publication date: June 19, 2008Inventors: Nico Braeuer, Bernd Buchmann, Koppitz Marcus, Antonius Ter Laak, Gernot Langer, Bernard Lindenthal, Olaf Peters, Tim Wintermantel
-
Publication number: 20080146575Abstract: 4-[3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl]-2H-phthalazin-1-one as crystalline Form A.Type: ApplicationFiled: October 17, 2007Publication date: June 19, 2008Inventors: Keith Allan Menear, Anthony Peter Ottridge, Derek John Londesbrough, Michael Raymond Hallett, Keith Raymond Mulholland, John David Pittam, David Dermot Patrick Laffan, Ian Woodward Ashworth, Martin Francis Jones, Janette Helen Cherryman
-
Publication number: 20080146544Abstract: The present invention provides analogs of a Lysofylline (LSF), and synthetic methods for the preparation of such analogs. The have the active side chain moiety (5-R-hydroxyhexyl) of LSF and can have greater potency and oral bioavailability than LSF.Type: ApplicationFiled: February 25, 2008Publication date: June 19, 2008Inventors: Timothy L. MacDonald, Jerry L. Nadler, Peng Cui
-
Publication number: 20080146547Abstract: The present invention relates to novel phthalazine derivatives and, more particularly, to phthalazine derivatives that are useful as protein kinase inhibitors. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: November 14, 2007Publication date: June 19, 2008Applicant: Forest Laboratories Holdings LimitedInventors: Gian-Luca Araldi, Matthew Ronsheim, Melanie Ronsheim
-
Patent number: 7388006Abstract: The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.Type: GrantFiled: March 11, 2003Date of Patent: June 17, 2008Assignee: Bayer Schering Pharma AGInventors: Norbert Schmees, Manfred Lehmann, Ulrike Fuhrmann, Peter Muhn, Christa Hegele-Hartung, Michael Klotzbuecher
-
Publication number: 20080139538Abstract: The present invention is directed to tertiary carbinamine compounds having substituted heterocycles, which are inhibitors of the beta-secretase enzyme, and are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: ApplicationFiled: January 13, 2006Publication date: June 12, 2008Inventors: Georgia B. McGaughey, Philippe G. Nantermet, Hemaka A. Rajapakse, Shaun R. Stauffer
-
Publication number: 20080132499Abstract: Compounds are provided which are useful as platelet ADP receptor inhibitors, for treating thrombosis and for reducing the likelihood and/or severity of a secondary ischemic event in a patient.Type: ApplicationFiled: September 17, 2007Publication date: June 5, 2008Applicant: Portola Pharmaceuticals, Inc.Inventors: Robert M. Scarborough, Carroll Anna Crew Scarborough, Shawn M. Bauer, Anjali Pandey
-
Publication number: 20080125435Abstract: The present invention relates to aryl-3-[(het)aryl-piperidin-4-yl]-thioureas, processes for the production thereof and the use thereof for the production of pharmaceutical agents for the treatment of diseases and indications which are connected with the EP2 receptor.Type: ApplicationFiled: September 6, 2007Publication date: May 29, 2008Inventors: Nico Brauer, Bernd Buchmann, Christoph Huwe, Marcus Koppitz, Antonius Ter Laak, Gernot Langer, Bernhard Lindenthal, Olaf Peters, Tim Wintermantel
-
Publication number: 20080119468Abstract: The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I wherein A1, A2, B, R1, R2, R3 and R4 are defined herein. The invention also comprises pharmaceutical compositions including one or more compounds of Formula I, uses of such compounds and compositions for treatment of kinase mediated diseases including rheumatoid arthritis, psoriasis and other inflammation disorders, as well as intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: September 4, 2007Publication date: May 22, 2008Applicant: Amgen Inc.Inventors: Andrew Tasker, Dawei Zhang, Liping H. Pettus, Rob M. Rzasa, Kelvin K.C. Sham, Shimin Xu, Partha Chakrabarti
-
Publication number: 20080096883Abstract: The invention relates to trifluoromethyl substituted benzamide compounds of the formula (I), pharmaceuticals comprising these compounds, their use as or for the manufacture of pharmaceuticals, particularly as inhibitors of protein kinases and/or the treatment of a condition, disorder or disease state mediated by a protein kinase activity and/or a proliferative disease, methods of treatment comprising administering the compounds, especially of therapeutic and prophylactic treatment, methods for the manufacture of the compounds and novel intermediates and partial steps for their synthesis.Type: ApplicationFiled: August 10, 2005Publication date: April 24, 2008Inventors: Giorgio Caravatti, Pascal Furet, Patricia Imbach, Georg Martiny-Baron, Lawrence Blas Perez, Tao Sheng
-
Publication number: 20080070915Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compnounds of formula (I) wherein R1, R2, R3, L, X, Y and Z have defined meanings.Type: ApplicationFiled: June 28, 2005Publication date: March 20, 2008Inventors: Jerome Emile Georges Guillemont, Ludo Edmond Josephine Kennis, Josephus Carolus Mertens, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
-
Patent number: 7329659Abstract: The present invention provides a compound of formula (I): in which Ar and R1 are phenyl or a heteroaromatic group, R2 is generally hydrogen, R3 is hydrogen or alkyl and X, Y and Z are generally CH or N as VR-1 antagonists; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; use of it to manufacture medicaments to treat pain or inflammation; and methods of treating pain or inflammationType: GrantFiled: April 5, 2004Date of Patent: February 12, 2008Assignee: Merck Sharp & Dohme LimitedInventors: Peter Blurton, Frank Burkamp, Stephen Robert Fletcher, A. Brian Jones, Edward Giles McIver
-
Patent number: 7312214Abstract: The present application describes 1,1-disubstituted cycloalkyl compounds and derivatives thereof, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: May 5, 2003Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Donald J. Pinto, Michael J. Orwat, Sarah R. Friedrich, Wei Han
-
Patent number: 7265115Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, are useful for controlling synaptic transmission in mammals.Type: GrantFiled: April 11, 2003Date of Patent: September 4, 2007Assignee: Abbott LaboratoriesInventors: William H. Bunnelle, Daniela Barlocco Cristina, Jerome F. Daanen, Michael J. Dart, Michael D. Meyer, Keith B. Ryther, Michael R. Schrimpf, Kevin B. Sippy, Richard B. Toupence
-
Patent number: 7232826Abstract: The present invention provides compounds of Formula I or II that are useful as anti-cancer agents and other diseases that can be treated by inhibiting tyrosine kinase enzymesType: GrantFiled: September 29, 2003Date of Patent: June 19, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Upender Velaparthi, Mark D. Wittman
-
Patent number: 7226923Abstract: Compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates are disclosed. Also disclosed are methods for the preparation of the above-mentioned compounds, pharmaceutical compositions containing them, as well as the use of the above-mentioned compounds in the treatment, control or prevention of illnesses such as cancer.Type: GrantFiled: September 23, 2005Date of Patent: June 5, 2007Assignee: Hoffman-La Roche Inc.Inventors: Edward Boyd, Frederick Brookfield, Guy Georges, Bernhard Goller, Sabine Huensch, Petra Rueger, Matthias Rueth, Stefan Scheiblich, Christine Schuell, Wolfgang von der Saal, Justin Warne, Stefan Weigand
-
Patent number: 7220746Abstract: The compounds of formula I in which the substituents have the meanings as indicated in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: August 6, 2003Date of Patent: May 22, 2007Assignee: Altana Pharma AGInventor: Geert Jan Sterk
-
Patent number: 7220858Abstract: The present invention relates to both a novel method of preparing hydralazine hydrochloride and to a novel method of preparing hydrazine derivatives of compounds containing a pyridazine ring, including, for example, pyridazines, phthalazines and other compounds containing the pyridazine ring.Type: GrantFiled: December 23, 2003Date of Patent: May 22, 2007Assignee: Barbeau Pharma, Inc.Inventor: Deanna J. Nelson
-
Patent number: 7196085Abstract: A compound of formula: or an isomer, salt, solvate, chemically protected form, or prodrug thereof, wherein A and B together represent an optionally substituted, fused aromatic ring; RL is a C5-7 aryl group substituted in the meta position by the group R2, and optionally further substituted; wherein R2 is selected from: and its use as a pharmaceutical, in particular for the treatment of diseases ameliorated by inhibiting the activity of PARP.Type: GrantFiled: April 29, 2003Date of Patent: March 27, 2007Assignees: KuDOS Pharmaceuticals Limited, Maybridge plcInventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Penny Jane Eversley, Xiao-Ling Cockcroft, Frank Kerrigan, Janet Hoare, Lesley Dixon
-
Patent number: 7186710Abstract: The compounds of formula I in which R1, R2, R3, R4 and R5 have the meanings as given in the description are PDE4/7 inhibitors.Type: GrantFiled: April 23, 2002Date of Patent: March 6, 2007Assignee: Altana Pharma AGInventor: Geert Jan Sterk
-
Patent number: 7186720Abstract: The present invention relates to compounds of formula (I): in which X represents N or CH; R1 represents a hydrogen or halogen atom or a CF3 group; R2 and R3 independently represent a hydrogen atom or a methyl group; n is 0 or 1; A represents an optionally substituted nitrogenous heterocycle; and to their N-oxides and to their salts or solvates, to the pharmaceutical compositions and the medicaments comprising them, and to a process for their preparation.Type: GrantFiled: April 19, 2002Date of Patent: March 6, 2007Assignee: Sanofi-AventisInventors: Marco Baroni, Bernard Bourrie, Pierre Casellas
-
Patent number: 7179810Abstract: The compounds of formula I in which the given substituents have the meanings as given in the description, are novel effective PDE4 inhibitors.Type: GrantFiled: June 3, 2005Date of Patent: February 20, 2007Assignee: Altana Pharma AGInventors: Gerhard Grundler, Beate Schmidt, Geert Jan Sterk
-
Patent number: 7176312Abstract: General methods for the solution phase as well as solid phase synthesis of various substituted heteroaryls has been demonstrated. These substituted heteroaryls can be further elaborated by aromatic substitution with amines at elevated temperature or by anilines, boronic acids and phenols via palladium catalyzed cross-coupling reactions.Type: GrantFiled: October 12, 2002Date of Patent: February 13, 2007Assignees: The Scripps Research Institute, IRM LLCInventors: Sheng Ding, Qiang Ding, Nathanael S. Gray
-
Patent number: 7151102Abstract: A method of treatment of a disease of the human or animal body mediated by PARP comprising administering to such a subject a therapeutically effective amount of a compound of formula: or an isomer, salt, solvate, chemically protected form, and prodrug thereof, wherein: A and B together represent an optionally substituted, fused aromatic ring; RC is represented by —L—RL, where L is of formula: —(CH2)n1-Qn2-(CH2)n3— wherein n1, n2 and n3 are each selected from 0, 1, 2 and 3, the sum of n1, n2 and n3 is 1, 2 or 3 and Q is selected from O, S, NH, C(?O) or —CR1R2—, where R1 and R2 are independently selected from hydrogen, halogen or optionally substituted C1-7 alkyl, or may together with the carbon atom to which they are attached form a C3-7 cyclic alkyl group, which may be saturated (a C3-7 cycloalkyl group) or unsaturated (a C3-7 cycloalkenyl group), or one of R1 and R2 may be attached to an atom in RL to form an unsaturated C3-7 cycloalkenyl group which comprises the carbon atoms to which R1 and R2 are aType: GrantFiled: October 30, 2001Date of Patent: December 19, 2006Assignees: Kudos Pharmaceuticals Limited, Maybridge PLCInventors: Niall Morrison Barr Martin, Graeme Cameron Murray Smith, Charles Richard White, Roger Frank Newton, Diane Gillian Douglas, Penny Jane Eversley, Julia Vile
-
Patent number: 7135471Abstract: Aryl oxime derivatives of the formula (I), in which R1, R2, R3, X and B are as defined in claim 1, act as phosphodiesterase IV inhibitors and can be employed for the treatment of osteoporosis, tumours, cachexia, atherosclerosis, rheumatoid arthritis, multiple sclerosis, diabetes mellitus, inflammatory processes, allergies, asthma, autoimmune diseases, myocardial diseases and AIDSType: GrantFiled: May 16, 2003Date of Patent: November 14, 2006Assignee: Merck Patent GmbHInventors: Hans-Michael Eggenweiler, Norbert Beier, Pierre Schelling, Michael Wolf
-
Patent number: 7132418Abstract: The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.Type: GrantFiled: July 25, 2002Date of Patent: November 7, 2006Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Michael J. Costanzo, Bruce E. Maryanoef, Stephen C. Yabut
-
Patent number: 7125863Abstract: Compounds according to formula (1), wherein R1 is H or CN, X1 is S, O, SO2 or CH2, X2 is CO, CH2 or a covalent bond, Het is a nitrogen-containing heterocycle and n is 1–5 are new. The compounds of the invention are inhibitors of dipeptidyl peptidase IV.Type: GrantFiled: April 26, 2001Date of Patent: October 24, 2006Assignee: Ferring BVInventors: David Michael Evans, Gary Robert William Pitt
-
Patent number: 7122544Abstract: Compounds having activity as inhibitors of IKK are disclosed, particularly IKK-2. The compounds of this invention are anilinopyrimidine derivatives having the following structure: wherein R1 and R6 are as defined herein. Such compounds have utility in the treatment of a wide range of conditions that are responsive to IKK inhibition. Thus, methods of treating such conditions are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.Type: GrantFiled: December 4, 2001Date of Patent: October 17, 2006Assignee: Signal Pharmaceuticals, LLCInventors: Adam Kois, Karen J. MacFarlane, Yoshitaka Satoh, Shripad S. Bhagwat, Jason S. Parnes, Moorthy S. S. Palanki, Paul E. Erdman
-
Patent number: 7115646Abstract: The present application describes cyclic diamino compounds, derivatives thereof, and pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of factor Xa.Type: GrantFiled: October 6, 2004Date of Patent: October 3, 2006Assignee: Bristol Myers Squibb, Co.Inventor: Jennifer X. Qiao
-
Patent number: 7091209Abstract: A class of 2-aryl-4,5-dihydroxy-6-carboxypyrimidines of formula (I): wherein Ar is an optionally substituted aryl or heterocyclicgroup; as well as compounds of formula (I) which are derivatized at one or more of the 4-hydroxy, 5-hydroxy or 6-carboxy groups; and tautomers thereof, and pharmaceutically acceptable salts or esters thereof; and inhibitors of viral polymerases, especially the hepatitis C virus (HCV) polymerase enzymeType: GrantFiled: July 11, 2001Date of Patent: August 15, 2006Assignee: Merck & Co., Inc.Inventors: Cristina Gardelli, Claudio Giuliano, Steven Harper, Uwe Koch, Frank Narjes, Jesus Maria Ontoria Ontoria, Marco Poma, Simona Ponzi, Ian Stansfield, Vincenzo Summa
-
Patent number: 7053093Abstract: Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof, wherein W, Q, X, X1, Y and Z are as defined herein. These compounds bind with high selectivity and/or high affinity to the benzodiazepine site of GABAA receptors and are therefore useful in the treatment of central nervous system (CNS) diseases and as probes for the localization of GABAA receptors in tissue samples. Also disclosed are intermediates useful in the preparation of these compounds.Type: GrantFiled: January 28, 2003Date of Patent: May 30, 2006Assignee: Neurogen CorporationInventors: Jun Yuan, Pamela Albaugh, Kenneth Shaw, Alan Hutchison
-
Patent number: 7045522Abstract: The present invention relates to novel 8-azabicyclo[3.2.1]oct-2-ene and -octane derivatives which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: December 4, 2003Date of Patent: May 16, 2006Assignee: Neurosearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon Feldbaek Nielsen, Elsebet Ostergaard Nielsen
-
Patent number: 7037880Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.Type: GrantFiled: August 8, 2002Date of Patent: May 2, 2006Assignee: Nissan Chemical Industries, Ltd.Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
-
Patent number: 7030239Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) useful in treating Alzheimer's disease and other similar diseases.Type: GrantFiled: May 18, 2004Date of Patent: April 18, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Roy Hom, Shumeye S. Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Y. Fang
-
Patent number: 7030120Abstract: Disclosed are compounds represented by formula (I) which have triglyceride biosynthesis inhibitory activity in the liver and inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein from the liver and particularly have excellent inhibitory activity against the secretion of apolipoprotein B-containing lipoprotein, are free from side effect of accumulation of lipids in the liver, and are useful for the treatment and prevention of hyperlipidemia and arteriosclerotic diseases.Type: GrantFiled: June 16, 2004Date of Patent: April 18, 2006Assignee: Meiji Seika Kaisha, Ltd.Inventors: Naoto Ohkura, Yukiko Hiraiwa, Tetsuya Matsushima, Kazue Sasaki, Takehiro Yamamoto, Masaharu Shiotani, Shigeki Suzuki, Yuuko Nakatani, Chizuko Kuroda, Mieko Nagasawa, Kiyoaki Katano
-
Patent number: 7022696Abstract: The compounds of formula I in which R1, R2, R3, A, X, s and R9 have the meanings as given in the description are novel effective PDE4 inhibitors.Type: GrantFiled: April 24, 2002Date of Patent: April 4, 2006Assignee: Altana Pharma AGInventors: Gerhard Grundler, Beate Schmidt, Geert Jan Sterk
-
Patent number: 6989447Abstract: Aminopiperidine derivatives and pharmaceutically acceptable derivatives thereof useful in methods of treatment of bacterial infections in mammals, particularly in man.Type: GrantFiled: November 24, 2003Date of Patent: January 24, 2006Assignee: SmithKline Beecham p.l.c.Inventors: Roger Edward Markwell, Neil David Pearson
-
Patent number: 6982264Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: GrantFiled: June 27, 2002Date of Patent: January 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Roy Hom, John Tucker
-
Patent number: 6953853Abstract: The compounds of a formula I, in which the given substituents have the meanings as given in the description, are novel effective PDE4 inhibitorsType: GrantFiled: February 14, 2002Date of Patent: October 11, 2005Assignee: Altana Pharma AGInventors: Gerhard Grundler, Beate Schmidt, Geert Jan Sterk