At 2-position Patents (Class 544/330)
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Publication number: 20090227592Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).Type: ApplicationFiled: February 2, 2009Publication date: September 10, 2009Applicant: AstraZeneca ABInventors: Scott BOYD, Peter William Rodney CAULKETT, Rodney Brian HARGREAVES, Suzanne Saxon BOWKER, Roger JAMES, Clifford David JONES, Darren McKERRECHER, Michael Howard BLOCK, Craig JOHNSTONE
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Publication number: 20090203710Abstract: Provided are a histamine-H3 receptor antagonist; and a preventive and/or a remedy for metabolic system diseases such as obesity, diabetes, hormone secretion disorder, hyperlipemia, gout, fatty liver, circulatory system diseases, for example, stenocardia, acute/congestive cardiac insufficiency, cardiac infarction, coronary arteriosclerosis, hypertension, nephropathy, sleep disorder and various diseases accompanied by sleep disorder such as idiopathic hypersomnia repetitive hypersomnia, true hypersomnia, narcolepsy, sleep periodic acromotion disorder, sleep apnea syndrome, circadian rhythm disorder, chronic fatigue syndrome, REM sleep disorder, senile insomnia, night worker sleep insanitation, idiopathic insomnia, repetitive insomnia, true insomnia, electrolyte metabolism disorder; and central and peripheral nervous system diseases such as bulimia, emotional disorder, melancholia, anxiety, epilepsy, delirium, dementia, shinzophrenia, attention deficit/hyperactivity disorder, memory disorder, Alzheimer's diseaseType: ApplicationFiled: March 6, 2009Publication date: August 13, 2009Inventors: Norikazu Ohtake, Ryo Yoshimoto, Shigeru Tokita, Akio Kanatani, Sayaka Mizutani
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Patent number: 7563894Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.Type: GrantFiled: October 31, 2007Date of Patent: July 21, 2009Assignees: IRM LLC, Novartis AGInventors: Valentina Molteni, Shuli You, Juliet Nabakka, Yi Liu, Xiaolin Li, Donatella Chianelli, Jon Loren, Xiaodong Liu, Shifeng Pan, Donald S. Karanewsky, Pascal Furet, Vito Guagnano
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Patent number: 7538215Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: June 2, 2005Date of Patent: May 26, 2009Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Christopher Semko, Christopher Joseph Soares, Christine M. Tarby
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Patent number: 7524849Abstract: This invention relates to certain 5-arylpyrimidine compounds or a pharmaceutically acceptable salt thereof, and compositions containing said compounds or a pharmaceutically acceptable salt thereof, wherein said compounds are anti-cancer agents useful for the treatment of cancer in mammals. This invention further relates to a method of treating or inhibiting the growth of cancerous tumor cells and associated diseases in a mammal and further provides a method for the treatment or prevention of cancerous tumors that express multiple drug resistance (MDR) or are resistant because of MDR, in a mammal in need thereof which method comprises administering to said mammal an effective amount of said compounds or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 24, 2004Date of Patent: April 28, 2009Assignee: Wyeth Holdings CorporationInventors: Nan Zhang, Semiramis Ayral-Kaloustian, Thai Nguyen
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Publication number: 20090099208Abstract: This invention relates to novel guanidine derivatives useful as modulators of small-conductance calcium-activated potassium channels (SK channels). In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: March 22, 2007Publication date: April 16, 2009Inventors: Ulrik Svane Sorensen, Birgitte L. Eriksen, Lene Teuber, Dan Peters, Dorte Strobaek, Tina Holm Johansen, Palle Christophersen
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Patent number: 7514447Abstract: Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors.Type: GrantFiled: September 26, 2006Date of Patent: April 7, 2009Assignees: IRM LLC, Novartis AGInventors: Valentina Molteni, Xiaolin Li, Donatella Chianelli, Jon Loren, Juliet Nabakka, Xiadong Liu, Shifeng Pan, Yi Liu, Donald S. Karanewsky, Pascal Furet, Vito Guagnano, Shuli You
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Patent number: 7511140Abstract: An improved process for manufacture of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl)(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid calcium salt, which is useful for the production of a pharmaceutical useful in the treatment of, inter alia, hypercholesterolemia, hyperlipoproteinemia and atherosclerosis, is described.Type: GrantFiled: August 7, 2003Date of Patent: March 31, 2009Assignee: AstraZeneca ABInventors: John Horbury, Nigel Philip Taylor
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Patent number: 7501417Abstract: This invention comprises the novel compounds of formula (I) wherein n, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: March 11, 2003Date of Patent: March 10, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Kristof Van Emelen, Hans Louis Jos De Winter, Alexey Borisovich Dyatkin, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Jimmy Arnold Viviane Van heusden
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Patent number: 7501415Abstract: Described herein are compounds that are useful as ERK2 inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including proliferative disorders such as cancer.Type: GrantFiled: December 20, 2005Date of Patent: March 10, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alexander Aronov, Michael Hale, Francois Maltais, Gabriel Martinez-Botella, Judith Straub, Qing Tang
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Publication number: 20090054392Abstract: The present invention relates to naphthylpyrimidine analogs, methods of making naphthylpyrimidine analogs, compositions comprising a naphthylpyrimidine analog, and methods for treating canonical Wnt-?-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analog.Type: ApplicationFiled: August 19, 2008Publication date: February 26, 2009Applicant: WyethInventors: Jeffrey Claude Pelletier, Luciana de Araujo Felix, Daniel Michael Green, Diane Barbara Hauze, Joseph Theodore Lundquist, IV, Charles William Mann, John Francis Mehlmann, John Francis Rogers, JR., Matthew Douglas Vera, Albert John Molinari
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Publication number: 20090048280Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.Type: ApplicationFiled: December 28, 2006Publication date: February 19, 2009
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Publication number: 20090048282Abstract: The present invention relates to pyrimidine sulfonamide analogs, methods of making pyrimidine sulfonamide analogs, compositions comprising a pyrimidine sulfonamide analog, and methods for treating canonical Wnt-?-catenin cellular messaging system-related disorders comprising administering to a subject in need thereof an effective amount of a pyrimidine sulfonamide analog.Type: ApplicationFiled: August 14, 2008Publication date: February 19, 2009Applicant: WyethInventors: Diane Barbara Hauze, Matthew Gregory Bursavich, Luciana de Araujo Felix, Adam Matthew Gilbert, Jeffrey Claude Pelletier
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Patent number: 7491821Abstract: Compounds of formula 1 are modulators of P2X3 useful for the treatment of pain and genitourinary, gastrointestinal, and respiratory disorders: wherein R1 is —C(?S)CH3, pyridyl, pyrimidinyl, pyrazinyl, thiazolyl, furyl, furylcarbonyl, acetyl, or carbamoyl; R2a and R2b are independently H, methyl, or ethyl; R3 is H or methyl; Y is a bond, —(CR4R5)n— or —CR4?CR5—; wherein R4 and R5 are each independently H or methyl and n is 1 or 2; X is N or CH; A is phenyl, 5-membered heterocyclyl, or 6-membered heterocyclyl; R6, R7 and R8 are each independently H, halo, lower alkyl, cycloalkyl, alkylthio, alkylthio-lower alkyl, alkylsulfonyl-lower alkyl, di(lower alkyl)amino-lower alkyl, morpholinyl-lower alkyl, 4-methyl-piperazinyl-methyl, trifluoromethyl, pyridyl, tetrazolyl, thiophenyl, phenyl, biphenyl, or benzyl (where thiophenyl, phenyl and benzyl are substituted with 0-3 lower alkyl, halo, sulfonamido, trifluoromethyl, lower alkoxy or lower alkylthio) or R6 and R7 together form a 5-membered or 6-membered carbocyclType: GrantFiled: August 11, 2006Date of Patent: February 17, 2009Assignee: Roche Palo Alto LLCInventors: Christine E. Brotherton-Pleiss, Michael Patrick Dillon, Shelley K. Gleason, Clara Jeou Jen Lin, Ryan Craig Schoenfeld, Marzia Villa, Yansheng Zhai
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Patent number: 7488727Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable derivative thereof. These compounds are inhibitors of protein kinases, particularly inhibitors of GSK3, Aurora2, and Syk mammalian protein kinases. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: June 15, 2007Date of Patent: February 10, 2009Assignee: Vertex Pharmaceuticals IncorporatedInventors: John Cochran, Suganthini Nanthakumar, Edmund Harrington, Jian Wang
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Patent number: 7482356Abstract: The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2?]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2?]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.Type: GrantFiled: November 5, 2004Date of Patent: January 27, 2009Assignee: The Procter & Gamble CompanyInventors: Michael Philip Clark, Steven Karl Laughlin, Adam Golebiowski, Todd Andrew Brugel, Mark Sabat
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Patent number: 7473695Abstract: The present invention relates to a compound of the formula [I]: wherein G1 is an alkyl which is substituted by a halogen atom or an alkoxy, or a group of the formula: wherein ring B is benzene ring which may be substituted, etc., Q1 and Q2 maybe the same or different, and each is hydrogen atom, a halogen atom or an alkyl, n is 0, 1, 2, 3 or 4, R1 is hydrogen atom, an alkyl which may be substituted, a cycloalkyl which may be substituted, a phenyl which may be substituted, etc., Z1, Z2, Z3 and Z4 may be the same or different, and each is CH or N, provided that 3 or more of Z1, Z2, Z3 and Z4 should not be N at the same time, G2 is hydrogen atom, —NR3R4, —OR5, etc., where R3 to R8 each is independently hydrogen atom, an alkyl which may be substituted, an alkenyl, an alkynyl, etc., or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 20, 2004Date of Patent: January 6, 2009Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Akira Kubo, Ritsuo Imashiro, Hiroaki Sakurai, Hidetaka Miyoshi, Akihito Ogasawara, Hajime Hiramatsu, Tatsuo Nakajima, Tetsu Nakane
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Patent number: 7462619Abstract: In accordance with the present invention, there is provided a novel class of heterocyclic compounds. Compounds of the invention contain a substituted or unsubstituted six membered heterocyclic ring that includes at least two nitrogen atoms. The ring additionally includes four carbon atoms. The heterocyclic ring has at least one substituent located at a ring position adjacent to a ring nitrogen atom. This mandatory substituent of the ring includes a moiety (B), linked to the heterocyclic ring via a carbon-carbon triple bond. The mandatory substituent is positioned adjacent to the ring nitrogen atom. Invention compounds are capable of a wide variety of uses. For example heterocyclic compounds can act to modulate physiological processes by functioning as agonists and antagonists of receptors in the nervous system. Invention compounds may also act as insecticides, and as fungicides. Pharmaceutical compositions containing invention compounds also have wide utility.Type: GrantFiled: April 1, 2005Date of Patent: December 9, 2008Assignee: Merck & Co., Inc.Inventors: Nicholas D. Cosford, Jeffrey R. Roppe, Lida R. Tehrani, Nicholas D. Smith, Brian Stearns, Dehua Huang, Bowei Wang, Thomas J. Seiders
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Publication number: 20080300266Abstract: The present invention relates to compounds of the Formula (I) which are useful for treating conditions associated with mGluR3 receptors, such as depression, schizophrenia and migraine, pharmaceutical compositions thereof, and methods of using the same.Type: ApplicationFiled: October 13, 2005Publication date: December 4, 2008Applicant: Eli Lilly And CompanyInventors: Thomas Charles Britton, Veronique Dehlinger, Colin Peter Dell, Bruce Anthony Dressman, Jason Kenneth Myers, Eric Samuel Nisenbaum
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Patent number: 7459460Abstract: Trisubstituted heteroaromatic compounds having the structure are provided, wherein X is C or N; A and B are each independently CH or N, with the proviso that A and B cannot both be CH; R1 is Ar-L-; R2 is hydrogen or alkyl; or R1 and R2 can be joined together to form a 4- to 7-membered cycloheteroalkyl ring; R3 to R8, Ar and L are as defined herein. A method for using these compounds to treat diseases associated with abnormal bone or mineral homeostasis is also provided.Type: GrantFiled: May 26, 2004Date of Patent: December 2, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Wu Yang, John K. Dickson, Christopher B. Cooper, Dharmpal S. Dodd, Zheming Ruan, Dora M. Schnur
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Patent number: 7459454Abstract: The present invention relates to aminopyrazine derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medcicaments. Such aminopyrazine derivatives are useful in the treatment of diseases associated with inappropriate tyrosine and/or serine/threonine kinase activity.Type: GrantFiled: March 18, 2004Date of Patent: December 2, 2008Assignee: SmithKline Beecham CorporationInventors: Michael John Alberti, David Harold Drewry, David Drysdale Miller, Paul Bamborough
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Publication number: 20080293942Abstract: The present invention is directed to a novel, high yield method for preparing 2-imidazol-1-yl-4-methyl-6-pyrrolidin-2-yl-pyrimidine, particularly to a method of preparing 4-(1-alkylpyrrolidin-2-yl)-2-(1H-imidazol-1-yl)-6-methylpyrimidine, more particularly, 2-(2-(2-(1H-imidazol-1-yl)-6-methylpyrimidin-4-yl)pyrrolidrn-1-yl)-N-(benzo[d][1,3]dioxol-5-yh-nethyl)-N-methylethanamine. These compounds and pharmaceutical compositions thereof are inhibitors of nitric oxide synthase, are selective for inducible nitric oxide synthase, and are useful in treating diseases and disorders including inflammation and pain.Type: ApplicationFiled: November 27, 2006Publication date: November 27, 2008Inventor: Russell D. Cousins
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Patent number: 7446109Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: March 11, 2003Date of Patent: November 4, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
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Publication number: 20080262007Abstract: HIV replication inhibitors of formula a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein A is —CH2—CH2—, —CH?CH—, —C?C—; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl, R2 hydroxy, halo, C1-6alkyl, carboxyl, cyano, —C(?O)R6, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl; X1 is —NR1—, —O—, —S—, —S(?O)p—; R3 is H, C1-6alkyl, halo; R4 is H, C1-6alkyl, halo; R5 is nitro, amino, mono- and diC1-4alkylamino, aryl, halo, —CHO, —CO—R6, —COOR7, —NH—C(?O)H, —NH—C(?O)R6, —CH?N—O—R8; R6 is C1-4alkyl, amino, mono- or di(C1-4alkyl)amino or polyhaloC1-4alkyl; R7 is hydrogen, C1-6alkyl, arylC1-6alkyl; R8 is hydrogen, C1-6alkyl, aryl; p is 1 or 2; aryl is optionally substituted phenyl; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compounds and compositions.Type: ApplicationFiled: September 29, 2005Publication date: October 23, 2008Inventors: Jerome Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Patent number: 7423148Abstract: Compounds having formula I are provided where the variables have the values described herein. Pharmaceutical formulations include the compounds or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier and combinations with other agents. A method of treating a patient comprises administering a pharmaceutical formulation according to the invention to a patient in need thereof.Type: GrantFiled: November 21, 2003Date of Patent: September 9, 2008Assignee: Chiron CorporationInventors: John N. Nuss, Sabina Pecchi, Paul A. Renhowe
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Publication number: 20080207590Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.Type: ApplicationFiled: October 26, 2007Publication date: August 28, 2008Applicant: METHYLGENE INC.Inventors: Robert Deziel, Silvana Leit, Patrick Beaulieu, Yves Andre Chantigny, John Mancuso, Pierre Tessier, Gideon Shapiro, Richard Chesworth, David Smil
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Patent number: 7414011Abstract: Disclosed are compounds of the formula (I) or salts thereof in which R1, R2, R3, R4, I, R5, Q, R4, W, X, Y, V and Z, are as defined in the specification, which are suitable for use as herbicides or plant growth regulators. Also disclosed are processes for preparing the compounds of formula (I) or salts thereof.Type: GrantFiled: September 12, 2005Date of Patent: August 19, 2008Assignee: Hoechst Schering Agrevo GmbHInventors: Hansjörg Dietrich, Christian Waldraff, Lothar Willms, Hermann Bieringer, Christopher Rosinger, Felix Thürwächter, Thomas Auler
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Patent number: 7414046Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: May 23, 2003Date of Patent: August 19, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul Charifson, Dean Stamos, Yusheng Liao, Michael Badia, Martin Trudeau
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Patent number: 7399856Abstract: Processes for the preparation of 4-[[4-[[4-(2-cyanoethenyl)-2,6-dimethylphenyl]-amino]-2-pyrimidinyl]amino]benzonitrile of formula (I), a N-oxide, a pharmaceutically acceptable acid addition salt, a quaternary amine or a stereochemically isomeric form thereof are provided, said processes comprise: a) reacting 4-(2-cyanoethenyl)-2,6-dimethylbenzenamine with an intermediate of formula (III) ?in the presence of a suitable solvent; b) reacting an intermediate of formula (IV) ?with acrylonitrile in the presence of a suitable palladium catalyst, a suitable base and a suitable solvent; c) dehydrating the corresponding amide of the compound of formula (I).Type: GrantFiled: August 7, 2003Date of Patent: July 15, 2008Assignee: Janssen Pharmaceutica N.V.Inventors: Didier Philippe Robert Schils, Joannes Josephus Maria Willems, Bart Petrus Anna Maria Jozef Medaer, Elisabeth Therese Jeanne Pasquier, Paul Adriaan Jan Janssen, Jan Heeres, Ruben Gerardus George Leenders, Jérôme Emile Georges Guillemont
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Patent number: 7396836Abstract: A compound having excellent adenosine receptor (A1, A2A, A2B receptor) antagonistic action, of the following formula, a salt thereof or a solvate of them: wherein, R1 and R2, same or different, each represents a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, a cycloalkyl group, a cycloalkenyl group, an aromatic hydrocarbon cyclic group, an acyl group or an alkylsulfonyl group, which groups may be substituted (except the hydrogen atom); R3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group, an alkenyl group, an alkynyl group, an aromatic hydrocarbon cyclic group, a nitrogen atom, an oxygen atom or a sulfur atom, which groups may be substituted (except the hydrogen atom, the halogen atom and the cyano group); R4 represents an aromatic hydrocarbon cyclic group which may be substituted, and R5 represents an aromatic hydrocarbon cyclic group which may be substituted.Type: GrantFiled: October 22, 2002Date of Patent: July 8, 2008Assignee: Eisai R&D Management Co., Ltd.Inventors: Hitoshi Harada, Masato Ueda, Yoshihiko Kotake, Masahiro Yasuda, Daisuke Iida, Junichi Nagakawa, Makoto Nakagawa
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Patent number: 7396927Abstract: The present invention provides processes for preparing calcium salts of statin, particularly rosuvastatin calcium salt substantially free of impurities on an industrial scale.Type: GrantFiled: August 24, 2004Date of Patent: July 8, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Valerie Niddam-Hildesheim, Greta Sterimbaum
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Publication number: 20080146595Abstract: The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.Type: ApplicationFiled: December 13, 2007Publication date: June 19, 2008Inventors: Denis John Kestesz, Christine E. Brotherton-Pleiss, Minmin Yang
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Publication number: 20080135803Abstract: The invention relates to a high dielectric anisotropy liquid crystal compound which is a pyridyl derivative with substituents of electrons push-pull effect. Furthermore, the high dielectric anisotropy liquid crystal compounds are colorless and have high thermal and photo stability as well as high compatibility in a liquid crystal host. A liquid crystal composition containing the high dielectric anisotropy liquid crystal compound can reduce threshold voltage of cholesteric reflective displays, thus saving power and extending lifetime of driver ICs.Type: ApplicationFiled: December 3, 2007Publication date: June 12, 2008Inventors: Kung-Lung Cheng, Shib-Hsien Liu, Ann-Cheng Chen, Peu-Jane Haung, Chih-Lung Chin
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Publication number: 20080125417Abstract: At least one chemical entity chosen from compounds of Formula 1 and pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, and mixtures thereof, is described herein. Pharmaceutical compositions comprising at least one chemical entity of Formula 1, together with at least one pharmaceutically acceptable vehicle chosen from carriers adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: September 11, 2007Publication date: May 29, 2008Inventors: Kevin S. Currie, Tony Lee, James W. Darrow, Peter A. Blomgren
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Patent number: 7371759Abstract: Compounds are provided having the following structure which are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia, dyslipidemia, hormone replacement therapy, hypercholsterolemia, hypertriglyceridemia and atherosclerosis as well as Alzheimer's disease and osteoporosis wherein X is N or CR5; and pharmaceutically acceptable salts thereof, wherein R1 to R7 are as defined herein. A method for treating the above diseases employing the above compounds is also provided.Type: GrantFiled: September 21, 2004Date of Patent: May 13, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Jeffrey A. Robl, Khehyong Ngu
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Patent number: 7358239Abstract: The present invention concerns compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein -Z1-Z2- is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical of formula; Alk is optionally substituted C1-6alkanediyl; the bivalent radical is a substituted piperidinyl, an optionally substituted pyrrolidinyl, homopiperidinyl, piperazinyl or tropyl; R5 is a radical of formula wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or ?NR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q isType: GrantFiled: March 14, 2005Date of Patent: April 15, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Marcel Frans Leopold De Bruyn, Kristof Van Emelen, Piet Tom Bert Paul Wigerinck, Wim Gaston Verschueren
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Patent number: 7358359Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: GrantFiled: July 22, 2005Date of Patent: April 15, 2008Assignee: University of WashingtonInventors: Niels H. Andersen, Jason Bowman
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Patent number: 7351711Abstract: The present invention is directed to substituted indanyl compounds of Formula (I): Useful for treating integrin-mediated disorders such as, but not limited to unstable angina, thromboemboic disorders, osteoporosis, growth and metastasis of malignant tumors, diabetic retinopathy, arthritis, viral disease and surgical adhesions.Type: GrantFiled: July 28, 2004Date of Patent: April 1, 2008Assignee: Janssen Pharmaceutical, N.V.Inventors: William A. Kinney, Diane K. Luci, Bruce E. Maryanoff
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Patent number: 7348335Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: November 5, 2003Date of Patent: March 25, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Randy S. Bethiel, Young-Choon Moon
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Patent number: 7332485Abstract: Novel PDF inhibitors and novel methods for their use are provided.Type: GrantFiled: July 8, 2004Date of Patent: February 19, 2008Assignee: SmithKline Beecham CorpInventors: Kelly M. Aubart, Siegfried Benjamin Christensen, IV, Chaya Duraiswami, Joseph M. Karpinski
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Patent number: 7321033Abstract: The invention is directed to 3-?-D-ribofuranosylthiazolo[4,5-d]pyridimine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.Type: GrantFiled: June 7, 2004Date of Patent: January 22, 2008Assignee: Anadys Pharmaceuticals, Inc.Inventors: Devron R. Averett, Stephen E. Webber, Joseph R. Lennox, Erik J. Rueden, David Louis Clark, Alan Xin Xiang
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Patent number: 7312216Abstract: The invention relates to N-phenyl-2-pyrimidine-amine derivatives of formula I wherein the substituents are defined as indicated in the description, to processes for the preparation thereof, to medicaments comprising those compounds, and to the use thereof in the preparation of pharmaceutical compositions for the therapeutic treatment of warm-blooded animals, including humans.Type: GrantFiled: June 7, 2006Date of Patent: December 25, 2007Assignee: Novartis AGInventors: Hans M Buerger, Giorgio Caravatti, Uerg Zimmermann, Paul W Manley, Werner Breitenstein, Margaret A Cudd
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Patent number: 7312329Abstract: An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to theType: GrantFiled: December 3, 2004Date of Patent: December 25, 2007Assignee: Glenmark Pharmaceuticals LimitedInventors: Narendra Joshi, Shekhar Bhaskar Bhirud, Batchu Chandrasekhar, K. Eswara Rao, Subhash Damle
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Patent number: 7312227Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of utilizing those compounds and compositions in the treatment of various protein kinase mediated disorders.Type: GrantFiled: November 3, 2003Date of Patent: December 25, 2007Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark Ledeboer, Brian Ledford
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Patent number: 7309704Abstract: The present invention relates to compounds represented by the structural Formula I: or a pharmaceutically acceptable salt thereof, which are useful for the treatment of metabolic and eating disorders such as obesity and hyperphagia, and for the treatment of diabetes and associated disorders.Type: GrantFiled: August 24, 2005Date of Patent: December 18, 2007Assignee: Schering CorporationInventors: Andrew Stamford, Youhao Dong, Stuart W. McCombie, Yusheng Wu
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Patent number: 7304156Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.Type: GrantFiled: July 12, 2002Date of Patent: December 4, 2007Assignee: AstraZeneca UK LimitedInventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
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Patent number: 7288544Abstract: Achiral pyrimidine derivatives and pyridine derivatives of the following formulae or analogs thereof have selective N-type calcium channel antagonistic activity and showed analgesic action when they were taken orally.Type: GrantFiled: March 14, 2003Date of Patent: October 30, 2007Assignee: Ajinomoto Co., Inc.Inventors: Seiji Ohno, Kayo Otani, Seiji Niwa, Satoshi Iwayama, Akira Takahara, Hajime Koganei, Yukitsugu Ono, Shinichi Fujita, Tomoko Takeda, Masako Hagihara, Akiko Okajima
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Publication number: 20070244140Abstract: The present invention relates to compounds of formula III: wherein R2, R3, R5 and R6 are as defined herein.Type: ApplicationFiled: April 10, 2007Publication date: October 18, 2007Applicant: WyethInventors: Yongbo Hu, Fuk-Wah Sum, Martin Di Grandi, Emily Norton
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Patent number: 7279576Abstract: Novel compounds and methods of using those compounds for the treatment of oncological conditions are provided. In a preferred embodiment, modulation of the activation states of abl or bcr-abl ?-kinase proteins comprises the step of contacting the kinase proteins with the novel compounds.Type: GrantFiled: December 24, 2003Date of Patent: October 9, 2007Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo
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Patent number: RE40245Abstract: The present invention relates to compounds of the formula I: or a pharmaceutically acceptable derivative or prodrug thereof. The compounds are useful as inhibitors of bacterial gyrase activity. The present invention also relates to methods for treating bacterial infections in mammala. The present invention also relates to methods for decreasing bacterial quantity in a biological sample.Type: GrantFiled: April 28, 2004Date of Patent: April 15, 2008Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anne-Laure Grillot, Paul S. Charifson, Dean Stamos, Yusheng Liao, Michael C. Badia, Martin Trudeau