Halogen Attached Directly To The Diazine Ring By Nonionic Bonding Patents (Class 544/334)
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Patent number: 7919618Abstract: Novel methods of synthesizing piperazines, piperidines and related compounds are disclosed, as are compounds useful for their preparation.Type: GrantFiled: August 2, 2007Date of Patent: April 5, 2011Assignee: Lexicon Pharmaceuticals, Inc.Inventors: Hugh Alfred Burgoon, Jr., Ramanaiah C. Kanamarlapudi, Wenxue Wu
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Publication number: 20110053943Abstract: This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: ApplicationFiled: June 1, 2010Publication date: March 3, 2011Inventors: David A. Claremon, Colin M. Tice, Linghang Zhuang, Katerina Leftheris, Yuanjie Ye, Suresh B. Singh
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Publication number: 20110039852Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.Type: ApplicationFiled: January 29, 2009Publication date: February 17, 2011Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott, Yen Pham Truong, Jeffrey Roger Roppe, Nicholas Simon Stock, Jeannie M. Arruda, Thomas Jon Seiders, Bowei Wang, Deborah Volkots
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Publication number: 20110009418Abstract: The present invention discloses compounds of formula: where Ar1, Ar2, X, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Phenylene Compound”); compositions comprising an effective amount of a Phenylene Compound; and methods for treating or preventing pain and other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Phenylene Compound.Type: ApplicationFiled: July 29, 2010Publication date: January 13, 2011Applicant: Purdue Pharma L.P.Inventor: Qun Sun
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Publication number: 20100331329Abstract: The invention concerns a compound of the formula (I) wherein Ring A is heterocyclyl; m is 0-4 and each R1 is a group such as hydroxy, halo, trifluoromethyl and cyano; R2 is halo and n is 0-2; and each R4 is a group such as hydroxy, halo, trifluoromethyl and cyano; p is 0-4; and R3 is amino or hydroxy; or pharmaceutically-acceptable salts or in-vivo-hydrolysable ester or amide thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or medical condions mediated by histone deacetylase.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicant: ASTRAZENECA ABInventors: Elaine Sophie Elizabeth Stokes, Craig Anthony Roberts, Michael James Waring
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Patent number: 7855291Abstract: Intermediates and synthetic processes for the preparation of substituted phenylalanine-based compounds (e.g.Type: GrantFiled: December 28, 2006Date of Patent: December 21, 2010
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Publication number: 20100317854Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Patent number: 7825128Abstract: The invention relates to sulfoximine-substituted pyrimidines of the general formula I processes for the preparation thereof and their use as drugs.Type: GrantFiled: December 21, 2006Date of Patent: November 2, 2010Assignee: Bayer Schering Pharma AGInventors: Ulrich Lücking, Duy Nguyen, Arne Von Bonin, Oliver Von Ahsen, Martin Krüger, Hans Briem, Georg Kettschau, Olaf Prien, Anne Mengel, Krolikiewicz Konrad, Ulf Boemer, Ulrich Bothe, Ingo Hartung
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Patent number: 7812160Abstract: The present invention relates to a pyrimidine derivative of the formula (I) and salts thereof which is useful as an active ingredient of pharmaceutical preparations. The pyrimidine derivative of the present invention has excellent CRTH2 (G-protein-coupled chemoattractant receptor, expressed on Th2 cells) antagonistic activity and can be used for the prophylaxis and treatment of diseases associated with CRTH2 activity, in particular for the treatment of allergic diseases, such as asthma, allergic rhinitis, atopic dermatitis, and allergic conjunctivitis; eosinophil-related diseases, such as Churg-Strauss syndrome and sinusitis; basophil-related diseases, such as basophilic leukemia, chronic urticaria and basophilic leukocytosis in human and other mammals; and inflammatory diseases characterized by T lymphocytes and profuse leukocyte infiltrates such as psoriasis, eczema, inflammatory bowel disease, ulcerative colitis, Crohn's disease, COPD (chronic obstructive pulmonary disorder) and arthritis.Type: GrantFiled: April 14, 2004Date of Patent: October 12, 2010Assignee: Actimis Pharmaceuticals, Inc.Inventors: Tai-wei Ly, Yuji Koriyama, Takashi Yoshino, Hiroki Sato, Kazuho Tanaka, Hiromi Sugimoto, Yoshihisa Manabe, Kevin Bacon, Klaus Urbahns, Masanori Seki, Takuya Shintani
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Patent number: 7803941Abstract: The present invention relates to an improved process for preparing ring-fluorinated aromatics of the general formula (I) by a halogen exchange reaction (halex reaction) of a plurality of halogen substituents in one stage in the presence of a catalyst.Type: GrantFiled: March 11, 2008Date of Patent: September 28, 2010Assignee: LANXESS Deutschland GmbHInventors: Axel Pleschke, Albrecht Marhold
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Publication number: 20100234398Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.Type: ApplicationFiled: May 26, 2010Publication date: September 16, 2010Applicant: DOW AGROSCIENCES LLCInventors: Michael R. Loso, Benjamin M. Nugent, Yuanming Zhu, Richard B. Rogers, Jim X. Huang, James M. Renga, Zoltan L. Benko, Gregory T. Whiteker, John F. Daeuble, SR.
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Publication number: 20100179127Abstract: The invention relates to novel heterocyclic compounds of the formula in free base form or in acid addition salt form, in which R1, R2, R3, R4 and A are as defined in the specification, to their preparation, to their use as medicaments and to medicaments comprising them.Type: ApplicationFiled: June 23, 2006Publication date: July 15, 2010Inventors: Philipp Floersheim, Wolfgang Froestl, Sebastien Guery, Kiemens Kaupmann, Manuel Koller
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Publication number: 20100160630Abstract: A process for producing a trichloropyrimidine compound represented by the formula (2): wherein R represents a hydrogen atom etc., comprising reacting a dihydroxypyrimidine compound represented by the formula (1): wherein R represents the same meaning as above, with sulfuryl chloride and at least one chlorinating agent selected from the group consisting of hydrogen chloride, thionyl chloride, phosgene, phosphorus oxychloride, phosphorus pentachloride and phosphorus trichloride in the presence of an organic base.Type: ApplicationFiled: March 26, 2008Publication date: June 24, 2010Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Koichi Nakazawa, Tomonori Yoshiyama, Kouji Yoshikawa
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Patent number: 7741329Abstract: Disclosed are N-aroyl cyclic amine derivatives having the formula: wherein the substituent variables are as defined herein, and their use as pharmaceuticals.Type: GrantFiled: October 29, 2007Date of Patent: June 22, 2010Assignee: SmithKline Beecham LimitedInventors: Clive Leslie Branch, Steven Coulton, Amanda Johns, Christopher Norbert Johnson, Roderick Alan Porter, Geoffrey Stemp, Kevin Thewlis
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Patent number: 7687501Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J3, X, Z, and R1, R3, and R4 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.Type: GrantFiled: August 16, 2006Date of Patent: March 30, 2010Assignee: Schering CorporationInventors: Chad E. Bennett, William J. Greenlee, Chad E. Knutson, Duane A. Burnett
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Publication number: 20100056534Abstract: Pesticide compositions and their use in controlling pests are provided.Type: ApplicationFiled: August 25, 2009Publication date: March 4, 2010Applicant: DOW AGROSCIENCES LLCInventors: Benjamin M. Nugent, Zoltan L. Benko, James M. Renga, Michael R. Loso, Timothy P. Martin
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Patent number: 7615634Abstract: Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.Type: GrantFiled: June 20, 2006Date of Patent: November 10, 2009Assignee: Hoffmann-La Roche Inc.Inventors: David Joseph Bartkovitz, Xin-Jie Chu, Qingjie Ding, Nan Jiang, Allen John Lovey, John Anthony Moliterni, John Guilfoyle Mullin, Jr., Binh Thanh Vu, Peter Michael Wovkulich
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Patent number: 7598236Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: December 15, 2007Date of Patent: October 6, 2009Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Publication number: 20090203906Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: April 13, 2009Publication date: August 13, 2009Applicant: Bayer AktiengesellschaftInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20090156804Abstract: The present invention relates to a production method of an optically active morpholine compound represented by the formula 10, which includes the following steps: wherein each symbol is as defined in the specification. The present invention also relates to a production method of an compound represented by the formula 55, which includes the following steps: wherein each symbol is as defined in the specification. According to the production method of the present invention, an optically active 2-aryl-substituted morpholine compound and 3-oxo-3-(pyrimidin-4-yl)propionate, which are important as starting materials for synthesizing 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4?]bipyrimidinyl-6-one having a tau protein kinase 1 inhibitory activity and useful as a therapeutic drug for Alzheimer's disease and the like, can be produced in a high yield by an industrially advantageous method.Type: ApplicationFiled: July 21, 2006Publication date: June 18, 2009Applicants: MITSUBISHI TANABE PHARMA CORPORATION, SANOFI-AVENTISInventors: Masahiro Okuyama, Fumiaki Uehara, Hiroshi Iwamura, Kazutoshi Watanabe
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Patent number: 7547700Abstract: The invention relates to compounds of general formula (1) in which X and Y=a carbon with a bonded hydrogen atom (CH) or a nitrogen atom, A=a methyl, fluoromethyl, cyano, hydroxyl, methoxy group, or a chlorine or fluorine atom on condition that when A=methyl (CH3) and X and Y both=a carbon bonded to a hydrogen atom, then B=a chlorine atom, B=a chlorine or a fluorine atom, D=a hydrogen, chlorine, fluorine atom, or a cyano or trifluoromethyl group and E=a hydrogen, fluorine or chlorine atom.Type: GrantFiled: June 18, 2003Date of Patent: June 16, 2009Assignee: PIERRE Fabre MedicamentInventors: Bernard Vacher, Bernard Bonnaud, Jean-Louis Maurel, Francis Colpaert
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Patent number: 7521555Abstract: A substitute aniline compound represented by the following formula (6): wherein, R1, R2 and R3 are each independently an alkyl group, an alkoxy group, an alkoxyalkyl group, a haloalkyl group, a carboxyl group, an alkoxycarbonyl group, an alkyl-carboxamide group, a nitro group, an aryl group, an arylalkyl group, an aryloxy group, a halogen atom or a hydrogen atom; and X and Y are each independently a hydrogen atom, an alkyl group, an alkoxy group, an alkoxyalkyl group, a haloalkyl group, a carboxyl group, an alkoxycarbonyl group or a halogen. A process for producing the compound formula (6) is also discussed.Type: GrantFiled: May 31, 2006Date of Patent: April 21, 2009Assignee: Ihara Chemical Industry Co., Ltd.Inventors: Hidetaka Hiyoshi, Mahito Ogawa
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Publication number: 20090093490Abstract: A compound of general formula (I): A process for preparing this compound. A fungicide composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: ApplicationFiled: May 2, 2006Publication date: April 9, 2009Inventors: Darren Mansfield, Pierre-Yves Coqueron, Heiko Rieck, Philippes Desbordes, Alain Villier, Marie-Claire Grosjean-Cournoyer, Pierre Genix
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Publication number: 20090088322Abstract: 6-Amino-4-pyrimidinecarboxylic acids having alkyl, alkenyl or alkynyl substituents in the 5-position and 4-aminopicolinic acids having alkyl, alkenyl or alkynyl substituents in the 3-position, and their amine and acid derivatives, are potent herbicides demonstrating a broad spectrum of weed control.Type: ApplicationFiled: October 1, 2008Publication date: April 2, 2009Applicant: Dow AgroSciences LLCInventors: Jeffrey B. Epp, Paul R. Schmitzer, Terry W. Balko, James M. Ruiz, Carla N. Yerkes, Thomas L. Siddall, Willuam C. Lo
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Patent number: 7504503Abstract: A substitute aniline compound represented by the following formula (6): wherein, R1, R2 and R3 are each independently an alkyl group, an alkoxy group, an alkoxyalkyl group, a haloalkyl group, a carboxyl group, an alkoxycarbonyl group, an alkylcarboxamide group, a nitro group, an aryl group, an arylalkyl group, an aryloxy group, a halogen atom or a hydrogen atom; and X and Y are each independently a hydrogen atom, an alkyl group, an alkoxy group, an alkoxyalkyl group, a haloalkyl group, a carboxyl group, an alkoxycarbonyl group or halogen. A process for producing the compound formula (6) is also discussed.Type: GrantFiled: April 30, 2007Date of Patent: March 17, 2009Assignee: Ihara Chemical Industry Co., Ltd.Inventors: Hidetaka Hiyoshi, Mahito Ogawa
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Patent number: 7501416Abstract: The present invention generally relates to quinoxaline compounds having Formula 1 or Formula 2 wherein the variables are as defined herein, and methods of using them.Type: GrantFiled: February 1, 2005Date of Patent: March 10, 2009Assignee: Bristol-Myers Squibb CompanyInventor: Kyoung S. Kim
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Publication number: 20090043098Abstract: A new method for the preparation of optionally 2-substituted 1,6-dihydro-6-oxo-4-pyrimidinecarboxylic acid compound of Formula 1 is disclosed wherein R1 is H or an optionally substituted carbon moiety.Type: ApplicationFiled: April 28, 2006Publication date: February 12, 2009Inventor: Rafael Shapiro
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Patent number: 7488732Abstract: 2-Substituted pyrimidines of the formula I in which the index n and the substituents L, Ra, Rb, Rc, Rz, Ru, Rv, A?, A? and A?? are as defined in the description and: R1 is C3-C10-alkyl, C3-C10-alkenyl, C3-C10-alkynyl, C3-C12-cycloalkyl, C3-C10-cycloalkenyl or a five- to ten-membered saturated, partially unsaturated or aromatic heterocycle which is attached via carbon and contains one to four heteroatoms from the group consisting of O, N and S, R2 is halogen, cyano, C1-C4-alkyl, C2-C4-alkenyl, C2-C4-alkynyl, C1-C4-alkoxy, C3-C4-alkenyloxy or C3-C4-alkynyloxy, where the alkyl, alkenyl and alkynyl radicals of R2 may be substituted by halogen, cyano, nitro, C1-C2-alkoxy or C1-C4-alkoxycarbonyl, and R3 is cyano, CO2Ra, C(?O)NRzRb, C(?O)—N—ORb, C(?S)—NRaRb, C(?NORa)NRzRb, C(?NRa)NRzRb, C(?O)NRa—NRzRb, C(?N—NRzRc)NRaRb, C(?O)Ra, C(?NORb)Ra, C(?N—NRzRb)Ra, CRaRb—ORz, CRaRb—NRzRc, ON(?CRaRb), O—C(?O)Ra, NRaRb?, NRa(C(?O)Rb), NRa(C(?O)ORb), NRa(C(?O)—NRzRb), NRa(C(?NRc)Rb), NRa(N?CRcRb), NRa—NRzRb, NRz—ORa, NRa(C(Type: GrantFiled: March 30, 2004Date of Patent: February 10, 2009Assignee: BASF AktiengesellschaftInventors: Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Peter Schäfer, Frank Schieweck, Anja Schwögler, Oliver Wagner, Maria Scherer, Siegfried Strathmann, Ulrich Schöfl, Reinhard Stierl
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Publication number: 20090023923Abstract: There is provided a novel process intermediate represented by the general formula (1) or (2): (where, X represents halogen atom, cyano group or the like, Y represents halogen atom, cyano group or the like, R1 represents C1-C6 haloalkyl group or C3-C8 halocycloalkyl group, R2 represents methyl group, halogen atom, cyano group or the like, m represents an integer of 1 to 5, and n represents an integer of 1 to 4).Type: ApplicationFiled: December 25, 2006Publication date: January 22, 2009Applicant: NISSAN CHEMICAL INDUSTRIES, LTDInventors: Takashi Mizukoshi, Yasuhiro Sakurai, Kazutaka Matoba, Manabu Yaosaka
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Patent number: 7465736Abstract: An azole derivative of formula (I) a medicament that contains the azole derivative of formula (I), a method of treating a disease with the azole derivative of formula (I), and a method of preparing the azole derivative of formula (I).Type: GrantFiled: June 13, 2003Date of Patent: December 16, 2008Assignee: Laboratoires Serono S.A.Inventors: Pascale Gaillard, Jean-Pierre Gotteland, Isabelle Jeanclaude-Etter, Matthias Schwarz, Russel J. Thomas
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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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Patent number: 7456281Abstract: Methods are provided for nucleic acid analysis wherein a target nucleic acid is mixed with a dsDNA binding dye to form a mixture. Optionally, an unlabeled probe is included in the mixture. A melting curve is generated for the target nucleic acid by measuring fluorescence from the dsDNA binding dye as the mixture is heated. Dyes for use in nucleic acid analysis and methods for making dyes are also provided.Type: GrantFiled: July 13, 2006Date of Patent: November 25, 2008Assignee: Idaho Technology, Inc.Inventor: Virginie E. Dujols
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Patent number: 7449471Abstract: 5-Phenylpyrimidines of the formula I in which the substituents and the index are as defined below: R1,R2 are hydrogen, alkyl, haloalkyl, cycloalkyl, halocycloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, and R1 and R2 together with the nitrogen atom to which they are attached may also form a saturated or unsaturated ring which may be interrupted by an ether, thio, sulfoxyl or sulfonyl group and may be substituted by one to four groups Ra and/or Rb; R3 is hydrogen, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy or alkenyloxy; R4 is hydrogen, halogen, cyano, hydroxyl, mercapto, azido, alkyl, alkenyl, alkynyl, haloalkyl, alkoxy, alkenyloxy, alkynyloxy, haloalkoxy, alkylthio, alkenylthio, alkynylthio, haloalkylthio, —ON?CRaRb, —CRc?NORa, —NRcN?CRaRb, —NRaRb, —NRcNRaRb, —NORa, —NRcC(?NRc?)NRaRb, —NRcC(?O)NRaRb, —NRaC(?O)Rc, —NRaC(?NORc)Rc?, —OC(?O)Rc, —C(?NORc)NRaRb, —CRc(?NNRaRb), —C (?O)NRaRb or —C(?O)Rc; in which Ra, Rb and Rc are as defined in the description; X is halogen, alkyl, alkoxy oType: GrantFiled: February 22, 2007Date of Patent: November 11, 2008Assignee: BASF AktiengesellschaftInventors: Andreas Gypser, Thomas Grote, Anja Schwögler, Joachim Rheinheimer, Frank Schieweck, Jordi Tormo i Blasco, Ingo Rose, Peter Schäfer, Markus Gewehr, Wassilios Grammenos, Bernd Müller, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Publication number: 20080261999Abstract: Compounds of the formula I or a pharmaceutically acceptable salt thereof: processes for their preparation, pharmaceutical compositions which contain them and their uses in therapy.Type: ApplicationFiled: February 23, 2006Publication date: October 23, 2008Inventors: Fionna Mitchell Martin, Claire June Flynn, Simon James Richards
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Publication number: 20080182986Abstract: The present invention relates to an improved process for preparing ring-fluorinated aromatics of the general formula (I) by a halogen exchange reaction (halex reaction) of a plurality of halogen substituents in one stage in the presence of a catalyst.Type: ApplicationFiled: March 11, 2008Publication date: July 31, 2008Inventors: Axel Pleschke, Albrecht Marhold
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Patent number: 7378409Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: GrantFiled: August 19, 2004Date of Patent: May 27, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Robert J. Cherney, Douglas G. Batt, Gregory D. Brown, John V. Duncia, Daniel S. Gardner, Michael G. Yang
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Publication number: 20080119651Abstract: Pyrimidine-5-carboxylates of formula: wherein R is C1-4 alkyl, R1 is C1-4 alkyl, trifluoromethyl, R2 is hydrogen or C1-4 alkyl and X is hydroxy, chlorine or bromine, are prepared from certain 3-oxoalkanoates of formula (II): with urea and orthoesters of formula (III) R2C(OR). The intermediate 2-acyl-3-ureidoacrylate, without being isolated, is reacted to give a 2-hydroxypyrimidine-5-carboxylate[(I), X?OH] or a hydrate thereof, which is optionally converted into the corresponding chloro or bromo compound (I, X?Cl, Br).Type: ApplicationFiled: November 4, 2005Publication date: May 22, 2008Inventors: Laurent Ducry, Bruno Rittiner
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Patent number: 7338958Abstract: This invention relates to pyrimidine derivatives of general formula I in which Q, R1, R2, R3, R4, R5, X, and m have the meanings that are contained in the description, as inhibitors of cyclin-dependent kinases and VEGF-receptor tyrosine kinases, their production as well as their use as medications for treatment of various diseases.Type: GrantFiled: October 18, 2004Date of Patent: March 4, 2008Assignee: Schering AGInventors: Ulrich Luecking, Gerhard Siemeister, Martin Krueger, Rolf Jautelat
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Patent number: 7317014Abstract: The present invention relates to novel derivatives of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their hydrates, their solvates, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them.Type: GrantFiled: July 21, 2003Date of Patent: January 8, 2008Assignees: Orchid Research Laboratories, Ltd., Bexel Pharmaceuticals Inc.Inventors: Shiv Kumar Agarwal, Ravikumar Tadiparthi, Pawan Aggarwal, Savithiri Shivakumar
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Patent number: 7312222Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.Type: GrantFiled: March 25, 2004Date of Patent: December 25, 2007Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Soo S. Ko, George V. Delucca, John V. Duncia, Joseph B. Santella, III, Dean A. Wacker
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Patent number: 7291624Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.Type: GrantFiled: May 11, 2004Date of Patent: November 6, 2007Assignee: Bayer Schering Pharma AGInventors: Thomas Brumby, Rolf Jautelat, Olaf Prien, Martina Schäfer, Gerhard Siemeister, Ulrich Lücking, Christoph Huwe
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Patent number: 7291730Abstract: Pyrimidine compounds of formula (1): wherein R1 is C3-C7 alkynyl optionally substituted with halogen; R2 and R3 are independently hydrogen or the like; and R4 is C3-C7 alkynyloxy optionally substituted with halogen, optionally substituted phenyl, or the like have an excellent pesticidal effect.Type: GrantFiled: October 15, 2004Date of Patent: November 6, 2007Assignee: Sumitomo Chemical Company, LimitedInventors: Hajime Mizuno, Noriyasu Sakamoto, Yoshiharu Kinoshita
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Patent number: 7271263Abstract: The present invention provides a process for producing a substituted aniline compound represented by the following general formula (6): (in the formula, R1, R2 and R3 are each independently an alkyl group, an alkoxy group, an alkoxyalkyl group, a haloalkyl group, a carboxyl group, an alkoxycarbonyl group, an alkyl-carboxamide group, a nitro group, an aryl group, an arylalkyl group, an aryloxy group, a halogen atom or a hydrogen atom; and X and Y are each independently a hydrogen atom, an alkyl group, an alkoxy group, an alkoxyalkyl group, a haloalkyl group, a carboxyl group, an alkoxycarbonyl group or a halogen atom), characterized by oxidizing a substituted indole compound represented by the following general formula (3): (in the formula, R1, R2, R3, X and Y have the same definitions as given above) to give rise to the ring opening of indole ring to produce an acetanilide compound represented by the following general formula (4): (in the formula, R1, R2, R3, X and Y have the same definitions asType: GrantFiled: October 15, 2001Date of Patent: September 18, 2007Assignee: Ihara Chemical Industry, Co., Ltd.Inventors: Hidetaka Hiyoshi, Mahito Ogawa
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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
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Patent number: 7153815Abstract: A insecticide characterized by containing as active ingredient a hydrazone derivative of formula (I) wherein A and Q are an aryl or a heterocyclic group, W is oxygen atom, an aminylene, an alkylene group, an oxyalkylene group or an alkyleneoxy, X1 and X2 are hydrogen atom, an alkyl, an alkenyl, an alkynyl, an aryl, a heterocyclic group, formyl, an acyl, an alkoxycarbonyl, an aryloxycarbonyl, a heterocyclic oxycarbonyl, an alkylsulfinyl, an arylsulfinyl, a heterocyclic sulfinyl, an alkylsulfonyl, an arylsulfonyl or a heterocyclic sulfonyl, Y is oxygen atom or sulfur atom, Z is hydrogen atom, a halogen atom, cyano, an alkyl, an alkenyl, an alkynyl, an amino, an alkoxy or an alkylthio, the substituents may be substituted; and novel hydrazon derivatives.Type: GrantFiled: January 10, 2003Date of Patent: December 26, 2006Assignee: Nihon Nohyaku Co., Ltd.Inventors: Shinji Kawata, Shuko Okui, Shigeru Suzuki, Toshiki Fukuchi, Akiyuki Suwa
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Patent number: 7129353Abstract: The invention relates to a novel process for preparing 4,6-dichloro-5-pyrimidine.Type: GrantFiled: June 3, 2003Date of Patent: October 31, 2006Assignee: Bayer CropScience AGInventors: Thomas Geller, Holger Weintritt
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Patent number: 7112676Abstract: Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.Type: GrantFiled: October 20, 2003Date of Patent: September 26, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Apostolos Dermatakis, Marek Michal Kabat, Kin-Chun Luk, Pamela Loreen Rossman, Sung-Sau So
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Patent number: 7083832Abstract: The invention provides LC compositions that exhibit V-shaped switching when aligned in an analog device configuration and exhibit bistability when aligned in a bookshelf-type device configuration. The invention more specifically provides LC compositions of formula 1 and particularly chiral nonracemic compounds of formula 1 which exhibit bistable switching as well as V-shaped switching when aligned in appropriate device configurations. The invention also provides methods of using the compounds of the invention in making LC compositions and electooptical devices comprising an aligned layer of the compositions of this invention.Type: GrantFiled: May 11, 2001Date of Patent: August 1, 2006Assignee: Displaytech, Inc.Inventors: Michael Wand, Neil Gough, Xin Hua Chen
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Patent number: RE39140Abstract: Novel heterocyclic compounds of the formula wherein, R1 represents a hydrogen atom or an alkyl group, A represents an ethylene group which may be substituted by alkyl or a trimethylene group which may be substituted by alkyl, X represents an oxygen or sulfur atom or the group in which R2 represents a hydrogen atom of an optionally substituted alkyl, an alkenyl, an alkynyl or an acyl group, and R3 represents a hydrogen atom or an alkyl group, and Z represents an optionally substituted 5- or 6-membered heterocyclic group which contains at least two hetero atoms selected from oxygen, sulfur and nitrogen atoms, or an optionally substituted 3- or 4-pyridyl group. The above defined novel heterocyclic compounds of formula (I) exhibit powerful insecticidal properties.Type: GrantFiled: February 4, 2002Date of Patent: June 20, 2006Assignee: Bayer Cropscience K.K.Inventors: Kozo Shiokawa, Shinichi Tsuboi, Shinzo Kagabu, Shoko Sasaki, Koichi Moriya, Yumi Hatori