Substituent On 5-position Contains Carbocyclic Ring Patents (Class 544/325)
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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: 7579466Abstract: 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 human or animal subject such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, Crohn's 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: February 26, 2007Date of Patent: August 25, 2009Assignee: Elan Pharmaceuticals, Inc.Inventors: Jenifer Smith, Christopher Semko, Ying-Zi Xu, Andrei W. Konradi
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Patent number: 7531548Abstract: HIV replication inhibitors of formula (I) N-oxides, a pharmaceutically acceptable addition salts, a quaternary amines or a stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; -b1=b2-b3=b4- is —CH?CH—CH?CH—, —N?CH—CH?CH—, —N?CH—N?CH—, —N?CH—CH?N—, —N?N—CH?CH—; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; optionally substituted C1-6alkyl; C1-6alkyloxycarbonyl; R2 is OH; halo; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; substituted carbonyl; carboxyl; CN; nitro; amino; substituted amino; polyhalomethyl; polyhalomethylthio; —S(?O)rR6; C(?NH)R6; R2a is CN; amino; substituted amino; optionally substituted C1-6alkyl; halo; optionally substituted C2-6alkyloxy; substituted carbonyl; —CH?N—NH—C(?O)—R16; optionally substituted C1-6alkyloxy C1-6alkyl; substituted C2-6alkenyl or C2-6alkynyl; —C(?N—O—R8)—C1-4alkyl; R7 or —X3—R7; X1 is —NR1—, —O—, —C(?O)—, CH2, —CHOH—, —S—, —S(?O)r—; R3 is CN; amino; C1-6alkyl; halo; optionally subsType: GrantFiled: September 29, 2005Date of Patent: May 12, 2009Assignee: Tibotec Pharmaceuticals LtdInventors: Jerôme Emile Georges Guillemont, Jan Heeres, Paulus Joannes Lewi
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Publication number: 20090099219Abstract: The invention relates to alkynylpyrimidines according to the general formula (I): in which A, R1, R2, R3, R4, R5, and R6 are as defined in the claims, and salts, N-oxides, metabolites, solvates, tautomers and prodrugs thereof, to pharmaceutical compositions comprising said alkynylpyrimidines, to methods of preparing said alkynylpyrimidines, as well as to uses thereof for manufacturing a pharmaceutical composition for the treatment of diseases of dysregulated vascular growth or of diseases which are accompanied with dysregulated vascular growth, wherein the compounds effectively interfere with Tie2 and VEGFR2 signalling.Type: ApplicationFiled: June 19, 2008Publication date: April 16, 2009Inventors: Ingo Hartung, Ulrich Bothe, Georg Kettschau, Ulrich Luecking, Anne Mengel, Martin Krueger, Karl Heinz Thierauch, Philip Lienau, Ulf Boemer
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Patent number: 7511052Abstract: 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 human or animal subject 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: September 28, 2006Date of Patent: March 31, 2009Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Christopher Michael Semko, Ying-zi Xu, Frank Stappenbeck, Jenifer Lea Smith, Kassandra Inez Rossiter, Juri Y. Fukuda, Andrei W. Konradi
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Publication number: 20090076047Abstract: 2-Substituted pyrimidines of the formula I, where the indices and substituents are as defined in the description.Type: ApplicationFiled: September 21, 2006Publication date: March 19, 2009Inventors: Joachim Rheinheimer, Thomas Grote, Bernd Muller, Jan Klaas Lohmann, Wassilios Grammenos, Udo Hunger, Frank Schieweck, Sarah Ulmschneider, Jochen Dietz, Jens Renner, John-Bryan Speakman, Maria Scherer, Siegfried Strathmann, Reinhard Stierl
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Patent number: 7491731Abstract: A crystal structure of the cfms kinase domain, co-crystal structure with a bound small molecule, as well as methods of using the same in the discovery of cfms inhibitors and in the treatment of diseases mediated by inappropriate cfms activity.Type: GrantFiled: May 9, 2006Date of Patent: February 17, 2009Assignee: SmithKline Beecham CorporationInventors: Holly Kathleen Emerson, David Lee Musso, Stanley Dawes Chamberlain, Gregory Edward Peckham
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Patent number: 7465735Abstract: 5-Phenylpyrimidines, their preparation, compositions comprising them and their use 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 whicType: GrantFiled: November 15, 2002Date of Patent: December 16, 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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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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Patent number: 7427628Abstract: Disclosed are compounds which bind ?4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by ?4 integrins, preferably 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: September 26, 2006Date of Patent: September 23, 2008Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupi, Jenifer Smith, Michael A. Pleiss, Eugene D. Thorsett
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Publication number: 20080176831Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and the substituents L and R1 to R3 are as defined in the description and X is a group —CH—Ra, —N— or —S—; R1 may be hydrogen, halogen, C1-C6-alkyl, C1-C6-alkoxy, cyano or C1-C6-alkoxycarbonyl; Rb is hydrogen, C1-C6-alkyl or C3-C6-cycloalkyl; T is a group —CH—Ra—; p is an integer from 1 to 4; Y is a group —CH—Ra— or —N—Rb o is 0 or 1; Z is O, S or a group N(Rc) Rc is hydrogen, C1-C6-alkyl or C1-C6-alkoxy, and to processes for their preparation, to pesticidal compositions comprising them and to their use as pesticides.Type: ApplicationFiled: May 17, 2005Publication date: July 24, 2008Applicant: BASF AktiengesellschaftInventors: Anja Schwogler, Frank Schieweck, Joachim Rheinheimer, Markus Gewehr, Bernd Muller, Thomas Grote, Wassilios Grammenos, Udo Hunger, Carsten Blettner, Peter Schafer, Oliver Wagner, Reinhard Stierl, Ulrich Schofl, Siegfried Strathmann, Maria Scherer
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Publication number: 20080132504Abstract: Novel pyrimidine derivatives of formula I to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising themType: ApplicationFiled: August 13, 2004Publication date: June 5, 2008Inventors: Carlos Garcia-Echeverria, Takanori Kanazawa, Eiji Kawahara, Keiichi Masuya, Naoko Matsuura, Takahiro Miyake, Osamu Ohmori, Ichiro Umemura, Ruo Steensma, Greg Chopiuk, Jiqing Jiang, Yongqin Wan, Qiang Ding, Qiong Zhang, Nathanael Schiander Gray, Donald Karanewsky
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Patent number: 7371758Abstract: Compounds of the formula (I) wherein R1 represents a hydrogen atom or a 3-halogen atom, and R2 represents a straight-chain alkyl group containing up to 6 carbon atoms, a straight-chain alkyl group containing up to 3 carbon atoms with unsubstituted or substituted aromatic ring, or alkoxycarbonyl substituent at the end position, or aryloxyalkoxyalkyl group have been found to possess antimalarial activity against Plasmodium falciparum lines, including those resistant against pyrimethamine and other antifolates. The compounds themselves, methods of making these compounds, and methods of using these compounds are all disclosed.Type: GrantFiled: March 13, 2003Date of Patent: May 13, 2008Assignee: National Science & Technology Development AgencyInventors: Yongyuth Yuthavong, Bongkoch Tarnchompoo, Sumalee Kamchonwongpaisan
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Patent number: 7319100Abstract: Compounds provided herein are novel substituted pyrazinones, pyridines and pyrimidines of Formula (I) and (II): Such compounds are particularly useful as CRF receptor ligands, and hence, in the treatment of various neurologically-related disorders such as affective disorder, anxiety and depression.Type: GrantFiled: February 14, 2007Date of Patent: January 15, 2008Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Argyrios G. Arvanitis, Paul J. Gilligan, Richard A. Hartz
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Patent number: 7317015Abstract: The invention relates to 2-substituted pyrimidines of the formula I in which the index n and these substituents R1, R2 and R3 are as defined in the description and R4 is as defined below: R4 corresponds to one of the formulae where Ra is hydrogen, C1-C6-alkyl, C2-C8-alkenyl, C2-C8-alkynyl, C3-C6-cycloalkyl or C1-C4-alkoxy and R5 is hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C1-C4-alkyloxy-C1-C2-alkyl, phenyl-C1-C2-alkyl or phenyloxy-C1-C2-alkyl, to processes for preparing these compounds, to compositions comprising these compounds and to their use as pesticides.Type: GrantFiled: July 3, 2004Date of Patent: January 8, 2008Assignee: BASF AktiengesellschaftInventors: Frank Schieweck, Jordi Tormo i Blasco, Carsten Blettner, Bernd Müller, Markus Gewehr, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Peter Schäfer, Anja Schwögler, Oliver Wagner, Siegfried Strathmann, Ulrich Schöfl, Maria Scherer, Reinhard Stierl
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Patent number: 7288547Abstract: This invention relates to 2-heteroaryl-pyrimidine derivatives of general formula I or If as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.Type: GrantFiled: October 27, 2003Date of Patent: October 30, 2007Assignee: Schering AGInventors: Ulrich Lücking, Martin Kruger, Rolf Jautelat, Olaf Prien, Gerhard Siemeister, Alexander Ernst
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Patent number: 7205297Abstract: The present invention relates to a series of novel substituted 5-alkynyl pyrimidines, pharmaceutical compositions which contain them, methods for their preparation, and their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral nervous systems, including age related cognitive disorders such as senility and Alzheimer's disease, nerve injuries, peripheral neuropathies, and seizure disorders such as epilepsy.Type: GrantFiled: July 20, 2001Date of Patent: April 17, 2007Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: Lilia M. Beauchamp, Thomas A. Krenitsky, James L. Kelley
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Patent number: 7205310Abstract: Disclosed are compounds which bind VLA-4 and/or LPAM-1. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4 and/or LPAM-1. 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: April 29, 2005Date of Patent: April 17, 2007Assignee: Elan Pharmaceuticals, Inc.Inventors: Andrei W. Konradi, Frank Stappenbeck, Michael A. Pleiss, Christopher Semko, Jenifer L. Smith
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Patent number: 7157455Abstract: Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 4-aminopyrimidine-5-one derivatives.Type: GrantFiled: February 2, 2004Date of Patent: January 2, 2007Assignee: 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: 7153860Abstract: The invention relates to 5-phenylpyrimidine of formula (I) wherein the substituents have the following designations: R1 represents a five to ten-membered saturated, partially unsaturated or aromatic monocyclic or bicyclic heterocycle which contains between one and four heteroatoms from the group O, N or S, and which can be substituted as defined in the description; R2 represents hydrogen, halogen, cyano, alkyl, halogenalkyl or alkoxy; R3 and R4 represent hydrogen, alkyl, halogenalkyl, cycloalkyl, halogencycloalkyl, alkenyl, halogenalkenyl, cycloalkenyl, alkinyl, halogenalkinyl or cycloalkinyl; together with the nitrogen atom to which they are bonded, R3 and R4 can also form a five or six-membered ring which can be split by a heteroatom and can carry at least one substituent; R5 and R6 represent hydrogen, halogen, alkyl, halogenalkyl or alkoxy; R1 and R8 represent hydrogen, halogen, alkyl or halogenalkyl; and R9 represents hydrogen, halogen, alkyl, alkoxy, cycloalkoxy, halogenalkoxy or alkoxycarbonyl.Type: GrantFiled: March 13, 2002Date of Patent: December 26, 2006Assignee: BASF AktiengesellschaftInventors: Thomas Grote, Andreas Gypser, Joachim Rheinheimer, Ingo Rose, Peter Schäfer, Frank Schieweck, Hubert Sauter, Markus Gewehr, Bernd Müller, Jordi Tormo i Blasco, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Reinhard Stierl
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Patent number: 7153964Abstract: Pyrimidine derivatives of formula (I) wherein: Qh1 and Q2 are independently selected from aryl or carbon linked heteroaryl optionally substituted as defined within; and one of Q1 and Q2 or both Q1 and Q2 is substituted on a ring carbon by one group selected from sulphamoyl, N—(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), N,N-di-(C1-4alkyl)sulphamoyl (optionally substituted by halo or hydroxy), C1-4alkylsulphonyl (optionally substituted by halo or hydroxy) or a substituent of the formula (Ia) or (Ia?): wherein Q1, Q2, G, R1, Y, Z, Q3, n and m are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described.Type: GrantFiled: February 26, 2001Date of Patent: December 26, 2006Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Gloria Anne Breault, Jeffrey James Morris
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Patent number: 7067522Abstract: Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.Type: GrantFiled: November 24, 2004Date of Patent: June 27, 2006Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Patent number: 7026328Abstract: Disclosed are compounds which bind ?4 integrins, preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by ?4 integrins, preferably 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: May 27, 2003Date of Patent: April 11, 2006Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupl, Jenifer L. Smith, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 7008949Abstract: Disclosed are compounds which bind ?4 integrins, where the ?4 integrin is preferably VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by ?4 integrins, where the ?4 integrin is preferably 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: May 27, 2003Date of Patent: March 7, 2006Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Christopher M. Semko, Ying-zi Xu, Frank Stappenbeck, Brian P. Stupi, Jenifer L. Smith, Michael A. Pleiss, Eugene D. Thorsett
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Patent number: 6953802Abstract: 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: July 20, 2001Date of Patent: October 11, 2005Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6951866Abstract: 1. A pyrimidine derivative of the formula (1) or a salt thereof; has an inhibitory activity of production of Th2 type cytokines such as IL-4, IL-5, etc., and is useful as an therapeutic agent for allergic diseases, autoimmune diseases such as systemic lupus erythemathosus, etc., and acquired immunodeficiecy syndrome (AIDS) and so on.Type: GrantFiled: August 19, 2002Date of Patent: October 4, 2005Assignee: Sumitomo Pharmaceuticals Company, LimitedInventors: Hitoshi Fujita, Fujio Antoku, Norio Fujiwara, Kiyotaka Iwai, Hiroshi Tanaka, Hajime Kawakami
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Patent number: 6943252Abstract: Pyrimidines of formula I in which R1 represents hydrogen or alkyl, haloalkyl, alkenyl, alkynyl, alkadienyl, alkoxy, cycloalkyl, phenyl, or 5- or 6-membered heteroaryl or 5- or 6-membered heterocyclyl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, or tri-alkyl-silyl, formyl or alkoxycarbonyl, wherein R1 groups are unsubstituted or substituted as defined in the specification; R2 represents phenyl, cycloalkyl or 5- or 6-membered heteroaryl, containing one to four nitrogen atoms or one to three nitrogen atoms and one sulfur or oxygen atom, which are unsubstituted or substituted; R3 represents hydrogen, halogen or alkyl, alkoxy, alkylthio, alkylamino or dialkylamino; which are unsubstituted or substituted; R4 represents hydrogen or alkyl, alkenyl or alkynyl; which are unsubstituted or substituted; and X represents O, S, NR5 or a single bond, wherein R5 represents hydrogen or alkyl; or R1 and R5 together with the interjacent nitrogen atom form a heterType: GrantFiled: July 9, 2003Date of Patent: September 13, 2005Assignee: BASF AktiengesellschaftInventors: Klaus-Juergen Pees, Waldemar Pfrengle, Gavin Heffernan
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Patent number: 6943172Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: GrantFiled: January 23, 2003Date of Patent: September 13, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Dhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Hans Pluempe
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Patent number: 6924290Abstract: Disclosed are compounds and derivatives thereof, their synthesis, and their use as Rho-kinase inhibitors. These compounds are useful for inhibiting tumor growth, treating erectile dysfunction, and treating other indications mediated by Rho-kinase, e.g., coronary heart disease.Type: GrantFiled: January 23, 2003Date of Patent: August 2, 2005Assignee: Bayer Pharmaceuticals CorporationInventors: Dhanapalan Nagarathnam, Jacques Dumas, Holia Hatoum-Mokdad, Stephen Boyer, Chunguang Wang, Hans Pluempe, Achim Feurer, Samir Bennabi
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Patent number: 6838464Abstract: Pyrimidine derivatives of formula (I) wherein Q1, Q2, G and R1 are as defined within; and pharmaceutically acceptable salts and in vivo hydrolysable esters thereof are described. Processes for their manufacture, pharmaceutical compositions and their use as cyclin-dependent serine/threonine kinase (CDK) and focal adhesion kinase (FAK) inhibitors are also described.Type: GrantFiled: February 26, 2001Date of Patent: January 4, 2005Assignee: AstraZeneca ABInventors: Elizabeth Janet Pease, Emma Jane Williams, Robert Hugh Bradbury, Stuart Eric Pearson
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Patent number: 6818649Abstract: This invention is concerned with substituted chromene derivatives of the general formula (I) in which R1-R4 are as defined in the specification and claims. The invention further relates to the pharmaceutically acceptable acid addition salts of these compounds, their use as therapeutically active substances; medicaments based on these substances, optionally in combination with sulphonamides, and their production; the use of these substances as medicaments and for the production of antibacterially-active medicaments; as well as the manufacture of the compounds of formula (I) and their pharmaceutically acceptable acid addition salts and intermediates for their manufacture.Type: GrantFiled: October 28, 2002Date of Patent: November 16, 2004Assignee: Basilea Pharmaceutica AGInventors: Peter Mohr, Philippe Pflieger
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Patent number: 6787539Abstract: The invention relates to compounds of the formula wherein R1 is lower alkyl, lower alkoxy, pyridinyl, pyrimidinyl, phenyl, —S-lower alkyl, —S(O)2-lower alkyl, —N(R)—(CH2)n—N(R)2, —O—(CH2)n—N(R)2, —N(R)2, or a cyclic tertiary amine of the group which may contain one additional heteroatom, selected from N, O or S, and wherein this group may be connected with the pyrimidine ring via the linker —O(CH2)n—; R2 is hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; R3/R3′ is, independently from each other, hydrogen or lower alkyl; R4 is independently from each other halogen, trifluoromethyl or lower alkoxy; R5 is hydrogen or lower alkyl; R is, independently from each other, hydrogen or lower alkyl; X is —C(O)N(R)— or —N(R)C(O)—; Y is —O—, —S—, —SO2—, - or —N(R)—; n is 1,2,3 or 4; and m is 0,1 or 2; or a pharmaceuticType: GrantFiled: October 15, 2001Date of Patent: September 7, 2004Assignee: Hoffmann-La Roche Inc.Inventor: Heinz Stadler
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Publication number: 20040030134Abstract: A novel process is provided for the preparation of chiral intermediates useful in the asymmetric syntheses of &agr;v&bgr;3 integrin receptor antagonists. Also provided are the enantiomerically enriched intermediates that are obtained from the process.Type: ApplicationFiled: September 11, 2003Publication date: February 12, 2004Inventors: James Christopher McWilliams, Elizabeth Buck, Kan K. Eng, Guy R. Humphrey, Peter E. Maligres, Jess W. Sager, Marjorie See Waters
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Patent number: 6656935Abstract: An aromatic nitrogen-containing 6-membered cyclic compound of the formula (I): wherein Ring A is a substituted or unsubstituted nitrogen-containing heterocyclic group; R1 is a substituted or unsubstituted lower alkyl group, —NH—Q—R3 (R3 is a substituted or unsubstituted nitrogen containing heterocyclic group, and Q is a lower alkylene group or a single bond), or —NH—R4 (R4 is a substituted or unsubstituted cycloalkyl group); R2 is a substituted or unsubstituted aryl group; one of Y and Z is ═CH—, and the other is ═N—, or a pharmaceutically acceptable salt thereof, these compounds exhibiting excellent selective PDE V inhibitory activities, and hence, being useful in the prophylaxis or treatment of penile erectile dysfunction, etc.Type: GrantFiled: August 10, 2001Date of Patent: December 2, 2003Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, Kenji Matsuki, Kenji Omori, Kohei Kikkawa
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Patent number: 6586459Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: July 1, 2003Inventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6583173Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: September 28, 2001Date of Patent: June 24, 2003Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffrey Bernard Franciskovich, Theodore Goodson, Junior, Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6583148Abstract: The present invention relates to novel derivatives of a series of substituted pyrimidines, to pharmaceutical compositions which contain them, to methods for their preparation and to their use in therapy, particularly in the treatment of neurodegenerative or other neurological disorders of the central and peripheral systems.Type: GrantFiled: April 8, 1999Date of Patent: June 24, 2003Assignee: Krenitsky Pharmaceuticals, Inc.Inventors: James L. Kelley, Thomas A. Krenitsky, Lilia M. Beauchamp
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Patent number: 6479498Abstract: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.Type: GrantFiled: November 9, 2001Date of Patent: November 12, 2002Assignee: Theravance, Inc.Inventors: Daniel Marquess, Seok-Ki Choi, David T. Beattie, John H. Griffin, Scott Armstrong, Timothy J. Church, Thomas E. Jenkins, David C. Green
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Patent number: 6313151Abstract: This application relates to a compound of formula (I), a pharmaceutically acceptable salt of the compound, or a prodrug thereof, as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.Type: GrantFiled: March 31, 2000Date of Patent: November 6, 2001Assignee: Eli Lilly and CompanyInventors: Douglas Wade Beight, Trelia Joyce Craft, Jeffry Bernard Franciskovich, Theodore Goodson, Jr., Steven Edward Hall, David Kent Herron, Valentine Joseph Klimkowski, Jeffrey Alan Kyle, John Joseph Masters, David Mendel, Guy Milot, Jason Scott Sawyer, Robert Theodore Shuman, Gerald Floyd Smith, Anne Louise Tebbe, Jennifer Marie Tinsley, Leonard Crayton Weir, James Howard Wikel, Michael Robert Wiley, Ying Kwong Yee
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Patent number: 6254669Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.Type: GrantFiled: August 5, 1999Date of Patent: July 3, 2001Assignee: Zeneca LimitedInventors: Aidan Joseph Lavery, Prahalad Manibhai Mistry, Ronald Wynford Kenyon
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Patent number: 6251900Abstract: Heterocyclic compounds in which s-triazine or pyrimidine is substituted with benzimidazole and morpholine and which are represented by the Formula I or phermaceutically acceptable acid addition salts thereof: wherein X and Y respectively represent nitrogen atom or one of them represents nitrogen atom and the other represents C—R7 wherein R7 represents hydrogen or halogen atom; R1, R2, R4, R5 and R6 represent hydrogen atom or C1-C6 alkyl; R3 represents morpholino, piperidino, piperazinyl, thiomorpholino, benzimidazolyl, cyano or the like.Type: GrantFiled: January 21, 2000Date of Patent: June 26, 2001Assignee: Zenyaku Kogyo Kabushiki KaishaInventors: Seiichiro Kawashima, Toshiyuki Matsuno, Shinichi Yaguchi, Tetsuo Watanabe, Masahiro Inaba
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Patent number: 6235746Abstract: Compounds of general formula (1) are described: wherein R1 is a hydrogen or halogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group or a group selected from hydroxyl (—OH), substituted hydroxyl, thiol (—SH), substituted thiol, amino (—NH2), or substituted amino; R2 and R3, which may be the same or different, is each an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R4 is a hydrogen atom or a straight or branched chain alkyl group; R5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R6 is a hydrogen or halogen atom or an amino (—NH2), substituted amino, nitro, carboxyl (—CO2H) or esterified carboxyl group or a group —X1—R6a where X1 is a direct bond or a linker atom or group and R6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom orType: GrantFiled: February 16, 1999Date of Patent: May 22, 2001Assignee: Celltech Therapeutics, LimitedInventors: Peter David Davis, David Festus Charles Moffat, Jeremy Martin Davis, Martin Clive Hutchings
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Patent number: 6229011Abstract: Compounds of the formula: are disclosed which have activity as inhibitors of binding between VCAM-1 and cells expressing VLA-4. Such compounds are useful for treating diseases whose symptoms and/or damage are related to the binding of VCAM-1 to cells expressing VLA-4.Type: GrantFiled: August 21, 1998Date of Patent: May 8, 2001Assignee: Hoffman-La Roche Inc.Inventors: Li Chen, Robert William Guthrie, Tai-Nang Huang, Achyutharao Sidduri, Jefferson Wright Tilley, Kenneth Gregory Hull
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Patent number: 6172066Abstract: This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.Type: GrantFiled: May 16, 1997Date of Patent: January 9, 2001Assignee: Synaptic Pharmaceutical CorporationInventors: Dhanapalan Nagarathnam, Wai C. Wong, Shou Wu Miao, Michael A. Patane, Charles Gluchowski
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Patent number: 6136971Abstract: The present invention provides a process for preparing 1,2-diheteroethylene sulfonamide of the formula: ##STR1## by reacting a pyrimidine monohalide of the formula: ##STR2## with a mono-protected 1,2-diheteroethylene anion of the formula M.sub.1 XCH.sub.2 CH.sub.2 YR.sub.5 and removing the protecting group, wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, Z, X, Y, M, M.sub.1 and W are defined herein.Type: GrantFiled: July 15, 1999Date of Patent: October 24, 2000Assignee: Roche Colorado CorporationInventors: Peter J. Harrington, Hiralal N. Khatri, Bradley S. Dehoff
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Patent number: 6124308Abstract: A pyrimidine of formula (I) ##STR1## and its pharmaceutically acceptable acid addition salts are useful as analgesics, as anticonvulsants or in the treatment of irritable bowel syndrome or bipolar disorder.Type: GrantFiled: February 26, 1998Date of Patent: September 26, 2000Assignee: Glaxo Wellcome Inc.Inventors: Malcolm Stuart Nobbs, Sandra Jane Rodgers
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Patent number: 5958935Abstract: 2-Anilinopyrimidines, processes for their preparation, pharmaceutical compositions containing them, their use in medicine. In a preferred embodiment, the compounds have the general formula (1): ##STR1## wherein R.sup.1 is preferably methoxy; R.sup.2 and R.sup.3 are preferably methyl; R.sup.4 is preferably a hydrogen atom; R.sup.5 is a hydrogen atom or an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; R.sup.6 is a hydrogen or halogen atom or an amino (--NH.sub.2), substituted amino, nitro, carboxyl (--CO.sub.2 H), esterified carboxyl or --X.sup.1 R.sup.6a where X.sup.1 is a direct bond or a linker atom or group and R.sup.6a is an optionally substituted straight or branched chain alkyl, alkenyl or alkynyl group; X is a direct bond or a linker atom or group; and R.sup.7 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group.Type: GrantFiled: November 19, 1996Date of Patent: September 28, 1999Assignee: Celltech Therapeutics LimitedInventors: Peter David Davis, David Festus Charles Moffat, Jeremy Martin Davis, Martin Clive Hutchings
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Patent number: 5939424Abstract: The invention relates to 4-Amino-2-ureidopyrimidine-5-carboxamides of the formula I ##STR1## in which R.sup.1 is H or (C.sub.1 -C.sub.8)-alkyl, where one or more H can be replaced by F; R.sup.2 is selected from the group consisting of F, Cl, Br, H, -O-(C.sub.1 -C.sub.8)-alkyl, and -S-(C.sub.1 -C.sub.8)-alkyl, where the alkyl groups have one or more H replaced by F; R.sup.3 is -O-(C.sub.1 -C.sub.8)-alkyl or -S-(C.sub.1 -C.sub.8)-alkyl, where the alkyl groups have one or more H replaced by F; or R.sup.2 and R.sup.3 together form -O-(C.sub.1 -C.sub.5)-alkylene-O-, where the alkylene portion has one or more H replaced by F; and their physiologically tolerable salts. The invention further provides processes for preparing the compounds of formula I. The compounds are suitable for the treatment of disorders of lipid metabolism.Type: GrantFiled: June 4, 1997Date of Patent: August 17, 1999Assignee: Hoechst AktiengesellschaftInventors: Hans Georg Boger, Axel Hoffmann, Gerhard Jahne, Norbert Krass, Hans-Ludwig Schafer
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Patent number: 5795899Abstract: Soluble salts of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl)pyrimidine-5-carboxylic acid N-methyl-N-(3-trifluoromethylphenyl)amide, a process for the preparation thereof, the use thereof as pharmaceuticals and starting materials.Salts, which are soluble and freely soluble in water, of 4-amino-2-(4,4-dimethylimidazolidin-2-on-1-yl)pyrimidine-5-carboxylic acid N-methyl-N-(3-trifluoromethylphenyl)-amide and a process for the preparation thereof are described. The compounds are suitable for the treatment of lipid metabolism disorders which are beneficially influenced by stimulation of the hepatic LDL receptor.Also described are the compounds of the formula IV ##STR1## and the salts thereof.Type: GrantFiled: February 23, 1995Date of Patent: August 18, 1998Assignee: Hoechst AktiengesellschaftInventors: Klaus-Dieter Kampe, Ernold Granzer, Michael Leineweber, Manfred Huttinger