The Second Ring Of The Bicyclo Ring System Is Six-membered, Consisting Of Five Ring Carbons And The Shared Ring Nitrogen (e.g., Pyrido[1,2-a]pyrimidine, Etc.) Patents (Class 514/259.4)
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Publication number: 20080255030Abstract: The invention provides compositions and methods for the treatment and diagnosis of diseases or disorders amenable to treatment through modulation of expression of a gene encoding a Jun N-terminal kinase 1 (JNK1 protein.Type: ApplicationFiled: August 6, 2007Publication date: October 16, 2008Inventors: Xing-Xian Yu, Sanjay Bhanot
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Publication number: 20080249112Abstract: The present invention relates to compounds that are useful for treating cellular proliferative diseases, for treating disorders mediated, at least in part, by KSP, and for inhibiting KSP. The invention also related to pharmaceutical compositions comprising such compounds, methods of treating cancer by the administration of such compositions, and processes for the preparation of the compounds. Compounds of the invention have the following formula: formula (I).Type: ApplicationFiled: April 6, 2005Publication date: October 9, 2008Applicant: CHIRON CORPORATIONInventors: Weibo Wang, Ryan N. Constantine, Liana M. Lagniton
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Patent number: 7414045Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula (A): are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: GrantFiled: December 18, 2003Date of Patent: August 19, 2008Assignee: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Publication number: 20080176869Abstract: Tetrahydro-4H-pyrido[1,2-a]pyrimidines and related compounds of Formula A: are described as inhibitors of HIV integrase and inhibitors of HIV replication, wherein n is an integer equal to zero, 1, 2 or 3, and R1, R3, R4, R12, R14, R16, R30, R32, R34 and R36 are defined herein. These compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: March 12, 2008Publication date: July 24, 2008Inventors: Benedetta Crescenzi, Olaf Kinzel, Ester Muraglia, Federica Orvieto, Giovanna Pescatore, Michael Rowley, Vincenzo Summa
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Patent number: 7326711Abstract: Pyridin[1,2-a]pyrimidinyl compounds, pharmaceutically acceptable salts, and prodrugs thereof; compositions that include a pharmaceutically acceptable carrier and one or more of the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent. Methods of using the pyridino[1,2-a]pyrimidinyl compounds, either alone or in combination with at least one additional therapeutic agent, in the prophylaxis or treatment of proliferative diseases.Type: GrantFiled: June 17, 2004Date of Patent: February 5, 2008Assignee: Chiron CorporationInventors: Weibo Wang, Ryan N. Constantine, Liana Marie Lagniton, Sabina Pecchi, Matthew T. Burger, Manoj C. Desai
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Publication number: 20070232624Abstract: The present invention provides a pharmaceutical composition, and provides for the use thereof for the treatment of excessive daytime sleepiness and/or a sleep disturbance in a psychiatric patient in need thereof. The pharmaceutical composition comprises a therapeutically effective amount of paliperidone, its pharmaceutically acceptable acid addition salts, enantiomeric forms, and esters thereof, together with a pharmaceutical carrier, and provides a relatively low plasma concentration variation of paliperidone to the psychiatric patient in need of treatment. The present invention also provides for the use of a pharmaceutical composition as defined above, in the preparation of a medicament for the treatment of excessive daytime sleepiness and/or a sleep disturbance in a psychiatric patient in need thereof.Type: ApplicationFiled: September 22, 2006Publication date: October 4, 2007Inventors: Joseph M. Palumbo, Marie-Henriette Eerdekens, Michelle Kramer
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Patent number: 7232827Abstract: The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein: (I) X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring optionally substituted; R2 represents a heterocyclic bicyclic rings, having 1–4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5–9 carbon atoms, of formula (II) R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom; R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy group or a halogen atom.Type: GrantFiled: February 26, 2003Date of Patent: June 19, 2007Assignees: Sanofi-Aventis, Mitsubishi Pharma CorporationInventors: Alistair Lochead, Alain Nedelec, Mourad Saady, Philippe Yaiche
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Patent number: 7230103Abstract: Substituted 3,4-dihydropyrido[1,2-a]pyrimidines of formula I and processes for the production thereof Also disclosed are substance libraries and pharmaceutical compositions containing the compound, and methods of treatment for pain, urinary incontinence, pruritus, tinnitus and/or diarrhoea using the pharmaceutical composition.Type: GrantFiled: April 11, 2003Date of Patent: June 12, 2007Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul, Utz-Peter Jagusch
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Patent number: 6875771Abstract: Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.Type: GrantFiled: July 15, 2003Date of Patent: April 5, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Shuanghua Hu, Paul M. Scola, Yazhong Huang, Katharine A. Grant-Young
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Patent number: 6864259Abstract: The present invention provides compounds of Formula (I): wherein R1-R6 and K have any of the values defined in the specification, and pharmaceutically acceptable salt thereof, that are useful as antibacterial agents. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula I, processes for preparing compounds of Formula I, and intermediates useful for preparing compounds of Formula I.Type: GrantFiled: May 29, 2002Date of Patent: March 8, 2005Assignee: Warner-Lambert CompanyInventors: Edmund Lee Ellsworth, Kim Marie Hutchings, Dai Nguyen, Rajeshwar Singh, Howard Daniel Hollis Showalter
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Publication number: 20040214836Abstract: Myocardial infarction in a mammal is treated by administering to the mammal a therapeutically effective amount of a chemical Src family tyrosine kinase protein inhibitor and the use of such inhibitor compounds for the preparation of a medicament for treating myocardial infarction. Myocardial infarction can be prevented by administering to the mammal a prophylactic amount of the inhibitor. The inhibitor preferably is an inhibitor of Src protein selected from the group consisting of a pyrazolopyrimidine class Src family tyrosine kinase inhibitor, a macrocyclic dienone class Src family tyrosine kinase inhibitor, a pyrido[2,3-d]pyrimidine class Src family tyrosine kinase inhibitor, a 4-anilino-3-quinolinecarbonitrile class Src family tyrosine kinase inhibitor, and a mixture thereof.Type: ApplicationFiled: March 15, 2004Publication date: October 28, 2004Inventors: David A. Cheresh, Robert Paul, Brian Eliceiri
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Patent number: 6750214Abstract: The invention provides compounds of formula (I), wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents H or C1-6 alkoxy optionally substituted by one or more fluorine atoms; R3 represents one or more groups independently selected from H, halogen, C1-4 alkoxy and CF3; in addition, R2 and one R3 group may together represent —OCH2—, the methylene group being attached to the ortho-position of the pendant phenyl ring; R4 represents a 4-, 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing 1 or 2 heteroatoms selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent or represents a cyclic group or an open chain group; and the pharmaceutically acceptable salts thereof.Type: GrantFiled: June 4, 2003Date of Patent: June 15, 2004Inventors: Alan John Collis, David Nathan Abraham Fox, Julie Newman
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Patent number: 6740654Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the saltType: GrantFiled: July 5, 2001Date of Patent: May 25, 2004Assignee: Celltech R & D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Publication number: 20040019064Abstract: Novel pyridopyrimidine derivatives which have a binding affinity for the human 5-HT6 receptor and, therefore, are useful in treating disorders responsive to antagonism of the 5-HT6 receptor such as psychosis, schizophrenia, manic depression, depression, neurological disorder, memory disorder, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease and Huntington's chorea.Type: ApplicationFiled: July 15, 2003Publication date: January 29, 2004Inventors: Yong-Jin Wu, Shuanghua Hu, Paul M. Scola, Yazhong Huang, Katharine A. Grant-Young
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Publication number: 20040002505Abstract: The present invention provides a medicinal composition having an excellent antitumor activity.Type: ApplicationFiled: March 31, 2003Publication date: January 1, 2004Inventors: Yoichi Ozawa, Kentaro Yoshimatsu, Junko Kai
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Publication number: 20030229104Abstract: Substituted 3,4-dihydropyrido[1,2-a]pyrimidines of formula I 1Type: ApplicationFiled: April 11, 2003Publication date: December 11, 2003Applicant: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul, Utz-Peter Jagusch
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Patent number: 6649604Abstract: Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-&agr;, IL-1&bgr;, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: GrantFiled: April 23, 2002Date of Patent: November 18, 2003Assignee: Amgen Inc.Inventors: Ulrike D. Spohr, Michael J. Malone, Nathan B. Mantlo, Jeffrey A. Zablocki
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Publication number: 20030114458Abstract: The present invention provides compounds of Formula (I): 1Type: ApplicationFiled: May 29, 2002Publication date: June 19, 2003Inventors: Edmund Lee Ellsworth, Howard Daniel Hollis Showalter
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Publication number: 20030022890Abstract: Novel heterocyclic dihydropyrimidine compounds useful as inhibitors of potassium channel function (especially inhibitors of the Kv1 subfamily of voltage gated K+ channels, especially inhibitors Kv1.5 which has been linked to the ultra-rapidly activating delayed rectifier K+ current IKur), methods of using such compounds in the prevention and treatment of arrhythmia and IKur-associated conditions, and pharmaceutical compositions containing such compounds.Type: ApplicationFiled: December 5, 2000Publication date: January 30, 2003Inventors: Karnail S. Atwal, Wayne Vaccaro, John Lloyd, Heather Finlay, Lin Yan, Rao S. Bhandaru
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Patent number: 6506762Abstract: The present invention also provides a general method to whereby mono-, bi-, or tricyclic heterocycles may be modified to obtain potent antagonists at the NPY1 receptor. The present invention provides novel, potent, non-peptidic antagonists of NPY receptors, particularly, the NPY1 receptors, designed from a selection of mono-, bi-, or tri-cyclic heterocyclic cores. This invention relates to novel compounds, compositions, and methods for the treatment of physiological disorders associated with an excess of neuropeptide Y. The novel compounds encompassed by the present invention are those of the formula I-XV.Type: GrantFiled: September 29, 2000Date of Patent: January 14, 2003Assignees: Neurogen Corporation, Pfizer Inc.Inventors: Raymond F. Horvath, Jennifer Tran, Stéphane De Lombaert, Kevin J. Hodgetts, Philip A. Carpino, David A. Griffith
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Patent number: 6479484Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.Type: GrantFiled: August 8, 2000Date of Patent: November 12, 2002Assignee: Euro-Celtique S.A.Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
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Publication number: 20020132817Abstract: A compound represented by the formula: 1Type: ApplicationFiled: March 13, 2002Publication date: September 19, 2002Inventors: Hideaki Natsugari, Takayuki Doi, Yoshinori Ikeura