Sulfur Attached Indirectly To The Diazine Ring By Nonionic Bonding (e.g., Thiamines, Etc.) Patents (Class 544/327)
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Publication number: 20110245257Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphoType: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: AMGEN INC.Inventors: Timothy D. Cushing, Jason A. Duquette, Xiao He, Julia Lohman, Youngsook Shin
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Publication number: 20110230485Abstract: This invention relates to novel 6-phenyl-phymidin-4-yl-(phenylannine or phenoxy) derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 9, 2009Publication date: September 22, 2011Applicant: NEUROSEARCH A/SInventors: Antonio Nardi, Jeppe Kejser Christensen, Dan Peters
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Publication number: 20110230445Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: May 26, 2011Publication date: September 22, 2011Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Publication number: 20110224233Abstract: The present invention relates compounds for stabilizing cells and methods of their use.Type: ApplicationFiled: June 1, 2011Publication date: September 15, 2011Applicant: The Scripps Research InstituteInventors: Yue Xu, Sheng Ding
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Publication number: 20110224432Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: February 1, 2011Publication date: September 15, 2011Applicant: AVILA THERAPEUTICS, INC.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 8013045Abstract: A process for mass-coloring high molecular weight material, in which process a compound of formula or a tautomer thereof, wherein M1 is H, ½ M2, ? M3 or NR4R5R6R7, preferably H, ½ M2 or NR4R5R6R7, especially H, M2 is an alkaline earth or transition metal in oxidation state II or an oxo-metal in oxidation state IV, M3 is Al(III), a transition metal in oxidation state III or an oxo-metal in oxidation state V, R1 is H or a non-ionic substituent, R2 is H or, independently of R1, a further non-ionic substituent, R3 is H, C1-C6alkyl, phenyl, CO—C1-C6alkyl or CO-phenyl, preferably H or CO—C1-C6alkyl, especially H, and R4, R5, R6 and R7 are each independently of the others H or phenyl, benzyl or C1-C6alkyl, which are unsubstituted or may be substituted by hydroxy or by halogen and in the case of C3-C6alkyl is uninterrupted or interrupted by O, is incorporated into the high molecular weight material before or during shaping.Type: GrantFiled: June 24, 2009Date of Patent: September 6, 2011Assignee: BASF SE LudwigshafenInventors: Thomas Ruch, Ursula Luterbacher
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Patent number: 8008307Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: GrantFiled: August 6, 2007Date of Patent: August 30, 2011Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
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Publication number: 20110201605Abstract: The invention relates to compounds of formula where hetaryl I, hetaryl II, R1, R2, R3, R4, m, n, and o are as defined in the specification or to pharmaceutically active acid addition salts thereof. The compounds of formula I are modulators for amyloid beta and thus may be useful for the treatment or prevention of a disease associated with the deposition of ?-amyloid in the brain, in particular Alzheimer's disease, and other diseases such as cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome.Type: ApplicationFiled: February 9, 2011Publication date: August 18, 2011Inventors: Karlheinz Baumann, Alexander Flohr, Erwin Goetschi, Luke Green, Synese Jolidon, Henner Knust, Anja Limberg, Thomas Luebbers, Andrew Thomas
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Publication number: 20110183957Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 4, 2009Publication date: July 28, 2011Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Publication number: 20110178300Abstract: The present invention is directed to a process for the manufacture of compounds of formula IV wherein R1 is an amino protecting group, and R2 is hydrogen or C1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M+ is a cation, preferably selected from the group consisting of Li+, Na+, K+, ms, ½ Mg2+ and ½ Zn2+, (formula 1a) with an ammonium salt NH4X?, wherein X? is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R2—CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B1.Type: ApplicationFiled: July 22, 2009Publication date: July 21, 2011Inventors: Reinhard Karge, Ulla Letinois, Gerhard Shiefer
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Publication number: 20110136666Abstract: The present invention relates to substituted pyrimidine derivatives as well as N-oxides and agriculturally acceptable salts thereof, and their use to control undesired plant growth, in particular in crops of useful plants. The invention extends to herbicidal compositions comprising such compounds, N-oxides and/or salts as well as mixtures of the same with one or more further active ingredient (such as, for example, an herbicide, fungicide, insecticide and/or plant growth regulator) and/or a safener.Type: ApplicationFiled: April 30, 2009Publication date: June 9, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: William Guy Whittingham, Caroline Louise Winn, John Williams, Harry Glithro
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Publication number: 20110110914Abstract: Methods and formulations for treating oncological disorders in humans using epimetabolic shifters, multidimensional intracellular molecules or environmental influencers are described.Type: ApplicationFiled: May 11, 2010Publication date: May 12, 2011Inventors: Niven Rajin Narain, John Patrick McCook, Rangaprasad Sarangarajan
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Publication number: 20110092695Abstract: A method of generating a chronic myelogenic leukemia (CML) acquired chemoresistant culture model is provided. Such a method may comprise providing a naïve blast crisis CML cell line; administering/contacting the cell line with a mutation-inducing dose of imatinib; maintaining a culture of the treated cell line for a period of time until the treated cell line relapses and repopulates the culture; and determining the repopulated cell culture is a CML acquired chemoresistant cell line by detecting a BCR-ABL mutation, wherein the acquired chemoresistance is achieved by a BCR-ABL mutation.Type: ApplicationFiled: October 8, 2010Publication date: April 21, 2011Inventors: WenYong Chen, Ravi Bhatia, Leila Su, Yate-Ching Yuan
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Patent number: 7910594Abstract: This invention relates to vitamin-mitomycin conjugates, to a method of using the conjugates to selectively eliminate a population of pathogenic cells in a host animal harboring the pathogenic cells, and to a method of preparation of the conjugates. The conjugate is of the general formula B-L-X wherein the group B is a vitamin, or an analog or a derivative thereof, that binds to a surface accessible vitamin receptor that is uniquely expressed, overexpressed, or preferentially expressed by a population of pathogenic cells, wherein the group L comprises a cleavable linker, and wherein the group X comprises a mitomycin compound, or an analog or a derivative thereof. An additional therapeutic agent, such as a chemotherapeutic agent, can be administered in combination with the conjugate.Type: GrantFiled: May 13, 2003Date of Patent: March 22, 2011Assignee: Endocyte, Inc.Inventors: Iontcho Radoslavov Vlahov, Christopher P. Leamon
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Publication number: 20110053916Abstract: The present invention relates to compounds useful as inhibitors of treating tuberculosis.Type: ApplicationFiled: August 12, 2010Publication date: March 3, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Brian Hanzelka, Ute Muh, Guy Bemis
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Publication number: 20110033560Abstract: The present invention relates to the use of a preparation comprising a substance that is capable of binding acetaldehyde, and to the use of a filter that is attached to a tobacco product to reduce tobacco and/or alcohol dependence.Type: ApplicationFiled: September 12, 2008Publication date: February 10, 2011Applicant: BIOHIT OYJInventors: Osmo Suovaniemi, Mikko Salaspuro, Ville Salaspuro, Martti Marvola
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Publication number: 20110028503Abstract: Compounds I and II as well as salts and pharmaceutical compositions containing them are useful for treating diseases and/or disorders of the eye.Type: ApplicationFiled: July 28, 2010Publication date: February 3, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Vanessa Taylor, Hui Li, Rajinder Singh
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Publication number: 20110021491Abstract: New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein X1, X2, X3, X4, Y1, Y2, A, R1, R2, R3, R4, m, n, p, and q are as defined herein, including stereoisomers, esters, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof in a patient in need thereof.Type: ApplicationFiled: June 23, 2010Publication date: January 27, 2011Applicants: BOEHRINGER INGELHEIM INTERNATIONAL GMBH, NEUROCRINE BIOSCIENCES, INC.Inventors: Joe A. TRAN, Chen CHEN
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Publication number: 20100331338Abstract: Novel compounds of the Formula (I) in which R1, R2, R3, and R4 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Type 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: February 2, 2009Publication date: December 30, 2010Applicant: Merck Patent GMBHInventors: Lars Burgdorf, Ulrich Emde, Johannes Gleitz, Norbert Beier, Christine Charon
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Publication number: 20100311743Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: May 7, 2010Publication date: December 9, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Marion Wannamaker, Tiansheng Wang
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Publication number: 20100298267Abstract: The present application relates to novel aminopyrimidinamides, to processes for their preparation and to their use for controlling animal pests, especially arthropods, in particular insects.Type: ApplicationFiled: February 17, 2010Publication date: November 25, 2010Applicant: Bayer CropScience AGInventors: Simon MAECHLING, Arnd Voerste, Eva-Maria Franken, Angela Becker, Ulrich Görgens, Mazen Es-Sayed, Markus Heil, Graham Holmwood, Johannes-Rudolf Jansen, Otto Schallner, Ulrich Ebbinghaus-Kintscher, Peter Lümmen, Silvia Cerezo-Galvez, Sachio Kudo, Takashi Hashihayata, Eiichi Shimojo, Teruyuki Ichihara, Masashi Ataka, Katsuhiko Shibuya
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Publication number: 20100286171Abstract: A phenylacetamide derivative having sulfonyl group and cycloalkyl group on the phenyl group and having heteroaryl group on the nitrogen atom in the amide has an excellent GK activation action, thereby completing the present invention. The compound of the present invention is useful as an agent for treating diabetes, in particular, type II diabetes, since it has an excellent GK activation action.Type: ApplicationFiled: January 16, 2009Publication date: November 11, 2010Applicant: ASTELLAS PHARMA INC.Inventors: Masahiko Hayakawa, Yoshiyuki Kido, Takahiro Nigawara, Mitsuaki Okumura, Akira Kanai, Keisuke Maki, Nobuaki Amino
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Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20100184780Abstract: The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceuticals compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases. formula (I).Type: ApplicationFiled: April 24, 2008Publication date: July 22, 2010Inventors: Heike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
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Publication number: 20100168132Abstract: Compounds of Formula (I) ; in salt or zwitterionic form wherein R1, R2, R3 and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor, especially inflammatory or obstructive airways diseases. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: ApplicationFiled: March 11, 2010Publication date: July 1, 2010Inventors: Neil John Press, Stephen Paul Collingwood, Urs Baettig, Brian Cox, Sudhakar Devidasrao Garad, Hyungshul Kim, Dimitris Papoutsakis, Simon James Watson
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Publication number: 20100160287Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: September 22, 2009Publication date: June 24, 2010Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marion W. Wannamaker, Francesco Salituro, Albert Pierce, Alex Aronov, Gabriel Martinez-Botella, Jian Wang, Luc Farmer, Mark Ledeboer, Tiansheng Wang, Randy Bethiel, Brian Ledford, Emilie Porter Huck
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Publication number: 20100137275Abstract: The present invention relates to the novel triaminopyrimidine derivatives of formula (I) in which R1, R2, W, R3, R4, and R5 are variable groups. These products have a Cdc25-phosphatase-inhibiting activity. The invention also relates to a process for synthesizing these compounds and also to therapeutic compositions containing these products and to the use thereof as medicaments.Type: ApplicationFiled: April 30, 2008Publication date: June 3, 2010Applicant: IPSEN PHARMA S.A.S.Inventors: Grégorie Prevost, Anne-Marie Liberatore, Dennis Bigg, Dominique Pons
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Publication number: 20100081812Abstract: Substituted pyrimidine derivatives of formula (I), salts, metabolites, prodrugs and diastereoisomeric forms (both isolated stereoisomers and mixtures of stereoisomers) thereof (wherein A=pyrimidine) pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and angiogenesis disorders, as a sole agent or in combination with other active ingredients, e.g., cytotoxic therapies.Type: ApplicationFiled: December 20, 2006Publication date: April 1, 2010Inventors: Roger Smith, Jacques Dumas, Gan Wang, Wendy Lee, Karl Miranda
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Publication number: 20100063063Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.Type: ApplicationFiled: September 9, 2009Publication date: March 11, 2010Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
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Publication number: 20100016296Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: April 20, 2009Publication date: January 21, 2010Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Publication number: 20090325981Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).Type: ApplicationFiled: February 11, 2005Publication date: December 31, 2009Applicant: IRM LLCInventors: Valentina Molteni, Xiaolin Li, Juliet Nabakka, David Archer Ellis, Beth Anaclerio, Enrique Saez, John Wityak
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Publication number: 20090227790Abstract: The present application is directed to therapeutic compounds, compositions, and methods for culturing neuronal cells and for preventing and the treatment of neurodegenerative diseases, such as Parkinson's disease and amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: April 7, 2009Publication date: September 10, 2009Inventor: Leu-Fen H. Lin
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Patent number: 7547782Abstract: The present invention is directed to compounds having the formula I or II: including salts thereof, and methods for using them for the treatment of cancer.Type: GrantFiled: September 28, 2006Date of Patent: June 16, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Robert M. Borzilleri, Xiao-Tao Chen, David K. Williams, John S. Tokarski, Robert F. Kaltenbach
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Publication number: 20090137588Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: October 17, 2008Publication date: May 28, 2009Applicant: Avila Therapeutics, Inc.Inventors: Juswinder Singh, Shomir Ghosh, Arthur F. Kluge, Russell C. Petter, Richland W. Tester
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Patent number: 7538215Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.Type: GrantFiled: June 2, 2005Date of Patent: May 26, 2009Assignees: Elan Pharmaceuticals, Inc., WyethInventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Christopher Semko, Christopher Joseph Soares, Christine M. Tarby
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Patent number: 7507733Abstract: Compounds of the formula (I): as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.Type: GrantFiled: June 27, 2005Date of Patent: March 24, 2009Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander Mayweg, Werner Neidhart
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Publication number: 20090075986Abstract: Novel compounds and methods of using those compounds for the treatment of inflammatory conditions are provided. In a preferred embodiment, modulation of the activation state of p38 kinase protein comprises the step of contacting the kinase protein with the novel compounds.Type: ApplicationFiled: June 9, 2006Publication date: March 19, 2009Inventors: Daniel L. Flynn, Peter A. Petillo
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Publication number: 20080293741Abstract: Compounds of Formula (I): (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.Type: ApplicationFiled: March 11, 2006Publication date: November 27, 2008Inventors: Matthew Colin Thor Fyfe, Martin James Procter
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Publication number: 20080275063Abstract: The present invention provides new compounds. The compounds are useful as CDK5 inhibitors, and accordingly they can be included in pharmaceutical compositions for treating any type of pain, inflammatory disorders, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases and neurodegenerative diseases.Type: ApplicationFiled: April 24, 2007Publication date: November 6, 2008Inventors: Heike Schauerte, Hans Allgeier, Michael A. Pleiss, Martin Augustin, Gisela Peraus, Gabriele Stumm, Philipp Wabnitz
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Publication number: 20080242681Abstract: Compounds of a certain formula 1 in which R1 and R2 have the meanings indicated in the description are novel kinase inhibitors. Formula (1), in which R1 is phenyl, phenyl substituted by R3 and/or R4, naphthalenyl, naphthalenyl substituted by and/or R6, aryl1, aryl1 substituted by R7 and/or R8, R9, R10 or R11, R2 is phenyl, phenyl substituted by R12 and/or R13, naphthalenyl, naphthalenyl substituted by R14 and/or R15, aryl2, aryl2 substituted by R16 and/or R17 or a radical selected from Formula (2).Type: ApplicationFiled: January 19, 2005Publication date: October 2, 2008Applicant: Altana Pharma AGInventors: Johannes Barsig, Monika Baudler, Daniela Bundschuh, Florian Gantner, Ulrich Graedler, Isabelle Heit, Thomas Martin, Michaela Schaefer, Imre Schlemminger, Josef Stadlwieser, Wolf-Ruediger Ulrich
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Publication number: 20080242863Abstract: The present invention relates to a novel process for the manufacture of Grewe-diamine comprising the following step: hydrolyzing a compound of formula (II), wherein R is hydrogen or straight- or branched chain C1-4 alkyl, with an aqueous alkali or alkaline-earth metal hydroxide solution, characterized in that the hydrolysis is carried out in the presence of an organic solvent.Type: ApplicationFiled: January 24, 2006Publication date: October 2, 2008Inventors: Werner Bonrath, Jocelyn Fischesser, Lisa Giraudi, Reinhard Karge
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Publication number: 20080207606Abstract: Novel heterocyclic compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof are described. These compounds are useful in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell-damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; adult respiratory distress syndrome (ARDS); psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever.Type: ApplicationFiled: February 8, 2008Publication date: August 28, 2008Applicant: ORCHID RESEARCH LABORATORIES LIMITED.Inventors: Akella Satya Surya Visweswara Srinivas, Ravikumar Tadiparthi, Ganapavarapu Veera Raghava Sharma, Sappanimuthu Thirunavukkarasu, Durairaj Peter Bhakiaraj, Virendra Kachhadia, Kilambi Narsimhan, Sathya Narayana Thara, Sriram Rajagopal, Gaddam Om Reddy, Sukunath Narayanan, Venkatesan Parameswaran, Venkatesan Janarthanam, Maruthikumar Narayanam, Sathyanarayana Gadde, Uma Ramachandran
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Publication number: 20080146599Abstract: The invention relates to a compound of the Formula (I) or salt, prodrug or solvate thereof, wherein Rx, Ry, Rz, R5, R6, A, B, L, n and m are as defined in the description. The invention also relates to pharmaceutical compositions of said compounds, the use of said compounds as medicaments and in the production of an anti-angiogenic effect in a warm blooded animal. The invention also relates to processes for the preparation of said compounds.Type: ApplicationFiled: January 27, 2006Publication date: June 19, 2008Applicant: ASTRAZENECA ABInventors: Clifford David Jones, Richard William Arthur Luke, William McCoull
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Patent number: 7348334Abstract: The present invention relates to novel hypolipidemic, antihyperglycemic compounds, their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them. More particularly, the present invention relates to novel ?-aryl-?-oxysubstituted alkylcarboxylic acids of the general formula (I), their derivatives, their analogs, their tautomeric forms, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutically acceptable compositions containing them.Type: GrantFiled: April 8, 2002Date of Patent: March 25, 2008Assignee: Dr. Reddy's Laboratories LimitedInventors: Javed Iqbal, Gurram Ranga Madhavan, Saibal Kumar Das, Debnath Bhunia, Ranjan Chakrabarti, Ramanujam Rajagopalan
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Publication number: 20080058356Abstract: 4-Aminopyrimidine derivatives of formula (I) FORMULA heteroaryl groups, including pharmaceutically acceptable salts thereof, wherein R1 and R2 are adenosine A2A receptor antagonists useful in the treatment of movement disorders such as Parkinson's disease.Type: ApplicationFiled: December 14, 2004Publication date: March 6, 2008Applicant: Neurocrine Biosciences, Inc.Inventors: Maria Isabel Crespo Crespo, Maria Prat Quinones, Siliva Gual Roig, Julio Cesar Castro Palomino Laria, Deborah H. Slee
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Patent number: 7317016Abstract: This invention relates to methods of treatment of cardiovascular disorders, thromboembolic disorders, inflammation, and disorders of the central nervous system using pyrazol pyridine derivatives of formula (I) wherein R1 is a radical of the formula —O—SO2—R3 in which R3 is optionally substituted C1-6-alkyl, optionally substituted C3-8-cycloalkyl, or optionally substituted phenyl; R2 is H, optionally substituted C1-6-alkyl-CO— or optionally substituted C1-6-alkyl-SO2—; as well as salts, stereoisomers, tautomers, and hydrates thereof.Type: GrantFiled: July 5, 2005Date of Patent: January 8, 2008Assignee: Bayer AktiengesellschaftInventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elisabeth Perzborn
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Patent number: 7291622Abstract: This invention relates to methods for treating sexual dysfunction, by administering a compound of the formula wherein R1 is H or a di-C1-6-alkylaminocarbonyl radical, and R2 is a radical of the formula —O—C(X)—NR3R4 wherein X is O or S. The compound may also be administered in combination with at least one organic nitrate or NO donor, or in combination with at least one compound which inhibits the breakdown of cyclic guanosine monophosphate (cGMP).Type: GrantFiled: July 29, 2005Date of Patent: November 6, 2007Assignee: Bayer AktiengesellschaftInventors: Johannes-Peter Stasch, Achim Feurer, Stefan Weigand, Elke Stahl, Dietmar Flubacher, Cristina Alonso-Alija, Frank Wunder, Dieter Lang, Klaus Dembowsky, Alexander Straub, Elizabeth Perzborn
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Patent number: RE42462Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: October 7, 1995Date of Patent: June 14, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Patent number: RE42477Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: March 27, 1997Date of Patent: June 21, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack