Additional Hetero Ring Attached Directly Or Indirectly To The Morpholines By Nonionic Bonding Patents (Class 514/232.2)
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Publication number: 20090215765Abstract: Neuroprotective compounds for treating optic neuropathies and screening methods for identifying neuroprotective compounds.Type: ApplicationFiled: April 24, 2006Publication date: August 27, 2009Applicant: The Johns Hopkins UniversityInventors: John Barnwell Kerrison, Donald J. Zack
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Publication number: 20090191177Abstract: The present invention relates to enantiomerically pure (?) 2-[1-(7-methyl-2-(morpholin-4-yl)-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)ethylamino]benzoic acid or pharmaceutically acceptable salts thereof, it being in a solid state, its use in medical therapy, pharmaceutical composition comprising it, its use in the preparation of a medicament for use in a method for preventing or treating diseases, and its use in method for preventing or treating disease. The present invention relates to a selective inhibitor of phosphoinositide (PI) 3-kinase ? and use of the selective inhibitor in e.g. anti-thrombotic therapy.Type: ApplicationFiled: January 25, 2009Publication date: July 30, 2009Inventors: Ola Fjellstrom, David Gustafsson, Jan A. Lindberg, Shaun Jackson
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Patent number: 7528130Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: January 6, 2006Date of Patent: May 5, 2009Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler
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Publication number: 20090054428Abstract: The invention concerns compounds of Formula I, or a pharmaceutically acceptable salt thereof, where R1, Q, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.Type: ApplicationFiled: July 17, 2008Publication date: February 26, 2009Applicant: ASTRAZENECA ABInventors: Bernard Christophe Barlaam, Richard Ducray
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Publication number: 20090036440Abstract: The invention concerns pyrimidine compounds of Formula I, or a pharmaceutically acceptable salt thereof, where A1, A2 A3, R1, n, R2, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.Type: ApplicationFiled: April 25, 2008Publication date: February 5, 2009Applicant: AstraZeneca ABInventors: Bernard Christophe BARLAAM, Richard DUCRAY
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Patent number: 7476669Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: April 18, 2007Date of Patent: January 13, 2009Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler
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Publication number: 20080287431Abstract: Heterocyclic compounds represented by the formula I and anti-malignant-tumor agents containing the heterocyclic compounds as effective components: wherein X represents nitrogen atom or CH; Y represents C1-C6 alkyl; R1 represents morpholino (which may be substituted with one to four C1-C6 alkyl); and R2 and R3 each represent hydrogen atom or C1-C6 alkyl.Type: ApplicationFiled: March 30, 2005Publication date: November 20, 2008Applicant: ZENYAKU KOGYO KABUSHIKI KAISHAInventors: Seiichiro Kawashima, Mitsuko Kawashima, Hiroto Kawashima, Masato Kawashima, Toshiyuki Matsuno, Shinichi Yaguchi, Yoshio Tsuchida, Kenichi Saitoh, Tetsuo Watanabe
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Publication number: 20080242663Abstract: The invention concerns compounds of Formula I, or a pharmaceutically acceptable salt thereof, where R1, n, R2, R3, and R4 are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours or other proliferative conditions which are sensitive to the inhibition of EphB4 kinases.Type: ApplicationFiled: February 28, 2008Publication date: October 2, 2008Applicant: ASTRAZENECA ABInventors: Susan Elizabeth Ashton, Darren Anthony Edward Cross, Simon John East, Jason Grant Kettle, Mark Andrew Pearson, Stephen Robert Wedge, Bernard Christophe Barlaam, Richard Ducray, Stuart Charles Purkiss
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Publication number: 20080194552Abstract: The invention relates to a compound of the Formula I or salt thereof wherein Rx, Ry, Rx, 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: March 30, 2006Publication date: August 14, 2008Applicant: ASTRAZENECA ABInventors: Clifford David Jones, Richard William, Arthur Luke, William McCoull
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Publication number: 20080167300Abstract: This invention features compounds of formula (I): pharmaceutical compositions of the compounds, and methods of using the compounds for the treatment of, inter alia, IL-12-related diseases and disorders.Type: ApplicationFiled: March 3, 2008Publication date: July 10, 2008Inventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Teresa Przewloka, Hao Li, Howard P. Ng, Zachary Demko
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Patent number: 7390804Abstract: An N-containing five-membered ring compound of formula (I) wherein all symbols are the same as described in the specification, and a non-toxic salt thereof. The compound of formula (I) has an inhibitory activity against cysteine protease and therefore it is useful as an agent for the prophylaxis and/or treatment of inflammatory diseases, diseases induced by apoptosis, diseases induced by disorders of immune responses, autoimmune diseases, diseases induced by decomposition of proteins which compose organism, shock, circulatory system disorders, blood coagulation systems disorders, malignant tumors, acquired immune deficiency syndrome (AIDS) and AIDS-related complex (ARC), parasitic diseases, nerve degeneration diseases, pulmonary disorders, bone resorption diseases, endocrinesthenia, etc.Type: GrantFiled: December 22, 2004Date of Patent: June 24, 2008Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Kazuyuki Ohmoto, Iori Itagaki
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Patent number: 7365067Abstract: The present invention provides a compound having the following general formula (I) which is useful as a neurokinin receptor antagonist: (wherein, R1, R2: optionally substituted (hetero)aryl, R3: —CO—R4, —CO—O—R4, etc., R4: alkyl, cycloalkyl, etc., A: CH2, CO, SO2, B: a single bond, etc., D: oxygen, CH2, E: alkylene, alkenylene, n: 1 to 3).Type: GrantFiled: February 24, 2005Date of Patent: April 29, 2008Assignee: Sankyo Company, LimitedInventors: Takahide Nishi, Toshiyasu Takemoto, Takuya Ikeda, Kiyoshi Morimoto
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Patent number: 7358247Abstract: Provided is an impurity of mycophenolate mofetil, processes for its preparation and its use as a reference.Type: GrantFiled: April 26, 2005Date of Patent: April 15, 2008Assignee: TEVA Gyógyszergyár Zártköruen Muködö RészvénytársaságInventors: Sandor Molnar, Tivadar Tamas, Janos Hajko, Beáta Kosztya, Amihai Eisenstadt
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Patent number: 7317008Abstract: A method of treating ischemic reperfusion injury in a subject. The method may include administering to the subject an effective amount of a pharmaceutically acceptable formulation. The pharmaceutically acceptable formulation may include a synthetic analog or derivative of a carotenoid. The subject may be administered a carotenoid analog or derivative, either alone or in combination with another carotenoid analog or derivative, or co-antioxidant formulation. The carotenoid analog may include a conjugated polyene with between 7 to 14 double bonds. The conjugated polyene may include a cyclic ring including at least one substituent. In some embodiments, a cyclic ring of a carotenoid analog or derivative may include at least one substituent. The substituent may be coupled to the cyclic ring with an ester functionality.Type: GrantFiled: March 4, 2004Date of Patent: January 8, 2008Assignee: Cardax Pharmaceuticals, Inc.Inventors: Samuel Fournier Lockwood, Sean O'Malley, David G. Watumull, Laura M. Hix, Henry Jackson, Geoff Nadolski
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Patent number: 7276499Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: January 13, 2006Date of Patent: October 2, 2007Assignee: Immunogen Inc.Inventors: Ravi V. J. Chari, Walter A. Blattler
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Patent number: 7208491Abstract: Mono-acylated o-phenylendiamines derivatives of formula I wherein X and R are as described herein, have been found useful for the treatment of diseases mediated by the inhibition of histone deacetylase, such as cancer.Type: GrantFiled: February 3, 2004Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 7183278Abstract: Disclosed are novel compounds useful for the control of harmful organisms, harmful organism control agents using the same, and processes for producing the novel compounds. The useful novel compounds according to the present invention include compounds represented by formula (1).Type: GrantFiled: November 4, 1999Date of Patent: February 27, 2007Assignee: Meiji Seika Kaisha, Ltd.Inventors: Keiichi Imamura, Kouichi Mitomo, Natsuko Yamada, Kazumi Yamamoto, Takashi Teraoka, Osamu Sakanaka, Hiroshi Kurihara, Makoto Taniguchi
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Patent number: 7173024Abstract: Compounds of the formula (I), wherein the symbol aa means a residue of an ?-amino acid. The invention is also directed to a method for the preparation of the compounds of formula (I), as well as their use as prolyl oligopeptide inhibitors, for example for the treatment of Alzheimer's disease.Type: GrantFiled: July 4, 2002Date of Patent: February 6, 2007Assignee: Orion CorporationInventors: Jukka Gynther, Pekka Männistö, Erik Wallen, Johannes Christiaans, Markus Forsberg, Antti Poso, Jarkko Venäläinen, Elina Jarho
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Patent number: 7166594Abstract: Group A streptogramin derivatives of general formula (I) in which: R1 represents a halogen atom or an azido or thiocyanato radical, R2 represents a hydrogen atom or a methyl or ethyl radical, R3 represents a hydrogen atom, or the residue of an aliphatic, cycloaliphatic, aromatic, araliphatic, heterocyclic or heterocyclylaliphatic ester which may be substituted, and the bond --- represents a single bond (stereochemistry 27R) or a double bond, as well as its salts when they existType: GrantFiled: December 6, 2002Date of Patent: January 23, 2007Assignee: Aventis Pharma S.A.Inventors: Daniel Achard, Eric Bacque, Jean-Claude Barriere, Jean Bouquerel, Pascal Desmazeau, Serge Grisoni, Jean-Pierre Leconte, Yves Ribeill, Baptiste Ronan
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Patent number: 7109186Abstract: The present invention describes novel compounds of Formula I which inhibit HIV integrase.Type: GrantFiled: July 9, 2003Date of Patent: September 19, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Michael A. Walker, Zhuping Ma, B. Narasimhulu Naidu, Margaret E. Sorenson, Annapurna Pendri, Jacques Banville, Serge Plamondon, Roger Remillard
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Patent number: 7037918Abstract: New pyrimidine or pyridine based compounds, compositions and methods of inhibiting the activity of glycogen synthase kinase (GSK3) in vitro and of treatment of GSK3 mediated disorders in vivo are provided. The methods, compounds and compositions of the invention may be employed alone, or in combination with other pharmacologically active agents in the treatment of disorders mediated by GSK3 activity, such as in the treatment of diabetes, Alzheimer's disease and other neurodegenerative disorders, obesity, atherosclerotic cardiovascular disease, essential hypertension, polycystic ovary syndrome, syndrome X, ischemia, traumatic brain injury, bipolar disorder, immunodeficiency or cancer.Type: GrantFiled: December 3, 2002Date of Patent: May 2, 2006Assignee: Chiron CorporationInventors: John M. Nuss, Stephen D. Harrison, David B. Ring, Rustum S. Boyce, Sean P. Brown, Dane A. Goff, Kirk W. Johnson, Keith B. Pfister, Savithri Ramurthy, Paul A. Renhowe, Lynn Seely, Sharadha Subramanian, Allan S. Wagman, Xiaohui A. Zhou
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Patent number: 7030110Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.Type: GrantFiled: October 4, 2002Date of Patent: April 18, 2006Assignee: Ortho-McNeil Pharmaceuticals, Inc.Inventors: Aihua Wang, Bruce Edward Tomczuk, Tianbao Lu, Richard M. Soll, John Curtis Spurlino, Roger Francis Bone
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Patent number: 7015223Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyrimidinone compounds useful as inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.Type: GrantFiled: November 20, 2000Date of Patent: March 21, 2006Assignee: Pharmacia CorporationInventors: Michael S. South, Ashton T. Hamme, II, William L. Neumann, Darin E. Jones, Melvin L. Rueppel
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Patent number: 7008942Abstract: A cytotoxic agent comprising one or more taxanes linked to a cell binding agent. A therapeutic composition for killing selected cell populations comprising: (A) a cytotoxic amount of one or more taxanes covalently bonded to a cell binding agent through a linking group, and (B) a pharmaceutically acceptable carrier, diluent or excipient. A method for killing selected cell populations comprising contacting target cells or tissue containing target cells with an effective amount of a cytotoxic agent comprising one or more taxanes linked to a cell binding agent. Novel sulfur-containing taxanes.Type: GrantFiled: October 15, 2003Date of Patent: March 7, 2006Assignee: Immunogen, Inc.Inventors: Ravi V. J. Chari, Walter A. Blättler
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Patent number: 6844347Abstract: The invention relates to compounds of formula I, in which R1, R2, R3 and R4 have the meanings given in the claims. Said compounds are valuable active ingredients for the treatment and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, heart failure, thrombosis or atherosclerosis. The compounds of the formula I are able to modulate the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the treatment and prophylaxis of disorders associated with impaired cGMP balance. The invention furthermore relates to methods for producing compounds of the formula I, their use in the treatment and prophylaxis of the above diseases and in the preparation of medicaments for such diseases, and pharmaceutical preparations containing the compounds of formula I.Type: GrantFiled: August 4, 1999Date of Patent: January 18, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schnidler, Karl Schoenafinger, Hartmut Strobel
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Publication number: 20040259864Abstract: The invention relates to novel substituted pyrimidone derivatives which bind to integrin receptors, to their preparation and to their use.Type: ApplicationFiled: May 24, 2004Publication date: December 23, 2004Inventors: Herve Geneste, Andreas Kling, Johann-Christian Zechel, Arnulf Lauterbach, Werner Seitz, Claudia Isabella Graef, Thomas Subkowski, Wilfried Hornberger, Rainer Spriestersbach
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Patent number: 6833364Abstract: The present invention relates to novel substituted pyrazole derivatives of the general formula (I) in which the substituents R1, R2, R3, A, X and Y are each as defined, and to processes for their preparation and to their use as medicaments, in particular as medicaments for the treatment of cardiovascular disorders.Type: GrantFiled: March 26, 2001Date of Patent: December 21, 2004Assignee: Bayer HealthCare AGInventors: Alexander Straub, Achim Feurer, Cristina Alonso-Alija, Elke Stahl, Johannes-Peter Stasch, Elisabeth Perzborn, Joachim Hütter, Klaus Dembowsky
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Patent number: 6831081Abstract: The present invention provides a compound of formula as described herein, which are useful as antiviral agents, in particular, as agents against viruses of the herpes family.Type: GrantFiled: August 27, 2003Date of Patent: December 14, 2004Assignee: Pharmacia & UpjohnInventors: Mark E. Schnute, Fred L. Ciske, Michael J. Genin, Joseph Walter Strohbach, Suvit Thaisrivongs
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Publication number: 20040248892Abstract: The present invention relates to a method for making an indolopyrrolocarbazole compound of the general formula [I], where the method includes the step of reacting a bisindolylmaleimide compound with an oxidizing agent in the presence of an oxygen containing gas at a temperature and for a time sufficient to yield the indolopyrrolocarbazole compound of the general formula [I]. Methods of making rebeccamycin analogs using the indolopyrrolocarbazole compound are also provided.Type: ApplicationFiled: July 21, 2004Publication date: December 9, 2004Inventor: Jianji Wang
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Patent number: 6828315Abstract: The present invention relates to triazolo[4,3-a]quinazoline-5-ones and 5-thiones of Formula I and Formula II, whereby I and II are position isomers of group R on nitrogen 3 or 4. Optionally, the invention also relates to the racemic forms, isomers and pharmaceutically acceptable salts thereof. The invention further relates to a method for the production thereof and to compositions containing said derivatives.Type: GrantFiled: October 25, 2001Date of Patent: December 7, 2004Assignee: Warner-Lambert LLCInventors: Bernard Gaudilliere, Remi Lavalette, Charles Andrianjara, Francine Breuzard
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Patent number: 6821970Abstract: The present invention provides oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R1, R2, R3 and R4 are described herein. These compounds are 5-HT ligands, and are useful for treating diseases wherein modulation of 5-HT activity is desired.Type: GrantFiled: May 16, 2002Date of Patent: November 23, 2004Assignee: Pharmacia & Upjohn CompanyInventor: Ruth Elizabeth TenBrink
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Publication number: 20040192685Abstract: This invention relates to compounds useful for treating or preventing obesity, breast cancer, osteoporosis, endometriosis, cardiovascular disease, prostatic disease, and the like, and to pharmaceutical composition, methods, and kits comprising such compounds.Type: ApplicationFiled: April 8, 2004Publication date: September 30, 2004Inventors: Kimberly O. Cameron, Richard Chesworth, Paul A. DaSilva-Jardine, Robert F. Day, Bruce A. Lefker, Michael P. Zawistoski
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Publication number: 20040116399Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.Type: ApplicationFiled: June 20, 2003Publication date: June 17, 2004Applicant: Millennium Pharmaceuticals, Inc.Inventors: Bing-Yan Zhu, Zhaozhong Jon Jia, Wenrong Huang, Yonghong Song, James Kanter, Robert M. Scarborough
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Patent number: 6743788Abstract: Disclosed are novel aromatic compounds of the formula(I) described herein, wherein G, E, W, Ar, X, Y and Z are disclosed herein. The compounds are useful for treating cytokine mediated diseases or conditions such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: May 17, 2002Date of Patent: June 1, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Pier Francesco Cirillo, Victor Kamhi, John Robinson Regan, Michele Tsang
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Publication number: 20040097497Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.Type: ApplicationFiled: August 27, 2003Publication date: May 20, 2004Applicant: Sugen, Inc.Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
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Publication number: 20040082589Abstract: Certain compounds of formula (I) below or a pharmaceutically acceptable salt or hydrate thereof: 1Type: ApplicationFiled: October 23, 2003Publication date: April 29, 2004Inventors: Carlo Farina, Stefania Gagliardi, Giuseppe Giardina, Mario Grugni, Marisa Martinelli, Guy Marguerite Marie Gerard
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Patent number: 6720319Abstract: Disclosed are novel cathepsin S, K, F, L and B reversible inhibitory compounds of the formula (Ia) and (Ib) where R2, R3, R4, R5, R6, R7, R8, Het and X are defined herein. The compounds are useful for treating autoimmune and other diseases. Also disclosed are processes for making such novel compounds.Type: GrantFiled: October 1, 2002Date of Patent: April 13, 2004Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Weimin Liu, Denice M. Spero, David S. Thomson, Yancey D. Ward, Erick R. R. Young
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Publication number: 20040067939Abstract: The present invention provides glucokinase activators of formula I: 1Type: ApplicationFiled: September 30, 2003Publication date: April 8, 2004Inventor: Wendy Lea Corbett
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Publication number: 20040043994Abstract: The present invention relates to a class of compounds represented by the Formula I.Type: ApplicationFiled: January 21, 2003Publication date: March 4, 2004Inventors: Ish Kumar Khanna, Yi Yu, Hwang-Fun Lu, Nizal S. Chandrakumar, Renee M. Huff, Mark Russell, Mark L. Boys, Lori A. Schretzman, Barbara B. Chen, Bipinchandra N. Desai, Srinivasan Raj Nagarajan, Alan F. Gasiecki, Thomas D. Penning, Thomas Rogers, John Adam Wendt, Albert Khilevich, Yaping Wang
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Publication number: 20040023954Abstract: 9,11-Cycloendoperoxide derivatives of biologically active prostaglandin analogs, and particularly of the ocular hypotensive drugs Bimatoprost, Latanaprost, Unoprostone, Travoprost and prostaglandin H2 1-ethanolamide or of structurally closely related analogs, are pro-drugs which hydrolyze under physiological conditions to provide prostaglandin analogues that are capable of providing sustained ocular and other in vivo concentrations of the respective drugs. The compounds of the invention have the formula shown below where the variables have the meaning defined in the specification.Type: ApplicationFiled: August 5, 2002Publication date: February 5, 2004Inventors: Kah-Hiing John Ling, Wu Yang, Jinsong Ni, Haiqing Yuan, Diane D.S. Tang-Liu
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Publication number: 20040019084Abstract: The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.Type: ApplicationFiled: April 21, 2003Publication date: January 29, 2004Applicant: SOCIETE DE CONSEILS DE RECHERCHES ET D'APPLICATION SCIENTIFIQUES (S.C.R.A.S)Inventors: Jeremiah Harnett, Michel Auguet, Pierre-Etienne Chabrier de Lassauhyere
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Publication number: 20040009976Abstract: This invention relates to certain novel imidazoline compounds and analogues thereof, to their use for the treatment of diabetes, diabetic complications, metabolic disorders, or related diseases where impaired glucose disposal is present, to pharmaceutical compositions comprising them, and to processes for their preparation.Type: ApplicationFiled: April 30, 2002Publication date: January 15, 2004Inventors: Kumiko Takeuchi, Michael Robert Jirousek, Michael Paal, Gerd Ruhter, Theo Schotten
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Patent number: 6670359Abstract: The present invention relates to new new piperidyl- or piperazinyl-substituted dihydro-2H-1-benzopyran derivatives compound having the formula (I) wherein X is N or CH; Y is NR2CH2, CH2NR2, NR2CO, CONR2, NR2SO2 or NR2CONR2 wherein R2 is H or C1-C6 alkyl; R1 is H, C1-C6 alkyl or C3-C6 cycloalkyl; R3 is C1-C6 alkyl, C3-C6 cycloalkyl or (CH2)n-aryl, wherein aryl is phenyl or a heteroaromatic ring containing one or two heteroatoms selected from N, O and S and which may be mono- or di-substituted with R4 and/or R5; and n is 0-4; as (R)-enantiomers, (S)-enantiomers or a racemate in the form of a free base or a pharmaceutically acceptable salt or solvate thereof, a process for their preparation, pharmaceutical compositions containing said therapeutically active compounds and to the use of said active compounds.Type: GrantFiled: November 1, 2002Date of Patent: December 30, 2003Assignee: AstraZeneca ABInventors: Stefan Berg, Martin Nylöf, Svante Ross, Seth-Olov Thorberg
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Publication number: 20030225069Abstract: The present invention relates to a group of aza-anthrapyrazole compounds having antitumor activity, and processes for their preparation. Compositions containing the aza-anthrapyrazole compounds and methods of treating tumors and cancer in mammals with the compounds of the present invention are also disclosed.Type: ApplicationFiled: March 12, 2002Publication date: December 4, 2003Inventor: Simon N. Haydar
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Publication number: 20030212057Abstract: The present invention relates to substituted piperidines of general formula 1Type: ApplicationFiled: November 7, 2002Publication date: November 13, 2003Inventors: Klaus Rudolf, Henri Doods, Eckhart Bauer, Rudolf Hurnaus, Wolfgang Eberlein, Alexander Dreyer, Stephan Georg Mueller
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Patent number: 6638930Abstract: Substituted heterocycles of the general structural formula: are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.Type: GrantFiled: April 17, 2001Date of Patent: October 28, 2003Assignee: Merck & Co. Inc.Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
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Publication number: 20030199500Abstract: The present invention relates compounds of the formula (1): wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 represent a variety of substituents; and pharmaceutically acceptable salts thereof. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migaine, emesis or postherpetic neuralgia.Type: ApplicationFiled: March 18, 2003Publication date: October 23, 2003Inventors: Brian John Williams, Christopher John Swain, Simon Neil Owen
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Publication number: 20030181445Abstract: The invention provides novel compounds of the formula I below: 1Type: ApplicationFiled: January 17, 2003Publication date: September 25, 2003Applicant: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Garrick Paul Smith, Christian Krog-Jensen, Klaus Peter Bogeso
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Patent number: 6608053Abstract: The present invention provides a pharmaceutical composition which is useful as a phosphatidylinositol 3 kinase (PI3K) inhibitor and an antitumor agent, and it provides a novel bicyclic or tricyclic fused heteroaryl derivative or a salt thereof which possesses an excellent PI3K inhibiting activity and cancer cell growth inhibiting activity.Type: GrantFiled: April 26, 2001Date of Patent: August 19, 2003Assignees: Yamanouchi Pharmaceutical Co., Ltd., Ludwig Institute for Cancer Research, Imperial Cancer Research Technology Ltd.Inventors: Masahiko Hayakawa, Hiroyuki Kaizawa, Hiroyuki Moritomo, Ken-Ichi Kawaguchi, Tomonobu Koizumi, Mayumi Yamano, Koyo Matsuda, Minoru Okada, Mitsuaki Ohta
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Patent number: RE38761Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, which is a substituted styrene compound which can also be a naphthalene, an indane or a benzoxazine; including nitrile and molononitrile compounds, and pharmaceutical compositions comprising, in admixture with a pharmaceutically acceptable carrier, a pharmaceutically-effective amount of such compound.Type: GrantFiled: October 14, 1994Date of Patent: July 19, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Alexander Levitzki, Chaim Gilon, Michael Chorev, Aviv Gazit