Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Five- Membered Hetero Ring Patents (Class 546/278.1)
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Publication number: 20080249091Abstract: There is provided compounds of formula I, wherein X1, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: December 22, 2005Publication date: October 9, 2008Inventors: Benjamin Pelcman, Kristofer Olofsson, Martins Katkevics, Vita Ozola, Edgars Suna, Ivars Kalvins, Peteris Trapencieris
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Publication number: 20080188472Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia, e.g. myocardial ischemia, or as cardioprotectants or inhibitors of abnormal cell growth.Type: ApplicationFiled: March 8, 2005Publication date: August 7, 2008Applicant: PROSIDION LIMITEDInventors: Stuart Edward Bradley, Revathy Perpetua Jeevaratnam, Thomas Martin Krulle, Martin James Procter, Robert John Rowley, Gerard Hugh Thomas, Ana Valdes
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Publication number: 20080188473Abstract: There is provided a compound of formula: (I) wherein X, R1, R2, R3, R4, R5, R6, R7 and R8 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: June 17, 2005Publication date: August 7, 2008Inventors: Kristofer Olofsson, Benjamin Pelcman, Wesley Schaal, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Publication number: 20080171772Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, o, A, A1, A2, X, Z, R1, R3, R2, p, q and r are as defined in the specification.Type: ApplicationFiled: January 11, 2008Publication date: July 17, 2008Inventors: Richard L. Beard, Haiging Yuan, John E. Donello, Xiaoxia Liu, Tien Duong
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Patent number: 7390907Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, 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, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, dType: GrantFiled: September 30, 2004Date of Patent: June 24, 2008Assignee: Amgen Inc.Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
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Publication number: 20080146616Abstract: There is provided a compound of formula (I), wherein X, R1, R2, R3, R4, R5 and R6 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of microsomal prostaglandin E synthase-1 is desired and/or required, and particularly in the treatment of inflammation.Type: ApplicationFiled: June 17, 2005Publication date: June 19, 2008Inventors: Kristofer Olofsson, Benjamin Pelcman, Wesley Schaal, Ivars Kalvins, Edgars Suna, Vita Ozola, Martins Katkevics
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Publication number: 20080114034Abstract: Compounds of the formula (1): in which A, R1, R2 and R3 are as defined in the description, the processes for the preparation of these compounds, the uses thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, and the pharmaceutical compositions comprising them.Type: ApplicationFiled: December 17, 2005Publication date: May 15, 2008Inventors: Nathalie Adje, Didier Roche, Stephane Yvon
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Patent number: 7365061Abstract: Novel compounds are provided which are glycogen phosphorylase inhibitors which are useful in treating, preventing or slowing the progression of diseases requiring glycogen phosphorylase inhibitor therapy such as diabetes and related conditions (such as hyperglycemia, impaired glucose tolerance, insulin resistance and hyperinsulinemia), the microvascular complications associated with diabetes (such as retinopathy, neuropathy, nephropathy and delayed wound healing), the macrovascular complications associated with diabetes (cardiovascular diseases such as atherosclerosis, abnormal heart function, myocardial ischemia and stroke), as well as Metabolic Syndrome and its component conditions including hypertension, obesity and dislipidemia (including hypertriglyceridemia, hypercholesterolemia and low HDL), and other maladies such as non-cardiac ischemia, infection and cancer.Type: GrantFiled: November 14, 2005Date of Patent: April 29, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Philip M. Sher, Gang Wu, Wei Meng, Alexandra A. Nirschl, William N. Washburn, Terry Stouch
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Patent number: 7323470Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, M1, M2, M3, M4, Y1 and Z are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: April 17, 2006Date of Patent: January 29, 2008Assignee: Boehringer Ingelheim International GmbHInventors: Marc-André Poupart, Pierre Louis Beaulieu, Jean Rancourt
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Patent number: 7304079Abstract: Disclosed are substituted indolealkanoic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.Type: GrantFiled: September 12, 2006Date of Patent: December 4, 2007Assignee: The Institute for Pharmaceutical Discovery, LLCInventors: Michael Jones, David Gunn, John Jones, Michael Van Zandt
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Patent number: 7285545Abstract: Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: April 29, 2005Date of Patent: October 23, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Daniel R. Goldberg, Ming-Hong Hao, Zhaoming Xiong, Ronald A. Aungst, Amy L. Davis
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Patent number: 7285551Abstract: The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.Type: GrantFiled: July 8, 2003Date of Patent: October 23, 2007Assignee: Japan Tobacco Inc.Inventors: Hiromasa Hashimoto, Kenji Mizutani, Atsuhito Yoshida
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Patent number: 7241801Abstract: A compound, represented by formula (I): wherein A, B, R1, R2, R3, R5, R6, R7, R9, and R10 are as defined herein, or an enantiomer, diastereoisomer or tautomer thereof, including a salt, ester or derivative thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: July 15, 2005Date of Patent: July 10, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Pierre Beaulieu, Christian Brochu, Stephen Kawai, Jean Rancourt, Timothy A. Stammers, Bounkham Thavonekham, Youla S. Tsantrizos
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Patent number: 7223765Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.Type: GrantFiled: March 15, 2006Date of Patent: May 29, 2007Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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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: 7205299Abstract: The invention relates to indole derivatives which are used as drugs for treating tumor diseases, in particular when there is drug resistance against other active compounds and where there is a metastasizing carcinoma.Type: GrantFiled: June 2, 2004Date of Patent: April 17, 2007Assignee: Zentaris GmbHInventors: Matthias Gerlach, Tilmann Schuster, Peter Ernig, Peter Schmidt, Silke Baasner, Eckhard Günther
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Patent number: 7183294Abstract: The invention relates to indole derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The indole derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.Type: GrantFiled: March 12, 2004Date of Patent: February 27, 2007Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, Justin Stephen Bryans, Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite, Simon John Mantell
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Patent number: 7166637Abstract: The invention relates to substituted 4- or/and 7-hydroxyindoles, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active compounds for treating diseases which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 4 activity in immunocompetent cells (e.g. macrophages and lymphocytes).Type: GrantFiled: November 13, 2003Date of Patent: January 23, 2007Assignee: Elbion AGInventors: Norbert Höfgen, Hildegard Kuss, Ute Egerland, Chris Rundfeldt, Helge Hartenhauer, Antje Gasparic
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Patent number: 7161009Abstract: The invention relates to new hydroxyindoles of the Formula, their use as inhibitors of phosphodiesterase 4 and processes for their preparation.Type: GrantFiled: February 21, 2002Date of Patent: January 9, 2007Assignee: Elbion AGInventors: Norbert Höfgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelényi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
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Patent number: 7135472Abstract: The present invention provides novel 3-heterocyclic benzylamides and related derivatives having the general Formula I wherein R1, R2, R3, R4, R5, R6, A and Het are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said novel 3-heterocyclic benzylamides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.Type: GrantFiled: November 21, 2003Date of Patent: November 14, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Yong-Jin Wu, Alexandre L'Heureux, Huan He
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Patent number: 7067536Abstract: The invention relates to substituted 4-, 6- or 7-hydroxyindoles with N-oxide groups, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.Type: GrantFiled: April 16, 2004Date of Patent: June 27, 2006Assignee: Elbion AGInventors: Nobert Hofgen, Hildegard Kuss, Karin Steinike, Ute Egerland, Chris Rundfeldt
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Patent number: 7045544Abstract: The invention relates to compounds of formula (I), to a method for the production thereof, and to the use of the same as pharmaceuticals for the treatment of diseases in humans and/or animalsType: GrantFiled: September 16, 2002Date of Patent: May 16, 2006Assignee: Bayer HealthCare AGInventors: Jens-Kerim Ergüden, Thomas Krahn, Christian Schröder, Johannes-Peter Stasch, Stefan Weigand, Hanno Wild, Michael Brands
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Patent number: 6992092Abstract: The present invention provides compounds of formula (I) the stereoisomers and prodrugs thereof, and the pharmaceutically acceptable salts of the compounds, stereoisomers, and prodrugs; wherein R1, R2, Ra, Rb, X, and Z are as defined herein; pharmaceutical compositions thereof; and uses thereof.Type: GrantFiled: April 15, 2004Date of Patent: January 31, 2006Assignee: Pfizer Inc.Inventors: Donald L. Bussolotti, Ronald B. Gammill
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Patent number: 6962942Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 16, 2002Date of Patent: November 8, 2005Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6958338Abstract: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyType: GrantFiled: February 4, 2003Date of Patent: October 25, 2005Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler
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Patent number: 6949572Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.Type: GrantFiled: August 13, 2003Date of Patent: September 27, 2005Assignee: Pfizer Inc.Inventors: Peter Bertinato, Brian S. Bronk, Alan E. Blize, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
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Patent number: 6900319Abstract: The invention relates to a compound of the formula I: or a salt thereof with a physiologically tolerated acid, or stereoisomers thereof, wherein R1, R2, A, B, C and D have the meanings described in the specification.Type: GrantFiled: March 19, 2002Date of Patent: May 31, 2005Assignee: Abbott GmbH & Co. KGInventors: Hans-Joachim Boehm, Hans Wolfgang Höffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
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Publication number: 20040266760Abstract: The invention relates to substituted 5-hydroxyindoles with N-oxide groups, processes for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.Type: ApplicationFiled: April 14, 2004Publication date: December 30, 2004Inventors: Nobert Hofgen, Hildegard Kuss, Karin Steinike, Ute Egerland, Chris Rundfeldt, Thomas Pfeifer
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Publication number: 20040242643Abstract: The invention relates to substituted 4-,6- or 7-hydroxyindoles with N-oxide groups, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.Type: ApplicationFiled: April 16, 2004Publication date: December 2, 2004Inventors: Nobert Hofgen, Hildegard Kuss, Karin Steinike, Ute Egerland, Chris Rundfeldt
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Publication number: 20040224971Abstract: The invention relates to substituted 7-azaindoles, process for their preparation, pharmaceutical preparations which comprise these compounds, and the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 4, as active ingredients for the treatment of disorders which can be influenced by inhibition of phosphodiesterase 4 activity in particular in immunocompetent cells (e.g. macrophages and lymphocytes) by the compounds of the invention.Type: ApplicationFiled: April 16, 2004Publication date: November 11, 2004Inventors: Nobert Hofgen, Hildegard Kuss, Matthias Olbrich, Ute Egerland, Chris Rundfeldt, Karin Steinike, Rudolf Schindler
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Publication number: 20040192736Abstract: A compound of formula (I): 1Type: ApplicationFiled: March 30, 2004Publication date: September 30, 2004Inventors: Gilbert Lavielle, Olivier Muller, Mark Millan, Alain Gobert
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Publication number: 20040176421Abstract: Compounds of formula (I) in which M, B1, B2, R1, R2, R6, R7, K1 and K2 have the meanings indicated in the description are novel active tryptase inhibitors.Type: ApplicationFiled: December 16, 2003Publication date: September 9, 2004Inventors: Thomas Martin, Wolf-Rudiger Ulrich
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Publication number: 20040157841Abstract: Mono-acylated o-phenylendiamines derivatives of formula I 1Type: ApplicationFiled: February 3, 2004Publication date: August 12, 2004Inventors: Georg Fertig, Frank Herting, Manfred Kubbies, Anja Limberg, Ulrike Reiff, Michael Weidner
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Patent number: 6759428Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.Type: GrantFiled: June 2, 2003Date of Patent: July 6, 2004Assignee: Roche Palo Alto LLCInventors: Joe Timothy Bamberg, Tobias Gabriel, Nancy Elisabeth Krauss, Taraneh Mirzadegan, Wylie Solang Palmer, David Bernard Smith
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Patent number: 6753342Abstract: 2-(1H-Indol-3-yl)-2-oxo-acetamides having antitumor activity, in particular against solid tumors, more precisely colon and lung tumors, of the following formula I: wherein Y is an oxygen of sulfur atom and X, R1, R2, R3, R4 and R5 are as defined in claim 1.Type: GrantFiled: September 18, 2002Date of Patent: June 22, 2004Assignee: Novuspharma S.p.A.Inventors: Ernesto Menta, Nicoletta Pescalli
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Publication number: 20040116504Abstract: This invention provides indole oxo-acetyl amino acetic acid derivatives which are useful as inhibitors of plasminogen activator inhibitor-1 (PAl-1) useful for treating fibrinolytic disorders, the compounds having the structure: 1Type: ApplicationFiled: December 9, 2003Publication date: June 17, 2004Applicant: WyethInventors: Hassan Mahmoud Elokdah, Geraldine Ruth McFarlane, David Zenan Li
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Patent number: 6727263Abstract: The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.Type: GrantFiled: August 16, 2002Date of Patent: April 27, 2004Assignee: H. Lundbeck A/SInventors: Ejner Knud Moltzen, Jens Kristian Perregaard, Ivan Mikkelsen, Garrick Paul Smith
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Publication number: 20030207892Abstract: The invention relates to novel N-substituted indole-3-glyoxylamides, to processes for their preparation and to their pharmaceutical use. The compounds have antiasthmatic, antiallergic and immuno-suppressant/immunomodulating actions.Type: ApplicationFiled: April 1, 2003Publication date: November 6, 2003Inventors: Guillaume Lebaut, Cecilia Menciu, Bernhard Kutscher, Peter Emig, Stefan Szelenyi, Kay Brune
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Patent number: 6638953Abstract: The invention relates to heterocyclic compounds having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety.Type: GrantFiled: January 22, 2001Date of Patent: October 28, 2003Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies, David Malcolm Duckworth, Ian Thomson Forbes, Graham Elgin Jones
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Publication number: 20030195360Abstract: The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents 1Type: ApplicationFiled: December 4, 2002Publication date: October 16, 2003Applicant: ASTA Medica AktiengesellschaftInventors: Bernd Nickel, Istvan Szelenyi, Jurgen Schmidt, Peter Emig, Dietmar Reichert, Eckhard Gunther, Kay Brune, Guillaume Le Baut
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Publication number: 20030148961Abstract: The present invention relates to compounds of the general formula 1 1Type: ApplicationFiled: August 9, 2002Publication date: August 7, 2003Inventors: Ulrich Heiser, Andre Niestroj, Torsten Hoffmann, Hans-Ulrich Demuth
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Publication number: 20030130281Abstract: The present invention relates to compounds of formula (I) 1Type: ApplicationFiled: October 14, 2002Publication date: July 10, 2003Inventors: Markus Boehringer, Daniel Hunziker, Holger Kuehne, Bernd M. Loeffler, Ramakanth Sarabu, Hans P. Wessel
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Publication number: 20030105140Abstract: The present invention is directed to substituted indole-2-carboxylic acid benzylidene-hydrazides and analogs thereof, represented by the general Formula I: 1Type: ApplicationFiled: November 19, 2002Publication date: June 5, 2003Applicant: Cytovia, Inc.Inventors: Sui Xiong Cai, John A. Drewe, Han-Zhong Zhang
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Patent number: 6545158Abstract: The invention relates to new hydroxyindoles of the Formula, their use as inhibitors of phosphodiesterase 4 and processes for their preparation.Type: GrantFiled: February 21, 2002Date of Patent: April 8, 2003Assignee: Arzneimittelwerk Dresden GmbHInventors: Norbert Höfgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelényi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
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Patent number: 6545025Abstract: The invention relates to nets hydroxyindoles of the Formula, their use as inhibitors of phosphodiesterase 4 and processes for their preparation.Type: GrantFiled: February 21, 2002Date of Patent: April 8, 2003Assignee: Arzneimittelwerk Dresden GmbHInventors: Norbert Höfgen, Ute Egerland, Hildegard Poppe, Degenhard Marx, Stefan Szelényi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer
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Patent number: 6541503Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by caType: GrantFiled: August 8, 2001Date of Patent: April 1, 2003Assignee: SmithKline Beecham CorporationInventors: Stephen Thomas Davis, Scott Howard Dickerson, Stephen Vernon Frye, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
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Publication number: 20030055087Abstract: The present invention relates to a compound of the formula [1′] 1Type: ApplicationFiled: May 10, 2002Publication date: March 20, 2003Applicant: Japan Tobacco Inc.Inventors: Hisashi Shinkai, Takao Ito, Hideki Yamada
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Publication number: 20030023093Abstract: The invention relates to the use of N-substituted indole-3-glyoxylamides of the general formula I as antitumor agents 1Type: ApplicationFiled: March 19, 2001Publication date: January 30, 2003Applicant: ASTA Medica AktiengesellschaftInventors: Bernd Nickel, Istvan Szelenyi, Jurgen Schmidt, Peter Emig, Dietmar Reichert, Eckhard Gunther, Kay Brune, Guillaume Le Baut
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Patent number: 6476035Abstract: The present invention relates to indole and 2,3-dihydroindole derivatives having formula (I) or any of its any of its enantiometers or any mixture thereof, or an acid addition salt thereof, wherein A, R1, R2, R3, W, X, Y and Z are as described in the description. The compounds are potent serotonin reuptake inhibitors and have 5-HT1A receptor antagonistic activity.Type: GrantFiled: January 25, 2000Date of Patent: November 5, 2002Inventors: Ejner Knud Moltzen, Jens Kristian Perregaard, Ivan Mikkelsen, Garrick Paul Smith
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Patent number: RE38624Abstract: The invention relates to new hydroxyindoles of the Formula, their use as inhibitors of phosphodiesterase 4 and processes for their preparation.Type: GrantFiled: September 19, 2002Date of Patent: October 12, 2004Assignee: Elbion AGInventors: Norbert Hofgen, Ute Egerland, Hildegard Kuss, Degenhard Marx, Stefan Szelenyi, Thomas Kronbach, Emmanuel Polymeropoulos, Sabine Heer