The Additional Polycyclo Ring System Is A Bicyclo Ring System Having Nitrogen As The Only Ring Hetero Atom [e.g., 5-(indolyl-3-methylene)- Hydantoin, Etc.] Patents (Class 548/312.1)
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Patent number: 7019021Abstract: Compounds of the formula (II) wherein R1, R2, R3, R4, and R5 are as set forth herein, pharmaceutical compositions containing them, and their use in treating urinary incontinence.Type: GrantFiled: April 19, 2004Date of Patent: March 28, 2006Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Franz Esser, Helmut Staehle, Sven Luettke, Ikunobu Muramatsu, Hisato Kitagawa, Shuji Uchida
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Patent number: 7002019Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.Type: GrantFiled: February 11, 2003Date of Patent: February 21, 2006Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Pawel K. Grzywacz, Rafal R. Sicinski
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Patent number: 6982264Abstract: The invention relates to substituted alcohol compounds of the formula (I): wherein X, R1, R2, R3, RN, R20 and RC are defined herein. The compounds are useful in the treatment or prevention of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers.Type: GrantFiled: June 27, 2002Date of Patent: January 3, 2006Assignee: Elan Pharmaceuticals, Inc.Inventors: Varghese John, Roy Hom, John Tucker
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Patent number: 6951881Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a disorder relating to or affected by the 5-HT6 receptor.Type: GrantFiled: May 9, 2003Date of Patent: October 4, 2005Assignee: WyethInventors: Derek Cecil Cole, Michael Gerard Kelly, Byron Abel Bravo, Yvette Latko Palmer
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Patent number: 6949564Abstract: The present invention provides NPY-5 receptor antagonists having a Formula (IA) Methods and pharmaceutical compositions useful for treating diseases, conditions and/or disorders modulated by the above NPY-5 receptor antagonists are also provided.Type: GrantFiled: December 1, 2003Date of Patent: September 27, 2005Assignee: Pfizer Inc.Inventor: Richard L. Elliott
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Patent number: 6943183Abstract: The present invention provides novel 5-substituted tetralones of Formulas I, II, III, and IV and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis.Type: GrantFiled: April 16, 2001Date of Patent: September 13, 2005Assignee: Pfizer IncInventors: William Alexander Denny, Richard H. Hutchings, Douglas S. Johnson, James Stanley Kaltenbronn, Ho Huat Lee, Daniele Marie Leonard, Jared Bruce John Milbank, Joseph Thomas Repine, Gordon William Rewcastle, Andrew David White
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Patent number: 6933295Abstract: The invention relates to the field of blood clotting, to novel compounds of formula (I), to a method for their production and to the use of these compounds as active ingredients in medicaments for preventing and/or treating diseases. The compounds are factor Xa inhibitors.Type: GrantFiled: July 3, 2002Date of Patent: August 23, 2005Assignee: Bayer AktiengesellschaftInventors: Alexander Straub, Thomas Lampe, Jens Pohlmann, Susanne Röhrig, Stephan Jordan, Elisabeth Perzborn, Karl-Heinz Schlemmer
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Patent number: 6909000Abstract: The present invention relates to peptidomimetic compounds which inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The compounds of this invention have a bridged bicyclic moiety at the P2 position. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: GrantFiled: July 11, 2002Date of Patent: June 21, 2005Assignee: Vertex Pharmaceuticals IncorporatedInventors: Luc J. Farmer, Janos Pitlik, Robert B. Perni, Lawrence F. Courtney, John van Drie
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Patent number: 6903216Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.Type: GrantFiled: June 12, 2002Date of Patent: June 7, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Thomas Böhme, Stefan Peukert, Heinz-Werner Kleemann
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Patent number: 6903104Abstract: The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formula, each R1 is independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R5; or when taken together with R2 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R2 is independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R5; or when taken together with R1 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5.Type: GrantFiled: December 5, 2002Date of Patent: June 7, 2005Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Patent number: 6903117Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a): wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substitued or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R6 and R7 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamiType: GrantFiled: November 20, 2002Date of Patent: June 7, 2005Assignee: Nikem Research S.R.L.Inventors: Carlo Farina, Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler
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Patent number: 6878735Abstract: A new class of imidazolines as 4-position acids or esters with very potent anti-inflammatory as well as antimicrobial activity is described. The synthesis of these imidazolines includes a multicomponent reaction applicable to a combinatorial synthetic approach. The combination of these two key characteristics provides an effective therapeutic drug in the treatment of septic shock as well as many other inflammatory (arthritis and asthma) and infectious disorders. The use of this novel class of non-steroidal agents as anti-inflammatory agents (for the treatment of asthma etc.), antibacterial agents and antiseptic agents is described. The compounds are also useful in the treatment of tumors (such as cancers). The imidazolines are potent inhibitors of the transcription factor NF-?B as well as potent activity against the Gram (+) bacterium B. subtillus and B. cereus with MIC values in the range of 50 ?m/mL.Type: GrantFiled: January 17, 2003Date of Patent: April 12, 2005Assignee: Board of Trustees of Michigan State UniversityInventors: Jetze J. Tepe, Satyamaheshwar Peddibhotla
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Patent number: 6852716Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.Type: GrantFiled: February 10, 2003Date of Patent: February 8, 2005Assignee: Pfizer IncInventors: Daniel Patrick Walker, David W. Piotrowski, Eric Jon Jacobsen, Brad A. Acker, Jason K. Myers, Vincent E. Groppi, Jr.
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Patent number: 6852726Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein X is —S(O)n— or —C(O)—, A is C1-6alkyl, aryl, heteroaryl, hydroxyalkyl, or —(CH2)p—NRaRb, and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.Type: GrantFiled: January 31, 2003Date of Patent: February 8, 2005Assignee: Syntex LLCInventors: Robert Greenhouse, Saul Jaime-Figueroa, Lubica Raptova
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Patent number: 6828331Abstract: What is disclosed are growth hormone secretagogues, and their uses, of the formula wherein R1 is C6H5CH2OCH2—, C6H5 (CH2)3— or indol-3-ylmethyl; Y is pyrrolidin-1-yl, 4-C1-C6 alkylpiperidin-1-yl or NR2R2; R2 are each independently a C1 to C6 alkyl; R3 is 2-napthyl or phenyl para-substituted by W; W is H, F, CF3, C1-C6 alkoxy or phenyl; and R4 is H or CH3, or a pharmaceutically acceptable salt or solvate thereof.Type: GrantFiled: July 25, 2001Date of Patent: December 7, 2004Assignee: Eli Lilly and CompanyInventors: Jeffrey Alan Dodge, Charles Willis Lugar, III
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Publication number: 20040235833Abstract: 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: ApplicationFiled: March 12, 2004Publication date: November 25, 2004Applicant: Pfizer IncInventors: 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: 6809098Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.Type: GrantFiled: August 21, 2002Date of Patent: October 26, 2004Assignee: AstraZeneca ABInventors: Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Publication number: 20040204448Abstract: The invention encompasses novel compounds, pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions of these compounds, and methods of using these compounds and compositions in mammals for treatment or prevention of diseases associated with PDE4.Type: ApplicationFiled: December 29, 2003Publication date: October 14, 2004Applicant: Celgene CorporationInventors: George W. Muller, Hon-Wah Man, Weihong Zhang
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Publication number: 20040204589Abstract: The invention provides a method for producing a compound represented by the following formula (II), comprising executing alkali hydrolysis of a compound represented by the following formula (I) with an alkali metal hydroxide in the presence of a barium compound to from the compound represented by formula (II), precipitating the barium compound in the form of a barium halide, and eliminating the barium halide: 1Type: ApplicationFiled: March 11, 2004Publication date: October 14, 2004Inventor: Hideto Mori
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Publication number: 20040198793Abstract: Process for the preparation of a compound of the general formula (I) and pharmaceutically acceptable salts and solvates thereof, (I) characterised by reacting an N-(amino-tioxo-methyl)-1H-indole-2-carboxamide of the general formula (II), with an &agr;-halogen-ketone of the general formula (III), wherein X stands for halogen.Type: ApplicationFiled: October 6, 2003Publication date: October 7, 2004Inventors: Sandor Bokotey, Gezane Galambos, Felix Hadju, Istvan Hermecz, Agnes Horvath, Maria Uzsoki, Gyulane Kiss, Lajos Nagy, Benjamin Podanyi, Attila Simon, Judit Sipos, Agota Esek Smelkone, Anna Szabo, Arpadne Vasvari
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Patent number: 6794406Abstract: The invention relates to new indole derivatives, processes for their preparation, and their use in medicaments.Type: GrantFiled: December 21, 2001Date of Patent: September 21, 2004Assignee: Bayer AktiengesellschaftInventors: Helmut Haning, Michael Woltering, Gunter Schmidt, Hilmar Bischoff, Axel Kretschmer, Verena Vöhringer, Christiane Faeste
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Patent number: 6784293Abstract: The present invention provides a process for the efficient assembly of Boc-protected 3-aminohydantoins/thiohydantoins and 3-aminodihydrouracils/dihydrothiouracils via a one-pot solution phase or solid phase synthesis from readily available starting materials.Type: GrantFiled: June 25, 2002Date of Patent: August 31, 2004Assignee: The Procter & Gamble CompanyInventors: Shengde Wu, John Michael Janusz
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Publication number: 20040167174Abstract: Imido and amido substituted acyihydroxamidic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin -2-yl)-3-(3-ethoxy-4-methoxyphenyl)propandylamino)propanoate.Type: ApplicationFiled: February 25, 2004Publication date: August 26, 2004Applicant: CelgeneInventors: Hon-Wah Man, George W. Muller, Shaei Y. Huang
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Patent number: 6770667Abstract: The present invention is a compound and pharmaceutical composition comprising a compound of formula (I): wherein R1 is a 4-(lower) alkyl-imidazol-1-yl or a 4,5-di(lower) alkyl-imidazol-1-yl group, R2 is a hydrogen atom or a lower alkyl group, and R3 is a fluorenyl group. The compound of formula (I) includes pharmaceutically acceptable salts: The compound of formula (I) and salts thereof have 5-HT antagonism activity.Type: GrantFiled: March 21, 2002Date of Patent: August 3, 2004Assignee: Fujisawa Pharmaceutical Co., Ltd.Inventors: Kiyotaka Ito, Glen W. Spears, Fumie Takahashi, Akira Yamada, Masaki Tomishima, Hiroshi Miyake
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Publication number: 20040147759Abstract: 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: ApplicationFiled: November 13, 2003Publication date: July 29, 2004Inventors: Norbert Hofgen, Hildegard Kuss, Ute Egerland, Chris Rundfeldt, Helge Hartenhauer, Antje Gasparic
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Publication number: 20040142987Abstract: The present invention relates to compounds of formula I which are antagonists of gonadotropin releasing hormone (GnRH) activity. The invention also relates to pharmaceutical formulations, the use of a compound of the present invention in the manufacture of a medicament, a method of therapeutic treatment using such a compound and processes for producing the compounds.Type: ApplicationFiled: March 1, 2004Publication date: July 22, 2004Inventors: James Michael Wardleworth, Alexander Graham Dossetter, Christopher Thomas Halsall
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Publication number: 20040133010Abstract: A photo-induced phase transition organic material is composed of a diheteroarylethene-based compound within which the photo-chromic reaction occurs in the crystalline state. The diheteroarylethene-based compound of the present invention reversibly changes in color with light irradiation and also changes in phase from the open-ring form in the crystalline state to the closed-ring form in the crystalline state, or from the closed-ring form in the crystalline state to the open-ring form in the crystalline state via the liquid state, and can be applicable to optical recording media, display panels, sensors, optical switch devices and the like, by taking advantages of its variations in color with light irradiation and also its changes in physical property, such as the refractive index and the permeability, with its changes in phase.Type: ApplicationFiled: December 9, 2003Publication date: July 8, 2004Inventor: Masahiro Irie
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Publication number: 20040122046Abstract: The present invention provides NPY-5 receptor antagonists having a Formula (IA) 1Type: ApplicationFiled: December 1, 2003Publication date: June 24, 2004Applicant: Pfizer IncInventor: Richard L. Elliott
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Publication number: 20040110770Abstract: The present invention relates to a compound of formula (I): 1Type: ApplicationFiled: August 20, 2003Publication date: June 10, 2004Applicant: AVENTIS PHARMA SAInventors: Jean-Francois Riou, Michel Maratrat, Lucile Grondard, Fabienne Thompson, Odile Petitgenet, Patrick Mailliet, Jacques Lavayre
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Publication number: 20040110814Abstract: The purpose of the invention concerns a family of pseudodipeptides which are coupling products between tryptamine, an indole-primary amine, and a selection of alpha-amino acids, the said pseudodipeptides having the following general formula (I) 1Type: ApplicationFiled: October 2, 2003Publication date: June 10, 2004Applicant: EXSYLMOL S.A.M.Inventor: Marie-Christine Seguin
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Publication number: 20040106657Abstract: The present invention provides compounds of formula I 1Type: ApplicationFiled: November 21, 2003Publication date: June 3, 2004Inventors: Alfred Binggeli, Uwe Grether, Hans Hilpert, Georges Hirth, Bernd Kuhn, Hans-Peter Maerki, Markus Meyer, Peter Mohr
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Patent number: 6743817Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.Type: GrantFiled: September 6, 2001Date of Patent: June 1, 2004Assignee: Neurogen CorporationInventors: George Maynard, LingHong Xie, Stanislaw Rachwal
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Publication number: 20040102480Abstract: This invention provides compounds of Formula I having the structure 1Type: ApplicationFiled: November 21, 2002Publication date: May 27, 2004Applicant: WyethInventors: Michael S. Malamas, Jay E. Wrobel, Arlene J. Dietrich, Zenan Li, Iwan Gunawan
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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: 20040067949Abstract: The present invention relates to novel indole derivatives, to their preparation and to their use, as inhibitors of the enzyme poly(ADP-ribose)polymerase or PARP (EC 2.4.2.30), for producing drugs.Type: ApplicationFiled: October 6, 2003Publication date: April 8, 2004Inventors: Roland Grandel, Wilfried Lubisch, Michael Kock, Thomas Hoger, Reinhold Muller, Sabine Schult, Uta Holzenkamp
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Publication number: 20040067998Abstract: The present invention relates to novel indole derivatives, their method of preparation and their pharmacological activity as antimycotic and/or antiparasitic compounds.Type: ApplicationFiled: July 25, 2003Publication date: April 8, 2004Inventors: Marc Le Borgne, Young Min Na, Fabrice Pagniez, Guillaume Le Baut, Patrice Le Pape, Hiam Abdala
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Publication number: 20040063642Abstract: The invention is directed to novel benzimidazolone peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted benzimidazolone peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.Type: ApplicationFiled: March 17, 2003Publication date: April 1, 2004Inventors: Han-Cheng Zhang, Bruce E. Maryanoff, David F. McComsey, Kimberly B. White
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Publication number: 20040053981Abstract: Abstract Asymmetric derivatives of furamidines with one of the phenyl rings of furamidine replaced with a benzimidazole have been found by quantitative footprinting analyses to bind GC containing sites on DNA more strongly than to pure AT sequences. These compounds have been shown to bind in the minor groove at specific GC containing sequences of DNA in a highly cooperative manner as a stacked dimer. Compounds of the present invention find use in selectively binding mixed sequence DNA, and may also be used in methods of regulating gene expression, methods of treating opportunistic infections and cancer, as well as in methods of detecting certain sequences of DNA.Type: ApplicationFiled: September 2, 2003Publication date: March 18, 2004Inventors: W. David Wilson, David W. Boykin, Richard R. Tidwell
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Publication number: 20040044222Abstract: Indolinones of general formula I 1Type: ApplicationFiled: August 22, 2003Publication date: March 4, 2004Applicant: Boehringer Ingelheim Pharma KGInventors: Rainer Walter, Armin Heckel, Gerald Roth, Joerg Kley, Gisela Schnapp, Martin Lenter, Jacobus Van Meel, Walter Spevak, Ulrike Weyer-Czernilofsky
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Publication number: 20040044053Abstract: Indolinones of general formula I 1Type: ApplicationFiled: August 22, 2003Publication date: March 4, 2004Applicant: Boehringer Ingelheim Pharma KGInventors: Rainer Walter, Armin Heckel, Gerald Roth, Joerg Kley, Gisela Schnapp, Martin Lenter, Jacobus Van Meel, Walter Spevak, Ulrike Weyer-Czernilofsky
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Patent number: 6699862Abstract: Novel indolyl-2-phenyl bisamidines are described which are DNA methyltransferase inhibiting agents, and pharmaceutical compositions containing them are used as antiproliferative agents for treating a disease, especially a neoplastic disease, characterized by abnormally rapid proliferation of tissue involved in said disease; said indolyl-2-phenyl bisamidines comprising a and a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen or (C1-C3)alkyl; R3, R4, R5, R8, R9, and R10 are hydrogen or (C1-C3)alkyl, or R3 and R4 may be taken together, or R8 and R9 may be taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; R14 is —H; —NHC(═O)(CH2)mR20; —(CH2)mR20; —CH(CH3)R20; —(CH2)m(C6H3)—R17; —(CH2)m(C6H3)—R20; —(CH2)m(heterocyclyl)—R17; —(CH2)m(heterocyclyl)—R20; —CH2CH═CHR20; —(CH2)mC(═O)NH—CHR20R21; or —(CH2)mC(═O)NH—CH2&mType: GrantFiled: March 24, 2000Date of Patent: March 2, 2004Assignee: Pfizer Inc.Inventors: Steven W. Goldstein, Banauara L. Mylari, Jose R. Perez, Edward A. Glazer
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Patent number: 6699883Abstract: The present invention relates to 3-pyrroloimidazole derivatives of the general formula (I) wherein the imidazole radical is an optionally substituted imidazole ring, X, Y, A and B are, each independently of the others, carbon or nitrogen atoms, the radicals Z denote, each independently of the others, a hydrogen atom, a halogen atom, a pseudohalogen, an optionally substituted alkyl, alkenyl, alkynyl, aralkyl, aralkenyl, aralkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, cycloaralkyl, cycloaralkenyl, cycloaralkynyl, aryl or alkoxy radical or an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and/or at least two of the radicals Z may be part of an optionally substituted ring, to which one or two further, optionally substituted rings may be fused, and to pharmaceutical compositions comprising at least one of the above-mentioned compounds, optionally in combination with carriers and/or adjuvants and/or excipients customary per se.Type: GrantFiled: April 4, 2002Date of Patent: March 2, 2004Assignee: Morphochem AGInventors: Alexander Doemling, Barbara Beck
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Patent number: 6699899Abstract: Imido and amido substituted acylhydroxamic acids which reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is (3-(1,3-dioxoisoindolin-2-yl)-3-(3-ethoxy-4-methoxyphenyl)propanoylamino)propanoate.Type: GrantFiled: December 21, 1999Date of Patent: March 2, 2004Assignee: Celgene CorporationInventors: Hon-Wah Man, George W Muller, Shaei Y Huang
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Publication number: 20040029858Abstract: 2-(III-Indol-3-yl)-2-oxo-acetamide derivatives of formula (I) having antitumor activity in particular against solid tumors, specifically colon and lung tumors.Type: ApplicationFiled: July 10, 2003Publication date: February 12, 2004Inventors: Ernesto Menta, Nicoletta Pescalli
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Publication number: 20040019207Abstract: The present invention discloses compounds of formula (1) any of its enantiomers or any mixture thereof, or a pharmaceutically acceptable salt thereof; wherein is a single or a double bond; R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or aralkyl; and R1 is (a), wherein R2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, amino; or aryl which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, aminoacyl, nitro, aryl and a monocyclic 5 to 6-membered heteroaryl group; a monocyclic 5 to 6-membered heteroaryl group which may be substituted one or more times with substituents selected from the group consisting of alkyl, cycloalkyl, cycloalkylalkyl alkenyl, alkynyl, alkoxy, cycloalkoxy, thioalkoxy, thiocycloalkoxy, methylenedioxy, aryloxy, halogen, CF3, OCF3, CN, amino, nitrType: ApplicationFiled: July 17, 2003Publication date: January 29, 2004Applicant: NeuroSearch A/SInventors: Dan Peters, Gunnar M. Olsen, Simon Feldback Nielsen, Elsebet Ostergaard Nielsen
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Publication number: 20040019092Abstract: The present invention provides compounds of formula (I), wherein X, Y, R1, R2, R3, and R4 are as defined in the description, and the preparation therof. The compounds of the formula bind to somatostatin receptiors and are useful as pharmaceuticals.Type: ApplicationFiled: November 14, 2002Publication date: January 29, 2004Inventors: Daniel Berney, Robin Breckenridge, Peter Neumann, Gideon Shapiro, Max Peter Seiler, J. Troxler Thomas
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Publication number: 20040014971Abstract: Polyarylcarboxamide compounds of formula (I) 1Type: ApplicationFiled: February 28, 2003Publication date: January 22, 2004Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Publication number: 20040006088Abstract: 1Type: ApplicationFiled: June 17, 2003Publication date: January 8, 2004Applicant: Pfizer Inc.Inventors: Dennis J. Hoover, Bernard Hulin, William H. Martin, Judith L. Treadway
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Publication number: 20040002531Abstract: The present invention is directed to imidazolyl derivatives of formula (II), wherein the variables are defined in the specification, which are useful as prenyl transeferase inhibitors.Type: ApplicationFiled: January 21, 2003Publication date: January 1, 2004Applicant: Societe de Conseils de Recherches et D'Application Scientefiques, S.A.S., a France corporationInventors: Zheng Xin Dong, Yeelana Shen
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Publication number: 20040002527Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a disorder relating to or affected by the 5-HT6 receptor.Type: ApplicationFiled: May 9, 2003Publication date: January 1, 2004Applicant: WyethInventors: Derek Cecil Cole, Michael Gerard Kelly, David Scott Nunn, Lynne Padilla Greenblatt