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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Publication number: 20100125064Abstract: The invention relates to 3-heterocyclyl indolyl compounds capable of inhibiting the interaction between p53, or variants thereof, and MDM2 and/or MDM4, or variants thereof, respectively, said compounds having the formula I, wherein R1, R2, R3, R4, RA, Y and Y are as defined in the specification. Due to their activity, the compounds are useful in the treatment of various disorders and diseases mediated by the activity of MDM2 and/or MDM4, or variants thereof, such as inflammatory or proliferative diseases or in the protection of cells.Type: ApplicationFiled: March 27, 2008Publication date: May 20, 2010Applicant: NOVARTIS AGInventors: Andreas Boettcher, Nicole Buschmann, Pascal Furet, Jean-Marc Groell, Jorg Kallen, Joanna Hergovich Lisztwan, Keiichi Masuya, Lorenz Mayr, Andrea Vaupel
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Publication number: 20100120838Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: ApplicationFiled: January 20, 2010Publication date: May 13, 2010Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong Heon Kim, De-Yi Yang, Razia Rizvi
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Publication number: 20100105726Abstract: The present invention relates to a pharmaceutical composition comprising compound for induction of apoptosis, a method for inducing cancer cell apoptosis, a method to suppress lymphocyte activation, a method to improve intracellular trafficking of misfolded mutants and a screening method to identify additional compounds useful for inducing apoptosis, and more specifically, it relates to pharmaceutical compositions comprising imidazole derivatives as active gradients for induction of apoptosis to treat various diseases including cancers and immune-related diseases, the method of inducing apoptosis by treating cancer cells with the said pharmaceutical composition, the method of inactivating human lymphocytes by treating lymphocytes with the said pharmaceutical composition, the method of improving intracellular trafficking of misfolded mutants by treating cells containing the mutants with the said pharmaceutical composition, and the screening method for identifying additional compound useful for inducing apoptosType: ApplicationFiled: February 26, 2007Publication date: April 29, 2010Applicant: Industry-Academic Cooperation Foundation, Yonsei UniversityInventors: In-Jae Shin, Myung-ryul Lee, Darren Williams
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Publication number: 20100093703Abstract: The present invention relates to substituted arylsulphonylglycines of general formula wherein R, R4, X, Y, Z and m are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof, which have valuable pharmacological properties, particularly the suppression of the interaction of glycogen phosphorylase a with the GL subunit of glycogen-associated protein phosphatase 1 (PP1), and their use as pharmaceutical compositions.Type: ApplicationFiled: February 15, 2008Publication date: April 15, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Holger Wagner, Elke Langkopf, Ruediger Streicher, Matthias Eckhardt, Annette Schuler-Metz, Alexander Pautsch, Corinna Schoelch
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Publication number: 20100087464Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful as protein kinase inhibitors, and methods for using such compounds to treat, ameliorate or prevent a condition associated with abnormal or deregulated kinase activity. In some embodiments, the invention provides methods for using such compounds to treat, ameliorate or prevent diseases or disorders that involve abnormal activation of TrkA, TrkB, TrkC, Abl, Bcr-Abl, cSrc, TPR-Met, Tie2, MET, FGFR3, Aurora, Axl, Bmx, BTK, c-kit, CHK2, Flt3, MST2, p70S6K, PDGFR, PKB, PKC?, Raf, ROCK-II, Rsk1, and SGK kinases, or a combination thereof.Type: ApplicationFiled: August 27, 2007Publication date: April 8, 2010Applicant: IRM LLCInventors: Yuan Mi, Pamela A. Albaugh
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Patent number: 7683088Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: GrantFiled: January 16, 2007Date of Patent: March 23, 2010Assignee: Schering CorporationInventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta M. Micula, Seong-Heon Kim, De-Yi Yang, Razia Rizvi
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Publication number: 20100022514Abstract: The invention relates to the use of compounds in the treatment of deacetylase-associated diseases and for the manufacture of pharmaceutical preparations for the treatment of said diseases.Type: ApplicationFiled: December 17, 2007Publication date: January 28, 2010Inventors: Young Shin Cho, Lei Jiang, Michael Shultz
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Publication number: 20090326011Abstract: Disclosed herein are compounds of formula (I) where G and Q are heteroaromatic groups. These compounds are useful for treating psychosis or a psychotic condition, substance abuse, premature ejaculation or cognition impairment.Type: ApplicationFiled: June 13, 2006Publication date: December 31, 2009Inventors: Luca Arista, Francesca Cardullo, Anna Checchia, Dieter Hamprecht, Fabrizio Micheli, Giovanna Tedesco, Silvia Terreni
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Publication number: 20090298900Abstract: Compounds represented by Formula I and II, or pharmaceutically acceptable salts thereof: inhibit bacterial 2-epimerase and are useful anti-infective agents.Type: ApplicationFiled: May 11, 2009Publication date: December 3, 2009Inventors: David J. Bearss, Hariprasad Vankayalapati, Yong Xu, Charles Erec Stabbins, Vincent A. Fischetti
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Publication number: 20090299058Abstract: Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.Type: ApplicationFiled: February 10, 2009Publication date: December 3, 2009Applicant: President and Fellows of Harvard CollegeInventors: Jose A. Halperin, Amarnath Natarajan, Huseyin Aktas, Yun-Hua Fan, Han Chen
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Patent number: 7612099Abstract: The invention is concerned with vinylogous acids derivatives of formula (I) wherein A and R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit chymase and can be used as medicaments.Type: GrantFiled: November 28, 2006Date of Patent: November 3, 2009Assignee: Hoffmann-La Roche Inc.Inventors: David Banner, Hans Hilpert, Bernd Kuhn, Harald Mauser
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Publication number: 20090181945Abstract: The present invention relates to a novel two cyclic cinnamide compound and a pharmaceutical agent comprising the compound as an active ingredient. The two cyclic cinnamide compound represented by the general formula (I): wherein represents a single bond or a double bond; Ar1 represents a phenyl group or pyridinyl group that may be substituted with 1 to 3 substituents; R1 and R2 each represent a C1-6 alkyl group, a hydroxyl group, or the like; Z1 represents a methylene group or vinylene group, which may be substituted with 1 or 2 substituents selected from Substituent Group A1, an oxygen atom, or an imino group that may be substituted with a substituent selected from Substituent Group A1; and p, q, and r each represent an integer of 0 to 2, which has an effect of reducing A?40 and A?42 production, and thus is particularly useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by A? such as Alzheimer's disease or Down's syndrome.Type: ApplicationFiled: March 13, 2009Publication date: July 16, 2009Inventors: Teiji Kimura, Koki Kawano, Eriko Doi, Noritaka Kitazawa, Mamoru Takaishi, Koichi Ito, Toshihiko Kaneko, Takeo Sasaki, Takehiko Miyagawa, Hiroaki Hagiwara, Yu Yoshida
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Publication number: 20090170875Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: July 2, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Umar Faruk Mansoor, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li
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Publication number: 20090163494Abstract: This invention relates to selenophene compounds of formula (I) shown below: Each variable in formula (I) is defined in the specification. These compounds can be used to treat cancer.Type: ApplicationFiled: December 19, 2007Publication date: June 25, 2009Inventors: Pao-Chiung Hong, Li-Jung Chen, Yann-Yu Lu, Tzu-Yun Lai, Huei-Ru Yang, Yi-Feng Kao, Kuei-Tai Lai, Young-Sun Lin
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Publication number: 20090156586Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.Type: ApplicationFiled: February 3, 2009Publication date: June 18, 2009Inventors: Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Bandarpalle B. Shankar, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Lei Chen, De-Yi Yang, Robert Feltz, Seong Heon Kim
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Patent number: 7547703Abstract: The present invention relates to indolinone derivatives, substituted in the 6-position, of the formula in which R1 to R6 and X are as defined in claim 1, to their tautomers, enantiomers, diastereomers, to their mixtures and to their salts, in particular their physiologically acceptable salts, which have useful pharmacological properties, in particular in inhibiting action on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, to medicaments comprising these compounds, to their use and to processes for their preparation.Type: GrantFiled: September 7, 2006Date of Patent: June 16, 2009Assignee: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: Gerald Juergen Roth, Armin Heckel, Thorsten Lehmann-Lintz, Joerg Kley, Frank Hilberg, Jacobus C. A. Van Meel, Ulrike Tontsch-Grunt
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Publication number: 20090137586Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate, ester or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: May 28, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankar, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Razia Rizvi, Aneta M. Micula, Robert Feltz
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Publication number: 20090131494Abstract: Certain 1H-indole-2-carboxylates and -2-carboxamides are HIV reverse transcriptase inhibitors. These indole compounds and their pharmaceutically acceptable salts are useful in the inhibition of HIV reverse transcriptase, the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: August 7, 2006Publication date: May 21, 2009Inventors: Theresa M. Williams, Xu-Fang Zhang
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Publication number: 20090111803Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF—or combinations thereof.Type: ApplicationFiled: December 18, 2008Publication date: April 30, 2009Inventors: Wensheng Yu, Ling Tong, Lei Chen, Joseph A. Kozlowski, Brian J. Lavey, Neng-Yang Shih, Vincent S. Madison, Guowei Zhou, Peter Orth, Zhuyan Guo, Michael K.C. Wong, De-Yi Yang, Seong Heon Kim, Bandarpalle B. Shankat
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Patent number: 7517902Abstract: Disclosed are novel substituted indazole compounds, pharmaceutical compositions comprising such compounds, and methods of treatment comprising such compounds.Type: GrantFiled: December 4, 2006Date of Patent: April 14, 2009Assignee: Aventis Pharma S.A.Inventors: Frank Halley, Michel Tabart, Hervé Bouchard, Catherine Souaille, Alain Le Brun, Fabrice Viviani, Laurence Gauzy-Lazo, Pascal Desmazeau, Odile Angouillant-Boniface, Bruno Filoche-Romme
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Publication number: 20090062541Abstract: The present invention relates to a process for preparing optionally substituted aromatic or heteroaromatic nitriles starting from haloaromatics. These are reacted in a copper-catalysed reaction with potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III) in the presence of heteroaromatic amines.Type: ApplicationFiled: August 27, 2007Publication date: March 5, 2009Inventors: Nikolaus Muller, Wolfgang Magerlein, Matthias Beller, Thomas Schareina, Alexander Zapf
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Publication number: 20090048228Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.Type: ApplicationFiled: December 9, 2005Publication date: February 19, 2009Inventors: Barbara Attenni, Federica Ferrigno, Philip Jones, Raffaele Ingenito, Olaf Kinzel, Laura Llauger Bufi, Jesus Maria Ontoria, Giovanna Pescatore, Michael Rowley, Rita Scarpelli, Carsten Schultz
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Patent number: 7491743Abstract: The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.Type: GrantFiled: August 30, 2004Date of Patent: February 17, 2009Assignees: President and Fellows of Harvard College, The Brigham and Women's Hospital, Inc.Inventors: Gregory D. Cuny, Junying Yuan, Prakash Jagtap, Alexei Degterev
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Publication number: 20090012070Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)=C(R7)N(R8)-, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)=C(R12)C(R13)=C(R14) 112, -, where R, R, R6, R7, R8, R11, R R13, R14, and X are described. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula (I), and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.Type: ApplicationFiled: August 22, 2008Publication date: January 8, 2009Applicant: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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Publication number: 20080275041Abstract: Compounds of formula Ia or Ib wherein P; R1; R2; m; and n are as defined in the application, salts thereof, processed for their preparation, new intermediates used therein, pharmaceutical formulations containing said compounds and the use of said compounds in therapy.Type: ApplicationFiled: September 21, 2004Publication date: November 6, 2008Applicant: AstraZeneca ABInventors: Stefan Berg, Sven Hellberg
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Patent number: 7446118Abstract: The present invention provides compounds of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein p, Ar, R1, R2, R3, Ra, Rb, Rc, Rd and Re are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: November 29, 2006Date of Patent: November 4, 2008Assignee: Roche Palo Alto LLCInventors: Pravin Iyer, Matthew C. Lucas, Ryan Craig Schoenfeld, Marzia Villa, Robert James Weikert
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Publication number: 20080261917Abstract: A compound of formula or a prodrug and/or a pharmaceutically acceptable salt thereof, wherein X is O, N or S; R1 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroaralkyl; R2 is hydrogen, halo, hydroxy, substituted or unsubstituted alkyl, substituted or unsubstituted hydroxyalkyl substituted or unsubstituted alkylamine, alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; R3 is hydrogen, halo, hydroxy, substituted or unsubstituted alloy substituted or unsubstituted hydroxyalkyl, substituted or unsubstituted alkylamine alkoxy, substituted or unsubstituted aryl or heteroaryl, and substituted or unsubstituted aralkyl or heteroalkyl; and R4-R7, is used to represent groups R4, R5, R6 and R7 which are H, OH, alkyl, alkoxy, alkylamine, hydroxyalkyl, hType: ApplicationFiled: August 26, 2005Publication date: October 23, 2008Inventors: Hendrika Maria Gerarda Willems, Per Kallblad, Ian Robert Hardcastle, Robert John Griffin, Bernard Thomas Golding, John Lunec, Martin E.M. Noble, David R. Newell, Alan H. Calvert
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Patent number: 7439370Abstract: The invention relates to new substituted imidazoles of general formula wherein R1 to R3 and X are defined as claims, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, and processes for preparing them and their use as intermediates for preparing pharmaceutical compositions or pesticides.Type: GrantFiled: May 9, 2005Date of Patent: October 21, 2008Assignee: Boehringer Ingelheim International GmbHInventor: Matthias Eckhardt
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Publication number: 20080255218Abstract: This invention relates generally to N-benzylamino cyclic thioureas, pharmaceutical compositions containing them, and their use as antagonists of melanin-concentrating hormone receptor (MCH receptor).Type: ApplicationFiled: March 23, 2005Publication date: October 16, 2008Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Richard A. Houghten, Colette Dooley, Adel Nefzi, Zhiwei Wang, Oliver Civelli, Hiroshi Nagasaki
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Publication number: 20080249110Abstract: The present invention relates to substituted indoles useful as pharmaceutical compounds for treating respiratory disorders.Type: ApplicationFiled: May 25, 2004Publication date: October 9, 2008Inventors: Roger Bonnert, Rukhsana Mohammed
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Publication number: 20080221152Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardiovascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: ApplicationFiled: May 20, 2008Publication date: September 11, 2008Applicant: ALLERGAN, INC.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
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Patent number: 7417057Abstract: It has now been found that certain novel heterocyclic derivatives have provided unexpected insecticidal activity. These compounds are represented by formula (I): R Preferred are those compounds of formula (I) where R2 and R3 taken together is ?NCH(R6)CH(R7)N(R8)—, ?NC(R6)?C(R7)N(R8)—, or ?CHN?C(R7)N(R8)—, and tautomers thereof, and where R4 and R5 taken together is —C(R11)?C(R12)C(R13)?C(R14) 1 12, —, where R,R,R 6, R 7, R8, R I1, R R 13, R 14, and X are described.Type: GrantFiled: April 28, 2003Date of Patent: August 26, 2008Assignee: Bayer Cropscience AGInventors: John A. Dixson, Zeinab M. Elshenawy, Harvey R. Wendt, Saroj Sehgel, Robert H. Henrie, II, David M. Roush, Ping Ding, John W. Lyga, Stephen F. Donovan
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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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Patent number: 7399868Abstract: Compounds of Formula 1 where the variables have the meaning defined in the specification are agonists of alpha2 adrenergic receptors. Several compounds of the disclosure are specific or selective to alpha2B and/or alpha2C adrenergic receptors in preference over alpha2A adrenergic receptors. Additionally some of the claimed compounds have no or only minimal cardivascular and/or sedatory activity. The compounds of Formula 1 are useful as medicaments in mammals, including humans, for treatment of diseases and or alleviations of conditions which are responsive to treatment by agonists of alpha2 adrenergic receptors. Compounds of Formula 1 which have no significant cardiovascular and/or sedatory activity are useful for treating pain and other conditions with minimal side effects.Type: GrantFiled: September 20, 2005Date of Patent: July 15, 2008Assignee: Allergan, Inc.Inventors: Todd M. Heidelbaugh, Ken Chow, Phong X. Nguyen, Daniel W. Gil, John E. Donello, Michael E. Garst, Larry A. Wheeler
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Patent number: 7375219Abstract: The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia.Type: GrantFiled: April 13, 2006Date of Patent: May 20, 2008Assignee: NeurAxon, Inc.Inventors: Shawn Maddaford, Jailall Ramnauth, Suman Rakhit, Joanne Patman, Paul Renton, Subhash C. Annedi
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Publication number: 20080113980Abstract: The present invention relates to compounds of formula I wherein R1 is selected from the group consisting of hydrogen and lower alkyl; each R2 is independently selected from the group consisting of hydrogen and lower alkyl; each R3 is independently selected from the group consisting of hydrogen, lower alkyl, lower alkoxy, phenyloxy, benzyloxy, halogen and lower alkyl substituted by halogen; X is selected from the group consisting of —CH2—, —CH— and —O—; Y is selected from the group consisting of —CH2—, —CH— and a bond with the proviso that, when X is —O—, Y may not be a bond; Z is selected from the group consisting of —CH2— and —CH—; m is 0, 1 or 2; and n is 0, 1 or 2; and to pharmaceutically-acceptable acid addition salts of such compounds.Type: ApplicationFiled: October 31, 2007Publication date: May 15, 2008Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 7348425Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: GrantFiled: February 3, 2006Date of Patent: March 25, 2008Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Publication number: 20070238771Abstract: Benzoimidazole and indole compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: March 30, 2007Publication date: October 11, 2007Inventors: James P. Edwards, Brad M. Savall, Chandravadan R. Shah
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Patent number: 7241900Abstract: 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: November 23, 2005Date of Patent: July 10, 2007Assignee: Wisconsin Alumni Research FoundationInventors: Hector F. DeLuca, Pawel K. Grzywacz, Rafal R. Sicinski
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Patent number: 7235664Abstract: 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: February 8, 2005Date of Patent: June 26, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Joachim Brendel, Thomas Boehme, Stefan Peukert, Heinz-Werner Kleemann
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Patent number: 7179910Abstract: The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: September 8, 2003Date of Patent: February 20, 2007Assignee: Agouron Pharmaceuticals, Inc.Inventors: Huiping Guan, Congxin Liang, Li Sun, Peng Cho Tang, Chung Chen Wei, Tomas Vojkovsky, Qingwu (Alan) Jin, Paul M. Herrinton, Michael A. Mauragis
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Patent number: 7176321Abstract: 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: wherein L represents a thiocyano group, an aryloxy group, an alkoxy group, an alkylthio group, an arylthio group, a heterocyclic thio group, an imide group, an imidazolyl group, a pyrazolyl group or a triazolyl group; R1 represents an unsubstituted or substituted alkyl group, or an unsubstituted or substituted aryl group; R2 represents a substituent; and n represents an integer of 0 to 5; in a case where n is 2 or larger, R2 may be the same or different.Type: GrantFiled: March 11, 2004Date of Patent: February 13, 2007Assignee: Fuji Photo Film Co., Ltd.Inventor: Hideto Mori
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Patent number: 7166607Abstract: The present invention relates to substituted indoles of formula (I) useful as pharmaceutical compounds for treating respiratory disordersType: GrantFiled: May 27, 2003Date of Patent: January 23, 2007Assignee: AstraZeneca ABInventors: Roger Bonnert, Stephen Brough, Tony Cook, Mark Dickinson, Rukhsana Rasul, Hitesh Sanganee, Simon Teague
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Patent number: 7153848Abstract: Indole compounds of Formula I are described. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV. Different forms and compositions comprising the compounds are also described as well as methods of preparing the compounds.Type: GrantFiled: July 14, 2005Date of Patent: December 26, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Thomas W. Hudyma, Xiaofan Zheng, Feng He, Min Ding, Carl P. Bergstrom, Piyasena Hewawasam, Scott W. Martin, Robert G. Gentles
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Patent number: 7141680Abstract: The present invention provides novel compounds possessing antibacterial, and/or antifungal activities. Pharmaceutical compositions containing these compounds, methods of making and methods for using these compounds are also provided.Type: GrantFiled: September 18, 2003Date of Patent: November 28, 2006Assignee: Genelabs Technologies, Inc.Inventors: Janos Botyanszki, Dong-Fang Shi, Christopher Don Roberts, Mikail Hakan Gezginci, Stephen Corey Valdez, Sherwin Sattarzadeh
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Patent number: 7119209Abstract: The present invention refers to a process for preparing indolinone derivatives of the general formula (VI) as defined in the specification and intermediates of that process.Type: GrantFiled: February 14, 2003Date of Patent: October 10, 2006Assignee: Pharmacia & Upjohn CompanyInventors: Qingwu Jin, Michael A. Mauragis, Paul D. May
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Patent number: 7094796Abstract: 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): in which: R1 represents a hydrogen atom, an acyl or acyloxy radical, R2 represents the side chain of an alpha-amino acid chosen among L-glutamic acid, L-arginine, L-cysteine, L-methionine, L-histidine, L-tryptophan, L-tyrosine. The present invention also concerns the process for the preparation of said products as well as their applications in neurocosmetic compositions or as active substances on the cutaneous nervous system.Type: GrantFiled: October 2, 2003Date of Patent: August 22, 2006Assignee: Exsymol S.A.M.Inventor: Marie-Christine Seguin
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Patent number: 7056348Abstract: A method for the synthesis of 5-aryl-1,3,3,-trimethyl-2-methylene-indoline derivatives of Formula (I) or its salts of Formula (Ia) wherein 1 mole of a 5-aryl-2,3,3-trimethyl-3H-indole derivative of Formula (VII) is reacted for 1 to 44 hours at a temperature of 20° to 180° C. in an apolar, aprotic or polar, protic or polar aprotic solvent with 1 to 50 moles of a compound of Formula R1-A; new compounds of Formulas (I)/(Ia) and (V), obtainable by this method as well as an agent containing at least one compound of Formula (I)/(Ia) and a carbonyl/imine compound for dyeing keratinic fibers and a method for temporarily dyeing keratin fibers, for which the keratin fiber is dyed with the aforementioned agent and the dyeing, so obtained, is removed again at any later time by a sulfite preparation.Type: GrantFiled: January 24, 2002Date of Patent: June 6, 2006Assignee: Wella AGInventors: Guido Sauter, Hans-Juergen Braun, Nadia Reichlin
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Patent number: 7034029Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptorType: GrantFiled: January 16, 2004Date of Patent: April 25, 2006Assignee: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Patent number: 7019004Abstract: The invention provides compounds of formula (I) wherein X, Y, R1, R2, R3 and R4 are as defined in the description, and the preparation thereof.Type: GrantFiled: May 7, 2001Date of Patent: March 28, 2006Assignee: Novartis AGInventors: Daniel Berney, Robin Breckenridge, Peter Neumann, Gideon Shapiro, Max Peter Seiler, Thomas J. Troxler