Polycyclo Ring System Which Includes Ring Chalcogen Patents (Class 548/525)
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Publication number: 20090203686Abstract: Compounds corresponding to formula I, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n have the meanings given in the description, and also a process for the preparation of these compounds and intermediate products of this process. Furthermore, pharmaceutical compositions comprising the compounds of Formula I and related methods of treatment.Type: ApplicationFiled: February 27, 2009Publication date: August 13, 2009Applicant: Solvay Pharmaceuticals GmbHInventors: Brian Moloney, Lester Marrison, Dieter Ziegler, Michael Mlinaric, Christiane Boecker, Reinhard Brueckner, Michael Weske, Klaus Witte, Yvan Fischer
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Publication number: 20090156831Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.Type: ApplicationFiled: February 19, 2009Publication date: June 18, 2009Inventors: Valeriano MERLI, Augusto CANAVESI, Paola DAVERIO
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Patent number: 7547685Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed herein. Details are provided herein. Compositions, methods, and medicaments related thereto are also disclosed.Type: GrantFiled: November 7, 2005Date of Patent: June 16, 2009Assignee: Allergan, Inc.Inventor: David W. Old
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Patent number: 7534475Abstract: A new liquid crystal compound comprises two condensed and substituted rings. The ring preferably is a five-membered heterocyclic ring. The heterocyclic ring is preferably condensed with benzene ring or an aromatic six-membered heterocyclic ring. The benzene ring or the aromatic six-membered heterocyclic ring is preferably substituted with a group comprising a cyclic structure and a chain structure. The liquid crystal compound is advantageously used in preparation of a thin phase retarder, such as a wide-ranged ?/4 plate, which gives inverse wavelength distribution. The phase retarder can be easily produced according to a simple process by using the new liquid crystal compound.Type: GrantFiled: March 8, 2005Date of Patent: May 19, 2009Assignee: Fujifilm CorporationInventors: Hideyuki Nishikawa, Ryo Hamasaki, Atsuhiro Ohkawa
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Publication number: 20090111992Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.Type: ApplicationFiled: October 17, 2008Publication date: April 30, 2009Applicant: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Noboru Iwakami, Tamotsu Takamatsu
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Patent number: 7524869Abstract: Taxanes having an ester substituent at C(10), a hydroxy substituent at C(7), and a range of C(2), C(9), C(14), and side chain substituents.Type: GrantFiled: October 1, 2003Date of Patent: April 28, 2009Assignee: Florida State University Research Foundation, Inc.Inventor: Robert A. Holton
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Publication number: 20090082308Abstract: The present invention relates to a novel class of benzothiophene amide derivatives. The hydroxamic acid compounds can be used to treat cancer. The benzothiophene amide compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: April 14, 2006Publication date: March 26, 2009Inventors: Jed Lee Hubbs, Dawn M. Mampreian, Joey L. Methot, Thomas A. Miller, Karin M. Otte, Phieng Siliphaivanh, David L. Sloman, Matthew G. Stanton, Kevin J. Wilson, David J. Witter
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Publication number: 20090048224Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.Type: ApplicationFiled: September 5, 2008Publication date: February 19, 2009Applicants: Amgen, Inc., Array BioPharma, Inc.Inventors: Robert D. Groneberg, Benny C. Askew, JR., Derin C. D'Amico, James Zhan, Andras Toro, Youngboo Kim, David A. Mareska, Nianhe Han, Christopher H. Fotsch, Qingyian Liu, Babak Riahi, Kevin Yang, Aiwen Li, Chester Chenguang Yuan, Kaustav Biswas, Scott Harried, Thomas Nguyen, Wenyuan Qian, Jian Jeffrey Chen, Rana Nomak
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Publication number: 20090041721Abstract: The present invention discloses compounds of Formula I or II, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering to the subject a pharmaceutical composition comprising a compound of the present invention.Type: ApplicationFiled: August 9, 2007Publication date: February 12, 2009Inventors: Deqiang Niu, Yonghua Gai, Yat Sun Or, Zhe Wang
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Publication number: 20090036421Abstract: [Problem] To provide a compound which may be used for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS). [Means for Resolution] It was found that a pyrrole derivative characterized by the possession of a guanidinocarbonyl group or amido group as a substituent group at the 3-position, or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT2B receptor and 5-HT7 receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT2B receptor and 5-HT7 receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).Type: ApplicationFiled: February 19, 2007Publication date: February 5, 2009Applicant: ASTELLAS PHARMA INCInventors: Ryushi Seo, Hidetaka Kaku, Hiroyoshi Yamada, Daisuke Kaga, Shinobu Akuzawa
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Patent number: 7482473Abstract: A compound represented by the following general formula (I) or a salt thereof [R1 represents hydrogen atom, or a C1-12 alkyl group; R2 represents a C1-12 alkyl group having one or more maleimide groups, an aryl group having two or more maleimide groups, a group represented by the formula (A): —(CH2)n—CO—N(R11)(R12) (R11 and R12 represent hydrogen atom, a C1-12 alkyl group, a C1-12 alkyl group having one or more maleimide groups, or an aryl group having one or more maleimide groups, and n represents an integer of 1 to 6), or a group represented by the formula (B): —(CH2)m—NH—CO—R13 (R13 represents a C1-12 alkyl group having one or more maleimide groups, or an aryl group having one or more maleimide groups, and m represents an integer of 1 to 6); R3 and R5 represent hydrogen atom, or a halogen atom; R4 represents hydroxyl group, a C1-12 acyloxy group, a C1-12 acyloxymethyloxy group, or an amino group], which is useful as a novel fluorescent labeling agent having a property of emitting intense fluorescence onlyType: GrantFiled: September 7, 2006Date of Patent: January 27, 2009Assignee: The University of TokyoInventors: Tetsuo Nagano, Yasuteru Urano, Takuji Shoda
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Publication number: 20090017546Abstract: The present invention provides novel reactive fluorescent compounds that incorporate stable isotopic (deuterium, 13-carbon, 15-nitrogen, 18-oxygen) substitutions. The invention includes the use of these compounds, in combination with non-isotopically substituted analogs, for the purification, identification and relative quantification of proteins, peptides, saccharides, metabolites, and other biologically important compounds by combining liquid chromatography (LC) and mass spectrometry (MS). Fluorescent labeling of target compounds in this manner provides orders-of-magnitude sensitivity enhancement over traditional stable isotope labels, and also affords the possibility of simultaneous multiplexed analysis due to the multiwavelength nature of different fluorophores.Type: ApplicationFiled: July 21, 2008Publication date: January 15, 2009Applicant: INVITROGEN CORPORATIONInventors: Brian Agnew, Kyle Richard Gee
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Publication number: 20090018113Abstract: The present application relates to a novel cyclopenta[b]benzofuran derivatives, processes for their preparation and their use for the manufacture of medicaments, in particular for the prophylaxis and/or therapy of acute or chronic disorders characterized by elevated cellular stress, by local or systemic inflammatory processes or by hyperproliferation.Type: ApplicationFiled: May 14, 2005Publication date: January 15, 2009Applicant: Bayer HealthCare AGInventors: Nicole Diedrichs, Thomas Fahrig, Irene Gerlach, Jaques Ragot, Joachim Schuhmacher, Kai Thede, Ervin Horvath
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Publication number: 20090018346Abstract: The present invention relates to amorphous form darifenacin hydrobromide and processes therefor. In addition, the present invention relates to compositions comprising amorphous form darifenacin hydrobromide.Type: ApplicationFiled: July 11, 2008Publication date: January 15, 2009Applicant: Medichem, S.A.Inventors: Monica Benito Velez, Stephen Benedict David Winter, Nuria Soldevilla Madrid
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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: 20090012011Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted pyrrolidines, according to Formula I Specifically, the invention is directed to compounds according to Formula I wherein R1 is H or C1-C6 alkyl; R2 is H or OH; and R3 is an optionally substituted aryl.Type: ApplicationFiled: January 11, 2007Publication date: January 8, 2009Applicant: SmithKline Beecham CorporationInventors: Linda N. Casillas, Robert W. Marquis, JR.
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Publication number: 20090005431Abstract: Disclosed herein are substituted pyrrolidine-based muscarinic receptor modulators of Formula I, process of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: June 30, 2008Publication date: January 1, 2009Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Sepehr Sarshar
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Patent number: 7468443Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.Type: GrantFiled: May 3, 2006Date of Patent: December 23, 2008Assignee: Toyama Chemical Co., Ltd.Inventors: Akihito Saitoh, Noboru Iwakami, Tamotsu Takamatsu
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Publication number: 20080312455Abstract: The present invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity, of darifenacin and its intermediate compounds and salts thereof. In addition, the invention relates to a method for differentiating and quantifying the enantiomers, thereby determining the enantiomeric purity of compounds of formula (I): wherein Y is hydrogen or a substituent of the formula: including the differentiation and quantification of compounds of formula (I) of varying enantiomeric purity from their corresponding enantiomers. The invention further relates to a process for preparing enantiomerically pure darifenacin using enantiomerically pure starting compounds which have been previously differentiated and quantified according to the method of the invention.Type: ApplicationFiled: June 13, 2008Publication date: December 18, 2008Applicant: Medichem, S.A.Inventors: Nuria Soldevilla Madrid, Jordi Bosch i Llado
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Patent number: 7465751Abstract: This invention generally relates to the derivatives of 1-substituted-3-pyrroli dines having the structure of Formula (I): The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention. pharmaceutical compositions containing the compounds of the present invention and the methods for treating the diseases mediated through muscarinic receptors.Type: GrantFiled: December 23, 2002Date of Patent: December 16, 2008Assignee: Ranbaxy Laboratories LimitedInventors: Anita Mehta, Jang Bahadur Gupta, Pakala Kumara Savithru Sarma
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Publication number: 20080300192Abstract: Auristatin-type peptides are disclosed which are highly cytotoxic, synthetically accessible, and can be conjugated to antibodies and other ligands.Type: ApplicationFiled: November 14, 2005Publication date: December 4, 2008Applicant: Seattle Genetics, Inc.Inventors: Svetlana o. Doronina, Brian A. Mendelsohn
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Publication number: 20080292587Abstract: The present invention discloses compounds of formulae I, or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 24, 2008Publication date: November 27, 2008Inventors: Ying Sun, Yat Sun Or, Zhe Wang
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Patent number: 7449483Abstract: The present invention relates to heteroaromate OSC inhibitors. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with 2,3-oxidosqualene-lanosterol cyclase such as hypercholesterolemia, hyperlipemia, arteriosclerosis, vascular diseases, mycoses, gallstones, tumors and/or hyperproliferative disorders, and treatment and/or prophylaxis of impaired glucose tolerance and diabetes.Type: GrantFiled: December 6, 2006Date of Patent: November 11, 2008Assignee: Hoffman-La Roche Inc.Inventors: Johannes Aebi, Jean Ackermann, Henrietta Dehmlow, Hans-Peter Maerki, Olivier Morand
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Publication number: 20080274907Abstract: A new class of pH sensitive fluorescent dyes and assays relating thereto are described. The dyes and assays are particularly suited for biological applications including phagocytosis and monitoring intracellular processes. The pH sensitive fluorescent dyes of the present invention include compounds of Formula I: wherein the variables are described throughout the application.Type: ApplicationFiled: October 29, 2007Publication date: November 6, 2008Applicant: INVITROGEN CORPORATIONInventors: Daniel Beacham, Jeffrey Dzubay, Kyle Gee, Vladimir Martin, Aleksey Rukavishnikov
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Patent number: 7446124Abstract: Novel wortmannin analogs and their use in inhibiting PI-3-kinase activity in mammals and the treatment or prevention of cancer and tumor formation in a subject are described herein. Preferably, the wortmannin analogs may be administered with other chemotherapeutic agents in the treatment of cancer.Type: GrantFiled: July 11, 2005Date of Patent: November 4, 2008Assignees: Prolx Pharmaceuticals Corp., The University of Pittsburgh, Arizona Board of Regents, Acting on Behalf of the University of ArizonaInventors: Lynn Kirkpatrick, Garth Powis, Peter Wipf
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Publication number: 20080269504Abstract: Provided are darifenacin hydrobromide free of oxidized darifenacin, and processes for the preparation thereof.Type: ApplicationFiled: July 1, 2008Publication date: October 30, 2008Inventors: Valeriano Merli, Augusto Canavesi, Paola Daverio, Alessandra Vailati
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Publication number: 20080269503Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.Type: ApplicationFiled: July 1, 2008Publication date: October 30, 2008Inventors: Valeriano Merli, Augusto Canavesi, Paola Daverio
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Publication number: 20080269505Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.Type: ApplicationFiled: July 1, 2008Publication date: October 30, 2008Inventors: Valeriano Merli, Augusto Canavesi, Paola Daverio
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Patent number: 7442806Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.Type: GrantFiled: December 27, 2006Date of Patent: October 28, 2008Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Valeriano Merli, Augusto Canavesi, Paola Daverio
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Publication number: 20080255221Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.Type: ApplicationFiled: November 14, 2007Publication date: October 16, 2008Applicant: PHARMACYCLICS, INC.Inventors: Erik J. Verner, Hon C. Hui
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Publication number: 20080227814Abstract: The present invention relates to a selective estrogen receptor modulator selected from the group consisting of: (I) or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and uterine leiomyoma.Type: ApplicationFiled: January 18, 2005Publication date: September 18, 2008Inventors: Jeffrey Alan Dodge, Scott Alan Frank, Ronald Jay Hinklin, Owen Brendan Wallace
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Publication number: 20080221338Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.Type: ApplicationFiled: May 6, 2008Publication date: September 11, 2008Inventors: Valeriano Merli, Augusto Canavesi, Paola Daverio
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Publication number: 20080214835Abstract: The invention encompasses processes for the preparation of darifenacin hydrobromide.Type: ApplicationFiled: May 6, 2008Publication date: September 4, 2008Inventors: Valeriano Merli, Augusto Canavesi, Paola Daverio
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Publication number: 20080214811Abstract: The invention provides a novel class of xanthene dyes, some of which are functionalized to allow their coupling to conjugation partners of interest, e.g. biomolecules, drugs, toxins and the like. Also provided are conjugates of the dyes, methods of preparing and using the dyes and their conjugates and kits including the dyes and their conjugates.Type: ApplicationFiled: February 25, 2008Publication date: September 4, 2008Applicant: Biosearch Technologies, Inc.Inventors: Mark Reddington, Matt Lyttle
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Publication number: 20080207691Abstract: The present invention provides compounds of formula I that are useful as potent and selective inhibitors of 11-beta hydroxysteroid dehydrogenase 1. The present invention further provides a pharmaceutical composition which comprises a compound of Formula I, or a pharmaceutical salt thereof, and a pharmaceutically acceptable carrier, diluent, or excipient. In addition, the present invention provides compositions comprising compounds of formula I for the treatment of metabolic syndrome, diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, other symptoms associated with hyperglycemia, and related disorders. Formula (I) wherein, Ru0 is (II), or (III) G1 is methylene or ethylene; L is a divalent linking group selected from —(C1-C4) alkylene-, —S—, —CH(OH)—, or —O—; A is methylene, —S—, —O—, or —NH—; and the other substituents are as defined in the claims.Type: ApplicationFiled: December 16, 2005Publication date: August 28, 2008Inventors: Thomas Daniel Aicher, Mark Joseph Chicarelli, Ronald Jay Hinklin, Hongqi Tian, Owen Brendan Wallace
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Patent number: 7417062Abstract: Substituted benzamide compounds are provided along with methods for the use of those compounds for treating cancer.Type: GrantFiled: August 11, 2005Date of Patent: August 26, 2008Assignee: ChemoCentryx, Inc.Inventors: Anita Melikian, John J. Kim Wright
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Publication number: 20080182876Abstract: The present patent application concerns new compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a saturated nitrogen-containing ring, A is a saturated C1-4 alkylene and B a C3-4 alkylene or alkenylene chain; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.Type: ApplicationFiled: April 26, 2006Publication date: July 31, 2008Inventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz
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Publication number: 20080177086Abstract: Compounds having the general of formula I and/or formula II wherein R1 and R2 are the same or different and are independently selected from the group consisting of —H, —C1-C18-alkyl or -?-sulfoalkyl; X and Y are the same or different and are independently selected from the group consisting of —O?, —OH, —SH, —NH—NH2, —F, —Cl, —Br, —I, —O-Su (succinimidyl/sulfosuccinimidyl), —O-STP (4-sulfo-2,3,5,6-tetrafluorophenyl), —O-TFP (2,3,5,6-tetrafluorophenyl), —O-benzotriazole, -benzotriazole, —NR—CO—CH2—I, —NR2, —NR-biomolecule, —NR-L-COO?, —NR-L-COOH, —NR-L-COO-Su, —NR-L-COO-STP, —NR-L-COO-TFP, —NR-L-CONR2, —NR-L-CO-biomolecule, —NR-L-CO—NH—NH2, —NR-L-OH, —NR-L-O-phosphoramidite, —NR-L-CHO, —NR-L-maleimid, or —NR-L-NH—CO—CH2—I; where R is equal to R1 and R2 and L is selected from the group consisting of a divalent linear (—(CH2)o—, o=1 to 15), crossed, or cyclic alkane group that can be substituted by at least one atom selected from the group consisting of oxygen, substituted niType: ApplicationFiled: January 22, 2007Publication date: July 24, 2008Applicant: PIERCE BIOTECHNOLOGY, INC.Inventors: Wilhelm G. Frank, Matthias S. Wenzel, Peter T. Czerney, Surbhi Desai, Greg Hermanson
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Patent number: 7402606Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.Type: GrantFiled: April 1, 2003Date of Patent: July 22, 2008Assignee: SmithKline Beecham CorporationInventors: David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
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Publication number: 20080167367Abstract: A stable solid hydrate of a muscarinic receptor antagonist is useful in the treatment of irritable bowel syndrome, diverticular disease, oesophageal achalasia, chronic obstructive airways disease, over active bladder (including symptoms of incontinence, urge and frequency), urinary incontinence, neurogenic urinary urgency or pollakiuria, treatment of bladder functional disorder, urinary leakage, painful or difficult urination caused by neurogenic bladder, spastic or hypertonic bladder, dysfunctional bladder syndrome, gastrointestinal disorders including gastrointestinal hyperactivity, and relaxing effect on intestinal smooth muscle cells.Type: ApplicationFiled: March 17, 2008Publication date: July 10, 2008Inventors: Peter James Dunn, John George Matthews, Trevor Jack Newbury, Garry O'Connor
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Publication number: 20080146607Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: December 18, 2007Publication date: June 19, 2008Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
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Publication number: 20080132710Abstract: Atrasentan Hydrochloride Crystalline Form 2, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.Type: ApplicationFiled: December 4, 2007Publication date: June 5, 2008Applicant: ABBOTT LABORATORIESInventors: Rodger F. Henry, Geoff G.Z. Zhang
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Publication number: 20080125444Abstract: The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: June 6, 2007Publication date: May 29, 2008Inventors: Ying Sun, Yat Sun Or, Zhe Wang
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Patent number: 7361755Abstract: This invention pertains to a novel process for preparing sterically hindered N-substituted alkyloxyamines from alkenes by the transition-metal-catalyzed reaction of a intermediate alkylborane with a sterically hindered nitroxyl radical.Type: GrantFiled: December 12, 2002Date of Patent: April 22, 2008Assignee: Ciba Specialty Chemicals CorporationInventors: Stephen Daniel Pastor, Sai Ping Shum
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Patent number: 7361663Abstract: This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: October 16, 2003Date of Patent: April 22, 2008Assignee: Aventis Pharmaceuticals Inc.Inventors: Mark Czekaj, Scott I. Klein, Heinz W. Pauls
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Publication number: 20080064679Abstract: Water-soluble cannabinoid compounds that are agonists of CB1 and CB2 cannabinoid receptors are provided. The compounds are made water-soluble by derivatization of the alkyl side chain and/or the phenolic hydroxyl group of tetrahydrocannabinol. The water-soluble cannabinoids are useful for the treatment of appetite loss, pain, multiple sclerosis, nausea and vomiting, and epilepsy.Type: ApplicationFiled: June 23, 2005Publication date: March 13, 2008Inventors: Billy R. Martin, Raj K. Razdan, Anu Mahadevan
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Patent number: 7335679Abstract: Novel Wortmannin analogs and their use in inhibiting inhibiting PI-3-kinase activity in mammals as well as tumor formation in a subject are described herein.Type: GrantFiled: April 7, 2006Date of Patent: February 26, 2008Assignees: Arizona Board of Regents on behalf of the University of Arizona, University of PittsburghInventors: Garth Powis, Peter Wipf
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Publication number: 20080014173Abstract: Hepatitis C virus inhibitors having the general formula are disclosed. Compositions comprising the compounds and methods for using the compounds to inhibit HCV are also disclosed.Type: ApplicationFiled: July 10, 2007Publication date: January 17, 2008Inventors: Paul Michael Scola, Li-Qiang Sun
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Patent number: 7314875Abstract: The present invention provides compounds of the structure: wherein the constituent members are defined herein, including pharmaceutical compositions thereof and methods of treating diseases therewith.Type: GrantFiled: April 12, 2005Date of Patent: January 1, 2008Assignee: Cephalon, Inc.Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John A. Gruner, Rabindranath Tripathy
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Patent number: 7304081Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: GrantFiled: May 4, 2005Date of Patent: December 4, 2007Assignee: Incyte CorporationInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang