Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 514/327)
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Patent number: 7700628Abstract: This application relates to a compound of formula (I) (or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa and/or thrombin, as well as a process for its preparation and intermediates therefor. An example of a compound of formula (I) is (a).Type: GrantFiled: November 10, 2005Date of Patent: April 20, 2010Assignee: Eli Lilly and CompanyInventors: Ankush Baburao Argade, Theodore Goodson, Jr., David Kent Herron, Sajan Joseph, Salvatore Donato Lepore, Angela Lynn Marquart, John Joseph Masters, David Mendel, Leander Merritt, Andrew Michael Ratz, Gerald Floyd Smith, Anne Louise Tebbe, Michael Robert Wiley, Ying Kwong Yee
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Publication number: 20100093753Abstract: The invention provides compounds of formula I: wherein a, b, c, m, n, q, r, W, Z1, Ar1, Z2, Y, R1, R2, and R3 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: December 17, 2009Publication date: April 15, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, Yu-Hua Ji, Mathai Mammen, Viengkham Malathong
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Patent number: 7683077Abstract: The present invention provides a piperidine derivative represented by the following formula or analogs thereto, which are used for agents for treating or preventing various diseases related to 5-HT7.Type: GrantFiled: May 19, 2004Date of Patent: March 23, 2010Assignee: Ajinomoto Co., Inc.Inventors: Shingo Makino, Naoyuki Fukuchi, Sayaka Asari, Masaki Hashimoto, Tetsuo Yano, Youji Yamada, Munetaka Tokumasu, Masataka Shoji, Itsuya Tanabe, Shinichi Fujita, Hideki Matsumoto
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Publication number: 20100069401Abstract: A catecholamine or related compound of formula (I) having (S)-configuration at ?-carbon and having a lipophilicity greater than (S)-noradrenalme, a physiologically tolerated salt thereof, a prodrug thereof, a physiologically functional derivative thereof or any mixture thereof is useful as an anti-angiogemc agent A catecholamine or related compound of formula (II) in which a ?-hydroxy group has been modified is also anti-angiogemcType: ApplicationFiled: January 29, 2008Publication date: March 18, 2010Inventors: Yasuo Konishi, Joanne Magoon, Suwatchai Jarussophon
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Publication number: 20100063040Abstract: The present invention provides an sulfonamide derivative having DP receptor antagonistic activity and a pharmaceutical composition comprising the said compound as an active ingredient, and further a therapeutic agent for treating allergic diseases. A compound of the general formula (II): wherein the ring A is an aromatic carbocyclic ring etc.; the ring B is a nitrogen-containing non-aromatic heterocyclic ring etc.; the ring C is an aromatic carbocyclic ring etc.; R1 is carboxy etc.; R2 is independently a halogen atom etc.; R3 is optionally substituted alkyloxy etc.; R4 is independently a halogen atom etc.; R5 is independently optionally substituted alkyl etc.; M is sulfonyl etc.; Y is a single bond etc.; L1 is a single bond etc.; L2 is a single bond etc.; k is 0, 1, 2, 3 or 4; n is 0, 1 or 2; and q is 0, 1, 2 or 3; provided that a) k is not 0 when the ring B is a 6-membered nitrogen-containing heterocyclic ring containing one or two nitrogen atom(s) and the ring C is a benzene ring, etc.Type: ApplicationFiled: September 25, 2006Publication date: March 11, 2010Inventor: Akira Kugimiya
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Publication number: 20100063096Abstract: The invention provides compounds of formula I: wherein a, b, c, p, W, A, X1, R1, R2, R3, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: November 12, 2009Publication date: March 11, 2010Applicant: THERAVANCE, INC.Inventors: YongQi Mu, YuHua Ji, Mathai Mammen, Eric L. Stangeland
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Patent number: 7674805Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.Type: GrantFiled: August 21, 2008Date of Patent: March 9, 2010Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Jacques Froissant, Christian Hoornaert
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Publication number: 20100055048Abstract: Methods of treating headache with antipsychotics are provided. A kit for treating headache is also provided, comprising an antipsychotic and a device for rapid delivery of the antipsychotic.Type: ApplicationFiled: November 9, 2009Publication date: March 4, 2010Applicant: Alexza Pharmaceuticals, Inc.Inventors: Ron L. Hale, Peter M. LIoyd, Amy T. Lu, Patrik Munzar, Joshua D. Rabinowitz, Roman Skowronski
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Publication number: 20100048550Abstract: The present invention relates to novel compounds of general formula (I) which are thyroid receptor ligands and are preferably selective for the thyroid hormone receptor beta(TR-Beta). Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them.Type: ApplicationFiled: October 15, 2007Publication date: February 25, 2010Inventors: Saurin Raval, Preeti Raval, Braj Lohray, Vidya Bhushan Lohray, Pankaj R. Patel
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Patent number: 7662816Abstract: Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is R is —C(O)—N(R27)(R28) or and the remaining variables are as defined in the specification. Also disclosed are pharmaceutical compositions comprising the compounds of formula I. Also disclosed are methods of treating cognitive or neurodegenerative diseases such as Alzheimer's disease. Also disclosed are pharmaceutical compositions and methods of treating cognitive or neurodegenerative diseases comprising the compounds of formula I in combination with a ?-secretase inhibitor other than those of formula I, an HMG-CoA reductase inhibitor, a gamma-secretase inhibitor, a non-steroidal anti-inflammatory agent, an N-methyl-D-aspartate receptor antagonist, a cholinesterase inhibitor or an anti-amyloid antibody.Type: GrantFiled: August 4, 2004Date of Patent: February 16, 2010Assignee: Schering CorporationInventors: Jared N. Cumming, Ulrich Iserloh, Andrew Stamford, Corey Strickland, Johannes H. Voigt, Yusheng Wu, Ying Huang, Yan Xia, Samuel Chackalamannil, Tao Guo, Douglas W. Hobbs, Thuy X. H. Le, Jeffrey F. Lowrie, Kurt W. Saionz, Suresh D. Babu
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Patent number: 7662838Abstract: The invention relates to the use of a deoxynojirimycin derivative, or pharmaceutically acceptable salt thereof, for the preparation of a medicament for the treatment of insulin resistance, hyperpigmentation and/or inflammatory processes in the skin, a fungal disease, overweight and obesity, or a microbacterial infection.Type: GrantFiled: October 29, 2004Date of Patent: February 16, 2010Assignee: Genzyme CorporationInventor: Johannes Maria Franciscus Gerardus Aerts
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Publication number: 20100035865Abstract: The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of formula (I), as defined in the specification. The invention is also directed to compositions containing the compounds of formula (I).Type: ApplicationFiled: March 26, 2008Publication date: February 11, 2010Inventors: Kimberly Gail Estep, Anton F.J. Fliri, Christopher J. O'Donnell
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Publication number: 20100029720Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.Type: ApplicationFiled: September 9, 2009Publication date: February 4, 2010Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
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Patent number: 7655626Abstract: The present invention refers to a pharmaceutical composition comprising an isolated antiangiogenic peptide or a recombinant protein comprising the antiangiogenic peptide, wherein the peptide is between 11 and 40 amino acids in length and having antiangiogenic activity, the peptide comprising the amino acid sequence: X1-X2-X3-X4-X5-X6-X7-X8-X9-X10-X11-X12-X13-X14, wherein X1 is any amino acid residue compatible with forming a helix; X2 is an amino acid residue of: Leu, Ile, Val; X3 is an amino acid residue of: Arg, Lys, His, Ser, Thr; X4 is an amino acid residue of: Ile, Leu, Val; X5 is any amino acid residue compatible with forming a helix; X6 is an amino acid residue of: Leu, Ile, Val; X7 is an amino acid residue of: Leu, Ile, Val, Ser, Thr; X8 is any amino acid residue compatible with forming a helix; X9 is any amino acid residue compatible with forming a helix; X10 is an amino acid residue of: Gln, Glu, Asp, Arg, His, Lys, Asn; X11 is an amino acid residue of: Ser, Thr; X12 is an amino acid residue of: TrpType: GrantFiled: August 11, 2005Date of Patent: February 2, 2010Assignees: Universite de Liege, Faculte Universitaire des Sciences Agronomiques de GemblouxInventors: Joseph Martial, Ingrid Struman, Ngoc-Quynh-Nhu Nguyen, Robert Brasseur, Laurence Lins
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Publication number: 20100022496Abstract: A galenical form for the administration transmucously of at least one active ingredient, characterized in that the active ingredient is in a stable and complete dissolved state in a hydroalcoholic solution that includes at least 20% by mass of alcohol so as to allow rapid absorption of the active ingredient through the mucous membranes of the buccal cavity and/or the oropharynx. Uses of the galenical form are also disclosed.Type: ApplicationFiled: September 21, 2007Publication date: January 28, 2010Inventors: Philippe Perovitch, Marc Maury
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Publication number: 20100016366Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical compositions containing them.Type: ApplicationFiled: July 1, 2009Publication date: January 21, 2010Inventors: Paul Alan Glossop, Charlotte Alice Louise Lane
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Publication number: 20100009983Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, in combination with one or more other neurogenic agents, or anti-astrogenic agent, to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: June 25, 2009Publication date: January 14, 2010Applicant: BrainCells, Inc.Inventors: Carrolee Barlow, Todd A. Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain
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Patent number: 7645774Abstract: There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.Type: GrantFiled: August 5, 2005Date of Patent: January 12, 2010Assignee: Schering CorporationInventors: Richard J. Friary, Joseph A. Kozlowski, Bandarpalle B. Shankar, Michael K. C. Wong, Guowei Zhou, Brian J. Lavey, Neng-Yang Shih, Ling Tong, Lei Chen, Youheng Shu
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Publication number: 20100004289Abstract: The present invention relates to a central nervous system-acting substituted butyrophenones. These compounds are useful in antipsychotic medications for psychosis, including schizophrenia, but especially for L-DOPA-induced psychosis, while having low or no risk of eliciting extrapyramidal side effects, hyperprolactinemia or tardive dyskinesia.Type: ApplicationFiled: May 1, 2006Publication date: January 7, 2010Applicant: CLERA INC.Inventor: Philip Seeman
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Publication number: 20090326010Abstract: The present application describes the compound of formula (I): or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and arthrosclerosis using the compound of the invention are disclosed.Type: ApplicationFiled: June 24, 2009Publication date: December 31, 2009Inventor: Joseph B. Santella
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Publication number: 20090325925Abstract: This invention provides thiophene compounds of formula I: wherein R1, R2, R3, R4, n, p, and m are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 26, 2009Publication date: December 31, 2009Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christelle C. Renou, Tricia J. Vos, Matthew O. Duffey, Robert Downham
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Publication number: 20090325949Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on use of a 5HTR agent, optionally in combination with one or more other neurogenic agents, to stimulate or activate the formation of new nerve cells.Type: ApplicationFiled: June 25, 2009Publication date: December 31, 2009Applicant: BrainCells, Inc.Inventors: Carrolee Barlow, Todd Carter, Andrew Morse, Kai Treuner, Kym I. Lorrain
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Patent number: 7638488Abstract: The present invention provides methods for treating a flavivirus infection, including hepatitis C virus (HCV) infection, in an individual suffering from a flavivirus infection. In some embodiments, the methods involve administering to an individual in need thereof an effective amount of an agent that inhibits enzymatic activity of a membrane-bound ?-glucosidase inhibitor. In other embodiments, the methods involve administering to an individual in need thereof effective amounts of an ?-glucosidase inhibitor and at least one additional therapeutic agent.Type: GrantFiled: March 7, 2006Date of Patent: December 29, 2009Assignee: Intermune, Inc.Inventors: Lawrence M. Blatt, Hua Tan, Scott Seiwert
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Patent number: 7635707Abstract: Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage for a time period, followed by administering to the patient pirfenidone at the full target dosage. The methods also include administering pirfenidone at the full target dose with no reduction and administering permanently reduced doses of pirfenidone.Type: GrantFiled: September 3, 2009Date of Patent: December 22, 2009Assignee: Intermune, Inc.Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
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Publication number: 20090312358Abstract: The present invention is directed to methods of treatment and/or management of diarrhea, such as chronic diarrhea using sequential administration of opioid agonists to suppress gut mobility and opioid antagonists to reverse the effect to controllably allow bowel movements. The agonists and antagonists are administered with a time interval in between the administration or between the release of the drugs from a pharmaceutical composition. The invention is further directed to methods of controlling, treating or managing side effects caused by the opioid agonists, specifically the side effects resulting from mast cell activation and/or granulation.Type: ApplicationFiled: March 22, 2007Publication date: December 17, 2009Applicant: TRUSTEES OF BOSTON UNIVERSITYInventor: Fouad A. Siddiqi
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Publication number: 20090311327Abstract: The present, invention provides an oral delivery system for a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof with pharmacological, physiological or biochemical activity. The present invention particularly provides a swallow formulation comprising a therapeutic compound that is an acid, a salt of an acid or an unionized compound or a proactive form thereof which facilitates the rapid delivery of the therapeutic compound to the circulatory system.Type: ApplicationFiled: November 28, 2006Publication date: December 17, 2009Applicant: IMAGINOT PTY LTDInventors: Michael Stephen Roberts, George Alexander Davidson, Ruoying Jiang, Geraldine Ann Elliott, Keivan Bezanehtak, Stephen Douglas Chandler, Greg Davey, Mantu Sarkar
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Publication number: 20090306134Abstract: Disclosed are multibinding compounds which are muscarinic receptor antagonists. The multibinding compounds of this invention containing from 2 to 10 ligands covalently attached to one or more linkers. Each ligand is, independently of each other, a muscarinic receptor antagonist or an allosteric modulator provided that at least one of said ligand is a muscarinic receptor antagonist. The multibinding compounds of this invention are useful in the treatment and prevention of diseases such as chronic obstructive pulmonary disease, chronic bronchitis, irritable bowel syndrome, urinary incontinence, and the like.Type: ApplicationFiled: September 30, 2008Publication date: December 10, 2009Inventors: James Aggen, John H. Griffin, Mathai Mammen, Daniel Marquess, Edmund J. Moran, David Oare
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Publication number: 20090304720Abstract: Active agent-loaded nanoparticles that are based on a hydrophilic protein or a combination of hydrophilic proteins, and methods for producing the nanoparticles and the use thereof. Functional proteins or peptide fragments are bound to the nanoparticles via polyethylene glycol-?-maleimide-?-NHS esters.Type: ApplicationFiled: February 27, 2007Publication date: December 10, 2009Applicant: LTS Lohmann Therapie-Systeme AGInventors: Jörg Kreuter, Klaus Langer, Kerstin Michaelis, Telli Hekmatara, Sebastian Dreis
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Patent number: 7625928Abstract: Pharmaceutical compositions useful in preventing and treating negative side effects accompanying radiotherapy are disclosed. More particularly, new formulations that can be applied to the skin and mucous membranes of patients undergoing radiotherapy and methods of using these formulations are disclosed.Type: GrantFiled: September 29, 2003Date of Patent: December 1, 2009Assignee: Mitos Pharmaceuticals, Inc.Inventors: Kameron W. Maxwell, Peter C. Hoyle
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Patent number: 7605173Abstract: A pharmaceutical liquid composition containing the Pirfenidone in a very high concentration of more or less 25% by weight can be obtained by dissolving the Pirfenidone in diethylene glycol monoethyl ether. Even when the liquid medicinal compositions are stored for a long period of time, the Pirfenidone will not be recrystallized with a good chemical and physical stability. Furthermore, the liquid compositions are little irritating to the wounds on the mucous membrane of the skin and suitable for the manufacture of pharmaceutical formulations to be administered either via the oral, percutaneous, nasal or vaginal routes or by means of spray, patch, inhalation, injection or intravenous drip.Type: GrantFiled: December 24, 2003Date of Patent: October 20, 2009Assignee: KDL, Inc.Inventor: Pyare L. Seth
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Publication number: 20090247522Abstract: The present invention provides Hsp90 family protein inhibitors comprising, as an active ingredient, a benzoyl compound represented by general formula (I): (wherein n represents an integer of 0 to 10; R1 represents substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkoxycarbonyl, CONR7R8 or the like; R2 represents substituted or unsubstituted aryl, a substituted or unsubstituted aromatic heterocyclic group or the like; R3 and R5, which may be the same or different, each represent a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl or the like; and R4 and R6, which may be the same or different, each represent a hydrogen atom, halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl or the like) or a prodrug thereof, or a pharmaceutically acceptable salt of said benzoyl compound or said prodrug.Type: ApplicationFiled: April 22, 2009Publication date: October 1, 2009Applicant: KYOWA HAKKO KOGYO CO., LTD.Inventors: Shinji Nara, Hiroshi Nakagawa, Yutaka Kanda, Takayuki Nakashima, Shiro Soga, Jiro Kajita, Jun-ichi Saito, Yukimasa Shiotsu, Shiro Akinaga
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Publication number: 20090247584Abstract: Compounds of the formula (I), in which R1, R2?, R2?, R2??, R3 and n are as defined in Claim 1, are effectors of the nicotinic and/or muscarinic acetylcholine receptor and are suitable for the prophylaxis or treatment of schizophrenia, depression, anxiety states, dementia, Alzheimer's disease, Lewy bodies dementia, neurodegenerative diseases, Parkinson's disease, Huntington's disease, Tourette's syndrome, learning and memory impairments, age-related memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds.Type: ApplicationFiled: February 26, 2009Publication date: October 1, 2009Inventors: Gunter HOLZEMANN, Helmut Prucher, Kai Schiemann, Joachim Leibrock, Hartmut Greiner, Christa Burger, Laurie von Melchner
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Patent number: 7595331Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl]piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: December 8, 2004Date of Patent: September 29, 2009Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Publication number: 20090239810Abstract: The present invention relates to piperidine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.Type: ApplicationFiled: March 20, 2009Publication date: September 24, 2009Applicant: Forest Laboratories Holdings LimitedInventors: Kumar Sundaresan, P.Bala Koteswara Rao, Bharathiraja Ainan, Hariharasubramanian Ayyamperumal, Girish A R, Srinivas Tatiparthy, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Publication number: 20090239829Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.Type: ApplicationFiled: July 25, 2007Publication date: September 24, 2009Applicant: BRACCO IMAGING SPAInventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
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Publication number: 20090233968Abstract: Novel compounds inhibiting the integrin ?2?1/GPIa-IIa receptor are disclosed. Also disclosed are pharmaceutical compositions containing the compounds, as well as methods of their therapeutic use. The compounds disclosed are useful, inter alia, as inhibitors of integrin ?2?1/GPIa-IIa-mediated activity.Type: ApplicationFiled: June 7, 2006Publication date: September 17, 2009Applicant: The Trustees of the University of PennsylvaniaInventors: William F. Degrado, Joel S. Bennett, Seth Elliott Snyder, Sungwook Choi
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Publication number: 20090233969Abstract: The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: ApplicationFiled: May 27, 2009Publication date: September 17, 2009Applicant: DECODE GENETICS EHFInventors: Vincent Sandanayaka, Jasbir Singh, Mahnaz Keyvan, Michael David Krohn, Mark E. Gurney
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Publication number: 20090232780Abstract: This invention generally provides compounds, pharmaceutical compositions, and methods for their use, which include methods that result in increased expression in an Atoh1 gene (e.g., Hath1) in a biological cell. More specifically, the invention relates to the treatment of diseases and/or disorders that would benefit from increased Atoh1 expression, e.g., a hearing impairment or imbalance disorder associated with a loss of auditory hair cells, or a disorder associated with abnormal cellular proliferation.Type: ApplicationFiled: February 9, 2009Publication date: September 17, 2009Applicant: Massachusetts Eye & Ear InfirmaryInventors: Albert Edge, Sang-Jun Jeon, Kathleen Seyb, Marcie Glicksman, Lixin Qiao, Gregory D. Cuny
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Publication number: 20090233965Abstract: The invention provides compounds of formula (I), wherein R1, R2, R3, R4, R5 and X are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them, a process for preparing pharmaceutical compositions and their use in therapy (I).Type: ApplicationFiled: April 23, 2007Publication date: September 17, 2009Applicant: ASTRAZENECA ABInventors: Andrew Bailey, Antonio Mete, Garry Pairaudeau, Michael Stocks, Mark Wenlock
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Patent number: 7589107Abstract: Methods to prevent, inhibit, or slow the development of vitrectomy-induced cataracts are disclosed. The methods comprise administering to the eye of a subject a composition comprising an ophthalmologically acceptable carrier or diluent and at least one hydroxylamine compound in a therapeutically sufficient amount to prevent, inhibit, or slow the development of a vitrectomy-induced cataract in the subject to which the composition is administered.Type: GrantFiled: May 22, 2006Date of Patent: September 15, 2009Assignee: Othera Holding, Inc.Inventors: William L. Matier, Ghanshyam Patil
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Patent number: 7582655Abstract: The present invention relates to 4-piperidone derivatives represented by the following formula (I) and the acid addition salts thereof. The method of preparation and antineoplastic activity of the said compounds are disclosed. A number of the compounds possess submicromolar IC50 and CC50 values and have a selective toxicity for colon cancers and leukemic cells. In addition, many of the compounds are able to reverse multidrug resistance.Type: GrantFiled: November 22, 2006Date of Patent: September 1, 2009Assignee: University of SaskatchewanInventors: Jonathan R. Dimmock, Umashankar Das
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Publication number: 20090215821Abstract: N-substituted azacycle derivative compounds represented by formula (I): wherein m, q, r, t and u are independently selected from 0 or 1; and p is 0, 1, 2, or 3; and A, B, D, X, Y, R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are fully described herein. The compounds being particularly useful in compositions comprising an insecticidally effective amount of at least one compound of formula I, and an 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: October 4, 2004Publication date: August 27, 2009Inventors: George Theodoridis, David Rosen, Shunxiang Zhang, Walter H. Yeager, Robert N. Henrie, II, Syed Z. Ahmed, Hongbin Men, Stephen Donovan
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Publication number: 20090209619Abstract: The use of an HERG channel inhibitor for controlling the proliferation of cancer cells. Examples of such HERG channel inhibitors include dofetilide, cisapride, E-4031 and a siRNA molecule targeting a sequence involved in the expression of an HERG channel. Other ERG channels are also targets for these inhibitors.Type: ApplicationFiled: October 14, 2005Publication date: August 20, 2009Inventors: Zhiguo Wang, Baofeng Yang
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Publication number: 20090209538Abstract: Herein are described compounds having a structure or a pharmaceutically acceptable salt thereof, wherein Y, A, and B are as described. Methods, compositions, and medicaments related thereto are also disclosed.Type: ApplicationFiled: February 12, 2009Publication date: August 20, 2009Applicant: ALLERGAN, INC.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20090203663Abstract: The present invention relates to compounds that inhibit a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.Type: ApplicationFiled: February 7, 2007Publication date: August 13, 2009Applicant: AstraZeneca ABInventors: Jean Claude Arnould, Benedicte Delouvrie, Jason Grant Kettle
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Patent number: 7569588Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: August 4, 2009Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Viengkham Malathong
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Patent number: 7566729Abstract: Methods are provided for administering pirfenidone to a patient that has exhibited abnormal biomarkers of liver function in response to pirfenidone administration. The methods include administering to a patient pirfenidone at doses lower than the full target dosage for a time period, followed by administering to the patient pirfenidone at the full target dosage.Type: GrantFiled: April 22, 2009Date of Patent: July 28, 2009Assignee: Intermune, Inc.Inventors: Williamson Ziegler Bradford, Javier Szwarcberg
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Patent number: 7560459Abstract: The present invention is directed to novel compounds of the formula (I) wherein X, R1, R2, R3, R4, R5 and R6 are as described in the specification, processes for the preparation of and pharmaceutical compositions comprising said derivatives. The compounds of the present invention are useful for the treatment of epilepsy. The invention is further directed to a process for the preparation of compounds of formula (XX), wherein X, R3, R4, R5 and R6 are as described in the specification.Type: GrantFiled: November 2, 2005Date of Patent: July 14, 2009Assignee: Janssen Pharmaceutica, N.V.Inventors: Ahmed Abdel-Magid, Cynthia Maryanoff, Steven Mehrman, Allen B. Reitz, Bruce Maryanoff
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Patent number: 7560483Abstract: The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.Type: GrantFiled: June 21, 2005Date of Patent: July 14, 2009Assignee: XenoPort, Inc.Inventors: Mark A. Gallop, Jia-Ning Xiang, Fenmei Yao, Laxminarayan Bhat, Cindy X. Zhou
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Publication number: 20090176767Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, r, R1, R2, R3, R4, R5, R6, W and X1 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: March 12, 2009Publication date: July 9, 2009Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Viengkham Malathong