Tricyclo Ring System Having The Five-membered Hetero Ring As One Of The Cyclos Patents (Class 514/411)
-
Patent number: 8314243Abstract: A process is described for catalytically preparing optionally substituted aromatic or heteroaromatic nitrites of the general formula (I) Ar—CN??(I) by reacting the corresponding aryl halides of the general formula (II) Ar—X??(II) in which X is chlorine, bromine, iodine, triflate, nonaflate, mesylate or tosylate and Ar is an optionally substituted aromatic or heteroaromatic radical, characterized in that the reaction is performed in the presence of a palladium compound, a phosphine of the general formula (III) or (IV) where R is an alkyl radical and R?, R? and R?? are each an alkyl radical or an aryl radical or heteroaryl radical and A is an alkylene or arylene radical, and potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III), optionally in a solvent and optionally with addition of a base.Type: GrantFiled: November 21, 2007Date of Patent: November 20, 2012Assignee: Saltigo GmbHInventors: Nikolaus Müller, Wolfgang Mägerlein, Alain Cotté, Matthias Beller, Thomas Schareina, Alexander Zapf
-
Publication number: 20120289470Abstract: The invention includes compositions for transmucosal administration to an animal comprising at least one active agent and a pharmaceutically acceptable carrier. A preferred active agent is selected from the group consisting of meloxicam, carprofen, enrofloxacin, clemastine, diphenhydramine, digoxin, levothyroxine, cyclosporine, ondansetron, lysine, zolpidem, propofol, nitenpyram, ivermectin, milbemycin, and pharmaceutically acceptable salts, solvates and esters thereof. In another embodiment, the invention includes methods of treating or preventing a condition in an animal comprising transmucosally administering a composition comprising a therapeutically or prophylactically effective amount of an active agent and a pharmaceutically acceptable carrier.Type: ApplicationFiled: December 15, 2011Publication date: November 15, 2012Inventors: Mark C. HEIT, Antonio M. BENITZ, Dennis F. STEADMAN, David M. PETRICK
-
Publication number: 20120277186Abstract: This application relates to tricyclic compounds of Formula I: including all stereoisomeric forms, all mixtures of stereoisomeric forms, and salts of these compounds. This application also relates to compositions comprising compounds of Formula I, stereoisomeric forms, all mixtures of stereoisomeric forms, and salts thereof and uses therefor.Type: ApplicationFiled: June 21, 2012Publication date: November 1, 2012Applicant: Cephalon, Inc.Inventors: Shawn P. Allwein, George C. Morton, Gerard C. Rosse, Yi Wang
-
Patent number: 8298581Abstract: A controlled release pharmaceutical composition for oral use is provided in the form of a coated matrix composition, the matrix composition comprising i) a mixture of a first and a second polymer that have plasticizing properties and which have melting points or melting intervals of a temperature of at the most 200° C.Type: GrantFiled: March 26, 2004Date of Patent: October 30, 2012Assignee: Egalet A/SInventors: Gina Fischer, Daniel Bar-Shalom, Lillian Slot, Anne-Marie Lademann
-
Publication number: 20120270876Abstract: Methods are provided for treating a subject for a condition caused by an abnormality in the subject's autonomic nervous system. In accordance with the subject methods, at least a portion of a subject's autonomic nervous system is pharmacologically modulated with at least one beta-blocker in a manner that is effective to treat the subject for the condition. The subject methods find use in the treatment of a variety of different conditions, where such conditions include various disease conditions. Also provided are systems and kits for use in practicing the subject methods.Type: ApplicationFiled: April 24, 2012Publication date: October 25, 2012Inventors: Anthony Joonkyoo Yun, Patrick Yuarn-Bor Lee
-
Publication number: 20120270881Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y1, as modulators of the serotonin receptor of subtype 5-HT2B, as blockers of the voltage-gated potassium channel Kv1.3 and as inhibitors of the ?-catenin-dependent “canonical” Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.Type: ApplicationFiled: August 3, 2010Publication date: October 25, 2012Applicant: POLYPHOR AGInventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
-
Publication number: 20120270878Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases and proteolytic enzyme mediated diseases, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: July 2, 2012Publication date: October 25, 2012Applicant: BAYER HEALTHERCARE LLCInventors: Scott MILLER, Martin OSTERHOUT, Jacques DUMAS, Uday KHIRE, Timothy B. LOWINGER, William J. SCOTT, Roger A. SMITH, Jill E. WOOD, David E. GUNN, Holia HATOUM-MOKDAD, Marell RODRIGUEZ, Robert SIBLEY, Ming WANG, Tiffany TURNER, Catherine BRENNAN
-
Publication number: 20120264765Abstract: The present invention relates to the identification of provided cyclohexane-1,3-diones (CHD compounds) and pharmaceutical compositions thereof for treating subjects with amyotrophic lateral sclerosis (ALS) and other neurodegenerative diseases. The invention also provides methods of preparing the provided CHD compounds.Type: ApplicationFiled: October 29, 2010Publication date: October 18, 2012Applicants: Cambria Pharmaceuticals, Inc., Northwestern UniversityInventors: Donald R. Kirsch, Radhia Benmohamed, Anthony C. Arvanties, Richard I. Morimoto, Wei Zhang, Richard B. Silverman
-
Publication number: 20120264703Abstract: The present invention provides novel methods and formulations for treating anxiety disorders, including Post Traumatic Stress Disorder, in human subjects employing coordinate treatment using ? and ? blockers alone or in combination with additional psychotherapeutic medications to treat the anxiety disorder and reduce symptomology in treated subjects.Type: ApplicationFiled: June 15, 2012Publication date: October 18, 2012Inventors: Arifulla Khan, John Frederick Reinhard, JR.
-
Publication number: 20120264771Abstract: Provided is a method of inhibiting growth of androgen receptor positive cancer cells. The method entails administering to an individual diagnosed with or suspected of having an androgen receptor positive cancer and administering to the individual a composition containing a compound that can inhibit the growth of the androgen receptor positive cancer.Type: ApplicationFiled: October 25, 2010Publication date: October 18, 2012Applicants: PANACELA LABS, INC., HEALTH RESEARCH INC.Inventors: Katerina Gurova, Natalya Narizhneva
-
Patent number: 8288430Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.Type: GrantFiled: March 25, 2009Date of Patent: October 16, 2012Assignee: Grunenthal GmbHInventors: Saskia Zemolka, Stefan Schunk, Klaus Linz, Wolfgang Schröder, Werner Englberger, Fritz Theil, Birgit Roloff
-
Patent number: 8288399Abstract: Method for treating Alzheimer's disease, Parkinson's disease, Huntington's chorea or Pick's disease by administering to a patient a compound of formula (I) wherein R1 represents hydrogen; R2 represents hydrogen, a C1-C6 alkyl group or C3-C6 cycloalkyl group; A represents nitrogen; D represents a methylene group, a methyl methylene group, a halogen atom substituted methylene group or a halogen substituted methyl methylene group; E represents CH2, CHR3 wherein R3 represents a C1-C6 alkyl group, CH or a carbon atom substituted by a C1-C6 alkyl group; Arom represents aryl, aryl having from 1 to 3 identical or different substituent groups selected from halogen, C1-C6 alkyl, and C1-C6 alkyloxy, heteroaryl or heteroaryl having from 1 to 3 substituent groups, selected from halogen, C1-C6 alkyl and C1-C6 alkyloxy. The part represented by is a single bond or double bond.Type: GrantFiled: August 12, 2008Date of Patent: October 16, 2012Assignee: BTG International LimitedInventors: Tomiichiro Oda, Shigeko Uryu, Shinya Tokuhiro
-
Publication number: 20120252859Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicant: ATHERSYS, INC.Inventors: Youssef L. Bennani, Bayard Huck, Michael J. Robarge
-
Publication number: 20120252740Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.Type: ApplicationFiled: July 2, 2010Publication date: October 4, 2012Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
-
Publication number: 20120252796Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: September 29, 2010Publication date: October 4, 2012Inventors: Harikishore Pingali, V.V.M. Sairam Kalapatapu, Pankaj Makadia, Mukul R. Jain
-
Publication number: 20120245212Abstract: A controlled release carvedilol formulation for less frequent, preferably once daily administration is described. The controlled release formulation comprises a therapeutically effective amount of carvedilol or a pharmaceutically acceptable salt thereof, a matrix forming polymer, a solubility enhancer and a pharmaceutically acceptable carrier. In one embodiment, a controlled release formulation having a therapeutically effective amount of carvedilol is contained in two or more subunits having different release profiles. The controlled release formulation is usable in the treatment and/or prophylaxis of one or more conditions such as cardiovascular disorders.Type: ApplicationFiled: September 29, 2010Publication date: September 27, 2012Applicants: INNOPHARMAX, INC., TSH BIOPHARM CORPORATION LTD.Inventors: Wei-Hua Hao, Tsung-Hsin Lin, Ta-Chien Lu
-
Publication number: 20120238533Abstract: The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.Type: ApplicationFiled: September 3, 2010Publication date: September 20, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Arwed Cleve, Ulrich Lücking, Stefan Bäurle, Martin Fritsch, Jens Schröder, Bernd-Wolfgang Igl
-
Publication number: 20120232063Abstract: The present invention relates to methods of treating a subject with malaria comprising administering a 2-aminoindole compound represented by Formula: (I)—The values and preferred values of the variables in Structural Formula I are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: September 13, 2012Inventors: Ralph Mazitschek, Jon C. Clardy, Dyann Wirth, Roger Wiegand, Sameer Urgaonkar, Mary Lynn Baniecki, Joseph Cortese, Cassandra Celatka, Yibin Xiang, Renato Skerlj, Elyse M.J. Bourque
-
Publication number: 20120232122Abstract: The present invention relates to a tricyclic heterocyclic derivative according to Formula (I), wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to pharmaceutical compositions comprising said tricyclic heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of serotonin mediated disorders, such as obesity.Type: ApplicationFiled: March 9, 2010Publication date: September 13, 2012Inventors: Keneth Davies, Takao Kiyoi, Ashvinkumar Dhirubhai Mistry, Peter Christopher Ray, Mark Reid, Grant Wishart
-
Patent number: 8263640Abstract: The present disclosure describes inhibitors of fatty acid uptake and methods of using such inhibitors. Specifically, the present disclosure describes inhibitors with specificity for FATP2.Type: GrantFiled: June 1, 2010Date of Patent: September 11, 2012Assignee: NUtech VenturesInventors: Concetta Dirusso, Paul Black
-
Publication number: 20120225922Abstract: The invention includes an amount of (3aR)-1,3a,8-trimethyl-1,2,3,3a,8,8a-hexahydropyrrolo[2,3-b]indol-5-yl phenylcarbamate for administering to a subject and also a method of preventing or treating neurotoxicity or neurodegenerative processes in a subject in need thereof using the amount thereof.Type: ApplicationFiled: March 4, 2011Publication date: September 6, 2012Inventor: Maria Maccecchini
-
Publication number: 20120225873Abstract: The invention provides novel compounds useful for the treatment of neurodegenerative disorders including Alzheimer's disease and dementia. The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: April 13, 2012Publication date: September 6, 2012Applicant: Myrexis, Inc.Inventors: Rachel Slade, Yevgeniya Klimova, Robert J. Halter, Ashantai J. Yungai, Warren S. Weiner, Ruth J. Walton, Jon Adam Willardsen, Mark B. Anderson, Kenton Zavitz
-
Publication number: 20120225923Abstract: The present invention relates to novel dithiinetetra(thio)carboximides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.Type: ApplicationFiled: September 3, 2011Publication date: September 6, 2012Applicant: Bayer CropScience AGInventors: Thomas Himmler, Thomas Seitz, Ulrike Wachendorff-Neumann
-
Publication number: 20120225845Abstract: The invention provides novel compounds useful for the treatment of disorders associated with a defect in vesicular transport (e.g., axonal transport). The compounds have a substituents chosen from -L-C(?O)OH, -L-CH?CHC(?O)OH, -L-C(?O)NH2, -L-C(?O)NH(C1-3 alkyl), -L-C(?O)N(C1-3 alkyl)2, -L-S(?O)2(C1-3alkyl), -L-S(?O)2NH2, -L-S(?O)2N(C1-3 alkyl)2, -L-S(?O)2NH(C1-3 alkyl), -L-C(?O)NHOH, -L-C(?O)CH2NH2, -L-C(?O)CH2OH, -L-C(?O)CH2SH, -L-C(?O)NHCN, -L-NHC(?O)ORo, -L-C(?O)NHRo, -L-NH(C?O)NHRo, -L-C(?O)N(Ro)2, -L-NH(C?O)N(Ro)2, -L-sulfo, -L-(2,6 difluorophenol), -L-phosphono, and -L-tetrazolyl, where L is a linker.Type: ApplicationFiled: May 4, 2012Publication date: September 6, 2012Applicant: Myrexis, Inc.Inventors: Christine Klein, Andrew D. Gassman, Leena Bhoite, John Manfredi
-
Patent number: 8258172Abstract: The present invention provides compounds and methods of administering compounds to a subject that can reduce ?APP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce ?APP production and that is not toxic in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease ?APP production.Type: GrantFiled: July 22, 2010Date of Patent: September 4, 2012Assignees: Raptor Pharmaceutical Corp, National Institutes of Health (NIH)Inventors: Nigel H. Greig, Karen T. Y. Shaw, Qiang-Sheng Yu, Harold W. Holloway, Tada Utsuki, Timothy T. Soncrant, Donald K. Ingram, Arnold Brossi, Anthony Giordano, Gordon Powers, Diane M. Davidson, Michael Sturgess
-
Patent number: 8258171Abstract: A compound represented by the following general formula (I): wherein R1 represents an amino group which may be substituted with one or two alkyl groups; R2, R3, R4 and R5 independently represent an alkyl group; and R6 and R7 independently represent a monocarboxyalkyl group, a salt thereof, or an ester thereof, which is useful as a pH-sensitive fluorescent probe which emits intense fluorescence in an acidic region.Type: GrantFiled: November 15, 2007Date of Patent: September 4, 2012Assignee: The University of TokyoInventors: Tetsuo Nagano, Yasuteru Urano, Daisuke Asanuma
-
Patent number: 8252833Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1 R2 R3, R4, R5, R6, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: GrantFiled: February 1, 2007Date of Patent: August 28, 2012Assignee: Glaxo Group LimitedInventors: Andrew Billinton, Nicholas Maughan Clayton, Gerard Martin Paul Giblin, Mark Patrick Healy
-
Patent number: 8247441Abstract: The invention relates to compounds of formula (I): wherein R1 and R2 together form the following carbon-containing chain: wherein: R3 represents a hydrogen atom or an alkyl group, R4 represents a hydrogen atom or an alkyl, aryl, heteroaryl, 3,4-dioxocyclobutenyl, alkylcarbonyl, cycloalkylcarbonyl, heterocycloalkylcarbonyl, benzoyl, arylsulphonyl or heteroarylsulphonyl group, each of those groups optionally being substituted, or R3 and R4 together with the nitrogen atom carrying them form a 5- to 8-membered ring, the ring thereby formed optionally being substituted. Medicinal products containing the same which are useful in treating conditions requiring a D3 receptor antagonist.Type: GrantFiled: July 20, 2010Date of Patent: August 21, 2012Assignee: Les Laboratoires ServierInventors: Guillaume De Nanteuil, Bernard Cimetiere, Anne Dekeyne, Mark Millan
-
Publication number: 20120202821Abstract: Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.Type: ApplicationFiled: August 5, 2009Publication date: August 9, 2012Applicant: POLYPHOR AGInventors: Daniel Obrecht, Philipp Ermert, Said Oumouch, Franck Lach, Anatol Luther, Karsten Marx, Kerstin Möhle
-
Publication number: 20120202868Abstract: The present invention relates to a method for the treatment of bronchial asthma and chronic obstructive pulmonary disease (COPD) comprising administering to the patient suffering from asthama and COPD an effective dose of carbazole derivatives or salt thereof, optionally along with pharmaceutically acceptable excipients. Structural formula of the compounds of general formula 1 useful as phosphodiesterase-4 (PDE-4) enzyme inhibitors, inhibitor for signalling molecule for the treatment of asthma and asthma related diseases is given below: wherein R1=H or OCH3; R2?CH3 or CHO; R3?H or OCH3; R4?H or OCH3 Herbal route for the isolation of compound of general formula 1 from the bark of plant Murraya Koenigii and chemical route for the preparation of such compounds from basic compounds such as vanillin is also reported.Type: ApplicationFiled: February 3, 2012Publication date: August 9, 2012Applicant: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Sibabrata MUKHOPADHYAY, Mumu CHAKRABORTY, Tulika MUKHERJEE, Arun BANDYOPADHYAY, Dipak KAR, Tanima BANERJEE, Aditya KONAR, Debaprasad JANA, Siddhartha ROY, Santu BANDYOPADHYAY, Balram GHOSH, Mabalirajan ULAGANATHAN, Rakesh Kamal JOHRI, Subhash Chander SHARMA, Gurdarshan SINGH, Bholanath PAUL, Vasanta Madhava Sharma GANGAVARAM, Jhillu Singh YADAV, Radha Krishna PALAKODETY
-
Publication number: 20120196819Abstract: Compositions and methods for the treatment and control of various conditions in an animal which comprises administering to said animal an effective amount of a immediate release composition of about 0.5% to 50% wt/wt of active ingredient together with excipients to a total of about 100%, wherein said compositon dissolves in a relatively short period of time, e.g., 75 seconds or less, 5 seconds or less, or 3 seconds or less, upon administration to said animal.Type: ApplicationFiled: January 4, 2012Publication date: August 2, 2012Applicant: NEWMARKET PHARMACEUTICALS LLCInventors: David ROCK, Mark RIDALL
-
Publication number: 20120196889Abstract: The present invention relates to novel catecholamine derivatives of Formula I, to processes for their preparation, pharmaceutical compositions containing them and to their use in therapy.Type: ApplicationFiled: February 24, 2010Publication date: August 2, 2012Applicant: H. Lundbeck A/SInventors: Benny Bang-Andersen, Mogens Larsen, Klaus Gundertofte, Morten Jorgensen, Jennifer Larsen, Niels Mork, HåKan Wikström
-
Patent number: 8232312Abstract: The present invention relates to substituted arylsulphonylglycines of general formula (I) wherein R, X, Y and Z 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: GrantFiled: March 14, 2008Date of Patent: July 31, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Holger Wagner, Elke Langkopf, Matthias Eckhardt, Ruediger Streicher, Corinna Schoelch, Annette Schuler-Metz, Alexander Pautsch
-
Patent number: 8232311Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are tricyclic indeno-pyrrole compounds. These compounds are serotonin receptor (5-HT) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT) is desired (e.g. anxiety, depression and obesity).Type: GrantFiled: March 25, 2011Date of Patent: July 31, 2012Assignee: Athersys, Inc.Inventors: Youssef L. Bennani, Bayard Huck, Michael J. Robarge
-
Patent number: 8227501Abstract: The invention provides new compounds of formula (I) wherein R1, R2, R3, R4, and X have different meanings. Preparative processes, pharmaceutical compositions, and uses thereof in the treatment or prevention of conditions mediated by melatonin receptors are also provided.Type: GrantFiled: July 29, 2009Date of Patent: July 24, 2012Assignee: Ferrer Internacional, S.A.Inventors: José L. Falcó, Albert Palomer, Antonio Guglietta
-
Publication number: 20120184493Abstract: Described herein are topical formulations for use in the treatment or prevention of dermatological diseases, disorders, or conditions in a mammal.Type: ApplicationFiled: July 28, 2010Publication date: July 19, 2012Applicant: PANMIRA PHARMACEEUTICALS, LLCInventor: John Howard Hutchinson
-
Publication number: 20120184496Abstract: Described herein are ophthalmic pharmaceutical compositions, wherein the ophthalmic pharmaceutical compositions are in a form suitable for administration to an eye of a mammal. Ophthalmic pharmaceutical compositions disclosed herein include at least one DP2 receptor antagonist compound and are used to treat or prevent ophthalmic diseases or conditions.Type: ApplicationFiled: July 28, 2010Publication date: July 19, 2012Applicant: PANMIRA PHARMACEUTICALS, LLCInventors: John Howard Hutchinson, Thomas Jon Seiders, Nicholas Simon Stock
-
Patent number: 8222425Abstract: The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of human diseases.Type: GrantFiled: July 19, 2011Date of Patent: July 17, 2012Assignee: Novartis AGInventors: Shawn D. Britt, Lech Andrzej Ciszewski, Jiping Fu, Subramanian Karur, Yugang Liu, Peichao Lu, David Thomas Parker, Mahavir Prashad, Prakash Raman, Pascal Rigollier, Mohindra Seepersaud, Aregahegn Yifru, Rui Zheng
-
Publication number: 20120178750Abstract: The present invention encompasses compounds of Formula I: as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: March 19, 2012Publication date: July 12, 2012Applicant: Merck Sharp & Dohme Corp.Inventors: Subharekha Raghavan, Steven L. Colletti, Fa-Xiang Ding, Hong Shen, James R. Tata, Ashley Rouse Lins, Abigail Lee Smenton, Weichun Chen, Darby Rye Schmidt, George Scott Tria
-
Publication number: 20120178757Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.Type: ApplicationFiled: December 8, 2011Publication date: July 12, 2012Applicant: NOTTINGHAM UNIVERSITY HOSPITALS NHS TRUSTInventor: Desmond George Powe
-
Publication number: 20120172408Abstract: The present invention relates to an active ingredient including indocyanine green and/or infracyanine green for use in treating dental or periodontal infectious diseases under irradiation with light, more particularly laser light, from a wavelength range between 790 nm and 830 nm.Type: ApplicationFiled: July 12, 2011Publication date: July 5, 2012Applicant: A.R.C. LASER GMBHInventor: Reinhardt Thyzel
-
Publication number: 20120172402Abstract: Substituted tricyclic diproline analogues of the formula (I): wherein the variables are as defined herein. Also disclosed are methods for the production thereof, the use thereof for the induction of an alpha-helix conformation in peptides and/or proteins, pharmaceuticals containing said compounds, methods for the production of a peptide library containing said compounds, and peptide libraries containing said compounds.Type: ApplicationFiled: July 9, 2010Publication date: July 5, 2012Applicants: FORSCHUNGSVERBUND BERLIN E.V., UNIVERSITAT ZU KOLNInventors: Hans-Günther Schmalz, Ronald Kuhne, Verena Hack, Cédric Reuter
-
Publication number: 20120171262Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.Type: ApplicationFiled: March 15, 2012Publication date: July 5, 2012Inventors: Tzuchi R. Ju, Claudia M. Davila, Yi Gao, Linda E. Gustavson, David LeBlond, Tong Zhu
-
Patent number: 8207213Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, X and Y are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.Type: GrantFiled: February 1, 2007Date of Patent: June 26, 2012Assignee: Glaxo Group LimitedInventors: Mark Patrick Healy, Gerard Martin Paul Giblin, Helen Susanne Price
-
Patent number: 8207216Abstract: Compounds of formula: and pharmaceutically acceptable salts, esters and solvates thereof, where variables are defined in the specification, useful generally as inhibitors of protein kinases and particularly useful for inhibition of GSK-3. Pharmaceutically compositions and medicaments containing a compound of the invention are provided. The invention provides methods of treatment of protein kinase-related disease, disorders or conditions. The invention provides methods of treatment of GSK-3-related diseases, disorders or conditions.Type: GrantFiled: June 19, 2009Date of Patent: June 26, 2012Assignee: The Board of Trustees of the University of IllinoisInventors: Alan P. Kozikowski, Irina Gaysina
-
Patent number: 8207214Abstract: A method for treating an inflammatory process selected from the group consisting of oedema, erythema, articular inflammation, rheumatoid arthritis, arthrosis, a colorectal tumor, a pulmonary carcinoma, an adenocarcinoma, and combinations thereof, in a person in need thereof, the method comprising administering to the person in need thereof, in an amount sufficient to treat the inflammatory process, a 3-aminocarbazole or a salt thereof.Type: GrantFiled: October 28, 2010Date of Patent: June 26, 2012Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Maria Alessandra Alisi, Patrizia Dragone, Guido Furlotti, Nicola Cazzolla, Vincenzo Russo, Giorgina Mangano, Isabella Coletta, Lorenzo Polenzani
-
Publication number: 20120149716Abstract: Methods of treating, preventing, and managing tuberculosis and other related disorders are disclosed. The methods comprise the administration of a PDE4 modulator, or a pharmaceutically acceptable salt, solvate, hydrate, clathrate, stereoisomer, or prodrug thereof, optionally in combination with a second active agent and/or other conventional therapies. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in such methods are also disclosed.Type: ApplicationFiled: February 9, 2010Publication date: June 14, 2012Inventor: Jerome B. Zeldis
-
Publication number: 20120148689Abstract: The present invention is related to the composition and methods of manufacture of orally-dissolvable, edible films as a vehicle for the non-invasive administration of active drugs through the mucosal tissues of the oral cavity. The films include a water soluble film-forming polymer such as pullulan. Methods for producing the films are also disclosed.Type: ApplicationFiled: February 17, 2012Publication date: June 14, 2012Inventor: Todd Maibach
-
Patent number: 8198313Abstract: This invention is directed to indolone derivatives which are antagonists for the GALR3 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: January 10, 2011Date of Patent: June 12, 2012Assignee: H. Lundbeck A/SInventors: Michael Konkel, John M. Werzel, Jamie Talisman
-
Publication number: 20120135996Abstract: Disclosed is a cytoprotective agent for use with respect to ischemic damage, including as an active ingredient a triprenyl phenol compound represented by the following general formula (I), wherein X is —CHY—C(CH3)2Z, Y and Z are each independently —H or —OH, or jointly form a single bond, and R represents a hydrogen atom or a substituent with a molecular weight of 1000 or less.Type: ApplicationFiled: February 5, 2010Publication date: May 31, 2012Inventors: Kazuo Honda, Terumasa Hashimoto, Keita Shibata, Keiko Hasegawa, Keiji Hasumi