Abstract: The invention provides compositions and methods utilizing a nicotinic receptor modulator, e.g., to reduce or eliminate a side effect associated with dopaminergic agent treatment. In some embodiments, the invention provides compositions and methods utilizing a combination of a dopaminergic agent and a nicotinic receptor modulator that reduces or eliminates a side effect associated with dopaminergic agent treatment.
Type:
Application
Filed:
August 4, 2009
Publication date:
July 1, 2010
Inventors:
Maryka Quik, Donato Di Monte, J. William Langston
Abstract: The present invention relates to novel compounds of formula (I) or a salt thereof: wherein: p is 0, 1, 2, 3, 4 or 5; R1 is independently selected from a group consisting of: halogen, hydroxy, cyano, C1-4alkyl, haloC1-4alkyl, C1-4alkoxy, haloC1-4alkoxy, C1-4alkanoyl and SF5; n is 3 or 4; R2 is hydrogen or C1-4alkyl; n is 2 or 3; X is —CH2—, —O— or —S—; Z may be —CH— or N; A is a group P or P1, wherein P is and P1 is and Y is hydrogen, —OH, C1-4alkyl, haloC1-4alkyl, phenyl or a heteroaromatic group, wherein the phenyl and the heteroaromatic group are optionally substituted by one or two substituents selected from a group consisting of C1-4alkyl, haloC1-4alkyl, C1-4alkoxy and haloC1-4alkoxy; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as modulators of dopamine D3 receptors, e.g. to treat substance related disorders, as antipsychotic agents premature ejaculation or cognition impairment.
Abstract: The invention includes compositions comprising substantially purified pyrroloquinoline quinone, that are useful in methods for the treatment and prevention of cardiac injury caused by hypoxia or ischemia. The invention also includes methods for the treatment and prevention of cardiac injury comprising contacting a composition of the invention with a human patient.
Type:
Application
Filed:
December 22, 2009
Publication date:
June 24, 2010
Applicant:
CLF Medical Technology Acceleration Program, Inc.
Inventors:
Paul J. Davis, Joel S. Karliner, Shaker A. Mousa, George L. Drusano
Abstract: The instant invention provides for compounds that inhibit JAK2 tyrosine kinase and/or PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting JAK2 tyrosine kinase activity and/or PDK1 kinase inhibitory activity by administering the compound to a patient in need of treatment or prevention of myeloproliferative disorders or cancer.
Type:
Application
Filed:
March 10, 2008
Publication date:
June 24, 2010
Inventors:
Tony Siu, Jonathan Young, Micheal Altman, Alan Northrup, Ekaterina Kozina, Christopher Dinsmore, David J. Guerin, Kevin A. Keenan, Joon O. Jung, Solomon Kattar, Rachel N. MacCoss
Abstract: The invention provides compositions and methods utilizing a nicotinic receptor modulator, e.g., to reduce or eliminate a side effect associated with dopaminergic agent treatment. In some embodiments, the invention provides compositions and methods utilizing a combination of a dopaminergic agent and a nicotinic receptor modulator that reduces or eliminates a side effect associated with dopaminergic agent treatment.
Type:
Application
Filed:
August 4, 2009
Publication date:
June 24, 2010
Inventors:
Maryka Quik, Donato Di Monte, J. William Langston
Abstract: The invention provides method for treating Cognitive Dysfunction Syndrome (CCDS), slowing the onset and/or development and/or progression of CCDS or preventing the development of CCDS in canines, such as dogs, using hydrogenated pyrido[4,3-b]indoles, including dimebon.
Abstract: The invention provides methods and combination therapies for treating and/or preventing and/or slowing the onset and/or development of Alzheimer's disease using a hydrogenated pyrido (4,3-b) indole (e.g., dimebon) in conjunction with another compound, pharmaceutically acceptable salt thereof or therapy for Alzheimer's disease.
Abstract: 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:
Application
Filed:
June 26, 2006
Publication date:
June 10, 2010
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
Abstract: The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.
Type:
Application
Filed:
April 13, 2007
Publication date:
June 10, 2010
Applicant:
PRANA BIOTECHNOLOGY LIMITED
Inventors:
Ashley Bush, Colin Louis Masters, Penelope Jane Huggins, Jack Gordon Parsons, Gaik Beng Kok, Vijaya Kenche, Mariana El Sous
Abstract: The present disclosure provides compounds based on the marine alkaloid makaluvamine. Described are compounds of the general formula (I) and (II). Also described are pharmaceutical compositions comprising one or more of the compounds of the general formula (I) and (II). The compounds and pharmaceutical compositions described inhibit the growth of several cancer lines, induce apoptosis and cell cycle arrest, display topoisomerase II inhibitory activity and modulate the activity and/or expression of key proteins involved in the regulation of cell growth. Methods of treatment and prevention using the compounds and pharmaceutical compositions described are also provided.
Type:
Application
Filed:
February 25, 2008
Publication date:
June 10, 2010
Applicant:
THE UAB RESEARCH FOUNDATION
Inventors:
Sadanandan E. Velu, Kevin P. Raisch, Ruiwen Zhang, Wei Wang
Abstract: The embodiments relate to derivatives of 9-alkyl-?-carboline, their production and pharmaceutical compositions containing these 9-alkyl-?-carboline derivatives. Further, the use of 9-alkyl-?-carboline derivatives and pharmaceutical compositions for the treatment and prevention of movement disorders, neurodegenerative diseases, Alzheimer's disease and Parkinson's disease is described. Additionally, these effects can be utilized for the cultivation of cells such as dopaminergic cells or stem cells which shall be engrafted for the treatment of Parkinson's disease.
Abstract: This invention relates to novel tetrahydro-1H-pyrido[4,3-b]indoles, their derivatives and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by NMDA antagonists, acetylcholinesterase inhibitors, 5-HT6 antagonists, other neuroprotectors, antihistamines and agents that delay age-related pathologies and conditions.
Abstract: A variety of diseases and disorders associated with the metabolic pathways involved in the activities of cyclooxygenase and the synthesis of prostaglandins, for example type 2 diabetes mellitus and its sequelae, ischemic vascular diseases, pain associated with inflammation, inflammatory skin conditions, spinal cord injury, peripheral neuropathy, multiple sclerosis, inflammatory bowel disease and rheumatoid arthritis, as well as various types of cancer may be treated or prevented by the use of an agent which selectively enhances production of 15-deoxy-prostaglandin J2.
Abstract: The present invention relates to new adamantane modulators of NMDA receptors and/or 5HT3 receptors, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: The present invention discloses nicotinic desensitizers and methods of selecting, testing, and using them. The present invention provides methods for selecting nicotinic desensitizers from one or more compounds by using receptor, cell, and tissue models; and methods for testing one or more nicotinic desensitizers for their therapeutic utility by using animal models. The present invention also provides compounds of formula (I) and (II) as nicotinic desensitizers. Nicotinic desensitizers of the present invention are useful for the treatment of a wide range of conditions, diseases, and disorders.
Abstract: The present invention relates to compounds having the structure (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.
Type:
Grant
Filed:
September 17, 2004
Date of Patent:
May 25, 2010
Assignee:
Merck Sharp & Dohme
Inventors:
B. Wesley Trotter, Christopher Claiborne, Gerald S. Ponticello, Charles J. McIntyre, Nigel Liverton, David A. Claremon
Abstract: In accordance with the present invention, compounds that inhibit the expression of VEGF post-transcriptionally have been identified, and methods for their use provided. In one aspect of the invention, compounds useful in the inhibition of VEGF production, in the inhibition of angiogenesis, and/or in the treatment of cancer, diabetic retinopathy or exudative macular degeneration are provided. In another aspect of the invention, methods are provided for the inhibition of VEGF production, the inhibition of angiogenesis, and/or the treatment of cancer, diabetic retinopathy or exudative macular degeneration using the compounds of the invention.
Type:
Application
Filed:
July 21, 2009
Publication date:
May 20, 2010
Inventors:
Young-Choon Moon, Liangxian Cao, Nadarajan Tamilarasu, Hongyan Qi, Soongyu Choi, William Joseph Lennox, Donald Thomas Corson, Seongwoo Hwang
Abstract: The present invention relates to new pyridoindole modulators of NMDA receptors, AMPA receptors, and/or L-type calcium channels, and/or inhibitors of acetylcholinesterase, pharmaceutical compositions thereof, and methods of use thereof.
Abstract: The present invention is directed to novel substituted fused aminopiperidines which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DPP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
Type:
Grant
Filed:
November 22, 2005
Date of Patent:
May 18, 2010
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Edmondson, Anthony Mastracchio, Jason M. Cox
Abstract: The invention relates to antagonists of serotonin 5-HT6 receptors simultaneously regulating homeostasis of Ca+2 ions in cells, representing substituted 2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indoles of the general formula 1, pharmaceutically acceptable salts and/or hydrate thereof. In the general formula 1: R1 represents amino group substituent selected from optionally substituted C1-C5 alkyl; R2, is one or more substituents selected from hydrogen, halogen, C1-C3 alkyl, CF3, OCF3; Ar is phenyl optionally substituted with halogen, C1-C6 alkyl, C1-C6 alkoxy, substituted amino group, or CF3; or optionally substituted aromatic 6-membered heterocycle comprising 1-2 nitrogen atoms in the cycle; W represents ethylene group —CH2—CH2—, ethenyl group —CH?CH—, or ethynyl group —C?C—. The invention also relates to the novel compounds selected from the compounds of the general formula 1, methods for their preparation, pharmaceutical compositions and methods of their use.
Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, R5, and R6 and m have the meanings indicated in Claim 1, can be employed, inter alia, for the treatment of tumours.
Type:
Application
Filed:
February 21, 2008
Publication date:
May 13, 2010
Applicant:
MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
Abstract: Compounds are provided for use with kinases that comprise a compound selected from the group consisting of formula (I) wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture in comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
Type:
Application
Filed:
October 8, 2007
Publication date:
May 13, 2010
Inventors:
Jason W. Brown, Qing Dong, Bheema R. Paraselli, Jeffrey A. Stafford, Michael B. Wallace, Hasanthi Wijesekera
Abstract: The present invention provides non-steroidal compounds of formula I which are selective modulators (i.e., agonists and antagonists) of a steroid receptor, specifically, the glucocorticoid receptor. The present invention also provides pharmaceutical compositions containing these compounds and methods for using these compounds to treat animals requiring glucocorticoid receptor agonist or antagonist therapy. Glucocorticoid receptor modulators are useful to the diseases, such as obesity, diabetes, inflammation and others as described below. The present invention also provides intermediates and processes for preparing these compounds.
Type:
Grant
Filed:
October 13, 2006
Date of Patent:
May 11, 2010
Inventors:
Robert L. Dow, Kevin K. Liu, Bradley P. Morgan, Andrew G. Swick
Abstract: Compounds of formulae I, or pharmaceutically acceptable salts thereof: wherein R1, R2 and R3 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
Type:
Application
Filed:
November 5, 2009
Publication date:
May 6, 2010
Applicant:
AMIRA PHARMACEUTICALS, INC.
Inventors:
John Howard Hutchinson, Brian Andrew Stearns, Jill Melissa Scott
Abstract: The invention is directed to naphthalene and quinoline sulfonylurea derivatives as EP4 receptor antagonists useful for the treatment of EP4 mediated diseases or conditions, such as acute and chronic pain, osteoarthritis, rheumatoid arthritis and cancer. Pharmaceutical compositions and methods of use are also included.
Type:
Application
Filed:
March 25, 2008
Publication date:
April 29, 2010
Applicant:
MERCK FROSST CANADA LTD.
Inventors:
Jason Burch, Julie Farand, Yongxin Han, Claudio Sturino
Abstract: The invention provides methods for treating and/or preventing and/or slowing the onset and/or development of ALS using hydrogenated pyrido(4,3-b)indoles, such as dimebon.
Abstract: This invention provides beta-carboline compounds of formula wherein Ring A is a substituted pyridinyl, pyrimidinyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, pyranyl, tetrahydrofuranyl, cyclohexyl, cyclopentyl or thiomorpholinyl ring and R1, R2 and R3 are as described in the specification. The compounds are IKK-2 inhibitors that are useful for treating IKK-2-mediated diseases such as inflammatory diseases and cancer.
Type:
Application
Filed:
December 17, 2009
Publication date:
April 15, 2010
Applicant:
Millennium Pharmaceuticals, Inc.
Inventors:
Michael E. Hepperle, Julie Fields Liu, Francois Soucy, Yingchun Ye, Robert S. Murray, Raman Prakash, Jeremy D. Little, Alfredo Castro, Hormoz Mazdiyasni, Paul E. Fleming, Dominic Reynolds
Abstract: An object of the present invention is to provide a safe and highly effective insulin resistance improving agent or therapeutic agent for type II diabetes. According to the present invention, an insulin resistance improving agent or a therapeutic agent for type II diabetes comprising a compound represented by general formula (I) (wherein R1, R2, and R3 are the same as or different from each other, and each represents lower alkyl, lower alkenyl, lower alkynyl, aralkyl, araryl, phenyl, or a hydrogen atom) or a salt thereof as an active ingredient can be provided.
Type:
Application
Filed:
September 19, 2007
Publication date:
April 15, 2010
Applicants:
KYOWA HAKKO BIO CO., LTD., MITSUBISHI GAS CHEMICAL COMPANY, INC.
Abstract: The present invention provides a method of treating basal cell carcinoma in a subject. Generally, the method includes administering to the subject an amount of IRM compound effective for treating basal cell carcinoma in a treatment cycle that includes at least two consecutive days in which the IRM compound is administered and at least one day in which the IRM compound is not administered.
Type:
Grant
Filed:
January 15, 2008
Date of Patent:
April 13, 2010
Assignee:
Graceway Pharmaceuticals, LLC
Inventors:
Mary L. Owens, Terrance L. Fox, Angela M. Ginkel
Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases, disorders or conditions that would benefit from inhibition of SOC channel activity.
Type:
Application
Filed:
October 5, 2009
Publication date:
April 8, 2010
Applicant:
CALCIMEDICA, INC.
Inventors:
Jeffrey P. Whitten, Yazhong Pei, Kenneth A. Stauderman, Jack Roos
Abstract: Compounds with cancer cell specific lethality are provided. In particular, RAS-selective lethal compounds and compositions are provided. Also provided are methods of screening for such compounds and methods of treating a condition in a mammal, by administering to the mammal a therapeutically effective amount of such compounds or compositions.
Type:
Application
Filed:
August 21, 2009
Publication date:
April 1, 2010
Inventors:
Brent R. Stockwell, Wan Seok Yang, Rohitha SriRamaratnam
Abstract: The present invention provides a method of preparing a 4-(arylmethyl)amino-1H-imidazo(4,5-c)quinoline of formula (4) by reacting an arylmethylamine of formula (3) with a 4-chloro-1H-imidazo(4,5-c)quinoline of formula (2). The present invention further provides a method of preparing an acid addition salt of formula (5) comprising the step of hydrolyzing a 4-(arylmethyl)amino-1H-imidazo(4,5-c)quinoline of formula (4) with a strong acid, HX. The present invention further provides a method of preparing a 4-amino-1H-imidazo(4,5-c)quinoline of formula (1) comprising the step of treating an acid addition salt of formula (5) with a base.
Abstract: The invention relates to the novel therapeutically valuable enantiomer-pure [3a?,8b?]-1,2,3a,4,8b-hexahydropyrrolocyclopentapyridine derivatives of the general formula (I), wherein Z is a single bond or CH2, R1 represents hydrogen or a straight-chain or branched, optionally unsaturated lower alkyl group which may be perfluorated, R2 and R3 independently represent hydrogen, a straight-chain or branched, optionally unsaturated lower alkyl group which may be perfluorated, lower alkoxy, lower alkylthio or halogen, and X and Y alternatively represent CH or N. The invention also relates to the pharmaceutical salts thereof, to a method for their production and to their use.
Type:
Application
Filed:
April 28, 2005
Publication date:
March 25, 2010
Inventors:
Dieter BINDER, Eva BINDER, Michael PYERIN
Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.
Abstract: The present invention provides tricyclic indoles and (4,5-dihydro) indoles of the formula (I) or a pharmaceutically acceptable salt thereof: wherein the ring A represents a fused pyrazole, pyridine or pyrimidine, means either simple or double carbon-carbon bond and R1, R2 and R3 are as defined in the specification. Further objects of the invention are a process for the preparation of the compounds of the formula (I), pharmaceutical compositions comprising them and methods for treating cell proliferative disorders. As a matter of fact, the compounds of the formula (I) are useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, in particular Cdc7 and AKT kinase activity, like cancer.
Type:
Application
Filed:
November 23, 2007
Publication date:
March 25, 2010
Applicant:
NERVIANO MEDICAL SCIENCES S.R.L.
Inventors:
Ermes Vanotti, Marina Caldarelli, Francesco Casuscelli, Barbara Forte, Maria Menichincheri, Alessandra Scolaro, Gabriella Traquandi, Paola Vianello
Abstract: A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: wherein the groups R1, R2, R3, R7 and X are as defined in the specification.
Type:
Application
Filed:
August 28, 2007
Publication date:
March 18, 2010
Inventors:
Laszlo Revesz, Achim Schlapbach, Rudolf Walchli
Abstract: The present invention provides compounds of Formula I (wherein R, R1, R3, R4, X, and ring Y are as defined herein). The present invention also provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.
Type:
Application
Filed:
December 19, 2007
Publication date:
March 18, 2010
Inventors:
Sunil Paliwal, Hon-Chung Tsui, Jose S. Duca, Charles A. Lesburg, Ronald J. Doll, Neng-Yang Shih
Abstract: Novel compounds of formula (I) to (VI), which more particularly include sulfonylurea derivatives, sulfonylthiourea derivatives, sulfonylguanidine derivatives, sulfonylcyanoguanidine derivatives, thioacylsulfonamide derivatives, and acylsulfonamide derivatives which are effective platelet ADP receptor inhibitors. These derivatives may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of cardiovascular diseases, particularly those diseases related to thrombosis. The invention also relates to a method for preventing or treating thrombosis in a mammal comprising the step of administering a therapeutically effective amount of a compound of formulae (I)-(VI), or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
November 23, 2005
Date of Patent:
March 16, 2010
Assignee:
Portola Pharmaceuticals, Inc.
Inventors:
Robert M. Scarborough, Hans-Michael Jantzen, Wolin Huang, David M. Sedlock, Charles Marlowe
Abstract: The present invention provides compounds for use in the preparation of pharmaceutical formulations and medicaments, which alleviate learning and/or mental impairment in people suffering from Down's syndrome.
Abstract: The present invention provides inhibitors of kinases, specifically I?B kinases, JAK1, JAK2, JAK3 and TYK2. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting said kinase activity by administering the compound to a patient in need of treatment for myeloproliferative disorders, cancer or NF-?B-mediated diseases.
Type:
Application
Filed:
November 17, 2006
Publication date:
February 25, 2010
Inventors:
Jean-Francois Truchon, Nicolas Lachance, Cheuk Lau, Yves Leblanc, Christophe Mellon, Patrick Roy, Elise Isabel, Ryan D. Otte, Jonathan R. Young
Abstract: The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is substituted in the 10-position by an alkyl, aryl or aralkyl group. The present invention also relates to a pharmaceutical composition comprises the substituted cytisine compound or the 10-substituted cytisine compound. The invention also relates to a method of modulation a nicotinic ACh receptor in a mammal, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. Another aspect of the present invention relates a method of treating a disease impacted by a nicotinic ACh receptor, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine.
Type:
Application
Filed:
March 29, 2007
Publication date:
February 25, 2010
Applicant:
Georgetown University Office of Technology Commercialization
Inventors:
Alan P. Kozikowski, Werner Tueckmantel, Sheela Chellappan, Kenneth J. Kellar, Yingxian Xiao
Abstract: This invention relates to pharmaceutical compositions comprising a combination of an AMPA/kainate antagonistic compound and an inhibitor of a multidrug resistance protein and its use for combating epileptic disorders.
Type:
Application
Filed:
September 12, 2007
Publication date:
February 18, 2010
Applicant:
NeuroSearch A/S
Inventors:
Pia Weikop, Mette Bjerg Nielsen, Lars Siim Madsen, Claus Mathiesen
Abstract: The present invention relates to compounds of formula I: methods of their use, processes for their preparation and isolated actinomycetes strains capable of preparing pyrrolo[4,3,2-de]quinolin-8-amine compounds.
Type:
Application
Filed:
August 12, 2009
Publication date:
February 18, 2010
Applicant:
Wyeth
Inventors:
Min He, Jeffrey Edwin Janso, Ker Yu, Leonard Alexander McDonald, Laurel Rita Barbieri, Ariamala Gopalsamy