Plural Hetero Atoms In The Polycyclo Ring System Patents (Class 514/321)
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Publication number: 20140275095Abstract: The present invention is directed to compounds of Formula I: wherein X is CR1 or N; Y is CR2 or N; Z is NH or O; R1 is alkoxy, triazolyl, oxazolyl, isoxazolyl, oxadiazolyl, or pyrimidinyl; R2 is H, alkyl, or halo; R3 is H, alkyl, alkoxy, halo, triazolyl, oxazolyl, or pyrimidinyl; R4 is alkyl; R5 is pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl; wherein the pyridyl; benzoxazolyl; pyrimidinyl; pyridazinyl; quinoxalinyl; pyrazinyl; or quinazolinyl is optionally substituted with one or two substituents independently selected from the group consisting of alkyl, halo, or phenyl; and R6 is H or alkyl. Methods of making the compounds of Formula I are also described. The invention also relates to pharmaceutical compositions comprising compounds of Formula I. Methods of using the compounds of the invention are also within the scope of the invention.Type: ApplicationFiled: March 12, 2014Publication date: September 18, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: Curt A. Dvorak, Brock T. Shireman
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Publication number: 20140255517Abstract: In certain embodiments, the disclosure relates to methods of treating or preventing posttraumatic stress disorder comprising administering a pharmaceutical composition comprising effective amount of an angiotensin-converting enzyme inhibitor to a subject in need thereof. In certain embodiments, the angiotensin-converting enzyme inhibitor is administered in combination with an angiotensin receptor blocker.Type: ApplicationFiled: March 5, 2014Publication date: September 11, 2014Applicant: EMORY UNIVERSITYInventors: Kerry J. Ressler, Paul J. Marvar
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Patent number: 8829029Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: GrantFiled: February 21, 2013Date of Patent: September 9, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Patent number: 8829028Abstract: This invention provides the use of a 5-HT4 receptor antagonist in the manufacture of a medicament for treating or preventing heart failure. Particular heart disorders to be treated are selected from the group comprising chronic heart failure, congestive heart failure, chronic congestive heart failure and heart failure resulting from ischaemic heart disease. Methods of treating heart failure using 5-HT4 receptor antagonists and pharmaceutical compositions containing 5-HT4 receptor antagonists are also provided.Type: GrantFiled: February 17, 2009Date of Patent: September 9, 2014Assignee: Serodus ASInventor: Finn Olav Levy
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Publication number: 20140249182Abstract: The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.Type: ApplicationFiled: May 13, 2014Publication date: September 4, 2014Applicant: NOVEN THERAPEUTICS, LLCInventor: Patricia Allison Tewes Richards
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Patent number: 8822498Abstract: The present invention provides a convenient and efficient process for the synthesis of d2-benzo[d][1,3]dioxoles.Type: GrantFiled: September 12, 2008Date of Patent: September 2, 2014Assignee: Concert Pharmaceuticals, Inc.Inventors: Andrew D. Jones, Robert E. Zelle, I. Robert Silverman
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Patent number: 8822476Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: GrantFiled: March 3, 2010Date of Patent: September 2, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle
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Publication number: 20140243370Abstract: Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: ApplicationFiled: August 22, 2012Publication date: August 28, 2014Applicant: MERCK PATENT GmbHInventors: Marianne Donnelly, Hui Qiu, Henry Yu, Lesley Liu-Bujalski, Andreas Goutopoulos
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Patent number: 8815895Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting the cell with a hedgehog antagonist of formula (I) in a sufficient amount to aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity.Type: GrantFiled: March 16, 2012Date of Patent: August 26, 2014Assignees: Curis, Inc., Genentech, Inc.Inventors: Oivin M. Guicherit, Edward Andrew Boyd, Shirley Ann Brunton, Stephen Price, John Harry Alexander Stibbard, Colin H. Mackinnon
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Patent number: 8815909Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: GrantFiled: July 16, 2012Date of Patent: August 26, 2014Assignee: Bristol-Myers Squibb CompanyInventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu, Scott A. Bolton, Laxman Pasunoori, Sunil Kumar Mandal, Philip M. Sher
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Patent number: 8816090Abstract: This invention relates to compounds of the formula (I): wherein A, B, R1, R4, m, and n are each as described herein or a pharmaceutically acceptable salt thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central 10 nervous system disease, Alzheimer's disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.Type: GrantFiled: February 15, 2006Date of Patent: August 26, 2014Assignee: Pfizer Inc.Inventors: Hirohide Noguchi, Isao Sakurada, Chikara Uchida, Nobuaki Waizumi
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Patent number: 8815293Abstract: A depot formulation comprising iloperidone and a biodegradable, biocompatible polymer. Preferably, the polymer is a star polymer.Type: GrantFiled: May 20, 2010Date of Patent: August 26, 2014Assignee: Novartis AGInventors: Markus Ahlheim, Rolf Loeffler
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Publication number: 20140235674Abstract: The present invention relates to a method for treating a patient suffering from a thermoregulatory dysfunction, especially hot flashes and flushes associated with hormonal changes due to naturally occurring menopause (whether male or female) or due to chemically or surgically induced menopause. The method is also applicable to treating the hot flashes, hot flushes, or night sweats associated with disease states that disrupt normal hormonal regulation of body temperature.Type: ApplicationFiled: January 17, 2014Publication date: August 21, 2014Applicant: NOVEN THERAPEUTICS, LLCInventor: Patricia Allison Tewes Richards
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Patent number: 8809331Abstract: Specific Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein m, X, R1, R2, R3, R5, R6 and R7 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.Type: GrantFiled: November 28, 2012Date of Patent: August 19, 2014Assignee: Genentech, Inc.Inventors: Charles Baker-Glenn, Daniel Jon Burdick, Mark Chambers, Bryan K. Chan, Huifen Chen, Anthony Estrada, Janet L. Gunzner-Toste, Daniel Shore, Zachary Kevin Sweeney, Shumei Wang, Guiling Zhao
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Publication number: 20140228377Abstract: A compound represented by formula (IA) or a pharmaceutically acceptable salt thereof, which acts relying on an orexin (OX) receptor antagonistic activity and is useful for the treatment or prevention of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, head ache, migraine, pain, gastrointestinal diseases, epilepsy, inflammations, immune-related diseases, endocrine-related diseases and hypertension.Type: ApplicationFiled: July 4, 2012Publication date: August 14, 2014Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Masahito Abe, Aya Futamura, Ryo Suzuki, Dai Nozawa, Hiroshi Ohta, Yuko Araki
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Publication number: 20140228402Abstract: The invention relates to a combination which comprises fingolimod and at least antidepressant compound.Type: ApplicationFiled: September 7, 2012Publication date: August 14, 2014Applicant: Novartis AGInventors: Matthias Meergans, Ferenc Tracik, Katrin Schuh
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Patent number: 8802664Abstract: The present patent application concerns new ligands of the H4-receptor of formula (I), their process of preparation and their therapeutic use.Type: GrantFiled: September 27, 2011Date of Patent: August 12, 2014Assignee: BioprojectInventors: Isabelle Berrebi-Bertrand, Xavier Billot, Thierry Calmels, Marc Capet, Denis Danvy, Stephane Krief, Olivier Labeeuw, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Philippe Robert, Jean-Charles Schwartz
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Patent number: 8802855Abstract: A method for preparation of iloperidone is provided which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride with 1-[4-(3-chloropropoxyl)-3-methoxyphenyl]ethyl ketone in an inorganic alkaline aqueous solution. A crystallization method of iloperidone is also provided which comprises adding seed crystal to the iloperidone solution in ethyl acetate, and then iloperidone crystal is obtained with high purity by controlling the temperature and the stirring speed.Type: GrantFiled: June 21, 2010Date of Patent: August 12, 2014Assignee: Zhejiang Huahai Pharmaceutical Co., Ltd.Inventors: Shiwei Zhou, Feng Jian
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Publication number: 20140221322Abstract: Certain heteroaryl-substituted piperidinyl and piperazinyl urea compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity, such as anxiety, pain, inflammation, sleep disorders, eating disorders, insulin resistance, diabetes, osteoporosis, and movement disorders (e.g., multiple sclerosis).Type: ApplicationFiled: November 5, 2013Publication date: August 7, 2014Applicant: JANSSEN PHARMACEUTICA NVInventors: J. Guy Breitenbucher, John M. Keith, Mark S. Tichenor, Alison L. Chambers, William M. Jones, Natalie A. Hawryluk, Amy K. Timmons, Jeffrey E. Merit, Mark J. Selerstad
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Publication number: 20140221426Abstract: Presystemic metabolism in intestine of bioactives such as phenylephrine is avoided by administering a subject (human or animal) the bioactive (e.g., phenylephrine) in combination with one or more inhibitors of sulfation (e.g., sulfotransferase enzymes aka SULTs). This can also be enhanced be co-administering inhibitors of monoamine oxidases aka, MAOs, and uridine diphosphate glucoronysl transferases, aka UGTs. Preferably the inhibitors are GRAS compounds. The one or more inhibitor compounds inhibit the enzymes responsible for rapid presystemic metabolism, thus allowing the bioactives (e.g., phenylephrine) to be more readily absorbed intact into the circulatory system.Type: ApplicationFiled: September 27, 2012Publication date: August 7, 2014Inventors: Phillip M. Gerk, William H. Barr, Joseph K. Ritter
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Publication number: 20140213584Abstract: The invention provides compounds for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc.Type: ApplicationFiled: November 8, 2011Publication date: July 31, 2014Applicants: Merck Sharp & Dohme Corp., Alectos Therapeutics Inc.Inventors: Craig A. Coburn, Kun Liu, Ernest J. McEachern, Changwei Mu, Harold G. Selnick, David J. Vocadlo, Yaode Wang, Zhongyong Wei, Yuanxi Zhou
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Publication number: 20140206667Abstract: The invention relates to methods and compositions for treating schizophrenia or bipolar disorder (in particular, mania) by using a combination of a synaptic vesicle protein 2A (SV2A) inhibitor and an antipsychotic or their pharmaceutically acceptable salts, hydrates, solvates, polymorphs thereof. In some embodiments, the methods and the compositions are for treating one or more positive and/or negative symptoms, as well as cognitive impairment, associated with schizophrenia or bipolar disorder (in particular, mania).Type: ApplicationFiled: November 14, 2013Publication date: July 24, 2014Inventor: Michela Gallagher
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Publication number: 20140194459Abstract: Methods and compositions for the treatment of alpha-adrenoceptor mediated conditions.Type: ApplicationFiled: March 5, 2014Publication date: July 10, 2014Applicant: Vanda Pharmaceuticals, Inc.Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt D. Wolfgang
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Patent number: 8772318Abstract: This invention provides compounds that selectively inhibit monoacylglycerol lipase (MAGL). The invention also provides methods of using the MAGL selective inhibitors to stimulate 2-Arachidonoylglycerol (2-AG) mediated endocannabinoid signaling in vivo, and to treat conditions that are associated with or linked to endocannabinoid signaling. The invention additionally provides methods of treating cancer or inhibiting tumor growth by targeting MAGL with MAGL specific inhibitors. The invention further provides methods of screening for MAGL inhibitors with improved biochemical and pharmaceutical properties.Type: GrantFiled: November 10, 2009Date of Patent: July 8, 2014Assignee: The Scripps Research InstituteInventors: Benjamin F. Cravatt, Jonathan Z. Long, Weiwei Li, Daniel K. Nomura
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Publication number: 20140187583Abstract: The present invention relates to novel crystal forms of 4-{[4-({[4-(2,2,2-trifluoroethoxy)-1,2-benzisoxazol-3-yl]oxy}methyl)piperidin-1-yl]methyl}-tetrahydro-2H-pyran-4-carboxylic acid. More particularly, the invention relates to polymorph forms (Polymorph Form I or Polymorph Form II), and to processes for the preparation of, compositions containing and to uses of, such polymorph forms.Type: ApplicationFiled: May 18, 2012Publication date: July 3, 2014Applicant: RAQUALIA PHARMA INC.Inventors: Toyoharu Numata, Hirohide Noguchi, Nobuaki Waizumi, Takashi Kojima
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Publication number: 20140187581Abstract: The present invention relates to novel compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to 5-HT4 receptors.Type: ApplicationFiled: January 5, 2012Publication date: July 3, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Abdul Rasheed Mohammed, Suresh Yarlagadda, Srinivasa Rao Ravella, Anil Karbhari Shinde, Ramasastri Kamphampati, Praveen Kumar Roayapalley, Pradeep Jayarajan, Gopinadh Bhyrapuneni, Sriramachandra Murthy Patnala, Jyothsna Ravula, Venkateswarlu Jasti
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Publication number: 20140187582Abstract: The invention relates to solid dispersions containing paroxetine mesylate. One solid dispersion contains amorphous paroxetine mesylate and a methacrylic acid-methyl methacrylate copolymer, where the weight ratio of paroxetine mesylate to polymer ranges from about 30:70 to about 90:10. Another solid dispersion contains amorphous paroxetine mesylate and a -vinylpyrrolidone/vinylacetate copolymer (PVP-VA), where the weight ratio of paroxetine mesylate to copolymer ranges from about 30:70 to about 50:50. An amorphous solid dispersion of the invention may have a single glass transition temperature. An amorphous solid dispersion is stable for at least 48 hours at 60° C. and 75% relative humidity. A further embodiment of the invention relates to pharmaceutical compositions of paroxetine mesylate comprising a solid dispersion of the invention and at least one pharmaceutically acceptable excipient.Type: ApplicationFiled: March 15, 2013Publication date: July 3, 2014Inventors: David A. ENGERS, Yonglai YANG, Stephan PARENT, Travis HOUSTON, Bruce Charles FRIEDMAN
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Patent number: 8759350Abstract: The pharmaceutical composition of the present invention comprises (1) a carbostyril derivative and (2) a serotonin reuptake inhibitor in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof, which is a dopamine-serotonin system stabilizer. The serotonin reuptake inhibitor may be fluoxetine, duloxetine, venlafaxine, milnacipran, citalopram, fluvoxamine, paroxetine, sertraline or escitalopram. The pharmaceutical composition of the present invention is useful for treating patients with mood disorders, particularly depression or major depressive disorder.Type: GrantFiled: December 25, 2003Date of Patent: June 24, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Tetsuro Kikuchi, Taro Iwamoto, Tsuyoshi Hirose
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Publication number: 20140171442Abstract: Disclosed are alicyclic[c]benzopyrone derivatives and use thereof. The alicyclic[c]benzopyrone derivatives are compounds represented by formula I or their salts. The present compounds not only significantly improve high activity induced by MK-801, but also effectively improve clambering symptom induced by Apomorphine and do not cause EPS within effective dose. These in vitro targets and in vivo pharmacological models are closely related to diseases of the nervous system caused by dopamine dysfunction, especially schizophrenia. Therefore the present compounds can be used for the treatment of central nervous system diseases, especially schizophrenia. ED50 is lower and effect is stronger in two animal models i.e. high activity induced by MK-801 and clambering symptom induced by Apomorphine, while ED50 is higher and therapeutic index is greater in animal models of catalepsy.Type: ApplicationFiled: July 31, 2012Publication date: June 19, 2014Inventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Xin Liu, Song Zhao, Bifeng Liu, Miquan Yu, Yinli Qiu
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Patent number: 8754097Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumors.Type: GrantFiled: August 22, 2012Date of Patent: June 17, 2014Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober
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Publication number: 20140161763Abstract: The methods, kits, and products for controlling a target insect population are disclosed in which a non-host plant containing a toxin and a chemical attractant known to attract the target insect is treated with chemical attractant from a plant of interest. The chemical attractant induces the target insect to lay eggs on the non-host plant. The resulting offspring die of starvation from refusing to feed on the non-host plant. The non-host plant and plant of interest contain at least one common chemical. The methods, kits, and products for controlling a target insect population using an extract from a non-host plant are also disclosed. The non-host plant extract is applied to the plant of interest, and when ingested or applied directly to the target insect, kills the target insect or causes it to develop with deformities.Type: ApplicationFiled: January 28, 2011Publication date: June 12, 2014Applicant: University of the West Indies, a Regional Institution, established by Royal CharterInventors: Trevor Herbert Yee, Charah Tabetha Watson, Eric Garraway, Dwight Robinson, Nemoi Nastassia Sri Garcia Chisholm
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Publication number: 20140148440Abstract: The present invention relates to heterocyclyl compounds of formula (I), and their pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their pharmaceutically acceptable salts. The compounds of formula (I) are useful in the treatment of various disorders that are related to Histamine H3 receptors, for example cognitive disorders, sleep disorders, obesity and pain.Type: ApplicationFiled: November 15, 2010Publication date: May 29, 2014Applicant: SUVEN LIFE SCIENCES LIMITEDInventors: Ramakrishna Nirogi, Anil Karbhari Shinde, Ramasastri Kambhampati, Rambabu Namala, Adi Reddy Dwarampudi, Laxman Kota, Murlimohan Gampa, Padmavathi Kodru, Taraka Naga Vinaykumar Tiriveedhi, Vishwottam Nagaraj Kandikere, Nageshwara Rao Muddana, Ramanatha Shrikantha Saralaya, Pradeep Jayarajan, Dhanalakshmi Shanmuganathan, Ishtiyaque Ahmad, Venkateswarlu Jasti
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Patent number: 8735427Abstract: Grease-like compositions are provided for repelling rodents. The compositions utilize nontoxic mineral, synthetic, or vegetable oil based gels containing silica, clay, urea, polytetrafluoroethylene, or metallic soap thickeners and capsaicin.Type: GrantFiled: April 7, 2011Date of Patent: May 27, 2014Assignee: Pacific Tech Industries, Inc.Inventors: Richard Numata, Ryan Willey
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Patent number: 8735428Abstract: Methods of treating, preventing and/or managing cancer as well as and diseases and disorders associated with, or characterized by, undesired angiogenesis are disclosed. Specific methods encompass the administration of an immunomodulatory compound alone or in combination with a second active ingredient. The invention further relates to methods of reducing or avoiding adverse side effects associated with chemotherapy, radiation therapy, hormonal therapy, biological therapy or immunotherapy which comprise the administration of an immunomodulatory compound. Pharmaceutical compositions, single unit dosage forms, and kits suitable for use in methods of the invention are also disclosed.Type: GrantFiled: March 1, 2013Date of Patent: May 27, 2014Assignee: Celgene CorporationInventor: Jerome B. Zeldis
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Patent number: 8735395Abstract: Compounds of the formula II: wherein R1 and R2 are independently H, F or CH3; or R1 forms an ethynyl bond and R2 is H or C3-C6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF3, OMe or halo; R3 is C1-C3 alkyl or C3-C6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R3 is C3-C6 cycloalkyl it may alternatively be gem substituted with fluoro; R4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A1 is CH or N, A2 is CR6R7 or NR6, provided at least one of A1 and A2 comprises N; R6 is H, C1-C4 alkyl, C1-C4 haloalkyl, C1-C3 alkyl-O—C1-C3 alkyl, or when A2 is C, R6 can also be C1-C4alkoxy or F; R7 is H, C1-C4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoType: GrantFiled: March 14, 2013Date of Patent: May 27, 2014Assignee: Medivir ABInventors: Lourdes Salvador Odén, Magnus Nilsson, Pia Kahnberg, Bertil Samuelsson, Urszula Grabowska
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Patent number: 8729100Abstract: Methods and compositions for the treatment of alpha-adrenoceptor mediated conditions.Type: GrantFiled: December 13, 2008Date of Patent: May 20, 2014Assignee: Vanda Pharmaceuticals, Inc.Inventors: Mihael H. Polymeropoulos, Paolo Baroldi, Curt D. Wolfgang
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Patent number: 8729075Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: GrantFiled: February 7, 2013Date of Patent: May 20, 2014Assignee: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas Natoli
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Publication number: 20140134187Abstract: The present invention relates to the field of autism. More specifically, the present invention provides methods for treating individuals with autism spectrum disorders. The present invention also provides methods for predicting a likelihood of ASD. In one embodiment, a method for treating a female patient having a high risk factor of having children with ASD comprises the steps of (a) identifying in a sample taken from the female patient the presence of AT-1 antibodies; and (b) administering an effective amount of an AT-1 inhibitor or inhibitor of AT-1 antibodies to the female patient.Type: ApplicationFiled: June 25, 2013Publication date: May 15, 2014Inventors: Avindra Nath, Tongguang Wang, Christina Michelle Morris-Berry, Harvey Singer
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Publication number: 20140135308Abstract: Benzoxepin compounds of Formula I, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 23, 2014Publication date: May 15, 2014Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Richard Goldsmith, Robert Heald, Timothy Heffron, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, BinQing Wei
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Publication number: 20140135310Abstract: Sulphonamide derivatives of alicyclic amines of formula (I), wherein A represents naphthyl or 9- or 10-membered bicyclic group, consisting of benzene ring fused with 5- or 6-membered heterocyclic ring; D represents phenyl, naphthyl, 5-membered aromatic heterocyclic group, bicyclic group consisting of a ring selected from benzene and pyridine, fused with aromatic or non-aromatic 5-membered heterocyclic ring; p, r independently represent 0 or 1; x, z independently represent 1 or 2; n is 2 or 3; and enancjomers, pharmaceutically acceptable salts and solvates thereof. The compounds may be useful for the treatment and/or prevention of the central nervous system disorders.Type: ApplicationFiled: June 29, 2012Publication date: May 15, 2014Applicant: Adamed Sp. z o.o.Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Maciej Pawlowski, Andrzej Krukowski, Rafal Rusiecki, Agata Magdalena Siwek, Malgorzata Anna Wolak
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Publication number: 20140135305Abstract: The present invention provides nucleic acid constructs, methods for identifying and validating compounds that increase the inclusion of exon 7 of SMN2 into mRNA transcribed from the SMN2 gene, compounds and pharmaceutical compositions that increase levels of SMN protein produced from the SMN2 gene, and methods for use thereof in treating of SMA.Type: ApplicationFiled: December 12, 2013Publication date: May 15, 2014Applicant: PTC THERAPEUTICS, INC.Inventors: Sergey V. Paushkin, Charles Romfo, Ellen Welch, Nikolai Naryshkin
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Publication number: 20140128433Abstract: The present invention relates to methods for the identification of genetic polymorphisms that may be associated with a risk for QT prolongation after treatment with iloperidone and related methods of administering iloperidone to patients with such polymorphisms.Type: ApplicationFiled: January 8, 2014Publication date: May 8, 2014Applicant: Vanda Pharmaceuticals, Inc.Inventors: Curt Wolfgang, Mihael Polymeropoulos
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Publication number: 20140121210Abstract: Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor.Type: ApplicationFiled: January 8, 2014Publication date: May 1, 2014Applicant: HELSINN HEALTHCARE SAInventors: Silvina GARCIA RUBIO, Claudio PIETRA, Claudio GIULIANO, Zhigang LI
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Publication number: 20140121242Abstract: The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed.Type: ApplicationFiled: June 26, 2012Publication date: May 1, 2014Applicant: TASLY PHARMACEUTICAL GROUP CO., LTD.Inventors: Xiaohui Ma, Yuanpeng Jin, Min Han, Shuiping Zhou, Wangyi Zhou, Xuejun Luo, Guocheng Wang, Lulu Yan, Lanlan Zhang, Yonghong Zhu
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Publication number: 20140113911Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a benzopyrone derivative and a use thereof. The benzopyrone derivative is compound having a structure of formula (I) or a pharmaceutically acceptable salt thereof. It has been found by experiments that, this type of compounds is useful in prevention or treatment of neuropsychical diseases.Type: ApplicationFiled: April 6, 2012Publication date: April 24, 2014Applicant: NHWA PHARMA CORPORATIONInventors: Guisen Zhang, Yin Chen, Xiangqing Xu, Bifeng Liu, Xin Liu, Song Zhao, Shicheng Liu, Minquan Yu, Heng Zhang, Xinghua Liu
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Patent number: 8697723Abstract: Compounds of formula I wherein X, Z, R1-R4, and m are as defined in the claims, exhibit alpha2C antagonistic activity, and are thus useful as alpha2C antagonists. Methods for the treatment of diseases and conditions of the peripheric system and the central nervous system are also disclosed.Type: GrantFiled: June 14, 2013Date of Patent: April 15, 2014Assignee: Orion CorporationInventors: David Din Belle, Patrik Holm, Arto Karljalainen, Arto Tolvanen, Gerd Wohlfahrt, Petteri Rummakko
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Publication number: 20140100248Abstract: The present invention relates to new heterocyclic compounds as modulators of sphingolipid signaling and uses thereof of as pharmaceutically active agents, suitable for treating proliferative, degenerative, infectious, and other diseases.Type: ApplicationFiled: April 2, 2012Publication date: April 10, 2014Applicants: UNIVERSITÄT BERN, JOHANN WOLFGANG GOETHE-UNIVERSITÄTInventors: Holger Stark, Aleksandra Zivkovic, Andrea Huwiler, Josef Pfeilschifter
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Publication number: 20140094493Abstract: A compound of Formula (I), and its pharmaceutically acceptable salt or salts and physiologically hydrolysable derivatives in free form or salt form: wherein R1 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alkyl, C1-4alkoxy, CONH2 (optionally mono- or di-substituted by C1-4alkyl) and SO2NH2, R2 is independently selected from C1-6allkyl substituted by R3 wherein the C1-6alkyl chain optionally comprises one or two heteroatoms select from O; R3 is selected from aryl, C3-6cycloalkyl, C3-6heterocyclyl and C3-6heteroaryl, wherein the heterocyclyl and heteroaryl rings are nitrogen containing; and wherein R3 is optonally substituted by one or more groups selected from R1; n1 is zero or an integer from 1 to 2; n2 is an integer from 1 to 2; and the sum of n1 and 2 is less than or equal to 2; R5 is selected from any group defined for R1 and R2; R6a and R6b are independently selected from H or C1-4alkyl; R7 is independently selected from F, Cl, Br, CN, NH2, OH, CHO, COOH, oxo, C1-4alType: ApplicationFiled: February 6, 2012Publication date: April 3, 2014Inventors: Jillian G. Baker, Peter M. Fischer, Christophe Fromont, Sheila M. Gardiner, Stephen J. Hill, Gopal Jadhav, Barrie Kellam, Shailesh Mistry, Jeanette Woolard
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Patent number: 8686021Abstract: Use of a benzoyl derivative of 3-aminocarbazole to produce a drug for the preventive or therapeutic treatment of a disorder selected form the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis. Method for the preventive or therapeutic treatment of a disorder selected from the group comprising inflammatory processes, pain, fever, tumors, Alzheimer's disease and atherosclerosis in which a therapeutically effective quantity of a benzoyl derivative of 3-aminocarbazole according to the invention is administered to an individual.Type: GrantFiled: May 3, 2006Date of Patent: April 1, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Lorenzo Polenzani, Giorgina Mangano, Isabella Coletta, Maria Alessandra Alisi, Nicola Cazzolla, Guido Furlotti, Caterina Maugeri
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Patent number: 8686028Abstract: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substitutedType: GrantFiled: May 14, 2009Date of Patent: April 1, 2014Assignee: Council of Scientific & Industrial ResearchInventors: Atul Goel, Amit Kumar, Sumit Chaurasia, Divya Singh, Abnish Kumar Gautam, Rashmi Pandey, Ritu Trivedi, Man Mohan Singh, Naibedya Chattopadhyay, Lakshmi Manickavasagam, Girish Kumar Jain, Anil Kumar Dwivedi