Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
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Patent number: 9012644Abstract: Compounds of formula (I) act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for treating and/or preventing broncho-obstructive and inflammatory diseases.Type: GrantFiled: June 8, 2012Date of Patent: April 21, 2015Assignee: Chiesi Farmaceutici S.p.A.Inventors: Fabio Rancati, Andrea Rizzi, Ian Linney, Wesley Blackaby, Chris Knight
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Patent number: 9012445Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: GrantFiled: January 12, 2013Date of Patent: April 21, 2015Assignee: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Publication number: 20150105365Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7 R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 16, 2015Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
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Publication number: 20150105376Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20150105369Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 14, 2014Publication date: April 16, 2015Inventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS
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Publication number: 20150105366Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 16, 2015Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings, William Moore Jones, Steven Goldberg
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Publication number: 20150105404Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 16, 2015Applicant: Janssen Pharmaceutica NVInventors: Kristi A. Leonard, Kent Barbay, James P. Edwards, Kevin D. Kreutter, David A. Kummer, Umar Maharoof, Rachel Nishimura, Maud Urbanski, Hariharan Venkatesan, Aihua Wang, Ronald L. Wolin, Craig R. Woods, Anne Fourie, Xiaohua Xue, Maxwell D. Cummings
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Publication number: 20150105372Abstract: The present invention comprises compounds of Formula I. wherein: R1, R2, R3, R4, R5, R6, R7, R8, and R9 are defined in the specification. The invention also comprises a method of treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is rheumatoid arthritis or psoriasis. The invention also comprises a method of modulating ROR?t activity in a mammal by administration of a therapeutically effective amount of at least one compound of claim 1.Type: ApplicationFiled: October 15, 2013Publication date: April 16, 2015Applicant: JANSSEN PHARMACEUTICA NVInventors: KRISTI A. LEONARD, KENT BARBAY, JAMES P. EDWARDS, KEVIN D. KREUTTER, DAVID A. KUMMER, UMAR MAHAROOF, RACHEL NISHIMURA, MAUD URBANSKI, HARIHARAN VENKATESAN, AIHUA WANG, RONALD L. WOLIN, CRAIG R. WOODS, ANNE FOURIE, XIAOHUA XUE, MAXWELL D. CUMMINGS
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Patent number: 9006444Abstract: The invention provides certain phenyl carboxamide-containing compounds of the Formula (I); or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: GrantFiled: October 1, 2012Date of Patent: April 14, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Maria Emilia Di Francesco, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Patent number: 9006256Abstract: The present invention provides pharmaceutical compositions and therapeutic methods for treating diseases such as multiple endocrine neoplasia type IIA, multiple endocrine neoplasia type IIB, familial medullary thyroid carcinoma, thyroid carcinoma, papillary thyroid carcinoma, sporadic medullary thyroid carcinoma, Hirschsprung disease, pheochromocytoma, parathyroid hyperplasia and mucosal neuromas of the gastrointestinal tract. The therapeutic methods and pharmaceutical compositions use a RET kinase inhibiting substance, such as 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide and pharmacologically acceptable salts thereof, and involve a step of administering the RET kinase inhibiting substance to a patient.Type: GrantFiled: April 8, 2011Date of Patent: April 14, 2015Assignee: Eisai R&D Management Co., Ltd.Inventor: Junji Matsui
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Patent number: 9006257Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: GrantFiled: February 7, 2013Date of Patent: April 14, 2015Assignee: Glenmark Pharmaceuticals S.A.Inventors: Laxmikant Atmaram Gharat, Abhisek Banerjee, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Patent number: 9006240Abstract: The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.Type: GrantFiled: August 2, 2006Date of Patent: April 14, 2015Assignee: Eisai R&D Management Co., Ltd.Inventors: Toshimitsu Uenaka, Yuji Yamamoto, Junji Matsui
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Publication number: 20150099778Abstract: A method of treating a condition chosen from the group consisting of interstitial cystitis, cystitis, chronic nonbacterial prostatitis, chronic cystitis, prostatic hyperplasia, prostatitis, prostatism, bladder neck contracture, bladder inflammation, and overactive bladder by administering an amount of rebamipide or a pharmaceutically acceptable salt thereof to a human.Type: ApplicationFiled: December 26, 2013Publication date: April 9, 2015Applicant: N.M.A. Co., Ltd.Inventors: Tomohiro Ueda, Yasuhito Funahashi
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Publication number: 20150099779Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.Type: ApplicationFiled: April 30, 2013Publication date: April 9, 2015Inventors: Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn
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Publication number: 20150099780Abstract: This invention relates to compounds of Formula I: 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 administering a CFTR potentiator.Type: ApplicationFiled: September 19, 2014Publication date: April 9, 2015Inventor: Adam J. Morgan
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Publication number: 20150099781Abstract: Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.Type: ApplicationFiled: December 16, 2014Publication date: April 9, 2015Inventors: Lizbeth K. Hedstrom, Gregory D. Cuny, Deviprasad R. Gollapalli, Sivapriya Kirubakaran, Sushil K. Maurya, Boris Striepen, Suresh K. Gorla, Corey R. Johnson, Mandapati Kavitha, Jihan Khan
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Patent number: 8999982Abstract: The present invention relates to 1-nitrogen-heterocyclic-2-carboxamides and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the treatment and/or prevention of Axl receptor tyrosine kinase subfamily induced disorders, including cancer and primary tumor metastases, and pharmaceutical compositions containing at least one of said 1-nitrogen-heterocyclic-2-carboxamide derivatives and/or pharmaceutically acceptable salts thereof.Type: GrantFiled: August 26, 2011Date of Patent: April 7, 2015Assignees: Lead Discovery Center GmbH, Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V.Inventors: Carsten Schultz-Fademrecht, Bert Klebl, Axel Choidas, Uwe Koch, Jan Eickhoff, Alexander Wolf, Axel Ullrich
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Patent number: 9000037Abstract: This invention relates to novel precursors suitable for 18F radiolabeling of glutamate derivatives, methods for preparing such compounds and its intermediates, compositions comprising such compounds, kits comprising such compounds or compositions and methods for 18F radiolabeling of glutamate derivatives wherein the obtained 18F radiolabeled glutamate derivatives are suitable for diagnostic imaging by Positron Emission Tomography (PET) of proliferative diseases e.g. tumor in mammals.Type: GrantFiled: April 30, 2012Date of Patent: April 7, 2015Assignee: Piramal Imaging SAInventors: Christina Hultsch, Michael Harre, Filip Novak, Mathias Berndt, Matthias Friebe, Heribert Schmitt-Willich, Dae Yoon Chi, Byoung Se Lee, Sang Don Park
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Publication number: 20150094331Abstract: The present invention relates to new quinolone inhibitors of lipoprotein-associated phospholipase A2 activity, pharmaceutical compositions thereof, and methods of use thereof.Type: ApplicationFiled: October 1, 2013Publication date: April 2, 2015Applicant: Auspex Pharmaceuticals, Inc.Inventors: Tadimeti Rao, Chengzhi Zhang
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Publication number: 20150093440Abstract: A method of making aggregate particles suitable for a powder aerosol composition that includes forming a dispersion of nanoparticulate drug and/or excipient in a non-aqueous liquid, and spray-drying the dispersion to generate aggregate particles having a mass median aerodynamic diameter of less than or equal to about 100 microns, and particles generated by such method, and compositions of said particles.Type: ApplicationFiled: October 13, 2011Publication date: April 2, 2015Applicant: GLAXO GROUP LIMITEDInventors: Michiel M. Van Oort, John N. Hong
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Publication number: 20150094289Abstract: Provided herein are small molecules that have a neuroprotective or modulatory effect in the nervous system. The small molecules provided herein modulate dopaminergic neuronal activity. Also provided herein are methods of for the prophylaxis of or preventing the progression of Parkinson's Disease (PD).Type: ApplicationFiled: June 3, 2013Publication date: April 2, 2015Inventors: Rudolfo Gonzalez, Ibon Garitaonandia, Ruslan Semechkin
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Publication number: 20150094332Abstract: The subject invention provides a method for treating a subject afflicted with a form of multiple sclerosis (MS) or presenting a clinically isolated syndrome (CIS) comprising periodically administering to the subject an amount of laquinimod and an amount of a compound of formula (I): as described herein. The subject invention also provides packages and pharmaceutical compositions comprising laquinimod and a compound of formula (I) as described herein. The subject invention further provides uses of said compounds, pharmaceutical compositions and packages in treating a subject afflicted with a form of MS or presenting a CIS.Type: ApplicationFiled: September 26, 2014Publication date: April 2, 2015Applicant: Teva Pharmaceutical Industries, Ltd.Inventors: Volker Knappertz, Joel Kaye
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Publication number: 20150087886Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-1) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers.Type: ApplicationFiled: October 9, 2014Publication date: March 26, 2015Inventors: Robert Hromas, Andrei Leitao, Tudor I. Oprea, Larry A. Sklar, Elizabeth A. Williamson, Justin Wray, Wei Wang
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Publication number: 20150087656Abstract: Prolongation compositions for prolonging the presence of drugs in blood.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Inventors: Aida Salatinjants, Robert Salatinjants
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Patent number: 8987299Abstract: Compounds of formula (I) described herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.Type: GrantFiled: December 6, 2013Date of Patent: March 24, 2015Assignee: Chiesi Farmaceutici S.p.A.Inventors: Fabio Rancati, Ian Linney
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Patent number: 8987301Abstract: Novel hetarylaminoquinoline derivatives of formula (I) wherein X, Z, Het, R1, R2, R3 and R4 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: October 12, 2010Date of Patent: March 24, 2015Assignee: Merck Patent GmbHInventors: Alfred Jonczyk, Christiane Amendt, Frank Zenke
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Patent number: 8987262Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.Type: GrantFiled: November 16, 2012Date of Patent: March 24, 2015Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de BordeauxInventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
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Patent number: 8987456Abstract: The invention provides certain 3-pyridyl carboxamide-containing compounds of the Formula (I) (I) or pharmaceutically acceptable salts thereof, wherein A and B are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: GrantFiled: October 1, 2012Date of Patent: March 24, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Michael D. Altman, Kaleen Konrad Childers, Anthony Donofrio, John Michael Ellis, Sandra Lee Knowles, Alan B. Northrup
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Patent number: 8987250Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: GrantFiled: April 19, 2013Date of Patent: March 24, 2015Assignee: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
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Publication number: 20150080377Abstract: The present invention relates to deuterium-enriched pyridinonecarboxamides and their derivatives of the formula 1, and pharmaceutically acceptable salts thereof, are partial or full agonists of serotonin (5-Hydroxytryptamine or 5-HT) receptor subtype 4 (5-HT4), and are useful compounds for the prevention and treatment of Alzheimer's disease, cognitive and memory dysfunction, mild cognition impairment, memory decline, cognitive impairment associated with schizophrenia, cognitive impairment associated with age-related dementia or Alzheimer's disease, cognitive impairment associated with post-coronary bypass surgery, attention deficit hyperactivity disorder, Obsessive compulsive disorder, depression, speech improvement in autistic children, sleep apnea in Alzheimer's patients, Age-related macular degeneration (AMD), irritable bowel syndrome, gastroesophageal reflux disease, Crohn's disease, emesis, nausea, vomiting, prokinesia, non-ulcer dyspepcia, anxiety, depression, pain, migraine, urinary incontinence, aType: ApplicationFiled: August 31, 2013Publication date: March 19, 2015Inventor: Daljit Singh Dhanoa
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Publication number: 20150080373Abstract: The antibacterial compound of formula I wherein X1, X3; X4 and X6, each independently of the others, represents a nitrogen atom or CR2, with the proviso that at least one of X1, X3; X4 and X6 represents a nitrogen atom; X2 represents C—H, C—(C1-C6alkyl), C—(C1-C6alkoxy), C-halogen, C—COOH; X5 represents C—H or C—(C1-C6alkyl), C-halogen; A1, A2, A3, R1 and R4 represent various substituents, G represents aryl or heteroaryl, which is unsubstituted or substituted which compounds show good activity against pathogenic bacteria.Type: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Inventors: Berangere Gaucher, Franck Hubert Danel, Patrick Roussel
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Publication number: 20150080324Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.Type: ApplicationFiled: November 25, 2014Publication date: March 19, 2015Inventors: Gavin David Heffernan, David Penman Jacobus, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
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Publication number: 20150080430Abstract: The present invention relates to methods of treating benign hyperproliferative diseases of the epidermis by administering a composition comprising at least one jasmonate ester derivative. In particular, the present invention provides jasmonate ester derivatives as potent compounds useful for the treatment of disorders such as actinic keratoses with reduced side effects.Type: ApplicationFiled: September 25, 2014Publication date: March 19, 2015Applicant: SEPAL PHARMA LTD.Inventors: Max HERZBERG, Frederic REVAH
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Publication number: 20150080431Abstract: The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), solids forms, and pharmaceutical compositions thereof for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations. The present invention also relates to the use of Compound 1 in combination with 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 2), and Compound 1 in combination with (S)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide (Compound 3), for the treatment of CFTR-mediated diseases, particularly cystic fibrosis, in patients possessing specific genetic mutations.Type: ApplicationFiled: November 26, 2014Publication date: March 19, 2015Inventors: Fredrick F. Van Goor, William Lawrence Burton, Haihui Yu, Beth Jennifer Hoffman
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Patent number: 8980913Abstract: Compounds of formula (I) defined herein act both as muscarinic receptor antagonists and beta2 adrenergic receptor agonists and are useful for the prevention and/or treatment of broncho-obstructive or inflammatory diseases.Type: GrantFiled: December 6, 2013Date of Patent: March 17, 2015Assignee: Chiesi Farmaceutici S.p.A.Inventors: Fabio Rancati, Ian Linney, Chris Knight, Wolfgang Schmidt
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Patent number: 8980895Abstract: The present invention relates to compounds and pharmaceutically acceptable salts, esters and prodrugs of Formula (I) or (II): which are useful as AMPK modulators effective in treating diabetes, obesity and cancer in a subject.Type: GrantFiled: August 9, 2012Date of Patent: March 17, 2015Assignee: Mercury Therapeutics, Inc.Inventors: Neal C. Birnberg, Hong Liu, Qing Ping Weng, Haibo Shang, Pan Yin, Sharanappa B. Rajur, Hwa-Ok Kim, Paresh D. Salgaonkar, Norton P. Peet
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Patent number: 8980919Abstract: The present invention relates to a medicament for treating occlusive and/or ischemic vascular disorder comprising a carbostyril derivative and carnitine.Type: GrantFiled: March 13, 2009Date of Patent: March 17, 2015Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takao Urabe, Yuji Ueno, Kensuke Orito, Hiroshi Ohno
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Publication number: 20150073016Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.Type: ApplicationFiled: April 30, 2013Publication date: March 12, 2015Inventors: Anderson GAWECO, Jefferson TILLEY, John WALKER, Samantha PALMER, James BLINN
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Publication number: 20150072977Abstract: New compounds of formula I are described. The compounds have potentially valuable pharmaceutical properties in the treatment of some central and peripheral nervous system disorders.Type: ApplicationFiled: November 14, 2014Publication date: March 12, 2015Inventors: David Alexander LEARMONTH, Laszlo Erno KISS, Pedro Nuno LEAL PALMA, Humberto DOS SANTOS FERREIRA, Patricio Manuel Vieira ARAUJO SOARES DA SILVA
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Publication number: 20150071919Abstract: The present application relates to compositions and methods for treating a proliferative disorder by administering to a subject a pharmaceutical composition of a dual kinase inhibitor. Catecholic butanes cane serve as dual kinase inhibitors for purposes of methods described herein. Patients to be treated include those that have been treated with Tarceva or other therapeutic compounds and relapsed or are resistant to treatment. The compounds described herein may exhibit a synergistic effect when administered with another agent.Type: ApplicationFiled: September 9, 2014Publication date: March 12, 2015Inventors: Thomas F. WHITE, Dan HOTH
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Publication number: 20150073015Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.Type: ApplicationFiled: May 23, 2014Publication date: March 12, 2015Inventors: John DeMattei, Adam R. Looker, Bobbianna Neubert-Langille, Martin Trudeau, Stefanie Roeper, Michael P. Ryan, Dahrika Milfred Yap Guerette, Brian R. Krueger, Peter D.J. Grootenhuis, Fredrick F. Van Goor, Martyn C. Botfield, Gregor Zlokarnik
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Patent number: 8975279Abstract: The subject invention provides a Laquinimod amine salt, which is laquinimod meglumine, laquinimod choline hydroxide, laquinimod L-lysine or laquinimod monoethanolamine.Type: GrantFiled: October 31, 2013Date of Patent: March 10, 2015Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Anton Frenkel, Avital Laxer, Judith Aronheim
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Patent number: 8975408Abstract: Methods for producing moxifloxacin hydrochloride compounds having very low levels of impurities are provided. Compounds produced using such methods and pharmaceutical compositions including such compounds are also provided.Type: GrantFiled: January 20, 2014Date of Patent: March 10, 2015Assignee: F.I.S.—Fabbrica Italiana Sintetici S.p.A.Inventors: Gianni Gottardo, Pierluigi Padovan, Sergio Osti
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Patent number: 8975275Abstract: The invention relates to the use of chemotherapeutic agents for the production of a medicament for the topical and/or local treatment of diseases caused by bacteria and/or for prophylaxis in humans or animals.Type: GrantFiled: December 22, 2000Date of Patent: March 10, 2015Assignee: Bayer Innovation GmbHInventors: Hans-Herrmann Schulz, Günther Schlimbach
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Publication number: 20150065502Abstract: The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.Type: ApplicationFiled: April 26, 2013Publication date: March 5, 2015Inventors: Jerome Emile Georges Guillemont, Magali Madeleine Simone Motte, David Francis Alain Lançois, Wendy Mia Albert Balemans
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Publication number: 20150065487Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fred Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Publication number: 20150065539Abstract: The present disclosure provides compounds effective in increasing mucociliary clearance in a subject. In one embodiment, the compounds are of the general formula I. The present disclosure further shows that such compounds are effective in increasing activation of the CFTR, thereby increasing mucociliary clearance in the subject. The present disclosure further shows that such compounds are effective in increasing the depth of ASL, thereby increasing mucociliary clearance in the subject. In one embodiment of each of the foregoing, the subject is free from congenital or genetic defect in the cellular mucociliary clearance apparatus and/or acquired abnormality in the cellular mucociliary clearance apparatus.Type: ApplicationFiled: March 15, 2013Publication date: March 5, 2015Inventors: Steven M. Rowe, Mark Dransfield
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Publication number: 20150059746Abstract: A method is disclosed for making a pharmaceutical composition for pulmonary administration, the method comprising a step in which an inhalable pharmaceutically active material is acoustically blended in a resonant acoustic blender. The invention also relates to compositions for inhalation prepared by the method.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventor: Matthew Green
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Publication number: 20150065471Abstract: The present invention is directed to a pharmaceutically acceptable crystalline addition salt of 5-[(1R)-2-({2-[4-({4-(2,2-difluoro-2-phenylethoxy)phenyl]ethyl}amino)-1-hydroxyethyl]-8-hydroxyquinolin-2(1H)-one, and (ii) a dicarboxylic acid, a sulfonic acid or a sulfimide, or a pharmaceutically acceptable solvate thereof.Type: ApplicationFiled: March 28, 2013Publication date: March 5, 2015Inventors: Carlos Puig Duran, Francesc Carrera Carrera, Juan Bautista Pérez Garcia, Enrique Moyes Valles, Iolanda Marchueta Hereu
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Publication number: 20150065490Abstract: Compounds of formula I in free or salt or solvate form, wherein X has the meaning indicated in the specification, are useful for treating conditions that are prevented or alleviated by activation of the ?2-adrenoreceptor. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: November 6, 2014Publication date: March 5, 2015Applicant: NOVARTIS AGInventors: Bernard CUENOUD, Robin Alec FAIRHURST, Roger John TAYLOR, David BEATTIE