The Additional Ring Is A Hetero Ring Patents (Class 514/326)
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Patent number: 8957062Abstract: Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.Type: GrantFiled: April 5, 2012Date of Patent: February 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Scott Edmondson, Zhiqiang Guo, Harold B. Wood, Andrew W. Stamford, Michael W. Miller, Duane E. DeMong, Gregori J. Morriello, Rajan Anand, Vincent J. Colandrea, Megan Macala, Milana Maletic, Cheng Zhu, Yuping Zhu, Wanying Sun, Kake Zhao, Yong Huang, Joel M. Harris, Lehua Chang, Nam Fung Kar, Zhiyong Hu, Liping Wang, Bowei Wang, Ping Liu, Jason W. Szewczyk, William B. Geiss
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Patent number: 8957063Abstract: Compounds which modulate the CB2 receptor are disclosed. The compounds are useful for treating CB2 receptor-mediated diseases such as pain.Type: GrantFiled: February 19, 2009Date of Patent: February 17, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Monika Ermann, Innocent Mushi
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Patent number: 8957066Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3) using compounds of formula (I), wherein the substituents are as defined herein.Type: GrantFiled: March 15, 2013Date of Patent: February 17, 2015Assignee: Biomarin Pharmaceutical Inc.Inventors: Vincent Jacques, James R Rusche, Norton P. Peet, Jasbir Singh
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Publication number: 20150045367Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.Type: ApplicationFiled: December 19, 2012Publication date: February 12, 2015Inventors: Erik Verner, Wei Chen, Sriram Balasubramanian
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Publication number: 20150045393Abstract: The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.Type: ApplicationFiled: February 1, 2013Publication date: February 12, 2015Inventors: Greg R. Thatcher, Isaac Thomas Schiefer, Ottavio Arancio, Mauro Fa
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Patent number: 8951536Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.Type: GrantFiled: February 28, 2013Date of Patent: February 10, 2015Assignee: Incyte CorporationInventors: Andrew P. Combs, Amy Takvorian, Wenyu Zhu, Richard B. Sparks
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Patent number: 8952031Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: March 5, 2012Date of Patent: February 10, 2015Assignee: Theravance Biopharma R&D IP, LLCInventors: Sean G. Trapp, Michael R. Leadbetter, Daniel D. Long, Lan Jiang, Sabine Axt
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Publication number: 20150038534Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.Type: ApplicationFiled: October 22, 2014Publication date: February 5, 2015Inventors: Erkan BALOGLU, Shomir Ghosh, Mercedes Lobera, Darby R. Schmidt
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Publication number: 20150038501Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Inventors: Leping LI, Min ZHONG
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Publication number: 20150037399Abstract: The present disclosure concerns the novel use of pipoxolan and its pharmaceutical composition. Pipoxolan is useful therapeutic drugs for pathological conditions caused by vascular smooth muscle cell proliferation and migration to relieve a body appeared vascular injury, cerebrovascular ischemia, intimal hyperplasia, atherosclerotic stenosis, cerebral ischemia, and stroke.Type: ApplicationFiled: May 2, 2014Publication date: February 5, 2015Applicant: China Medical UniversityInventors: Yuh-Fung CHEN, Huei-Yann TSAI
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Publication number: 20150038483Abstract: The present invention is related to a compound represented by formula (I) wherein R1 is a hydrogen atom, substituted or unsubstituted alkyl, substituted or unsubstituted aromatic carbocyclyl, or the like; X is —N(R3)—, —O—, or —S—; Y is ?C(R4)—, or ?N—; Z is —N(R7)—, —O—, or —S—; R2 is substituted or unsubstituted alkyloxy, or the like, or a group represented by the following formula: —(CR2aR2b)n—R2c, wherein R2a is each independently a hydrogen atom, halogen, or the like; R2b is each independently a hydrogen atom, halogen, or the like; R2a and R2b which are attached to the same carbon atom may be taken together to form oxo, a substituted or unsubstituted non-aromatic carbocycle, or the like; two of R2a which are attached to the adjacent carbon atoms and/or two of R2b which are attached to the adjacent carbon atoms may be taken together to form a bond; R2c is substituted or unsubstituted aromatic carbocyclyl, or the like; n is an integer from 1 to 3; R3 and R7 are each independently a hydrogen atom, subType: ApplicationFiled: March 26, 2013Publication date: February 5, 2015Inventors: Akira Yukimasa, Naotake Kobayashi, Kenji Takaya, Yoshio Hato
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Patent number: 8945592Abstract: Compositions and methods effective to minimize or eliminate the presence of oxidative degradation products in solid dosage forms comprising sufentanil are provided.Type: GrantFiled: November 21, 2008Date of Patent: February 3, 2015Assignee: AcelRx Pharmaceuticals, Inc.Inventors: Shamim Pushpala, Larry Hamel, Stelios Tzannis, Evangeline Cruz
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Patent number: 8946446Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 13, 2012Date of Patent: February 3, 2015Assignee: Phenex Pharmaceuticals AGInventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Publication number: 20150031686Abstract: Disclosed are phenyl-oxazolyl derivatives having a general formula (I), a preparation method thereof, and an application of the phenyl-oxazolyl derivatives as an inosine monophosphate dehydrogenase (IMPDH) inhibitor.Type: ApplicationFiled: March 6, 2013Publication date: January 29, 2015Inventors: Zhaojin Zhong, Zhuorong Li, Dajun Zhang, Yuhuan Li, Zhen Wang, Rongmei Gao, Jiajia Shen
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Publication number: 20150031541Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are useful as a pesticides.Type: ApplicationFiled: February 27, 2013Publication date: January 29, 2015Applicant: Syngenta Participations AGInventors: Clemens Lamberth, Sarah Sulzer-Mosse, Fredrik Cedarbaum, Jayant Umarye, Ravindra Sonawane
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Patent number: 8940768Abstract: Disclosed are novel triazole derivatives. Exhibiting excellent antifungal activity and in vivo safety, they are useful for the treatment or prevention of fungal infections caused by a wide spectrum of fungi.Type: GrantFiled: February 11, 2011Date of Patent: January 27, 2015Assignee: Daewoong Pharmaceutical Co., Ltd.Inventors: Joon Seok Park, Kyung A Yu, Yun Soo Yoon, Mi Ryeong Han, Ji Duck Kim
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Publication number: 20150024935Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols RA1, RA2, X, Y, L1, L2, RB1, RB2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).Type: ApplicationFiled: December 21, 2012Publication date: January 22, 2015Applicant: Bayer Intellectual Property GmbHInventors: Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Thomas Seitz, Stefan Hillebrand, Jürgen Benting, Jan Peter Schmidt, Pierre Cristau
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Publication number: 20150025076Abstract: The present invention relates to modulator of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Inventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D.J. Grootenhuis
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Publication number: 20150025054Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula I as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection.Type: ApplicationFiled: October 22, 2012Publication date: January 22, 2015Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Maria de los Angeles Estirate Martínez, Nuria Valls Vidal, Guido Kurz, Julio Cesar Castro Palomino Lar
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Publication number: 20150025056Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
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Patent number: 8937181Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.Type: GrantFiled: April 13, 2007Date of Patent: January 20, 2015Assignee: Purdue Pharma L.P.Inventors: Akira Matsumura, Hidenori Mikamiyama, Bin Shao, Naoki Tsuno, Jiangchao Yao
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Publication number: 20150018330Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: ApplicationFiled: July 30, 2014Publication date: January 15, 2015Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATIONInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. MacDonald, Thomas Eric Ballard, JR.
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Publication number: 20150018374Abstract: Disclosed is a fungicidal composition comprising (a) at least one compound selected from the compounds of Formula 1, N-oxides, and salts thereof, wherein R1 is F, Cl or Br; R2 is H or F; and R3 is Cl or Br; and (b) at least one fungicidal compound selected from (b1) through (b13) as disclosed herein. Also disclosed is a method for controlling plant diseases caused by fungal plant pathogens comprising applying to the plant or portion thereof, or to the plant seed, a fungicidally effective amount of a compound of Formula 1, an N-oxide, or salt thereof (e.g., as a component in the aforesaid composition). Also disclosed are process intermediate compounds useful for preparing compounds of Formula 1.Type: ApplicationFiled: January 30, 2013Publication date: January 15, 2015Inventors: Andrew Edmund Taggi, Jeffrey Keith Long, James Francis Bereznak
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Publication number: 20150018332Abstract: The invention generally relates to nuclear transport modulators, e.g CRM1 inhibitors, and more particularly to a compound represented by formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula (I), or a pharmaceutically acceptable salt or composition thereof, e.g, in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.Type: ApplicationFiled: July 26, 2012Publication date: January 15, 2015Applicant: KARYOPHARM THERAPEUTICS INC.Inventors: Vincent P. Sandanayaka, Sharon Shacham, Michael Kauffman, Sharon Shechter, Dilara McCauley, Yosef Landesman, William Senapedis, Jean-Richard Saint-Martin
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Publication number: 20150018346Abstract: The present invention relates to methods of inhibiting one or more signs of aging and/or degenerative disorder in a subject in need of such treatment, which comprise administering, to the subject, an effective amount of one or more of the compounds as set forth herein. “Inhibiting a sign of aging or degenerative disorder” means reducing the risk of occurrence, delaying the onset, slowing the progression, and/or reducing the severity and/or manifestation, of a sign of aging or degenerative disorder, and includes, but is not limited to, preventing the occurrence, development or progression of a sign of aging or degenerative disorder.Type: ApplicationFiled: March 18, 2014Publication date: January 15, 2015Applicant: University of Pittsburgh - Of the Commonwealth System of Higher EducationInventors: Laura J. Niedernhofer, Paul D. Robbins, Peter Wipf
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Patent number: 8933102Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I).Type: GrantFiled: October 24, 2011Date of Patent: January 13, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Gregori J. Morriello, Lehua Chang, Scott D. Edmondson
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Patent number: 8933101Abstract: The present invention relates to [1-(benzyl)-piperidin-4-yl]-([1,3,4]thiadiazol-2-yl)-amine and [1-(benzyl)-piperidin-4-yl]-(thiazol-2-yl)-amine derivatives of formula (I) that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.Type: GrantFiled: April 18, 2008Date of Patent: January 13, 2015Assignee: Janssen Pharmaceutica NVInventors: Gregor James MacDonald, José Manuel Bartolomé-Nebreda, Michiel Luc Maria Van Gool
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Publication number: 20150011511Abstract: Compounds represented by formula (I): wherein each symbol is as defined in the description, and pharmaceutically acceptable salts thereof are useful as hyperglycemic inhibitors having a serine protease inhibitory action and as prophylactic or therapeutic drugs for diabetes.Type: ApplicationFiled: September 25, 2014Publication date: January 8, 2015Applicant: AJINOMOTO CO., INC.Inventors: Atsushi KONISHI, Munetaka TOKUMASU, Tamotsu SUZUKI, Takahiro KOSHIBA, Koji OHSUMI, OSAMU IKEHARA, Yuko KODAMA
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Publication number: 20150011526Abstract: The present invention relates to 2-oxo-piperidinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: October 10, 2012Publication date: January 8, 2015Inventors: Ali Ates, Florian Montel, Anne Valade, Olivier Lorthioir
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Patent number: 8927551Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: GrantFiled: May 18, 2010Date of Patent: January 6, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 8927534Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.Type: GrantFiled: January 31, 2007Date of Patent: January 6, 2015Assignee: Shire Orphan Therapies GmbHInventors: Gunther Zischinsky, Roland Stragies, Frank Osterkamp, Dirk Scharn, Gerd Hummel, Holger Kalkhof, Grit Zahn, Doerte Vossmeyer, Claudia Christner-Albrecht, Ulrich Reineke
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Publication number: 20150005275Abstract: The present invention discloses compounds according to Formula I: wherein R1, R2, R3, L, and the subscript m are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions, and methods of treatment using the same, for the treatment of cystic fibrosis by administering a compound of the invention.Type: ApplicationFiled: May 6, 2014Publication date: January 1, 2015Inventors: Steven Emiel Van der Plas, Oscar Mammoliti, Christel Jeanne Marie Menet, Giovanni Alessandro Tricarico, Ann De De Blieck, Caroline Martine Andrée Marie Joannesse, Hans Kelgtermans, Tom Roger Lisette De Munck
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Publication number: 20150005277Abstract: The invention is compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.Type: ApplicationFiled: June 21, 2014Publication date: January 1, 2015Inventors: Zhiwei Wang, Yunhang Guo
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Publication number: 20150005319Abstract: The invention relates generally to macrocyclic compounds of formula I and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of IL-17 and/or are useful in the treatment of medical conditions, such as inflammatory diseases and other IL-17-associated disorders.Type: ApplicationFiled: February 1, 2013Publication date: January 1, 2015Inventors: Michael Taylor, Nicholas K. Terrett, William H. Connors, Cheri Snedeker, Kelley C. Shortsleeves, Benjamin A. Seigal, Stephen P. Hale, Timothy F. Briggs, Frank G. Favaloro, Jr., Tyler J. Cipriani, Dingxue Yan, Sethu L. Alexander, Atli Thorarensen, Li Xing
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Patent number: 8921559Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: November 30, 2011Date of Patent: December 30, 2014Assignee: Janssen Pharmaceutica NVInventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
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Patent number: 8921398Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: GrantFiled: June 6, 2012Date of Patent: December 30, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Frank Himmelsbach, Elke Langkopf, Bernd Nosse, Neil J. Ashweek, Nicole Harriott
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Publication number: 20140378430Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.Type: ApplicationFiled: January 4, 2013Publication date: December 25, 2014Applicant: SPINIFEX PHARMACEUTICALS PTY LTDInventors: Thomas David McCarthy, Alan Naylor
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Publication number: 20140377292Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Publication number: 20140378457Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: September 9, 2014Publication date: December 25, 2014Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson, Bruce E. Tomczuk
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Publication number: 20140377219Abstract: Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.Type: ApplicationFiled: September 6, 2012Publication date: December 25, 2014Applicant: New York Blood CEnter, Inc.Inventors: Asim Kumar Debnath, Francesca Curreli, Peter D. Kwong, Young Do Kwon
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Publication number: 20140378444Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.Type: ApplicationFiled: November 22, 2013Publication date: December 25, 2014Applicant: University of Pittsburgh - Of the Commonwealth System of Higher EducationInventors: Peter Wipf, Marie-Celine Frantz
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Publication number: 20140378509Abstract: The compound 1-(2-{4-[3-(3,4-dimethoxyphenyl)-4,4-dimethyl-5-oxo-4,5-dihydro-1H-pyrazol-1-yl]piperidin-1-yl}-2-oxoethyl)pyrrolidine-2,5-dione is a novel effective inhibitor of the type 4 phosphodiesterase useful in the treatment of psoriasis or atopic dermatitis.Type: ApplicationFiled: August 29, 2014Publication date: December 25, 2014Inventors: Beate SCHMIDT, Christian SCHEUFLER, Jürgen VOLZ, Martin FETH, Rolf-Peter HUMMEL, Armin HATZELMANN, Christof ZITT, Andrea WOHLSEN, Degenhard MARX, Hans-Peter KLEY, Deborah OCKERT, Anke HEUSER, Johannes A.M. CHRISTIAANS, Geert Jan STERK, Wiro M.P.B. MENGE
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Patent number: 8916552Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygType: GrantFiled: October 12, 2007Date of Patent: December 23, 2014Assignee: Astex Therapeutics LimitedInventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
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Publication number: 20140371239Abstract: The present invention relates generally to compounds that inhibit the binding of menin and MLL or MLL fusion proteins and methods of use thereof. In particular embodiments, the present invention provides compositions comprising piperidine-containing compounds and methods of use thereof to inhibit the interaction of menin with MLL oncoproteins (e.g., MLL1, MLL2, MLL-fusion oncoproteins), for example, for the treatment of leukemia, solid cancers, diabetes, and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, MLL-PTD and/or menin.Type: ApplicationFiled: June 11, 2014Publication date: December 18, 2014Inventors: Jolanta Grembecka, Tomasz Cierpicki, Sunil Kumar Upadhyay, Shaun R. Stauffer, Rocco D. Gogliotti, Timothy J. Senter
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Publication number: 20140371238Abstract: The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:Type: ApplicationFiled: March 13, 2014Publication date: December 18, 2014Applicant: FLATLEY DISCOVERY LABInventors: Michael P. Zawistoski, Yevgen Barsukov, Bridget M. Cole, Richard A. Nugent
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Publication number: 20140371147Abstract: A combination of compounds is described for the treatment and/or prevention of skin conditions linked to hypopigmentation. Also described, is a combination product that includes at least one prostaglandin receptor agonist and at least one MC1R receptor agonist, as a medicament for use simultaneously, separately or spread out over time for the treatment and/or prevention of skin conditions linked to hypopigmentation, such as vitiligo.Type: ApplicationFiled: December 17, 2012Publication date: December 18, 2014Inventors: Philippe Martel, Itaru Suzuki, Johannes Voegel, Philippe Andres, Sandrine Rethore
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Publication number: 20140371269Abstract: The present invention provides compounds of Formula I or a pharmaceutical salt thereof, where the variables for R1, R2, and R3 are as described herein; methods of treating a condition such as hypertriglyceridemia; and processes for preparing the compounds.Type: ApplicationFiled: January 16, 2013Publication date: December 18, 2014Applicant: Eli Lilly and CompanyInventors: Maria Carmen Fernandez, Maria Rosario Gonzalez-Garcia, Bin Liu, Lance Allen Pfeifer
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Publication number: 20140371213Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: May 19, 2014Publication date: December 18, 2014Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20140371176Abstract: This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer.Type: ApplicationFiled: September 3, 2014Publication date: December 18, 2014Inventors: Neil W. Johnson, Jiri Kasparec, Meagan B. Rouse, Xinrong Tian
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Patent number: RE45323Abstract: Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 7, 2014Date of Patent: January 6, 2015Assignee: Boehringer Ingelheim International GmbHInventors: Marc Grundl, Horst Dollinger, Riccardo Giovannini, Christoph Hoenke, Matthias Hoffmann, Jan Kriegl, Domnic Martyres, Georg Rast, Peter Seither