Three Or More Hetero Atoms In The Tricyclo Ring System Patents (Class 514/293)
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Publication number: 20150133434Abstract: The present disclosure provides compositions and methods for reactivating latent immunodeficiency vims. The methods generally involve contacting an HIV-infected cell in which HIV is latent with an agent that binds a bromodomain (BRD) in the cell. Latently infected cells contain replication-competent integrated HIV-1 genomes that are blocked at the transcriptional level, resulting in the absence of viral protein expression. The present disclosure provides methods for reducing the reservoir of latent immunodeficiency virus in an individual.Type: ApplicationFiled: March 13, 2013Publication date: May 14, 2015Inventors: Melanie Ott, Eric M. Verdin, Ming-Ming Zhou
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Publication number: 20150133436Abstract: The use of compounds in the treatment of autoimmune and inflammatory diseases or conditions, pharmaceutical compositions containing such compounds and to methods for identifying compounds for use in the treatment of such diseases or conditions.Type: ApplicationFiled: January 23, 2015Publication date: May 14, 2015Inventors: Chun-Wa CHUNG, Edwige NICODEME
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Publication number: 20150133443Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.Type: ApplicationFiled: November 7, 2014Publication date: May 14, 2015Inventors: Roberto Pellicciari, Flavio Moroni
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Patent number: 9029388Abstract: The present invention provides a compound having a superior PDE10A inhibitory action and use thereof. The compound is a compound represented by the following formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.Type: GrantFiled: March 15, 2012Date of Patent: May 12, 2015Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiko Taniguchi, Jun Kunitomo, Masato Yoshikawa, Tomoaki Hasui, Eiji Honda, Keisuke Imamura, Haruhi Kamisaki, Shinkichi Suzuki, Kasei Miura
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Publication number: 20150126501Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.Type: ApplicationFiled: January 7, 2015Publication date: May 7, 2015Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
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Patent number: 9023863Abstract: The present invention provides a foamable composition comprising water and an organic solvent, wherein the organic solvent comprises a fatty acid. The composition may further comprise a pharmaceutically active agent. The composition of the invention is also useful for the treatment of a dermatological disorder in a mammal by the topical administration of the composition.Type: GrantFiled: July 12, 2007Date of Patent: May 5, 2015Assignee: Stiefel Research Australia Pty LtdInventors: Albert Zorko Abram, Iulian Goldstein
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Publication number: 20150110784Abstract: The present invention provides therapeutic combinations that include an immune response modifier (IRM) component and an anti-inflammatory component. The inventions further provide methods of treating a condition by administering to one having the condition a therapeutic combination that includes an IRM component and an anti-inflammatory component.Type: ApplicationFiled: December 23, 2014Publication date: April 23, 2015Inventors: Mark A. Tomai, Gary W. Gullikson, David M. Hammerbeck, Elaine A. Egging, Michael J. Reiter, Christopher D. Gram, John P. Vasilakos
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Patent number: 9012470Abstract: The invention provides a novel chemical series of formula I, as well as methods of use thereof for binding to the benzodiazepine site of the GABAA receptor and negatively modulating the ?5 subtype of GABAA, and use of the compound of formula I in the manufacture of a medicament for the treatment of GABAA receptor associated disorders. The invention further provides a method of modulation of one or more GABAA subtypes in an animal comprising administering to the animal an effective amount of a compound of formula (I).Type: GrantFiled: October 11, 2011Date of Patent: April 21, 2015Assignee: Dart NeuroScience (Cayman) Ltd.Inventors: Varsha Gupta, Joel Renick, Graeme Freestone, Alan P. Kaplan
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Publication number: 20150105417Abstract: The invention relates to a pharmaceutical combination which comprises (a) a phosphoinositide 3-kinase inhibitor compound and (b) a compound which modulates the Ras/Raf/Mek pathway for the treatment of a proliferative disease, especially a solid tumor disease; a pharmaceutical composition comprising such a combination; the use of such a combination for the preparation of a medicament for the treatment of a proliferative disease; a commercial package or product comprising such a combination as a combined preparation for simultaneous, separate or sequential use; and to a method of treatment of a warm-blooded animal, especially a human.Type: ApplicationFiled: December 19, 2014Publication date: April 16, 2015Inventors: Carlos Garcia-Echeverria, Sauveur-Michel Maira, Darrin Stuart, Susan Wee, Christine Fritsch, Tobi Nagel
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Publication number: 20150105415Abstract: The present invention relates to the compound represented by formula (I): (wherein, all the symbols have the same meaning as that of the specification), a salt thereof, a solvate thereof or a prodrug thereof. Since the compound of the present invention has an anti stress action, it is useful for preventive and/or therapeutic agent for a disease caused by stress, especially a digestive system disease caused by stress and is superior to oral absorption.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Kazuyuki OHMOTO, Masashi KATO, Yoshifumi KAGAMIISHI, Junichiro MANAKO
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Patent number: 9006246Abstract: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.Type: GrantFiled: July 5, 2011Date of Patent: April 14, 2015Assignee: Ono Pharmaceutical Co., Ltd.Inventors: Akira Ohata, Shingo Nakatani, Tetsuya Sugiyama, Takashi Morimoto
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Patent number: 9006264Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems (particularly quinolines, tetrahydroquinolines, pyridines, [1,5]naphthyridines, [1,5]tetrahydronaphthyridines) substituted at the 1-position with a cyclic substituent, pharmaceutical compositions containing the compounds, methods of making these compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: September 9, 2013Date of Patent: April 14, 2015Assignee: 3M Innovative Properties CompanyInventors: Doris Stoermer, Joseph F. Dellaria, Jr., David T. Amos, Bernhard M. Zimmermann, Luke T. Dressel, Jason D. Bonk
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Patent number: 9000153Abstract: The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).Type: GrantFiled: July 26, 2011Date of Patent: April 7, 2015Assignee: Merck Patent GmbHInventors: Thomas Fuchss, Werner Mederski, Frank Zenke
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Patent number: 8993765Abstract: The present invention relates to tetrahydro-azacarboline derivatives of formula (I): having the substituents as described herein which are melanin-concentrating hormone (MCH-1) receptor antagonists. The present invention also relates to pharmaceutical compositions including these compounds, and methods of preparation and use thereof.Type: GrantFiled: December 20, 2011Date of Patent: March 31, 2015Assignee: Albany Molecular Research, Inc.Inventors: Matthew D. Surman, Peter R. Guzzo, Emily Freeman
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Publication number: 20150087636Abstract: The use of BETi as a potential treatment for FSHD is provided. Specifically, the use of BETi, and particularly selective BETi for BRD4, are shown to inhibit DUX4 expression which is expected to result in a decrease in the severity of symptoms of FSHD. Further, the treatments are shown to work when pulsed as opposed to continuous. This allows for a BETi to be supplied to a human in a pulse, and then allows the human to not need any additional treatment for a window at least as long as the one of the treatment pulse.Type: ApplicationFiled: September 19, 2014Publication date: March 26, 2015Inventor: Francis M. Sverdrup
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Publication number: 20150087627Abstract: The present invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In another aspect, the invention provides for a method for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject. In yet another aspect, a method of inhibiting phosphorylation of both Akt (S473) and Akt (T308) in a cell is set forth. The present invention also provides a pharmaceutical kit effective for treating a disease condition associated with PI3-kinase ? and/or mTOR in a subject.Type: ApplicationFiled: April 15, 2014Publication date: March 26, 2015Applicant: Intellikine LLCInventors: Pingda Ren, Yi Liu, Katayoun Jessen, Xin Guo, Christian Rommel, Troy Edward Wilson
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Publication number: 20150087630Abstract: Methods of use of compounds of formula (I) for treating cancer: wherein X, Y, X, R3, R5 and R6 are as defined herein.Type: ApplicationFiled: April 17, 2014Publication date: March 26, 2015Applicant: Genentech, Inc.Inventors: Huifen Chen, Hazel Joan Dyke, Charles Ellwood, Emanuela Gancia, Lewis Gazzard, Simon Goodacre, Samuel Kintz, Joseph Lyssikatos, Calum MacLeod, Karen Williams
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Patent number: 8987274Abstract: The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.Type: GrantFiled: October 23, 2012Date of Patent: March 24, 2015Assignee: Merck Sharp & Dohme CorpInventors: Latha G. Nair, Stephane L. Bogen, Ronald J. Doll, Yao Ma, Yuan Tian
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Publication number: 20150080389Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: September 16, 2014Publication date: March 19, 2015Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
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Publication number: 20150080366Abstract: Compounds of Formula (I) wherein n, A, R1, R2, R3 and R5 are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.Type: ApplicationFiled: April 3, 2013Publication date: March 19, 2015Applicant: Boehringer Ingelheim International GmbHInventors: Lee Fader, Pierre Louis Beaulieu, Murray Bailey, Francois Bilodeau, Rebekah J. Carson, André Giroux, Cédrickx Godbout, Oliver Hucke, Marc-André Joly, Mélissa Leblanc, Olivier Lepage, Benoit Moreau, Julie Naud, Martin Poirier, Elisia Villemure
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Publication number: 20150072975Abstract: The present invention relates to antibacterial compounds of formula I: wherein all variable substituents are defined as described herein, which are useful for the treatment of bacterial infections.Type: ApplicationFiled: November 18, 2014Publication date: March 12, 2015Inventors: Berangere Gaucher, JR., Franck Hubert Danel, XiaoHu Tang, Tong Xie, Lin XU
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Publication number: 20150072978Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: ApplicationFiled: November 17, 2014Publication date: March 12, 2015Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew J. Souers
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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: 20150065431Abstract: The present invention provides methods of reducing cutaneous scar formation by treating a cutaneous wound with a composition comprising a therapeutic agent that is a sodium channel blocker and/or an inhibitor of the Nax/SCN7A pathway. The present invention also provides wound cover components impregnated with such compositions, kits composed of such compositions with a wound dressing or sterile wipe, and mixtures of such compositions with a topical component (e.g., cream, ointment, or gel) suitable for application to a cutaneous wound. The present invention also provides compositions, kits, devices, and methods for treating skin conditions (e.g., dermatitis, psoriasis, or other skin conditions) with such compositions and devices. Examples of such therapeutic agents include, but are not limited to, an inhibitor of a gene or protein selected from: ENac, COX-2, PGE2, PI3K, PKB, Nax Prss8, IL-1?, IL-8, SAPK, Erk gene, p38 gene, PAR2, S100A8, S100A9, S100A12.Type: ApplicationFiled: August 27, 2014Publication date: March 5, 2015Inventors: Wei Xu, Seok Jong Hong, Robert D. Galiano, Thomas A. Mustoe
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Publication number: 20150065468Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.Type: ApplicationFiled: August 29, 2014Publication date: March 5, 2015Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
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Publication number: 20150065447Abstract: This application relates to methods of increasing survival or progression-free survival in a patient with a solid tumor, wherein the patient has an elevated serum concentration of C-reactive protein (CRP), by administering a JAK inhibitor or an inhibitor of IL-6 signaling to the patient, as well as methods of predicting survival benefit in these patients from such therapy.Type: ApplicationFiled: August 19, 2014Publication date: March 5, 2015Applicant: Incyte CorporationInventor: Victor Sandor
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Patent number: 8962649Abstract: A multidose package containing an imiquimod formulation suitable for treating topical conditions includes: a) a dispensing aperture for dispensing the formulation from the package; b) a reservoir containing sufficient formulation to provide two or more doses; c) a metered dosage element for measuring a predetermined dose of the formulation, the element including an inlet from the reservoir and an outlet to the dispensing aperture; and d) an actuating element operating the dosage element so the predetermined dose is delivered to the dispensing aperture; wherein the dose is dispensed without microbial or other contamination or degradation of the formulation in reservoir. A corresponding course of treatment for various maladies includes providing a multidose package containing an imiquimod formulation suitable for the treatment. A corresponding method of treatment of diseases with multiple doses of an imiquimod formulation includes multiple doses provided by a multidose package.Type: GrantFiled: April 1, 2010Date of Patent: February 24, 2015Assignee: iNova Pharmaceuticals (Australia) Pty LimitedInventors: Mark J. Hutchings, Christiaan M. Van Niekerk
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Patent number: 8962620Abstract: The present invention relates to substituted 6,5-fused bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: November 4, 2013Date of Patent: February 24, 2015Assignee: Epizyme, Inc.Inventors: Kevin Wayne Kuntz, Edward James Olhava, Richard Chesworth, Kenneth William Duncan
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Publication number: 20150051209Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.Type: ApplicationFiled: August 5, 2014Publication date: February 19, 2015Applicant: NOVARTIS AGInventors: Mark Gary BOCK, Henrik MOEBITZ, Sunil Kumar PANIGRAHI, Ramulu PODDUTOORI, Susanta SAMAJDAR
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Publication number: 20150045374Abstract: The invention provides compounds and salts thereof as d herein. The invention also provides pharmaceutical compositions comprising a compound disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection, treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal using compounds disclosed herein.Type: ApplicationFiled: January 3, 2013Publication date: February 12, 2015Inventors: Kerim Babaoglu, Kyla L. Bjornson, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu
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Patent number: 8946279Abstract: The present invention belongs to the technical field of medicine, relating in particular to: a fused ring compound as represented by Formula (I) for use as a mineralocorticoid receptor antagonist, a pharmaceutically acceptable salt thereof, and an isomer thereof; a preparation method for these compounds; a pharmaceutical preparation containing these compounds; and an application of these compounds, the pharmaceutically acceptable salt thereof, or the isomers thereof in the preparation of medicants for the treatment and/or prevention of kidney injury, cardiovascular diseases such as hypertension, and/or endocrine disease. The definitions of X, Y1, Y2, Y3, R1, R2a, R2b, R3a, R3b, R4, Cy and n are as presented in the description.Type: GrantFiled: August 18, 2011Date of Patent: February 3, 2015Assignee: KBP Biosciences Co., Ltd.Inventors: Zhenhua Huang, Jinyuan Wang, Dedong Zhang
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Publication number: 20150030587Abstract: Methods of treating a head and neck cancer are disclosed.Type: ApplicationFiled: February 11, 2014Publication date: January 29, 2015Applicant: FOUNDATION MEDICINE, INC.Inventors: Chris Hendrik Boshoff, Timothy Robert Fenton, Matthias Alexander Lechner, Philip James Stephens, Matthew J. Hawryluk, Garrett Michael Frampton, Roman Yelensky
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Patent number: 8940737Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: October 11, 2012Date of Patent: January 27, 2015Assignee: AbbVie Inc.Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
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Patent number: 8940755Abstract: The present invention provides therapeutic combinations that include an immune response modifier (IRM) component and an anti-inflammatory component. The inventions further provide methods of treating a condition by administering to one having the condition a therapeutic combination that includes an IRM component and an anti-inflammatory component.Type: GrantFiled: December 2, 2004Date of Patent: January 27, 2015Assignee: 3M Innovative Properties CompanyInventors: Mark A. Tomai, Gary W. Gullikson, David M. Hammerbeck, Elaine A. Egging, Michael J. Reiter, Christopher D. Gram, John P. Vasilakos
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Publication number: 20150011579Abstract: The invention relates to novel heterocyclic compounds which are pyrazolopyridine derivatives that induce fibroblast growth factor receptor (FGFR) dimerization, having the general formula: M1-L-M2 in which M1 or M2, which may be identical or different, each represent, independently of one another, a monomer unit M and L represents a linker group which links M1 and M2 covalently with the monomer unit which follows: Process for the preparation thereof and therapeutic use thereof.Type: ApplicationFiled: December 26, 2012Publication date: January 8, 2015Inventors: Marie-Line Clary-Ceccato, Nathalie Guillo
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Publication number: 20140364443Abstract: Disclosed are 1,4-dihydro-naphthyridine derivatives and pharmaceutical composition and uses thereof. The 1,4-dihydro-naphthyridine derivatives are a compound capable of inhibiting acetylcholinesterase activity and preventing extracellular calcium from flowing into a cell via a calcium channel, i.e., having a dual-activity, which are of potential importance as a pharmaceutical and can be used to prepare the drugs for treating cardiovascular diseases, cerebrovascular diseases and dementia.Type: ApplicationFiled: December 7, 2012Publication date: December 11, 2014Applicant: Jiangsu Simovay Pharmaceutical Co., Ltd.Inventors: Rong Chen, Lin Feng, Zhengping Zhang, Fang Fang, Qingli Dong, Fulong Li, Lei Wang, Yao Hua, Shibao Yang, Peng Wang
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Patent number: 8906935Abstract: The present invention relates to substituted thiazolyl- and oxazolyl-isoquinolinones that act, for example, as modulators of poly(ADP-ribose) polymerase (PARP). The present invention also relates to processes for the preparation of substituted thiazolyl- and oxazolyl-isoquinolinones and to their use in treating various diseases and disorders.Type: GrantFiled: October 18, 2012Date of Patent: December 9, 2014Inventors: Roberto Pellicciari, Flavio Moroni, Adam Gilbert
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Publication number: 20140357615Abstract: In one aspect, the invention relates to substituted 1H-pyrazolo[3?,4?:4,5]thieno[2,3-b]pyridin-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); 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: ApplicationFiled: September 16, 2012Publication date: December 4, 2014Inventors: Jeffrey P. Conn, Craig W. Lindsley, Michael R. Wood, Corey R. Hopkins, James M. Salovich, Bruce J. Melancon
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Patent number: 8900566Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 18, 2013Date of Patent: December 2, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Makonen Belema, Van N. Nguyen
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Publication number: 20140350043Abstract: The invention relates to FSH receptor antagonist according to general formula (I) or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.Type: ApplicationFiled: September 14, 2012Publication date: November 27, 2014Inventors: Wesley Peter Blackaby, Martin De Kort, Mark Enthoven, Paul Stuart Hinchliffe, Christian Bernard Matthijs Poulie, Cornelis Marius Timmers, Saskia Verkaik
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Publication number: 20140349970Abstract: The invention provides a compound of Formula (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ii), (Ij), (Ik), or (Il) as defined herein, pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: ApplicationFiled: June 9, 2014Publication date: November 27, 2014Applicant: ABBVIE INC.Inventors: Neil Wishart, Maria A. Argiriadi, Eric C. Breinlinger, David J. Calderwood, Anna M. Ericsson, Bryan A. Fiamengo, Kristine E. Frank, Michael Friedman, Dawn M. George, Eric R. Goedken, Michael Z. Hoemann, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Kelly D. Mullen, Gagandeep Somal, Kent D. Stewart, Jeffrey W. Voss, Grier A. Wallace, Lu Wang, Kevin R. Woller
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Patent number: 8895580Abstract: The present invention is directed to quinolinone-pyrazolone compounds of formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.Type: GrantFiled: October 1, 2010Date of Patent: November 25, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Douglas C. Beshore, Scott D. Kuduk, Robert M. DiPardo
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Patent number: 8895579Abstract: Disclosed are heterotricyclic compounds, pharmaceutical compositions, methods of treatment, and methods for selectively antagonizing a glutamate receptor. The pharmaceutical compositions may include and the methods may utilize heterotricyclic compounds that are glutamate analogues which have specificity for AMPA receptors. The pharmaceutical compositions may be utilized to treat or prevent neurological diseases or disorders.Type: GrantFiled: March 21, 2011Date of Patent: November 25, 2014Assignee: Northwestern UniversityInventors: Geoffrey T. Swanson, Martin B. Gill, Ryuichi Sakai, Masato Oikawa
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Patent number: 8895581Abstract: The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.Type: GrantFiled: May 17, 2011Date of Patent: November 25, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Darryl McConnell, Harald Engelhardt, Christiane Kofink
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Publication number: 20140343092Abstract: Provided are compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections mediated by a member of the retrovirus family of viruses such as the Human Immunodeficiency Virus (HIV).Type: ApplicationFiled: September 18, 2012Publication date: November 20, 2014Inventors: Simon N. Haydar, Brian Alvin Johns, Emile Johann Velthuisen
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Patent number: 8889675Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-xL protein.Type: GrantFiled: October 11, 2012Date of Patent: November 18, 2014Assignee: AbbVie Inc.Inventors: Le Wang, George Doherty, Xilu Wang, Zhi-Fu Tao, Milan Bruncko, Aaron R. Kunzer, Michael D. Wendt, Xiaohong Song, Robin Frey, Todd M. Hansen, Gerard M. Sullivan, Andrew Judd, Andrew Souers
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Patent number: 8889867Abstract: The present invention provides amorphous solid forms of the compound of Formula I, as well as methods for preparing the compound of Formula I by precipitation.Type: GrantFiled: May 7, 2013Date of Patent: November 18, 2014Assignee: Corcept Therapeutics, Inc.Inventors: Robin Clark, Doug Fry
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Patent number: 8889154Abstract: A packaged composition of 1-(2-methylpropyl)-1H-imidazo[4,5-c]quinolin-4-amine dissolved in a fatty acid formulation and contained in a laminated packaging material having a contact layer that includes an acrylonitrile-methyl acrylate copolymer; an outer layer; and a moisture barrier layer disposed between the contact layer and outer layer.Type: GrantFiled: September 12, 2006Date of Patent: November 18, 2014Assignee: Medicis Pharmaceutical CorporationInventors: Alexis S. Statham, Julie M. Henderson, Kevin G. Lundquist
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Publication number: 20140328823Abstract: The present invention relates to the use of a 2,5-dihydroxybenzene derivative of formula (I) or a pharmaceutically acceptable salt, solvate, isomer, or prodrug thereof for the treatment and/or prophylaxis of, inter alia, skin cancer.Type: ApplicationFiled: July 15, 2014Publication date: November 6, 2014Inventors: Pedro Cuevas Sànchez, Guillermo Gimenez Gallego, Inigo Saenz de Tejada Gorman, Javier Angulo Frutos, Serafin Valverde Lopez, Antonio Romero Garrido, Rosa Maria Lozano Puerto
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Publication number: 20140329800Abstract: The present invention relates to a tri-heterocyclic derivatives, preparation process and uses thereof, specifically relates to a tri-heterocyclic derivatives of the formula (I) or a pharmaceutically acceptable salt thereof, preparation process, and further relates to a pharmaceutically acceptable composition comprising compounds of formula (I), or a pharmaceutically acceptable salt thereof, and their pharmaceutical use as inhibitors of kinase.Type: ApplicationFiled: December 13, 2012Publication date: November 6, 2014Inventors: Daxin Gao, Heping Yang, Yajun Yu