Three Or More Ring Hetero Atoms In The Tricyclo Ring System Patents (Class 546/82)
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Publication number: 20150141625Abstract: The present invention provides IRM conjugates that includes an IRM moiety and a second active moiety covalently linked to the IRM moiety in which the covalent link does not depend on UV irradiation.Type: ApplicationFiled: January 20, 2015Publication date: May 21, 2015Inventors: Doris Stoermer, George W. Griesgraber, James D. Mendoza, Jason D. Bonk
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Patent number: 9034336Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.Type: GrantFiled: August 30, 2012Date of Patent: May 19, 2015Assignee: Regents of the University of MinnesotaInventors: David M. Ferguson, John Ohlfest, Courtney Aldrich
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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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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: 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: 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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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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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: 8946421Abstract: The compounds of the subject invention are adjuvant molecules that comprise an imidazoquinoline molecule covalently linked to a phospho- or phosphonolipid group. The compounds of the invention have been shown to be inducers of interferon-a, IL-12 and other immunostimulatory cytokines and possess an improved activity profile in comparison to known cytokine inducers when used as adjuvants for vaccine antigens.Type: GrantFiled: December 20, 2013Date of Patent: February 3, 2015Assignee: GlaxoSmithKline Biologicals S.A.Inventor: David A. Johnson
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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: 20150030540Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.Type: ApplicationFiled: October 14, 2014Publication date: January 29, 2015Inventors: Anna Katrin Szardenings, Hartmuth C Kolb, Joseph C Walsh, Gang Chen, Umesh B Gangadharmath, Dhanalakshmi Kasi, Changhui Liu, Anjana Sinha, Eric Wang, Chul Yu, Wei Zhang, Kai Chen, Vani P Mocharla, Peter J. H. Scott
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Publication number: 20150023990Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.Type: ApplicationFiled: September 30, 2014Publication date: January 22, 2015Inventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah J. Slania
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Patent number: 8932557Abstract: Disclosed here in are compounds and methods of diagnosing Alzheimer's Disease or a predisposition thereto in a mammal, the method comprising administering to the mammal a diagnostically effective amount of a radiolabeled compound, wherein the compound is selected from the group consisting of radiolabeled carbazoles and derivatives thereof and triazoles derivatives, allowing the compound to distribute into the brain tissue, and imaging the brain tissue, wherein an increase in binding of the compound to the brain tissue compared to a normal control level of binding indicates that the mammal is suffering from or is at risk of developing Alzheimer's Disease.Type: GrantFiled: May 22, 2012Date of Patent: January 13, 2015Assignee: Eli Lilly and CompanyInventors: Gang Chen, Umesh B. Gangadharmath, Dhanalakshmi Kasi, Anjana Sinha, Wei Zhang, Kai Chen, Vani P. Mocharla
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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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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: 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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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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Publication number: 20140336385Abstract: Provided herein are organic compounds useful in a variety of OLED applications.Type: ApplicationFiled: December 12, 2012Publication date: November 13, 2014Inventors: Ivan Abrahamian, Xin Su
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Patent number: 8877747Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: GrantFiled: October 21, 2009Date of Patent: November 4, 2014Assignee: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
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Patent number: 8871782Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.Type: GrantFiled: October 1, 2004Date of Patent: October 28, 2014Assignee: 3M Innovative Properties CompanyInventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah C. Johannessen
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Patent number: 8865713Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: September 3, 2013Date of Patent: October 21, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 8859774Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: GrantFiled: May 24, 2013Date of Patent: October 14, 2014Assignee: Corcept Therapeutics, Inc.Inventors: Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
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Patent number: 8853391Abstract: Disclosed are dipyridyl-pyrrole derivative compounds and analogs thereof, pharmaceutical compositions comprising such compounds and processes for preparing the same. The compounds are useful in the treatment of diseases amenable to protein kinase signal transduction inhibition, regulation and/or modulation.Type: GrantFiled: December 3, 2009Date of Patent: October 7, 2014Assignee: Merck Patent GmbHInventors: Bayard R. Huck, Amanda E. Sutton, Benny C. Askew, Jr., Christopher Charles Victor Jones, Garry R. Smith, Nadia Brugger
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Patent number: 8846709Abstract: Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.Type: GrantFiled: April 19, 2012Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Emmanuel Hubert Demont, Katherine Louise Jones, Robert J. Watson
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Patent number: 8846710Abstract: A method of preferentially inducing IFN-? biosynthesis in an animal comprising administering certain imidazo[4,5-c] ring compounds with a hydroxymethyl or hydroxyethyl substituent at the 2-position or pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of using these compounds a immunomodulators for treatment of diseases including viral and neoplastic diseases comprising preferentially inducing IFN-? biosynthesis in an animal are disclosed.Type: GrantFiled: February 22, 2006Date of Patent: September 30, 2014Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Bryon A. Merrill, Scott E. Langer, Kyle J. Lindstrom, Sarah C. Slania, Gregory J. Marszalek, Joshua R. Wurst, Karl J. Manske, Shri Niwas, Gregory D. Lundquist, Jr., Philip D. Heppner, George W. Griesgraber, Michael E. Danielson
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Publication number: 20140286988Abstract: 1H-Imidazo[4,5-c]quinolin-4-amines substituted at the 1-position with a substituent bearing a hydrazinobenzamide or hydrazinonicotinamide, a salt thereof, or a protected hydrazinobenzamide or hydrazinonicotinamide and conjugates made from such compounds are disclosed. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed.Type: ApplicationFiled: June 1, 2012Publication date: September 25, 2014Applicant: 3M Innovative Properties CompanyInventor: Paul D. Wightman
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Publication number: 20140288062Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Publication number: 20140256922Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.Type: ApplicationFiled: May 16, 2014Publication date: September 11, 2014Inventors: Sunil David, Nikunj M. Shukla
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Publication number: 20140249143Abstract: Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: GlaxoSmithKline LLCInventors: Anna Lindsey Banka, Janos Botyanszki, Eric Gregory Burroughs, John George Catalano, Wendy Huang Chern, Hamilton D. Dickson, Margaret J. Gartland, Robert Hamatake, Hans Hofland, Jesse Daniel Keicher, Christopher Brooks Moore, John Bradford Shotwell, Matthew David Tallant, Jean-Philippe Therrien, Shihyun You
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Patent number: 8822448Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: GrantFiled: March 7, 2013Date of Patent: September 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
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Publication number: 20140243321Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Coferon, Inc.Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
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Publication number: 20140243322Abstract: Described herein are compounds capable of modulating one or more biomolecules substantially simultaneously, e.g., modulating two or more binding domains (e.g., bromodomains) on a protein or on different proteins.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Coferon, Inc.Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
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Publication number: 20140235616Abstract: The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.Type: ApplicationFiled: September 24, 2012Publication date: August 21, 2014Applicant: SANOFIInventors: Alexandre Benazet, Olivier Duclos, Nathalie Guillo, Gilbert Lassalle, Karim Macary, Valerie Vin
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Publication number: 20140227317Abstract: Conjugates of an immune response modifier, a linker, and an antigen are disclosed. The linker is represented by formula (I): wherein A is CH or N, p is in a range from 1 to 50, R? is a bond or -alkylene-O—, R? is alkylene that is optionally interrupted or terminated with one or more amide or ether groups, and E is an amine- or thiol-reactive group. Pharmaceutical compositions containing the compound or the conjugate, methods of making a conjugate, and methods of use of the compounds or conjugates as immunomodulators for inducing cytokine biosynthesis in an animal and for vaccinating an animal are also disclosed. An antigen modified by the linker is also disclosed.Type: ApplicationFiled: June 1, 2012Publication date: August 14, 2014Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventor: Paul D. Wightman
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Patent number: 8802712Abstract: The invention relates to compounds of the formulae (I), (II) and (III), 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 sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.Type: GrantFiled: June 24, 2011Date of Patent: August 12, 2014Assignee: Merck Patent GmbHInventors: Thomas Fuchss, Werner Mederski, Frank Zenke
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Publication number: 20140213610Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: ApplicationFiled: August 27, 2013Publication date: July 31, 2014Applicant: AbbVie Inc.Inventors: Thomas D. Penning, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda
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Publication number: 20140212442Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.Type: ApplicationFiled: August 30, 2012Publication date: July 31, 2014Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTAInventors: David M. Ferguson, John Ohlfest, Courtney Aldrich
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Patent number: 8791131Abstract: The present invention is directed to compounds of Formula (I), and to salts thereof, their synthesis, and their use as PI3-K? inhibitors and/or PI3-K?/mTOR dual inhibitors.Type: GrantFiled: September 18, 2009Date of Patent: July 29, 2014Assignee: Pfizer Inc.Inventors: Hengmiao Cheng, Ted William Johnson, Jacqui Elizabeth Hoffman, Lisa Chen Guo, Zhengyu Liu
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Patent number: 8791133Abstract: The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.Type: GrantFiled: October 16, 2012Date of Patent: July 29, 2014Assignee: SanofiInventors: Karl Schoenafinager, Henning Steinhagen, Bodo Scheiper, Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Jacques Mauger, Pavel Safar
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Patent number: 8785639Abstract: The invention provides a compound of Formula (Ie), pharmaceutically acceptable salts, or stereoisomers thereof wherein the variables are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.Type: GrantFiled: December 1, 2010Date of Patent: July 22, 2014Assignee: AbbVie Inc.Inventors: Neil Wishart, Maria A. Argiriadi, David J. Calderwood, Anna M. Ericsson, Kristine E. Frank, Dawn M. George, Eric R. Goedken, Michael Friedman, Nathan S. Josephsohn, Biqin C. Li, Michael J. Morytko, Jeffrey W. Voss, Lu Wang, Eric C. Breinlinger, Kelly D. Mullen, Gagandeep Somal, Michael Z Hoemann
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Patent number: 8785429Abstract: Disclosed are JAK inhibitors of formula I where G1, R1, R2, R3, R4, R5, R6, and R7 are defined in the specification. Also disclosed are pharmaceutical compositions, kits and articles of manufacture which contain the compounds, methods and materials for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions involving the immune system and inflammation, including rheumatoid arthritis, hematological malignancies, epithelial cancers (i.e., carcinomas), and other diseases, disorders or conditions associated with JAK.Type: GrantFiled: March 6, 2013Date of Patent: July 22, 2014Inventors: John David Lawson, Toufike Kanouni, Michael B. Wallace, Qing Dong
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Publication number: 20140200344Abstract: Novel tricyclic pyrimidine compounds and tricyclic pyridine compounds having JAK inhibitory activities are provided. A tricyclic heterocyclic compound represented by the formula (Ia): wherein the rings Aa and Ba, Xa, Ya, R1a, R2a, R3a, L1a L2a, L3a and na are as defined in the description.Type: ApplicationFiled: August 10, 2012Publication date: July 17, 2014Applicant: Nissan Chemical Industries, Ltd.Inventors: Keishi Hayashi, Tsuneo Watanabe, Koji Toyama, Junji Kamon, Masataka Minami, Miyuki Uni, Mariko Nasu
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Publication number: 20140194414Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 8, 2013Publication date: July 10, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: MEDIVATION TECHNOLOGIES, INC.
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Publication number: 20140194628Abstract: Imidazo ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, methods of making the 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: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: 3M INNOVATIVE PROPERTIES COMPANYInventors: Larry R. Krepski, Joseph F. Dellaria, Jr., Daniel E. Duffy, Matthew R. Radmer, David T. Amos