Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/278)
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Patent number: 9006253Abstract: The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal. The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.Type: GrantFiled: March 26, 2014Date of Patent: April 14, 2015Assignee: ASKA Pharmaceutical Co., Ltd.Inventors: Hiroyuki Hayashi, Takayoshi Nakagawa, Koichi Miyazaki
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Patent number: 8999973Abstract: The present invention relates to a thieno[3,2-d]pyrimidine derivative of formula (I), or a pharmaceutically acceptable salt, hydrate or solvate thereof, which has an excellent inhibitory activity on protein kinases, and a pharmaceutical composition comprising the same is effective in preventing or treating abnormal cell growth diseases.Type: GrantFiled: January 31, 2011Date of Patent: April 7, 2015Assignees: Hanmi Science Co., Ltd, Korea Institute of Science and Technology, Catholic University Industry Academic Cooperation FoundationInventors: Jung Beom Son, Seung Hyun Jung, Wha II Choi, Young Hee Jung, Jae Yul Choi, Ji Yeon Song, Kyu Hang Lee, Jae Chul Lee, Eun Young Kim, Young Gil Ahn, Maeng Sup Kim, Hwan Geun Choi, Tae Bo Sim, Young Jin Ham, Dong-sik Park, Hwan Kim, Dong-Wook Kim
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Publication number: 20150094275Abstract: The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: ApplicationFiled: November 13, 2014Publication date: April 2, 2015Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
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Patent number: 8987278Abstract: The present invention is related to novel thienopyrimidinedione derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: GrantFiled: June 25, 2013Date of Patent: March 24, 2015Assignee: Glenmark Pharmaceuticals S.A.Inventors: Sukeerthi Kumar, Abraham Thomas, Nayan Taterao Waghmare, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
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Publication number: 20150080416Abstract: This invention provides thieno[2,3-d]pyrimidine derivatives containing isoxazole heterocycle represented by formula (I), or pharmaceutically acceptable salts thereof Wherein: R1 and R2 may be the same or different and is independently to each other selected from H, C1-6 alkyl, C1-6 alkoxy, halo-C1-6 alkyl or halo-C1-6 alkoxy, aryl group optionally substituted by R7 or heteroaryl group optionally substituted by R8; or R1 and R2 together with the carbon atoms to which they are attached, may form a 4- to 6-membered carbocyclic ring or heterocyclic ring; said carbocyclic ring or heterocyclic ring is optionally substituted by H, C1-6 alkyl, halogen, nitro, or amino; said heterocyclic ring contains at least one heteroatom selected from N, O or S; Z is —NR6—, C(R6)2, —S— or —O—, in which R5 is H or C1-6 alkyl, and R6 is the same or different, selected from H, C1-6 alkyl or hydroxyl substituted C1-6 alkyl; R3 is selected from H, halogen, C1-6 alkyl, C1-6 alkoxy, halo-C1-6 alkyl or halo-C1-6 alkoxy; n is an inteType: ApplicationFiled: September 19, 2012Publication date: March 19, 2015Applicant: FUJIAN INSTITUTE OF RESEARCH ON THE STRUCTURE OF MATTER, CHINESE ACADEMY OF SCIENCESInventors: Canzhong Lu, Jianping Yong
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Patent number: 8981084Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, Y, Q, X, B and L are as defined herein, and methods of making and using the same.Type: GrantFiled: January 13, 2011Date of Patent: March 17, 2015Assignee: Tempero Pharmaceuticals, Inc.Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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Publication number: 20150072998Abstract: Compounds and methods of modulating 15-PGDH activity, modulating tissue prostaglandin levels, treating disease, diseases disorders, or conditions in which it is desired to modulate 15-PGDH activity and/or prostaglandin levels include 15-PGDH inhibitors and 15-PGDH activators described herein.Type: ApplicationFiled: April 16, 2013Publication date: March 12, 2015Inventors: Sanford Markowitz, James K.V. Willson, Bruce A. Posner, Joseph Ready, Yongyou Zhang, Hsin-Hsiung Tai, Melissa Moss, Monika Antczak, Stanton Gerson, KiBeom Bae, Sung Yeun Yang, Amar Desai
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Publication number: 20150072959Abstract: Substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.Type: ApplicationFiled: November 13, 2014Publication date: March 12, 2015Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
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Publication number: 20150065501Abstract: The invention relates to N-substituted hetero-bicyclic furanone compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these N-substituted hetero-bicyclic furanone compounds, and of compositions comprising thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such N-substituted hetero-bicyclic furanone compounds. The N-substituted hetero-bicyclic furanone compounds of the present invention are defined by the following formula I: wherein A, X, Het, W1, W2, W3, R1, R2 and R4 are defined as in the description.Type: ApplicationFiled: March 27, 2013Publication date: March 5, 2015Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
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Patent number: 8969363Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein.Type: GrantFiled: July 18, 2012Date of Patent: March 3, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Alfredo C. Castro, Catherine A. Evans, Somarajannair Janardanannair, Andre Lescarbeau, Tao Liu, Daniel A. Snyder, Martin R. Tremblay, Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan
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Patent number: 8969557Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.Type: GrantFiled: November 9, 2012Date of Patent: March 3, 2015Assignee: Nimbus Apollo, Inc.Inventors: Geraldine C. Harriman, Craig E. Masse, James Harwood, Sathesh Bhat, Jeremy Robert Greenwood
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Publication number: 20150057286Abstract: This invention relates to bis-amido pyridines of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R4 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Ulrich REISER
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Publication number: 20150057260Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: ApplicationFiled: August 22, 2014Publication date: February 26, 2015Applicant: Genentech, Inc.Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Xingyu Lin, Jason Burch
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Publication number: 20150057295Abstract: This invention relates to 6-alkynyl-pyridine of general formula (I) their use as SMAC mimetics, pharmaceutical compositions containing them, and their use as a medicaments for the treatment and/or prevention of diseases characterized by excessive or abnormal cell proliferation and associated conditions such as cancer. The groups R1 to R5 have the meanings given in the claims and in the specification.Type: ApplicationFiled: August 20, 2014Publication date: February 26, 2015Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ulrich REISER, James MADDEN
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Publication number: 20150045377Abstract: The present invention relates to compounds that are useful as inhibitors of the activity of one or more isoforms of the serine/threonine kinase, AKT. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.Type: ApplicationFiled: March 25, 2013Publication date: February 12, 2015Inventors: Timothy Harrison, Colin O'Dowd, Steven Shepherd, Graham Trevitt, Lixin Zhang, Frank Burkamp
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Publication number: 20150045324Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.Type: ApplicationFiled: October 23, 2014Publication date: February 12, 2015Applicant: HANMI SCIENCE CO., LTDInventors: Mi Young CHA, Seok Jong KANG, Mi Ra KIM, Ju Yeon LEE, Ji Young JEON, Myoung Gi JO, Eun Joo KWAK, Kwang Ok LEE, Tae Hee HA, Kwee Hyun SUH, Maeng Sup KIM
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Patent number: 8946239Abstract: The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of formula III, and 5,6-saturated and unsaturated and pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.Type: GrantFiled: July 10, 2008Date of Patent: February 3, 2015Assignee: Duquesne University of the Holy SpiritInventor: Aleem Gangjee
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Publication number: 20150031709Abstract: Provided herein are thiophene compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.Type: ApplicationFiled: February 8, 2013Publication date: January 29, 2015Applicant: SUNOVION PHARMACEUTICALS, INC.Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
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Patent number: 8940752Abstract: The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: GrantFiled: June 28, 2010Date of Patent: January 27, 2015Assignee: Incyte CorporationInventors: Yun-Long Li, Brian W. Metcalf
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Publication number: 20150025070Abstract: The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.Type: ApplicationFiled: July 13, 2012Publication date: January 22, 2015Applicant: Novartis AGInventors: Atwood Kim Cheung, Donovan Noel Chin, Jianmei Fan, Karen Marie Miller-Moslin, Michael David Shultz, Troy D. Smith, Ronald Charles Tomlinson, Bakary-Barry Toure, Michael Scott Visser
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Patent number: 8937075Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: January 20, 2015Assignee: Janssen Pharmaceutica, NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Publication number: 20150018350Abstract: The present invention relates to N-containing heterocyclic compounds that are inhibitors of protein kinases including JAK kinases. In particular, the compounds are selective for JAK1, JAK2, JAK3 or TYK2 kinases and combinations thereof such as JAK1 and JAK2. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: May 15, 2014Publication date: January 15, 2015Inventors: David G. Bourke, Christopher J. Burns, Anthony N. Cuzzupe, John T. Feutrill, Marcel R. Kling, Tracy L. Nero
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Patent number: 8933084Abstract: Compounds of Formula I: and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R2, R2a, R3, R3a, and Z are as defined herein, are inhibitors of Trk kinases and are useful in the treatment of pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: GrantFiled: May 13, 2011Date of Patent: January 13, 2015Assignee: Array BioPharma Inc.Inventors: Steven Wade Andrews, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Gabrielle R. Kolakowski, Jeongbeob Seo, HongWoon Yang, Qian Zhao
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Patent number: 8927555Abstract: Thieno- and furo-pyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the modulation of histamine H4 receptor activity and for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as inflammation.Type: GrantFiled: April 25, 2012Date of Patent: January 6, 2015Assignee: Janssen Pharmaceutica, NVInventors: James P. Edwards, Danielle K. Neff, Deborah M. Smith, Jennifer D. Venable
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Patent number: 8921336Abstract: The present invention provides novel heteroaryl compounds of formula (I) having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.Type: GrantFiled: November 28, 2008Date of Patent: December 30, 2014Assignees: Dana-Farber Cancer Institute, Inc., The Scripps Research InstituteInventors: Nathanael Gray, Jianming Zhang, Barun Okram, Xianming Deng, Jae Won Chang
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Publication number: 20140378475Abstract: Disclosed are compounds of Formula (I) wherein: the two dotted lines represent either two single or two double bonds; Q is: R1 is F, Cl, —CN, or —CH3; R2 is Cl or —CH3; R3 is —C(CH3)2OH or —CH2CH2OH; Ra is H or —CH3; each Rb is independently F, Cl, —CH3, and/or —OCH3; and n is zero, 1, or 2. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: June 25, 2014Publication date: December 25, 2014Inventors: Douglas G. Batt, Myra Beaudoin Bertrand, George Delucca, Michael A. Galella, Soo Sung Ko, Charles M. Langevine, Qingjie Liu, Qing Shi, Anurag S. Srivastava, Joseph A. Tino, Scott Hunter Watterson
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Patent number: 8916554Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: July 22, 2013Date of Patent: December 23, 2014Assignee: Janssen Pharmaceutica, N.V.Inventors: Patrick René´ Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
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Publication number: 20140371219Abstract: Provided are a thieno[3,2-d]pyrimidine derivative of formula (I) or a pharmaceutically acceptable salt thereof having inhibitory activity for protein kinase, and a pharmaceutical composition comprising same for prevention and treatment of abnormal cell growth diseases.Type: ApplicationFiled: December 27, 2012Publication date: December 18, 2014Applicant: HANMI PHARM. CO., LTDInventors: In Hwan Bae, Jung Beom Son, Sang Mi Han, Eun Joo Kwak, Ho Seok Kim, Ji Young Song, Eun Young Byun, Seung Ah Jun, Young Gil Ahn, Kwee Hyun Suh
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Publication number: 20140371203Abstract: The present invention provides compounds of formula (I): (Formula (I); wherein A, R1, R2, R3I, V, X, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.Type: ApplicationFiled: November 15, 2012Publication date: December 18, 2014Inventors: David Madge, Fiona Chan, Derek Edward John, Simon D. Edwards, Richard Blunt, Basil Hartzoulakis, Lindsay Brown
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Publication number: 20140350034Abstract: The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; in free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.Type: ApplicationFiled: January 25, 2013Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Trixi Brandl, Stefanie Flohr, Christian Markert, Kenji Namoto, Bernard Pirard, Martin Renatus
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Publication number: 20140350033Abstract: ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrimidinone of formula I wherein R1 is —(CH2)n-CO—OH; —(CH2)n-CO—OR; —(CH2)n-CO—NHR; —(CH2)n-CO—N(R, R?); —(CH2)n-OH; —(CH2)n-OR; —(CH2)n-OAr; —(CH2)n-C(R,R?)—(CH2)n-OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.Type: ApplicationFiled: June 5, 2014Publication date: November 27, 2014Applicants: MITOLOGICS, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE VERSAILLES-SAINT QUENTIN-EN-YVELINES (UVSQ)Inventors: Annie BORGNE-SANCHEZ, Etienne JACOTOT, Catherine BRENNER
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Patent number: 8895729Abstract: Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 9, 2013Date of Patent: November 25, 2014Assignee: Genentech, Inc.Inventors: Srinivasan Babu, Zhigang Cheng, Francis Gosselin, Pirmin Hidber, Ursula Hoffmann, Theresa Humphries, Reinhard Reents, Qingping Tian, Herbert Yajima
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Patent number: 8889862Abstract: The present invention is related to 2-amino-4-arylthiazole derivatives as TRPA (Transient Receptor Potential subfamily A) modulators. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by TRPA1 (Transient Receptor Potential subfamily A, member 1). Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by TRPA1.Type: GrantFiled: October 21, 2013Date of Patent: November 18, 2014Assignee: Glenmark Pharmaceuticals, S.A.Inventors: Sukeerthi Kumar, Abraham Thomas, Sachin Sundarlal Chaudhari, Bipin Parsottam Kansagra, Venkata Ramana Yemireddy, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay, Girish Gudi
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Patent number: 8883781Abstract: The present invention relates to compounds of formula IA-i useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: June 12, 2007Date of Patent: November 11, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lev T. D. Fanning, Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson, Yulian Zhang
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Publication number: 20140323466Abstract: Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.Type: ApplicationFiled: October 23, 2012Publication date: October 30, 2014Inventors: Hong Liu, Jia Li, Jian Li, Jingya Li, Jiang Wang, Mingbo Su, Jie Lian, Hualiang Jiang, Kaixian Chen
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Publication number: 20140323435Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: ApplicationFiled: May 22, 2014Publication date: October 30, 2014Applicants: Cancer Research Technology Limited, Cephalon, Inc.Inventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R.A. Roffey, Christelle N. Soudy, Jason C. Wagner
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Publication number: 20140323503Abstract: The present intervention generally relates to compositions comprising a PDE11 inhibitor for increasing cortisol levels in a subject, or for increasing the production of cortisol from adenocortical cells in a subject. Aspects of the invention relate to the use of a PDE11 inhibitor in a method of treatment of low cortisol levels and/or adrenal insufficiency in a subject, or a method of treating a disease or disorders associated with adrenal insufficiency. Aspects of the invention relate to PDE11 inhibitors belonging to compounds of formula (I)-(VI), and their use alone or in combination with long-term corticosteroid treatment to elevate cortisol levels in a subject, and/or to treat adrenal insufficiency.Type: ApplicationFiled: November 29, 2012Publication date: October 30, 2014Inventors: Charles Stuart Hoffman, Ozge Ceyhan
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Patent number: 8865623Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: GrantFiled: January 6, 2010Date of Patent: October 21, 2014Assignee: Syngenta LimitedInventors: Christopher John Mathews, John Finney, James Nicholas Scutt, Louisa Robinson, John Stephen Delaney
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Publication number: 20140309222Abstract: A series of monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.Type: ApplicationFiled: August 15, 2012Publication date: October 16, 2014Applicants: KATHOLIEKE UNIVERSITEIT LEUVEN, K.U.LEUVEN R&D, UCB PHARMA S.A.Inventors: Daniel Christopher Brookings, Daniel James Ford, Anant Ramrao Ghawalkar, Jean Herman, Qiuya Huang, Claire Louise Kulisa, Thierry Louat, Judi Charlotte Neuss, James Thomas Reuberson, Bart Vanderhoydonck
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Publication number: 20140303149Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.Type: ApplicationFiled: April 2, 2014Publication date: October 9, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Andreas Kuglstatter, Sharada Shenvi Labadie, Clara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai
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Patent number: 8853193Abstract: The present invention relates to novel thienopyrimidine compounds of general formula pharmaceutical compositions comprising these compounds and their therapeutic use for the prophylaxis and/or treatment of diseases which can be influenced by the inhibition of the kinase activity of Mnk1 and/or Mnk2 (Mnk2a or Mnk2b) and/or variants thereof.Type: GrantFiled: February 25, 2011Date of Patent: October 7, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Armin Heckel, Frank Himmelsbach, Joerg Kley, Thorsten Lehmann-Lintz, Norbert Redemann, Achim Sauer, Leo Thomas, Dieter Wiedenmayer, Phillip Black, Wesley Blackaby, Ian Linney, Matthias Austen, John Danilewicz, Martin Schneider, Kay Schreiter
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Patent number: 8853208Abstract: The invention relates to amino alcohol-substituted arylthienopyrimidinones having a formula I and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one amino alcohol-substituted arylthienopyrimidinone of the invention or its derivative, and the use of the amino alcohol-substituted arylthienopyrimidinones of the invention and their derivatives as MCH antagonists.Type: GrantFiled: August 14, 2008Date of Patent: October 7, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Publication number: 20140288071Abstract: Compounds are disclosed for the treatment, management and prevention of diseases and disorders affecting the bone. Particular compounds are potent inhibitors of Notum Pectinacetylesterase, and are of the formula: wherein E, G, Y, Z, R1, R2, and R3 are defined herein.Type: ApplicationFiled: June 10, 2014Publication date: September 25, 2014Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Wei HE, Victoria LOMBARDO, Praveen PABBA, James TARVER, JR.
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Publication number: 20140275070Abstract: The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin).Type: ApplicationFiled: March 10, 2014Publication date: September 18, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li
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Patent number: 8828991Abstract: The invention relates to azacyclyl-substituted arylthienopyrimidinones and their derivatives, of the Formula (I); and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one azacyclyl-substituted arylthienopyrimidinone according to Formula (I) or its derivative, and the use of the azacyclyl-substituted arylthienopyrimidinones according to Formula (I) and their derivatives as MCH antagonists.Type: GrantFiled: August 14, 2008Date of Patent: September 9, 2014Assignee: SanofiInventors: Lothar Schwink, Siegfried Stengelin, Matthias Gossel, Gerhard Hessler, Torsten Haack, Petra Lennig
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Patent number: 8822474Abstract: The invention relates to new dihydrothienopyrimidine of formula 1, as well as pharmacologically acceptable salts, diastereomers, enantiomers, racemates, hydrates or solvates thereof, wherein X is SO or SO2, but preferably SO, and wherein R1, R2 and R3 have the meanings given in the description, and which are suitable for the treatment of respiratory or gastrointestinal complaints or diseases, inflammatory diseases of the joints, skin or eyes, diseases of the peripheral or central nervous system or cancers, as well as pharmaceutical compositions which contain these compounds.Type: GrantFiled: September 5, 2013Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Pascale Pouzet, Christoph Hoenke, Rolf Goeggel, Birgit Jung, Peter Nickolaus, Dennis Fiegen, Thomas Fox
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Publication number: 20140235615Abstract: Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.Type: ApplicationFiled: March 24, 2014Publication date: August 21, 2014Applicant: Takeda Pharmaceutical Company LimitedInventors: Misaki HOMMA, Toru MIYAZAKI, Yuya OGURO, Osamu KURASAWA
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Publication number: 20140235650Abstract: The invention relates to a compound of formula (I), where R1, R2, R7, m, n, and L1 are as defined in claim 1, and to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.Type: ApplicationFiled: June 22, 2012Publication date: August 21, 2014Applicant: MetabolysInventors: Gerard Moinet, Gabriel Baverel, Remi Nazaret, Bernard Ferrier
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Publication number: 20140235655Abstract: The invention provides a crystal of 2-(3,4-dichlorobenzyl)-5-methyl-4-oxo-3,4-dihydrothieno[2,3-d]pyrimidine-6-carboxylic acid (which has the chemical structure shown below) and a mixed crystal comprising such a crystal. The invention also provides methods of producing such crystals, pharmaceutical compositions comprising such crystals, and methods of modulating phosphodiesterase-9 activity and treating disorders such as overactive bladder syndrome by administration of an effective amount of the crystals.Type: ApplicationFiled: March 26, 2014Publication date: August 21, 2014Applicant: ASKA Pharmaceutical Co., Ltd.Inventors: Hiroyuki HAYASHI, Takayoshi NAKAGAWA, Koichi MIYAZAKI
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Patent number: 8809346Abstract: The invention relates to molecules ANT-ligands having a substituted nitrogeneous heterocycle A wherein A is a substituted pyrazinone of formula I wherein R1 is —(CH2)n—CO—OH; —(CH2)n—CO—OR; —(CH2)n—CO—NHR; —(CH2)n—CO—N(R,R?); —(CH2)n—OH; —(CH2)n—OR; —(CH2)n—OAr; —(CH2)n—C(R,R?)—(CH2)n—OH, R and R?, in the above radicals, being identical or different and representing H or a C1-C12 alkyl or cycloalkyl radical; and Ar is a phenyl or Het., Het.Type: GrantFiled: May 29, 2009Date of Patent: August 19, 2014Assignees: Universite de Versailles-Saint-Quentin-en-Yvelines, Center National de la Recherche Scientifique (CNRS), MitologicsInventors: Annie Borgne-Sanchez, Etienne Jacotot, Catherine Brenner