Plural Ring Nitrogens In The Additional Hetero Ring (e.g., Imidazole, Pyrazine, Etc.) Patents (Class 514/235.8)
-
Patent number: 9095590Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: GrantFiled: March 31, 2014Date of Patent: August 4, 2015Assignee: AbbVie Inc.Inventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
-
Patent number: 9062035Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is c1-6 alkyl; R2 is hydroxy, c1-6 alkyl that may have one or more substituents, —(C?O)—N(R2)(R4), or —(C?O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or c1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or c1-6 alkyl that may have one or more 15 substituents; and n is 1 or 2; or a salt thereof.Type: GrantFiled: January 8, 2014Date of Patent: June 23, 2015Assignee: Taiho Pharmaceutical Co., Ltd.Inventors: Yoshihiro Urade, Makoto Kitade, Kazuhiko Shigeno, Keiko Yamane, Katsunao Tanaka
-
Publication number: 20150148327Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.Type: ApplicationFiled: June 17, 2013Publication date: May 28, 2015Applicant: Merck Canada Inc.Inventors: Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio, Joel Robichaud
-
Publication number: 20150148345Abstract: Provided herein are methods, compositions, and kits for treating myeloproliferative disorders or neoplasms, including polycythemia vera, primary myelofibrosis, thrombocythemia, and essential thrombocythemia.Type: ApplicationFiled: November 25, 2014Publication date: May 28, 2015Inventors: Brian Lannutti, Sarah Meadows, Christophe Queva, Matthew Robert Warr, James Andrew Whitney
-
Publication number: 20150148330Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: January 16, 2015Publication date: May 28, 2015Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
-
Publication number: 20150141427Abstract: The present invention relates to compounds of formula I: in which Y, Y1, Y4, Y5, Y6, R1, R2, R3 and R4 are defined in the Summary of the Invention; capable of inhibiting the activity of BCR-ABL1 and mutants thereof. 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 in the treatment of cancers.Type: ApplicationFiled: May 9, 2013Publication date: May 21, 2015Applicant: Novartis AGInventors: Pascal Furet, Robert Martin Grotzfeld, Wolfgang Jahnke, Darryl Brynley Jones, Paul William Manley, Andreas Marzinzik, Saliha Moussaoui, Xavier Francois Andre Pelle, Bahaa Salem, Joseph Schoepfer
-
Publication number: 20150141428Abstract: The present invention is directed to benzyl urea compounds, which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C.Type: ApplicationFiled: May 17, 2013Publication date: May 21, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: Shawn J. Stachel, Melissa Egbertson, Edward Brnardic, Kristen G. Jones, John M. Sanders, Darrell Henze
-
Publication number: 20150141396Abstract: The present invention provides compounds of Formula (I) for the treatment of cancer, rheumatoid arthritis and other diseases.Type: ApplicationFiled: July 3, 2013Publication date: May 21, 2015Applicant: Ares Trading S.A.Inventors: Stefano Crosignani, Catherine Jorand-Lebrun, Patrick Gerber, Mathilde Muzerelle
-
Publication number: 20150141426Abstract: The present invention relates to a dosage regimen for a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof. More specifically, the present invention relates to a dosage regimen for the treatment of patients suffering from a proliferative disease, such as, for example, cancer, with a phosphatidylinositol 3-kinase (PI3K) inhibitor compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 14, 2013Publication date: May 21, 2015Inventors: Samit HIRAWAT, Cristian MASSACESI
-
Publication number: 20150141397Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.Type: ApplicationFiled: August 5, 2014Publication date: May 21, 2015Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
-
Patent number: 9034850Abstract: Disclosed are compounds useful as gonadotrophin-releasing hormone (“GnRH”) receptor antagonist.Type: GrantFiled: November 19, 2010Date of Patent: May 19, 2015Assignee: SK Chemicals Co., Ltd.Inventors: Seon Mi Kim, Min Hee Lee, Jae Sun Kim, Hoe Chul Jung, So Young Lee, Soo Min Lee, Eun Jeong Kim, Eui Sun Park, Sung Hoon Park, Bong Yong Lee, Key An Um
-
Publication number: 20150133441Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.Type: ApplicationFiled: June 6, 2014Publication date: May 14, 2015Inventor: Gerard M. Housey
-
Publication number: 20150126471Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to 5-[[4-[[morpholin-2-yl]methylamino]-5-(trifluoromethyl)-2-pyridyl]amino]pyrazine-2-carbonitrile compounds (referred to herein as “TFM compounds”) which, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc.Type: ApplicationFiled: May 14, 2013Publication date: May 7, 2015Inventors: Ian Collins, Thomas Peter Matthews, Tatiana Faria Da Fonseca Mchardy, James Osborne, Michael Lainchbury, Michael Ian Walton, Michelle Dawn Garrett
-
Publication number: 20150126504Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: January 12, 2015Publication date: May 7, 2015Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald Payan, Susan Molineaux, Sacha Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander Rossi
-
Publication number: 20150111892Abstract: The present invention concerns, in a first aspect, compounds of Formula I as defined herein, pharmaceutically acceptable salts thereof and pharmaceutical compositions containing such compounds. The present invention also relates to compounds of Formula I for use as acid ceramidase inhibitors, and in the treatment of cancer and other disorders in which modulation of the levels of ceramide is clinically relevant.Type: ApplicationFiled: May 27, 2013Publication date: April 23, 2015Inventors: Daniele Piomelli, Natalia Realini, Marco Mor, Chiara Pagliuca, Daniela Pizzirani, Rita Scarpelli, Tiziano Bandiera
-
Publication number: 20150111871Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: October 16, 2014Publication date: April 23, 2015Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
-
Publication number: 20150111891Abstract: 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: April 23, 2015Applicant: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongyan Guo, Paul Hrvatin, Eric Lansdon, John O. Link, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Randall W. Vivian, Lianhong Xu, Hong Yang
-
Publication number: 20150111865Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.Type: ApplicationFiled: April 25, 2013Publication date: April 23, 2015Applicant: ONO PHARMACEUTICAL CO., LTD.Inventors: Jun Takeuchi, Masahiro Ikura, Masato Higashino, Maki Iwahashi, Kazuya Hashimura
-
Publication number: 20150111866Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.Type: ApplicationFiled: April 26, 2013Publication date: April 23, 2015Applicant: Merck Sharp & Dohme Corp.Inventors: John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
-
Patent number: 9012461Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.Type: GrantFiled: July 6, 2012Date of Patent: April 21, 2015Assignee: Cancer Therapeutics CRC Pty LtdInventors: Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Choi, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
-
Publication number: 20150105354Abstract: Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(?S)—, —S(O)—, —S(O)2—, —C(?O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(?N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(?O)— or —C(?NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(?NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I.Type: ApplicationFiled: December 18, 2014Publication date: April 16, 2015Applicants: MERCK SHARP & DOHME CORP., PHARMACOPEIA, LLCInventors: Zhaoning Zhu, Brian McKittrick, Zhong-Yue Sun, Yuanzan C. Ye, Johannes H. Voigt, Corey Strickland, Elizabeth M. Smith, Andrew W. Stamford, William J. Greenlee, Robert D. Mazzola, JR., John Caldwell, Jared N. Cumming, Lingyan Wang, Yusheng Wu, Ulrich Iserloh, Tao Guo, Thuy X.H. Le, Kurt W. Saionz, Suresh D. Babu, Rachael C. Hunter
-
Publication number: 20150105387Abstract: Compounds of formula (1) wherein R1 is 2-indanyl, R2 is 1-methylpropyl, R3 is 2-methyl-1,3-oxazol-4-yl and R4 and R5 together with the nitrogen atom to which they are attached represents morpholino, process for their preparation, pharmaceutical compositions containing them and their use in medicine.Type: ApplicationFiled: December 15, 2014Publication date: April 16, 2015Inventor: John Liddle
-
Publication number: 20150105390Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: ApplicationFiled: December 17, 2014Publication date: April 16, 2015Applicant: IRM LLC, a Delaware Limited Liability CompanyInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, III, Wenshuo Lu, Bei Chen, Tetsuo Uno, Yunho Jin, Tao Jiang
-
Patent number: 9006232Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: GrantFiled: August 11, 2010Date of Patent: April 14, 2015Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
-
Patent number: 9006243Abstract: HIV replication inhibitors of formula R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; R2, R3, R6 and R7 are hydrogen; hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R4 and R5 are hydroxy; halo; C3-7cycloalkyl; C1-6alkyloxy; carboxyl; C1-6alkyloxycarbonyl; formyl; cyano; nitro; amino; mono- or di(C1-6alkyl)amino; polyhaloC1-6alkyl; polyhaloC1-6alkyloxy; —C(?O)R9; cyano; —S(?O)rR9; —NH—S(?O)2R9; —NHC(?O)H; —C(?O)NHNH2; —NHC(?O)R9; Het; —Y-Het; optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl; R5 is pyridyl, —C(?O)NR5aR5b; —CH(OR5c)R5d; —CH2—NR5eR5f; —CH?NOR5a; —CH2—O—C2-6alkenyl; —CH2—O—P(?O)(OR5g)2; —CH2—O—C(?O)—NH2; —C(?O)—R5d; X is —NR1—, —O—, —CH2—, —S—; pharmaceutical compositions containing these compounds as active ingredient and processes for preparing said compouType: GrantFiled: December 28, 2007Date of Patent: April 14, 2015Assignee: Janssen R&D IrelandInventors: Jerôme Emile Georges Guillemont, Céline Isabelle Mordant
-
Publication number: 20150099749Abstract: This invention concerns pyrimidine derivatives of formula having HIV (Human Immunodeficiency Virus) replication inhibiting properties, the preparation thereof and pharmaceutical compositions comprising these compounds.Type: ApplicationFiled: December 10, 2014Publication date: April 9, 2015Inventors: Jerôme Emile Georges Guillemont, Mikaël Paugam, Bruno François Marie Delest
-
Publication number: 20150099748Abstract: Multiheteroaryl compounds, their preparation, pharmaceutical compositions comprising these compounds, and their pharmaceutical use in the prevention and treatment of prostaglandin D2 mediated diseases and conditions that may be modulated by the inhibition of hematopoietic prostaglandin D synthase (H-PGDS).Type: ApplicationFiled: September 29, 2014Publication date: April 9, 2015Inventors: Gregory W. Endres, Pil Heui Lee, Kirk Lang Olson, James Bernard Kramer, Fred Lawrence Ciske, Stephen Douglas Barrett
-
Publication number: 20150094298Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: December 5, 2014Publication date: April 2, 2015Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Mukund Mehrotra, Yonghong Song, Qing Xu, Wolin Huang, Chandrasekar Venkataramani, Jack W. Rose, Anjali Pandey
-
Publication number: 20150094307Abstract: Amino, amido, and heterocyclic compounds are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, diabetes complications, inflammation, and neurodegeneration, obesity, cancer, ischemia/reperfusion injury, cardiovascular disease and other diseases related to RAGE activity.Type: ApplicationFiled: October 1, 2014Publication date: April 2, 2015Inventors: Ann Marie Schmidt, Ravichandran Ramasamy, Alexander Shekhtman, Vivek Rai, Michaele B. Manigrasso
-
Publication number: 20150094520Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.Type: ApplicationFiled: December 8, 2014Publication date: April 2, 2015Inventors: Carl R. ILLIG, Shelley K. BALLENTINE, Jinsheng CHEN, Sanath K. MEEGALLA, M. Jonathan RUDOLPH, Mark J. WALL, Kenneth J. WILSON, Renee Louise DESJARLAIS, Carl M. MANTHEY, Christopher J. MOLLOY
-
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
-
Publication number: 20150094296Abstract: The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: ApplicationFiled: March 27, 2013Publication date: April 2, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Tetsuya Tsukamoto, Yusuke Ohba, Takafumi Yukawa, Hiroyuki Nagamiya, Taku Kamei, Norihito Tokunaga, Morihisa Saitoh, Atsutoshi Okabe
-
Patent number: 8993565Abstract: The invention relates to the novel materials of formula (I), wherein each of the substituents R, R1, R2, R3, R4 and R5 is as defined herein. The materials are useful as inhibitors of AKT(PKB) phosphorylation.Type: GrantFiled: June 23, 2014Date of Patent: March 31, 2015Assignee: SanofiInventors: Jean-Christophe Carry, Victor Certal, Frank Halley, Karl Andreas Karlsson, Laurent Schio, Fabienne Thompson
-
Patent number: 8993567Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: GrantFiled: March 27, 2014Date of Patent: March 31, 2015Assignee: Bristol-Myers Squibb CompanyInventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M. P. Doweyko, Joel C. Barrish, John Wityak
-
Publication number: 20150086491Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 5, 2014Publication date: March 26, 2015Inventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
-
Publication number: 20150087644Abstract: The invention relates to compounds of formula I wherein A1, A2, A3, B, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used as medicaments.Type: ApplicationFiled: November 26, 2014Publication date: March 26, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Alexander Flohr, Katrin Groebke Zbinden, Matthias Koerner, Christian Lerner
-
Publication number: 20150087639Abstract: The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.Type: ApplicationFiled: July 18, 2013Publication date: March 26, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Yingjun Zhang, Jiancun Zhang, Xiaojun Wang, Runfeng Lin, Shengtian Cao, Zhaohe Wang, Jing Li
-
Patent number: 8987261Abstract: The present application relates to novel substituted dihydropyrazolone derivatives, processes for their preparation, their use for treatment and/or prophylaxis of diseases and their use for the preparation of medicaments for treatment and/or prophylaxis of diseases, in particular cardiovascular and hematological diseases and kidney diseases, and for promoting wound healing.Type: GrantFiled: February 18, 2013Date of Patent: March 24, 2015Assignee: Bayer Intellectual Property GmbHInventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
-
Publication number: 20150080363Abstract: The present invention relates to compounds defined by formula I: wherein the variables A1, A2, Cy1 Cy2, Cy3, E, R1a, R1b, R2, R3, n, and Q are as defined herein, possessing valuable pharmacological activity. Particularly, the compounds are inhibitors of 11 ?-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity, and dyslipidemia.Type: ApplicationFiled: September 26, 2014Publication date: March 19, 2015Inventors: Matthias Eckhardt, Frank Himmelsbach, Katerina Leftheris, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Linghang Zhuang
-
Publication number: 20150080368Abstract: The present invention relates to a compound of the formula I wherein R1 to R6, A, B, n and m are as defined herein. Such novel sulfonyl amide derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: ApplicationFiled: November 24, 2014Publication date: March 19, 2015Applicant: VERASTEM, INC.Inventors: Michael Joseph Luzzio, Kevin Daniel Freeman-Cook, Samit Kumar Bhattacharya, Matthew Merrill Hayward, Catherine Angela Hulford, Christopher Lowell Autry, Xumiao Zhao, Jun Xiao, Kendra Louise Nelson
-
Publication number: 20150079154Abstract: The invention provides a pharmaceutical composition comprising Sorafenib in combination with an inhibitor of a specific kinase inhibitor as a medicament for the treatment or prevention of liver cancer.Type: ApplicationFiled: July 9, 2012Publication date: March 19, 2015Applicant: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBHInventors: Lars Zender, Ramona Rudalska, Daniel Dauch
-
Publication number: 20150080396Abstract: The invention concerns compounds of Formula (I): wherein L1, R1, R2, R3, R4 and X are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of disease, for example cancer.Type: ApplicationFiled: August 26, 2014Publication date: March 19, 2015Applicants: DAINIPPON SUMITOMO PHARMA CO., LTD., ASTRAZENECA ABInventors: Nicholas James Bennett, Stephen Thom, Thomas McInally
-
Publication number: 20150080364Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.Type: ApplicationFiled: March 15, 2013Publication date: March 19, 2015Applicants: Abide Therapeutics, Inc., The Scripps Research InsitituteInventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
-
Patent number: 8980890Abstract: The invention relates to compounds and methods for treating cell proliferation disorders.Type: GrantFiled: November 19, 2010Date of Patent: March 17, 2015Assignee: Kinex Pharmaceuticals, LLCInventor: David G. Hangauer, Jr.
-
Publication number: 20150072983Abstract: The present invention relates to the use of substituted dihydroimidazolones, particularly [1-(4-Chlorophenyl)-4-(4-morpholinyl)-2,5-dihydro-1H-imidazol-2-one] (AWD 131-138) or a physiologically acceptable salt thereof for the treatment of epilepsy in dogs.Type: ApplicationFiled: November 17, 2014Publication date: March 12, 2015Inventors: Chris RUNDFELDT, Rita DOST, Wolfgang LOSCHER, Andrea TIPOLD, Klaus UNVERFERTH, Hans-Joachim LANKAU
-
Publication number: 20150072969Abstract: The present invention relates to phenyl alkanoic acid derivatives (the compounds of Formula (I)); and their isotopic forms, stereoisomeric and tautomeric forms and mixtures thereof in all ratios, or pharmaceutically acceptable salts, pharmaceutically acceptable solvates, prodrugs, polymorphs, N-oxides, S-oxides or carboxylic acid isosteres thereof. The invention also relates to processes for the preparation of compounds of Formula (I) and pharmaceutical compositions comprising one or more of the compounds of Formula (I). The said compounds and the pharmaceutical composition function as GPR (G-protein coupled receptor) agonists, particularly as GPR40 agonists, and are useful in the treatment of diseases or conditions mediated by GPR40. The present invention further relates to a method of treatment of diseases or conditions mediated by GPR40 comprising administering to a subject in need thereof a therapeutically effective amount of the compounds of Formula (I).Type: ApplicationFiled: February 27, 2013Publication date: March 12, 2015Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Sanjay Kumar, Rajiv Sharma, Vishal Ashok Mahajan, Sangameshwar Prabhakar Sawargave
-
Patent number: 8975249Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: GrantFiled: October 31, 2011Date of Patent: March 10, 2015Assignee: Celgene Avilomics Research, Inc.Inventors: Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
-
Publication number: 20150065478Abstract: 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: ApplicationFiled: November 11, 2014Publication date: March 5, 2015Inventors: Patrick Rene Angibaud, Kristof Van Emelen, Virginie Sophie Poncelet, Bruno Roux
-
Publication number: 20150065505Abstract: The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: March 29, 2013Publication date: March 5, 2015Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
-
Patent number: 8969335Abstract: Compounds of the formula I, in which R1, R2, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: GrantFiled: August 13, 2012Date of Patent: March 3, 2015Assignee: MERCK PATENT GmbHInventors: Guenter Hoelzemann, Dieter Dorsch, Hans-Michael Eggenweiler