Three Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 544/278)
  • Patent number: 10336765
    Abstract: The present invention relates to a novel dihydropyranopyrimidinone derivative, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof; and a pharmaceutical composition for preventing or treating a tankyrase-related disease, which contains the same as an active ingredient.
    Type: Grant
    Filed: December 1, 2016
    Date of Patent: July 2, 2019
    Assignee: ST. PHARM CO., LTD.
    Inventors: Kyungjin Kim, Uk-Il Kim, Ji Hye Yoon
  • Patent number: 10183950
    Abstract: 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: Grant
    Filed: January 26, 2017
    Date of Patent: January 22, 2019
    Assignee: Cancer Research Technology Limited
    Inventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R. A. Roffey, Christelle N. Soudy, Jason C. Wagner
  • Patent number: 10087195
    Abstract: Provided are compound of formula (I) as certain CDK4/6 inhibitors, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: May 27, 2015
    Date of Patent: October 2, 2018
    Assignees: SHANGHAI FOCHON PHARMACEUTICAL CO., LTD., CHONGQING FOCHON PHARMACEUTICAL CO., LTD.
    Inventors: Weibo Wang, Xingdong Zhao, Tongshuang Li, Qiang Tian, Huajie Zhang, Haohan Tan, Xianlong Wang, Qihong Liu, Zhifu Li, Weipeng Zhang, Zhifang Chen, Lihua Jiang, Yanxin Liu, Li Linghu, Min Lin, Jing Sun
  • Patent number: 10016433
    Abstract: The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.
    Type: Grant
    Filed: July 12, 2017
    Date of Patent: July 10, 2018
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kazumichi Jo, Hideki Takeuchi
  • Patent number: 10000498
    Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: June 19, 2018
    Assignee: Duquesne University of the Holy Spirit
    Inventors: Aleem Gangjee, Larry H. Matherly
  • Patent number: 9988399
    Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
    Type: Grant
    Filed: May 8, 2014
    Date of Patent: June 5, 2018
    Assignee: Gilead Apollo, LLC
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, George Borg, Craig E. Masse
  • Patent number: 9890168
    Abstract: The present invention relates to a 2,4-disubstituted 7H-pyrrolo[2,3-d]pyrimidine derivative, a preparation method and a medicinal use thereof. In particular, the present invention discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. For the definition of each group in formula (I), see the description tbr details.
    Type: Grant
    Filed: July 24, 2015
    Date of Patent: February 13, 2018
    Assignees: Shanghai Haiyan Pharmaceutical Technology Co., Ltd., Yangtze River Pharmaceutical Group Co., Ltd.
    Inventors: Jiong Lan, Yunzhou Jin, Fusheng Zhou, Jing Lei, Chong Wen, Zhiyuan Zhang, Xiangyu He
  • Patent number: 9737539
    Abstract: The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt having excellent solubility and storage stability.
    Type: Grant
    Filed: September 28, 2015
    Date of Patent: August 22, 2017
    Assignee: KISSEI PHARMACEUTICALS CO., LTD.
    Inventors: Kazumichi Jo, Hideki Takeuchi
  • Patent number: 9732090
    Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
    Type: Grant
    Filed: September 21, 2015
    Date of Patent: August 15, 2017
    Assignee: Duquesne University of the Holy Ghost
    Inventor: Aleem Gangjee
  • Patent number: 9642852
    Abstract: A sulfur-containing bicyclic compound of the present invention has a PAM action of GABAB. A composition containing the sulfur-containing bicyclic compound. And, a method for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease by administering the sulfur-containing bicyclic compound.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: May 9, 2017
    Assignee: Astellas Pharma Inc.
    Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
  • Patent number: 9586928
    Abstract: The invention provides small molecule modulators of retinoic acid receptor-related orphan receptors such as ROR?, ROR?, or ROR?, of formula with the variable atoms as defined herein and R1 comprising a hydroxyl- or alkoxyl-substituted fluoroalkyl group. Compounds of the invention can be effective modulators at concentrations ineffective to act on LXR receptors, or on other nuclear receptors, or other biological targets. Methods of modulation the RORs and methods of treating metabolic disorders, immune disorders, cancer, and CNS disorders wherein modulation of an ROR is medically indicated are also provided.
    Type: Grant
    Filed: May 16, 2012
    Date of Patent: March 7, 2017
    Assignee: The Scripps Research Institute
    Inventors: Theodore Mark Kamenecka, Patrick R. Griffin, Youseung Shin, Yuanjun He, Anne-Laure Blayo, Brent R. Lyda, Marcel Koenig, Naresh Kumar, Thomas Burris
  • Patent number: 9540392
    Abstract: The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: January 10, 2017
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Georg Kettschau, Florian Puehler, Knut Eis, Ulrich Klar, Dirk Kosemund, Detlev Sülzle, Philip Lienau, Andrea Hägebarth, Ulf Bömer, Lars Wortmann, Keith Graham, Antje Margret Wengner
  • Patent number: 9422307
    Abstract: A substituted thieno pyrimidine compound of Formula 1, pharmaceutically acceptable salts and a pharmaceutical composition thereof is provided. The compound of Formula 1 exhibits superior inhibition activity against various protein kinases involved in growth factor signal transduction. The compound of Formula 1 and its compositions are useful for the prevention and treatment of diseases caused by abnormal cell growth including cancer.
    Type: Grant
    Filed: October 22, 2010
    Date of Patent: August 23, 2016
    Assignee: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY
    Inventors: Tae Bo Sim, Jung Mi Hah, Hwan Geun Choi, Young Jin Ham, Jung Hun Lee, Dong Sik Park, Hwan Kim
  • Patent number: 9271979
    Abstract: The present invention is concerned with deuterium-enriched pyrimidine compounds of formula 1, their derivatives and pharmaceutically acceptable salts and methods of use thereof for the prevention and treatment of neuroendocrine neoplasia including metastasis and fibrosis, fibrotic processes associated with neuroendocrine cell dysregulation for example Crohn's disease, pulmonary arterial hypertension, pulmonary hypertension associated with chronic obstructive pulmonary disease (COPD), right ventricular hypertrophy, pulmonary vascular remodeling, asthma, cystic fibrosis, hypertension, ischemic stroke, angina pectoris, congestive heart failure, arrhythmia, arterial fibrillation, neurodenerative diseases, gastrointestinal disorders , stress disorders, obsessive compulsive disorders, demyelinating diseases, cereberal vascular disorders, bronchoconstriction, vasodilation, smooth muscle contraction, brain disorders, vascular disorders, neuropathological diseases and cardiovascular system regulation.
    Type: Grant
    Filed: September 14, 2011
    Date of Patent: March 1, 2016
    Inventor: Daljit Singh Dhanoa
  • Patent number: 9169266
    Abstract: An objective of the present invention is to improve the solubility of 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid. The present invention provides 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyl-oxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt has excellent solubility and storage stability.
    Type: Grant
    Filed: February 9, 2011
    Date of Patent: October 27, 2015
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kazumichi Jo, Hideki Takeuchi
  • Patent number: 9156852
    Abstract: 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: Grant
    Filed: December 27, 2012
    Date of Patent: October 13, 2015
    Assignee: HANMI PHARM. CO., LTD
    Inventors: 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
  • Patent number: 9139590
    Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.
    Type: Grant
    Filed: February 2, 2012
    Date of Patent: September 22, 2015
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Patent number: 9133209
    Abstract: The compounds of general formula I, wherein X, R1, R2, R3 and A are defined as in the description, are of the class of 4-amino-thieno[2,3-d]-pyrimidine compounds useful to control pests that damage plants and crops, and parasites that harm animals:
    Type: Grant
    Filed: July 29, 2010
    Date of Patent: September 15, 2015
    Assignee: MERIAL, INC.
    Inventors: Mark David Soll, Charles Meng, Matthias Pohlman, Ernst Baumann, Ralph Paulini
  • Patent number: 9051339
    Abstract: A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.
    Type: Grant
    Filed: October 17, 2014
    Date of Patent: June 9, 2015
    Assignee: Astellas Pharma Inc.
    Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
  • Patent number: 9045491
    Abstract: 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: Grant
    Filed: October 23, 2012
    Date of Patent: June 2, 2015
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Cisen Pharmaceutical Co., Ltd.
    Inventors: Hong Liu, Jia Li, Jian Li, Jingya Li, Jiang Wang, Mingbo Su, Jie Lian, Hualiang Jiang, Kaixian Chen
  • Publication number: 20150148322
    Abstract: The invention relates to novel piperidino-dihydrothienopyrimidine sulfoxides of formula I, wherein Ring A is a 6-membered aromatic ring which may optionally comprise one or two nitrogen atoms and wherein R is Cl and wherein R may be located either in the para-, meta- or ortho-position of Ring A, wherein S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.
    Type: Application
    Filed: March 15, 2012
    Publication date: May 28, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Pascale A.J. Pouzet, Peter Nickolaus, Ulrike Werthmann, Rogelio P. Frutos, Bing-Shiou Yang, Soojin Kim, Jason Alan Mulder, Nitinchandra Patel, Chris H. Senanayake, Thomas G. Tampone, Xudong Wei
  • Patent number: 9040693
    Abstract: The present invention provides a compound useful as an agent for the prevention or treatment of a sex hormone-dependent disease or the like. That is, the present invention provides a fused heterocyclic derivative represented by the following general formula (I), a pharmaceutical composition containing the same, a medicinal use thereof and the like. In the formula (I), ring A represents 5-membered cyclic unsaturated hydrocarbon or 5-membered heteroaryl; RA represents halogen, alkyl, alkenyl, alkynyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like ; ring B represents aryl or heteroaryl; RB represents halogen, alkyl, carboxy, alkoxy, carbamoyl, alkylcarbamoyl or the like; E1 and E2 represent an oxygen atom or the like; U represents a single bond or alkylene; X represents a group represented by Y, —SO2—Y, —O—(alkylene)—Y, —O—Z in which Y represents Z, amino or the like; Z represents cycloalkyl, heterocycloalkyl, aryl, heteroaryl or the like; or the like.
    Type: Grant
    Filed: October 17, 2006
    Date of Patent: May 26, 2015
    Assignee: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kohsuke Ohno, Takashi Miyagi, Tomonaga Ozawa, Nobuhiko Fushimi
  • Publication number: 20150126513
    Abstract: The present invention provides for compounds of formula (I): wherein R1-R4 and n 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: Application
    Filed: July 13, 2012
    Publication date: May 7, 2015
    Applicant: Novartis AG
    Inventors: Christine Hiu-Tung Chen, Donovan Noel Chin, Lucian V. DiPietro, Jianmei Fan, Mark G. Palermo, Michael David Shultz, Bakary-Barry Toure
  • Patent number: 9023858
    Abstract: The present invention provides a compound useful for the prophylaxis or treatment of eicosanoid-associated diseases such as atherosclerosis, atherothrombosis, diabetes, obesity, asthma, fever, pain, cancer, rheumatism, osteoarthritis, atopic dermatitis and the like, and having superior pharmacological action, physicochemical properties and the like. The present invention relates to a compound represented by the following formula: wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: July 22, 2011
    Date of Patent: May 5, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nobuyuki Matsunaga, Hideo Suzuki, Kouhei Asano, Hidekazu Tokuhara, Takeshi Yamamoto, Rei Okamoto
  • Patent number: 9018209
    Abstract: The present invention relates to compounds according to the formula I: Where Ra is H or an optionally OH-substituted C1-C3 alkyl; R1 is OR1, an optionally substituted C4-12 carbocyclic group which may be saturated or unsaturated (including aromatic) or an optionally substituted heterocyclic group; R1 is an optionally substituted C1-C14 hydrocarbyl group or an optionally substituted heterocyclic group; R2, R3 and R4 are each independently H, an optionally substituted C1-C4 alkyl group (preferably CH3, CH2CH3 or CF3), halogen (preferably F, Cl, Br), OR, CN, NO2, a C1-C6 thioether, a C1-C6 thioester group, an optionally substituted CO2R group, an optionally substituted COR group or an optionally substituted OCOR group (preferably R4 is H); R is H or an optionally substituted C1-C6 alkyl group; RHET is an optionally substituted heterocyclic group; and pharmaceutically acceptable salts, solvates or polymorphs thereof.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: April 28, 2015
    Assignee: Yale University
    Inventors: William L. Jorgensen, Juliana Ruiz-Caro, Andrew D. Hamilton
  • Patent number: 9018175
    Abstract: The compounds of Formula (1), in which A, R1, R2, R3 and R5 have the meanings as given in the description, are novel effective inhibitors of type 4 and 5 phosphodiesterase.
    Type: Grant
    Filed: December 15, 2010
    Date of Patent: April 28, 2015
    Assignee: Takeda GmbH
    Inventors: Dieter Flockerzi, Thomas Stengel, Alexander Mann, Harald Ohmer, Ulrich Kautz, Steffen Weinbrenner, Stefan Fischer, Christof Zitt, Armin Hatzelmann, Torsten Dunkern, Christian Hesslinger, Thomas Maier, Hermann Tenor, Clemens Braun, Raimund Külzer, Degenhard Marx
  • Publication number: 20150111894
    Abstract: The present invention provides an aromatic ring compound having a melanin-concentrating hormone receptor antagonistic action and useful as an agent for the prophylaxis or treatment of obesity and the like. The present invention relates to a compound represented by the formula wherein each symbol as defined in the specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2013
    Publication date: April 23, 2015
    Inventors: Shizuo Kasai, Hideyuki Igawa, Masashi Takahashi, Asato Kina
  • Publication number: 20150111876
    Abstract: A sulfur-containing bicyclic compound having a PAM action of GABAB, and it use for preventing and/or treating schizophrenia, CIAS, cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, or Charcot-Marie-Tooth disease. A pharmaceutical composition for preventing and/or treating schizophrenia, cognitive impairment associated with schizophrenia (CIAS), cognitive impairment, fragile X syndrome, autism spectrum disorder, spasticity, anxiety disorder, substance addiction, pain, fibromyalgia, Charcot-Marie-Tooth disease, or the like, which has a positive allosteric modulator (PAM action) of GABAB.
    Type: Application
    Filed: October 17, 2014
    Publication date: April 23, 2015
    Applicant: Astellas Pharma Inc.
    Inventors: Nobuyuki Shiraishi, Hiroaki Hoshii, Wataru Hamaguchi, Eriko Honjo, Tomofumi Takuwa, Yuji Kondo, Takayuki Goto
  • Publication number: 20150111038
    Abstract: The present disclosure is directed to salts of N-{4-[2,4-difluoro-3-(trifluoromethyl)phenyl]-1,3-thiazol-2-yl}dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[2,3-d]pyrimidin-5-yl)acetamide and process for the preparation thereof (formula II).
    Type: Application
    Filed: June 8, 2013
    Publication date: April 23, 2015
    Applicant: GLENMARK PHARMACEUTICALS S.A.
    Inventors: Suresh Mahadev Kadam, Abraham Thomas, Sukumar Sinha, Sukeerthi Kumar, Bipin Parsottam Kansagra, Sachin Gavhane, Sandeep Bandu Khandagale, Shailesh Pawase, Jayant Prakashrao Patil, Shailendra Bhadane, Bhavna Mishra, Rajesh Dwivedi
  • Publication number: 20150105407
    Abstract: The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, and Formula IV, and pharmaceutically acceptable salts, 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 and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.
    Type: Application
    Filed: December 17, 2014
    Publication date: April 16, 2015
    Inventor: Aleem Gangjee
  • Patent number: 9006253
    Abstract: 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: Grant
    Filed: March 26, 2014
    Date of Patent: April 14, 2015
    Assignee: ASKA Pharmaceutical Co., Ltd.
    Inventors: Hiroyuki Hayashi, Takayoshi Nakagawa, Koichi Miyazaki
  • Patent number: 8999973
    Abstract: 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: Grant
    Filed: January 31, 2011
    Date of Patent: April 7, 2015
    Assignees: Hanmi Science Co., Ltd, Korea Institute of Science and Technology, Catholic University Industry Academic Cooperation Foundation
    Inventors: 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
  • Publication number: 20150094275
    Abstract: 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: Application
    Filed: November 13, 2014
    Publication date: April 2, 2015
    Applicants: THE SCRIPPS RESEARCH INSTITUTE, DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Nathanael S. GRAY, Jianming ZHANG, Barun OKRAM, Xianming DENG, Jae Won CHANG, Amy WOJCIECHOWSKI
  • Patent number: 8987278
    Abstract: 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: Grant
    Filed: June 25, 2013
    Date of Patent: March 24, 2015
    Assignee: Glenmark Pharmaceuticals S.A.
    Inventors: Sukeerthi Kumar, Abraham Thomas, Nayan Taterao Waghmare, Sanjay Margal, Neelima Khairatkar-Joshi, Indranil Mukhopadhyay
  • Publication number: 20150080416
    Abstract: 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 inte
    Type: Application
    Filed: September 19, 2012
    Publication date: March 19, 2015
    Applicant: FUJIAN INSTITUTE OF RESEARCH ON THE STRUCTURE OF MATTER, CHINESE ACADEMY OF SCIENCES
    Inventors: Canzhong Lu, Jianping Yong
  • Patent number: 8981084
    Abstract: 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: Grant
    Filed: January 13, 2011
    Date of Patent: March 17, 2015
    Assignee: Tempero Pharmaceuticals, Inc.
    Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
  • Publication number: 20150072959
    Abstract: 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: Application
    Filed: November 13, 2014
    Publication date: March 12, 2015
    Inventors: Dane Goff, Jing Zhang, Catherine Sylvain, Rajinder Singh, Sacha Holland, Jiaxin Yu, Thilo J. Heckrodt, Pingyu Ding
  • Publication number: 20150072998
    Abstract: 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: Application
    Filed: April 16, 2013
    Publication date: March 12, 2015
    Inventors: 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
  • Publication number: 20150065501
    Abstract: 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: Application
    Filed: March 27, 2013
    Publication date: March 5, 2015
    Inventors: Nina Gertrud Bandur, Ralph Paulini, Florian Kaiser, Arun Narine, Joachim Dickhaut, Karsten Körber
  • Patent number: 8969363
    Abstract: 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: Grant
    Filed: July 18, 2012
    Date of Patent: March 3, 2015
    Assignee: 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
  • Patent number: 8969557
    Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.
    Type: Grant
    Filed: November 9, 2012
    Date of Patent: March 3, 2015
    Assignee: Nimbus Apollo, Inc.
    Inventors: Geraldine C. Harriman, Craig E. Masse, James Harwood, Sathesh Bhat, Jeremy Robert Greenwood
  • Publication number: 20150057295
    Abstract: 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: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ulrich REISER, James MADDEN
  • Publication number: 20150057286
    Abstract: 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: Application
    Filed: August 20, 2014
    Publication date: February 26, 2015
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventor: Ulrich REISER
  • Publication number: 20150057260
    Abstract: 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: Application
    Filed: August 22, 2014
    Publication date: February 26, 2015
    Applicant: Genentech, Inc.
    Inventors: Nicole Blaquiere, Georgette Castanedo, Jianwen A. Feng, Baihua Hu, Steven Staben, Po-wai Yuen, Guosheng Wu, Xingyu Lin, Jason Burch
  • Publication number: 20150045377
    Abstract: 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: Application
    Filed: March 25, 2013
    Publication date: February 12, 2015
    Inventors: Timothy Harrison, Colin O'Dowd, Steven Shepherd, Graham Trevitt, Lixin Zhang, Frank Burkamp
  • Publication number: 20150045324
    Abstract: 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: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Applicant: HANMI SCIENCE CO., LTD
    Inventors: 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
  • Patent number: 8946239
    Abstract: 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: Grant
    Filed: July 10, 2008
    Date of Patent: February 3, 2015
    Assignee: Duquesne University of the Holy Spirit
    Inventor: Aleem Gangjee
  • Publication number: 20150031709
    Abstract: 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: Application
    Filed: February 8, 2013
    Publication date: January 29, 2015
    Applicant: SUNOVION PHARMACEUTICALS, INC.
    Inventors: John Emmerson Campbell, Una Campbell, Taleen G. Hanania, Liming Shao
  • Patent number: 8940752
    Abstract: 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: Grant
    Filed: June 28, 2010
    Date of Patent: January 27, 2015
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, Brian W. Metcalf
  • Patent number: RE47451
    Abstract: 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: Grant
    Filed: October 13, 2017
    Date of Patent: June 25, 2019
    Assignee: Hanmi Pharm. Co. Ltd.
    Inventors: 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