Acyclic Nitrogen Containing Patents (Class 544/119)
  • Patent number: 11220486
    Abstract: Herein are provided, inter alia, compounds capable of modulating the level of activity of low molecular weight protein tyrosine phosphatase (LMPTP) and methods of using the same. In embodiments, the compound has a structure according to Formula (I-A).
    Type: Grant
    Filed: February 18, 2020
    Date of Patent: January 11, 2022
    Assignees: LA JOLLA INSTITUTE OF ALLERGY & IMMUNOLOGY, SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTE
    Inventors: Nunzio Bottini, Jiwen Zou, Santhi R. Ganji, Stephanie Stanford, Anthony Pinkerton, Thomas D. Y. Chung, Michael Hedrick, Robert Ardecky
  • Patent number: 11075008
    Abstract: Various embodiments predict drug-disease associations. In one embodiment, a plurality of disease similarity matrices and a plurality of disease similarity matrices are accessed. Each of the plurality of drug similarity matrices is associated with a different drug information source. Each of the plurality of disease similarity matrices is associated with a different disease information source. A known drug-disease association matrix is also accessed. The known drug-disease association matrix indicates if a given drug identified is known to treat a given disease. At least one drug-disease association prediction is generated based on the plurality of drug similarity matrices, the plurality of disease similarity matrices, and the known drug-disease association matrix. The at least one drug-disease association prediction identifies a previously unknown association between a given drug and a given disease, and a probability that the given disease is treatable by the given drug.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: July 27, 2021
    Assignee: International Business Machines Corporation
    Inventors: Jianying Hu, Fei Wang, Ping Zhang
  • Patent number: 11037684
    Abstract: Various embodiments predict drug-disease associations. In one embodiment, a plurality of disease similarity matrices and a plurality of disease similarity matrices are accessed. Each of the plurality of drug similarity matrices is associated with a different drug information source. Each of the plurality of disease similarity matrices is associated with a different disease information source. A known drug-disease association matrix is also accessed. The known drug-disease association matrix indicates if a given drug identified is known to treat a given disease. At least one drug-disease association prediction is generated based on the plurality of drug similarity matrices, the plurality of disease similarity matrices, and the known drug-disease association matrix. The at least one drug-disease association prediction identifies a previously unknown association between a given drug and a given disease, and a probability that the given disease is treatable by the given drug.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: June 15, 2021
    Assignee: International Business Machines Corporation
    Inventors: Jianying Hu, Fei Wang, Ping Zhang
  • Patent number: 10336755
    Abstract: The present invention relates to pyrazole fused-ring derivatives, their preparation methods, and use thereof in medicine. In particular, the present invention relates to a novel derivative represented by formula (I), and a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising the same and a method for preparing the same. The present invention also relates to use of the derivatives and the pharmaceutically acceptable salt thereof or the pharmaceutical composition comprising the same in the preparation of therapeutic agents, in particular Bruton tyrosine kinase inhibitors, and preparing a medicament for treating and/or preventing tumors and inflammatory associated diseases. The substituents on formula (I) are defined same as in the specification.
    Type: Grant
    Filed: December 28, 2016
    Date of Patent: July 2, 2019
    Assignee: Beijing Innocare Pharma Tech Co., Ltd.
    Inventors: Xiangyang Chen, Yucheng Pang
  • Patent number: 9637488
    Abstract: The present application discloses a novel class of heterocycles as class I PI3Ks inhibitors. The compounds claimed herein could be used alone or in combination therapies for the treatment of a wide range of disorders such as autoimmune, inflammatory and allergic diseases, asthma, COPD, parasitic infections, diabetes, and cancer.
    Type: Grant
    Filed: January 27, 2016
    Date of Patent: May 2, 2017
    Inventor: Fuqiang Ruan
  • Publication number: 20150141421
    Abstract: Compounds of formula (I) in which: R1 is: and R2 is —CH3 or —CH2CH3; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the compound of formula (I) and a pharmaceutically acceptable carrier. Processes for preparing the compound of formula (I). Methods of inhibiting a receptor tyrosine kinase in a subject in need thereof. Methods of inhibiting the growth of a tumor cell in a subject in need thereof. Methods of treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods of treating HER2 positive breast cancer in a subject in need of treatment for HER2 positive breast cancer. Methods of treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 26, 2014
    Publication date: May 21, 2015
    Inventors: Bhujanga rao ADIBHATLA KALI SATYA, Ramanadham JYOTHI PRASAD, Bollepalli NAGESHWARA RAO, Nannapaneni VENKAIAH CHOWDARY
  • Publication number: 20150126492
    Abstract: The present invention provides a compound of formula I a method for manufacturing the compounds of the invention, and its therapeutic uses as inhibitor of the complement alternative pathway and particularly as inhibitor of Factor B for the treatment of e.g. age-related macular degeneration and diabetic retinopathy. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: June 19, 2013
    Publication date: May 7, 2015
    Applicant: NOVARTIS AG
    Inventors: Michael Dechantsreiter, Jonathan E. Grob, Aengus Macsweeney, Wolfgang Miltz, Stefan Andreas Randl, Richard Sedrani, Holger Sellner, Finton Sirockin, Eric Valeur
  • Publication number: 20150119394
    Abstract: The present invention relates to compounds that are capable of inhibiting, modulating and/or regulating Insulin-Like-Growth Factor I Receptor and Insulin Receptor. The compounds of the instant invention possess a core structure that comprises a sulfonyl indole moiety. The present invention is also related to the pharmaceutically acceptable salts, hydrates and stereoisomers of these compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: April 30, 2015
    Inventors: Abhijit Roychowdhury, Rajiv Sharma, Malcolm Mascarenhas, Chandrika B-Rao, Shashikant M. Patil, Sambhaji Chavan, Nitin Lad, Smriti Khanna, Christopher J. Dinsmore
  • Publication number: 20150105368
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 2, 2014
    Publication date: April 16, 2015
    Applicant: ASTEX THERAPEUTICS LTD
    Inventors: Gordon SAXTY, Christopher William MURRAY, Valerio BERDINI, Gilbert Ebai BESONG, Christopher Charles Frederick HAMLETT, Christopher Norbert JOHNSON, Steven John WOODHEAD, Michael READER, David Charles REES, Laurence Anne MEVELLEC, Patrick René ANGIBAUD, Eddy Jean Edgard FREYNE, Tom Cornelis Hortense GOVAERTS, Johan Erwin Edmond WEERTS, Timothy Pietro Suren PERERA, Ronaldus Arnodus Hendrika Joseph GILISSEN, Berthold WROBLOWSKI, Jean Fernand Armand LACRAMPE, Alexandra PAPANIKOS, Oliver Alexis Georges QUEROLLE, Elisabeth Thérèse Jeanne PASQUIER, Isabelle Noëlle Constance PILATTE, Pascal Ghislain André BONNET, Werner Constant Johan EMBRECHTS, Rhalid AKKARI, Lieven MEERPOEL
  • Publication number: 20150080392
    Abstract: A class of quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof with novel structures is provided; meanwhile, a pharmaceutical composition comprising a pharmaceutically effective amount of said quinazoline derivatives or pharmaceutically acceptable salts or solvates thereof, and pharmaceutically acceptable excipients or additives is also provided. By modifying and transforming the quinazoline and screening of the transformed compounds on the activity of tyrosine kinase inhibition, most of the compounds have been found to possess inhibitory activity against one or several of EGFR, VEGFR-2, c-erbB-2, c-erbB-4, c-met, tie-2, PDGFR, c-src, lck, Zap70 and fyn kinases. The present invention has the advantages of reasonable design, broad source of and easy access to the raw materials, simple and easy operation of the preparation methods, mild reaction conditions, high yield of the products and being beneficial for industrial-scale production.
    Type: Application
    Filed: July 21, 2012
    Publication date: March 19, 2015
    Applicants: HANGZHOU MINSHENG PHARMACEUTICAL CO. LTD, HANGZHOU MINSHENG INSTITUTES FOR PHARMA RESEARCH
    Inventors: Shulong Wang, Jian Cai, Qiufu Ge, Dianwu Guo, Lan Yang, Binnan Huang, Zhenhua Liu, Zhonghua Peng, Ximing Shen, Feiyu Feng
  • 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: 20150065468
    Abstract: Biaryl acetamide compounds and compositions and their methods of use are provided for modulating the activity of class III receptor tyrosine kinases and for the treatment, prevention or amelioration of one or more symptoms of disease of disorder mediated by class III receptor tyrosine kinases.
    Type: Application
    Filed: August 29, 2014
    Publication date: March 5, 2015
    Inventors: Mark W. HOLLADAY, Gang LIU, Martin W. ROWBOTTON
  • Publication number: 20150057263
    Abstract: This invention relates to quinazoline compounds of Formula (I) which are inhibitors of the histone lysine methyltransferase (HKMTase) EZH2, and to uses of such compounds as medicaments, in particular in the treatment of a disease or disorder in which inhibition of EZH2 provides a therapeutic or prophylactic effect.
    Type: Application
    Filed: March 19, 2013
    Publication date: February 26, 2015
    Inventors: Robert Brown, Matthew John Fuchter, Nadine Chapman-Rothe, Nitipol Srimongkolpithak, Joachim Caron, James Synder, Thota Ganesh, Jin Liu, Aiming Sun
  • Publication number: 20150057277
    Abstract: Chemical entities that are quinoxaline kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: January 25, 2013
    Publication date: February 26, 2015
    Inventors: Yong-liang Zhu, Xiangping Qian
  • Publication number: 20150057276
    Abstract: Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
    Type: Application
    Filed: September 20, 2012
    Publication date: February 26, 2015
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Publication number: 20150051189
    Abstract: Compounds of formula (I): wherein Ra, Rb, Rc, Rd, R1, R2, R3, R4, R5, X, Y and Het are as defined in the description. Medicinal products containing the same which are useful in treating pathologies involving a deficit in apoptosis, such as cancer, auto-immune diseases, and diseases of the immune system.
    Type: Application
    Filed: January 23, 2013
    Publication date: February 19, 2015
    Inventors: Thierry Le Diguarher, Patrick Casara, Jérôme-Benoît Starck, Jean-Michel Henlin, James Edward Paul Davidson, James Brooke Murray, Christopher John Graham, I-Jen Chen, Olivier Geneste, John Hickman, Stéphane Depil, Arnaud Le Tiran, Miklos Nyerges, Guillaume De Nanteuil
  • Publication number: 20150038494
    Abstract: The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1. The present invention also relates to a method for their preparation, as well as to pharmaceutical compositions thereof. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of disorders and pathologic conditions such as, but not limited to, immune and auto-immune disorders, organ and cells transplant rejections.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: Katholieke Universiteit Leuven, K.U.Leuven R&D
    Inventors: Piet Herdewijn, Steven De Jonghe, Ling-Jie Gao, Mi-Yeon Jang, Bart Vanderhoydonck, Mark Jozef Albert Waer, Yuan Lin, Jean Ferdinand Herman, Thierry Andre Michel Louat
  • Publication number: 20150038510
    Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, and R5 are defined in the specification. The compounds are inhibitors of Bruton's tyrosine kinase (BTK). This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders or conditions associated with BTK.
    Type: Application
    Filed: March 25, 2013
    Publication date: February 5, 2015
    Inventors: John David Lawson, Mark Sabat, Christopher Smith, Haixia Wang, Young K. Chen, Toufike Kanouni
  • Publication number: 20150031669
    Abstract: The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
    Type: Application
    Filed: October 26, 2012
    Publication date: January 29, 2015
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Steven John Woodhead, Christopher William Murray, Valerio Berdini, Gordon Saxty, Gilbert Ebai Besong, Lieven Meerpoel, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet
  • Publication number: 20150031672
    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: Application
    Filed: October 10, 2014
    Publication date: January 29, 2015
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Alfredo C. Castro, Catherine A. Evans, Daniel A. Snyder
  • Publication number: 20150018345
    Abstract: The present invention relates to a compound according to formula (A) wherein n is 1 or 2; R1 and R2 are independently hydrogen, C1-4 alkyl, C1-4 haloalkyl, C1-4 alkoxy, CD3 or halogen; R3 is hydrogen, C(?O)OR7 or C1-4 alkyl optionally substituted with hydroxy or NR8R9; R4 is hydrogen or oxo; R5 and R6 are independently hydrogen, hydroxy, NR8R9, C(?O)R7, C(?O)OR7, C(?O)NR8R9, C1-4 alkyl, wherein said C1-4 alkyl is optionally substituted with hydroxy, NR8R9 or a 5- or 6-membered heterocyclic ring, wherein said 5- or 6-membered heterocyclic ring is optionally substituted with C1-4 alkyl or C(?O)R7; or R5 and R6, together with the carbon atom to which they are attached, form ?CH2 or a 5- or 6-membered heterocycloalkyl, wherein said heterocycloalkyl is optionally substituted with C1-4 alkyl; R7 is hydrogen or C1-4 alkyl; R8 and R9 are independently hydrogen or C1-4 alkyl, or R8 and R9, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocyclic ring, or a pharmaceutically accep
    Type: Application
    Filed: February 20, 2013
    Publication date: January 15, 2015
    Inventors: Morten Dahl Sørensen, Romano Di Fabio, Alfonso Pozzan, Maria Pia Catalani, Haakon Bladh, Jakob Felding
  • Publication number: 20150018331
    Abstract: Antibacterial compounds of formula (I) are provided: as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 15, 2015
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
  • Publication number: 20150011547
    Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Application
    Filed: September 2, 2014
    Publication date: January 8, 2015
    Applicant: ASANA BIOSCIENCES, LLC
    Inventors: Roger Astbury Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam
  • Publication number: 20140364431
    Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.
    Type: Application
    Filed: December 7, 2012
    Publication date: December 11, 2014
    Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
  • Publication number: 20140336182
    Abstract: The present invention relates to chemical compounds having a general formula I wherein A1-8, D?, L1, L2, R1, R6-8 and n are defined herein, and synthetic intermediates, which are capable of modulating various protein kinase receptor enzymes and, thereby, influencing various disease states and conditions related to the activities of such kinases. For example, the compounds are capable of modulating Aurora kinase thereby influencing the process of cell cycle and cell proliferation to treat cancer and cancer-related diseases. The invention also includes pharmaceutical compositions, including the compounds, and methods of treating disease states related to the activity of Aurora kinase.
    Type: Application
    Filed: May 13, 2013
    Publication date: November 13, 2014
    Inventors: Victor J. CEE, Holly L. DEAK, Bingfan DU, Stephanie D. GEUNS-MEYER, Zihao HUA, Matthew W. MARTIN, Isaac MARX, Hanh Nho NGUYEN, Philip R. OLIVIERI, Kathleen PANTER FABER, Karina ROMERO, Laurie SCHENKEL, Ryan WHITE
  • Patent number: 8853197
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Grant
    Filed: June 3, 2014
    Date of Patent: October 7, 2014
    Assignee: Wockhardt Ltd.
    Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawasar, Sachin Bhagwat, Mohammad Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
  • Publication number: 20140294764
    Abstract: This disclosure relates to compounds, compositions and methods of epigenetically transforming cells. In certain embodiments, the disclosure relates to methods of generating epigenetically altered cells comprising mixing isolated cells with compositions disclosed herein under conditions such that epigenetically altered cells are formed. In certain embodiments, the disclosure contemplates inducing cells, such as adult somatic cells or cells that are not naturally pluripotent, into cells with chemically induce pluripotency. In certain embodiments, the disclosure contemplates certain compounds disclosed herein, compounds disclosed herein optionally substituted with one or more substituents, derivatives, or salts thereof, for these purposes.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 2, 2014
    Applicants: ISTITUTO PASTEUR - FONDAZIONE CENCI BOLOGNETTI, EMORY UNIVERSITY
    Inventors: Young-Sup Yoon, Xiaodong Cheng, Ji Woong Han, Antonello Mai
  • Publication number: 20140275059
    Abstract: 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: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Publication number: 20140275024
    Abstract: 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: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux
  • Publication number: 20140249129
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: February 20, 2014
    Publication date: September 4, 2014
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: Christian GNAMM, Thorsten OOST, Stefan PETERS, Klaus RUDOLF
  • Publication number: 20140249146
    Abstract: The present invention relates to 4-alkyl substituted 3,4-dihydropyrrolo[1,2-a]pyrazin-1(2H)-one derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such these compounds or the pharmaceutical compositions containing them.
    Type: Application
    Filed: October 4, 2012
    Publication date: September 4, 2014
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Francesco Casuscelli, Alessandra Badari, Sten Christian Orrenius, Claudia Piutti, Teresa Disingrini
  • Patent number: 8815879
    Abstract: Selenophene compounds of formula (I) are described herein. In the compounds of Formula (I), ring A is a 6-membered aromatic fused ring, optionally containing one, two or three nitrogen atoms; a 5-membered heteroaromatic fused ring; or a mono- or bicyclic saturated heterocyclic fused ring having at least one ring member selected from the group consisting of N, O, S, SO and SO2; Y in ring B is nitrogen or substituted carbon; X is NR6, O, S, S(O), or S(O)2. R1, R2, R3, R4, and R6 are defined in the specification. Selenophene compounds of formula (I) may be used in methods of treating cell proliferative disorders, particularly cancer. Pharmaceutical compositions containing selenophene compounds of formula (I) may be used for treatment, inhibition, or control of cancer.
    Type: Grant
    Filed: May 17, 2013
    Date of Patent: August 26, 2014
    Assignee: Kasina Laila Innova Pharmaceuticals Private Limited
    Inventors: Sudhakar Kasina, Ganga Raju Gokaraju, Venkateswarlu Somepalli, Rama Raju Gokaraju, Venkata Kanaka Ranga Raju Gokaraju, Kiran Bhupathiraju, Trimurtulu Golakoti, Krishanu Sengupta, Venkata Krishna Raju Alluri
  • Publication number: 20140234317
    Abstract: Methods are disclosed for preventing toxic drug-drug interactions during combination cancer therapy with a drug that is an anti-ErbB3 agent, such as an anti-ErbB3 antibody, together with a drug that is a tyrosine kinase inhibitor and/or a drug that binds to alpha-1 acid glycoprotein (e.g., erlotinib). Health care practitioners obtaining any one of the drugs are warned that when co-administering the drug that is an anti-ErbB3 agent with either or both of a drug that is a tyrosine kinase inhibitor and a drug that binds to alpha-1 acid glycoprotein, at least one of the co-administered drugs should be administered using a reduced dosage to prevent toxicity. In a reduced dosage, the amount of drug administered per unit time is reduced as compared to a dose that would be administered if the drug was administered as monotherapy. The reduced dosage can be, for example, a reduced drug dose or a reduced drug dosing frequency, or both. Compositions useful in practicing the disclosed methods are also provided.
    Type: Application
    Filed: May 4, 2012
    Publication date: August 21, 2014
    Applicant: Merrimack Pharmaceuticals, Inc.
    Inventors: Matthew David Onsum, Clet Niyikiza, Victor Moyo, William Kubasek, Akos Czibere
  • Publication number: 20140235634
    Abstract: Described herein are compounds of Formula (I) or Formula (VI), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Also provided are particles (e.g., nanoparticles) comprising compounds of Formula (I) or Formula (VI) and pharmaceutical compositions thereof that are mucus penetrating. Methods of using the compounds or pharmaceutical compositions thereof for treating diseases are also provided.
    Type: Application
    Filed: February 14, 2014
    Publication date: August 21, 2014
    Applicant: Kala Pharmaceuticals, Inc.
    Inventors: Winston Zapanta ONG, Pawel Wojciech NOWAK, Ben C. ASKEW, Jinsoo KIM
  • Publication number: 20140235633
    Abstract: The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic.
    Type: Application
    Filed: May 10, 2012
    Publication date: August 21, 2014
    Applicants: SHANGHAI INSTITUTE OF PHARMACEUTICAL INDUSTRY, JIANGSU HENGYI PHARMACEUTICAL CO. LTD.
    Inventors: Jianqi Li, Qingwei Zhang, Wangping Cai
  • Publication number: 20140221335
    Abstract: This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
    Type: Application
    Filed: January 28, 2014
    Publication date: August 7, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christian GNAMM, Thorsten OOST, Stefan PETERS
  • Publication number: 20140206688
    Abstract: Disclosed are compounds having the formula (Formula I)): wherein R1, R2, R3 and Z are as defined herein, and methods of making and using the same.
    Type: Application
    Filed: August 17, 2012
    Publication date: July 24, 2014
    Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam K. Charnley, Michael P. Demartino, Xiaoyang Dong, Patrick M. Eidam, Pamela A. Haile, Robert W. Marquis, JR., Joshi M. Ramanjulu, Joseph J. Romano, Ami Lakdawala Shah, Robert R. Singhaus, JR., Gren Wang
  • Publication number: 20140206686
    Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective ROCK inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating cardiovascular, smooth muscle, oncologic, neuropathologic, autoimmune, fibrotic, and/or inflammatory disorders using the same.
    Type: Application
    Filed: January 17, 2014
    Publication date: July 24, 2014
    Inventors: Peter W. Glunz, Yan Zou, Mimi L. Quan
  • Publication number: 20140187550
    Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.
    Type: Application
    Filed: December 16, 2013
    Publication date: July 3, 2014
    Applicant: Novartis AG
    Inventor: Roger John Taylor
  • Publication number: 20140179668
    Abstract: Fused pyrimidine compounds as kinase inhibitors, such as multi-kinase inhibitors, are provided. Fused pyrimidine compounds as IGF-IR inhibitors are provided. The compounds may be used in a method of treating cancer. Pharmaceutical compositions containing a fused pyrimidine compound and a pharmaceutically acceptable carrier are also provided, as are kits containing a fused pyrimidine compound or salt thereof and instructions for use, e.g., in a method of treating cancer.
    Type: Application
    Filed: December 26, 2013
    Publication date: June 26, 2014
    Applicant: MEDIVATION TECHNOLOGIES, INC.
    Inventors: Sarvajit CHAKRAVARTY, Roopa RAI, Michael John GREEN
  • Publication number: 20140179673
    Abstract: The present disclosure provides phosphatidylinositol 3-kinase (PI3K) inhibitors of formula (I), or pharmaceutically acceptable salts thereof, in which R1, R2, n, R3, R4, R5 and R6 are as defined herein. These compounds are useful for treatment of conditions mediated by one or more PI3K isoforms, such as PI3K?. The present disclosure further provides pharmaceutical compositions that include a compound of formula (I), or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by one or more PI3K isoforms, such as PI3K?.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: GILEAD CALISTOGA LLC
    Inventors: Jerry EVARTS, Leena PATEL, Jennifer A. TREIBERG, Stephane PERREAULT, Arthur YEUNG, Lafe J. PURVIS, II, Musong KIM
  • Publication number: 20140163028
    Abstract: Compounds, compositions, and methods for specific inhibition of activated cdc42-associated kinase 1 (Ack1) are provided.
    Type: Application
    Filed: January 24, 2014
    Publication date: June 12, 2014
    Applicant: Institute for Cancer Research d/b/a The Research Institute of Fox Chase Cancer Center
    Inventors: Jeffrey R. Peterson, Haiching Ma, Sean Deacon
  • Publication number: 20140155396
    Abstract: The present invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. More specifically, the invention provides quinazolines and quinolines which inhibit, regulate, and/or modulate kinase receptor, particularly c-Met, KDF, c-Kit, flt-3 and flt-4, signal transduction pathways related to the changes in cellular activities as mentioned above, compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions. The present invention also provides methods for making compounds as mentioned above, and compositions which contain these compounds.
    Type: Application
    Filed: June 27, 2013
    Publication date: June 5, 2014
    Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Jeff Chen, Lisa Esther Dalrymple, Timothy Patrick Forsyth, Tai Phat Huynh, Vasu Jammalamadaka, Richard George Khoury, James William Leahy, Morrison B. Mac, Grace Mann, Larry W. Mann, John M. Nuss, Jason Jevious Parks, Craig Stacy Takeuchi, Yong Wang, Wei Xu
  • Patent number: 8742098
    Abstract: This application discloses compounds according to generic Formula I: wherein the variables are defined as described herein, and which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 6, 2012
    Date of Patent: June 3, 2014
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Christine E. Brotherton-Pleiss, Francisco Javier Lopez-Tapia, Yan Lou
  • Publication number: 20140148431
    Abstract: Compounds of Formula (I), their preparation and use in preventing or treating bacterial infection is disclosed.
    Type: Application
    Filed: August 24, 2012
    Publication date: May 29, 2014
    Inventors: Mahesh Vithalbhai Patel, Prasad Keshav Deshpande, Satish Bhawsar, Sachin Bhagwat, Mohammed Alam Jafri, Amit Mishra, Laxmikant Pavase, Sunil Gupta, Rajesh Kale, Sanjeev Joshi
  • Publication number: 20140128390
    Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and mutant c-kit protein kinases.
    Type: Application
    Filed: September 5, 2013
    Publication date: May 8, 2014
    Inventors: JACK LIN, JOHN BUELL, KATRINA CHAN, TODD EWING, PRABHA IBRAHIM, MARIKA NESPI, PHUONGLY PHAM, SONGYUAN SHI, WAYNE SPEVAK, GUOXIAN WU, JIAZHONG ZHANG, YING ZHANG
  • Patent number: 8685969
    Abstract: Compounds having formula (I), and enantiomers, and diastereomers, stereoisomers, pharmaceutically-acceptable salts thereof, formula (I) are useful as kinase modulators, including Btk modulation.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: April 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Chunjian Liu, James Lin, George V. DeLucca, Douglas G. Batt, Qingjie Liu
  • Publication number: 20140088100
    Abstract: Described herein are inhibitors of FGFR, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions to inhibit the activity of tyrosine kinases.
    Type: Application
    Filed: July 11, 2013
    Publication date: March 27, 2014
    Applicant: BLUEPRINT MEDICINES
    Inventors: Neil Bifulco, JR., Natasja Brooijmans, Brian L. Hodous, Joseph L. Kim, Chandrasekhar V. Miduturu
  • Patent number: 8673908
    Abstract: Provided is a kynurenine production inhibitor comprising a nitrogen-containing heterocyclic compound represented by formula (I): (wherein R50 and R51 may be the same or different and each represent a hydrogen atom or the like, G1 and G2 may be the same or different and each represent a nitrogen atom or the like, X represents formula (III): (wherein m1 and m2 may be the same or different and each represent an integer of 0 or 1, Y represents an oxygen atom or the like, and R6 and R7 may be the same or different and each represent a hydrogen atom or the like), R1 represents optionally substituted lower alkyl or the like, R2 represents a hydrogen atom or the like, and R3 represents optionally substituted lower alkyl or the like), and the like.
    Type: Grant
    Filed: November 9, 2009
    Date of Patent: March 18, 2014
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Nobuyoshi Amishiro, Yuichi Fukuda, Keisuke Kimpara, Motoya Mie, Hisashi Tagaya, Takeshi Takahashi
  • Publication number: 20140073782
    Abstract: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
    Type: Application
    Filed: November 11, 2013
    Publication date: March 13, 2014
    Applicant: Endo Pharmaceuticals Inc.
    Inventors: Roger A. Smith, Scott Kevin Thompson, Subramanya Hosahalli, Mallesham Bejugam, Srinivas Nanduri, Sunil Kumar Panigrahi, Natarajan Mahalingam