Spiro Patents (Class 544/70)
  • Publication number: 20150148328
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Application
    Filed: June 21, 2013
    Publication date: May 28, 2015
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo
  • Publication number: 20150111884
    Abstract: Described herein are antibacterial compounds of formula I, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Michael P. Curtis, Timothy Allan Johnson, Manjinder S. Lall, Peter Laurence Toogood, Joseph S. Warmus
  • Publication number: 20150105370
    Abstract: Embodiments of the disclosure relate to selectively substituted quinoline compounds that act as antagonists or inhibitors for Toll-like receptors 7 and/or 8, and their use in pharmaceutical compositions effective for treatment of systemic lupus erythematosus (SLE) and lupus nephritis.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: ERIC CARLSON, HANS HANSEN, LYNN HAWKINS, SALLY ISHIZAKA, MATTHEW MACKEY, SHAWN SCHILLER, CHIKAKO OGAWA, HEATHER DAVIS
  • Publication number: 20150080393
    Abstract: The present invention is directed to spirocyclic compounds which are inhibitors of tryptophan hydroxylase (TPH), particularly isoform 1 (TPH1), that are useful in the treatment of diseases or disorders associated with peripheral serotonin including, for example, gastrointestinal, cardiovascular, pulmonary, inflammatory, metabolic, and low bone mass diseases, as well as serotonin syndrome, and cancer.
    Type: Application
    Filed: September 5, 2014
    Publication date: March 19, 2015
    Inventors: Stéphane De Lombaert, Daniel R. Goldberg, Kenneth Brameld, Eric Brian Sjogren, Andrew Scribner
  • Patent number: 8969325
    Abstract: Disclosed herein are compounds of formula (I): or pharmaceutically acceptable salts thereof, wherein X1, L, Rx, Ry, G, Z, A, m, n, and p are as defined in the specification. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: December 17, 2012
    Date of Patent: March 3, 2015
    Assignee: AbbVie Inc.
    Inventors: Michael J. Dart, Philip R. Kym, Eric A. Voight, Anurupa Shrestha, Jerome F. Daanen, Tammie K. Jinkerson, Ryan G. Keddy, Sridhar Peddi, Arthur Gomtsyan, Michael E. Kort, Gregory A. Gfesser, Kevin R. Woller, Derek W. Nelson
  • 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
  • Patent number: 8957251
    Abstract: This disclosure describes the molecular cloning of a pactamycin biosynthetic gene cluster from Streptomyces pactum ATCC 27456, characterization of individual genes in the gene cluster and the proteins encoded thereby as well as uses thereof. The pactamycin gene cluster is located within an 86.35 kilobases genetic locus and includes 53 open reading frames, 26 of which are considered to be the core cluster directly involved in the biosynthesis of pactamycin. The present disclosure also relates to the use of the pactamycin biosynthetic genes located within the identified gene cluster for drug design and development purposes, including the development of pactamycin analogs that are more efficacious and less toxic. Also provided are drugs and antibiotics so produced, as well as methods of their use.
    Type: Grant
    Filed: April 18, 2008
    Date of Patent: February 17, 2015
    Assignee: State of Oregon Acting by and Through the State Board of Higher Education on Behalf of Oregon State University
    Inventors: Taifo Mahmud, Takuya Ito, Patricia M. Flatt, Niran Roongsawang, Norifumi Shirasaka
  • Patent number: 8952149
    Abstract: Described herein are antibacterial compounds of formula I, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical composition.
    Type: Grant
    Filed: September 24, 2013
    Date of Patent: February 10, 2015
    Assignee: Zoetis LLC
    Inventors: Michael Curtis, Timothy Allan Johnson, Manjinder S. Lall, Peter Laurence Toogood, Joseph S. Warmus
  • Publication number: 20150038490
    Abstract: The present invention is directed to spiropyrrolidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
    Type: Application
    Filed: October 20, 2014
    Publication date: February 5, 2015
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Kun Liu, Shawn J. Stachel, Craig A. Coburn, Thomas G. Steele, Richard Soll, Hao Wu, Xuanjin Peng, Yaxian Cai, Xiaoxiang Du, Jian Li
  • Patent number: 8933070
    Abstract: Provided herein are methods, uses and compositions for treating a patient with cancer wherein the cancer is characterized by a PTEN gene mutation. In particular embodiments, the methods comprise administering to the patient a composition comprising a therapeutically effective amount of a PLK4 antagonist, and identifying a patient that is likely to be responsive to PLK4 antagonist therapy, if PTEN gene mutation is present.
    Type: Grant
    Filed: July 4, 2011
    Date of Patent: January 13, 2015
    Assignee: University Health Network
    Inventors: Guohua Pan, Jacqueline M. Mason, Xin Wei, Miklos Feher
  • Publication number: 20150011752
    Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.
    Type: Application
    Filed: September 4, 2014
    Publication date: January 8, 2015
    Inventors: Aranapakam Mudumbai VENKATESAN, Zecheng CHEN, Christoph Martin DEHNHARDT, Osvaldo DOS SANTOS, Efren Guillermo DELOS SANTOS, Arie ZASK, Jeroen Cunera VERHEIJEN, Joshua Aaron KAPLAN, David James RICHARD, Semiramis AYRAL-KALOUSTIAN, Tarek Suhayl MANSOUR, Ariamala GOPALSAMY, Kevin Joseph CURRAN, Mengxiao SHI
  • Publication number: 20150005295
    Abstract: Inhibitors of HBV replication of formula (I) including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R1-R5, B and Z have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HBV inhibitors, in HBV therapy.
    Type: Application
    Filed: January 4, 2013
    Publication date: January 1, 2015
    Inventors: Koen Vandyck, Geerwin Yvonne Paul Haché, Geert Rombouts, Wim Gaston Verschueren, Pierre Jean-Marie Raboisson
  • Publication number: 20150005304
    Abstract: The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: January 15, 2013
    Publication date: January 1, 2015
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Vijayalaksmi Arumugam, Michael Paul Deninno, Bryan A. Frieman, Edward Adam Kallel, Mark Thomas Miller, Johnny Uy, Jinglan Zhou
  • Patent number: 8921363
    Abstract: The present invention relates to a compound represented by general formula I: or a stereoisomer, tautomer, hydrate, solvate or pharmaceutically acceptable salt thereof, wherein A1, A2, A3, A4, A5, A6, R2, R7, W, X, Y and Z are defined within. These compounds are useful for the modulation of ?-secretase enzyme activity and for the treatment of ?-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions.
    Type: Grant
    Filed: August 4, 2011
    Date of Patent: December 30, 2014
    Assignee: Amgen Inc.
    Inventors: Ana Elena Minatti, Yuan Cheng, Wenge Zhong
  • Patent number: 8921576
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: December 30, 2014
    Assignee: Kowa Company, Ltd.
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Patent number: 8921545
    Abstract: The present invention is directed to novel synthetic methods for preparing a spiro cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein.
    Type: Grant
    Filed: April 6, 2011
    Date of Patent: December 30, 2014
    Assignee: University Health Network
    Inventors: Graham Cumming, Narendra Kumar B. Patel, Bryan T. Forrest, Yong Liu, Sze-Wan Li, Peter Brent Sampson, Louise G. Edwards, Heinz W. Pauls
  • Publication number: 20140378680
    Abstract: Provided herein are compounds, compositions, and methods in the field of medicinal chemistry. The compounds and compositions provided herein relate to spiro-oxindoles which function as antagonists of the interaction between p53 and MDM2, and their use as therapeutics for the treatment of cancer and other diseases.
    Type: Application
    Filed: September 12, 2014
    Publication date: December 25, 2014
    Inventors: Shaomeng Wang, Shanghai Yu, Wei Sun, SanJeev Kumar, Duxin Sun, Peng Zou, Donna McEachern, Yujun Zhao
  • Publication number: 20140350005
    Abstract: Provided are D2 or D3 antagonist compounds and pharmaceutical compositions of formula I and pharmaceutically acceptable salts thereof, or isomers thereof, wherein R1, R2 and R3 are as defined herein. The invention further comprises methods for making the compounds of the invention and methods for the treatment of conditions mediated by the dopamine D2 or D3 receptor from the compounds of the invention.
    Type: Application
    Filed: February 19, 2014
    Publication date: November 27, 2014
    Inventors: GARY W. LUEHR, ARATHI SUNDARAM, PRIYADARSHINI JAISHANKAR, PHILIP W. PAYNE, PASCAL DRUZGALA
  • Patent number: 8895750
    Abstract: The present invention encompasses compounds of the formula (I) wherein the groups ring A and Cy are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: November 25, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Todd Bosanac, Michael J. Burke, Darren Disalvo, Wang Mao, John Westbrook
  • Publication number: 20140343032
    Abstract: The invention provides novel compounds having the general formula: wherein R1, R2, R3 and R4 are as defined in the description and in the claims, as well as or pharmaceutically acceptable salts, or tautomerism isomers, or enantiomers, or diastereomers thereof. The invention also contains compositions including the compounds and methods of using the compounds.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Lei Guo, Taishan Hu, Yimin Hu, Buelent Kocer, Buyu Kou, Gangqin Li, Xianfeng Lin, Haixia Liu, Hong Shen, Houguang Shi, Guolong Wu, Zhisen Zhang, Mingwei Zhou, Wei Zhu
  • Patent number: 8889671
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
    Type: Grant
    Filed: January 21, 2014
    Date of Patent: November 18, 2014
    Assignee: AstraZeneca AB
    Inventors: Gregory Steven Basarab, Madhusudhan Reddy Gowravaram, Sheila Irene Hauck, Fei Zhou
  • Publication number: 20140326979
    Abstract: Novel spirobifluorene compounds for light emitting devices where an SBF or Open SBF unit is substituted by a nitrogen atom, which is part of a ring system comprising two aromatic or heteroaromatic rings.
    Type: Application
    Filed: September 24, 2012
    Publication date: November 6, 2014
    Inventors: Dominique Bascour, Jonathan Maunoury, Enrico Orselli
  • Patent number: 8871210
    Abstract: The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
    Type: Grant
    Filed: November 8, 2013
    Date of Patent: October 28, 2014
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Masaya Kokubo, Motoyuki Tanaka, Hiroshi Ochiai, Yoshikazu Takaoka, Shiro Shibayama
  • Publication number: 20140315902
    Abstract: The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
    Type: Application
    Filed: April 18, 2014
    Publication date: October 23, 2014
    Inventors: Yaping Sun, Liang Lu, Wenqing Yao, Jincong Zhuo, Liangxing Wu, Meizhong Xu, Ding-Quan Qian, Chunhong He, Fenglei Zhang
  • Publication number: 20140309207
    Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.
    Type: Application
    Filed: October 18, 2012
    Publication date: October 16, 2014
    Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
  • Publication number: 20140302988
    Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising, firstly, the 1,2,4-triazolyl-substituted ketoenols and, secondly, a crop plant compatibility-improving compound. The present invention furthermore relates to the boosting of the action of crop protection compositions comprising, in particular, 1,2,4-triazolyl-substituted ketoenols, through the addition of ammonium salts or phosphonium salts and optionally penetrants, to the corresponding compositions, to processes for producing them and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.
    Type: Application
    Filed: August 10, 2012
    Publication date: October 9, 2014
    Applicant: Bayer Intellectual Property GMBH
    Inventors: Wolfgang Gienckle, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
  • Publication number: 20140288063
    Abstract: The present invention pertains to the field of medical technology, and particularly relates to a heterocyclic substituted pyrimidine compound represented by General Formula (I) and its pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4 and R5 are as defined in the description, the present invention also relates to a preparation method of the compound, a pharmaceutical composition containing the compound, and a use of the compound and the pharmaceutical composition in preparation of a medicine for enhancing a cGMP signal transduction function or a medicine for treating or preventing sexual dysfunction and diseases with lower urinary tract symptoms.
    Type: Application
    Filed: July 19, 2012
    Publication date: September 25, 2014
    Applicant: Xuanzhu Pharma Co., Ltd.
    Inventors: Yongqian Wu, Aichen Wang
  • Patent number: 8841296
    Abstract: This invention provides novel substituted 1,4-dioxa-8-azaspiro[4,5]decane compounds of the general formula (1), wherein R1 is selected from phenethyl, 4,6-dimethoxypyrimidin-2-yl and (2-chloro-5-thiazolyl)methyl and R2 is selected from the group consisting of hydroxy, 4-bromo-2-chlorophenoxy, morpholin-4-yl, (2-chloro-5-thiazolyl)methyloxy, benzyloxy, phenylsulfanyl, benzotriazol and 5-chloro-2-fluoroanilino. The present invention also relates to a process for the preparation of novel substituted 1,4-dioxa-8-azaspiro[4,5]decanes of general formula (1). The novel substituted 1,4-dioxa-8-azaspiro[4,5]decane of general formula (1) has fungicidal activity.
    Type: Grant
    Filed: March 23, 2010
    Date of Patent: September 23, 2014
    Assignee: Council of Scientific and Industrial Research, Anusandhan Bhawan, Rafi Marg
    Inventors: Mukund Vinayak Deshpande, Sunita Ranjan Deshpande, Fazal Shirazi, Preeti Madhukar Chaudhary, Nelavelli Malleswara Rao, Baidyanath Mohanty, Nageshwar Nath Sharma, Anand Kumar Bachhawat, Ganesan Kaliannan, Sanjoy Paul, Raj Kumar, Bommena Vittal Rao, Bhimrao Bodhanrao Gawali, Vaddu Venkata Narayana Reddy, Jhillu Singh Yadav
  • Publication number: 20140275017
    Abstract: Compounds of Formula I: (wherein variables A1, A2, A3, ring-B, m, n, J, E1, E2, E3, R5, RPG and Y are as described herein), which are useful as antagonists of CGRP receptors, and useful in the treatment or prevention of diseases in which CGRP receptors are involved, such as headache, and in particular migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising the compounds of formula (I) and the use of these compounds and compositions in the prevention or treatment of diseases in which CGRP receptors are involved.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Craig A. Stump, Amy G. Quigley, Cory R. Theberge, Michael R. Wood
  • Publication number: 20140275066
    Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: G1 THERAPEUTICS, INC.
    Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
  • Publication number: 20140275067
    Abstract: This invention is in the area of improved compounds, compositions and methods of transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC) as well as renal cells, from damage associated with DNA damaging chemotherapeutic agents. In one aspect, improved protection of healthy cells is disclosed using disclosed compounds that act as highly selective and short, transiently-acting cyclin-dependent kinase 4/6 (CDK 4/6) inhibitors when administered to subjects undergoing DNA damaging chemotherapeutic regimens for the treatment of proliferative disorders.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: G1 Therapeutics, Inc.
    Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
  • Publication number: 20140274896
    Abstract: This invention is in the area of improved compounds and methods for transiently protecting healthy cells, and in particular hematopoietic stem and progenitor cells (HSPC), from the damage associated with ionizing radiation (IR) exposure using selective radioprotectants.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: G1 THERAPEUTICS, INC.
    Inventors: Norman E. Sharpless, Jay Copeland Strum, John Emerson Bisi, Patrick Joseph Roberts, Francis Xavier Tavares
  • Publication number: 20140275019
    Abstract: The present invention relates to tetrahydropyridine derivatives of formula (1) which may be therapeutically useful as anti-bacterial agents, more particularly FabI inhibitors. in which X, Y, Z and “n” have the same meanings given in the specification, and pharmaceutically acceptable salts and pharmaceutically acceptable stereoisomers thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage in inhibiting Enoyl-ACP reductase enzyme (FabI) activity. The present invention also provides methods for synthesizing and administering the FabI inhibitory compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitory compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 18, 2014
    Applicants: Aurigene Discovery Technologies Limited, UM Pharmauji Sdn.BHD
    Inventors: Mohamed Takhi, Subramanya Hosahalli, Sunil Kumar Panigrahi, Muni Kumar Mahadari, Chandrashekar Reddy Kottam, Noorsaadah Abd Rahman, Rohana Yusof
  • 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: 20140256935
    Abstract: The present invention relates to naphthopyran compounds that include at least one compound represented by the following Formulas (I), (II), and (III): With reference to Formulas (I), (II), and (III), there is the proviso that: (i) at least one R1 is a group L; and/or (ii) B and/or B? is substituted with at least one group L. The group L can be described as a lengthening group. The present invention also relates to photochromic-dichroic naphthopyran compounds and photochromic-dichroic articles containing such compounds.
    Type: Application
    Filed: March 11, 2013
    Publication date: September 11, 2014
    Applicant: Transitions Optical, Inc.
    Inventors: Darrin R. Dabideen, Meng He, Anil Kumar
  • Publication number: 20140225040
    Abstract: The present invention relates to compounds for use in electronic devices, preferably organic electroluminescent devices. The invention furthermore relates to processes for the preparation of these compounds and to electronic devices comprising these compounds, preferably in a function as matrix materials and/or as electron-transport materials.
    Type: Application
    Filed: July 3, 2012
    Publication date: August 14, 2014
    Applicant: Merck Patent GmbH Patents & Scientific Information
    Inventors: Amir Hossain Parham, Christof Pflumm, Anja Jatsch
  • Patent number: 8791109
    Abstract: Compositions, preferably pharmaceutical compositions, containing micronized tanaproget, or pharmaceutically acceptable salt thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, butylated hydroxyanisole, povidone, and magnesium stearate, are provided. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic to disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.
    Type: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Wyeth LLC
    Inventors: Arwinder S. Nagi, Ramarao S. Chatlapalli, Shamim Hasan, Rolland W. Carson, Mohamed Ghorab
  • Publication number: 20140206677
    Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Applicant: AstraZeneca AB
    Inventors: Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
  • Publication number: 20140206663
    Abstract: The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treating immunological and oncological conditions.
    Type: Application
    Filed: March 19, 2014
    Publication date: July 24, 2014
    Inventors: Jianfei Wang, Eric C. Breinlinger, Martine Barth, Michael M. Friedman, Fabrice Guillier, Maria A. Argiriadi, Jeremy Edmunds, Dominique Potin, Adrian D. Hobson, Wentao Wu, Dominique Bonafoux, Didier Thomas, Dawn M. George, Linlin Dai, Yang Zhang
  • Patent number: 8778938
    Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit RNA-containing virus, particularly the Hepatitis C Virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the Hepatitis C Virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
    Type: Grant
    Filed: June 3, 2011
    Date of Patent: July 15, 2014
    Assignee: Enanta Pharmaceuticals, Inc.
    Inventors: Yao-Ling Qiu, Ce Wang, Hui Cao, Xiaowen Peng, Datong Tang, Yat Sun Or
  • Patent number: 8772271
    Abstract: The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, magnesium stearate, micronized edetate calcium disodium hydrous, and micronized sodium thiosulfate pentahydrate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.
    Type: Grant
    Filed: May 9, 2013
    Date of Patent: July 8, 2014
    Assignee: Wyeth LLC
    Inventors: Arwinder S. Nagi, Ramarao Chatlapalli, Shamim Hasan, Mohamed Ghorab, Dhaval Gaglani
  • Patent number: 8772288
    Abstract: The present disclosure is directed to new inhibitors of the p38 mitogen-activated protein kinase having the general formula (I), processes for preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: July 8, 2014
    Assignee: Almirall, S.A.
    Inventors: Paul Robert Eastwood, Jacob Gonzalez Rodriguez, Bernet Vidal Juan, Nuria Aguilar Izquierdo
  • Patent number: 8765940
    Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110 activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lymphob
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: July 1, 2014
    Assignee: Amgen Inc.
    Inventors: Matthew Brown, Yi Chen, Timothy David Cushing, Felix Gonzalez Lopez De Turiso, Xiao He, Todd J. Kohn, Julia Winslow Lohman, Vatee Pattaropong, Jennifer Seganish, Youngsook Shin, Jillian L. Simard
  • Patent number: 8765744
    Abstract: The present invention relates to compounds defined by formula I wherein the variables R1, R2, R3, R4, R7, A, Z and m are as defined herein. The compounds of formula (I) are inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 (11beta-HSD1) 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: Grant
    Filed: June 23, 2011
    Date of Patent: July 1, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventor: Frank Himmelsbach
  • Publication number: 20140179695
    Abstract: The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing or treating diseases or conditions associated with and/or mediated by ?-secretase activity, hydrolysis of a ?-secretase site of a ?-amyloid precursor protein, and/or ?-amyloid protein accumulation, including a pharmaceutical composition for preventing or treating diseases including, but not limited to, Glaucoma, MCI (Mild cognitive impairment) or Alzheimer's disease, especially, Alzheimer's disease.
    Type: Application
    Filed: February 27, 2014
    Publication date: June 26, 2014
    Applicants: CoMentis, Inc., ASTELLAS PHARMA INC.
    Inventors: Ryosuke MUNAKATA, Makoto INOUE, Hiroaki TOMINAGA, Shingo YAMASAKI, Yasuhiro SHIINA, Kiyohiro SAMIZU, Hisao HAMAGUCHI, Lin HONG
  • Publication number: 20140161801
    Abstract: The invention relates to a quinazoline derivative represented by the general formula (I), a pharmaceutical acceptable salt and a stereoisomer thereof as tyrosine kinase inhibitor, wherein R1, R2, R3, R3?, R4, R5, R6, X, L, T, Z and q are as defined in the specification. The invention also relates to a process for preparing the same, a pharmaceutical composition and a pharmaceutical formulation containing the derivative, use of the derivative for treating excessive proliferative diseases and chronic obstructive pulmonary disease and use of the derivative in the manufacture of a medicament for treating excessive proliferative diseases and chronic obstructive pulmonary disease.
    Type: Application
    Filed: May 28, 2012
    Publication date: June 12, 2014
    Applicant: XUANZHU PHARMA CO., LTD.
    Inventors: Frank Wu, Aichen Wang
  • Publication number: 20140154527
    Abstract: A chromene compound having a short fading half period, especially, a short fading half period even at a low temperature in a general-purpose polymer solid matrix. The chromene compound is represented by the following formula (1). wherein R1 is a hydroxyl group or the like, R2 and R3 are each an aryl group or the like, C* is a spiro carbon atom, a spiro ring A represented by the following formula is a saturated hydrocarbon ring having 4 to 12 ring member carbon atoms or the like, and at least one ring member carbon atom constituting the ring A is a group represented by the following formula (4), and X is a divalent group such as arylene group, wherein R7 and R8 are each a cycloalkyl group or the like.
    Type: Application
    Filed: June 19, 2012
    Publication date: June 5, 2014
    Applicant: TOKUYAMA CORPORATION
    Inventors: Shinobu Izumi, Kazuhiro Teranishi, Yusuke Daikoku, Mitsuyoshi Sando
  • Publication number: 20140147412
    Abstract: Disclosed are spiro compounds of formula (I), or stereomers, geometric isomers, tautomers, nitrogen oxides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof. The compounds can be used to treat hepatitis C virus (HCV) infection or hepatitis C disease. Furthermore disclosed are pharmaceutical compositions containing the compounds and the method of using the compounds or pharmaceutical compositions in the treatment of HCV infection or hepatitis C disease.
    Type: Application
    Filed: July 9, 2012
    Publication date: May 29, 2014
    Applicant: SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Jiancun Zhang, Yingjun Zhang, Hongming Xie, Qingyun Ren, Huichao Luo, Tianzhu Yu, Yumei Tan
  • Patent number: 8729079
    Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.
    Type: Grant
    Filed: August 23, 2012
    Date of Patent: May 20, 2014
    Assignee: Endo Pharmaceuticals Inc.
    Inventors: Aranapakam Venkatesan, Roger Astbury Smith, Subramanya Hosahalli, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
  • Publication number: 20140128371
    Abstract: The present invention relates to compounds of Formula (I): to pharmaceutically acceptable salts thereof, to methods of using them to treat bacterial infections, and to methods for their preparation.
    Type: Application
    Filed: January 13, 2014
    Publication date: May 8, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Kevin BARVIAN, Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU