Ring Nitrogen In The Additional Hetero Ring Patents (Class 546/208)
  • Patent number: 10407403
    Abstract: The present invention discloses a preparation method of cobimetinib (XL518, GDC-0973) (I). The preparation steps include: taking (2S)-2-piperidinecarboxylic acid as the raw material, performing acyl cyanation, hydrolysis, esterification and Boc protection to obtain an intermediate [2-oxo-2-((2S)-1-tert-butoxycarbonylpiperidin-2-yl)]acetate, performing an addition reaction, a reduction reaction and a cyclization reaction on the intermediate to obtain an intermediate (2S)-1-tert-butoxycarbonyl-2-(3-hydroxyazetidin-3-yl)piperidine, and performing a condensation reaction with a side chain to obtain the cobimetinib (I). The preparation method has the advantages of accessible raw materials, simple technique, high economy and environment friendliness, and is suitable for industrial production.
    Type: Grant
    Filed: May 31, 2018
    Date of Patent: September 10, 2019
    Assignee: Suzhou Miracpharma Technology Co., Ltd.
    Inventor: Xuenong Xu
  • Patent number: 10030035
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 receptor and which are useful in the treatment of muscarinic M1 receptor mediated diseases. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where m, p, q, W, Z, Y, X1, X2, R1, R2 R3 and R4 are as defined herein.
    Type: Grant
    Filed: March 19, 2015
    Date of Patent: July 24, 2018
    Assignee: Heptares Therapeutics Limited
    Inventors: Miles Stuart Congreve, Giles Albert Brown, Benjamin Gerald Tehan, Mark Pickworth, Julie Elaine Cansfield
  • Patent number: 9555139
    Abstract: Described herein are compounds, pharmaceutical compositions and methods for treating pathogenic cell populations. The compounds described herein include conjugates of tubulysins and vitamin receptor binding ligands. The conjugates also include a releasable bivalent linker.
    Type: Grant
    Filed: March 13, 2008
    Date of Patent: January 31, 2017
    Assignee: Endocyte, Inc.
    Inventors: Iontcho Radoslavov Vlahov, Christopher Paul Leamon, Yu Wang
  • Patent number: 9505747
    Abstract: The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: November 29, 2016
    Assignee: Endocyte, Inc.
    Inventors: Iontcho Radoslavov Vlahov, Hari Krishna R. Santhapuram, Paul Joseph Kleindl, Christopher Paul Leamon, Fei You
  • Publication number: 20150141399
    Abstract: Disclosed are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
    Type: Application
    Filed: February 5, 2015
    Publication date: May 21, 2015
    Inventors: Naing Aay, Neel Kumar Anand, Charles M. Blazey, Owen Joseph Bowles, Joerg Bussenius, Simona Costanzo, Jeffry Kimo Curtis, Steven Charles DeFina, Larisa Dubenko, Anagha Abhijit Joshi, Abigail R. Kennedy, Angie Inyoung Kim, Elena S. Koltun, Jean-Claire Limun Manalo, Csaba J. Peto, Kenneth D. Rice, Tsze H. Tsang
  • Publication number: 20150141397
    Abstract: Aniline compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer.
    Type: Application
    Filed: August 5, 2014
    Publication date: May 21, 2015
    Inventors: Trevor T. Charvat, Junfa Fan, Christopher W. Lange, Manmohan Reddy Leleti, Yandong Li, Venkat Reddy Mali, Jeffrey P. McMahon, Jay Powers, Sreenivas Punna, Ju Yang
  • Publication number: 20150141425
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Application
    Filed: November 3, 2014
    Publication date: May 21, 2015
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20150133368
    Abstract: Antiviral protease inhibitors, including macrocylic transition state inhibitors and peptidomimetics are disclosed, along with related antiviral compounds, and methods of using the same to treat or prevent viral infection and disease. The compounds possess broad-spectrum activity against viruses that belong to the picornavirus-like supercluster, which include important human and animal pathogens including noroviruses, sapoviruses, enteroviruses, poliovirus, foot-and-mouth disease virus, hepatitis A virus, human rhinovirus (cause of common cold), human coronavirus (another cause of common cold), transmissible gastroenteritis virus, murine hepatitis virus, feline infectious peritonitis virus, and severe acute respiratory syndrome coronavirus.
    Type: Application
    Filed: May 2, 2013
    Publication date: May 14, 2015
    Inventors: Kyeong-Ok Chang, Yunjeong Kim, William C. Groutas
  • Publication number: 20150126518
    Abstract: The present invention relates to biguanide compounds and use thereof, more particularly, to biguanide derivatives exhibiting excellent effects for inhibition of cancer cell proliferation and inhibition of cancer metastasis and recurrence, a method for preparing the same, a pharmaceutical composition containing the same as an active ingredient, and a method of prevention or treatment of cancer comprising the step of administering an effective amount of the composition to a subject in need thereof.
    Type: Application
    Filed: October 30, 2014
    Publication date: May 7, 2015
    Applicant: HANALL BIOPHARMA CO., LTD.
    Inventors: Hong Woo KIM, Ji Sun LEE, Hye Jin HEO, Hong Bum LEE, Jae Kap JEONG, Ji Hyun PARK, Seo-il KIM, Young Woo LEE
  • Publication number: 20150126516
    Abstract: A piperidine compound represented by the following Formula (1): wherein ring A, ring B, and ring C are the same or different and each represent a benzene ring or a nitrogen-containing heteroaromatic ring; W represents a C1-C4 alkylene or alkenylene group; X, Y, and Z are the same or different and each represent a halogen atom, a C1-C6 alkyl group, a halo C1-C6 alkyl group, a C1-C6 alkoxy group, or a halo C1-C6 alkoxy group; m, n, and p are the same or different and each represent an integer of 0 to 5; when m is greater than or equal to 2, the Xs are the same or different; when n is greater than or equal to 2, the Ys are the same or different; and when p is greater than or equal to 2, the Zs are the same or different has an excellent controlling efficacy against pests.
    Type: Application
    Filed: April 12, 2013
    Publication date: May 7, 2015
    Inventor: Sadayuki Arimori
  • 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: 9023656
    Abstract: A mass label for labelling and detecting a biological molecule by mass spectroscopy, which label comprises the following structure: X-L-M wherein X is a mass marker moiety comprising the following group: formula (I), wherein the cyclic unit is aromatic or aliphatic and comprises from 0-3 double bonds independently between any two adjacent atoms; each Z is independently N, N(R1), C(R1), CO, CO(R1), C(R1)2, O or S; X is N, C or C(R1); each R1 is independently H, a substituted or unsubstituted straight or branched C1-C6 alkyl group, a substituted or unsubstituted aliphatic cyclic group, a substituted or unsubstituted aromatic group or a substituted or unsubstituted heterocyclic group; and y is an integer from 0-10, L is a cleavable linker comprising an amide bond and M is a mass normalization moiety.
    Type: Grant
    Filed: July 26, 2006
    Date of Patent: May 5, 2015
    Assignee: Electrophoretics Limited
    Inventors: Christian Hamon, Josef Schwarz, Wolfgang Becker, Stefan Kienle, Karsten Kuhn, Juergen Schaefer
  • Patent number: 9018200
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Grant
    Filed: October 18, 2012
    Date of Patent: April 28, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Patent number: 9000174
    Abstract: The invention relates to piperidinyl compounds of Formula (I): or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to an assay useful for identifying such compounds as N-type calcium channel modulators or blockers. The invention is also directed to the compounds of Formula (I) and compounds identified by the above assay, and the use of such compounds to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: October 14, 2005
    Date of Patent: April 7, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Elfrida R. Benjamin, Zhengming Chen, Deyou Sha, Laykea Tafesse, Samuel F. Victory, John W. F. Whitehead
  • Publication number: 20150094267
    Abstract: The present invention relates to succinimide-activated nitroxyl compounds and methods for the synthesis of such compounds. The present invention also relates to the use of succinimide-activated nitroxyl compounds to prepare nitroxylated proteins, for example nitroxylated heme proteins (e.g., nitroxylated hemoglobin and nitroxylated myoglobin). The nitroxylated proteins are optionally also conjugated to a polyalkylene oxide (PAO), for example to a polyethylene glycol (PEG). Polynitroxylated heme proteins are useful as oxygen therapeutic agents (OTAs). The invention further relates to pharmaceutical compositions of the nitroxylated proteins and methods for the use of nitroxylated proteins in the treatment of various conditions.
    Type: Application
    Filed: March 15, 2013
    Publication date: April 2, 2015
    Inventors: Kim D. Vandegriff, Ashok Malavalli, Gnel Mkrtchyan
  • Publication number: 20150087629
    Abstract: The invention relates to a DGAT inhibitor of formula including any stereochemically isomeric form thereof, wherein A represents CH or N; the dotted line represents an optional bond in case A represents a carbon atom; X represents —O—C(?O)—; —C(?O)—C(?O)—; —NRx—C(?O)—; —Z—C(?O)—; —Z—NRx—C(?O)—; —C(?O)—Z—; —NRx—C(?O)—Z—; —C(?S)—; —NRx—C(?S)—; —Z—C(?S)—; —Z—NRx—C(?S)—; —C(?S)—Z—; —NRx—C(?S)—Z—; Z represents a bivalent radical selected from C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl; wherein each of said C1-6alkanediyl, C2-6alkenediyl or C2-6alkynediyl may optionally be substituted; and wherein two hydrogen atoms attached to the same carbon atom in C1-6alkanediyl may optionally be replaced by C1-6alkanediyl; Y represents —C(?O)—NRx— or —NRx—C(?O)—; R1 represents adamantanyl, C3-6cycloalkyl; aryl1 or Het1; R2 represents C3-6cycloalkyl, phenyl, naphtalenyl, 2,3-dihydro-1,4-benzodioxinyl, 1,3-benzodioxolyl, 2,3-dihydrobenzofuranyl or a 6-membered aromatic heterocycle containing 1 or 2 N atoms, wherein said
    Type: Application
    Filed: December 5, 2014
    Publication date: March 26, 2015
    Inventors: Jean-Pierre Andre Marc Bongartz, Joannes Theodorus Maria Linders, Lieven Meerpoel, Guy Rosalia Eugeen Van Lommen, Erwin Coesemans, Mirielle Braeken, Christophe Francis Robert Nestor Buyck, Monique Jenny Marie Berwaer, Katharina Antonia Germania J.M. De Waepenaert, Peter Walter Maria Roevens, Petr Vladimirivich Davidenko
  • Patent number: 8987248
    Abstract: The invention relates to novel substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular disorders and tumor disorders.
    Type: Grant
    Filed: March 12, 2010
    Date of Patent: March 24, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
  • Publication number: 20150080364
    Abstract: Provided herein are carbamate compounds which may be useful in the treatment of for example, pain, solid tumors and/or obesity.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 19, 2015
    Applicants: Abide Therapeutics, Inc., The Scripps Research Insititute
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Dong-Hui Wang, Olivia Weber, Benjamin F. Cravatt, Micah J. Niphakis, Armand Cognetta, Jae Won Chang
  • Publication number: 20150073139
    Abstract: The invention is directed to arylpyrrolidines compounds which exhibit excellent insecticidal efficacy and which may be used as in the agrochemical field or in the vield of veterinary medicine. The compounds are represented by formula (I): wherein the respective substituents are defined in the specification.
    Type: Application
    Filed: July 21, 2014
    Publication date: March 12, 2015
    Inventors: Ulrich GÖRGENS, Jun MIHARA, Tetsuya MURATA, Daiei YAMAZAKI, Yasushi YONETA, Koichi ARAKI, Norio SASAKI, Kei DOMON, Mamoru HATAZAWA, Eiichi SHIMOJO, Teruyuki ICHIHARA, Masashi ATAKA, Katsuhiko SHIBUYA
  • Publication number: 20150065392
    Abstract: A reactive mass label for labelling a biological molecule for detection by mass spectrometry includes the following structure: X-L-M-S-Re, wherein X is a mass marker moiety, L is a cleavable linker, M is a mass normalization moiety, and S is a mass series modifying group including the following group: wherein J is C?O, K is NH, and n is 2 or J and K are both CH2 and n is 1, m is at least 1; and Re is a reactive functionality for attaching the reactive mass label to a biological molecule.
    Type: Application
    Filed: September 15, 2014
    Publication date: March 5, 2015
    Applicant: Electrophoretics Limited
    Inventors: Christian Baumann, Stefan Kienle, Karsten Kuhn, Harald Legner
  • Patent number: 8962846
    Abstract: Melanocortin receptor antagonist compounds, processes for preparing them and uses thereof in human medicine and cosmetics are described. Melanocortin receptor antagonist compounds corresponding to the general formula (I): compositions containing them, and processes for their preparation and their use in pharmaceutical or cosmetic compositions are also described.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: February 24, 2015
    Assignee: Galderma Research & Development
    Inventors: Claire Bouix-Peter, Isabelle Carlavan, Catherine Soulet, Veronique Parnet, Johannes Voegel
  • Patent number: 8951536
    Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.
    Type: Grant
    Filed: February 28, 2013
    Date of Patent: February 10, 2015
    Assignee: Incyte Corporation
    Inventors: Andrew P. Combs, Amy Takvorian, Wenyu Zhu, Richard B. Sparks
  • Patent number: 8946446
    Abstract: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administrating these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo sulfonamide compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: April 13, 2012
    Date of Patent: February 3, 2015
    Assignee: Phenex Pharmaceuticals AG
    Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
  • Publication number: 20150025056
    Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.
    Type: Application
    Filed: October 3, 2014
    Publication date: January 22, 2015
    Applicant: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
  • Patent number: 8937181
    Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.
    Type: Grant
    Filed: April 13, 2007
    Date of Patent: January 20, 2015
    Assignee: Purdue Pharma L.P.
    Inventors: Akira Matsumura, Hidenori Mikamiyama, Bin Shao, Naoki Tsuno, Jiangchao Yao
  • Publication number: 20150011526
    Abstract: The present invention relates to 2-oxo-piperidinyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: October 10, 2012
    Publication date: January 8, 2015
    Inventors: Ali Ates, Florian Montel, Anne Valade, Olivier Lorthioir
  • Patent number: 8927726
    Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, (Het)Ar1, (Het)Ar2 and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.
    Type: Grant
    Filed: July 22, 2013
    Date of Patent: January 6, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf, Neil J. Ashweek, Nicole Harriott
  • Publication number: 20150005277
    Abstract: The invention is compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
    Type: Application
    Filed: June 21, 2014
    Publication date: January 1, 2015
    Inventors: Zhiwei Wang, Yunhang Guo
  • Patent number: 8921559
    Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, R3, R4, X, Y, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
    Type: Grant
    Filed: November 30, 2011
    Date of Patent: December 30, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: James C. Lanter, Thomas P. Markotan, Nalin Subasinghe, Zhihua Sui, Xuqing Zhang
  • Publication number: 20140378444
    Abstract: Provided herein are compositions and related methods useful for free radical scavenging, with particular selectivity for mitochondria. The compounds comprise a nitroxide-containing group attached to a mitochondria-targeting group. The compounds can be cross-linked into dimers without loss of activity. Also provided herein are methods, for preventing, mitigating and treating damage caused by radiation. The method comprises delivering a compound, as described herein, to a patient in an amount and dosage regimen effective to prevent, mitigate or treat damage caused by radiation.
    Type: Application
    Filed: November 22, 2013
    Publication date: December 25, 2014
    Applicant: University of Pittsburgh - Of the Commonwealth System of Higher Education
    Inventors: Peter Wipf, Marie-Celine Frantz
  • Publication number: 20140378430
    Abstract: The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to pyrrolidine and azetidine compounds, compositions containing them and their use in methods of treating or preventing disorders or diseases associated with AT2 receptor function including neuropathic pain, inflammatory pain, conditions associated with neuronal hypersensitivity, impaired nerve conduction velocity, cell proliferation disorders, disorders associated with an imbalance between bone resorption and bone formation and disorders associated with aberrant nerve regeneration.
    Type: Application
    Filed: January 4, 2013
    Publication date: December 25, 2014
    Applicant: SPINIFEX PHARMACEUTICALS PTY LTD
    Inventors: Thomas David McCarthy, Alan Naylor
  • Publication number: 20140376082
    Abstract: A compound is disclosed. The compound has the general structure: wherein Y is selected from the group consisting of hydrocarbons, hydrocarbons including nitrogen in the carbon backbone, and hydrocarbons including oxygen in the carbon backbone; wherein R1 and R2 are each independently selected from the group consisting of hydrogen, linear hydrocarbons, branched hydrocarbons, and cyclic hydrocarbons and wherein R1 and R2 are not both hydrogen; wherein X is selected from the group consisting of CH2, O, N—R3, S, and nothing and wherein R3 is selected from the group consisting of hydrogen, branched hydrocarbons, linear hydrocarbons, and cyclic hydrocarbons; wherein m is an integer between 1 and 50, inclusive; wherein n is an integer between 1 and 10,000, inclusive; and wherein p, q, and z are each independently an integer greater than 0.
    Type: Application
    Filed: January 24, 2012
    Publication date: December 25, 2014
    Applicant: HEWLETT-PACKARD DEVELOPMENT COMPANY, L.P.
    Inventors: Zhang-Lin Zhou, Qin Liu, Gregg Combs, James R. Owen
  • Patent number: 8912334
    Abstract: This invention provides compounds of formula I: wherein a, b, c, d, m, n, p, s, t, W, Ar1, R1, R2, R3, R4, R6, R7, and R8 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Grant
    Filed: September 11, 2013
    Date of Patent: December 16, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
  • Patent number: 8906938
    Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.
    Type: Grant
    Filed: May 14, 2013
    Date of Patent: December 9, 2014
    Assignee: ChemoCentryx, Inc.
    Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
  • Publication number: 20140357650
    Abstract: The present invention relates to novel inhibitors having high selectivity and specificity for FAP (fibroblast activation protein). Said inhibitors are useful as a human and/or veterinary medicine, in particular for the treatment and/or prevention of FAP-related disorders such as but not limited to proliferative disorders.
    Type: Application
    Filed: January 17, 2013
    Publication date: December 4, 2014
    Applicant: Fox Chase Cancer Center
    Inventors: Koen Jansen, Ingrid De Meester, Leen Heirbaut, Jonathan D. Cheng, Jurgen Joossens, Koen Augustyns, Pieter Van Der Veken
  • Publication number: 20140349368
    Abstract: The present invention relates to compounds that exhibit vasodilatory and anti-inflammatory effects by inhibiting the activity of soluble epoxide hydrolase (sEH). The present invention is also directed to methods of identifying such compounds, and use of such compounds for the treatment of diseases related to dysfunction of vasodilation, inflammation, and/or endothelial cells. In particular non-limiting embodiments, components of the invention may be used to treat hypertension.
    Type: Application
    Filed: February 17, 2014
    Publication date: November 27, 2014
    Applicant: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORK
    Inventors: Donald W. Landry, Yuli Xie, Yidong Lu, Gangli Gong, Shi-Xian Deng, Kirsten Alison Rinderspacher
  • Patent number: 8889716
    Abstract: Certain compounds and pharmaceutically acceptable salts are provided herein. Also provided are pharmaceutical compositions comprising at least one compound or pharmaceutically acceptable salt therein and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain disease states responsive to the inhibition of transglutaminase TG2 activity are described. These disease states include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one compound or pharmaceutically acceptable salt thereof as a single active agent or administering at least one compound or pharmaceutically acceptable salt thereof in combination with one or more other therapeutic agents.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: November 18, 2014
    Assignee: CHDI Foundation, Inc.
    Inventors: Michael Prime, Stephen Martin Courtney, Richard Marston, Celia Dominguez, Douglas MacDonald, John Wityak
  • Publication number: 20140336158
    Abstract: A NK1 antagonist having the formula (I), wherein Ar1 and Ar2 are optionally substituted phenyl or heteroaryl, X1 is an ether, thio or imino linkage, R4 and R5 are not both H or alkyl, and the remaining variables are as defined in the specification, useful for treating a number of disorders, including emesis, depression, anxiety and cough. Pharmaceutical compositions. Methods of treatment and combinations with other agents are also disclosed.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Inventors: Sunil Paliwal, Gregory A. Reichard, Cheng Wang, Dong Xiao, Hon-Chung Tsui, Neng-Yang Shih, Juan D. Arredondo, Michelle Laci Wrobleski, Anandan Palani
  • Publication number: 20140330010
    Abstract: Provided are novel compounds that are useful in the prevention or treatment of such diseases as dementia, Alzheimer's disease, attention-deficient hyperactivity disorder, schizophrenia, epilepsy, central convulsion, obesity, diabetes mellitus, hyperlipidemia, narcolepsy, idiopathic hypersomnia, behaviorally induced insufficient sleep syndrome, sleep apnea syndrome, circadian rhythm disorder, parasomnia, sleep related movement disorder, insomnia, and depression, or allergic rhinitis, or pharmaceutically acceptable salts of such compounds.
    Type: Application
    Filed: December 7, 2012
    Publication date: November 6, 2014
    Applicant: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Toshio Nakamura, Seiji Masuda
  • Publication number: 20140329815
    Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
    Type: Application
    Filed: July 21, 2014
    Publication date: November 6, 2014
    Inventors: Carl R. ILLIG, Shelley K. Ballentine, Jinsheng Chen, Renee Louise Desjarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
  • Patent number: 8877761
    Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of Formulas A and B: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined above. The invention further relates to pharmaceutical compositions comprising the compounds and pharmaceutically acceptable salts and to methods of treating diabetes mellitus and its complications, cancer, ischemia, inflammation, central nervous system disorders, cardiovascular disease, Alzheimer's disease and dermatological disase pression, virus diseases, inflammatory disorders, or diseases in which the liver is a target organ.
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: November 4, 2014
    Assignee: Pfizer Inc.
    Inventors: Hui Li, Seiji Nukui, Stephanie Anne Scales, Min Teng, Chunfeng Yin
  • Patent number: 8871790
    Abstract: Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders.
    Type: Grant
    Filed: March 8, 2012
    Date of Patent: October 28, 2014
    Assignee: 3-V Biosciences, Inc.
    Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu
  • Publication number: 20140309193
    Abstract: There are provided inter alia compounds of formula (I) wherein R1, R2, R3, R4a and R4b are as defined in the specification and their use in therapy, especially in the treatment of bacterial (e.g. pneumococcal) infections.
    Type: Application
    Filed: December 5, 2012
    Publication date: October 16, 2014
    Inventors: Peter William Andrew, Rana Lonnen, Mafalda Pires Damaso, Fritz-Frieder Frickel, Simon Christopher Hirst, Mark William Davies, Daniel Hamza
  • Publication number: 20140296202
    Abstract: Substituted piperidinyl compounds of the formula (I): are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119.
    Type: Application
    Filed: October 18, 2012
    Publication date: October 2, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Milana Maletic, Harold B. Wood, Wanying Sun
  • Publication number: 20140296196
    Abstract: A compound having the general structure shown in Formula I: or pharmaceutically acceptable salts and/or solvates thereof are useful in treating diseases or conditions mediated by NK1 receptors, for example various physiological disorders, symptoms or diseases, including emesis, depression, anxiety and cough.
    Type: Application
    Filed: June 13, 2014
    Publication date: October 2, 2014
    Inventors: Anandan Palani, Xianhai Huang, Dong Xiao, Sunil Paliwal, Hon-Chung Tsui, Michelle Laci Wrobleski, Ashwin U. Rao, Cheng Wang, Sapna S. Shah, Neng-Yang Shih
  • Publication number: 20140288065
    Abstract: The present invention provides a pyrrolidine compound of General Formula (1) or a salt thereof, wherein R101 and R102 are each independently a phenyl group or a pyridyl group, the phenyl group or the pyridyl group may have one or more substituents selected from halogen atoms and lower alkyl groups optionally substituted with one or more halogen atoms, etc. The pyrrolidine compound or a salt thereof of the present invention is usable to produce a pharmaceutical preparation having a wider therapeutic spectrum and being capable of exhibiting sufficient therapeutic effects after short-term administration.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Muneaki KURIMURA, Shinichi TAIRA, Takahiro TOMOYASU, Nobuaki ITO, Kuninori TAI, Noriaki TAKEMURA, Takayuki MATSUZAKI, Yasuhiro MENJO, Shin MIYAMURA, Yohji SAKURAI, Akihito WATANABE, Yasuyo SAKATA, Takumi MASUMOTO, Kohei AKAZAWA, Haruhiko SUGINO, Naoki AMADA, Satoshi OHASHI, Tomoichi SHINOHARA, Hirofumi SASAKI, Chisako MORITA, Junko YAMASHITA, Satoko NAKAJIMA
  • Publication number: 20140288045
    Abstract: Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Inventors: Pingda Ren, Yi Liu, Liansheng Li, Jun Feng, Tao Wu
  • Publication number: 20140275480
    Abstract: The disclosure includes novel processes for producing Sovaprevir comprising adding compound E to F-1 to provide Sovaprevir. The disclosure further includes intermediates useful for producing Sovaprevir. The disclosure also include a novel crystalline form of Sovaprevir, Form F, and a method for preparing spray-dried amorphous Sovaprevir from crystalline Form F.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: Achillion Pharmaceuticals, Inc.
    Inventors: Avinash Phadke, Akihiro Hashimoto, Venkat Gadhachanda
  • Publication number: 20140275010
    Abstract: The present invention provides quaternary salts, such as those of Formula I: as well as the use thereof in methods of treatment for cancer.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Inventors: Guo Zhu Zheng, Yuan Wang, Gregg F. Keany, Kenzo Arai, Kazunobu Kira, Xiang Liu, Nick Gearhart, Baudouin Gerard
  • Patent number: RE45323
    Abstract: Object of the present invention are novel substituted compounds of the formula 1, wherein A, R1, R2, R3 and R4 are defined as in the description. Another object of the present invention is to provide antagonists of CCR3, more particularly to provide pharmaceutical compositions comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of at least one of the compounds of the present invention or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 7, 2014
    Date of Patent: January 6, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Marc Grundl, Horst Dollinger, Riccardo Giovannini, Christoph Hoenke, Matthias Hoffmann, Jan Kriegl, Domnic Martyres, Georg Rast, Peter Seither