Five-membered Hetero Ring Consisting Of One Nitrogen And Four Carbons Patents (Class 544/372)
  • Patent number: 10150772
    Abstract: The present disclosure relates to crystalline forms of 4,5,6,7-tetrahydro-11-methoxy-2-[(4-methyl-1-piperazinyl)methyl]-1H-cyclopenta[a]pyrrolo[3,4-c]carbazole-1,3(2H)-dione, including salts forms and free base forms.
    Type: Grant
    Filed: November 25, 2015
    Date of Patent: December 11, 2018
    Assignee: CEPHALON, INC.
    Inventors: Stephen J. Bierlmaier, Ralph C. Haltiwanger, Martin J. Jacobs
  • Publication number: 20150148330
    Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.
    Type: Application
    Filed: January 16, 2015
    Publication date: May 28, 2015
    Inventors: Justin S. Cisar, Cheryl A. Grice, Todd K. Jones, Micah J. Niphakis, Jae Won Chang, Kenneth M. Lum, Benjamin F. Cravatt
  • Publication number: 20150141646
    Abstract: In certain aspects, compounds and uses thereof are provided. In certain aspects, compound-conjugates and uses thereof are provided.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 21, 2015
    Applicant: Concortis Biosystems, Corp., a wholly owned subsidary of Sorrento Therapeutics, Inc,
    Inventors: Zhenwei Miao, Yufeng Hong, Tong Zhu
  • 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
  • Patent number: 9029404
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.
    Type: Grant
    Filed: October 14, 2013
    Date of Patent: May 12, 2015
    Assignee: AbbVie Inc.
    Inventors: George A. Doherty, Steven W. Elmore, Laura A. Hexamer, Robert A. Mantei, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Todd M. Hansen
  • Patent number: 9029381
    Abstract: Disclosed herein is at least one cyclopropyl amide derivative, at least one pharmaceutical composition comprising at least one cyclopropyl amide derivative disclosed herein, and at least one method of using at least one cyclopropyl amide derivative disclosed herein for treating at least one histamine H3 receptor associated condition therewith.
    Type: Grant
    Filed: November 21, 2011
    Date of Patent: May 12, 2015
    Assignee: Astrazeneca AB
    Inventors: James Arnold, Todd Andrew Brugel, Scott Throner, Steven Wesolowski, Phil Edwards, Andrew Griffin, Thierry Groblewski, Denis Labrecque
  • Publication number: 20150105552
    Abstract: This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
    Type: Application
    Filed: October 14, 2014
    Publication date: April 16, 2015
    Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
  • 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
  • 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
  • Patent number: 8981094
    Abstract: The invention relates to a DGAT inhibitor of formula (I): 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 —C(?O)—; —O—C(?O)—; C(?O)—C(?O)—; —NRx—C(?O)—; —Z1—C(O)—; —Z1—NRx—C(?O)—; —C(?O)—Z1—; —NRx—C(?O)—Z1—; —S(?O)p-; —C(?S)—; —NRx—C(?S)—; —Z1—C(?S)—; —Z1—NRx—C(?S)—; —C(?S)—Z1-; —NRx—C(?S)—Z—; Y represents NRx—C(=0)-Z2—; —NRx—C(=0)-Z2—NRy—; —NRx—C(=0)-Z2—NRy—C(=0)-; —NRx—C(=0)-Z2—NRy—C(=0)-O—; —NRx—C(=0)-Z2-0-; —NRx—C(=0)-Z2-0-C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-; —NRx—C(=0)-0-Z2—C(=0)-0-; —NRx—C(?O)—O—Z2—O—C(?O)—; —NRx—C(?O)—Z2—C(?O)—NRy—; —NRx—C(?O)—Z2—NRy—C(=0)-NRy—; —C(?O)—Z2—; —C(?O)—Z2—O—; —C(=0)-NRx—Z2—; —C(=0)-NRx—Z2-0-; —C(=0)-NRx—Z2—C(=0)-0-; —C(=0)-NRx—Z2-0-C(=0)-; —C(=0)-NRx—Z2—NRy—; —C(=0)-NRx—Z2—NRy—C(=0)-; —C(=0)-NRx—Z2—NRy—C(=0)-0-; R1 represents C1-12alkyl optionally substituted with cyano, C1-4alkyloxy, C1-4alkyl-oxyC1-4alkylox
    Type: Grant
    Filed: June 6, 2008
    Date of Patent: March 17, 2015
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Jean-Pierre André 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, Gustaaf Maria Boeckx, Petr Vladimirivich Davidenko
  • Publication number: 20150065498
    Abstract: The present invention is directed to N-linked lactam compounds of general formula (I) which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor.
    Type: Application
    Filed: May 11, 2012
    Publication date: March 5, 2015
    Inventors: Scott D. Kuduk, Douglas C. Beshore, Zhi-Qiang Yang, Youheng Shu, Daniel Pitts
  • Patent number: 8962607
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: April 22, 2013
    Date of Patent: February 24, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M McDonnell, Philip M Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Patent number: 8957069
    Abstract: The present invention provides a compound represented by the following formula (I): wherein: Ring A represents an optionally substituted piperazine ring, an optionally substituted morpholine ring, or an optionally substituted bromopiperazine ring; R1 and R2 are the same or different from each other, and represent a hydrogen atom or optionally substituted lower alkyl; R3 and R4 are the same or different from each other, and represent a hydrogen atom or halogenated or non-halogenated lower alkyl; R3 to R7 are the same or different from each other, and represent a hydrogen atom, hydroxy, optionally substituted lower alkyl, optionally substituted lower alkenyl, optionally substituted lower alkoxy, optionally substituted cycloalkyl, optionally substituted aryl, an optionally substituted aromatic heterocyclic ring, optionally substituted amino, or acyl; and represents a single bond or double bond, wherein R2 and R3 do not exist when carbon atoms respectively adjacent to R2: and R3 form a double bond, and there is n
    Type: Grant
    Filed: March 9, 2010
    Date of Patent: February 17, 2015
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Tetsuya Tsukamoto, Takeshi Wakabayashi, Taiichi Ohra
  • Publication number: 20150018369
    Abstract: The disclosure provides methods of treating glioblastoma, methods of screening for compounds that treat glioblastoma, and pharmaceutical compositions useful in the treatment of glioblastoma.
    Type: Application
    Filed: January 9, 2013
    Publication date: January 15, 2015
    Inventors: Nephi Stella, Philippe Diaz
  • 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: 20140364420
    Abstract: The present invention relates to compounds useful as Chemokine Receptor antagonists. Compounds of general formula I are provided: or pharmaceutically acceptable salts thereof. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compounds and compositions for the inhibition of Chemokine Receptors and also for the treatment of various diseases, conditions, or disorders, including acute or chronic inflammatory disease, cancer or osteolytic bone disorders.
    Type: Application
    Filed: January 13, 2014
    Publication date: December 11, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
  • Patent number: 8895558
    Abstract: The present invention relates to novel arylpiperazine-containing pyrrole 3-carboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof which is useful for preventing or treating depressive disorders. The present invention also provides a method for preparing the arylpiperazine-containing pyrrole 3-carboxamide derivatives or the pharmaceutically acceptable salt thereof, a pharmaceutical composition containing same, and a method for preventing or treating depressive disorders.
    Type: Grant
    Filed: September 23, 2009
    Date of Patent: November 25, 2014
    Assignee: Green Cross Corporation
    Inventors: Jinhwa Lee, Suk Youn Kang, Eun-Jung Park, Kwang-Seop Song, Min Ju Kim, Hee Jeong Seo, Suk Ho Lee, Jeongmin Kim, Ae Nim Pae, Woo-Kyu Park
  • Publication number: 20140315889
    Abstract: The present invention relates to a novel hydroxamate derivatives, more specifically, to novel hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC), isomers thereof, pharmaceutically acceptable salts thereof, hydrates or solvates thereof, use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, treatment method using said composition, and a preparing method of novel hydroxamate derivatives. The novel selective hydroxamate derivatives having inhibitory activity against Histone Deacetylase (HDAC) compositions can be used for treatment of inflammatory disease, rheumatoid arthritis, or degenerative disease.
    Type: Application
    Filed: October 26, 2012
    Publication date: October 23, 2014
    Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.
    Inventors: Yuntae Kim, Changsik Lee, Hyun-mo Yang, Hojin Choi, Jaeki Min, Soyoung Kim, Dal-Hyun Kim, Nina Ha, Jung-Min Kim, Hyojin Lim, Eunhee Ko
  • Patent number: 8865714
    Abstract: This invention relates to a piperazine compound represented by Formula (I), wherein R1 is C1-6 alkyl; R2 is hydroxy, C1-6 alkyl that may have one or more substituents, —(C?O)—N(R3)(R4), or —(C?O)—OR5; R3 and R4 are the same or different, and each represents hydrogen or C1-6 alkyl that may have one or more substituents, or R3 and R4, taken together with a nitrogen atom to which R3 and R4 are attached, may form a saturated heterocyclic group; R5 is hydrogen or C1-6 alkyl that may have one or more substituents; and n is 1 or 2; or a salt thereof.
    Type: Grant
    Filed: March 8, 2010
    Date of Patent: October 21, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Yoshihiro Urade, Makoto Kitade, Kazuhiko Shigeno, Keiko Yamane, Katsunao Tanaka
  • Patent number: 8865702
    Abstract: Disclosed are compounds of the formula I wherein A, Y, R1, R2, R3, R4 and R5 are defined, suitable for treating diseases and symptoms of diseases caused at least to some extent by stimulation of bradykinin-B1 receptors, the preparation thereof and the use thereof.
    Type: Grant
    Filed: July 23, 2008
    Date of Patent: October 21, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Iris Kauffmann-Hefner, Angelo Ceci, Henri Doods, Norbert Hauel, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Publication number: 20140309192
    Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: that are useful in methods of treatment and alleviation of diseases and disorders of the heart, brain, kidney, immune, and reproductive system resulting from ischemia, or reperfusion subsequent to ischemia, and any downstream complication(s) related thereto. The present invention further relates to methods of treatment and alleviation of diseases and disorders of the vasculature resulting from vasoconstriction or hypertension and any downstream complication(s) resulting from elevated blood pressure and/or reduced tissue perfusion.
    Type: Application
    Filed: November 7, 2012
    Publication date: October 16, 2014
    Inventors: Thuy-Anh Tran, Anthony C. Blackburn, Bryan A. Kramer, Maiko Nagura, Carleton R. Sage, Young-Jun Shin, Ning Zou
  • 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: 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: 20140275079
    Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, and R10 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Inventors: Lisa A. Hasvold, John Pratt, Keith F. McDaniel, George S. Sheppard, Dachun Liu, Steven W. Elmore, Robert D. Hubbard
  • Publication number: 20140243305
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Application
    Filed: April 22, 2013
    Publication date: August 28, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J. Connolly, Christopher Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark M. McDonnell, Philip M. Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Patent number: 8802678
    Abstract: The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
    Type: Grant
    Filed: June 21, 2007
    Date of Patent: August 12, 2014
    Assignee: Bioprojet
    Inventors: Marc Capet, Denis Danvy, Nicolas Levoin, Isabelle Berrebi-Bertrand, Thierry Calmels, Philippe Robert, Jeanne-Marie Lecomte, Jean-Charles Schwartz, Xavier Ligneau
  • Publication number: 20140221391
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Application
    Filed: December 27, 2013
    Publication date: August 7, 2014
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Publication number: 20140206865
    Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein, with selectivity versus MMP-1. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role.
    Type: Application
    Filed: March 21, 2014
    Publication date: July 24, 2014
    Applicant: SYMPHONY EVOLUTION, INC.
    Inventors: Lynne Canne Bannen, Erick Wang Co, Vasu Jammalamadaka, John M. Nuss, Moon Hwan Kim, Donna Tra Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, Zhaoyang Wen, Wei Xu, Richard George Khoury
  • Publication number: 20140187556
    Abstract: Anti-amyloid compounds are provided along with methods of use thereof.
    Type: Application
    Filed: March 2, 2012
    Publication date: July 3, 2014
    Applicant: Treventis Corporation
    Inventors: Mark A. Reed, Arun Yadav, Scott C. Banfield, Christopher J. Barden
  • Publication number: 20140187531
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.
    Type: Application
    Filed: March 3, 2014
    Publication date: July 3, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, Steven W. Elmore, Aaron R. Kunzer, Christopher L. Lynch, William J. McClellan, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Xilu Wang, Noah P. Tu, Michael D. Wendt, Alexander R. Shoemaker, Michael J. Mitten
  • Patent number: 8722658
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: May 13, 2014
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Peter J Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Patent number: 8710060
    Abstract: To find a therapeutic and/or prophylactic agent for gastrointestinal disorders and so on, the agent having excellent activity and high safety. A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof. In the formula, A represents an optionally substituted phenylene group; B represents an optionally substituted 4- to 10-membered heterocyclic group, an optionally substituted C6-C10 aryl group, or an optionally substituted C3-C10 cycloalkyl group; R1 represents a hydrogen atom or a C1-C3 alkyl group; R2 represents a hydrogen atom or a C1-C3 alkyl group; R3 represents a C1-C6 alkyl group, a C3-C10 cycloalkyl group, a C1-C3 alkoxy C1-C3 alkyl group, or a C1-C3 hydroxyalkyl group; R4 represents a hydrogen atom, a C1-C6 alkyl group, or a halogen atom; n represents an integer of 1 to 4; and X represents methylene, —O—, —NH—, —N(C1-C3 alkyl)-, —C(?O)—, —S—, —S(O)—, —S(O2)—, or a single bond.
    Type: Grant
    Filed: March 26, 2013
    Date of Patent: April 29, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Narihiro Toda, Rieko Takano, Takeshi Shida, Takahiro Katagiri, Mitsuhiro Iwamoto, Shinji Ashida, Mami Yamazaki
  • Patent number: 8691184
    Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.
    Type: Grant
    Filed: January 24, 2012
    Date of Patent: April 8, 2014
    Assignee: The Regents of the University of Michigan
    Inventors: Shaomeng Wang, Haibin Zhou, Jianfang Chen, Angelo Aguilar, Jennifer L. Meagher, Duxin Sun, Chao-Yie Yang, Liu Liu, Longchuan Bai, Donna McEachem, Jeanne Stuckey, Xiaoqin Li
  • Patent number: 8691816
    Abstract: The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: April 8, 2014
    Assignee: N30 Pharmaceuticals, Inc.
    Inventors: Jan Wasley, Gary J. Rosenthal, Xicheng Sun, Sarah Strong, Jian Qiu
  • Patent number: 8691805
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.
    Type: Grant
    Filed: May 1, 2013
    Date of Patent: April 8, 2014
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
  • Patent number: 8679773
    Abstract: This invention pertains to methods, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.
    Type: Grant
    Filed: January 16, 2007
    Date of Patent: March 25, 2014
    Assignee: DH Technologies Development Pte. Ltd.
    Inventors: Darryl J. C. Pappin, Michael Bartlett-Jones
  • Patent number: 8680102
    Abstract: The subject of the invention is compounds of formula (I): in which R1-R10 are as defined within, the method of preparation and therapeutic application as cannabinoid CB1 receptor antagonists.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: March 25, 2014
    Assignee: Sanofi
    Inventors: Francis Barth, Daniel Bichon, Murielle Rinaldi-Carmona, Christian Congy
  • Publication number: 20140073609
    Abstract: Compositions and methods are disclosed in embodiments relating to induction of cell death such as in cancer cells. Compounds and related methods for synthesis and use thereof, including the use of compounds in therapy for the treatment of cancer and selective induction of apoptosis in cells are disclosed. Compounds are disclosed in connection with modification of procaspases such as procaspase-3. In embodiments, compositions are capable of activation of procaspase-3.
    Type: Application
    Filed: May 14, 2013
    Publication date: March 13, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Paul J. HERGENROTHER, Karson S. PUTT, Quinn P. PETERSON, Valerie FAKO
  • Publication number: 20140066426
    Abstract: The invention relates to pyrrole carboxamides bearing a fluoromethyl-moiety as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
    Type: Application
    Filed: August 29, 2013
    Publication date: March 6, 2014
    Inventors: Stefan SCHUNK, Melanie REICH, Henning STEINHAGEN, Nils DAMANN, Michael HAURAND, Achim KLESS, Philip SKONE, Richard HAMLYN, Robert KIRBY, Marc ROGERS, Kathy SUTTON
  • Patent number: 8664407
    Abstract: The present disclosure provides drug-ligand conjugates that are potent cytotoxins and include a linker between the drug and ligand where the linker has a single amino acid. The disclosure is also directed to compositions containing the drug-ligand conjugates, and to methods of treatment using them.
    Type: Grant
    Filed: February 20, 2008
    Date of Patent: March 4, 2014
    Assignee: Medarex, LLC
    Inventors: Liang Chen, Sanjeev Gangwar, Vincent Guerlavais, Nils Lonberg, Qian Zhang
  • Publication number: 20140057890
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140057889
    Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 or Bcl-xL proteins, compositions containing the compounds and methods of treating diseases during which are expressed anti-apoptotic Bcl-2 protein.
    Type: Application
    Filed: October 18, 2013
    Publication date: February 27, 2014
    Applicant: AbbVie Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa Hasvold, Laura A. Hexamer, Aaron R. Kunzer, Robert A. Mantei, William J. McClellan, Chang H. Park, Cheol-Min Park, Andrew M. Petros, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt
  • Publication number: 20140038979
    Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.
    Type: Application
    Filed: October 14, 2013
    Publication date: February 6, 2014
    Applicant: Janssen Pharmaceutica NV
    Inventors: Kristof VAN EMELEN, Janine Arts, Leo-Jacobus Jozef Backx, Hans Louis Jos De Winter, Sven Franciscus Anna Van Brandt, Marc Gustaaf Celine Verdonck, Lieven Meerpoel, Isabelle Noelle Constance Pilatte, Virginie Sophie Poncelet, Alexey Borisovich Dyatkin, Jimmy Arnold Viviene Van Heusden
  • Publication number: 20140024647
    Abstract: A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I), wherein R1a is substituted or unsubstituted alkyl or the like; R1b is hydrogen or substituted or unsubstituted alkyl; R1c is hydrogen, halogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted nonaromatic heterocyclic group or the like; -L- is —C(=0)—NR2? or the like; X is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or the like, or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 18, 2012
    Publication date: January 23, 2014
    Inventor: Akira Yukimasa
  • Patent number: 8633314
    Abstract: The present invention provides alternative forms of Compound I, processes to reproducibly make them and methods of treating patients using them.
    Type: Grant
    Filed: February 24, 2012
    Date of Patent: January 21, 2014
    Assignee: Cephalon, Inc.
    Inventors: Stephen Bierlmaier, Michael Christie, R. Scott Field, R. Curtis Haltiwanger, Linli He, Martin J. Jacobs, Michael Kress, Robert E. McKean, Dale R. Mowrey, Joseph Petraitis, Mehran Yazdanian, Veronique Courvoisier
  • Publication number: 20130345235
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. Glucuronidase inhibitors described include phenoxy thiophene sulfonamides. Other compounds, for instance pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls, are also contemplated. Also contemplated are compositions including one or more of such compounds for use inhibiting glucuronidase and methods of using one or more of such compounds as a co-drug to be used in combination with the anticancer drug CPT-11.
    Type: Application
    Filed: March 10, 2011
    Publication date: December 26, 2013
    Applicants: THE UNIVERSITY OF NORTH CAROLINA AT CHAPEL HILL, NORTH CAROLINA CENTRAL UNIVERSITY
    Inventors: Alfred L. Williams, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • Publication number: 20130345196
    Abstract: This invention relates generally to compounds that are glucuronidase inhibitors. The glucuronidase inhibitors include phenoxy thiophene sulfonamides, and other compounds such as pyridine sulfonyls, benzene sulfonyls, thiophene sulfonyls, thiazole sulfonyls, thiophene carbonyls, and thiazole carbonyls. These compounds include nialamide, isocarboxazid, phenelzine, amoxapine, loxapine and mefloquine. Also compositions including one or more of such compounds for use in inhibiting glucuronidase and methods of using one or more of such compounds for selective inhibition of bacterial ?-glucuronidase. These compounds may be used as a co-drug in combination with the anticancer drug CPT-11. Also a method for screening compounds to determine their usefulness in reducing diarrhea associated with irinotecan chemotherapy.
    Type: Application
    Filed: May 24, 2012
    Publication date: December 26, 2013
    Inventors: Alfred L. WILLIAMS, John Scott, Li-An Yeh, Matthew Robert Redinbo
  • Publication number: 20130324531
    Abstract: There are provided compounds of the formula wherein X, Y, Z, R1, R2 and R3 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
    Type: Application
    Filed: May 29, 2013
    Publication date: December 5, 2013
    Applicant: Hoffmann-La Roche Inc.
    Inventors: David Joseph Bartkovitz, Xin-Jie Chu, George Kenneth Ehrlich, Jin-Jun Liu, Hanspeter Michel, Binh Thanh Vu, Chunlin Zhao
  • Patent number: 8598162
    Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.
    Type: Grant
    Filed: October 11, 2011
    Date of Patent: December 3, 2013
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Jun Matsubara, Yohji Sakurai
  • Patent number: 8575173
    Abstract: The present invention relates to compounds of chemical formula 1 and having CCR2 (chemokine receptor 2) antagonistic effects, and salts or isomers thereof. These compounds are very useful for treating, preventing, or relieving rheumatoid arthritis, arteriosclerosis, multiple sclerosis, asthma, and various diseases related to CCR2. wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 is the same as defined in the specification.
    Type: Grant
    Filed: June 11, 2010
    Date of Patent: November 5, 2013
    Assignee: Yang Ji Chemical Co., Ltd.
    Inventors: Jee Woong Lim, Jong-Hoon Kim, Min-Ho Oak, Yongho Na, Youna Oh, So-Hee Kang, Jung-Ok Lee, Jung-Duk Sohn, Seung-Woo Lee