Polycyclo Ring System Having The Additional Five-membered Nitrogen Hetero Ring As One Of The Cyclos Patents (Class 514/254.08)
  • Patent number: 9693993
    Abstract: The subject invention describes a method of use of Rotigotine™ to alleviate and control menopausal symptoms in women, and in particular, hot flashes. The invention describes the use of Rotigotine as a dopamine agonist with affinity for the dopamine D2, D3, or D4 receptors. The use of Rotigotine provides a useful new method for treatment of menopausal symptoms that are most disruptive to the functioning in activities of daily living.
    Type: Grant
    Filed: December 17, 2013
    Date of Patent: July 4, 2017
    Inventor: Robert L. Knobler
  • Patent number: 9533002
    Abstract: The invention provides methods of treatment of metabolic syndrome with HSP90 inhibitors, particularly HSP90? inhibitors. The invention provides methods of diagnosis and monitoring of metabolic syndrome using HSP90, particularly HSP90?, expression and activity level.
    Type: Grant
    Filed: May 24, 2013
    Date of Patent: January 3, 2017
    Assignee: Berg LLC
    Inventors: Niven Rajin Narain, Rangaprasad Sarangarajan, Vivek K. Vishnudas, Enxuan Jing
  • Publication number: 20150105375
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
  • Patent number: 8975286
    Abstract: The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
    Type: Grant
    Filed: August 16, 2010
    Date of Patent: March 10, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Vadim Y. Dudkin, Mark E. Fraley, Cheng Wang, Robert M. Garbaccio, Douglas C. Beshore, Scott K. Kuduk, Jason W. Skudlarek
  • 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
  • Publication number: 20150045362
    Abstract: The invention provides compounds of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxygen, nitrogen and sulphur. The compounds have activity as Hsp90 inhibitors.
    Type: Application
    Filed: August 25, 2014
    Publication date: February 12, 2015
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueroa Navarro, Alison Jo-Anne Woolford
  • Publication number: 20150031697
    Abstract: Provided herein are methods of preventing skin cancer, where the methods comprise the step of administering an effective amount of at least one Hsp90 inhibitor to a subject at the risk of developing skin cancer, whereby the skin cancer is prevented in the subject.
    Type: Application
    Filed: July 25, 2014
    Publication date: January 29, 2015
    Inventor: Ajit K. Verma
  • 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
  • Patent number: 8916552
    Abstract: The invention provides combinations comprising (or consisting essentially of) one or more ancillary compound(s) and a compound of the formula (I): or salts, tautomers, solvates and N-oxides thereof; wherein R1 is hydroxy or hydrogen; R2 is hydroxy; methoxy or hydrogen; provided that at least one of R1 and R2 is hydroxy; R3 is selected from hydrogen; halogen; cyano; optionally substituted C1-5 hydrocarbyl and optionally substituted C1-5 hydrocarbyloxy; R4 is selected from hydrogen; a group —(O)n—R7 where n is 0 or 1 and R7 is an optionally substituted acyclic C1-5 hydrocarbyl group or a monocyclic carbocyclic or heterocyclic group having 3 to 7 ring members; halogen; cyano; hydroxy; amino; and optionally substituted mono- or di-C1-5 hydrocarbyl-amino; or R3 and R4 together form a monocyclic carbocyclic or heterocyclic ring of 5 to 7 ring members; and NR5R6 forms an optionally substituted bicyclic heterocyclic group having 8 to 12 ring members of which up to 5 ring members are heteroatoms selected from oxyg
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: December 23, 2014
    Assignee: Astex Therapeutics Limited
    Inventors: Neil James Gallagher, John Francis Lyons, Neil Thomas Thompson, Stephen Murray Yule, Christopher William Murray
  • Patent number: 8901117
    Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).
    Type: Grant
    Filed: December 23, 2011
    Date of Patent: December 2, 2014
    Assignee: The Regents of The University of Michigan
    Inventors: Shaomeng Wang, Ke Ding, Yipin Lu, Zaneta Nikolovska-Coleska, Su Qiu, Guoping Wang, Dongguang Qin, Sanjeev Kumar
  • Publication number: 20140349986
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula I and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Application
    Filed: July 24, 2014
    Publication date: November 27, 2014
    Applicant: SANOFI
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Patent number: 8877927
    Abstract: The present invention relates to compounds of formula (I), and pharmaceutically acceptable salts thereof, A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof (I), wherein: one of R1 and R2 is H, and the other is selected from F and Cl, or R1 and R2 are both F; R3 is selected from cyclopentyl and cyclohexyl; R4 is an optionally substituted 5- or 6-membered monocyclic or an 8- to 10-membered bicyclic aryl or heteroaryl ring which includes up to four heteroatoms. The invention further relates to pharmaceutical compositions comprising compounds of formula (I), and the use of such compounds in the treatment of a disease selected from osteoporosis, Paget's disease, Chagas's disease, malaria, gingival diseases, hypercalaemia, metabolic bone disease, diseases involving matrix or cartilage degradation, and bone cancer disorders such as bone metastases and associated pain.
    Type: Grant
    Filed: January 8, 2009
    Date of Patent: November 4, 2014
    Assignee: Grunenthal GmbH
    Inventors: Martin Quibell, John Paul Watts
  • 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
  • Publication number: 20140275025
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid(benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
  • Publication number: 20140275114
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 18, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Ralf ANDERSKEWITZ, Marc GRUNDL, Gerd MORSCHHAEUSER, Thorsten OOST, Alexander PAUTSCH
  • Patent number: 8822449
    Abstract: The invention relates to substituted aminoindanes and analogs thereof of formula (I) and the pharmaceutical use thereof. Medicaments which comprise compounds of this type are suitable for the prevention or treatment of diverse disorders such as, for example, of respiratory disorders, cystic fibrosis disorders, acute or chronic renal disorders or bowel disorders.
    Type: Grant
    Filed: August 25, 2009
    Date of Patent: September 2, 2014
    Assignee: Sanofi
    Inventors: Nils Rackelmann, Laurent Bialy, Heinrich Englert, Klaus Wirth, Petra Arndt, John Weston, Uwe Heinelt, Markus Follmann
  • Publication number: 20140221394
    Abstract: The invention provides an acid addition salt of a compound of the formula (1). Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
    Type: Application
    Filed: January 7, 2014
    Publication date: August 7, 2014
    Applicant: Astex Therapeutic Ltd.
    Inventors: Martyn Frederickson, John Francis Lyons, Neil Thomas Thompson, Mladen Vinkovic, Brian John Williams, Andrew James Woodhead, Alison Jo-Anne Woolford
  • Patent number: 8772285
    Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: July 8, 2014
    Assignee: High Point Pharmaceuticals, LLC
    Inventors: Florencio Zaragoza Dorwald, Inge Thoger Christensen
  • Publication number: 20140187537
    Abstract: This disclosure relates to diagnostic and therapeutic methods and systems related thereto. In certain embodiments, the disclosure contemplates methods of improving chemotherapy treatments by administering chemotherapy agents, analyzing CHFR gene expression, methylation, or both, and determining an appropriate therapeutic strategy. Analysis of data herein revealed that reduced CHFR expression levels was a predictor of improved overall survival of subject with non-small cell lung cancer.
    Type: Application
    Filed: January 2, 2014
    Publication date: July 3, 2014
    Applicant: EMORY UNIVERSITY
    Inventor: Johann C. Brandes
  • 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: 8748426
    Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of the compounds or their pharmaceutical compositions, to a mammal in need thereof.
    Type: Grant
    Filed: December 30, 2010
    Date of Patent: June 10, 2014
    Assignee: Piramal Enterprises Limited
    Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
  • Publication number: 20140094471
    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: Application
    Filed: September 26, 2013
    Publication date: April 3, 2014
    Applicants: AbbVie Inc., The Walter and Eliza Hall Institute of Medical Research, Genentech, Inc.
    Inventors: Milan Bruncko, Hong Ding, George A. Doherty, Steven W. Elmore, Lisa A. Hasvold, Laura Hexamer, Aaron R. Kunzer, Xiaohong Song, Andrew J. Souers, Gerard M. Sullivan, Zhi-Fu Tao, Gary T. Wang, Le Wang, Xilu Wang, Michael D. Wendt, Robert A. Mantei, Todd M. Hansen
  • Patent number: 8685982
    Abstract: A compound of Formula I, including pharmaceutically acceptable salts thereof: wherein A is selected from the group of:
    Type: Grant
    Filed: April 11, 2012
    Date of Patent: April 1, 2014
    Assignee: Bristol-Myers Squibb Company
    Inventors: Nicholas A. Meanwell, Tao Wang, Zhongxing Zhang, Lawrence G. Hamann, John F. Kadow
  • 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
  • Patent number: 8664218
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.
    Type: Grant
    Filed: January 30, 2013
    Date of Patent: March 4, 2014
    Assignee: Astex Therapeutics Ltd.
    Inventors: Brian John Williams, Martyn Frederickson
  • Publication number: 20140057924
    Abstract: Inhibitors of IAP proteins and compositions containing the same are disclosed. Methods of using the IAP protein inhibitors in the treatment of diseases and conditions wherein inhibition of IAP proteins provides a benefit, like cancers, also are disclosed.
    Type: Application
    Filed: August 16, 2013
    Publication date: February 27, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Rong Sheng, Haiying Sun, Liu Liu, Jianfeng Lu, Donna McEachern
  • Patent number: 8653084
    Abstract: The invention provides an acid addition salt of a compound of the formula (1) Also provided by the invention are processes for preparing the compound of formula (1) and alkyl analogues thereof, novel intermediates for use in the process and methods for preparing the intermediates. The invention also provides new medical uses of compounds of the formula (1) and its ethyl analogue.
    Type: Grant
    Filed: October 12, 2007
    Date of Patent: February 18, 2014
    Assignee: Astex Therapeutics Ltd.
    Inventors: Martyn Frederickson, Mladen Vinkovic, Andrew James Woodhead, Alison Jo-Anne Woolford, Marian Williams
  • Publication number: 20130338117
    Abstract: This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided.
    Type: Application
    Filed: August 27, 2013
    Publication date: December 19, 2013
    Applicant: The Trustees of the University of Pennsylvania
    Inventor: Robert P. RICCIARDI
  • Publication number: 20130331396
    Abstract: Certain piperazinyl and piperidinyl urea compounds are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).
    Type: Application
    Filed: August 13, 2013
    Publication date: December 12, 2013
    Applicant: Janssen Pharmaceutica NV
    Inventors: Richard Apodaca, J. Guy Breitenbucher, Kanaka Pattabiraman, mark Seierstad, Wei Xiao
  • Publication number: 20130267511
    Abstract: The present invention relates to inhibitors of HCV replication of formula (I), the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein R1; R3; and R4 have the meaning defined in the claims. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use in HCV therapy.
    Type: Application
    Filed: June 3, 2013
    Publication date: October 10, 2013
    Inventors: Pierre Jean-Marie Bernard Raboisson, Lili Hu, Sandrine Vendeville, Origene Nyanguile
  • Publication number: 20130259830
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed.
    Type: Application
    Filed: June 24, 2011
    Publication date: October 3, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Timothy Barden, Colleen Hudson, James Jia, Charles Kim, Regina Graul, Ara Mermerian, Joel Moore, Kevin Sprott, Yueh-tyng Chien
  • Publication number: 20130252969
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected from C1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R9 is selected from the following: wherein: R4 is selected from C1-8-alkyl and C3-8-cycloalkyl; G is selected from: CH, CMe and N; E is selected from: O, S, SO2, NH, NMe and N-oxide (N?O); J and R are independently selected from: CH, N and N-oxide (N?O); and R41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-1-yl, 4-(2-methoxyethyl)piperazin-1-yl, 1-morpholinoethyl, 1-(dimethylamino)ethyl, 1-(methylamino)ethyl, 4-fluoro-1-methylpyrrolidin-2-yl, 4,4-difluoropiperidin-
    Type: Application
    Filed: May 23, 2013
    Publication date: September 26, 2013
    Applicant: Amura Therapeutics Limited
    Inventors: Martin Quibell, John P. Watts
  • Patent number: 8518936
    Abstract: Monohydrochloride acid addition salts of a polyacidic basic compound, or a water adduct having basic site(s) stronger than pyridine. These monohydrochlorides can be produced by reacting a polyacidic basic compound with an acid salt of pyridine.
    Type: Grant
    Filed: April 16, 2010
    Date of Patent: August 27, 2013
    Assignee: Kowa Co., Ltd.
    Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takayuki Matsuda
  • Publication number: 20130210820
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof.
    Type: Application
    Filed: January 30, 2013
    Publication date: August 15, 2013
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventor: ASTEX THERAPEUTICS LIMITED
  • Patent number: 8501744
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, hydrate, complex or pro-drug thereof, wherein one of R1 and R2 is H, and the other is selected from C1-8-alkyl, C3-6-cycloalkyl and C1-8-alkyl-C5-10-aryl; R3 is selected from tert-butylmethyl, iso-propylmethyl, sec-butyl, tert-butyl, cyclopentyl, cyclohexyl and 1-methylcyclopentyl; R9 is selected from the following: wherein: R4 is selected from C1-8-alkyl and C3-8-cycloalkyl; G is selected from: CH, CMe and N; E is selected from: O, S, SO2, NH, NMe and N-oxide (N?O); J and R are independently selected from: CH, N and N-oxide (N?O); and R41 is selected from amino, methylamino, dimethylamino, isopropylamino, isopropyl(methyl)amino, cyclopropylamino, cyclopropyl(methyl)amino, cyclopentylamino, morpholino, piperidin-1-yl, piperidin-1-ylmethyl, morpholinomethyl, 4-methylpiperazin-1-yl, 4-(2-methoxyethyl)piperazin-1-yl, 1-morpholinoethyl, 1-(dimethylamino)ethyl, 1-(methylamino)ethyl, 4-fluoro-1-methylpyrrolidin-2-yl, 4,4-difluoropiperidin-1
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: August 6, 2013
    Assignee: Amura Therapeutics, Limited
    Inventors: Martin Quibell, John Paul Watts
  • Publication number: 20130143893
    Abstract: The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
    Type: Application
    Filed: January 30, 2013
    Publication date: June 6, 2013
    Applicant: MERCK SERONO SA
    Inventors: Sharad Magar, Andreas Goutopoulos, Yihua Liao, Matthias Schwarz, Russell J. Thomas
  • Publication number: 20130143877
    Abstract: A composition which comprises substance represented by Formula (I), [Meanings of the symbols that are included in the formula are given in the specification as definitions] a pharmaceutically acceptable carrier, and a dissolution aid. is useful for improving solubility, oral absorbability and/or absorbability in blood of a poorly water-soluble or water insoluble tetracyclic compounds having an ALK inhibitory activity that are useful as a prophylactic and/or therapeutic agent for cancer, depression, and cognitive function disorder.
    Type: Application
    Filed: August 19, 2011
    Publication date: June 6, 2013
    Inventors: Kentaro Furumoto, Koji Shiraki, Tomoaki Hirayama
  • Patent number: 8431563
    Abstract: The present invention relates to compounds of Formula I, or pharmaceutically acceptable salts thereof, that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: April 30, 2013
    Assignee: Amgen Inc.
    Inventors: Kate Ashton, Michael David Bartberger, Yunxin Bo, Marian C. Bryan, Michael Croghan, Christopher Harold Fotsch, Clarence Henderson Hale, Roxanne Kay Kunz, Longbin Liu, Nobuko Nishimura, Mark H. Norman, Lewis Dale Pennington, Steve Fong Poon, Markian Myroslaw Stec, David Joseph St. Jean, Jr., Nuria A. Tamayo, Christopher Michael Tegley, Kevin Chao Yang
  • Patent number: 8415347
    Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: April 9, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: José Maria Cid-Núñez, Antonius Adrianus Hendrikus Petrus Megens, Andrés Avelino Trabanco-Suárez, Mohamed Koukni, Georges Joseph Cornelius Hoornaert, Frans Josef Cornelius Compernolle, Tomasz Kozlecki, Hua Mao, Sushil Chandra Jha, Francisco Javier Fernández-Gadea
  • Patent number: 8410110
    Abstract: Piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R0, R1, R2, R3, k, l, m, n, and X are defined herein:
    Type: Grant
    Filed: September 6, 2011
    Date of Patent: April 2, 2013
    Assignee: Merck Serono SA
    Inventors: Serge Halazy, Dennis Church, Bruno Antonsson, Agnes Bombrun, Patrick Gerber, Jean-Claude Martinou
  • Publication number: 20130072497
    Abstract: Novel N-alkyl substituted piperazines have been discovered, which are useful as insecticides or fungicides. Such compounds are of Formula (I) wherein X, Y, R1 and R2 are as defined herein.
    Type: Application
    Filed: November 14, 2012
    Publication date: March 21, 2013
    Applicant: Dow AgroSciences LLC
    Inventor: Dow AgroSciences LLC
  • Patent number: 8383619
    Abstract: The invention provides a compound of the formula (1): or a salt, solvate, N-oxide or tautomer thereof; wherein either R1 is R1a and R2 is R2a; or R1 is R1b and R2 is R2b; provided that in each case at least one of R1 and R2 is other than hydrogen; R1a and R2a are the same or different and each is selected from hydrogen, C1-4 alkyl, C2-4 alkenyl and C2-4 alkynyl wherein the C1-4 alkyl is optionally substituted by C1-2 alkoxy; R1b and R2b are the same or different and are selected from hydrogen, C(O)NR4R5, C(O)R6 and C(O)OR6 where R6 is C1-4 alkyl, R4 and R5 are both C1-4 alkyl, or NR4R5 forms a 4 to 7 membered saturated heterocyclic ring optionally containing a second heteroatom ring member selected from O, N or S and oxidized forms of N and S, the heterocyclic ring being optionally substituted by one or two C1-4 alkyl groups and/or one or two oxo groups; and R3 is a group D: wherein the asterisk denotes the point of attachment to the isoindoline ring; but excluding acetic acid 5-acetoxy-4-isopro
    Type: Grant
    Filed: October 12, 2010
    Date of Patent: February 26, 2013
    Assignee: Astex Therapeutics Limited
    Inventors: Martyn Frederickson, Marian Williams
  • Publication number: 20130029970
    Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.
    Type: Application
    Filed: July 9, 2010
    Publication date: January 31, 2013
    Applicant: IRONWOOD PHARMACEUTICALS, INC
    Inventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
  • Patent number: 8354412
    Abstract: The present invention relates to new compounds, ligands of the beta-3 adrenergic receptor, their preparation and their use in therapy or as research tools for said receptor; the invention also relates to a process for the preparation of the compounds of the invention and the use of inverse agonists of the beta-3 adrenergic receptor as medicaments.
    Type: Grant
    Filed: August 3, 2011
    Date of Patent: January 15, 2013
    Assignee: Universita' Degli Studi di Bari
    Inventors: Antonio Scilimati, Maria Grazia Perrone, Ernesto Santandrea
  • Patent number: 8324194
    Abstract: The present invention provides methods of treating cancer comprising treating a patient in need thereof with hormone therapy and administering to the patient a therapeutically effective amount of at least one metalloprotease inhibitor. The present invention also provides pharmaceutical compositions comprising a therapeutically effective amount of at least one hormone therapy agent, at least one metalloprotease inhibitor, and a pharmaceutically acceptable carrier.
    Type: Grant
    Filed: November 21, 2006
    Date of Patent: December 4, 2012
    Assignee: Incyte Corporation
    Inventor: Jordan S. Fridman
  • Publication number: 20120283240
    Abstract: Compounds useful as antibacterial agents are provided. The compounds are analogs of indole-3-carbinol and have a backbone selected from dihydroindolo[2,3-b]carbazole, 2,2?-diindolylmethane, 2?,3-diindolylmethane, and 3,3?-diindolylmethane. The compounds are useful therapeutic and prophylactic treatment of bacterial infections in mammals. Methods of synthesis of the compounds are provided, as are pharmaceutical compositions containing the compounds.
    Type: Application
    Filed: June 26, 2012
    Publication date: November 8, 2012
    Inventors: Ling Jong, Faming Jiang, Gaoquan Li, Kristien Mortelmans
  • Publication number: 20120277238
    Abstract: The present invention provides a compound which indicates a histamine H4 receptor modulating activity. A compound represented by a formula (I): wherein A ring is a ring represented by the following formula: wherein R1 is substituted or unsubstituted alkyl, etc., W is —O—, etc., n is an integer of 0 to 6; X is —N(R7)— or —O—; R7 is hydrogen, substituted or unsubstituted alkyl, etc.; Y is —C(R8)? or —N?; R8 is hydrogen, substituted or unsubstituted alkyl, etc.; Z is ?O, ?S, etc.; B ring is a ring represented by the following formula: wherein R10 is each independently substituted or unsubstituted alkyl, halogen, hydroxy, substituted or unsubstituted alkyloxy, substituted or unsubstituted amino; R11, R12a and R12b are each independently hydrogen or substituted or unsubstituted alkyl, etc.; p is an integer of 0 to 4, or its pharmaceutically acceptable salt, or a solvate thereof.
    Type: Application
    Filed: July 29, 2010
    Publication date: November 1, 2012
    Applicant: Shionogi & Co., Ltd
    Inventors: Yuuki Tachibana, Masayoshi Miyagawa, Tsutomu Masuda, Tsuyoshi Hasegawa
  • Publication number: 20120251545
    Abstract: The invention provides a combination comprising an Hsp90 inhibitor compound of the formula (VII): or tautomer or salt thereof and one or more therapeutic agents selected from topoisomerase I inhibitors; antimetabolites; tubulin targeting agents; DNA binder and topoisomerase II inhibitors; alkylating agents; monoclonal antibodies; anti-hormones; signal transduction inhibitors; proteasome inhibitors; DNA methyl transferases; cytokines; retinoids and HDAC or HAT modulators.
    Type: Application
    Filed: October 12, 2011
    Publication date: October 4, 2012
    Inventors: Gianni Chessari, Miles Stuart Congreve, Martyn Frederickson, Christopher William Murray, Eva Figueron Navarro, Alison Jo-Anne Woolford
  • Publication number: 20120252740
    Abstract: Histone deacetylases inhibitors (HDACIs) and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC provides a benefit, like a cancer, a neurodegenerative disorder, a neurological disease, traumatic brain injury, stroke, malaria, an autoimmune disease, autism, and inflammation, also are disclosed.
    Type: Application
    Filed: July 2, 2010
    Publication date: October 4, 2012
    Inventors: Alan Kozikowski, Kyle V. Butler, Jay H. Kalin
  • Publication number: 20120245142
    Abstract: There are provided substituted 3-oxo-2,3-dihydro-1H-isoindole-4-carboxamide derivatives (I) which selectively inhibit the activity of poly (ADP-ribose) polymerase PARP-1 with respect to poly (ADP-ribose) polymerase PARP-2. The compounds of this invention are therefore useful in treating diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating, diseases utilizing pharmaceutical compositions comprising these compounds.
    Type: Application
    Filed: July 6, 2010
    Publication date: September 27, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Gianluca Mariano Enrico Papeo, Alina Anatolievna Busel, Alexander Khvat, Mikhail Yurievitch Krasavin, Barbara Forte, Fabio Zuccotto