Bicyclo Ring System Having The Diazole Ring As One Of The Cyclos Patents (Class 548/302.7)
  • Patent number: 9000186
    Abstract: A ring-fused heterocyclic derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof having a T-type calcium channel regulatory effect and useful as a pruritus therapeutic and/or preventive agent, and the like are provided. In the general formula (I), R1 represents optionally substituted lower alkyl, and the like; R2 represents an optionally substituted cycloalkyl, and the like; Q represents a hydrogen atom, and the like; R3 represents —C(?O)NR8R9 (wherein R8 and R9 may be the same or different, and each represents a hydrogen atom, and the like), and the like; L1 represents —CR11AR11B— (wherein R11A and R11B may be the same or different, and each represents a hydrogen atom, and the like), and the like; and W1 and W2 may be the same or different, and each represents C—R12 (wherein R12 represents a hydrogen atom, and the like), and the like.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: April 7, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Takashi Sawada, Tomohiro Danjo, Keiichi Motosawa, Takayuki Furuta, Maki Ichioka, Masamori Sugawara, Noriaki Uesaka
  • Patent number: 8993778
    Abstract: A process for preparing telmisartan by reacting 2-n-propyl-4-methyl-6-(1?-methylbenzimidazol-2?-yl)benzimidazole with a compound of formula (IV) wherein Z is a leaving group, to obtain the compound 2-cyano-4?-[2?-n-propyl-4?-methyl-6?-(1??-methylbenzimidazol-2??-yl)benzimidazol-1?-ylmethyl]biphenyl, and subsequently hydrolyzing the nitrile function to obtain the acid function.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: March 31, 2015
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Norbert Hauel, Rolf Dach, Helmut Heitger, Oliver Meyer
  • Patent number: 8980920
    Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.
    Type: Grant
    Filed: May 28, 2010
    Date of Patent: March 17, 2015
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
  • Patent number: 8969345
    Abstract: A dibenzoxepin derivative represented by the following general formula (I) wherein Y is a hydrogen atom and the like, RA is a hydrogen atom and the like, X is the formula (b3) wherein RB is a hydrogen atom and the like, and the like, A is the formula (a18) wherein R1 is a hydrogen atom and the like, and RC and RD are the same or different and each is a hydrogen atom and the like, and the like, which has a PPAR? agonist activity and the like, and useful as a therapeutic agent and/or prophylaxis agent and the like for type 2 diabetes and the like, or a pharmaceutically acceptable salt thereof and the like is provided.
    Type: Grant
    Filed: August 3, 2012
    Date of Patent: March 3, 2015
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Keisuke Yamamoto, Tomohiro Tamura, Rina Nakamura, Kimihisa Ueno, Shintaro Hosoe
  • Publication number: 20150051257
    Abstract: Sulphonamide derivatives of benzylamine of formula (I), wherein A represents phenyl unsubstituted or substituted; or 9- or 10-membered bicyclic group, linked to —(O)x—(CH2)y— through one of its aromatic carbon atoms, consisting of benzene ring fused with -membered heteroaromatic ring containing 1 or 2 heteroatoms independently selected from the group consisting of N and O, wherein such bicyclic group is unsubstituted or substituted or with 5- or 6-membered non-aromatic heterocyclic ring having 1 or 2 O atoms, wherein heterocyclic ring is unsubstituted or substituted with one or more C1-C3-alkyls; D represents a group selected from: phenyl unsubstituted or substituted; naphthyl unsubstituted or substituted; thiophene unsubstituted or substituted; bicyclic group consisting of imidazolering fused with 5-membered non-aromatic carbocyclic ring; bicyclic group consisting of benzene ring fused with 5-membered heteroaromatic ring, having 1 or 2 heteroatoms independently selected from the group consisting of N, O and
    Type: Application
    Filed: March 20, 2013
    Publication date: February 19, 2015
    Applicant: ADAMED SP. ZO.O
    Inventors: Marcin Kolaczkowski, Monika Marcinkowska, Adam Bucki, Tomasz Lysakowski, Maciej Pawlowski
  • Patent number: 8957222
    Abstract: A process for preparing the S or R enantiomer of a compound of formula A, the process comprising subjecting a compound of formula B to asymmetric hydrogenation in the presence of a chiral transition metal catalyst and a source of hydrogen, wherein X is CH2, oxygen, or sulphur; R1, R2 and R3 are the same or different and signify hydrogens, halogens, alkyl, alkyloxy, hydroxy, nitro, alkylcarbonylamino, alkylamino, or dialkylamino group; and R4 is alkyl or aryl, wherein the transition metal catalyst comprises a chiral ligand having the formula wherein p is from 1 to 6, and Ar means aryl group; wherein the term alkyl means hydrocarbon chains, straight or branched, containing from one to six carbon atoms, optionally substituted by aryl, alkoxy, halogen, alkoxycarbonyl or hydroxycarbonyl groups; the term aryl means an aromatic or heteroaromatic group, optionally substituted by alkyloxy, halogen, or nitro group; and the term halogen means fluorine, chlorine, bromine, or iodine.
    Type: Grant
    Filed: March 17, 2009
    Date of Patent: February 17, 2015
    Assignee: Bial-Portela & CA, S.A.
    Inventors: Alexander Beliaev, David Alexander Learmonth, Wenge Li
  • Patent number: 8951831
    Abstract: The present invention relates to a new binaphthalene derivative, a preparation method thereof, and an organic electronic device using the same. The binaphthalene derivative according to the present invention can perform functions of hole injection and transportation, electron injection and transportation, or light emission in an organic electronic device including an organic light-emitting device, and the device according to the present invention has excellent characteristics in terms of efficiency, drive voltage and stability, and in particular excellent effects such as a low voltage and a long life time.
    Type: Grant
    Filed: February 6, 2014
    Date of Patent: February 10, 2015
    Assignee: LG Chem, Ltd.
    Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Jae Chol Lee, Jun Gi Jang
  • Patent number: 8933095
    Abstract: Compounds of Formula I: wherein X, Y, Z, R1, R2, R3, R4 are as defined herein, and pharmaceutically acceptable salts thereof, are described as useful for the treatment of cognitive deficits associated with schizophrenia and other psychiatric, neurodegenerative and/or neurological disorders in mammals, including humans.
    Type: Grant
    Filed: October 31, 2013
    Date of Patent: January 13, 2015
    Assignee: Pfizer Inc.
    Inventors: Amy Beth Dounay, Laura Ann McAllister, Vinod Dipak Parikh, Suobao Rong, Patrick Robert Verhoest
  • Patent number: 8921369
    Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.
    Type: Grant
    Filed: December 2, 2009
    Date of Patent: December 30, 2014
    Assignee: Presidio Pharmaceuticals, Inc.
    Inventors: Min Zhong, Leping Li
  • Publication number: 20140364470
    Abstract: The invention relates to a phosphate salt or a nitrate salt of 4-(R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl-3-fluoro-benzonitrile, especially in crystalline form, and specific forms of these salts, as well as related invention embodiments. The salts and salt forms allow for the prophylactic and/or therapeutic treatment of aldosterone synthase and/or aromatase mediated diseases or disorders.
    Type: Application
    Filed: January 15, 2013
    Publication date: December 11, 2014
    Applicant: Novartis AG
    Inventors: Paul Alan Sutton, Eric Loeser
  • Publication number: 20140357621
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Application
    Filed: August 14, 2014
    Publication date: December 4, 2014
    Applicant: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8883800
    Abstract: The present invention relates to substituted quinazolines of formula (I): wherein X and Y are defined as in claim 1, the tautomers, stereoisomers, mixtures and salts thereof, which have valuable pharmacological properties, particularly an inhibitory effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).
    Type: Grant
    Filed: July 13, 2012
    Date of Patent: November 11, 2014
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Waldemar Pfrengle, Markus Frank, Thomas Klein
  • Publication number: 20140329858
    Abstract: The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
    Type: Application
    Filed: December 3, 2012
    Publication date: November 6, 2014
    Inventors: Mark Gary Bock, Dinesh Chikkanna, Marc Gerspacher, Vinayak Khairnar, Bharat Lagu, Chetan Pandit
  • Patent number: 8859599
    Abstract: The present invention concerns compounds of general formula (I): Method of preparation and uses thereof.
    Type: Grant
    Filed: February 11, 2010
    Date of Patent: October 14, 2014
    Assignees: CNR—Consiglio Nazionale delle Ricerche, Istituto Scientifico Romagnolo per lo Studio e la Cura dei Tumori (I.R.S.T.) S.r.l.
    Inventors: Greta Varchi, Andrea Guerrini, Anna Tesei, Giovanni Brigliadori
  • Patent number: 8835646
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: September 16, 2014
    Assignee: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8785002
    Abstract: The present invention includes high triplet energy compositions of matter, methods of their manufacture, devices incorporating the compositions of matter, and methods of using those compositions of matter and devices. The devices incorporating the high triplet energy compositions of matter include electroluminescence devices including organic light-emitting diodes (OLEDs). The present invention also includes methods of using the compositions of matter, such as by operating the devices of the present invention incorporating them, to provide light through electroluminescence, as well as obtaining and/or operating devices of the present invention through the application of electrical energy or potential, as well as methods of providing light through electroluminescence through their operation.
    Type: Grant
    Filed: March 10, 2009
    Date of Patent: July 22, 2014
    Assignee: Bowling Green State University
    Inventors: Pavel Anzenbacher, Jr., Shin-ya Takizawa
  • Publication number: 20140171392
    Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4) alkyl, or —(C1-C4) alkyl-(C5-C7) aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4) alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10) aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: November 13, 2013
    Publication date: June 19, 2014
    Applicant: Novartis AG
    Inventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
  • Patent number: 8729096
    Abstract: The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2).
    Type: Grant
    Filed: February 12, 2013
    Date of Patent: May 20, 2014
    Assignee: Allergan, Inc.
    Inventors: Richard L. Beard, Vidyasagar Vuligonda, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8703964
    Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: April 22, 2014
    Assignee: Supratek Pharma Inc.
    Inventors: Tomasz Popek, Kishore Patel, Valery Alakhov, Grzegorz Pietrzynski
  • Patent number: 8703099
    Abstract: The present invention provides compositions and methods for synthesizing labeled drugs. The present invention further provides methods for preventing or stopping prescription drug abuse for all agents registered as a Drug Enforcement Agency (DEA) schedule II through schedule V medications. According to the present invention, methods are provided for monitoring patient compliance with prescribed drug treatment. The present invention also provides methods for facilitating a replacement prescription when a patient is left without access to their prescribed drug. Furthermore, the present invention provides a method to improve employee compliance with an employer's drug policies via either a voluntary or compulsory system for enhanced drug testing.
    Type: Grant
    Filed: February 23, 2006
    Date of Patent: April 22, 2014
    Assignee: DR Pharma Nova, LLC
    Inventors: Alan J. Reis, Christian Schafmeister
  • Patent number: 8697885
    Abstract: An object is to provide a novel carbazole compound that can be used for a transport layer, a host material, or a light-emitting material in a light-emitting element. A carbazole compound where nitrogen of a carbazole group, the carbazole skeleton of which whose 3-position is bonded to the 4-position of a dibenzofuran skeleton or a dibenzothiophene skeleton, is bonded to a benzimidazole skeleton through a phenylene group, is provided. The carbazole compound has a high carrier-transport property, and can be suitably used for a material for a light-emitting element or for an organic semiconductor material.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: April 15, 2014
    Assignee: Semiconductor Energy Laboratory Co., Ltd.
    Inventors: Sachiko Kawakami, Nobuharu Ohsawa
  • Publication number: 20140100373
    Abstract: The present invention provides an advantageous production method of an imidazole derivative, which is suitable for industrial production. Compound (VI) is produced by reacting compound (I) with a Grignard reagent or a magnesium reagent, and a lithium reagent, and then reacting the resulting compound with compound (V).
    Type: Application
    Filed: June 14, 2012
    Publication date: April 10, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Yoichi Kawabata, Yasuhiro Sawai, Kazuaki Kanno, Naotaka Sawada
  • Publication number: 20140093450
    Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has a flattened structure as a result of the position of at least two exocyclic bonds.
    Type: Application
    Filed: May 7, 2012
    Publication date: April 3, 2014
    Applicant: KONINKLIJKE PHILIPS N.V.
    Inventors: Marc Stefan Robillard, Johan Lub, Raffaella Rossin, Sandra Martina Van Ben Bosch, Ronny Mathieu Versteegen
  • Patent number: 8674138
    Abstract: The present invention relates to a new binaphthalene derivative, a preparation method thereof, and an organic electronic device using the same. The binaphthalene derivative according to the present invention can perform functions of hole injection and transportation, electron injection and transportation, or light emission in an organic electronic device including an organic light-emitting device, and the device according to the present invention has excellent characteristics in terms of efficiency, drive voltage and stability, and in particular excellent effects such as a low voltage and a long life time.
    Type: Grant
    Filed: October 20, 2006
    Date of Patent: March 18, 2014
    Assignee: LG Chem. Ltd.
    Inventors: Jae Soon Bae, Dae Woong Lee, Dong Hoon Lee, Jae Chol Lee, Jun Gi Jang
  • Publication number: 20140051730
    Abstract: Dimiracetam is a suitable drug for treating and preventing allodynia, in particular allodynia of the hands and feet, that is or may be induced by antitumoral chemotherapeutic treatment with sorafenib.
    Type: Application
    Filed: October 25, 2011
    Publication date: February 20, 2014
    Applicant: NEUROTUNE AG
    Inventors: Ruggero G. Fariello, Carlo Farina, Carla Ghelardini
  • Publication number: 20140038873
    Abstract: The present invention concerns a dynamic mixture obtained by combining, in the presence of water, at least one diamine derivative, comprising at least one heteroaryl moiety, with at least two perfuming aldehydes and/or ketones. The invention's mixture is capable of releasing in a controlled and prolonged manner said perfuming compounds, in particular perfuming ingredients, into the surrounding environment. The invention's dynamic mixture gives rise to a more evenly distributed positive effect for the release of the different carbonyl compounds which are part of the mixture than other examples reported in the prior art.
    Type: Application
    Filed: April 2, 2012
    Publication date: February 6, 2014
    Applicant: FIRMENICH SA
    Inventors: Andreas Herrmann, Christian Chapuis
  • Patent number: 8633235
    Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.
    Type: Grant
    Filed: September 24, 2004
    Date of Patent: January 21, 2014
    Assignee: Neomed Institute
    Inventors: Ziping Liu, Daniel Pagé, Christopher Walpole, Hua Yang
  • Patent number: 8623899
    Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.
    Type: Grant
    Filed: August 6, 2010
    Date of Patent: January 7, 2014
    Assignee: Janssen Research & Development Ireland
    Inventors: David McGowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
  • Patent number: 8618150
    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, R1, R2, and are defined herein.
    Type: Grant
    Filed: December 9, 2011
    Date of Patent: December 31, 2013
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, Mingde Xia, James J. McNally, Jay M. Matthews
  • Patent number: 8609862
    Abstract: The present invention relates to a method of treating a disease or disorder characterised by increased stress hormone levels and/or decreased androgen hormone levels in a subject, comprising administering to the subject a therapeutically effective amount of a compound represented by formula (I): wherein n is 1 or 3; R is hydrogen or —C(O)N(Ra)(Rb) wherein Ra and Rb are independently —(C1-C4)alkyl, or —(C1-C4)alkyl-(C5-C7)aryl, wherein each of Ra and Rb is optionally substituted by —(C1-C4)alkoxy; R1, R2, and R3, are independently hydrogen, halogen, cyano or —(C6-C10) aryl, wherein said —(C6-C10)aryl is optionally substituted by halogen, with the proviso that no more than one of R1, R2, and R3 is hydrogen; and R4 and R5 are hydrogen; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 13, 2011
    Date of Patent: December 17, 2013
    Assignee: Novartis AG
    Inventors: Qi-Ying Hu, Gary Michael Ksander, Erik Meredith, Lauren G. Monovich, Julien Papillon, Christoph Schumacher
  • Patent number: 8603947
    Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.
    Type: Grant
    Filed: July 20, 2011
    Date of Patent: December 10, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Hartmut Ahrens, Dieter Feucht, Elmar Gatzweiler, Isolde Haeuser-Hahn, Christopher Hugh Rosinger
  • Patent number: 8586762
    Abstract: The present invention provides an industrially advantageous process for producing a steroid C17,20 lyase inhibitor represented by the general formula (I):
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: November 19, 2013
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Jun-Ichi Kawakami, Shigeru Nuwa, Miki Shokyo
  • Publication number: 20130287789
    Abstract: The present invention provides a compound of formula I: Said compound is inhibitor of aldosterone synthase and aromatase, and thus can be employed for the treatment of a disorder or disease mediated by aldosterone synthase or aromatase. Accordingly, the compound of formula I can be used in treatment of hypokalemia, hypertension, congestive heart failure, atrial fibrillation, renal failure, in particular, chronic renal failure, restenosis, atherosclerosis, syndrome X, obesity, nephropathy, post-myocardial infarction, coronary heart diseases, inflammation, increased formation of collagen, fibrosis such as cardiac or myocardiac fibrosis and remodeling following hypertension and endothelial dysfunction, gynecomastia, osteoporosis, prostate cancer, endometriosis, uterine fibroids, dysfunctional uterine bleeding, endometrial hyperplasia, polycystic ovarian disease, infertility, fibrocystic breast disease, breast cancer and fibrocystic mastopathy.
    Type: Application
    Filed: June 26, 2013
    Publication date: October 31, 2013
    Applicant: Novartis AG
    Inventors: Gary Michael Ksander, Erik Meredith, Lauren Monovich, Julien Papillon, Fariborz Firooznia, Qi-Ying Hu
  • Patent number: 8546440
    Abstract: The present invention is concerned with novel substituted bicyclic imidazole derivatives of Formula (I) wherein R0, R1, R3, R4, X, A1, A2, A3, A4, Y1, Y2 and Y3 have the meaning defined in the claims. The compounds according to the present invention are useful as gamma secretase modulators. The invention further relates to processes for preparing such novel compounds, pharmaceutical compositions comprising said novel compound as an active ingredient as well as the use of said compounds as a medicament.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: October 1, 2013
    Assignee: Janssen Pharmaceuticals, Inc.
    Inventors: Henricus Jacobus Maria Gijsen, Gregor James MacDonald, François Paul Bischoff, Gary John Tresadern, Andrés Avelino Trabanco-Suárez, Sven Franciscus Anna Van Brandt, Didier Jean-Claude Berthelot
  • Patent number: 8541555
    Abstract: Conjugationally extended hydrazine compositions of the formula (RR2)N(H)n(NH2)n, fluorescent hydrazone compositions of the formula (RR2)NN?C(R1R2), methods of the formation of hydrazones from the reaction of conjugationally extended hydrazines with conjugationally extended carbonyls and methods of their use in assays systems are described. Use of these conjugationally extended hydrazine and oxime compositions for direct calorimetric and fluorometric assays wherein a chromophore or the fluorophore is incorporated into the linker that is positioned between a reactive linking moiety and a biotin molecule.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: September 24, 2013
    Assignee: Solulink Biosciences, Inc.
    Inventors: David A. Schwartz, Leopoldo Mendoza
  • Publication number: 20130231377
    Abstract: Disclosed are pactamycin analogs, pharmaceutical compositions including the analogs, and methods of using the analogs, such as to inhibit tumor growth or a pathogenic infection such as a bacterial or parasitic infection. The pactamycin analogs have a general formula where R1 is H, lower aliphatic, amide, acyl, or aminoacyl; R2 is —C(O)NR8R9 where R8 and R9 independently are hydrogen or lower aliphatic, or R1 and R2 together form a cyclic structure; R3 and R4 independently are hydrogen, hydroxyl, or lower aliphatic, or R2 and R3 together form a cyclic structure; R5 is hydrogen or acyl; R6 and R7 independently are hydrogen, hydroxyl, halogen, lower aliphatic, or amino.
    Type: Application
    Filed: August 2, 2011
    Publication date: September 5, 2013
    Applicants: Oregon State University
    Inventor: Taifo Mahmud
  • Publication number: 20130217720
    Abstract: The present invention relates to novel imidazolidine-2,4-dione derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor 2 (FPR2).
    Type: Application
    Filed: February 12, 2013
    Publication date: August 22, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Patent number: 8486980
    Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
    Type: Grant
    Filed: August 6, 2009
    Date of Patent: July 16, 2013
    Assignee: Kyowa Hakko Kirin Co., Ltd.
    Inventors: Arata Yanagisawa, Keiji Uehara, Masahiro Matsubara, Kimihisa Ueno, Michihiko Suzuki, Takeshi Kuboyama, Keisuke Yamamoto, Tomohiro Tamura
  • Patent number: 8476453
    Abstract: The invention relates to a method of manufacture of dimiracetam (2,5-dioxohexahydro-1 H-pyrrolo[1,2-a]imidazole), characterized in that a 4-oxo-butanoic acid ester is condensed with glycinamide in a one-pot reaction with a controlled pH. The reaction may be performed in aqueous solution or in an anhydrous lower alcohol solution.
    Type: Grant
    Filed: July 25, 2011
    Date of Patent: July 2, 2013
    Assignee: Neurotune AG
    Inventors: Carlo Farina, Jacopo Roletto, Stefano Gobbato
  • Publication number: 20130123509
    Abstract: The invention relates to a method of manufacture of dimiracetam (2,5-dioxohexahydro-1 H-pyrrolo[1,2-a]imidazole), characterized in that a 4-oxo-butanoic acid ester is condensed with glycinamide in a one-pot reaction with a controlled pH. The reaction may be performed in aqueous solution or in an anhydrous lower alcohol solution.
    Type: Application
    Filed: July 25, 2011
    Publication date: May 16, 2013
    Applicant: NEUROTUNE AG
    Inventors: Carlo Farina, Jacopo Roletto, Stefano Gobbato
  • Publication number: 20130112946
    Abstract: A heterocyclic compound represented by Formula 1 below and an organic light-emitting device including the heterocyclic compound: wherein X1 and X2, X1 and R1 to R10 are defined as in the specification.
    Type: Application
    Filed: February 29, 2012
    Publication date: May 9, 2013
    Applicant: SAMSUNG MOBILE DISPLAY CO., LTD.
    Inventors: Bum-Woo Park, Yoon-Hyun Kwak, Sun-Young Lee, Chang-Ho Lee, Se-Jin Cho
  • Patent number: 8436032
    Abstract: The present invention is directed to pharmaceutical compositions comprising: (a) bendamustine, (b) a charged cyclopolysaccharide, and (c) a stabilizing agent having a charge opposite to that of the cyclopolysaccharide. Such composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. Such compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: May 7, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Tomasz Popek, Kishore Patel, Valery Alakhov, Grzegorz Pietrzynski
  • Patent number: 8431608
    Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
    Type: Grant
    Filed: February 16, 2010
    Date of Patent: April 30, 2013
    Assignee: Icagen Inc.
    Inventors: Thomas Eugene Christos, George S. Amato, Robert N. Atkinson, Maria Graciela Barolli, Lilli Ann Wolf-Gouveia, Mark J. Suto
  • Patent number: 8399444
    Abstract: The present invention relates to compounds of formula (I): or pharmaceutically acceptable salts or solvates thereof, processes for their preparation, pharmaceutical compositions containing these compounds, and their use in the treatment of allergic disorders, such as allergic rhinitis and asthma.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: March 19, 2013
    Assignee: GlaxoSmithKline Intellectual Property Development Ltd.
    Inventors: Ian Baxter Campbell, Simon Peace, John Martin Pritchard, Daniel Tape, Robert Charles Wheeler
  • Publication number: 20130065893
    Abstract: The present invention provides a compound of formula (I) or pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, R5, R7 and p are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Application
    Filed: November 29, 2010
    Publication date: March 14, 2013
    Applicant: NOVARTIS AG
    Inventors: Robert Sun, Lauren G. Monovich, Sylvie Chamoin, John Westbrook
  • Patent number: 8389558
    Abstract: The present invention is directed to pharmaceutical compositions comprising bendamustine and one or more amphiphilic anionic compounds and self assembled aggregates, which aggregates exhibit enhanced stability in aqueous solutions, including plasma, are disclosed. The unexpectedly enhanced stability afforded by such aggregates permits patients to be treated with bendamustine in lower and/or with less frequent dosages or to improve its therapeutic effect while using the same as presently used treatment protocol.
    Type: Grant
    Filed: July 19, 2010
    Date of Patent: March 5, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegroz Pietrzynski, Patel Kishore, Thomasz Popek
  • Patent number: 8383663
    Abstract: The present invention is directed to pharmaceutical compositions including: (a) bendamustine, (b) a first charged cyclopolysaccharide, and (c) a stabilizing agent which is a second charged cyclopolysaccharide having a charge opposite to that of the first charged cyclopolysaccharide. The composition provides unexpectedly desirable stability in reactive environments such as plasma, coupled with unexpectedly desirable anticancer activity. The compositions are suitable for injection or infusion into patients in need for treatment with bendamustine.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: February 26, 2013
    Assignee: Supratek Pharma Inc.
    Inventors: Valery Alakhov, Grzegorz Pietrzynski, Patel Kishore, Thomasz Popek
  • Patent number: 8354434
    Abstract: The invention relates to cyclourea compounds of Formula I: or a pharmaceutically acceptable salt or solvate thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use of 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: January 15, 2007
    Date of Patent: January 15, 2013
    Assignee: Purdue Pharma L.P.
    Inventor: Xiaoming Zhou
  • Patent number: RE44338
    Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 2, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky
  • Patent number: RE44354
    Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form-amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.
    Type: Grant
    Filed: July 17, 2012
    Date of Patent: July 9, 2013
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Hank F. Kung, Mei-Ping Kung, Zhi-Ping Zhuang, Virginia M. Y. Lee, John Q. Trojanowski, Daniel M. Skovronsky