Quinoline Or Isoquinoline (including Hydrogenated) Patents (Class 544/363)
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Publication number: 20150011551Abstract: Described herein are compounds that modulate the activity of TNAP. In some embodiments, the compounds described herein inhibit TNAP. In certain embodiments, the compounds described herein are useful in the treatment of conditions associated with hyper-mineralization.Type: ApplicationFiled: February 21, 2013Publication date: January 8, 2015Applicant: Sanford- Burnham Medical Reseach InstituteInventors: Anthony B. Pinkerton, Russell Dahl, Nicholas D.P. Cosford, Jose Luis Millan
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Publication number: 20150011562Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R10 and X have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: ApplicationFiled: January 9, 2013Publication date: January 8, 2015Inventors: Henry Yu, Thomas E. Richardson, Pandi Bharathi, Brian H. Heasley, Matthew G. Jenks, Robert J. Foglesong
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Patent number: 8927546Abstract: The invention includes a compound of formula I: wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of PDE4 function and are useful for improving cognitive function and/or treating cognitive disorders or impairment, traumatic and/or ischemic injuries of the central and peripheral nervous system and/or psychiatric disorders in animals, especially humans.Type: GrantFiled: September 22, 2010Date of Patent: January 6, 2015Assignee: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Michael I. Weinhouse, Mark E. Wilson, Andrew K. Lindstrom, William C. Ripka, Mi Chen
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Publication number: 20150005287Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: ApplicationFiled: February 28, 2014Publication date: January 1, 2015Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Publication number: 20150004597Abstract: Chemical compounds having a high selectivity for double stranded DNA over RNA and single stranded DNA are disclosed. The chemical compounds are stains that become fluorescent upon illumination and interaction with double stranded DNA, but exhibit reduced or no fluorescence in the absence of double stranded DNA. The compounds can be used in a variety of biological applications to qualitatively or quantitatively assay DNA, even in the presence of RNA.Type: ApplicationFiled: September 17, 2014Publication date: January 1, 2015Inventors: Jolene BRADFORD, Ching-Ying CHEUNG, Shih-Jung HUANG, Patrick PINSON, Stephen YUE
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Publication number: 20150000691Abstract: The invention relates to the use of specific heterocyclic couplers which are 7-amino-1,2,3,4-tetrahydroquinoline derivatives of formula (I) for dyeing keratin fibres such as the hair in which formula (I): R1 to R6, Ra to Rc and X are as defined in the description.Type: ApplicationFiled: December 17, 2012Publication date: January 1, 2015Inventor: Aziz Fadli
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Publication number: 20140371204Abstract: The invention relates to compounds of Formula (I) wherein ring A, X, (R1)n, R2, R3, R4, R4?, R5, n, and p are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.Type: ApplicationFiled: February 1, 2013Publication date: December 18, 2014Inventors: Eva Caroff, Marcel Keller, Thierry Kimmerlin, Emmanuel Meyer
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Publication number: 20140364431Abstract: The present invention relates to a series of quinoline and cinnoline derivatives of general formula I, pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof. And the compounds of general formula I show potent inhibitory activity gainst c-Met kinase. The present invention further relates to the uses of the compounds, pharmaceutically acceptable salts and hydrates for the preparation of medicaments for the treatment and/or prevention of diseases caused by abnormal expression of c-Met kinase, especially for treatment and/or prevention of cancer.Type: ApplicationFiled: December 7, 2012Publication date: December 11, 2014Inventors: Ping Gong, Yanfang Zhao, Yajing Liu, Xin Zhai, Sai Li, Wufu Zhu, Mingze Qin
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Publication number: 20140364420Abstract: 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: ApplicationFiled: January 13, 2014Publication date: December 11, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Kenneth G. Carson, Shomir Ghosh, Prakash Raman, Francois Soucy, Qing Ye
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Publication number: 20140352713Abstract: The invention relates to the use of specific heterocyclic couplers which are cationic 7-amino-1,2,3,4-tetrahydroquinoline derivatives of formula (I) for dyeing keratin fibres such as the hair: in which formula (I): R1 to R6, CAT+, An?, and Ra to Rb are as defined in the description.Type: ApplicationFiled: December 17, 2012Publication date: December 4, 2014Inventor: Aziz Fadli
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Patent number: 8901303Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.Type: GrantFiled: June 29, 2011Date of Patent: December 2, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
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Patent number: 8901130Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous Aripiprazole crystals is stored for an extended period.Type: GrantFiled: May 21, 2012Date of Patent: December 2, 2014Assignee: Ostuka Pharmaceutical Co., Ltd.Inventors: Takuji Bando, Satoshi Aoki, Junichi Kawasaki, Makoto Ishigami, Youichi Taniguchi, Tsuyoshi Yabuuchi, Kiyoshi Fujimoto, Yoshihiro Nishioka, Noriyuki Kobayashi, Tsutomu Fujimura, Masanori Takahashi, Kaoru Abe, Tomonori Nakagawa, Koichi Shinhama, Naoto Utsumi, Michiaki Tominaga, Yoshihiro Ooi, Shohei Yamada, Kenji Tomikawa
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Publication number: 20140350254Abstract: Lactam compounds of Formula I and their use for the treatment of neurological and psychiatric disorders including schizophrenia, bipolar disorder, anxiety disorder and insomnia is disclosed.Type: ApplicationFiled: June 5, 2014Publication date: November 27, 2014Inventors: Julius F. Remenar, Laura Cook Blumberg, Tarek A. Zeidan
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Publication number: 20140350014Abstract: The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.Type: ApplicationFiled: December 12, 2012Publication date: November 27, 2014Applicant: NOVARTIS AGInventors: Daniel Ford, John Robert Porter, Michael Scott Visser, Naeem Yusuff
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Patent number: 8895558Abstract: 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: GrantFiled: September 23, 2009Date of Patent: November 25, 2014Assignee: Green Cross CorporationInventors: 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
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Publication number: 20140343277Abstract: The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by General Formula (1) or a salt thereof, wherein R1, R2, R3, and R4 are each independently hydrogen, lower alkyl, cyclo lower alkyl or lower alkoxy lower alkyl; R2 and R3 may be linked to form lower alkylene; A1 is lower alkylene optionally substituted with one or more substituents selected from the group consisting of hydroxyl and oxo; Y1 and Y2 are each independently —N? or —CH?; and R5 is group represented by wherein R6 and R7 are each independently hydrogen or organic group; R6 and R7 may be linked to form a ring together with the neighboring group —XA—N—XB—; XA and XB are each independently a bond, lower alkylene, etc.Type: ApplicationFiled: June 25, 2014Publication date: November 20, 2014Inventors: Shinichi TAIRA, Kunio OSHIMA, Takashi OSHIYAMA, Yasuhiro MENJO, Yasuo KOGA, Hokuto YAMABE, Sunao NAKAYAMA, Kenji TSUJIMAE, Toshiyuki ONOGAWA, Kuninori TAI, Motohiro ITOTANI
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Patent number: 8889676Abstract: The invention relates to 3-ureidoisoquinolin-8-yl derivatives of formula I wherein R1 is alkyl, haloalkyl or cyclopropyl; R2 is H, halogen, pyridazin-4-yl, pyrimidin-5-yl or an optionally substituted pyridin-3-yl, pyridin-4-yl or phenyl group; R3 is alkyl, alkynyl, aminoalkyl, carbamoylalkyl, methylcarbamoylalkyl, alkoxy, haloalkoxy, alkynyloxy, (4-hydroxybut-2-yn-1-yl)oxy, (4-aminobut-2-yn-1-yl)oxy, dimethylaminoalkoxy, carbamoylalkoxy, alkylamino, cycloalkyl, cycloalkylalkyl, cycloalkylalkoxy, hydroxyalkyl, hydroxyalkoxy, alkoxyalkyl, alkoxyalkoxy, carboxyalkyl, carboxyalkoxy, alkoxycarbonylalkoxy, aryl, heteroaryl, benzyl, benzyloxy, 2-cyanoethoxy, 2,3-dihydroxypropoxy, 3,4-dihydroxybutoxy, —CH2Ra, —CH2CH2Rb, —(CH2)n—C(O)O—Rd, —(CH2)n—N(Rc)C(O)O—Rd, —O—(CH2)n—N(Rc)C(O)O—Rd, —(CH2)n—Re or —O—(CH2)n—Re; Ra is cyano, acetylamino or N,N-dimethylamino; Rb is cyano or carbamoyl; Rc is H or methyl; Rd is alkyl; Re is pyrrolidin-1-yl, piperidin-1-yl, piperidin-3-yl, morpholin-1-yl, 2-oxopyrrolidin-1-yl, 5-oxType: GrantFiled: March 28, 2012Date of Patent: November 18, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Markus Gude, Christian Hubschwerlen, Philippe Panchaud
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Patent number: 8889677Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: January 11, 2013Date of Patent: November 18, 2014Assignee: Boehringer Ingellheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf
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Patent number: 8889667Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: GrantFiled: December 29, 2011Date of Patent: November 18, 2014Assignee: Agios Pharmaceuticals, IncInventors: Francesco G. Salituro, Jeffrey Saunders, Shunqi Yan
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Publication number: 20140336178Abstract: The present invention is based, in part, on assays we conducted that revealed compounds that may be used to treat or prevent diseases characterized by an abnormal or undesirable association of one protein with another.Type: ApplicationFiled: April 29, 2014Publication date: November 13, 2014Applicants: The General Hospital Corporation, Massachusetts Institute of TechnologyInventors: Aleksey G. Kazantsev, Anne B. Young, David E. Housman, Steven M. Hersch
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Patent number: 8883791Abstract: This invention relates to certain N-heteroaryl compounds that are generally useful as medicaments, more specifically as medicaments for animals. The medicament can preferably be used for the treatment of helminth infections and the treatment of parasitosis, such as caused by helminth infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to the preparation of the N-heteroaryl compounds. Moreover this invention relates to pharmaceutical compositions and kits comprising the compounds.Type: GrantFiled: September 28, 2011Date of Patent: November 11, 2014Assignee: Intervet Inc.Inventors: Michael Berger, Christopher Kern, Marko Eck, Jörg Schröder
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Patent number: 8883792Abstract: The present invention provides a novel isoquinoline-6-sulfonamide derivative that is useful as a medicine. The present invention provides an isoquinoline-6-sulfonamide derivative represented by Formula (1), a salt thereof, or a solvate of the derivative or the salt, wherein R1 and R2 each independently represent a hydrogen atom, or the like; R3 and R4 each independently represent a hydrogen atom, an alkyl group, or the like; R5 represents a hydrogen atom, an optionally substituted alkyl group, an optionally substituted alkenyl group, an optionally substituted alkynyl group, an optionally substituted cycloalkyl group, an optionally substituted alkanoyl group, or the like; and A represents a linear or branched alkylene group having 2 to 6 carbon atoms.Type: GrantFiled: December 21, 2011Date of Patent: November 11, 2014Assignee: D. Western Therapeutics Institute, Inc.Inventors: Hiroyoshi Hidaka, Kengo Sumi, Kouichi Takahashi, Yoshihiro Inoue
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Patent number: 8883789Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. R1, R2, R3, R4, Q have meanings given in the description.Type: GrantFiled: December 10, 2012Date of Patent: November 11, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Annekatrin Heimann, Georg Dahmann, Marc Grundl, Stephan Georg Mueller, Bernd Wellenzohn
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Publication number: 20140328796Abstract: The invention provides 4-amino-4-oxobutanoyl peptide compounds of Formula I and the pharmaceutically salts and hydrates thereof. The variables R1-R9, R16, R18, R19, n, M, n, M, and Z are defined herein. Certain compounds of Formula I are useful as antiviral agents. Certain 4-amino-4-oxobutanoyl peptide compounds disclosed herein are potent and/or selective inhibitors of viral replication, particularly Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more 4-amino-4-oxobutanoyl peptide compounds and one or more pharmaceutically acceptable carriers. Such pharmaceutical compositions may contain 4-amino-4-oxobutanoyl peptide compound as the only active agent or may contain a combination of 4-amino-4-oxobutanoyl peptide containing peptides compound and one or more other pharmaceutically active agents. The invention also provides methods for treating viral infections, including Hepatitis C infections, in mammals.Type: ApplicationFiled: July 21, 2014Publication date: November 6, 2014Inventors: Avinash Phadke, Xiangzhu Wang, Suoming Zhang, Atul Agarwal
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Publication number: 20140329830Abstract: The present invention relates to a compound of formula (I), and to pharmaceutical compositions containing said compound and to the use of said compound in therapy, for instance in treating cognitive disorders, as well as to intermediates useful in the preparation thereof.Type: ApplicationFiled: December 19, 2011Publication date: November 6, 2014Applicant: AstraZeneca ABInventors: Helena Gybäck, Jonas Malmström, Elgaard Gitte Terp
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Publication number: 20140329794Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: ApplicationFiled: December 20, 2013Publication date: November 6, 2014Applicant: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof, Lei Jin
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Patent number: 8877752Abstract: Provided are 4(1H)-quinolone derivatives effective in inhibiting or eliminating the viability of at least one of the stages in the life-cycle of the malarial parasite, and to show a reduced propensity to induce resistance to the compound by the target parasite. In particular, the compounds can be derivatives of phenoxyethoxy-quinolones, and including, but not only, 7-(2-phenoxyethoxy)quinolin derivatives. These compounds may be administered by themselves, with at least one other derivative compound, or with other antimalarial compounds, to an animal or human subject. The therapeutic compositions can be and formulated to reduce the extent of a Plasmodium infection in the recipient subject, or to reduce the likelihood of the onset or establishment of a Plasmodium infection if administered prior to the parasite contacting the subject. The therapeutic compositions can be formulated to provide an effective single dose amount of an antimalarial compound or multiple doses for administering over a period of time.Type: GrantFiled: October 26, 2012Date of Patent: November 4, 2014Assignee: University of South FloridaInventors: Roman Manetsch, Richard Matthew Cross, Niranjan Kumar Namelikonda, Dennis Edward Kyle, Tina Susanna Mutka, Alexis Nichole LaCrue, Jordany Richarlson Maignan, Fabian Ernesto Saenz
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Patent number: 8877945Abstract: The present invention provides redox drug derivatives. In particular, 9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid, 1-ethyl-6-fluoro-1,4-dihydro-7-(4-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, (3R,4R,5S)-4-(acetylamino)-5-amino-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylic acid ethyl ester, (3S)-3-(aminomethyl)-5-methylhexanoic acid, (3S)-1-[2-(2,3-dihydro-5-benzofuranyl)ethyl]-?-?-diphenyl-3-pyrrolidineacetamide, (1S,2S,3S,4R)-3-[(1S)-1-acetamido-2-ethyl-butyl]-4-(diaminomethylideneamino)-2-hydroxy-cyclopentane-1-carboxylic acid and (2R,3R,4S)-4-[(diaminomethylidene)amino]-3-acetamido-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid redox derivatives.Type: GrantFiled: May 17, 2010Date of Patent: November 4, 2014Assignee: Redx Pharma LimitedInventors: Derek Lindsay, Peter Jackson
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Publication number: 20140323467Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: May 23, 2014Publication date: October 30, 2014Applicant: AGIOS PHARMACEUTICALS, INCInventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
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Publication number: 20140323482Abstract: The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.Type: ApplicationFiled: December 17, 2012Publication date: October 30, 2014Inventors: Yao Ma, Manami Shizuka, Timothy J. Guzi, Yuan Liu, Yuan Tian, Brian R. Lahue, Craig R. Gibeau, Gerald W. Shipps, JR., Yaolin Wang, Stephane L. Bogen, Latha G. Nair, Weidong Pan, Mark A. McCoy, Matthew E. Voss, Margarita Kirova-Snover, W. Bent Clayton
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Patent number: 8871757Abstract: 6- and 7-amino isoquinoline compounds are provided that influence, inhibit or reduce the action of a kinase. Pharmaceutical compositions including therapeutically effective amounts of the 6- and 7-aminoisoquinoline compounds and pharmaceutically acceptable carriers are also provided. Various methods using the compounds and/or compositions to affect disease states or conditions such as cancer, obesity and glaucoma are also provided.Type: GrantFiled: February 12, 2010Date of Patent: October 28, 2014Assignee: Aerie Pharmaceuticals, Inc.Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Geoffrey Richard Heintzelman, Susan M. Royalty
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Patent number: 8865720Abstract: 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: GrantFiled: October 14, 2013Date of Patent: October 21, 2014Assignee: Janssen Pharmaceutica NVInventors: 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 Viviane Van Heusden
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Patent number: 8865704Abstract: The present invention relates to known and novel compounds of formula (I) as herein described and pharmaceutical compositions thereof. The compounds of formula (I) have inhibitory effect on the Wnt pathway and are therefore useful in the preparation of a medicament, in particular for the treatment of cancer.Type: GrantFiled: October 6, 2010Date of Patent: October 21, 2014Assignee: Siena Biotech S.p.A.Inventors: Maurizio Varrone, Arianna Nencini, Joanna Margaret Quinn, Andrea Caricasole, Annette Cornelia Bakker, Giovanni Gaviraghi, Massimilano Salerno
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Publication number: 20140309227Abstract: The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, such as Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 26, 2012Publication date: October 16, 2014Inventors: Christopher James Bungard, Antonella Converso, Pablo De Leon, Barbara Hanney, Timothy John Hartingh, Jesse Josef Manikowski, Peter J. Manley, Robert Meissner, Zhaoyang Meng, James J. Perkins, Michael T. Rudd, Youheng Shu
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Publication number: 20140309236Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.Type: ApplicationFiled: October 9, 2013Publication date: October 16, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Takuji BANDO, Satoshi AOKI, Junichi KAWASAKI, Makoto ISHIGAMI, Youichi TANIGUCHI, Tsuyoshi YABUUCHI, Kiyoshi FUJIMOTO, Yoshihiro NISHIOKA, Noriyuki KOBAYASHI, Tsutomu FUJIMURA, Masanori TAKAHASHI, Kaoru ABE, Tomonori NAKAGAWA, Koichi SHINHAMA, Naoto UTSUMI, Michiaki TOMINAGA, Yoshihiro OOI, Shohei YAMADA, Kenji TOMIKAWA
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PHARMACEUTICALLY ACCEPTABLE SALTS OF QUINOLINONE COMPOUNDS HAVING IMPROVED PHARMACEUTICAL PROPERTIES
Publication number: 20140303182Abstract: A lacate salt of a compound of Formula I or a tautomer of the compound, wherein Formula I has the following structure and R1-R9 and R12-R14 are as defined hereinType: ApplicationFiled: March 17, 2014Publication date: October 9, 2014Applicant: NOVARTIS AGInventors: Shaopei Cai, Joyce Chou, Eric Harwood, Timothy Machajewski, David Ryckman, Xiao Shang, Shuguang Zhu, Augustus Okhamate, Marc S. Tesconi -
Publication number: 20140303153Abstract: The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof: In formula I the variables Het, A, X, Y, Z, R1, R2, R3, R4, R5 and Q are as defined in the claims. The compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof are inhibitors of phosphodiesterase type 10A. Thus, the invention also relates to the use of the compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof for the manufacture of a medicament and which thus are suitable for treating or controlling of medical disorders selected from neurological disorders and psychiatric disorders, for ameliorating the symptoms associated with such disorders and for reducing the risk of such disorders.Type: ApplicationFiled: March 13, 2014Publication date: October 9, 2014Inventors: Hervé GENESTE, Michael OCHSE, Karla DRESCHER, Berthold BEHL, Loic LAPLANCHE, Jürgen DINGES, Clarissa JAKOB
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Publication number: 20140296251Abstract: Novel quinoline derivatives are disclosed. Also disclosed are synthesis and use thereof for treating neurodegenerative diseases.Type: ApplicationFiled: April 2, 2013Publication date: October 2, 2014Applicant: Annji Pharmaceutical Co., Ltd.Inventors: Ji-Wang Chern, Chen-Wei Huang, Pei-Teh Chang, Rahul Subhash Talekar
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Publication number: 20140296214Abstract: The present invention provides compounds of Formula (I): or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: October 2, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
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Publication number: 20140296215Abstract: The present disclosure provides pharmaceutical compositions, pharmaceutical preparations and methods for increasing activity of a mutant cystic fibrosis transmembrane conductance regulator protein (mutant-CFTR). The pharmaceutical compositions, pharmaceutical preparations and methods are useful for the study and treatment of disorders associated with mutant-CFTR, such as cystic fibrosis. The pharmaceutical compositions and pharmaceutical preparations may include one or more cyanoquinoline-containing compounds of the embodiments, or an analog or derivative thereof.Type: ApplicationFiled: May 25, 2012Publication date: October 2, 2014Applicant: The Regents of the University of CaliforniaInventors: Alan S. Verkman, Puay-Wah Phuan, Mark J. Kurth, John Knapp
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Publication number: 20140288088Abstract: The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds act as diuretics and natriuretics and are valuable pharmaceutically active compounds for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension and conditions resulting from excessive salt and water retention.Type: ApplicationFiled: October 22, 2012Publication date: September 25, 2014Inventors: Haifeng Tang, Barbara Pio, Harry R. Chobanian
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Publication number: 20140275060Abstract: Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of certain neurologic disorders, including disorders related to NMDA receptor activity, including neuropsychiatric disorders, neurodegenerative disorders and other neurologic diseases, disorders and conditions including stroke, brain injury, epilepsy, neuropsychiatric disorders, mood disorders, chronic pain and related conditions.Type: ApplicationFiled: March 14, 2014Publication date: September 18, 2014Inventors: David Steven Menaldino, George Walter Koszalka, Ruppa Poornachary Kamalesh Babu, Scott James Myers
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Publication number: 20140274960Abstract: The present invention provides compounds of Formula (I) or stereoisomers, pharmaceutically acceptable salts thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of factor XIa and/or plasma kallikrein which may be used as medicaments.Type: ApplicationFiled: October 12, 2012Publication date: September 18, 2014Inventors: Michael J. Orwat, Donald J.P. Pinto, Leon M. Smith, II, Shefali Srivastava
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Patent number: 8835436Abstract: A novel arylpiperazine-containing imidazole 4-carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition comprising the same as an active ingredient for preventing or treating a depressive disorder are provided.Type: GrantFiled: July 9, 2010Date of Patent: September 16, 2014Assignee: Green Cross CorporationInventors: Jinhwa Lee, Hee Jeong Seo, Suk Youn Kang, Eun-Jung Park, Min Ju Kim, Suk Ho Lee, Jong Yup Kim, Jeongmin Kim, Myung Eun Jung, Hyun Jung Kim, Mi-soon Kim, Ho Kyun Han, Kwang Woo Ahn, Min Woo Lee, Ki-Nam Lee, Ae Nim Pae, Woo-Kyu Park
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Publication number: 20140256666Abstract: The present invention describes single drug entities, formed by connecting an antibiotic moiety via a linker with a non-steroidal anti-inflammatory drug (NSAID) moiety. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual antibiotic and NSAID drug.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Publication number: 20140256658Abstract: The present invention describes antibiotic conjugates. These single drug entities are formed connecting one antibiotic with another antibiotic. Upon topical application to the eye, the conjugate hybrid would undergo enzymatic and/or hydrolytic cleavage to release the individual drugs.Type: ApplicationFiled: March 6, 2014Publication date: September 11, 2014Applicant: Allergan, Inc.Inventors: Santosh C. Sinha, Smita S. Bhat, Ken Chow, LIMING WANG, MICHAEL E. GARST, MAYSSA ATTAR, BRANDON D. SWIFT
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Patent number: 8829002Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: GrantFiled: December 13, 2011Date of Patent: September 9, 2014Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Publication number: 20140249144Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: ApplicationFiled: May 12, 2014Publication date: September 4, 2014Applicant: KOWA COMPANY, LTD.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Publication number: 20140249148Abstract: Provided herein are inhibitors of HDAC3, as well as methods of treatment comprising administering those compounds to a subject in need thereof.Type: ApplicationFiled: January 31, 2014Publication date: September 4, 2014Inventors: John H. van Duzer, Ralph Mazitschek
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Patent number: 8822464Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, Ar, R1, R2, R3 have meanings given in the description.Type: GrantFiled: November 26, 2012Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Grauert, Daniel Bischoff, Georg Dahmann, Raimund Kuelzer, Klaus Rudolf