Plural Ring Nitrogens In The Polycyclo Ring System Patents (Class 514/322)
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Publication number: 20120088751Abstract: Tricyclic pyrazole derivatives of the following formula (I) having affinity for the cannabinoidergic CB1 and/or CB2 receptors: wherein: A represents a group selected from one of the following: (CH2)t—, —(CH2)—S(O)z—, or —S(O)z—(CH2)—, B is a heteroaryl, optionally substituted; R is a group selected from the following: alkyl, aryl, arylalkyl or arylalkenyl, not substituted or having from one to four substituents, equal to or different from each other; R? is a group selected from the following: an ether group of formula —(CH2)—O—(CH2)v—R?, a ketonic group of formula —C(O)—Z?, wherein Z? is as defined below; a substituent having an hydroxyl function of formula —CH(OH)—Z?; an amide substituent of formula —C(O)—NH-T?.Type: ApplicationFiled: December 16, 2011Publication date: April 12, 2012Applicant: NEUROSCIENCZE PHARMANESS S.C. A R.L.Inventors: Paolo LAZZARI, Stefania RUIU, Gerard Aime PINNA, Gabrielle MURINEDDU
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Patent number: 8153658Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).Type: GrantFiled: November 14, 2007Date of Patent: April 10, 2012Assignee: Astellas Pharma, Inc.Inventors: Shunichiro Hachiya, Kazuhiro Ikegai, Ryotaro Ibuka, Taisuke Takahashi, Makoto Oku, Ryushi Seo, Yoh Terada, Masanao Sanagi
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Patent number: 8148363Abstract: The present invention relates to novel heterocyclic compounds of Formulae I-III; as disclosed herein or a pharmaceutically acceptable salt, solvate, ester, prodrug or stereoisomer thereof. Also disclosed are pharmaceutical compositions comprising said compounds, and methods for using said compounds for treating or preventing a thromboembolic disorder.Type: GrantFiled: May 18, 2009Date of Patent: April 3, 2012Assignee: Schering CorporationInventors: Martin C. Clasby, William J. Greenlee, Yan Xia, Tin-Yau Chan, Mariappan V. Chelliah, Samuel Chackalamannil, Haiyan Pu, Keith A. Eagen, Henry Vaccaro, Brian A. McKittrick, Liyuan Wang, Xiaobang Gao
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Patent number: 8148401Abstract: The present invention relates to a compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3A, R3B, R4, R5, X, m, and n are as defined herein. Such novel benzamidazole derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: June 19, 2008Date of Patent: April 3, 2012Assignee: Pfizer Inc.Inventors: Michael J. Munchhof, Lawrence A. Reiter, Susan D. La Greca, Christopher S. Jones, Qifang Li
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Publication number: 20120076755Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B-W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: October 4, 2011Publication date: March 29, 2012Inventors: Yao-Ling Qiu, Ce Wang, Xiaowen Peng, Lu Ying, Hui Cao, Yat Sun Or
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Patent number: 8143282Abstract: The present invention relates to compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to heterocyclic compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.Type: GrantFiled: August 1, 2006Date of Patent: March 27, 2012Assignee: S*BIO Pte Ltd.Inventors: Dizhong Chen, Weiping Deng, Ken C. Lee, Pek L. Lye, Eric T. Sun, Haishan Wang, Niefang Yu
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Patent number: 8138168Abstract: The invention relates to compounds having the formulae: wherein the variables are as defined herein. The invention further relates to methods of making and using these compounds, and pharmaceutical compositions, kits and articles of manufacture comprise the compounds.Type: GrantFiled: September 26, 2008Date of Patent: March 20, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Benjamin Jones, Stephen W. Kaldor, Walter Keung, Andre A. Kiryanov, Zhe Li, Jeffrey A. Stafford, John Tyhonas, Craig Behnke
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Patent number: 8138207Abstract: The present invention comprises the use of amino-carbonyl-substituted 8-N-benzimidazoles compounds of formula I wherein R3, R4-R5, R11 and R20-R21 are hereinafter defined which display a therapeutically utilizable blood sugar-lowering action. These compounds are intended to be particularly suitable in the treatment of diabetes, carbohydrate and lipid metabolic disorders and other blood sugar complications.Type: GrantFiled: September 14, 2007Date of Patent: March 20, 2012Assignee: Sanofi-AventisInventors: Elisabeth DeFossa, Karl Schoenafinger, Gerhard Jaehne, Christian Buning, Georg Tschank, Ulrich Werner
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Patent number: 8138177Abstract: This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: A, B, R1, R2 and R3 are each as described herein, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by CB2 receptor binding activity such as, but not limited to, inflammatory pain, nociceptive pain, neuropathic pain, fibromyalgia, chronic low back pain, visceral pain, acute cerebral ischemia, pain, chronic pain, acute pain, post herpetic neuralgia, neuropathies, neuralgia, diabetic neuropathy, HIV-related neuropathy, nerve injury, rheumatoid arthritic pain, osteoarthritic pain, back pain, cancer pain, dental pain, fibromyalgia, neuritis, sciatica, inflammation, neurodegenerative disease, cough, broncho constriction, irritable bowel syndrome (IBS), inflammatory bowel disease (IBD), colitis, cerebrovascular ischemia, emesis such as cancer chemotherapy-induced emesis, rheumatoid arthritis, asthma, Crohn's disease, ulcerative colitis, asthmaType: GrantFiled: March 2, 2006Date of Patent: March 20, 2012Assignee: Pfizer Inc.Inventors: Kazuo Ando, Makoto Kawai, Tsutomu Masuda, Hirofumi Omura
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Publication number: 20120065167Abstract: The invention relates to the use of domperidone or a pharmaceutically acceptable salt thereof at low doses to prevent and/or treat a disease associated with an alteration of the immune response such as Leishmaniosis.Type: ApplicationFiled: March 30, 2010Publication date: March 15, 2012Applicant: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: David Sabate Elias, Josep M. Homedes Beguer, Pablo Gomez Ochoa
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Publication number: 20120064152Abstract: The present invention provides a method for eliciting an onset hastened analgesic and anti-inflammatory response and combating nausea in acute migraine attacks. This method comprises administering a pharmaceutical composition comprising more than one active ingredient, wherein said more than one active ingredient consist essentially of: (i) domperidone or an analogue thereof in an amount sufficient to hasten the onset of the analgesic and anti-inflammatory response and to combat nausea in an acute migraine attack, and (ii) a NSAID, a pharmaceutically acceptable salt thereof or a pure (?) or pure (+) optical isomeric form thereof in an analgesically and anti-inflammatory effective amount, wherein said NSAID is selected from the group consisting of proprionic acid derivatives, acetic acid derivatives, fenamic acid derivatives, biphenylcarboxylic acid derivatives and oxicams.Type: ApplicationFiled: November 18, 2011Publication date: March 15, 2012Applicant: THE BOOTS COMPANYInventor: Ninh ON
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Publication number: 20120065210Abstract: There are provided compounds of formula I or a pharmaceutically acceptable salt thereof, wherein X, Y, R1, R1?, R2, R2?, R3, R4, R5 are as defined herein. The compounds exhibit activity as anticancer agents.Type: ApplicationFiled: September 7, 2011Publication date: March 15, 2012Inventors: Xin-Jie Chu, Qingjie Ding, Nan Jiang, Jin-Jun Liu, Tina Morgan Ross, Zhuming Zhang
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Publication number: 20120059016Abstract: The present invention relates to piperidine and pyrazine derivatives according to formulae (Ia), (Ib) and (II) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.Type: ApplicationFiled: March 3, 2010Publication date: March 8, 2012Inventors: Kai Schiemann, Melanie Schultz, Wolfgang Staehle
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Publication number: 20120058201Abstract: The present invention describes an association between genetic polymorphisms in the FAM13A1 (family with sequence similarity 13, member A1) gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval- prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation.Type: ApplicationFiled: April 5, 2010Publication date: March 8, 2012Applicant: VANDA PHARMACEUTICALS, INC.Inventors: Christian Lavedan, Simona Volpi, Louis Licamele
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Patent number: 8129374Abstract: Compounds, compositions and methods are provided for modulating the activity of receptor kinases and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by receptor kinases.Type: GrantFiled: August 4, 2010Date of Patent: March 6, 2012Assignee: Ambit Bioscience CorporationInventors: Shripad Bhagwat, Qi Chao, Robert M. Grotzfeld, Hitesh K. Patel, Kelly G. Sprankle
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Publication number: 20120053166Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.Type: ApplicationFiled: March 5, 2010Publication date: March 1, 2012Inventors: Julie Nicole Hamblin, Zoe Alicia Harrison, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Nigel James Parr
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Publication number: 20120046303Abstract: Compounds which inhibit the activity of poly(ADP-ribose)polymerase (PARP), compositions containing the compounds and methods of treating diseases using them are disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 23, 2012Applicant: ABBOTT LABORATORIESInventors: Virajkumar B. Gandhi, Vincent L. Giranda, Jianchun Gong, Thomas D. Penning, Gui-Dong Zhu
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Publication number: 20120046275Abstract: The present invention is directed to synthetic cytoskeletal active compounds that are inhibitors of rho-associated protein kinase. The present invention is also directed to pharmaceutical compositions comprising such compounds and a pharmaceutically acceptable carrier. The invention is additionally directed to a method of preventing or treating diseases or conditions associated with cytoskeletal reorganization. In one embodiment of the invention, the method treats increased intraocular pressure, such as primary open-angle glaucoma. The method comprises administering to a subject a therapeutically effective amount of a cytoskeletal active compound of Formula I or Formula II, wherein said amount is effective to influence the actomyosin interactions, for example by leading to cellular relaxation and alterations in cell-substratum adhesions.Type: ApplicationFiled: October 13, 2011Publication date: February 23, 2012Inventors: John W. Lampe, Paul S. Watson, David J. Slade, Ward M. Peterson, Christopher S. Crean, Jason L. Vittitow, Jonathan Bryan DeCamp, Nicholas F. Pelz
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Patent number: 8119621Abstract: This invention is directed to a tetrahydro-cyclopentyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: July 15, 2010Date of Patent: February 21, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Fina Liotta, Mingde Xia, Michael P. Wachter, Scott A. Beers
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Patent number: 8119661Abstract: Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein R2, R3, X, m and n 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: GrantFiled: September 8, 2008Date of Patent: February 21, 2012Assignee: AstraZeneca ABInventors: Yun-Xing Cheng, Xuehong Luo, Vijayaratnam Santhakumar, Miroslaw Jerzy Tomaszewski
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Publication number: 20120041028Abstract: Compounds of formula (I), salts and solvates are provided: Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: David Gwyn COOPER, Ian Thomas Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Publication number: 20120041027Abstract: Compounds of formula (I) and salts and solvates are provided: wherein Uses of the compounds for therapy, for example in the treatment of psychotic disorders and cognitive impairment, are also disclosed.Type: ApplicationFiled: October 27, 2011Publication date: February 16, 2012Inventors: David Gwyn COOPER, Ian Thomson Forbes, Vincenzo Garzya, Jian Jin, Yann Louchart, Graham Walker, Paul Adrian Wyman
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Publication number: 20120035214Abstract: The present invention relates to biaryl piperidine-based renin inhibitor compounds, and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: April 1, 2010Publication date: February 9, 2012Applicants: Merck Canada Inc., Merck Sharp & Dohme Corp.Inventors: Daniel J. McKay, Melissa Arbour, Renee Aspiotis, Austin Chen, Pierre-Andre Fournier, Michel Gallant, Yongxin Han, Helene Juteau, Patrick Lacombe, Sebastien Laliberte, Sophie Lauzon, Carmela Molinaro, Paul O'Shea, Yeeman Ramtohul, Daniel Simard, Dwight MacDonald, Bruce Mackay, Christophe Mellon, Krista Morley, Chit Tsui, Sarah Jennifer Dolman, Greg Hughes, Jacob Janey
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Publication number: 20120035164Abstract: The invention is directed to novel indole carboxamide derivatives. Specifically, the invention is directed to compounds according to formula I: where R1, R2, R3, U and V are defined below and to pharmaceutically acceptable salts thereof. The compounds of the invention are inhibitors of IKK2 and can be useful in the treatment of disorders associated with inappropriate IKK2 (also known as IKK?) activity, such as rheumatoid arthritis, asthma, and COPD (chronic obstructive pulmonary disease). Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting IKK2 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.Type: ApplicationFiled: October 14, 2011Publication date: February 9, 2012Inventors: Jianghe DENG, Jeffrey K. KERNS, Qi JIN, Guoliang LIN, Xichen LIN, Michael LINDENMUTH, Christopher NEIPP, Hong NIE, Sonia M. THOMAS, Katherine L. WIDDOWSON
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Publication number: 20120035131Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I: wherein R1, R2, R3A, R3B, R4, R5, R6, R7, R8, and X are as defined in the detailed description of the invention. Corresponding pharmaceutical compositions, methods of treatment, and intermediates are also disclosed.Type: ApplicationFiled: October 20, 2011Publication date: February 9, 2012Inventors: Marvin J. Meyers, Graciela B. Arhancet, Xiangyang Chen, Susan Hockerman, Scott A. Long, Matthew W. Mahoney, David B. Reitz, Joseph G. Rico
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Publication number: 20120035173Abstract: This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson's disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, among numerous others. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.Type: ApplicationFiled: September 6, 2011Publication date: February 9, 2012Inventors: Leslie Street, Rudolf Mueller, Steven Lee
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Publication number: 20120028962Abstract: A compound represented by the following formula or a salt thereof, which has an GPR119 agonist action, is useful for the prophylaxis or treatment of diabetes, obesity and the like, and shows superior efficacy: wherein P: substituted 6-membered aromatic ring, Q: (substituted) 6-membered aromatic ring, CR4aR4b, NR4c, O, S, SO or SO2 {R4a-4c: H etc.}, L1: (substituted) C1-5 alkylene, L2: a bond or (substituted) C1-3 alkylene, L3-4: (substituted) C1-3 alkylene, R1: H, X, CN, (substituted) hydrocarbon, (substituted) heterocycle or (substituted) OH, or (substituted) 4- to 8-membered (heterocyclic) ring together with A1, R2: H, CN, (substituted) hydrocarbon, and R3a: —COSRA1, (substituted) 5- or 6-membered aromatic ring {RA1: (substituted) hydrocarbon or (substituted) heterocycle}.Type: ApplicationFiled: February 17, 2010Publication date: February 2, 2012Inventors: Kentaro Rikimaru, Hiroshi Imoto, Masahiro Kamaura
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Publication number: 20120022090Abstract: The present invention is concerned with novel substituted benzoxazole, benzimidazole, oxazolopyridine and imidazopyridine derivatives of Formula (I) wherein R1, R2, R3, R4, X, A1, A2, A3, A4, Y1, Y2, Y3 and Z 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 compounds as an active ingredient as well as the use of said compounds as a medicament.Type: ApplicationFiled: February 15, 2010Publication date: January 26, 2012Inventors: Henricu Jacobus Maria Gijsen, Francois Paul Bischoff, Wei Zhuang, Sven Franciscus Anna Van Brandt, Michel Surkyn, Mirko Zaja, Didier Jean-Claude Berthelot, Michel Anna Jozef Cleyn, Gregor James Macdonald, Daniel Oehlrich
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Patent number: 8101592Abstract: This invention is directed to a hexahydro-cyclooctyl pyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.Type: GrantFiled: May 24, 2010Date of Patent: January 24, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Mingde Xie, Fina Liotta, Huajun Lu, Meng Pan, Michael P. Wachter
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Publication number: 20120015932Abstract: Indazole compounds, processes for their preparation, intermediates usable in these processes, pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: February 24, 2010Publication date: January 19, 2012Inventors: Heather Hobbs, Simon Teanby Hodgson, Yannick Maurice LaCroix, Deborah Needham, Nigel James Parr, Panayiotis Alexandrou Procopiou, Timothy John Ritchie, Michael David Woodrow
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Publication number: 20120015035Abstract: The present invention provides compositions and methods for treating ocular disorders such as myopia.Type: ApplicationFiled: January 11, 2010Publication date: January 19, 2012Inventors: Christine F. Wildsoet, James Su, Kevin E. Healy
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Publication number: 20120015959Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumours.Type: ApplicationFiled: March 3, 2010Publication date: January 19, 2012Inventors: Wolfgang Staehle, Kai Schiemann, Melanie Schultz
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Publication number: 20120004196Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: May 4, 2011Publication date: January 5, 2012Applicant: ABBOTT LABAORATORIESInventors: David A. DeGoey, Warren M. Kati, Charles W. Hutchins, Pamela L. Donner, Allan C. Krueger, John T. Randolph, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, Mark A. Matulenko, Ryan G. Keddy, Tammie K. Jinkerson, Yi Gao, Dachun Liu, John K. Pratt, Todd W. Rockway, Clarence J. Maring, Douglas K. Hutchinson, Charles A. Flentge, Rolf Wagner, Michael D. Tufano, David A. Betebenner, Kathy Sarris, Kevin R. Woller, Seble H. Wagaw, Jean C. Califano, Wenke Li, Daniel D. Caspi, Mary E. Bellizzi, William A. Carroll
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Publication number: 20110319417Abstract: Methods of treating a TRPC5 mediated disorder in a subject by administering an effective amount of a TRPC5 antagonist, such as a compound disclosed herein, are described.Type: ApplicationFiled: August 6, 2009Publication date: December 29, 2011Inventors: Jayhong Chong, Christopher Fanger, Magdalene M. Moran, Elisha Singer, Timothy Strassmaier, Howard Ng
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Publication number: 20110319393Abstract: This invention is directed to compounds and salts that are generally useful as anthelmintic agents or as intermediates in processes for making anthelmintic agents. This invention also is directed to processes for making the compounds and salts, pharmaceutical compositions and kits comprising the compounds and salts, uses of the compounds and salts to make medicaments, and treatments comprising the administration of the compounds and salts to animals in need of the treatments.Type: ApplicationFiled: March 17, 2010Publication date: December 29, 2011Inventors: Christophe Pierre Alain Chassaing, Thorsten Meyer
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Publication number: 20110312949Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSD1 and may be useful in the treatment, prevention and/or prophylaxis of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.Type: ApplicationFiled: August 30, 2011Publication date: December 22, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: John Paul Kilburn, Henrik Sune Andersen, Gita Camilla Tejlgaard Kampen, Soren Ebdrup
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Publication number: 20110311485Abstract: The present disclosure relates to 1, 2, 4 oxadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.Type: ApplicationFiled: December 15, 2009Publication date: December 22, 2011Applicant: ALMIRALL S.A.Inventors: Victor Giulio Matassa, Nuria Aguilar Izquierdo, Marta Mir Cepeda, Marta Carrascal Riera, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Julio Cesar Castro Palomino Laria, Montserrat Erra Sola
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Publication number: 20110306601Abstract: Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicant: The Regents of the University of CaliforniaInventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
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Publication number: 20110306611Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.Type: ApplicationFiled: August 3, 2009Publication date: December 15, 2011Applicant: Paratek Pharmaceuticals, Inc.Inventors: Michael N. Alekshun, Victor Amoo, Oak K. Kim, Atul K. Verma
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Publication number: 20110306638Abstract: The invention relates to a benzisoxazolyl piperidine derivative having the following general formula, a salt or a hydrate thereof, wherein R, X, Y, R? and T are defined as in the specification. Such compounds have serotonin system modulating effects such as antagonizing effect on 5-HT2A and inhibitory effect on 5-HT reuptake. The compounds have good analgesic and sedative activities with mild toxic and side effects. The invention also relates to a composition comprising said derivative and the use thereof.Type: ApplicationFiled: December 22, 2009Publication date: December 15, 2011Applicant: NHWA PHARMA. CORPORATIONInventors: Jianqi Li, Guan Wang, Guisen Zhang, Na Lv, Guangjun Jiao, Shicheng Liu, Shixia Zhou
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Publication number: 20110301154Abstract: The present invention involves new and original sigma receptors Ligands: (Mono-or dialkylaminoalkyl)-?-butyro-lactones, their analogues aminotetrahydroturanes, the (1-adamantyl) benzene alkylamines, the N,N Dialkyl ?-[(adamantyl-1)ben-zyloxy-2] alkylamines and the 3-cyclopentyl adamantyl-amines or alkylamines or-alkyl phenylamines, their enantiomers or di-astereoisomers, their pharmaceutically acceptable salts and Quinacrine Me-thylene blue, Astemizole and their relative analogues with pro-apoptotic and/or anti-apoptotic properties over cellular biochemical mechanisms, with prototypical anti-cancer, an-timetastatic and antiviral activities associated with antagonism of the neuropatic pain and, at very low doses, with cytoprotectve and cytoregenerative activity against the cytodegenerative diseases.Type: ApplicationFiled: February 17, 2010Publication date: December 8, 2011Inventor: Alexandre Vamvakides
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Publication number: 20110301146Abstract: GSK-3beta inhibitors comprising 7-Hydroxy-benzoimidazole-4-yl-methanone Derivatives are provided. For example, the inhibitors have following general formula (I).Type: ApplicationFiled: September 29, 2009Publication date: December 8, 2011Applicant: ONCOTHERAPY SCIENCE, INC.Inventors: Yo Matsuo, Ryuji Ohsawa, Shoji Hisada
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Publication number: 20110301191Abstract: Compounds and methods are provided for the treatment of disease conditions in which modification of serotonergic receptor activity has a beneficial effect. In the method, an effective amount of a compound is administered to a patient in need of such treatment.Type: ApplicationFiled: March 21, 2011Publication date: December 8, 2011Inventors: Carl-Magnus A. ANDERSSON, Glenn Croston, E.L. Hansen, Allan Kjaersgaard Uldam
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Publication number: 20110301192Abstract: The present invention provides compounds that inhibit cyclin kinase inhibitor p21, such as compounds of formula I. The present invention also provides compositions including compounds of Formula I and a pharmaceutically acceptable excipient. In addition, the present invention provides methods of inhibiting cyclin kinase inhibitor p21 and of treating cancer.Type: ApplicationFiled: September 29, 2009Publication date: December 8, 2011Applicant: The regents of the University of CaliforniaInventors: Robert Weiss, See-Hyoung Park, Kit S. Lam, Ruiwu Liu
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Patent number: 8071623Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts, stereoisomers or tautomers thereof which are inhibitors of poly (ADP-ribose) polymerase (PARP) and thus useful for the treatment of cancer, inflammatory diseases, reperfusion injuries, ischemic conditions, stroke, renal failure, cardiovascular diseases, vascular diseases other than cardiovascular diseases, diabetes, neurodegenerative diseases, retroviral infection, retinal damage or skin senescence and UV-induced skin damage, and as chemo- and/or radiosensitizers for cancer treatment.Type: GrantFiled: January 8, 2008Date of Patent: December 6, 2011Assignee: Instituto di Ricerche di Biologia Molecolare P. Angeletti SpAInventors: Philip Jones, Jesus Maria Ontoria Ontoria, Rita Scarpelli, Carsten Schultz-Fademrecht
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Patent number: 8071622Abstract: The present invention is concerned with novel indol-2-yl-carbonyl-piperidin-benzoimidazolon and indol-2-yl-carbonyl-piperidin-benzoxazolon derivatives as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of anxiety and depressive disorders and other diseases. In particular, the present invention concerns compounds of formula (I) wherein R1 to R11, X and Y are as defined in the specification.Type: GrantFiled: November 29, 2007Date of Patent: December 6, 2011Assignee: Hoffman-La Roche Inc.Inventors: Caterina Bissantz, Christophe Grundschober, Raffaello Masciadri, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
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Publication number: 20110294780Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: May 24, 2011Publication date: December 1, 2011Inventors: Gilles Bignan, Wing Cheung, Micheal Gaul, Hui Huang, Xun Li, Raymond Patch, Sharmila Patel, Mark Player, Guozhang Xu, Bao-Ping Zhao, Jian Liu
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Publication number: 20110294777Abstract: Substituted bicyclic beta-lactams of Formula I: (I), are ?-lactamase inhibitors, wherein a, X, R1 and R2 are defined herein. The compounds and pharmaceutically acceptable salts thereof are useful in the treatment of bacterial infections in combination with ?-lactam antibiotics. In particular, the compounds can be employed with a ?-lactam antibiotics (e.g., imipenem, piperacillin, or ceftazidime) against microorganisms resistant to ?-lactam antibiotics due to the presence of the ?-lactamases.Type: ApplicationFiled: January 15, 2009Publication date: December 1, 2011Inventors: Timothy A. Blizzard, Helen Chen, Candido Gude, Jeffrey D. Hermes, Jason Imbriglio, Seongkon Kim, Jane Y. Wu, Sookhee Ha, Christopher J. Mortko, Ian Mangion, Nelo Rivera, Rebecca T. Ruck, Michael Shevlin
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Publication number: 20110294804Abstract: The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like.Type: ApplicationFiled: December 25, 2009Publication date: December 1, 2011Applicant: DAINIPPON SUMITOMO PHARMA CO., LTD.Inventors: Katsunori Tsubio, Yusuke Yamai, Hitoshi Watanabe, Hironori Kinoshita
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Publication number: 20110294808Abstract: Disclosed indazoles compounds that are useful as antagonists of CCR1 activity and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. Also disclosed are pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: July 18, 2011Publication date: December 1, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Daniel KUZMICH, Can MAO, Alan David SWINAMER, David Smith THOMSON