Carbocyclic Ring Bonded Directly To The -c(=x)- (e.g., 3-benzoyl Pyrrolidine, Etc.) Patents (Class 548/539)
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Patent number: 9670155Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methy19243-yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.Type: GrantFiled: September 8, 2014Date of Patent: June 6, 2017Assignee: ObsEva S.A.Inventor: Andre Chollet
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Publication number: 20150080350Abstract: The present invention provides bumetanide, analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide, analogs and methods for their use. These analogs are particularly useful for the treatment and/or prophylaxis of conditions that involve the Na+K+Cl? co-transporter or GABAA receptor including but not limited to addictive disorders, Alzheimer's Disease, anxiety disorders, ascites, autism, bipolar disorder, cancer, depression, endothelial corneal dystrophy, edema, epilepsy, glaucoma. Huntington's Disease, insomnia, ischemia, migraine, migraine with aura, neuropathic pain, nociceptive neuralgia, nociceptive pain, ocular diseases, pain, Parkinson's disease, personality disorders, postherpetic neuralgia, psychosis, schizophrenia, seizure disorders, tinnitus, and withdrawal syndromes.Type: ApplicationFiled: August 28, 2014Publication date: March 19, 2015Inventors: John J. PARTRIDGE, Daryl W. HOCHMAN
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Publication number: 20150073032Abstract: The present invention relates to a compound of formula (3Z,5S)-5-(hydroxymethyl)-1-[(2?-methyl-1,1?-biphenyl-4-yl)carbonyl]pyrrolidin-3-one O-methy19243-yloxime, and/or an active metabolite thereof having antagonist action at the oxytocin receptor and/or vasopressin V1a receptor, to processes for their preparation, pharmaceutical compositions containing them and their use.Type: ApplicationFiled: September 8, 2014Publication date: March 12, 2015Inventor: Andre CHOLLET
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Publication number: 20150045408Abstract: The present invention is concerned with a novel process for the preparation of a compound of formula I and its hydrates The compounds of formula I and the corresponding hydrates are pharmaceutically active substances.Type: ApplicationFiled: October 24, 2014Publication date: February 12, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Jean-Michel Adam, Charles Alois Dvorak, Daniel Fishlock, Eric R. Humphreys, Hans Iding, Christophe Pfleger, Pankaj D. Rege, Xianqing Shi, Justin Vitale, Shaoning Wang, Marian Zajac
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Patent number: 8946478Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.Type: GrantFiled: November 3, 2011Date of Patent: February 3, 2015Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.Inventors: Hua Bai, Xuyang Zhao, Yongxiang Gong, Jinqing Zhong, Qifeng Zhu, Xiaoyu Liu, Lifei Liu, Qixian Zhou
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Publication number: 20150031663Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.Type: ApplicationFiled: October 13, 2014Publication date: January 29, 2015Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Shahriar Mobashery, Dusan Hesek, Mayland Chang
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Publication number: 20150025056Abstract: The present invention provides compounds of the formula I: its enantiomers, diastereomers, racemic mixtures thereof, prodrugs, crystalline forms, non-crystalline forms, amorphous forms thereof, solvates thereof, metabolites thereof, and pharmaceutically acceptable salts, wherein the ring A substituent groups are fully defined in the following disclosure. The compounds of formula I are inhibitors of metalloproteases such as matrix metalloproteases and sheddases, and are useful in treating diseases such as rheumatoid arthritis, psoriasis, neoplastic diseases, allergies and all those diseases wherein inhibition of MMPs is desirable.Type: ApplicationFiled: October 3, 2014Publication date: January 22, 2015Applicant: Incyte CorporationInventors: Yun-Long Li, Jincong Zhuo, David M. Burns, Wenqing Yao, Ravi Kumar Jalluri
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Patent number: 8853390Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.Type: GrantFiled: September 14, 2011Date of Patent: October 7, 2014Assignee: AbbVie Inc.Inventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
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Patent number: 8829184Abstract: A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.Type: GrantFiled: April 15, 2011Date of Patent: September 9, 2014Assignee: Spirogen SARLInventors: Philip Wilson Howard, Luke Masterson, Arnaud Tiberghien
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Publication number: 20140206537Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: March 25, 2014Publication date: July 24, 2014Applicant: DOW AGROSCIENCES LLCInventors: James E. Hunter, William C. Lo, Gerald B. Watson, Akshay Patny, Gary D. Gustafson, Dan Pernich, William K. Brewster, Debra L. Camper, Beth Lorsbach, Michael R. Loso, Thomas C. Sparks, Hemant Joshi, Adiraj Mandaleswaran, Ramadevi Sanam, Rambabu Gundla, Pravin S. Iyer
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Publication number: 20140171314Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: Dow AgroSciences LLCInventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
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Publication number: 20140171311Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: DOW AGROSCIENCES LLCInventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
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Publication number: 20140171309Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: DOW AGROSCIENCES LLCInventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
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Publication number: 20140171308Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: Dow AgroSciences LLCInventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
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Publication number: 20140171312Abstract: This document discloses molecules having the following formula (“Formula One”): and processes associated therewith.Type: ApplicationFiled: December 18, 2013Publication date: June 19, 2014Applicant: Dow AgroSciences LLCInventors: William C. Lo, James E. Hunter, Gerald B. Watson, Akshay Patny, Pravin S. Iyer, Joshodeep Boruwa
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Patent number: 8722725Abstract: The present invention provides caffeoylquinic acid derivatives and a method of preparing for the same, and also provides pharmaceutical compositions containing caffeoylquinic acid derivatives, and uses of caffeoylquinic acid derivatives in preparation of a medicament for the treatment or prophylaxis of virus diseases, in particular, uses of respiratory syncytial virus and hepatitis B virus, which has the characteristics of safety, high effectiveness and low toxicity.Type: GrantFiled: March 21, 2008Date of Patent: May 13, 2014Assignee: Zhejiang Medicine Co., Ltd. Xinchang Pharmaceutical FactoryInventors: Wu Zhanggui, Wei Wei
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Publication number: 20140080984Abstract: The present invention relates to a kind of novel carbene ligands and ruthenium catalysts, which is highly active and selective for ROMP and RCM reactions, respectively. It discloses the significant electronic and steric effect of different substituted carbene ligands on the catalytic activity and stability of corresponding carbene ruthenium complexes; some of novel ruthenium complexes in the invention can be broadly used as catalysts highly effectively and selective for ROMP and RCM reactions. The invention also relates to preparation of new ruthenium catalysts and the uses in metathesis. Moreover, the invention also provides effective methods of making various functional polymers by ROMP reaction in the presence of new ruthenium catalysts.Type: ApplicationFiled: November 21, 2013Publication date: March 20, 2014Applicant: ZANNA SCITECH CO., LTD.Inventor: Zheng-Yun James ZHAN
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Patent number: 8541572Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF—or combinations thereof.Type: GrantFiled: November 9, 2009Date of Patent: September 24, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Joseph A. Kozlowski, Wensheng Yu, Michael K. C. Wong, Seong Heon Kim, Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, De-Yi Yang, Robert Feltz, Aneta Maria Kosinski, Guowei Zhou, Razia K. Rizvi, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristin E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20130225810Abstract: Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.Type: ApplicationFiled: November 3, 2011Publication date: August 29, 2013Applicant: Zhejiang Hisun Pharmaceutical Co., Ltd.Inventors: Hua Bai, Xuyang Zhao, Yongxiang Gong, Jinqing Zhong, Qifeng Zhu, Xiaoyu Liu, Lifei Liu, Qixian Zhou
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Patent number: 8507544Abstract: The present invention relates to (2S)-2-({3?-Chloro-4?-[(2,2-dimethylpyrrolidin-1-yl) carbonyl]-5-fluorobiphenyl-2-yl}oxy)propanoic acid and (2R)-2-({3?-chloro-4?-[(2,2-dimethylpyrrolidin-1-yl) carbonyl]-5-fluorobiphenyl-2-yl}oxy)propanoic acid of formula (I), and crystalline forms and pharmaceutically acceptable salts thereof useful as pharmaceuticals.Type: GrantFiled: July 3, 2008Date of Patent: August 13, 2013Assignee: Astrazeneca ABInventors: Roger Victor Bonnert, Timothy Jon Luker, Anil Patel, Aaron Rigby
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Publication number: 20130184249Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: February 28, 2013Publication date: July 18, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130178457Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).Type: ApplicationFiled: July 5, 2012Publication date: July 11, 2013Applicant: LUPIN LIMITEDInventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
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Publication number: 20130143926Abstract: The invention provides a compound which is (a) a phenylamide derivative of formula (I) or a tautomer thereof, or (b) a pharmaceutically acceptable salt, N-oxide, hydrate, prodrug or solvate thereof: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The compounds are useful in the treatment of diseases mediated by HSP90.Type: ApplicationFiled: June 10, 2011Publication date: June 6, 2013Inventors: Alastair David Graham Donald, Joanne McDermott, Sanjay Ratilal Patel, David Festus Charles Moffat
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Publication number: 20130137018Abstract: The invention provides a dye compound having a partial structure represented by the following formula (5): wherein in formula (5), Dye represents a dye structure; G1 represents NR or an oxygen atom; G2 represents a monovalent substituent group having an ?Es? value as a steric parameter of 1.5 or more; p represents an integer from 1 to 8; when p is 2 or greater, the two or more structures represented by p may be the same or different from each other; and R represents a hydrogen atom or a monovalent substituent group.Type: ApplicationFiled: January 22, 2013Publication date: May 30, 2013Applicant: FUJIFILM CORPORATIONInventor: FUJIFILM CORPORATION
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Patent number: 8404679Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, Ar and n are as defined herein and pharmaceutically active salts, racemic mixtures, enantiomers, optical isomers or tautomeric forms thereof. The compounds can be used for the treatment of depression, anxiety or schizophrenia.Type: GrantFiled: April 23, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Caterina Bissantz, Philippe Jablonski, Henner Knust, Andreas Koblet, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Publication number: 20130040932Abstract: A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.Type: ApplicationFiled: September 24, 2012Publication date: February 14, 2013Applicants: Neuromed Pharmaceuticals Ltd., Merck Sharp & Dohme Corp.Inventors: Merck Sharp & Dohme Corp., Neuromed Pharmaceuticals Ltd.
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Publication number: 20130035484Abstract: A compound of formula (I): which is substantially free of any of the corresponding compound of formula (IB): methods of making such compounds, and the further transformation of such compounds.Type: ApplicationFiled: April 15, 2011Publication date: February 7, 2013Applicant: SPIROGEN DEVELOPMENTS SÀRLInventors: Philip Wilson Howard, Luke Masterson, Arnaud Tiberghien
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Publication number: 20120289710Abstract: The invention relates to a new process for producing useful intermediates for the manufacture of NEP inhibitors or prodrugs thereof, in particular NEP inhibitors comprising a g-amino-d-biphenyl-a-methylalkanoic acid, or acid ester, backbone, such as N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: January 21, 2011Publication date: November 15, 2012Inventors: David Hook, Jianguang Zhou, Yunzhong Li
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Publication number: 20120220564Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
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Publication number: 20120214858Abstract: Imidamide (amidine) analogs that can inhibit the activity of sphingosine kinase 1 and sphingosine kinase 2 (SphK1 & SphK2) are provided. The compounds can prevent angiogenesis in tumors.Type: ApplicationFiled: August 16, 2010Publication date: August 23, 2012Applicant: University of Virginia Patent FoundationInventors: Kevin R. Lynch, Timothy L. Macdonald, Thomas P. Mathews, Andrew Kennedy, Yugesh Kharel
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Publication number: 20120190700Abstract: The present invention provides compounds of formula or pharmaceutically acceptable salts, esters or stereoisomers thereof, wherein R1 to R4, A and Y have the meanings given herein, as well as methods for making those compounds and their use as medicament, in particular as medicament for the treatment of cancer.Type: ApplicationFiled: January 17, 2012Publication date: July 26, 2012Inventors: Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Jason Christopher Wong, Zhenshan Zhang
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Publication number: 20120190820Abstract: Provided are methods for forming a reactive S-nitroso thioacid (NTA), comprising nitrosation of a thioacid with a nitrosation reagent. Also provided are methods for: acylating a nucleophile including selective acylation with a high degree of selectivity toward amines over hydroxyls; amide or peptide bond formation; forming a dipeptide or polypeptide; and peptide coupling/ligation, comprising use of thioacid and amine starting materials, wherein the reactions are mediated by very reactive S-nitroso thioacid (NTA) intermediates enabling extremely fast reactions under mild conditions, providing for broad applications.Type: ApplicationFiled: January 26, 2012Publication date: July 26, 2012Inventors: Ming Xian, Jia Pan
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Publication number: 20120184438Abstract: This invention relates to agrochemical compositions comprising a benzamide compound of formula (I) where R1 is fluoro, methoxy or C1-4 alkyl; R2 and R3 are each independently optionally substituted C1-6 alkyl or optionally substituted C2-6 alkenyl; or R3 is hydrogen and R3 is optionally substituted C5-8 alkyl or optionally substituted C4-6 alkenyl or optionally substituted benzyl; or R2 and R3 and the nitrogen atom to which they are both attached together form an optionally substituted 5-, 6- or 7-membered ring, which ring optionally contains at least one further heteroatom selected from O, N and S; to the use of those benzamide compounds as solvents; to certain novel compounds of formula (I); and to a process for preparing those novel compounds.Type: ApplicationFiled: July 15, 2010Publication date: July 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Gordon Alistair Bell, David Stock, Jeffrey Steven Wailes
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Publication number: 20120178732Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: ApplicationFiled: December 6, 2011Publication date: July 12, 2012Inventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20120178761Abstract: The invention provides compounds of formula wherein R1, R2, R3, R4, R5, and R6 are as defined herein or a pharmaceutically suitable acid addition salt thereof. The present compounds are high potential NK-3 receptor antagonists useful for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: January 2, 2012Publication date: July 12, 2012Inventors: Henner Knust, Matthias Nettekoven, Hasane Ratni, Walter Vifian
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Publication number: 20120142916Abstract: The present invention relates to pyrrolidin-2-ones according to the formula (1), or salts thereof, wherein R1 is hydrogen or a nitrogen protecting group, methods for their preparation and their use in the preparation of NEP-inhibitors, particularly in the preparation of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-(2R)-methyl butanoic acid ethyl ester or salt thereof.Type: ApplicationFiled: December 21, 2011Publication date: June 7, 2012Inventors: David Hook, Thomas Ruch, Bernhard Riss, Bernhard Wietfeld, Gottfried Sedelmeier, Matthias Napp, Markus Bänziger, Steven Hawker, Lech Ciszewski, Liladhar Murtidhar Waykole
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Patent number: 8163727Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.Type: GrantFiled: December 18, 2009Date of Patent: April 24, 2012Assignee: AstraZeneca ABInventors: Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
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Publication number: 20120077959Abstract: Cobalt(II) complexes of the D2-symmetric chiral porphyrins are effective catalysts for asymmetric cyclopropanation reactions with succinimidyl diazoacetate. The Co-catalyzed reaction is suitable for various olefins, providing the corresponding cyclopropane succinimidyl esters in high yields and excellent diastereo- and enantio-selectivity.Type: ApplicationFiled: February 16, 2010Publication date: March 29, 2012Inventors: X. Peter Zhang, Joshua V. Ruppel
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Publication number: 20120071651Abstract: The present invention relates to processes for preparing enantiomerically pure cyclopropyl amine derivatives and salts thereof; the chiral intermediates such as the chiral salts are useful for the preparation of such chiral compounds and salts; pharmaceutical compositions comprising the compounds and salts; and method of using such compositions. The chiral cyclopropyl amine derivatives are useful for binding to histamine H3 receptor sites and for providing therapeutic agents for histamine H3 mediated disease.Type: ApplicationFiled: September 14, 2011Publication date: March 22, 2012Applicant: ABBOTT LABORATORIESInventors: Yi-Yin Ku, Timothy A. Grieme, Jeffrey M. Kallemeyn, Mathew M. Mulhern
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Publication number: 20120065225Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: ApplicationFiled: November 21, 2011Publication date: March 15, 2012Inventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
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Publication number: 20120053200Abstract: The present invention relates to N-1-Benzyl-2-hydroxy-3-(hetero)arylamino-propyl)-isophthalamides of formula I having BACE2 inhibitory activity and their use as therapeutically active substances, their manufacture and pharmaceutical compositions. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. type 2 diabetes.Type: ApplicationFiled: August 23, 2011Publication date: March 1, 2012Inventors: Harald Mauser, Matthias Nettekoven, Sébastien Schmitt
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Publication number: 20120015928Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.Type: ApplicationFiled: September 23, 2011Publication date: January 19, 2012Applicant: INCYTE CORPORATIONInventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang
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Publication number: 20120010264Abstract: The present invention provides a medicament for preventing and/or treating cognitive impairment, in particular Alzheimer's dementia, comprising 2-methyl-2-[(4-{(1E)-3-[2-(4-methylbenzoyl)-1H-pyrrol-1-yl]prop-1-en-1-yl}benzyl)oxy]propionic acid or a pharmaceutically acceptable salt or solvate thereof.Type: ApplicationFiled: March 26, 2010Publication date: January 12, 2012Applicant: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Hiroyoshi Kakuyama, Keiko Sakoda, Yoshihiro Iwamura, Atsushi Ikeda, Atsushi Tsuchida
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Patent number: 8084623Abstract: Compounds of the formula: or pharmaceutically acceptable salts thereof, wherein m, n, Ar, R1, R2, Ra and Rb are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.Type: GrantFiled: December 18, 2007Date of Patent: December 27, 2011Assignee: Roche Palo Alto LLCInventors: Pravin Iyer, Clara Jeou Jen Lin, Stephen M. Lynch, Matthew C. Lucas, Ann Marie Madera, Kerem Erol Ozboya, Robert James Weikert, Ryan Craig Schoenfeld
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Publication number: 20110306775Abstract: Disclosed are a serious of 2?,5?-dimethoxychalcone derivatives for treating cancer, wherein 2,5-dimethoxyacetophenone and methyl 4-formylbenzoate are condensed to form 4-carboxyl-2?,5?-dimethoxychalcone (compound 1), which is further reacted with alkyl halides or amines to synthesize the chalcone derivatives of compounds 2-17. In addition, 2,5-dimethoxyacetophenone is reacted with 5-formyl-2-thiophenecarboxylic acid to form compound 18 (3-(3-thiophene)carboxyl-1-(2,5-dimethoxyphenyl)prop-2-en-1-one). The synthesized 2?,5?-dimethoxychalcone derivatives can be acted as microtubule-targeted tubulin-polymerizing agents.Type: ApplicationFiled: October 1, 2010Publication date: December 15, 2011Applicant: KAOHSIUNG MEDICAL UNIVERSITYInventors: Chun-Nan Lin, Huang-Yao Tu, A-Mei Huang, Tzyh-Chyuan Hoar, Shyh-Chyun Yang, Yeong-Shiau Pu, Jan-Gowth Chang
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Patent number: 8063075Abstract: The present invention relates to compounds of formula I wherein R1, R2, R3, R?, Ar, m, n, and o are as defined herein. The invention also relates to pharmaceutical compositions containing compounds of formula I and methods for the manufacture of such compounds and compositions. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: GrantFiled: June 2, 2009Date of Patent: November 22, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Philippe Jablonski, Kenichi Kawasaki, Henner Knust, Anja Limberg, Matthias Nettekoven, Hasane Ratni, Claus Riemer
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Patent number: 8058455Abstract: A compound having a structure expressed by the following Structural Formula (1) and a compound having a structure expressed by the following Structural Formula (2):Type: GrantFiled: February 23, 2011Date of Patent: November 15, 2011Assignee: Kinki UniversityInventors: Masayuki Igarashi, Ryutaro Utsumi
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Publication number: 20110263674Abstract: Active compounds of Formula I are described: wherein: R1 and R2 are each independently C1-C4 alkyl; or R1 and R2 together form a C2-C7 alkylene chain; and Z is a non-steroidal anti-inflammatory drug (NSAID); along with pharmaceutically acceptable salts and prodrug thereof, and methods of using the same.Type: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Inventor: S. Bruce King
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Publication number: 20110263428Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: July 1, 2009Publication date: October 27, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephane Andre Marie Jeanmart, Russell Colin Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Mangala Govenkar, Matthew Robert Cordingley, Claire Janet Russell, Melloney Tyte