Carbonyl Or Thiocarbonyl Bonded Directly To The Nitrogen Patents (Class 548/163)
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Patent number: 10227315Abstract: The present disclosure relates to benzamide compounds, prodrugs of the compounds, pharmaceutical compositions containing the compounds and/or the prodrugs and methods of using the compounds, prodrugs and pharmaceutical compositions in the treatment of diseases related to lipid metabolism including diabetes, Non-Alcholic Fatty Liver Disease (NAFLD), Non-Alcholic Steathohepatitis (NASH), diseases caused by abnormal cell proliferation including cancer, psoriasis, and infectious diseases.Type: GrantFiled: May 18, 2017Date of Patent: March 12, 2019Assignee: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Shengkan Jin, David J. Augeri, Bin Cao, Hanlin Tao
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Patent number: 9012481Abstract: Novel benzoarylureido compounds and a use thereof for prevention and/or treatment of the neurodegenerative brain disease are provided. The neurodegenerative brain diseases may include Alzheimer's disease, dementia, Parkinson's disease, stroke, amyloidosis, Pick's disease, Lou Gehrig's disease, Huntington's disease, Creutzfeld-Jakob disease, and the like.Type: GrantFiled: December 29, 2009Date of Patent: April 21, 2015Assignee: Korea Institute of Science and TechnologyInventors: Hoh-Gyu Hahn, Kee-Dal Nam, Dong-Yun Shin, Chan-Ho Park, Sung-Woo Cho, Eun-A Kim, Ghil-Soo Nam, Kyung-Il Chol, Seon-Hee Seo, Hee-Sup Shin, Dong-Jin Kim, Ae-Nim Pae, Hye-Jin Chung, Hyun-Ah Choo, Hye-Whon Rhim, Yong-Seo Cho, Eun-Joo Roh, Gyo-Chang Keum, Kee-Hyun Choi, Kye-Jung Shin, Chan-Seong Cheong, Jae-Kyun Lee, Yong-Koo Kang, Young-Soo Kim, Woong-Seo Park, Key-Sun Kim, He-Sson Chung, Chi-Man Song, Sun-Joon Min, Eunice Eun-Kyeong Kim, Cheol-Ju Lee, Soon-Bang Kang
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Publication number: 20150105337Abstract: The present invention provides novel enterobactin-cargo conjugates, such as compounds of Formula (I), and salts thereof, where X is the cargo and may be an antibiotic, a fluorophore, or biotin. The present invention also provides complexes, compositions, kits, and methods that involve the compounds of Formula (I) and are useful in delivering a cargo to a bacterium, treating a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, preventing a bacterial infection, cystic fibrosis, and/or inflammatory bowel disease in a subject, inhibiting the growth of or killing a bacterium, or determining the concentration of a bacterium in a biological sample. In certain embodiments, the bacterium is a Gram-negative bacterium.Type: ApplicationFiled: October 16, 2014Publication date: April 16, 2015Applicant: MASSACHUSETTS INSTITUTE OF TECHNOLOGYInventors: Elizabeth Marie Nolan, Tengfei Zheng, Phoom Chairatana
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Publication number: 20150087646Abstract: The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.Type: ApplicationFiled: June 10, 2013Publication date: March 26, 2015Applicant: GLENMARK PHARMACEUTICALS S.A.Inventors: Laxmikant Atmaram Gharat, Nagarajan Muthukaman, Neelima Khairatkar-Joshi, Vidya Ganapati Kattige
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Publication number: 20150045393Abstract: The invention provides for novel cysteine protease inhibitors and compositions comprising novel cysteine protease derivatives. The invention further provides for methods for treatment of neurodegenerative diseases comprising administration novel cysteine protease inhibitors or compositions comprising novel cysteine protease inhibitors. In some embodiments, the cysteine protease inhibitors are calpain inhibitors.Type: ApplicationFiled: February 1, 2013Publication date: February 12, 2015Inventors: Greg R. Thatcher, Isaac Thomas Schiefer, Ottavio Arancio, Mauro Fa
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Patent number: 8951999Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: GrantFiled: October 20, 2010Date of Patent: February 10, 2015Assignee: Orexo ABInventors: Henning Priepke, Henri Doods, Raimund Kuelzer, Roland Pfau, Dirk Stenkamp, Robert Roenn, Benjamin Pelcman
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Publication number: 20150017718Abstract: The present invention relates to a method for inducing cardiac differentiation of a pluripotent stem cell, which comprises the steps of (1) culturing a pluripotent stem cell in a medium containing one or more WNT signaling activators, and (2) culturing a cell produced in the step (1) in a medium containing one or more WNT signaling inhibitor.Type: ApplicationFiled: January 25, 2013Publication date: January 15, 2015Inventors: Norio Nakatsuji, Itsunari Minami, Motonari Uesugi, Kazuhiro Aiba
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Publication number: 20150011528Abstract: Provided is a phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt can selectively inhibit the protein-protein interaction between KRS and a laminin receptor (LR), thereby inhibiting migration of cancer cells. Therefore, the phenylimide-containing benzothiazole derivative or its pharmaceutically acceptable salt may be usefully applied for preventing or treating the diseases associated with cancer cell metastasis.Type: ApplicationFiled: September 21, 2012Publication date: January 8, 2015Applicant: YUHAN CORPORATIONInventors: Youn Hur, Dong-Hyun Kim, Eun-Kyung Kim, Jin-Hwi Park, Jae-Eun Joo, Ho-Woong Kang, Se-Woong Oh, Dong-Kyun Kim, Kyoung-Kyu Ahn
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Patent number: 8927551Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: GrantFiled: May 18, 2010Date of Patent: January 6, 2015Assignee: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 8865752Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.Type: GrantFiled: July 4, 2013Date of Patent: October 21, 2014Assignee: Angion Biomedica Corp.Inventors: Bijoy Panicker, Dong Sung Lim, Rama K. Mishra, Lambertus J. W. M. Oehlen, James G. Tarrant, Xiaokang Zhu, Dawoon Jung
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Publication number: 20140296257Abstract: The present invention relates to water-soluble carrier-linked prodrugs of formula (I), wherein B, A and Hyp form the carrier, B is a branching core, each A is independently a poly(ethylene glycol)-based polymeric chain, each Hyp is independently a branched moiety, each SP is independently a spacer moiety, each L is independently a reversible prodrug linker moiety, each D is independently a biologically active moiety, each x is independently 0 or 1, each m is independently an integer of from 2 to 64, n is an integer from 3 to 32; or the pharmaceutically acceptable salt thereof. It further relates to pharmaceutical compositions comprising said water-soluble carrier-linked prodrugs, their use as medicament or diagnostic, and methods of treatment.Type: ApplicationFiled: August 10, 2012Publication date: October 2, 2014Applicant: Ascendis Pharma A/SInventors: Ulrich Hersel, Guillaume Maitro, Harald Rau, Dirk Vetter
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Publication number: 20140221657Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.Type: ApplicationFiled: April 7, 2014Publication date: August 7, 2014Applicant: PRISM BioLab CorporationInventors: Hiroyuki Kouji, Yuji Kogami, Takenao Odagami
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Publication number: 20140171438Abstract: The present disclosure provides compounds, or pharmaceutically acceptable salts thereof, for inhibiting the growth of a microbe; treating a mammal having a microbial infection, malaria, mucositis, an ophthalmic infection, an otic infection, a cancer, or a Mycobacterium infection; killing or inhibiting the growth of a Plasmodium species; inhibiting the growth of a Mycobacterium species; modulating an immune response in a mammal; or antagonizing unfractionated heparin, low molecular weight heparin, or a heparin/low molecular weight heparin derivative.Type: ApplicationFiled: December 9, 2013Publication date: June 19, 2014Applicant: CELLCEUTIX CORPORATIONInventors: Wenxi Pan, Haizhong Tang
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Publication number: 20140127737Abstract: The present invention relates to a two-photon fluorescent probe, more particularly a two-photon fluorescent probe represented by Formula 1, a method for preparing same and a method for imaging thiols in mitochondria using same. The two-photon fluorescent probe according to the present invention, having two probes introduced in one molecule, can selectively dye mitochondria and emit intense fluorescence by reacting with thiols. Accordingly, it can be used to image the distribution and activation of thiols in a living cell or an intact living tissue.Type: ApplicationFiled: October 17, 2011Publication date: May 8, 2014Applicant: AJOU UNIVERSITY INDUSTRY-ACADEMIC COOPERTION FOUNDInventor: Hwan Myung Kim
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Publication number: 20140127807Abstract: The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cellsType: ApplicationFiled: January 14, 2014Publication date: May 8, 2014Applicant: KYOTO UNIVERSITYInventors: Norio Nakatsuji, Motonari Uesugi, Kouhei Yamada, Itsunari Minami, Tomomi Otsuji, Shinya Otsuka
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Patent number: 8703962Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: October 22, 2009Date of Patent: April 22, 2014Assignee: Purdue Pharma L.P.Inventors: Donald J. Kyle, Laykea Tafesse
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Patent number: 8658425Abstract: The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cells.Type: GrantFiled: February 26, 2013Date of Patent: February 25, 2014Assignee: Kyoto UniversityInventors: Norio Nakatsuji, Motonari Uesugi, Kouhei Yamada, Itsunari Minami, Tomomi Otsuji
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Publication number: 20140005189Abstract: The disclosure relates to compounds of formula (I): wherein , A, W, X, and Ra are as defined in the disclosure, and salts thereof, and to pharmaceutical compositions comprising said compounds, to processes for preparing them, and to their use as medicaments, in particular as MET inhibitors.Type: ApplicationFiled: August 27, 2013Publication date: January 2, 2014Applicant: SANOFIInventors: Eva Albert, Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler
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Publication number: 20140005190Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: June 27, 2013Publication date: January 2, 2014Applicants: Genentech, Inc., The Walter and Eliza Hall Institute of Medical Research, AbbVie Inc.Inventors: JONATHAN BAYLDON BAELL, CHINH THIEN BUI, PETER COLMAN, DANETTE A. DUDLEY, WAYNE J. FAIRBROTHER, JOHN A. FLYGARE, GUILLAUME LAURENT LESSENE, CHUDI NDUBAKU, GEORGE NIKOLAKOPOULOS, CARL STEVEN RYE, BRAD EDMUND SLEEBS, BRIAN JOHN SMITH, KEITH GEOFFREY WATSON, STEVEN W. ELMORE, ANDREW M. PETROS, ANDREW J. SOUERS, PETER CZABOTAR
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Publication number: 20130317231Abstract: The present invention provides a compound of general formulae A useful as potential anti-cancer agents against human cancer cell lines and a process for the preparation thereof.Type: ApplicationFiled: August 2, 2013Publication date: November 28, 2013Inventors: Kamal Ahmed, Adla Malla Reddy, Suresh Paidakula, Neigapula Sankara Rao, Rajesh V. C. R. N. C. Shetti
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Patent number: 8546563Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: October 30, 2008Date of Patent: October 1, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
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Patent number: 8513291Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.Type: GrantFiled: June 1, 2011Date of Patent: August 20, 2013Assignee: Angion Biomedica Corp.Inventors: Bijoy Panicker, Lambertus J. W. M. Oehlen, James G. Tarrant, Dong Sung Lim, Xiaokang Zhu, Dawoon Jung, Rama K. Mishra
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Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
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Patent number: 8497274Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.Type: GrantFiled: January 10, 2012Date of Patent: July 30, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Masanori Okaniwa, Terufumi Takagi, Masaaki Hirose
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Publication number: 20130183753Abstract: The present invention relates to a composition for promoting differentiation of pluripotent stem cells into cardiac muscle cells, and a method for inducing differentiation of pluripotent stem cells into cardiac muscle cells and a method for preparing cardiac muscle cells.Type: ApplicationFiled: February 26, 2013Publication date: July 18, 2013Applicant: KYOTO UNIVERSITYInventor: Kyoto University
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Patent number: 8470829Abstract: An imidazole derivative represented by formula (I): wherein Q is: A is hydrogen, halogen, or a substituted or unsubstituted C1-4 alkyl group; E is independently selected from a C1-6 alkyl group; R2 and R3 are independently selected from C1-6 alkyls; X1 and X2 are independently selected from O and S; Y is selected from a substituted or unsubstituted arylene group and a substituted or unsubstituted divalent 5- or 6-membered monocyclic or 8- to 10-membered condensed heterocyclic group; Z is —CON(—Ra)—, —CO—, —OOO—, —NRa—C(?NH)NRb—, —NRa—C(?N—CN)NRb—, —N(—Ra)COO—, —C(?NH)—, —SO2—, —SO2N(—Ra)—, —SO2NR1—, —N(—Ra)CO—, —N(—Ra)CON(—Rb)—, —N(COR1)CO—, —N(—Ra)SO2—, —N(SO2R1)SO2—, —N(—Ra)— or —N(—Ra)SO2N(—Rb)—; R1 is independently a hydrogen atom, a hydroxyl group, or substituted or unsubstituted group selected from C1-6 alkyl group, heterocyclic group, aryl group, C3-8 cycloalkyl group and C3-8 cycloalkenyl group; or salt or prodrug thereof.Type: GrantFiled: September 9, 2005Date of Patent: June 25, 2013Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Kazutaka Tachibana, Haruhiko Sato, Masateru Ohta, Mitsuaki Nakamura, Takuya Shiraishi, Hitoshi Yoshino, Takashi Emura, Akie Honma, Etsuro Onuma, Hiromitsu Kawata, Kenji Taniguchi
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Publication number: 20130102643Abstract: The present invention provides compounds having the general structural formula (I) and pharmaceutically acceptable derivatives thereof, as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof for the treatment of any of a number of conditions or diseases involving fibrosis and proliferation, and where anti-fibrotic or anti-proliferative activity is beneficial.Type: ApplicationFiled: June 1, 2011Publication date: April 25, 2013Inventors: Bijoy Panicker, Lambertus J.W.M. Oehlen, James G. Tarrant, Dong Sung Lim, Xiaokang Zhu, Dawoon Jung, Rama K. Mishra
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Patent number: 8394842Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings,! of the general formula (1): having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: GrantFiled: March 22, 2007Date of Patent: March 12, 2013Assignee: High Point Pharmaceuticals, LLCInventors: Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Knud Erik Andersen
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Patent number: 8324395Abstract: Provided is a heterocyclic compound showing strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.Type: GrantFiled: August 22, 2008Date of Patent: December 4, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Masanori Okaniwa, Takashi Imada
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Publication number: 20120283300Abstract: This application relates to a novel benzo-heterocycle derivative and more particularly, it relates a composition for preventing and treating cancer or for inhibiting metastasis comprising benzo-heterocycle derivative or pharmaceutically acceptable salts thereof as an active ingredient. The present inventors confirmed that KRS has an effect on cancer metastasis by facilitating cancer (or tumor) cell migration through interaction with 67LR, and also found that a substance inhibiting the interaction between KRS and 67LR can prevent and treat cancer by inhibiting cancer cell metastasis. Accordingly, the composition of the present invention can inhibit cancer metastasis, and thus provide a novel means for prevention and treatment of cancer.Type: ApplicationFiled: May 7, 2012Publication date: November 8, 2012Applicant: SNU R&DB FOUNDATIONInventors: Sunghoon Kim, Jin Woo Choi, Jin Young Lee, Dae Gyu Kim, Gyoon Hee Han, Jee Sun Yang, Chul Ho Lee
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Publication number: 20120270868Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to 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: October 17, 2011Publication date: October 25, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Thomas Martin KIRRANE, Daniel Richard MARSHALL, Robert SIBLEY, Roger John SNOW, Fariba SOLEYMANZADEH, Ronald John SORCEK
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Patent number: 8293774Abstract: The present invention relates to an optically active (R)-aryloxypropionic acid amide compound which has high selectivity and safety for protecting a crop such as rice, wheat, barley and soy bean, and exhibits excellent herbicidal activity against weeds, and a herbicidal composition comprising the same.Type: GrantFiled: July 2, 2008Date of Patent: October 23, 2012Assignee: Kyung Nong CorporationInventors: Joo-kyung Kim, Dong-hoo Kim, Hyung-ho Kim, Kyung-hyun Kim, Cheol-su Yoon, In-cheon Hwang
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Publication number: 20120214808Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Prosidion LimitedInventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
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Publication number: 20120191039Abstract: The present invention relates to a carrier linked pramipexole prodrug or a pharmaceutical acceptable salt thereof, wherein pramipexole is bound via a linker to a polymeric carrier. The invention also relates to pharmaceutical compositions comprising said polymeric pramipexole prodrug and their use as medicaments.Type: ApplicationFiled: July 30, 2010Publication date: July 26, 2012Applicant: ASCENDIS PHARMA A/SInventors: Harald Rau, Julia Baron, Ulrich Hersel
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Publication number: 20120178752Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and X are as defined herein. The invention also relates to 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: June 29, 2011Publication date: July 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: John David GINN, Daniel Richard MARSHALL, Robert SIBLEY, Ronald John SORCEK, Erick Richard Roush YOUNG, Yunlong ZHANG
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Publication number: 20120165326Abstract: The invention relates to novel products of the formula (I) where: (II) is a single or double bond; F is a fluorine atom, Ra is H, HaI, alkoxy, O-cycloalkyl, —O— heterocycloalkyl; —NH-heterocycloalkyl, heteroaryl, phenyl, NHCOalk NHCOcycloalk or NR1 R2; X is S, SO or SO2, A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl optionally substituted by NR3R4, alkoxy, hydroxy, phenyl, heteroaryl or heterocycloalkyl; alkoxy optionally substituted by NR3R4, i.e. a O—(CH2)n-NR3R4 radical, an O-phenyl or an O—(CH2)n-phenyl radical, with phenyl optionally substituted and n=1 to 4; or the NR1 R2 radical; R1 is H or alk and R2 is H, cycloalkyl or alkyl; R3 and R4 are H, alk, cycloalkyl, heteroaryl or phenyl; R1, R2 and/or R3, R4 form a cycle together with N optionally containing O, S, N and/or NH; heterocycloalkyl, heteroaryl and phenyl and cycles all being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors.Type: ApplicationFiled: February 4, 2010Publication date: June 28, 2012Applicant: SANOFIInventors: Conception Nemecek, Antonio Ugolini, Eric Bacque, Dominique Damour, Gilles Barbalat, Sylvie Wentzler
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Publication number: 20120165322Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein. The invention also relates to 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: June 29, 2011Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Brian Nicholas Cook, Jennifer A. Kowalski, Xiang Li, Daniel Richard Marshall, Sabine Schlyer, Robert Sibley, Lana Louise Smith-Keenan, Fariba Soleymanzadeh, Ronald John Sorcek, Erick Richard Roush Young, Yunlong Zhang
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Patent number: 8207349Abstract: The present invention encompasses compounds of the general formula (1) in which R1 to R3 are defined as in claim 1, which are suitable for treating diseases which are characterized by excessive or anomalous cell proliferation, and their use for producing a pharmaceutical having the abovementioned properties.Type: GrantFiled: January 11, 2010Date of Patent: June 26, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Bodo Betzemeier, Trixi Brandl, Steffen Breitfelder, Ralph Brueckner, Thomas Gerstberger, Michael Gmachl, Matthias Grauert, Frank Hilberg, Christoph Hoenke, Matthias Hoffmann, Maria Impagnatiello, Dirk Kessler, Christian Klein, Bernd Krist, Udo Maier, Darryl McConnell, Charlotte Reither, Stefan Scheuerer, Andreas Schoop, Norbert Schweifer, Oliver Simon, Martin Steegmaier, Steffen Steurer, Irene Waizenegger, Ulrike Weyer-Czernilofsky, Andreas Zoephel
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Publication number: 20120156260Abstract: The present invention relates to a prodrug or a pharmaceutically acceptable salt thereof comprising a drug linker conjugate D-L, wherein an aromatic amine containing biologically active moiety is connected (bound) by an amido bound to a linker. The invention also relates to pharmaceutical compositions comprising said prodrugs and their use as medicaments.Type: ApplicationFiled: July 30, 2010Publication date: June 21, 2012Applicant: ASCENDIS PHARMA A/SInventors: Harald Rau, Julia Baron, Ulrich Hersel, Mathias Krusch
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Publication number: 20120142666Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: June 8, 2010Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
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Publication number: 20120115845Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: November 7, 2011Publication date: May 10, 2012Inventors: Jack McQueen ALLEN, Roger John Butlin, Clive Green, William McCoull, Graeme Richard Robb, James Matthew Wood
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Publication number: 20120115903Abstract: Substituted heteroaromatic carboxamide and urea compounds corresponding to formula (i) processes for the preparation thereof, pharmaceutical compositions containing these compounds and also a method of using these compounds in pharmaceutical compositions for treating or inhibiting pain and other conditions mediated at least in part via the vanilloid receptor 1.Type: ApplicationFiled: November 9, 2011Publication date: May 10, 2012Applicant: Gruenenthal GmbHInventors: Robert Frank, Thomas Christoph, Bernhard Lesch, Jeewoo Lee
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Publication number: 20120095021Abstract: The present disclosure provides a compound of general formula A useful as potential anti-tubercular agents.Type: ApplicationFiled: September 14, 2011Publication date: April 19, 2012Inventors: Ahmed Kamal, Rajesh VCRNC Shetti, P. Swapna, Shaik Azeeza, A. Malla Reddy, Inshad Ali Khan, Sheikh Tasduq Abdullah, Sandeep Sharma, Nitin Pal Kalia
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Patent number: 8143258Abstract: Provided is a fused heterocycle derivative showing a strong Raf inhibitory activity. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.Type: GrantFiled: December 1, 2009Date of Patent: March 27, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Masanori Okaniwa, Terufumi Takagi, Masaaki Hirose
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Publication number: 20120071475Abstract: Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: April 26, 2010Publication date: March 22, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Daisuke Taniyama, Yasunori Mitsuoka, Kayoko Hata
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Publication number: 20120046250Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: March 2, 2010Publication date: February 23, 2012Applicant: STEMSYNERGY THERAPEUTICS, INCInventor: Darren Orton
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Publication number: 20120040987Abstract: The invention relates to novel products of the formula (I) where: (II) is a single or double bond; Rb is a hydrogen or fluorine atom; Ra is a NH-Rc radical in which Rc is an optionally substituted heterocycloalkyl, aryl, heteroaryl or -alkylcycloalkyl radical; X is S, SO, or SO2; A is NH or S; W is H, alkyl, or COR with R being cycloalkyl; alkyl; alkoxy; O-phenyl; —O— (CH2)n-phenyl with n=1 to 4; or NR1R2 with R1 being H or alk and R2 is H, cycloalkyl or alkyl; or R1, R2 form a cycle together with N optionally containing O, S, N and/or NH; all of said radicals being optionally substituted; wherein said products can be in any isomer or salt form, and can be used as drugs, in particular as MET inhibitors.Type: ApplicationFiled: February 4, 2010Publication date: February 16, 2012Applicant: SANOFIInventors: Eric Bacque, Conception Nemecek, Antonio Ugolini, Sylvie Wentzler
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Publication number: 20120020881Abstract: This invention relates to novel compounds suitable for labeling by positron emitting isotopes, such as 18F, 11C, 13N and 15O, through appropriate labeling reagents, such as 18F reagents and methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).Type: ApplicationFiled: December 4, 2009Publication date: January 26, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Lutz Lehmann, Timo Stellfeld, Keith Graham, Jessica Becaud, Linjing Mu
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Patent number: 8097758Abstract: The invention relates to the compounds of formula (I) having antithrombotic activity which especially inhibit blood clotting factor IXa, to methods for producing the same and to the use thereof as drugs.Type: GrantFiled: March 9, 2009Date of Patent: January 17, 2012Assignee: Sanofi-AventisInventors: Henning Steinhagen, Markus Follmann, Jochen Goerlitzer, Herman Schreuder