At Least Three Ring Hetero Atoms In The Polycyclo Ring System Patents (Class 548/242)
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Patent number: 11708355Abstract: Provided are novel organic molecules containing fused indole and benzimidazole moieties, or their boron containing analogs. Also provided are OLEDs and related consumer products that utilize these compounds containing the fused indole and benzimidazole moieties.Type: GrantFiled: July 15, 2020Date of Patent: July 25, 2023Assignee: UNIVERSAL DISPLAY CORPORATIONInventors: Tyler Fleetham, Peter Wolohan, Hsiao-Fan Chen
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Patent number: 11332478Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.Type: GrantFiled: March 24, 2020Date of Patent: May 17, 2022Assignee: H. Lundbeck A/SInventors: Carla De Faveri, Florian Anton Martin Huber
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Patent number: 8962858Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.Type: GrantFiled: June 26, 2014Date of Patent: February 24, 2015Assignee: Eisai R&D Management Co., Ltd.Inventors: Branko Mitasev, Dae-Shik Kim, Huiming Zhang, Christopher N. Farthing
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Patent number: 8927560Abstract: The present invention provides 4-Aza-2,3-didehydropodophyllotoxin compound of general formula A (4a-4z and 4aa-4ae) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4-Aza-2,3-didehydropodophyllotoxin compounds (4a-4z and 4aa-4ae).Type: GrantFiled: March 25, 2011Date of Patent: January 6, 2015Assignee: Council of Scientific & Industrial ResearchInventors: Kamal Ahmed, Suresh Paidakula, Ashwini Kumar Banala, Mallareddy Adla, Venkat Reddy Papagari, Rasheed Tamboli Jaki
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Publication number: 20140309429Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.Type: ApplicationFiled: June 26, 2014Publication date: October 16, 2014Inventors: Branko Mitasev, Dae-Shik Kim, Huiming Zhang, Christopher N. Farthing
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Patent number: 8772307Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.Type: GrantFiled: May 17, 2006Date of Patent: July 8, 2014Assignee: Gruenenthal GmbHInventors: Robert Frank, Melanie Reich, Ruth Jostock, Gregor Bahrenberg, Hans Schick, Birgitta Henkel, Helmut Sonnenschein
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Publication number: 20140163238Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.Type: ApplicationFiled: October 25, 2013Publication date: June 12, 2014Applicant: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Mark G. Charest, Christian D. Lerner, Jason D. Brubaker, Dionicio R. Siegel
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Patent number: 8592498Abstract: Disclosed herein are a reaction method and a production method of an organic compound which are capable of achieving high reaction selectivity according to the purpose and a high production rate of a target substance. The methods include at least two fluids, wherein at least one kind of the fluids is a fluid containing at least one organic compound and at least one kind of the fluids other than the above fluid is a fluid containing at least one reactant in the form of a liquid or solution, and the respective fluids join together in a thin film fluid foamed between processing surfaces arranged to be opposite to each other so as to be able to approach to and separate from each other, at least one of which rotates relative to the other, whereby an organic reaction is performed in the thin film fluid.Type: GrantFiled: September 11, 2008Date of Patent: November 26, 2013Assignee: M. Technique Co., Ltd.Inventor: Masakazu Enomura
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Patent number: 8580956Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: GrantFiled: May 28, 2008Date of Patent: November 12, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Zhaoning Zhu, William J. Greenlee, Zhong-Yue Sun, Gioconda Gallo, Ruo Xu, Xianhai Huang, Xiaohong Zhu
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Publication number: 20130252962Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: March 6, 2013Publication date: September 26, 2013Inventors: Mikhail CHAFEEV, Sultan CHOWDHURY, Lauren FRASER, Jianmin FU, Jonathan LANGILLE, Shifeng LIU, Jianyu SUN, Shaoyi SUN, Serguei SVIRIDOV, Mark WOOD, Alla Yurevna ZENOVA, Qi JIA, Jean-Jacques Alexandre CADIEUX, Simon J. GAUTHIER, Amy Frances DOUGLAS, Tom HSIEH, Nagasree CHAKKA, Zoran CIKOJEVIC
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Patent number: 8426584Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.Type: GrantFiled: January 20, 2012Date of Patent: April 23, 2013Assignee: Eisai R&D Management Co., Ltd.Inventors: Branko Mitasev, Dae-Shik Kim, Kazuhiro Yoshizawa
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20120214767Abstract: Disclosed are compounds of Formula (I) or stereoisomers or salts thereof, wherein: X1, X2, X3, W, Q1, Q2, and G2 are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: October 29, 2010Publication date: August 23, 2012Inventors: T.G. Murali Dhar, Hai-Yun Xiao, Scott Hunter Watterson, Soo S. Ko, Alaric J. Dyckman, Charles M. Langevine, Jagabandhu Das
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Publication number: 20120190848Abstract: Provided are compounds and methods useful for the preparation of compounds useful as inhibitors of beta-site amyloid precursor protein (APP)-cleaving enzyme.Type: ApplicationFiled: January 20, 2012Publication date: July 26, 2012Inventors: Branko Mitasev, Dae-Shik Kim, Huiming Zhang, Matthew J. Schnaderbeck, Christopher N. Farthing, Kazuhiro Yoshizawa
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Publication number: 20110213145Abstract: The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer.Type: ApplicationFiled: April 19, 2011Publication date: September 1, 2011Applicant: Infinity Discovery, Inc.Inventors: Alfredo C. Castro, Kristopher M. Depew, Michael J. Grogan, Charles W. Johannes, Edward B. Holson, Brian T. Hopkins, Gregg F. Keaney, Nii O. Koney, Tao Liu, David A. Mann, Marta Nevalainen, Stephane Peluso, Lawrence B. Perez, Daniel A. Snyder, Thomas T. Tibbitts
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Publication number: 20110178199Abstract: Disclosed herein are a reaction method and a production method of an organic compound which are capable of achieving high reaction selectivity according to the purpose and a high production rate of a target substance. The methods include at least two fluids, wherein at least one kind of the fluids is a fluid containing at least one organic compound and at least one kind of the fluids other than the above fluid is a fluid containing at least one reactant in the form of a liquid or solution, and the respective fluids join together in a thin film fluid foamed between processing surfaces arranged to be opposite to each other so as to be able to approach to and separate from each other, at least one of which rotates relative to the other, whereby an organic reaction is performed in the thin film fluid.Type: ApplicationFiled: September 11, 2008Publication date: July 21, 2011Applicant: M. Technique Co., Ltd.Inventor: Masakazu Enomura
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Publication number: 20110165120Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease.Type: ApplicationFiled: February 28, 2011Publication date: July 7, 2011Applicant: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
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Patent number: 7902376Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: GrantFiled: January 22, 2009Date of Patent: March 8, 2011Assignees: Merck Sharp & Dohme Corp., Banyu Pharmaceutical Co., Ltd.Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Publication number: 20110009639Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.Type: ApplicationFiled: July 9, 2010Publication date: January 13, 2011Inventors: Andrew G. Myers, Jason D. Brubaker
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Patent number: 7846949Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of liver X receptors (LXRs).Type: GrantFiled: February 11, 2005Date of Patent: December 7, 2010Assignee: IRM LLCInventors: Valentina Molteni, Xiaolin Li, Fang Liang, Juliet Nabakka, Enrique Saez, John Wityak
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Publication number: 20100234609Abstract: Provided are a compound represented by Formula (I): wherein R1, R2, R3, and R4 are each independently selected from a hydrogen atom, a C1-6 alkyl group which may be substituted, a C7-14 aralkyl group which may be substituted and —C(?O)Rx; n denotes an integer selected from 1 and 2; and ring Ar is selected from the groups represented by the following Formula (a) to (f). or a prodrug thereof or a pharmaceutically acceptable salt thereof as well as a pharmaceutical agent and a pharmaceutical composition containing such a compound or a prodrug thereof, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: July 27, 2007Publication date: September 16, 2010Inventors: Tsutomu Sato, Yoshihito Ohtake, Masahiro Nishimoto, Takashi Emura, Takamitsu Kobayashi, Marina Yamaguchi, Kyouko Takami
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Patent number: 7763735Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.Type: GrantFiled: October 11, 2007Date of Patent: July 27, 2010Assignee: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Jason D. Brubaker
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Publication number: 20100184992Abstract: C-nitroso compound capable of releasing neutral nitric oxide is made stable by forming a Diels Alder adduct thereof which is functionalized at the Diels-Alder double bond to impart the stability. Treatment of the stabilized adduct with agent that removes functionalization and regenerates Diels Alder double bond triggers delivery of neutral nitric oxide via retro Diels-Alder reaction and homolytic scission.Type: ApplicationFiled: April 16, 2008Publication date: July 22, 2010Applicant: Duke UniversityInventors: Eric J. Toone, Harinath Chakrapani
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Publication number: 20100168422Abstract: Provided herein are compounds and methods useful for preparing hexahydrofuro[2,3-b]furan-3-ol. Hexahydrofuro[2,3-b]furan-3-ol can be efficiently synthesized in four steps from readily available starting materials.Type: ApplicationFiled: December 30, 2008Publication date: July 1, 2010Inventor: Weiping Chen
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Publication number: 20100093788Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein W1, W2, W3, R1, R1a, R2, R2a, R3, V, Q, and X are defined herein.Type: ApplicationFiled: October 9, 2009Publication date: April 15, 2010Inventors: Mark R. Player, Daniel J. Parks, William Parsons, Senath K. Meegalla, Carl R. Illig, Shelley K. Ballentine
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Publication number: 20100051928Abstract: An organic electroluminescence device includes: a pair of electrodes; and at least one organic layer including a light emitting layer, the light emitting layer being provided between the pair of electrodes, wherein at least one layer of the at least one organic layer contains a compound represented by formula (1): wherein each of Z11 and Z12 independently represents an aromatic heterocyclic ring or an aromatic hydrocarbon ring; R11 represents a hydrogen atom or a substituent, provided that a plurality of R11s are the same or different; m represents an integer of 1 or more; and L1 represents a single bond or an m-valent linking group and is linked to any one of C atoms in R11, Z11 and Z12, provided that when m is 1, L1 does not exist.Type: ApplicationFiled: September 4, 2009Publication date: March 4, 2010Applicant: FUJIFILM CORPORATIONInventor: Eiji FUKUZAKI
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Publication number: 20100016299Abstract: The present application relates to novel substituted benzoxepinoisoxazole derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders, especially of dyslipidemias, arteriosclerosis, restenosis and ischemias.Type: ApplicationFiled: June 28, 2007Publication date: January 21, 2010Applicant: BAYER HEALTHCARE AGInventors: Nils Griebenow, Anja Buchmüller, Peter Kolkhof, Hilmar Bischoff
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Publication number: 20090187028Abstract: A novel process is provided for the preparation of chiral trans-2,3-disubstituted 5-oxotetrahydropyrans of structural formula (I): wherein Ar is optionally substituted phenyl and P is a primary amine protecting group. These compounds are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of Type 2 diabetes. Also provided are useful intermediates obtained from the process.Type: ApplicationFiled: January 22, 2009Publication date: July 23, 2009Inventors: Feng Xu, Mary M. Kim, Yoshinori Kohmura, Tricia Sladicka, Jonathan D. Rosen, Michael J. Zacuto
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Publication number: 20090093640Abstract: The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides a more efficient route for preparing the enone intermediate.Type: ApplicationFiled: October 11, 2007Publication date: April 9, 2009Inventors: Andrew G. Myers, Jason D. Brubaker
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Publication number: 20090048247Abstract: The present invention relates to isoxazoline derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV. In particular, compounds disclosed herein can be useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn's disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis, ulcerative colitis and other inflammatory diseases in a patient, particularly in humans. The present invention also relates to processes for the preparation of disclosed compounds, as well as pharmaceutical compositions thereof, and their use as phosphodiesterase (PDE) type IV inhibitors.Type: ApplicationFiled: February 13, 2006Publication date: February 19, 2009Inventors: Venkata P. Palle, Sarala Balachandran, Nidhi Gupta, Nagarajan Muthukamal, Mandadapu Raghu Ramaiah, Manoj Kumar Khera, Lailt Kumar Baregama, Vinayak Vasantrao Khairnar, Abhijit Ray, Sunanda G. Dastidar
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Publication number: 20090042866Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.Type: ApplicationFiled: November 23, 2005Publication date: February 12, 2009Inventors: William Lennox, Hongyan Qi, Duck-Hyung Lee, Soongyu Choi, Young-Choon Moon
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Publication number: 20090012074Abstract: The present invention relates to aromatic compounds of the formula I wherein Ar is phenyl or an aromatic 5- or 6-membered C-bound heteroaromatic radical, wherein Ar may carry 1 radical Ra and wherein Ar may also carry 1 or 2 radicals Rb; X is N or CH; Y is O, S, —CH?N—, —CH?CH— or —N?CH—; A is CH2, O or S; E is CR6R7 or NR3; R1 is C1-C4-alkyl, C3-C4-cycloalkyl, C3-C4-cycloalkylmethyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, fluorinated C3-C4-cycloalkylmethyl, fluorinated C3-C4-alkenyl, formyl or C1-C3-alkylcarbonyl; R1a is H, C2-C4-alkyl, C3-C4-cycloalkyl, C3-C4-alkenyl, fluorinated C1-C4-alkyl, fluorinated C3-C4-cycloalkyl, or R1a and R2 together are (CH2)n with n being 2 or 3, or R1a and R2a together are (CH2)n with n being 2 or 3; R2 and R2a are independently of each other H, CH3, CH2F, CHF2 or CF3; R3 is H or C1-C4-alkyl; R6, R7 independently of each other are selected from H, C1-C2-alkyl and fluorinated C1-C2-alkyl; and the physiologically tolerated acid addition saltsType: ApplicationFiled: October 14, 2005Publication date: January 8, 2009Inventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry
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Publication number: 20080269271Abstract: The present invention relates to substituted spiro compounds, to processes for preparing them, to medicaments comprising these compounds and to the use of these compounds for producing medicaments.Type: ApplicationFiled: May 17, 2006Publication date: October 30, 2008Applicant: Gruenenthal GmbHInventors: Robert Frank, Melanie Reich, Ruth Jostock, Gregor Bahrenberg, Hans Schick, Birgitta Henkel, Helmut Sonnenschein
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Publication number: 20080132565Abstract: The invention provides novel polycyclic macrolactones which can be produced, in particular, by a representative of the bacterial genus Verrucosispora. These substances are preferentially distinguished by their pharmacological effect. In particular, they exhibit an antibiotic effect. This antibiotic effect is preferably directed against Gram-positive bacteria.Type: ApplicationFiled: September 23, 2004Publication date: June 5, 2008Inventors: Hans-Peter Fiedler, Roderich Suebmuth, Hana Zaehner, Alan Bull
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Patent number: 7091199Abstract: The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: September 13, 2000Date of Patent: August 15, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: George E. Lee, John G. Jurcak, Timothy A. Ayers
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Patent number: 7009059Abstract: The invention relates to a method for the 1,3 dipolar cycloaddition of organic compounds, characterized in that the reaction is carried out in a microreactor.Type: GrantFiled: March 6, 2001Date of Patent: March 7, 2006Assignee: Merck Patent GmbHInventors: Hanns Wurziger, Joeran Stoldt, Guido Pieper, Norbert Schwesinger
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Patent number: 6800642Abstract: Compounds of the formula: useful for treatment of disorders such as schizophrenia, schizoaffective disorder, bipolar disorder, Parkinson's disease, L-DOPA induced pychoses and dyskinesias, Tourette's syndrome and hyperprolactinemia and in the treatment of drug addiction such as the addiction to ethanol, nicotine or cocaine and related illnesses.Type: GrantFiled: April 24, 2002Date of Patent: October 5, 2004Assignee: WyethInventors: Megan Tran, Gary P. Stack
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Publication number: 20040122037Abstract: The invention concerns substituted isoxazolines derivatives according to Formula (I): wherein X=CH?2#191, N—R7, S or O, R1, R2 and R3 are certain specific substituents, Pir is an optionally substituted piperidyl or piperazyl radical and R3 represents an optionally substituted aromatic homocyclic or heterocyclic ring system including a partially or completely hydrogenated hydrocarbon chain of maximum 6 atoms long with which the ring system is attached to the Pir radical and which may contain one or more heteroatoms selected from the group of O, N and S ; a process for their preparation, pharmaceutical compositions comprising them and their use as a medicine, in particular for the treatment of depression and/of anxiety and disorders of body weight.Type: ApplicationFiled: August 21, 2003Publication date: June 24, 2004Inventors: Jose Ignacio Andres-Gil, Francisco Javier Fernandez-Gadea, Manuel Jesus Alcazar-Vaca, Jose Maria Cid-Nunez, Joaquin Pastor-Fernandez, Antonius Adrianus Henrikus Petrus Megens, Godelieve Maria Heylen, Xavier Jean Michel Langlois, Margaretha Henrica Maria Bakker, Thomas Horst Wolfgang Steckler
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Publication number: 20040116353Abstract: The invention relates to compounds of formula: 1Type: ApplicationFiled: September 18, 2003Publication date: June 17, 2004Inventors: Bernard Ferrari, Jean Gougat, Yvette Muneaux, Pierre Perreaut, Lionel Sarran
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Patent number: 6703348Abstract: There are described benzoylcyclohexanediones of the formula I, their preparation, and their use as herbicides and plant growth regulators. In this formula (I), R1, R2, R3, R4, R5, R6, R7, Ra, Rb and Rc are various radicals, and Y and Z are a monoatomic bridge element.Type: GrantFiled: August 30, 2001Date of Patent: March 9, 2004Assignee: Aventis CropScience GmbHInventors: Andreas van Almsick, Lothar Willms, Thomas Auler, Hermann Bieringer, Felix Thürwächter
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Patent number: 6583089Abstract: Tricyclic benzoylcyclohexanedione derivatives of the formula I where X, Y, R1, R2, R3, R4, R5, R9, and m are defined herein, and their agriculturally useful salts. Process for preparing the tricyclic benzoylcyclohexanedione derivatives; compositions comprising them and the use of these derivatives or of the compositions comprising them for controlling undesirable plants are described.Type: GrantFiled: November 29, 2001Date of Patent: June 24, 2003Assignee: BASF AktiengesellschaftInventors: Matthias Witschel, Steffen Kudis, Klaus Langemann, Ernst Baumann, Wolfgang von Deyn, Guido Mayer, Ulf Misslitz, Ulf Neidlein, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Publication number: 20030082830Abstract: The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis.Type: ApplicationFiled: June 27, 2002Publication date: May 1, 2003Inventors: Stuart L. Schreiber, Matthew D. Shair, Derek S. Tan, Michael A. Foley, Brent R. Stockwell
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Publication number: 20030055094Abstract: The invention provides compounds of the formula I 1Type: ApplicationFiled: July 31, 2002Publication date: March 20, 2003Inventors: Chongqing Sun, Jeffrey A. Robl, Mark E. Salvati, Tammy Wang, Lawrence Hamann, David Augeri
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Publication number: 20030023082Abstract: The present invention relates to bicyclic compounds wherein one of the cyclic moieties is a 16-membered macrocycle and to methods for making and using these compounds.Type: ApplicationFiled: May 13, 2002Publication date: January 30, 2003Inventors: Gary Ashley, Brian Metcalf
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Publication number: 20020198217Abstract: Compounds of the formula: 1Type: ApplicationFiled: April 24, 2002Publication date: December 26, 2002Applicant: WyethInventors: Megan Tran, Gary P. Stack
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Patent number: 6489351Abstract: A compound represented by the formula: wherein X represents a sulfur atom or an oxygen atom; Y represents an optionally oxidized sulfur atom or an oxygen atom; Z represents a bond or a divalent hydrocarbon group; R1 represents an optionally substituted hydrocarbon group; R2 represents an optionally amidated or esterified carboxyl group; ring A represents an optionally substituted aromatic 5-membered heterocyclic ring; or a salt thereof. A compound of the above formula possesses cell differentiation inducing factor action-enhancing activity and anti-matrix metalloprotease activity and that is useful in the prevention and treatment of bone diseases such as osteoporosis, bone fractures, osteoarthritis and rheumatoid arthritis, arteriosclerosis, cancer metastasis, and diseases based on nerve degeneration.Type: GrantFiled: March 26, 2002Date of Patent: December 3, 2002Assignee: Takeda Chemical Industries, Ltd.Inventors: Tsuneo Yasuma, Tsuneo Oda, Masatoshi Hazama, Shigehisa Taketomi
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Patent number: 6245796Abstract: A tricyclic pyrrole or pyrazole derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof, which shows strong affinity and selectivity for the 5-HT2C receptor and is useful for the treatment of central nervous system diseases such as sexual disorders, eating disorders, anxiety, depression and sleeping disorders. (In the above formula, each symbol means as follows; Y ring: an unsaturated five-membered ring which may have 1 to 3 of one or more types of hetero atom(s) each selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom or an unsaturated six-membered ring having 1 or 2 nitrogen atom(s), X: a bond or a carbon atom, a double bond or a single bond, V: a nitrogen atom or a group represented by a formula CH, and A: a straight or branched lower alkylene group which may be substituted with a halogen atom or a cycloalkyl group).Type: GrantFiled: December 2, 1999Date of Patent: June 12, 2001Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Kyoichi Maeno, Ken-ichi Kazuta, Hideki Kubota, Itsuro Shimada, Tetsuya Kimizuka, Shuichi Sakamoto, Fumikazu Wanibuchi
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Patent number: 6180411Abstract: A new class of optical indicators which are capable of memorizing and preserving the spatial localization of intracellular analytes in a time resolved manner is described. The compounds comprise a chromophore carrying a photolabile group capable of undergoing an irreversible and detectable chemical transformation upon irradiation by light. The chromophore is linked to a binding site capable of binding an analyte, wherein binding of the analyte to the binding site alters an optical property of the chromophore, thus altering the ability of the photolabile group to undergo the chemical transformation. Methods and kits for memorizing the spatial localization of the analytes are also described.Type: GrantFiled: July 30, 1998Date of Patent: January 30, 2001Assignee: The Regents of the University of CaliforniaInventors: Roger Y. Tsien, Stephen R. Adams
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Patent number: 6143773Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein A is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, arylC.sub.1-6 alkyl, aryl, S(O).sub.p R.sup.1, OR.sup.1 or NR.sup.1 R.sup.12 ;B is optionally substituted 5- or 6-membered heteroaromatic ring or C(O)NR.sup.10 R.sup.11 ;R.sup.1 is hydrogen, optionally substituted C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl or C.sub.3-6 cycloalkenyl, optionally substituted aryl, arylC.sub.1-6 alkyl, arylC.sub.2-6 alkenyl or arylC.sub.2-6 alkynyl or an optionally substituted 5- or 6-membered heteroaromatic ring;R.sup.2 and R.sup.3 are hydrogen or C.sub.1-6 alkyl;R.sup.4 is hydrogen, C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.2-8 alkynyl, aryl or CH.sub.2 (CO).sub.m NR.sup.8 R.sup.9 ;R.sup.5 is NR.sup.6 R.sup.7, C.sub.1-6 alkyl or C.sub.1-6 alkoxy;R.sup.6 is independently as defined for R.sup.4 ;R.sup.Type: GrantFiled: April 22, 1999Date of Patent: November 7, 2000Assignee: Merck Sharp & Dohme LimitedInventors: Howard Barff Broughton, Mark Stuart Chambers
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Patent number: 6096755Abstract: Compounds of the formula I ##STR1## where B, R.sup.1, R.sup.2, n, R.sup.3, A, X, Y and Z have the meanings stated in the description, and their preparation are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: February 1, 1999Date of Patent: August 1, 2000Assignee: BASF AktiengesellschaftInventor: Gerd Steiner