Chalcogen Bonded Directly To The Oxazine Ring Patents (Class 544/92)
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Publication number: 20110118241Abstract: The invention provides compounds of the general formula (I) which are inhibitors of the human aldosterone synthase, and also pharmaceutical compositions containing these compounds, and the use of these compounds and other heteroaryl substituted quinolinone derivatives for the treatment of hyperaldosteronism and/or disorders or diseases that are mediated by 11 ?-hydroxylase (CYP11 B1).Type: ApplicationFiled: May 5, 2009Publication date: May 19, 2011Applicant: Universitat des SaarlandesInventors: Rolf W. Hartmann, Ralf Heim, Simon Lucas
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Patent number: 7943607Abstract: Compounds of formula (I), wherein R1, R4, HET-1 and HET-2 are as described in the specification, and their salts and pro-drugs, are activators of glucokinase (GLK) and are thereby useful in the treatment of, for example, type 2 diabetes. Processes for preparing compounds of formula (I) are also described.Type: GrantFiled: May 23, 2006Date of Patent: May 17, 2011Assignee: AstraZeneca ABInventors: Darren McKerrecher, Kurt Gordon Pike, Michael James Waring
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Publication number: 20110112084Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.Type: ApplicationFiled: November 13, 2009Publication date: May 12, 2011Inventors: Lin Zhi, Christopher Tegley, Barbara Pio, Corneils Arjan Van Oeveren, Mehrnouch Motamedi, Esther Martinborough, Robert Higuchi, Lawrence G. Hamann
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Publication number: 20110104109Abstract: The present invention relates to Tetracyclic Indole Derivatives, compositions comprising at least one Tetracyclic Indole Derivative, and methods of using the Tetracyclic Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Frank Bennett, Qingbei Zeng, Srikanth Venkatraman, Mousumi Sannigrahi, Kevin X. Chen, Gopinadhan N. Anilkumar, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Publication number: 20110077397Abstract: A simple, cost-effective process for preparation of efavirenz of formula (I) comprising reacting a solution of 5-chloro-?-(cyclopropylethynyl)-2-amino-?-trifluoromethyl) benzene methanol of formula (II) in an organic solvent with triphosgene in the presence of an inorganic base at a temperature range ?5° C. to 25° C., adding water and isolating compound of formula (I).Type: ApplicationFiled: May 27, 2009Publication date: March 31, 2011Inventors: Mukund Keshav Gurjar, Abdulrakheeb Abdulsubhan Deshmukh, Sanjay Shankar Deshmukh, Satish Ramanlal Mehta
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Patent number: 7915406Abstract: The invention relates to a method for preparing a benzoxazinone comprising reacting an isatoic anhydride with an acylating compound in the presence of an N-alkyl imidazole, to a method for preparing a photo-stabilised composition, comprising adding a benzoxazinone and to the use of a benzoxazinone as a light-absorber or as a stabiliser for a light-sensitive compound.Type: GrantFiled: January 5, 2007Date of Patent: March 29, 2011Assignee: Temsa International Inc.Inventor: Asim Kumar Sarkar
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Publication number: 20110071287Abstract: The present invention relates to a process for the preparation of Efavirenz (Formula I), wherein triphosgene is used as a cyclizing agent.Type: ApplicationFiled: May 1, 2009Publication date: March 24, 2011Applicant: RANBAXY LABORATORIES LIMITEDInventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Mukesh Sharma, Chandra Has Khanduri
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Publication number: 20110071141Abstract: Condensed-ring aryl compounds of formula (I) and use of the same as a agrochemical for controlling noxious organisms wherein (X)mQ, A, R1, (Y)n and the grouping —W1—W2—W3—W4— are as defined herein.Type: ApplicationFiled: March 13, 2009Publication date: March 24, 2011Inventors: Tetsuya Murata, Yasushi Yoneta, Jun Mihara, Kei Domon, Mamoru Hatazawa, Koichi Araki, Eiichi Shimojo, Katsuhiko Shibuya, Teruyuki Ichihara, Ulrich Görgens, Arnd Voerste, Angela Becker, Eva-Maria Franken, Klaus-Helmut Müller
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Publication number: 20110053926Abstract: The present invention relates to the use of the compounds of general formula 1 wherein the groups R1, R2 and R3 may have the meanings specified in the claims and in the description, for preparing a pharmaceutical composition for the treatment of respiratory complaints, as well as new compounds of formula 1, processes for preparing them, and pharmaceutical formulations containing them.Type: ApplicationFiled: November 5, 2010Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Ingo KONETZKI, Thierry BOUYSSOU, Philipp LUSTENBERGER, Andreas SCHNAPP
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Patent number: 7897761Abstract: A compound represented by the following Formula (1): wherein, Het1 represents a bivalent five- or six-membered aromatic heterocyclic residue and may further be substituted; Xa to Xd each independently represent a heteroatom and may further be substituted; Ya to Yf each independently represent a heteroatom or a carbon atom and may further be substituted; the ring bound to Het1 may have a double bond at any position.Type: GrantFiled: March 28, 2008Date of Patent: March 1, 2011Assignee: Fujifilm CorporationInventors: Ichiro Amasaki, Naoyuki Hanaki
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Publication number: 20110046112Abstract: The invention is concerned with novel heterobicyclic derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, V, W, X and Y are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.Type: ApplicationFiled: November 8, 2010Publication date: February 24, 2011Inventors: Jean Ackermann, Konrad Bleicher, Simona M. Ceccarelli, Odile Chomienne, Patrizio Mattei, Ulrike Obst Sander
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Publication number: 20110021772Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: The invention also relates to a process for the preparation of these compounds as well as their use as medicaments, in particular as anti-bacterial agents.Type: ApplicationFiled: April 16, 2010Publication date: January 27, 2011Inventors: Maxime Lampilas, Jozsef Aszodi, David Alan Rowlands, Claude Fromentin
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Publication number: 20110015314Abstract: An ultraviolet absorbent containing a compound represented by the following formula (I), having an aluminum ion in a concentration of less than 2 ppm, and an iron ion in a concentration of less than 2 ppm. wherein R1 represents a substituent; n1 represents an integer of 0 to 4; R2 represents an n2-valent substituent or a linking group; and n2 represents an integer of 1 to 4.Type: ApplicationFiled: March 30, 2009Publication date: January 20, 2011Applicant: FUJIFILM CorporationInventors: Youichiro Takeshima, Keizo Kimura
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Publication number: 20110015189Abstract: The present invention provides a process for the preparation of Efavirenz. A compound of Formula 1 may be prepared by a process comprising cyclizing, in the presence of a first base, a compound of Formula 5 with a haloformate of Formula 6. Other processes are also provided as well as novel compounds prepared by and used in such processes.Type: ApplicationFiled: July 20, 2009Publication date: January 20, 2011Applicant: APOTEX PHARMACHEM INC.Inventors: Bo CHEN, Zhi-Xian WANG, Yutao XUE, Lihong LIU, Hao CHEN
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Patent number: 7858617Abstract: The use of a compound comprising formula (I): or a salt, ester, amide or prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is a 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.Type: GrantFiled: March 7, 2008Date of Patent: December 28, 2010Assignee: Norgine B.V.Inventors: Harold Francis Hodson, Robert Downham, Timothy John Mitchell, Beverley Jane Carr, Christopher Robert Dunk, Richard Michael John Palmer
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Publication number: 20100274007Abstract: Disclosed herein is a novel process for preparing polymorphic Forms of (S)-6-chloro-(cyclopropylethynyl)-1,4-di-hydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one referred as M1, I, II, ?, and ?.Type: ApplicationFiled: December 24, 2008Publication date: October 28, 2010Applicant: MATRIX LABORATORIES LIMITEDInventors: Om Dutt Tyagi, Ram K. R. Jetti, B. A. Ramireddy
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Publication number: 20100267715Abstract: Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject.Type: ApplicationFiled: June 3, 2010Publication date: October 21, 2010Applicant: Wyeth LLCInventors: Marc Sadler Tesconi, Mannching Sherry Ku, Yan Xu
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Publication number: 20100267714Abstract: The invention provides novel heterocyclic compounds, pharmaceutical compositions and methods of treatment that modulate levels of MIF expression and treat disorders associated with high or low levels of MIF expression.Type: ApplicationFiled: May 4, 2010Publication date: October 21, 2010Inventors: William L. Jorgensen, Richard J. Bucala
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Publication number: 20100256362Abstract: A method of producing a compound represented by Formula (I), which comprises a step A of reacting an anthranilic acid compound with a carboxylic halide in the absence of a base, but does not comprise a step of isolating of an amide intermediate compound represented by Formula (II): wherein R1 represents a substituent; n1 is an integer of 0 to 4; R2 represents an n2-valent substituent or a linking group; and n2 is an integer of 1 to 4.Type: ApplicationFiled: September 25, 2008Publication date: October 7, 2010Inventors: Keizo Kimura, Takashi Kitagawa, Osamu Uchida
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Patent number: 7799913Abstract: This invention related to the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for higher order behaviors. These brain networks are involved in cognitive abilities related to memory impairment, such as is observed In a variety of dementias, and in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson?s disease, schizophrenia and affective disorders. In a particular aspect, the present invention relates to compounds useful for treatment of such conditions and methods of using these compounds for such treatment.Type: GrantFiled: November 25, 2002Date of Patent: September 21, 2010Assignee: Cortex Pharmaceuticals, Inc.Inventors: Gary A. Rogers, Matthew Allan, Clayton Harris, Jianjie Huang, Christopher M. Marrs, Rudolf Mueller, Stanislaw Rachwal
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Publication number: 20100234363Abstract: Disclosed is a compound which is useful as an 11?-hydroxysteroid dehydrogenase type 1 inhibitor.Type: ApplicationFiled: September 17, 2008Publication date: September 16, 2010Applicants: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC., SHIONOGI & CO., LTD.Inventors: Akiko Itai, Susumu Muto, Ryuko Tokuyama, Hiroshi Fukasawa, Takeshi Yanase
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Publication number: 20100233268Abstract: The present invention relates to powder formulations for inhalation containing enantiomerically compounds of general Formula (I) wherein the groups R1, R2 and R3 may have the meanings indicated in the claims and in the specification, optionally in the form of the pharmaceutically acceptable acid addition salts thereof, and optionally in combination with a pharmaceutically acceptable excipient, processes for preparing them and their use as medicaments, particularly as medicaments for the treatment of respiratory complaints.Type: ApplicationFiled: August 21, 2007Publication date: September 16, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael Trunk, Marc Egen
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Patent number: 7786297Abstract: Micronized tanaproget, purified tanaproget Form I, and micronized, purified tanaproget Form I are provided. Also provided are compositions containing one or more of the prepared tanaproget forms, methods of using one or more of the prepared tanaproget forms, and kits containing one or more of the prepared tanaproget forms.Type: GrantFiled: April 26, 2006Date of Patent: August 31, 2010Assignee: Wyeth LLCInventors: Ramarao Chatlapalli, Arwinder Nagi, John Potoski, Jean Louise Helom, Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Vladimir Dragan
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Publication number: 20100210636Abstract: [PROBLEMS] To provide a compound useful as an agent for the treatment of circulatory diseases, nervous system diseases, metabolic diseases, reproductive system diseases, and digestive tract diseases. [MEANS FOR SOLVING PROBLEMS] The compound, which is for use as an active ingredient, is represented by the formula (I): [wherein R1 represents optionally halogenated C1-6 alkyl, etc.; R2 represents, e.g., a group represented by the formula (II-1) or (II-4) (wherein W represents C1-6 alkylene, etc. and R represents C1-6 alkyl, etc.); R3 represents hydrogen, C1-6 alkyl, etc.; X represents —O—, —NH—, etc.; and Y1, Y2, Y3, and Y4 each independently represents —CH—, —N—, etc.].Type: ApplicationFiled: October 2, 2008Publication date: August 19, 2010Inventors: Shiho Ishikawa, Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi
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Patent number: 7767668Abstract: The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget. The compositions can also contain microcrystalline cellulose, croscarmellose sodium, anhydrous lactose, magnesium stearate, micronized edetate calcium disodium hydrous, and micronized sodium thiosulfate pentahydrate. The compositions are useful in contraception and hormone replacement therapy and in the treatment and/or prevention of uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, and carcinomas and adenocarcinomas of the pituitary, endometrium, kidney, ovary, breast, colon, and prostate and other hormone-dependent tumors, and in the preparation of medicaments useful therefor. Additional uses include stimulation of food intake.Type: GrantFiled: April 26, 2006Date of Patent: August 3, 2010Assignee: Wyeth LLCInventors: Arwinder S. Nagi, Ramarao Chatlapalli, Shamim Hasan, Mohamed Ghorab, Dhaval Gaglani
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Patent number: 7759341Abstract: Tanaproget polymorph Form II, processes for preparing tanaproget polymorph Form II, pharmaceutical compositions including tanaproget polymorph Form II, micronized tanaproget polymorph Form II, and processes for converting Form II to tanaproget Form I are provided. Also provided are methods of contraception, hormone replacement therapy, stimulation of food intake and treating or preventing uterine myometrial fibroids, benign prostatic hypertrophy, benign and malignant neoplastic disease, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, or carcinomas and adenocarcinomas comprising administering polymorph Form II to a mammalian subject.Type: GrantFiled: April 26, 2006Date of Patent: July 20, 2010Assignee: Wyeth LLCInventors: Marc Sadler Tesconi, Mannching Sherry Ku, Yan Xu
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Publication number: 20100168093Abstract: The present invention relates to substituted pyrrolidine compounds of general formula (I), methods for their preparation, medicaments comprising these compounds as well as their use for the preparation of a medicament for the treatment of humans and animal.Type: ApplicationFiled: April 30, 2007Publication date: July 1, 2010Inventors: Miguel Angel Pericas-Brondo, Antoni Torrens-Jover, Susana Yenes-Minguez, Félix Cuevas Cordobés, Carmen Garcia Granda
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Publication number: 20100160304Abstract: The present invention provides a compound represented by the following formula (I): [wherein, A represents a group of the following formula (A-1): etc., R1 and R2 each independently represent a hydrogen atom etc., Z represents CR3 etc., W represents CR4 etc., Q represents CR5 etc., R3, R4 and R5 each independently represent a hydrogen atom etc., Y represents an oxygen atom or sulfur atom, X represents an oxygen atom etc. and B represents an optionally substituted aryl group or optionally substituted heteroaryl group], the prodrug thereof or the pharmaceutically acceptable salt thereof for preventing or treating various diseases such as hypertension, cerebral stroke, cardiac failure, etc.Type: ApplicationFiled: January 17, 2006Publication date: June 24, 2010Applicant: Dainippon Sumitomo Pharma Co., LtdInventor: Seiji Katayama
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Publication number: 20100160307Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a bezoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.Type: ApplicationFiled: March 5, 2010Publication date: June 24, 2010Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: GEORGE PHILIP LAHM, Stephen Frederick McCann, Kanu Maganbhai Patel, Thomas Paul Selby, Thomas Martin Stevenson
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Patent number: 7740693Abstract: The present disclosure provides Benzoxazinone compounds represented by the formula: wherein each R1, R2, R3, and R4 is independently selected from hydrogen, alkyl of 1-12 carbon atoms, substituted alkyl, aryl of 6-12 carbon atoms, substituted aryl, halo, and alkoxy; and R5 is selected from alkyl of 1-12 carbon atoms, substituted alkyl, aryl of 6-12 carbon atoms, substituted aryl, halo, and alkoxy; wherein each of the substituted alkyl and the substituted aryl groups have a substituent selected from alkyl, aryl, halo, and alkoxy. The present disclosure provides a mark having a benzoxazinone compound, and a method for applying the mark onto an article. Also provided is a process for preparing benzoxazinone compounds.Type: GrantFiled: October 1, 2007Date of Patent: June 22, 2010Inventors: Thomas Potrawa, Joachim Schulz
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Patent number: 7713966Abstract: The present invention relates generally to azabicyclic containing pharmaceutical agents, and in particular, to azabicyclic metalloprotease inhibiting compounds. More particularly, the present invention provides a new class of azabicyclic MMP-3, MMP-8 and/or MMP-13 inhibiting compounds, which exhibit an increased potency and selectivity in relation to currently known MMP-13, MMP-8 and MMP-3 inhibitors.Type: GrantFiled: November 20, 2007Date of Patent: May 11, 2010Assignee: Alantos Pharmaceuticals Holding, Inc.Inventors: Christian Gege, Matthias Schneider, Carine Chevrier, Hongbo Deng, Irving Sucholeiki, Brian M. Gallagher, Jr., Michael Bosies, Christoph Steeneck, Xinyuan Wu, Matthias Hochgürtel, Bert Nolte, Arthur Taveras
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Publication number: 20100113770Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group rType: ApplicationFiled: October 14, 2009Publication date: May 6, 2010Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Susumu MUTO, Akiko ITAI
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Patent number: 7709474Abstract: The present invention relates to enantiomerically pure compounds of formula 1 wherein the groups R1, R2, R3, m and Ym? may have the meanings given in the claims and specification, processes for preparing them and their use as medicaments, particularly as medicaments for the treatment of respiratory complaints.Type: GrantFiled: August 21, 2007Date of Patent: May 4, 2010Assignee: Boehringer Ingelheim International GmbHInventors: Ingo Konetzki, Peter Sieger
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Patent number: 7696201Abstract: The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases.Type: GrantFiled: August 15, 2007Date of Patent: April 13, 2010Assignee: Vertex Pharmaceuticals IncorporatedInventors: Lewis R. Makings, Dennis J. Hurley, Gabriel Raffai
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Publication number: 20100069379Abstract: The present invention is directed to compounds, pharmaceutical compositions, and methods for modulating processes mediated by AR and PR. More particularly, the invention relates to nonsteroidal compounds and compositions that are high affinity, high specificity agonists, partial agonists (i.e., partial activators and/or tissue-specific activators) and antagonists for AR and PR. Also provided are methods of making such compounds and pharmaceutical compositions, as well as critical intermediates used in their synthesis.Type: ApplicationFiled: November 13, 2009Publication date: March 18, 2010Inventors: Lin Zhi, Christopher Tegley, Barbara Pio, Corneils Arjan Van Oeveren, Mehrnouch Motamedi, Esther Martinborough, Robert Higuchi, Lawrence G. Hamann
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Patent number: 7659280Abstract: The present invention provides 3-hydroxyphenyl-2,4-pyrimidinediamine compounds of formula I, as well as related compositions and methods for treating a variety of autoimmune diseases.Type: GrantFiled: February 16, 2007Date of Patent: February 9, 2010Assignee: Rigel Pharmaceuticals, Inc.Inventors: Jeffrey Wayne Clough, Somasekhar Bhamidipati, Rajinder Singh, Esteban Masuda, Haoran Zhao
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Publication number: 20100004439Abstract: A compound represented by the following Formula (1): wherein, Het1 represents a bivalent five- or six-membered aromatic heterocyclic residue and may further be substituted; Xa to Xd each independently represent a heteroatom and may further be substituted; Ya to Yf each independently represent a heteroatom or a carbon atom and may further be substituted; the ring bound to Het1 may have a double bond at any positionType: ApplicationFiled: March 28, 2008Publication date: January 7, 2010Applicant: FUJIFLM CorporationInventors: Ichiro Amasaki, Naoyuki Hanaki
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Publication number: 20090318431Abstract: The present invention provides a compound of formula (I) wherein X is a structure of the following formula (i), (ii) (iii), or iv G is O, or S; U is —(CR3R4)n—; W is CH2NHC(=G)R1, CH2NH-het, CH2-G-het, CH2het, C(?O)NHR2; and Y1, Y2 and Y3 are independently CH, or CF. The compounds of the present invention are useful as antibacterial agents.Type: ApplicationFiled: February 5, 2007Publication date: December 24, 2009Inventors: Gary Wayne Luehr, Adam Robert Renslo, Mikhail Fedorovich Gordeev, Hongwu Gao, Vara Prasad Venkata Nagendra Josyula
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Publication number: 20090312313Abstract: The present invention provides compounds represented by formula (I) and pharmaceutically acceptable salts and solvates thereof: wherein X represents CH or N; Z represents —O—, —NH— or —C(?O)—; R and R? represent a hydrogen atom, hydroxyl, a halogen atom, optionally substituted alkyl, optionally substituted alkenyl optionally substituted alkoxy, amino, aminocarbonyl, or an optionally substituted heterocyclic group; and A represents an optionally substituted specific carbocyclic or heterocyclic group. The compounds according to the present invention have excellent TGF? inhibitory activity.Type: ApplicationFiled: May 26, 2009Publication date: December 17, 2009Applicant: KIRIN BEER KABUSHIKI KAISHAInventors: Kiyoshi Shimizu, Toshiyuki Shimizu, Kaname Kimura, Kazuki Kawakami, Masayoshi Nakoji
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Publication number: 20090306371Abstract: Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided. Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl.Type: ApplicationFiled: July 24, 2009Publication date: December 10, 2009Applicant: WyethInventor: Bogdan Kazimierz Wilk
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Publication number: 20090281096Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.Type: ApplicationFiled: April 8, 2009Publication date: November 12, 2009Applicant: WyethInventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
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Patent number: 7601743Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: April 18, 2006Date of Patent: October 13, 2009Assignee: Syngenta Crop Protection, Inc.Inventors: Andre Jeanguenat, Anthony O'Sullivan, Michael Muehlebach, Stephan Trah, Roger Graham Hall
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Publication number: 20090221567Abstract: Compounds of Formula I, or pharmaceutically acceptable salts thereof: wherein Y, X, A, R1, R2, m, p, and q are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: ApplicationFiled: February 25, 2009Publication date: September 3, 2009Applicant: ASTRAZENECA ABInventors: Yun-Xing Cheng, Xuehong Luo, Mehrnaz Pourashraf, Vijayaratnam Santhakumar, Miroslaw Jerzy Tomaszewski
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Patent number: 7582755Abstract: Methods for preparing cyclic carbamates and thiocarbamates containing cyanopyrrole moieties and of the formula are provided. Z are the same or different and are H, optionally substituted C1 to C6 alkyl, or CORA; RA is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl; Q are the same or different and are H, OH, NH2, CN, halogen, optionally substituted C1 to C6 alkyl, optionally substituted C2 to C6 alkenyl, optionally substituted C1 to C6 alkynyl, optionally substituted C1 to C6 alkoxy, optionally substituted C1 to C6 aminoalkyl, or CORB; and RB is H, optionally substituted C1 to C6 alkyl, optionally substituted C1 to C6 alkoxy, or optionally substituted C1 to C6 aminoalkyl.Type: GrantFiled: April 25, 2005Date of Patent: September 1, 2009Assignee: WyethInventor: Bogdan Kazimierz Wilk
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Patent number: 7572824Abstract: Methods for minimizing the formation of thioamide compounds using decoy agents during reactions, such as thionations of carbonyl compounds containing nitrile groups, and the products thereby are provided.Type: GrantFiled: November 16, 2007Date of Patent: August 11, 2009Assignee: WyethInventor: Bogdan K. Wilk
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Publication number: 20090197878Abstract: Compounds of formula (I), or pharmaceutically acceptable salts thereof, are provided, wherein R1-R6 and X are defined herein. Also provided are methods of preparing the compounds of formula (I), pharmaceutical compositions and kits containing a compound of formula (I), as are methods of treating endometriosis, hormone-dependent carcinomas, leiomyoma, fibroids, dysfunctional bleeding, polycystic ovary syndrome, and menopause related symptoms; methods of contraception; methods of providing hormone replacement therapy; methods of stimulating food intake; methods of synchronizing estrus; and methods of treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder by administering to a mammal in need thereof a pharmaceutically effective amount of a compound of formula (I).Type: ApplicationFiled: January 29, 2009Publication date: August 6, 2009Applicant: WyethInventors: Thomas Joseph Commons, Douglas John Jenkins, Eugene John Trybulski, Andrew Fensome
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Patent number: 7569564Abstract: Methods of using compounds which are progesterone receptor agonists for contraception and the treatment of progesterone-related maladies alone or in combination with an estrogen receptor agonist or progesterone receptor antagonist are provided. These compounds have the structure: wherein R1, R2, R3, R4, R5, and Q1 are defined herein.Type: GrantFiled: February 9, 2006Date of Patent: August 4, 2009Assignee: WyethInventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
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Patent number: 7566780Abstract: The present invention provides phosphorus-based oxazine compounds and the preparation method thereof. The phosphorus-based oxazine compounds of the present invention can provide better fire-resistant characteristics, while the preparation method for the phosphorus-based oxazine compound of the present invention can offer high yields and/or high purity phosphorus-based oxazine compounds.Type: GrantFiled: January 21, 2008Date of Patent: July 28, 2009Assignees: Chang Chun Plastics Co., Ltd., National Chung Hsing UniversityInventors: Ching-Hsuan Lin, Ya-Ru Taso, Chau-Wei Hsieh, Hao-Hsin Lee, Fang-Hsien Su, An-Pang Tu, Kuen-Yuan Hwang
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Patent number: 7566707Abstract: The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula wherein Y and R1 to R4 are defined as in claim 1, the tautomers, enantiomers, diastereomers, the mixtures thereof and the salts thereof, which have valuable pharmacological properties, particularly an inhibiting effect on the activity of the enzyme dipeptidylpeptidase-IV (DPP-IV).Type: GrantFiled: June 10, 2004Date of Patent: July 28, 2009Assignee: Boehringer Ingelheim International GmbHInventors: Matthias Eckhardt, Norbert Hauel, Elke Langkopf, Frank Himmelsbach, Iris Kauffmann-Hefner, Mohammad Tadayyon, Michael Mark
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Publication number: 20090176773Abstract: The invention relates to non-peptidic molecules which modulate, especially inhibit, the interaction of protein kinase A (PKA) and A kinase anchor proteins (AKAP) and to a host or target organism that comprises said non-peptidic compounds or recognition molecules directed to said compounds, such as e.g. antibodies or chelating agents. The invention also relates to a pharmaceutical agent, especially for use in the treatment of diseases that are associated with a disturbance of the cAMP signal path, especially insipid diabetes, hypertonia, pancreatic diabetes, duodenal ulcer, asthma, heart failure, obesity, AIDS, edema, hepatic cirrhosis, schizophrenia and others. The invention also relates to the use of the inventive molecules.Type: ApplicationFiled: May 18, 2006Publication date: July 9, 2009Applicant: FORSCHUNGSVERBUND BERLIN E.V.Inventors: Enno Klussmann, Walter Rosenthal, Jorg Rademann, Frank Christian, Sina Meyer