Chalcogen Bonded Directly To The Oxazine Ring Patents (Class 544/92)
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Publication number: 20130028879Abstract: 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 benzoxazinone 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: August 10, 2012Publication date: January 31, 2013Applicant: 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: 8354403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: GrantFiled: August 17, 2010Date of Patent: January 15, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent J. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Publication number: 20130012702Abstract: Methods for purifying a compound of formula I are provided, wherein A, B, X, Q, and R1 are defined herein. The methods include mixing the compound of formula I and a solvent; adding a base to the solvent; and precipitating purified compound of formula I.Type: ApplicationFiled: September 14, 2012Publication date: January 10, 2013Applicant: Wyeth LLCInventors: Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Anthony Francis Hadfield, Jean Louise Helom
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Patent number: 8343965Abstract: Compositions, preferably pharmaceutical compositions, containing micronized tanaproget, or pharmaceutically acceptable salt thereof, microcrystalline cellulose, croscarmellose sodium, sodium lauryl sulfate, butylated hydroxyanisole, povidone, and magnesium stearate, are provided. 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: January 1, 2013Assignee: Wyeth LLCInventors: Arwinder S. Nagi, Ramarao Chatlapalli, Shamim Hasan, Rolland W. Carson, Mohamed Ghorab
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Patent number: 8329690Abstract: 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: April 8, 2009Date of Patent: December 11, 2012Assignee: Wyeth LLCInventors: 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: 8318930Abstract: 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: GrantFiled: December 24, 2008Date of Patent: November 27, 2012Assignee: Matrix Laboratories LimitedInventors: Om Dutt Tyagi, Ramakoteswara Rao Jetti, B. A. Ramireddy
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Patent number: 8314094Abstract: [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: GrantFiled: October 2, 2008Date of Patent: November 20, 2012Assignee: MSD K.KInventors: Shiho Ishikawa, Takashi Mizutani, Tsuyoshi Nagase, Nagaaki Sato, Hidekazu Takahashi
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Publication number: 20120289493Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.Type: ApplicationFiled: May 8, 2012Publication date: November 15, 2012Inventors: Britton Kenneth Corkey, Elfatih Elzein, Robert H. Jiang, Rao V. Kalla, Tetsuya Kobayashi, Dmitry Koltun, Xiaofen Li, Ruben Martinez, Gregory Notte, Eric Q. Parkhill, Thao Perry, Jeff Zablocki, Chandrasekar Venkataramani, Michael Graupe, Juan Guerrero
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Patent number: 8304538Abstract: 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: GrantFiled: September 25, 2008Date of Patent: November 6, 2012Assignee: FUJIFILM CorporationInventors: Keizo Kimura, Takashi Kitagawa, Osamu Uchida
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Publication number: 20120270863Abstract: The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.Type: ApplicationFiled: October 21, 2010Publication date: October 25, 2012Applicant: Fibrotech Therapeutics Pty LtdInventors: Spencer John Williams, Steven Zammit, Darren James Kelly
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Publication number: 20120271047Abstract: The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.Type: ApplicationFiled: July 3, 2012Publication date: October 25, 2012Applicant: HETERO DRUGS LIMITEDInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Publication number: 20120264933Abstract: The present invention provides an efficient method to induce the enantioselectivity in procarbonyl compounds using chiral organometallic complexes. The present invention also provides a method for producing chiral organometallic complexes using a chiral additive, achiral additive, a base and a metal salt.Type: ApplicationFiled: June 22, 2012Publication date: October 18, 2012Applicant: Laurus Labs Private LimitedInventors: Ravindra Babu BOLLU, Narasimha Rao Ketavarapu, Venkata Sunil Kumar Indukuri, Seeta Ramanjaneyulu Gorantla, Satyanarayana Chava
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Publication number: 20120252941Abstract: It is an object of the present invention to provide a bisbenzoxazinone compound which does not substantially contain an alkali metal salt, has high purity and provides a resin composition having excellent resistance to hydrolysis when it is contained in a resin, a production method thereof, and a resin composition comprising the compound. The present invention is a bisbenzoxazinone compound represented by the following formula (4): (R1 and R2 are each independently a hydrogen atom, hydroxyl group, alkyl group having 1 to 3 carbon atoms, or the like), and has (i) a purity of 98% or more, (ii) a content of a compound represented by the following formula (7) of less than 0.15 wt %: (iii) a maximum peak in the measurement of the light reflectance at a visible range of its powder at 380 to 480 nm and a maximum light reflectance of 100 to 120%, (iv) a metal sodium content of less than 50 ppm and (v) a YI value of ?10 to 10.Type: ApplicationFiled: November 26, 2009Publication date: October 4, 2012Inventors: Shun Ibusuki, Takashi Koga, Akira Miyake, Masayuki Hayashi, Masaya Yoshida
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Publication number: 20120245346Abstract: Disclosed is a benz[d][1,3]oxazine derivative having excellent stability when used as an active ingredient for a medicinal agent, and also having excellent solubility and crystallinity. Specifically disclosed is 2-[2-((S)-3-dimethylaminopyrrolidin-1-yl)pyridin-3-yl]-5-ethyl-7-methoxy-4H-benz[d][1,3]oxazin-4-one maleate.Type: ApplicationFiled: September 27, 2010Publication date: September 27, 2012Applicant: Kyorin Pharmaceutical Co., Ltd.Inventors: Takeshi Tsubuki, Tetsuya Sagawa, Keiko Funada, Ichiro Araya
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Publication number: 20120232069Abstract: The present invention relates to a process for the preparation of crystalline non-hygroscopic form H1 of efavirenz, and pharmaceutical compositions containing it. In accordance with the present invention efavirenz was dissolved in acetone at 25° C.-30° C., the solution was slowly added to water at 0° C.-5° C., the separated solid was filtered, washed with mixture of acetone and water and dried at 25° C.-35° C. under below 65% relative humidity for 18 hours to give crystalline non-hygroscopic efavirenz form H1.Type: ApplicationFiled: December 22, 2008Publication date: September 13, 2012Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Publication number: 20120225121Abstract: The present invention provides a suitable technique namely wet milling and the process for reducing the particle size of efavirenz and making a tablet or capsule formulation with desired bioavailability equivalent to the reference listed drug without loosing its characteristics.Type: ApplicationFiled: November 4, 2009Publication date: September 6, 2012Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasarad-Hi Reddy, Podili Khadgapathi, Goli Kamalakar Reddy
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Patent number: 8258131Abstract: The present invention provides a novel fused bicyclic compound having an affinity to a receptor of mineral corticoid (MR), shown by the formula [I]: wherein the ring A is a benzene ring having a substituent R1, fused to an adjacent 6-membered heterocyclic ring and further optionally having a substituent(s) other than R1, R1 is an alkylsulfonylamino group etc.Type: GrantFiled: July 21, 2008Date of Patent: September 4, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Yoichi Takahashi, Nobumasa Awai, Hidenori Akatsuka, Takayuki Kawaguchi, Toru Iijima
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Publication number: 20120208797Abstract: A compound represented by the formula (I) or a pharmaceutically acceptable salt thereof: wherein Z represents nitrogen atom or C—X; X represents hydrogen atom or fluorine atom; R1 is hydrogen atom or a C1-C3 alkyl group; L represents single bond or a C1-C6 alkylene group which may be substituted; Y represents single bond, sulfur atom, oxygen atom, NH, or the like; R2 represents hydrogen atom or a cyclic group which may be substituted, which is used for preventive and/or therapeutic treatment of a disease caused by abnormal activity of tau protein kinase 1 such as a neurodegenerative diseases (e.g. Alzheimer disease).Type: ApplicationFiled: August 11, 2010Publication date: August 16, 2012Applicants: SANOFI, MITSUBISHI TANABE PHARMA CORPORATIONInventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
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Patent number: 8242267Abstract: The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.Type: GrantFiled: July 1, 2011Date of Patent: August 14, 2012Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Publication number: 20120202782Abstract: The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Applicant: IRM LLCInventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
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Publication number: 20120178915Abstract: This invention relates with the arylheterocycle-fused pyrimidines, derivatives and analogs of formula I: or stereoisomers, tautoers, prodrugs, pharmaceutically acceptable salts, complex salts or solvates thereof, wherein: A-cycle is of 3-8 saturated or unsaturated arylheterocycles or aliheterocyclic, containing 1-4 heteroatoms, B-cycle 5-8 member saturated or unsaturated heterocycle containing 1-4 heteroatoms; X1, X2, X3, X4 are, independently at each occurrence, C, O, S, Se, N and P elements; R1, R2, R3 is a substituent containing alicyclic group, arylcycle group, heterocyclic group, adamantane alkyl, adamantane heterocycle, adamantane analogs, sugar group, hydroxyl group, amino acid group or a combination of the above substituents. This invention also relates with their preparative methods and applications.Type: ApplicationFiled: December 24, 2009Publication date: July 12, 2012Inventor: Lifeng Xu
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Publication number: 20120157432Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: August 17, 2010Publication date: June 21, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent j. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Patent number: 8178526Abstract: The invention provides a novel class of compounds of formula (I), pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or dysregulated B cell activities, particularly diseases or disorders that involve aberrant activation of inositol 1,4,5-trisphosphate 3-kinase B (ITPKb).Type: GrantFiled: June 12, 2008Date of Patent: May 15, 2012Assignee: IRM LLCInventors: Badry Bursulaya, Dai Cheng, Jiqing Jiang, Donald S. Karanewsky, Yi Liu, Shifeng Pan, Yongqin Wan, Xia Wang, Yun Feng Xie, Yang Yang
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Publication number: 20120115858Abstract: 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: January 10, 2012Publication date: May 10, 2012Applicant: Wyeth LLCInventors: Marc Sadler Tesconi, Mannching Sherry Ku, Yan Xu
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Publication number: 20120115857Abstract: The present invention relates to novel amorphous and crystalline forms of efavirenz, processes for their preparation and pharmaceutical compositions containing them. In accordance with the present invention efavirenz crude is dissolved in acetone at 25° C.-30° C., the solution is slowly added to water for 30 minutes at 0° C.-5° C., stirred for 1 hour at the same temperature, the separated solid is filtered, washed with water and dried at 55° C.-60° C. for 5 hours to give amorphous efavirenz.Type: ApplicationFiled: July 1, 2011Publication date: May 10, 2012Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Publication number: 20120108809Abstract: An improved process for Efavirenz, which has several advantages over reported methods like low cost, high yield, better optical purity and industrial feasibility.Type: ApplicationFiled: July 12, 2010Publication date: May 3, 2012Applicant: LUPIN LIMITEDInventors: Girij Pal Singh, Gurvinder Pal Singh, Pravin Mahajan, Ganesh Salunke, Dabeer Karnalkar
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Patent number: 8148521Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.Type: GrantFiled: January 31, 2011Date of Patent: April 3, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20120071471Abstract: The present invention encompasses novel 1,4-dihydro-3,1-benzoxazin-2-one derivatives, which are surprisingly found to be efficacious in animal models of CNS disorders and, as such, are valuable candidates for the prevention or treatment of CNS (Central Nervous System) diseases or disorders.Type: ApplicationFiled: March 11, 2010Publication date: March 22, 2012Applicant: NEUROSEARCH A/SInventors: Antonio Nardi, Karin de Linde Troelsen, Helle Kirstein Erichsen
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Publication number: 20120065189Abstract: The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R1 and R2, each independently represent hydrogen; a phenyl lower alkyl group that may have a substituent(s) selected from the group consisting of a lower alkyl group and the like on a benzene ring and/or a lower alkyl group; or a cyclo C3-C8 alkyl lower alkyl group; or the like; R3 represents a lower alkynyl group or the like; R4 represents a phenyl group that may have a substituent(s) selected from the group consisting of a 1,3,4-oxadiazolyl group that may have e.g., halogen or a heterocyclic group selected from pyridyl group and the like; the heterocyclic group may have at least one substituent(s) selected from a lower alkoxy group and the like or a salt thereof.Type: ApplicationFiled: May 27, 2010Publication date: March 15, 2012Inventors: Akira Takahashi, Masaki Suzuki, Yuichi Nakamura, Yohji Sakurai
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Patent number: 8129524Abstract: 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: July 11, 2011Date of Patent: March 6, 2012Assignee: Wyeth LLCInventor: Bogdan Kazimierz Wilk
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Patent number: 8129523Abstract: A convenient preparation of boron-containing compounds, borate salts, pyrrolecarbonitrile boron-containing compounds, N-substituted-pyrrole-2-carbonitrile boron-containing compounds, and derivatives thereof is provided. The present invention also provides for the use of these boron-containing compounds and derivatives thereof in coupling reactions to provide bi-aryl compounds.Type: GrantFiled: September 26, 2008Date of Patent: March 6, 2012Assignee: Wyeth LLCInventors: Bogdan Kazimierz Wilk, Arkadiy Zinoviy Rubezhov, Jean Louise Helom
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Publication number: 20120053342Abstract: The present invention provides methods of forming carbamates, ureas, and isocyanates. In certain embodiments these methods include the step of reacting an amine with an ester-substituted diaryl carbonate to form an activated carbamate which can be further derivatized to form non-activated carbamate or a urea. The urea or carbamate can be subjected to a pyrolysis reaction to form isocyanate.Type: ApplicationFiled: November 4, 2011Publication date: March 1, 2012Applicant: SABIC INNOVATIVE PLASTICS IP B.V.Inventors: Hatem Abdallah Belfadhel, Hans-Peter Brack, Ricardo Godoy-Lopez, Dennis James Patrick Maria Willemse
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Publication number: 20120046462Abstract: The invention is directed to a process for the preparation of a chiral cyclic carbamate of formula and/or mirror image, and/or a salt thereof, from the corresponding o-aminobenzyl alcohol and/or salts thereof.Type: ApplicationFiled: April 9, 2010Publication date: February 23, 2012Inventors: Aleksander Warm, Miriam Lorenzi, Gareth Griffiths
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Publication number: 20120040974Abstract: 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: August 18, 2009Publication date: February 16, 2012Applicant: YALE UNIVERSITYInventors: William L. Jorgensen, Richard J. Bucala
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Patent number: 8114869Abstract: 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: May 12, 2011Date of Patent: February 14, 2012Assignee: Wyeth LLCInventors: Marc Sadler Tesconi, Mannching Sherry Ku, Yan Xu
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Publication number: 20120028920Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: ApplicationFiled: October 11, 2011Publication date: February 2, 2012Inventors: Hiroshi YAMASHITA, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20120022058Abstract: Mineralocorticoid receptor antagonists (MRa), pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, diabetic nephropathy and hypertension in mammals, including humans.Type: ApplicationFiled: March 26, 2010Publication date: January 26, 2012Inventors: Graciela Barbieri Arhancet, Agustin Casimiro-Garcia, Xiangyang Chen, David Hepworth, Marvin Jay Meyers, David Walter Piotrowski, Raj Kumar Raheja
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Publication number: 20120016118Abstract: 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 11, 2011Publication date: January 19, 2012Applicant: Wyeth LLCInventor: Bogdan Kazimierz Wilk
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Publication number: 20110319611Abstract: A benzoxazinone compound having the following formula (I): wherein one of R1 and R2 is H, and the other of R1 and R2 is a halogen group, and R1 and R2 cannot be the same at the same time; and R3, R4, R5, R6, and R7 are independently selected from the group consisting of H, a halogen group, a C1-C4 alkyl group, and a C1-C4 alkoxyl group.Type: ApplicationFiled: December 14, 2010Publication date: December 29, 2011Applicant: Chang Gung UniversityInventors: Pei-Wen Hsieh, Tsong-Long Hwang, Huang-Ping Yu
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Publication number: 20110312953Abstract: The present invention relates to novel anthranilic acid derivatives of the general formula (I) in which R1, R2, R3, R4, R5, Qx, A, Qy and n have the meanings given in the description, to their use as insecticides and acaricides for controlling animal pests, also in combination with other agents for activity boosting, and to a plurality of processes for their preparation.Type: ApplicationFiled: June 14, 2011Publication date: December 22, 2011Applicant: BAYER CROPSCIENCE AGInventors: Rùdiger FISCHER, Christoph GRONDAL, Markus HEIL, Heinz-Juergen WROBLOWSKY, Ernst Rudolf GESING, Arnd VOERSTE, Ulrich GÖGENS
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Patent number: 8080655Abstract: 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: GrantFiled: July 20, 2009Date of Patent: December 20, 2011Assignee: Apotex Pharmachem Inc.Inventors: Bo Chen, Zhi-Xian Wang, Yutao Xue, Lihong Liu, Hao Chen
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Patent number: 8071600Abstract: A heterocyclic compound or a salt thereof represented by the formula (1): where R2 represents a hydrogen atom or a lower alkyl group; A represents a lower alkylene group or lower alkenylene group; and R1 represents an aromatic group or a heterocyclic group. The compound of the present invention has a wide treatment spectrum for mental disorders including central nervous system disorders, no side effects and high safety.Type: GrantFiled: August 31, 2006Date of Patent: December 6, 2011Assignee: Otsuka Pharmaceutical Co., Ltd.Inventors: Hiroshi Yamashita, Hideaki Kuroda, Nobuaki Ito, Shin Miyamura, Kunio Oshima, Jun Matsubara, Haruka Takahashi, Tae Fukushima, Satoshi Shimizu, Kazumi Kondo, Yohji Sakurai, Takeshi Kuroda, Shinichi Taira, Motohiro Itotani, Tatsuyoshi Tanaka
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Publication number: 20110262369Abstract: The invention relates to a crystalline, enantiomerically pure hydrochloride salt of N-(5-{2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino]-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methane sulfonamide, preferably N-(5-{(R)-2-[3-(4,4-diethyl-2-oxo-4H-benzo[d][1,3]oxazin-1-yl)-1,1-dimethyl-propylamino]-1-hydroxy-ethyl}-2-hydroxy-phenyl)-methane sulfonamide, and the effect thereof as a long-term betamimetic agent, alone or combined with at least one other active ingredient, in the treatment of respiratory diseases.Type: ApplicationFiled: February 17, 2009Publication date: October 27, 2011Inventors: Ulrike Werthmann, Marco Santagostino, Adil Duran
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Publication number: 20110251199Abstract: The present invention comprises a new class of compounds capable of modulating Raf kinase and, accordingly, useful for treatment of Raf kinase mediated diseases, including melanomas, tumors and other cancer-related conditions. The compounds have a general Formula I and A1, A2, A3, A4, X, Z, Z?, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further comprises pharmaceutical compositions, methods for treatment of Raf kinase mediated diseases, and intermediates and processes useful for the preparation of compounds of the invention.Type: ApplicationFiled: June 17, 2011Publication date: October 13, 2011Applicant: Amgen Inc.Inventors: Frenel F. De Morin, Jian J. Chen, Elizabeth M. Doherty, Stephen Hitchcock, Qi Huang, Joseph L. Kim, Gang Liu, Thomas Nixey, Nick A. Paras, Jeffrey Petkus, Daniel M. Retz, Adrian L. Smith, Jiawang Zhu
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Publication number: 20110212953Abstract: 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: May 12, 2011Publication date: September 1, 2011Applicant: Wyeth LLCInventors: Marc Sadler Tesconi, Mannching Sherry Ku, Yan Xu
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Patent number: 8003784Abstract: 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: July 24, 2009Date of Patent: August 23, 2011Assignee: Wyeth LLCInventor: Bogdan Kazimierz Wilk
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Publication number: 20110196151Abstract: The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropy-lethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I) comprising reacting the intermediate of formula (II) [0045] as a free base or a salt thereof, with diphosgene (TCMCF, trichlormethylchloroformate) Cl3CO—COCl in an organic solvent or in a biphasic medium comprised of an organic solvent and water, preferably but not mandatorily in the presence of a weak base in an amount sufficient to neutralise the reaction mixture or in an up to 30% molar excess of such amount.Type: ApplicationFiled: January 30, 2009Publication date: August 11, 2011Inventors: Alessandro Leganza, Marco Galvagni
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Publication number: 20110195963Abstract: There is provided a novel carbamoyloxy arylalkanoyl arylpiperazine derivative compound having abundant racemic or enantiomeric characteristics, represented by the Formula 1, and pharmaceutically available salts or hydrates thereof. Also, there are provided a pharmaceutical composition for treating pain, anxiety or depression including an effective amount of the compound, and a method for treating pain, anxiety or depression in mammals by administering an effective amount of the compound to the mammals in need of treatment thereof.Type: ApplicationFiled: April 30, 2008Publication date: August 11, 2011Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
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Patent number: 7968709Abstract: 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: June 3, 2010Date of Patent: June 28, 2011Assignee: Wyeth LLCInventors: Marc Sadler Tesconi, Mannching Sherry Ku, Yan Xu
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Publication number: 20110124857Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.Type: ApplicationFiled: January 31, 2011Publication date: May 26, 2011Applicant: E. I. DU PONT DE NEMOURS AND COMPANYInventors: GEORGE PHILIP LAHM, THOMAS PAUL SELBY, THOMAS MARTIN STEVENSON