Chalcogen Bonded Directly To The Oxazine Ring Patents (Class 544/92)
  • Patent number: 10954199
    Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.
    Type: Grant
    Filed: August 6, 2019
    Date of Patent: March 23, 2021
    Assignee: Gilead Sciences, Inc.
    Inventors: Stacy Bremner, Jerry Evarts, Keiko Sujino, Duong Tran, Dragos Vizitiu
  • Patent number: 10689353
    Abstract: This invention relates to a method for the manufacture of optically pure (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one. Specifically, this invention relates to a flow synthesis method for the manufacture of (S)-6-chloro-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-one.
    Type: Grant
    Filed: February 15, 2018
    Date of Patent: June 23, 2020
    Assignee: NELSON MANDELA METROPOLITAN UNIVERSITY
    Inventors: Paul Watts, Sravanthi Chada
  • Patent number: 10414737
    Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.
    Type: Grant
    Filed: July 2, 2018
    Date of Patent: September 17, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Stacy Bremner, Jerry B. Evarts, Keiko Sujino, Duong Tran, Dragos Vizitiu
  • Patent number: 10072024
    Abstract: The present invention relates to methods and compositions for inhibiting the activity of skin proteases, especially human kallikrein 7 (KLK7), human kallikrein 5 (KLK5), and human kallikrein 14 (KLK14). More specifically, the invention relates to the use of substituted 3,1-benzoxazin-4-ones being selective inhibitors of human skin kallikreins for the treatment of skin diseases, more specifically for the treatment of inflammatory skins diseases, especially Netherton syndrome.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: September 11, 2018
    Assignee: SIXERA PHARMA AB
    Inventors: Fredrik Wagberg, Goran Leonardsson
  • Patent number: 10059677
    Abstract: A process for the synthesis of benzoxazinone containing compounds which may be useful precursors for synthesizing compounds for the treatment of cancer, is hereby disclosed.
    Type: Grant
    Filed: December 28, 2016
    Date of Patent: August 28, 2018
    Assignee: Gilead Calistoga LLC
    Inventors: Stacy Bremner, Jerry Evarts, Keiko Sujino, Duong Tran, Dragos Vizitiu
  • Patent number: 9695194
    Abstract: The present invention relates to methods and compositions for inhibiting the activity of skin proteases, especially human kallikrein 7 (KLK7), human kallikrein 5 (KLK5), and human kallikrein 14 (KLK14). More specifically, the invention relates to the use of substituted 3,1-benzoxazin-4-ones being selective inhibitors of human skin kallikreins for the treatment of skin diseases, more specifically for the treatment of inflammatory skins diseases, especially Netherton syndrome.
    Type: Grant
    Filed: January 22, 2015
    Date of Patent: July 4, 2017
    Assignee: SIXERA PHARMA AB
    Inventors: Fredrik Wagberg, Goran Leonardsson
  • Patent number: 9567337
    Abstract: A process for the synthesis of quinazolinone containing compounds which may be useful for the treatment of cancer, is hereby disclosed. In addition, compound intermediates relating to these processes are also disclosed.
    Type: Grant
    Filed: December 18, 2014
    Date of Patent: February 14, 2017
    Inventors: Stacy Bremner, Jerry Evarts, Keiko Sujino, Duong Tran, Dragos Vizitiu
  • Publication number: 20150148340
    Abstract: The present application relates to novel bicyclically substituted uracil derivatives, to processes for preparation thereof, to the use thereof alone or in combinations for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases.
    Type: Application
    Filed: May 3, 2013
    Publication date: May 28, 2015
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Chantal Fürstner, Jens Ackerstaff, Alexander Straub, Heinrich Meier, Hanna Tinel, Katja Zimmermann, Adrian Tersteegen, Dmitry Zubov, Raimund Kast, Jens Schamberger, Martina Schäfer, Kirsten Börngen
  • Patent number: 9012445
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: January 12, 2013
    Date of Patent: April 21, 2015
    Assignee: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20150105548
    Abstract: The present invention relates to anti-HCV compounds, compositions comprising the same and methods of using the same to treat HCV infection.
    Type: Application
    Filed: May 25, 2012
    Publication date: April 16, 2015
    Inventors: Allan Krueger, Warren M. Kati, Clarence J. Maring, Rolf Wagner, Charles W. Hutchins
  • Patent number: 9006232
    Abstract: 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: Grant
    Filed: August 11, 2010
    Date of Patent: April 14, 2015
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Kazuki Nakayama, Daiki Sakai, Kazutoshi Watanabe, Toshiyuki Kohara, Keiichi Aritomo
  • Patent number: 8993751
    Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilic acid diamide derivatives of the formula (I) in which R1, R2, R3, R4, Q and Z have the meanings given in the description, by reacting benzoxazinones with amines.
    Type: Grant
    Filed: August 24, 2012
    Date of Patent: March 31, 2015
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Sergii Pazenok, Werner Lindner, Hartmut Scheffel
  • Patent number: 8981087
    Abstract: Compounds of formula (I): wherein: W is O, N—H, N-alkyl, N-alkenyl, N-alkynyl, N-aryl, N-heteroaryl or S; each X is independently CH or N; R1 is formula (b) or R3 is H, alkyl, NH2, OH, =0 or halogen; each A and B are independently CH or N; D is NHR4; R4 is H, alkyl, —C(O)-alkyl.
    Type: Grant
    Filed: July 23, 2010
    Date of Patent: March 17, 2015
    Assignee: Karus Therapeutics Limited
    Inventors: Stephen Joseph Shuttleworth, Franck Alexandre Silva, Alexander Richard Liam Cecil, Thomas James Hill
  • Patent number: 8969550
    Abstract: The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: March 3, 2015
    Assignee: Lonza Ltd.
    Inventors: Meinrad Brenner, Erick M. Carreira, Nicka Chinkov, Miriam Lorenzi, Aleksander Warm, Lothar Zimmermann
  • Patent number: 8957204
    Abstract: The invention is directed to a process for the preparation of a cyclic carbamate starting with a chiral propargylic alcohol and/or a suitable salt thereof, which is reacted with a cyclization agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane. Another aspect of the invention is directed to a process for the synthesis of said cyclic carbamate starting described above, wherein also a process for the preparation of the chiral propargylic alcohol is provided.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: February 17, 2015
    Assignee: Lonza Ltd.
    Inventors: Meinrad Brenner, Erick M. Carreira, Nicka Chinkov, Miriam Lorenzi, Aleksander Warm, Lothar Zimmermann
  • Patent number: 8921400
    Abstract: This invention provides a composition comprising a biologically effective amount of a compound of Formula 1, an N-oxide or an agriculturally suitable salt thereof wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure, and an effective amount of at least one fungicide.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: December 30, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
  • Patent number: 8907083
    Abstract: The invention provides a novel process for the synthesis of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one, the process comprising of reacting the salicylic acid with salicylamide in the presence of p-toluenesulfonyl chloride, base and solvent. The use of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one in the preparation of Deferasirox is also disclosed in the invention.
    Type: Grant
    Filed: August 23, 2011
    Date of Patent: December 9, 2014
    Assignee: Ramamohan Rao Davuluri
    Inventors: Ramamohan Rao Davuluri, Ravi Ponnaiah, Guruswamy Batthni, Chandra Murthy V. R. Medida, Santhosh Dummu
  • Publication number: 20140357628
    Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.
    Type: Application
    Filed: June 27, 2014
    Publication date: December 4, 2014
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, David Stapleton, Steven Zammit, Darren James Kelly, Richard Ernest Gilbert, Henry Krum
  • Publication number: 20140296230
    Abstract: The present invention encompasses compounds of general formula (I) wherein the groups R1 to R4 and A1 to A5 have the meanings given in the claims and in the specification. The compounds of the invention are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation pharmaceutical preparations containing such compounds and their uses as a medicament.
    Type: Application
    Filed: March 26, 2014
    Publication date: October 2, 2014
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Christian SMETHURST, Harald ENGELHARDT, Davide GIANNI, Ulrich REISER
  • Patent number: 8815852
    Abstract: 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: Grant
    Filed: April 30, 2008
    Date of Patent: August 26, 2014
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Ki Ho Lee, Han Ju Yi, Hyeon Cho, Dae Joong Im, Eun Hee Chae, Yeon Jung Choi
  • Publication number: 20140235628
    Abstract: This invention relates to compounds having structural Formula I: and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
    Type: Application
    Filed: September 10, 2012
    Publication date: August 21, 2014
    Inventors: Shawn Walsh, Alexander Pasternak, Brian Cato, Paul E. Finke, Jessica Frie, Qinghong Fu, Dooseop Kim, Barbara Pio, Aurash Shahripour, Zhi-Cai Shi, Haifeng Tang
  • Patent number: 8796266
    Abstract: 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: Grant
    Filed: May 30, 2013
    Date of Patent: August 5, 2014
    Assignee: Wyeth LLC
    Inventors: Puwen Zhang, Andrew Fensome, Eugene A. Terefenko, Lin Zhi, Todd K. Jones, James P. Edwards, Christopher M. Tegley, Jay E. Wrobel, Mark A. Collins
  • Patent number: 8791109
    Abstract: 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 to 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: Grant
    Filed: November 29, 2012
    Date of Patent: July 29, 2014
    Assignee: Wyeth LLC
    Inventors: Arwinder S. Nagi, Ramarao S. Chatlapalli, Shamim Hasan, Rolland W. Carson, Mohamed Ghorab
  • Publication number: 20140206676
    Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: January 12, 2013
    Publication date: July 24, 2014
    Applicant: Vanderbilt University
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
  • Publication number: 20140206681
    Abstract: The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds in the treatment of Btk mediated disorders.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 24, 2014
    Inventors: RONALD M. KIM, Jian Liu, Xiaolei Gao, Sobhana Babu Boga, Deodialsingh Guiadeen, Joseph A. Kozlowski, Wensheng Yu, Rajan Anand, Younong Yu, Oleg B. Selyutin, Ying-Duo Gao, Hao Wu, Shilan Liu, Chundao Yang, Hongjian Wang
  • Patent number: 8784684
    Abstract: A compound which has a benzoxazinone ring and an aromatic ring that directly bonds to the benzoxazinone ring, and has a mesogenic core substituted by a substituent having a polymerizable functional group is excellent in terms of durability, colorless, and exhibits a high ?n while having an azomethine bond.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: July 22, 2014
    Assignee: FUJIFILM Corporation
    Inventors: Satoshi Shimamura, Mitsuyoshi Ichihashi
  • Publication number: 20140194623
    Abstract: The present invention relates to a process for preparing tetrazole-substituted anthranilic acid diamide derivatives of the formula (I) in which R1, R2, R3, R4, Q and Z have the meanings given in the description, by reacting benzoxazinones with amines.
    Type: Application
    Filed: August 24, 2012
    Publication date: July 10, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Sergii Pazenok, Werner Lindner, Hartmut Scheffel
  • Patent number: 8772271
    Abstract: 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: Grant
    Filed: May 9, 2013
    Date of Patent: July 8, 2014
    Assignee: Wyeth LLC
    Inventors: Arwinder S. Nagi, Ramarao Chatlapalli, Shamim Hasan, Mohamed Ghorab, Dhaval Gaglani
  • Publication number: 20140140973
    Abstract: 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: Application
    Filed: January 27, 2014
    Publication date: May 22, 2014
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: GEORGE PHILIP LAHM, Stephen Frederick McCann, Kanu Maganbhai Patel, Thomas Paul Selby, Thomas Martin Stevenson
  • Patent number: 8710218
    Abstract: An improved process for Efavirenz, which has several advantages over reported methods like low cost, high yield, better optical purity and industrial feasibility.
    Type: Grant
    Filed: July 12, 2010
    Date of Patent: April 29, 2014
    Assignee: Lupin Limited
    Inventors: Girij Pal Singh, Gurvinder Pal Singh, Pravin Mahajan, Ganesh Salunke, Dabeer Karnalkar
  • Publication number: 20130338356
    Abstract: The invention provides a novel process for the synthesis of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one, the process comprising of reacting the salicylic acid with salicylamide in the presence of p-toluenesulfonyl chloride, base and solvent. The use of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one in the preparation of Deferasirox is also disclosed in the invention.
    Type: Application
    Filed: August 23, 2011
    Publication date: December 19, 2013
    Inventors: Ramamohan Rao Davuluri, Ravi Ponnaiah, Guruswamy Batthni, Chandra Murthy V. R. Medida, Santhosh Dummu
  • Publication number: 20130338151
    Abstract: 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: Application
    Filed: October 21, 2010
    Publication date: December 19, 2013
    Applicant: Fibrotech Therapeutics Pty Ltd
    Inventors: Spencer John Williams, Steven Zammit, Darren James Kelly
  • Patent number: 8604189
    Abstract: 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: Grant
    Filed: May 27, 2009
    Date of Patent: December 10, 2013
    Assignee: Emcure Pharmaceuticals Limited
    Inventors: Mukund Keshav Gurjar, Abdulrakheeb Abdulsubhan Deshmukh, Sanjay Shankar Deshmukh, Satish Ramanial Mehta
  • Publication number: 20130320260
    Abstract: A compound which has a benzoxazinone ring and an aromatic ring that directly bonds to the benzoxazinone ring, and has a mesogenic core substituted by a substituent having a polymerizable functional group is excellent in terms of durability, colorless, and exhibits a high ?n while having an azomethine bond.
    Type: Application
    Filed: August 7, 2013
    Publication date: December 5, 2013
    Applicant: FUJIFILM Corporation
    Inventors: Satoshi SHIMAMURA, Mitsuyoshi ICHIHASHI
  • Publication number: 20130317214
    Abstract: [Problem] To efficiently (without carrying out column purification) provide a high-purity maleate having excellent storage stability, solubility, crystallinity and ease of handling according to the present invention. [Solution] This method for producing the maleate represented by formula (1) includes obtaining the compound represented by formula (2) by reacting the compound represented by formula (3) with the compound represented by formula (4) in the presence of a salt, precipitating crystals of the compound represented by formula (2) by mixing the obtained compound represented by formula (2) with acetone and water, and obtaining the maleate represented by formula (1) by adding maleic acid to an acetone solution of the compound represented by formula (2), prepared by dissolving the crystals of the obtained compound represented by formula (2) in acetone.
    Type: Application
    Filed: November 30, 2011
    Publication date: November 28, 2013
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventor: Takeshi Tsubuki
  • Publication number: 20130317215
    Abstract: [Problem] To provide a stable industrially-manufactured intermediate, enabling an industrially stable supply of 2-pyridyl-benz[d][1,3]oxazine to be provided. [Solution] The compound represented by formula (6) (wherein M represents sodium or potassium).
    Type: Application
    Filed: November 30, 2011
    Publication date: November 28, 2013
    Applicant: KYORIN PHARMACEUTICAL CO., LTD.
    Inventors: Takeshi Tsubuki, Takahiro Tanase, Masashi Suzuki
  • Patent number: 8541409
    Abstract: 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: Grant
    Filed: April 30, 2008
    Date of Patent: September 24, 2013
    Assignee: SK Biopharmaceuticals Co., Ltd.
    Inventors: Byong Sung Kwak, Hong Sik Moon, Han Ju Yi, Young Soon Kang, Dae Joong Im, Eun Hee Chae, Sang Mi Chae, Ki Ho Lee
  • Publication number: 20130231333
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Application
    Filed: September 15, 2011
    Publication date: September 5, 2013
    Applicant: ARAGON PHARMACEUTICALS, INC.
    Inventors: Nicholas D. Smith, Mehmet Kahraman, Steven P. Govek, Johnny Y. Nagasawa, Andiliy G. Lai, Jackaline D. Julien, Mark R. Herbert, Celine Bonnefous, Karensa L. Douglas
  • Publication number: 20130217875
    Abstract: The invention is directed to a process for the preparation of a cyclic carbamate starting with a chiral propargylic alcohol and/or a suitable salt thereof, which is reacted with a cyclisation agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction is carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane. Another aspect of the invention is directed to a process for the synthesis of said cyclic carbamate starting described above, wherein also a process for the preparation of the chiral propargylic alcohol is provided.
    Type: Application
    Filed: October 14, 2011
    Publication date: August 22, 2013
    Applicant: LONZA LTD
    Inventors: Meinrad Brenner, Erick M. Carreira, Nicka Chinkov, Miriam Lorenzi, Aleksander Warm, Lothar Zimmermann
  • Publication number: 20130211077
    Abstract: The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclisation agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane.
    Type: Application
    Filed: October 14, 2011
    Publication date: August 15, 2013
    Applicant: LONZA LTD
    Inventors: Meinrad Brenner, Erick M. Carreira, Nicka Chinkov, Miriam Lorenzi, Aleksander Warm, Lothar Zimmermann
  • Publication number: 20130165650
    Abstract: A process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-3,1-benzoxazin-2-one, of formula (I): comprising reacting the intermediate of formula (II): as a free base or a salt thereof, with diphosgene (TCMCF, trichloromethylchloroformate) 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 neutralize the reaction mixture or in an up to 30% molar excess of such amount.
    Type: Application
    Filed: February 26, 2013
    Publication date: June 27, 2013
    Applicant: F.I.S. Fabbrica Italiana Sintetici S.p.A
    Inventor: F.I.S. Fabbrica Italiana Sintetici S.p.A
  • Patent number: 8466279
    Abstract: 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: Grant
    Filed: July 3, 2012
    Date of Patent: June 18, 2013
    Assignee: Hetero Drugs Limited
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
  • Publication number: 20130137684
    Abstract: The present invention generally relates to compounds that inhibit haematopoietic-prostaglandin D2 synthase (H-PGDS), to compositions containing them and to their use in treating or preventing conditions and diseases associated with H-PGDS, such as allergies and inflammation.
    Type: Application
    Filed: June 1, 2011
    Publication date: May 30, 2013
    Applicant: THE UNIVERSITY OF QUEENSLAND
    Inventors: Mark Leslie Smythe, Jack Urquhart Flanagan
  • Patent number: 8450312
    Abstract: 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: Grant
    Filed: April 1, 2010
    Date of Patent: May 28, 2013
    Assignee: Wyeth LLC
    Inventors: Arwinder S. Nagi, Ramarao Chatlapalli, Shamim Hasan, Mohamed Ghorab, Dhaval Gaglani
  • Patent number: 8420808
    Abstract: The present invention is directed to a process for the preparation of Efavirenz, (4S)-6-chloro-4-(cyclopropylethynyl)-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: Grant
    Filed: January 30, 2009
    Date of Patent: April 16, 2013
    Assignee: F.I.S. Fabbrica Italiana Sintetici S.p.A.
    Inventors: Alessandro Leganza, Marco Galvagni
  • Publication number: 20130079511
    Abstract: The oxidative functionalization of olefins is a common method for the formation of vicinal carbon-heteroatom bonds. However, oxidative methods to transform allenes into synthetic motifs containing three contiguous carbon-heteroatom bonds are much less developed. The use of bicyclic methylene aziridines (MAs), prepared via intramolecular allene aziridination, as scaffolds for functionalization of all three allene carbons, among other reactions, is described herein.
    Type: Application
    Filed: August 29, 2012
    Publication date: March 28, 2013
    Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATION
    Inventors: Jennifer SCHOMAKER, Luke BORALSKY, John HERSHBERGER, Jared RIGOLI, Christopher S. ADAMS
  • Publication number: 20130079338
    Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, antagonists of the NR2B receptor and may be useful for the treatment of various disorders of the central nervous system.
    Type: Application
    Filed: September 24, 2012
    Publication date: March 28, 2013
    Applicant: BRISTOL-MYERS SQUIBB COMPANY
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8389698
    Abstract: A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
    Type: Grant
    Filed: June 26, 2009
    Date of Patent: March 5, 2013
    Assignee: Wyeth LLC
    Inventors: Li Shen, Kelly Keating, Oliver McConnell, William DeMaio, Appavu Chandrasekaran
  • Patent number: 8383811
    Abstract: 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: Grant
    Filed: December 22, 2008
    Date of Patent: February 26, 2013
    Assignee: Hetero Research Foundation
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
  • Publication number: 20130028879
    Abstract: 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: Application
    Filed: August 10, 2012
    Publication date: January 31, 2013
    Applicant: E I DU PONT DE NEMOURS AND COMPANY
    Inventors: GEORGE PHILIP LAHM, STEPHEN FREDERICK MCCANN, KANU MAGANBHAI PATEL, THOMAS PAUL SELBY, THOMAS MARTIN STEVENSON