The Hetero Ring Contains Nitrogen Patents (Class 540/95)
-
Patent number: 11801252Abstract: The present disclosure relates to a pharmaceutical composition. Specifically, a pharmaceutical composition of abiraterone acetate is provided, wherein a 300 mg dose of abiraterone acetate is bioequivalent to a 1000 mg dose of Zytiga® in healthy male subjects in a fasting state.Type: GrantFiled: March 4, 2022Date of Patent: October 31, 2023Assignee: Jiangsu Hengrui Pharmaceuticals Co., Ltd.Inventors: Caiyun Pan, Ailing Chen, Kai Pan, Kai Liu, Zhirong Mo
-
Patent number: 11756656Abstract: A method is provided for treating or preventing symptoms of asthma in a subject in need thereof by administering a corticosteroid pharmaceutical composition to a subject qualified for over-the-counter access to the corticosteroid pharmaceutical composition. In some embodiments, the corticosteroid pharmaceutical composition includes a class B corticosteroid, a glucocorticosteroid, budesonide, ciclesonide, fluticasone furoate, mometasone furoate, fluticasone propionate, or beclomethasone dipropionate.Type: GrantFiled: June 13, 2019Date of Patent: September 12, 2023Assignee: ASTRAZENECA UK LIMITEDInventors: Robert Peter Prybolsky, Judy Firor
-
Patent number: 9970139Abstract: The invention refers to a process for the preparation of a microfibrous non-woven fabric based on polyester or polyamide microfibers immersed in a polyurethane matrix, and having a thickness equal to or less than 0.65 mm, a flat or slightly mottled appearance and a nap length of less than 350 ?m. The non-woven fabric is used for the preparation of coverings for consumer goods, particularly for the preparation of covers and cases for electronic products.Type: GrantFiled: March 25, 2016Date of Patent: May 15, 2018Assignee: ALCANTARA S.P.A.Inventors: Giovanni Belloni, Carmine Carlo Ammirati, Giovanni Addino, Francesco Panetti, Walter Cardinali, Gianni Romani, Carlo Costa, Marcello Concezzi
-
Patent number: 9676815Abstract: The present invention relates to a novel process for the synthesis of abiraterone and in particular abiraterone acetate, a compound of formula (I) reported below: having pharmacological activity suitable for slowing down the progression of advanced stage prostate cancer. The process is characterized by the fact that the intermediate triflation step is carried out on prasterone (DHEA) or its 3-acetate using Ar—N(OTf)2 as the triflation reagent, but where Ar is not phenyl, and by the fact that the base used in this step is an alkali metal alcoholate.Type: GrantFiled: July 23, 2014Date of Patent: June 13, 2017Assignee: INDUSTRIALE CHIMICA S.R.L.Inventors: Roberto Lenna, Riccardo Di Brisco
-
Patent number: 9663550Abstract: A method for preparing abiraterone acetate.Type: GrantFiled: August 19, 2014Date of Patent: May 30, 2017Assignees: Wuhan Biocause Pharmaceutical Development Co., Ltd., Wuhan Biocause Pharmaceutical Co., Ltd.Inventors: Zhigang Cheng, Xuyong Dai, Xudong Wang, Shaokui Li, Liwei Li, Siyu He, Sen Cheng
-
Patent number: 9650410Abstract: The present invention relates to a novel process for the synthesis of abiraterone, and in particular of abiraterone acetate, compound of formula (I) reported below: N O (I) which has pharmacological activity useful for slowing down the progression of prostate cancer at an advanced stage. The process is characterized by an intermediate step wherein DHEA-acetate is triflated using Ar—N(OTf)2 as the triflation reagent.Type: GrantFiled: July 29, 2013Date of Patent: May 16, 2017Assignee: INDUSTRIALE CHIMICA S.R.L.Inventors: Roberto Lenna, Riccardo Di Brisco
-
Patent number: 9637516Abstract: The invention relates to novel betulinic acid derivatives and related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.Type: GrantFiled: December 26, 2013Date of Patent: May 2, 2017Assignee: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Lanka Vl Subrahmanyam, Gazula Levi David Krupadanam, Mukkera Venkati, Neela Sudhakar, Kallem Srinivas Reddy
-
Patent number: 9556218Abstract: The present invention provides intermediates for preparing abiraterone, and processes for preparing abiraterone and intermediates thereof. The intermediates include a compound of formula (IV): wherein R represents a hydroxy-protecting group.Type: GrantFiled: June 26, 2014Date of Patent: January 31, 2017Assignee: ScinoPharm Taiwan, Ltd.Inventors: Lung-Huang Kuo, Hsiao-Ping Fang, Ming-Feng Wu, Yu-Sheng Chang
-
Patent number: 9512169Abstract: The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.Type: GrantFiled: July 5, 2013Date of Patent: December 6, 2016Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Ulrich Bothe, Matthias Busemann, Oliver Martin Fischer, Naomi Barak, Andrea Rotgeri, Tobias Marquardt, Christian Stegmann
-
Patent number: 9359395Abstract: Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and phamacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.Type: GrantFiled: July 10, 2014Date of Patent: June 7, 2016Assignee: Tokai Pharmaceuticals, Inc.Inventor: David S. Casebier
-
Patent number: 9353145Abstract: The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-formate intermediate.Type: GrantFiled: October 9, 2012Date of Patent: May 31, 2016Assignee: ZACH SYSTEMInventors: Yvon Derrien, Patricia Poirier, Massimiliano Forcato, Tony Pintus, Livius Cotarca, Sebastien Meunier, Laurence Graindorge
-
Patent number: 9315541Abstract: Disclosed is a method for the conversion of a compound of formula 3 to a compound of formula 4, wherein R is an acetyl group or an alcohol-protecting group. The process involves reacting 3 with a triflating agent in the presence of a nicotinate (3-pyridinecarboxylate) of a C1-C4 alcohol, preferably methyl nicotinate (methyl 3-pyridinecarboxylate) or ethyl nicotinate (ethyl 3-pyridinecarboxylate), to give 4. The method can be conveniently used in a process for the preparation of Abiraterone or Abiraterone acetate.Type: GrantFiled: May 15, 2015Date of Patent: April 19, 2016Assignee: OLON S.P.A.Inventors: Marco Alpegiani, Tania Cristiano
-
Publication number: 20150139905Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.Type: ApplicationFiled: October 9, 2014Publication date: May 21, 2015Inventors: Dinesh Chimmanamada, Weiwen Ying
-
Publication number: 20150133652Abstract: Provided are acetaic abiraterone trifluoroacetate, a preparation method and an application of same. The acetaic abiraterone trifluoroacetate is obtained through a salt-forming reaction between acetaic Abiraterone and trifluoroacetic acid. The acetaic abiraterone trifluoroacetate undergoes self-purification through recrystallization, and dissociation and recrystallization are performed on the purified abiraterone acetate trifluoroacetate, so that the obtained acetaic abiraterone has a high purity, a high yield and stable quality, and is capable of meeting the requirement for mass production of acetaic abiraterone.Type: ApplicationFiled: February 20, 2013Publication date: May 14, 2015Inventors: Xiaoxia An, Chengjun Huang, Fengwang Mao
-
Publication number: 20150051179Abstract: Steroidal C-17 nitrogen-containing heterocycles of Formula I: wherein: the ABCD ring structure is the nucleus of a steroid, or an analog thereof; X is a group capable of coordinating a heme group of CYP17, and Y is an hydroxyl functionality, a suitable ester, or a prodrug group, for the treatment of urogenital and/or androgen-related cancers, such as castration-resistant prostate cancer. The invention provides methods of synthesizing new chemical entities and methods of using the same in treating urogenital and/or androgen-related cancers.Type: ApplicationFiled: June 24, 2014Publication date: February 19, 2015Inventor: David Casebier
-
Publication number: 20150005489Abstract: The present invention provides intermediates for preparing abiraterone, and processes for preparing abiraterone and intermediates thereof. The intermediates include a compound of formula (IV): wherein R represents a hydroxy-protecting group.Type: ApplicationFiled: June 26, 2014Publication date: January 1, 2015Inventors: Lung-Huang Kuo, Hsiao-Ping Fang, Ming-Feng Wu, Yu-Sheng Chang
-
Publication number: 20140287039Abstract: Pharmaceutical compositions, including unit dosage forms, comprising fine particle abiraterone acetate with or without an antioxidant and or a sequestering agent as well as methods for producing and using such compositions are described.Type: ApplicationFiled: March 17, 2014Publication date: September 25, 2014Applicant: ICEUTICA INC.Inventors: H. William Bosch, Marck Norret, Paul Nemeth, Matt Callahan
-
Publication number: 20140256932Abstract: The present invention relates to a process for the preparation of 17-substituted steroids and, more particularly, to an improved method of synthesizing abiraterone or derivatives thereof in high yield and purity by means of a key 3-formate intermediate.Type: ApplicationFiled: October 9, 2012Publication date: September 11, 2014Applicant: ZACH SYSTEMInventors: Yvon Derrien, Patricia Poirier, Massimiliano Forcato, Tony Pintus, Livius Cotarca, Sebastien Meunier, Laurence Graindorge
-
Publication number: 20140249119Abstract: The invention relates to AKR1C3 inhibitors and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular bleeding disorders and endometriosis.Type: ApplicationFiled: September 24, 2012Publication date: September 4, 2014Inventors: Ulrich Bothe, Naomi Barak, Matthias Busemann, Oliver Martin Fischer, Andrea Rotgeri, Isabella Gashaw, Ingo Hartung, Tobias Marquardt
-
Patent number: 8822501Abstract: Disclosed is a composition for use as a pest control agent, comprising a compound represented by formula (I) or an agriculturally and horticulturally acceptable salt thereof as active ingredient and an agriculturally and horticulturally acceptable carrier:Type: GrantFiled: January 3, 2013Date of Patent: September 2, 2014Assignees: Meiji Seika Pharma Co., Ltd., The Kitasato InstituteInventors: Kimihiko Goto, Ryo Horikoshi, Mariko Tsuchida, Kazuhiko Oyama, Satoshi Omura, Hiroshi Tomoda, Toshiaki Sunazuka
-
Patent number: 8791095Abstract: Steroidal C-17 nitrogen-containing heterocycles of Formula I: wherein: the ABCD ring structure is the nucleus of a steroid, or an analog thereof, X is a group capable of coordinating a heme group of CYP17, and Y is an hydroxyl functionality, a suitable ester, or a prodrug group, for the treatment of urogenital and/or androgen-related cancers, such as castration-resistant prostate cancer. The invention provides methods of synthesizing new chemical entities and methods of using the same in treating urogenital and/or androgen-related cancers.Type: GrantFiled: February 5, 2010Date of Patent: July 29, 2014Assignee: Tokai Pharmaceuticals, Inc.Inventor: David Casebier
-
Patent number: 8791094Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. Such compounds include inhibitors of cytochrome C17?-hydroxylase/C17,20-lyase such as 3-?-Hydroxy-17-(1H-benzimidazol-1-yl)androsta-5,16-diene.Type: GrantFiled: August 5, 2010Date of Patent: July 29, 2014Assignee: Tokai Pharmaceuticals, Inc.Inventors: Jodie Pope Morrison, Cy Aaron Stein, David Scott Casebier
-
Publication number: 20140155363Abstract: The present invention relates to a process for the synthesis of (3beta)17-(3-pyridinyl)androsta-5,16-dien-3-yl acetate (Abiraterone acetate) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates in such processes.Type: ApplicationFiled: February 10, 2014Publication date: June 5, 2014Applicant: MAPI PHARMA LTD.Inventors: Ehud MAROM, Shai RUBNOV, Michael MIZHIRITSKII
-
Publication number: 20140011992Abstract: The present invention relates to processes for obtaining abiraterone and derivatives thereof, such as abiraterone acetate, by means of a Suzuki coupling through a steroid borate of general formula (IV) or a C—C coupling through a steroid hydrazone of general formula (II), as well as to intermediates useful in said processes.Type: ApplicationFiled: December 20, 2012Publication date: January 9, 2014Applicant: CRYSTAL PHARMA, S.A.U.Inventors: Alfonso Perez Encabo, Jose Angel Turiel Hernandez, Francisco Javier Gallo Nieto, Antonio Lorente Bonde-Larsen, Celso Miguel Sandoval Rodriguez
-
Publication number: 20140005132Abstract: The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase ?4 and are useful as contraceptive agents.Type: ApplicationFiled: July 1, 2013Publication date: January 2, 2014Applicants: REGENTS OF THE UNIVERSITY OF MINNESOTA, THE UNIVERSITY OF KANSASInventors: Gustavo Blanco, Gunda I. Georg, Shameem Sultana Syeda
-
Publication number: 20140005156Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.Type: ApplicationFiled: August 28, 2013Publication date: January 2, 2014Applicant: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)Inventors: MARC POIROT, PHILIPPE DE MEDINA, SANDRINE POIROT
-
Publication number: 20130252930Abstract: Provided herein are inhibitors of CYP11B, CYP17, and/or CYP21 enzymes of Formula (Z), (IX), (X), (XI), (XII), (XIII), (XIV), (XV), (XVI), or (XVII). Also described herein are pharmaceutical compositions that include at least one compound described herein and the use of a compound or pharmaceutical composition described herein to treat androgen-dependent diseases, disorders and conditions.Type: ApplicationFiled: December 16, 2011Publication date: September 26, 2013Applicant: BIOMARIN PHARMACEUTICAL INC.Inventors: Daniel Chu, Bing Wang, Tao Ye
-
Patent number: 8524694Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.Type: GrantFiled: April 1, 2011Date of Patent: September 3, 2013Assignee: Institut National de la Sante et de la Recherche Medicale (INSERM)Inventors: Marc Poirot, Philippe De Medina, Sandrine Poirot
-
Publication number: 20130123224Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.Type: ApplicationFiled: November 9, 2012Publication date: May 16, 2013Applicant: SUZHOU NEUPHARMA CO., LTD.Inventor: SUZHOU NEUPHARMA CO., LTD.
-
Publication number: 20130090468Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).Type: ApplicationFiled: November 26, 2012Publication date: April 11, 2013Applicant: BTG International LimitedInventor: BTG International Limited
-
Patent number: 8389714Abstract: A compound of formula (I) or a pharmaceutically-acceptable salt thereof, may be made by a process including a triflating step by which a ketone of formula (II) is converted into a triflate of formula (III) in the presence of a base comprising a tertiary or heterocyclic amine such that the pKa of the conjugate acid at 25° C. is within the range 5.21 to 12.Type: GrantFiled: July 27, 2011Date of Patent: March 5, 2013Assignee: BTG International LimitedInventor: Paul S Bury
-
Patent number: 8338588Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).Type: GrantFiled: November 2, 2011Date of Patent: December 25, 2012Assignee: BTG International LimitedInventor: Neil John Hunt
-
Patent number: 8334280Abstract: The invention relates to novel ligands of the estrogen receptors ? and ? of general formula II, which are useful as an active substance of pharmaceuticals, for example pharmaceutical compositions useful for hormone replacement therapy, as well as for the treatment of tumors and inflammatory diseases. The invention also relates to a novel preparation method of these ligands comprising cyclotrimerization of ethynylestradiol with the appropriate diyne in an organic solvent. Further, the invention relates to pharmaceuticals comprising the novel compounds according to the invention.Type: GrantFiled: May 5, 2009Date of Patent: December 18, 2012Assignees: Ustav Molekularni Genetikv AV CR, V.V.I., Ustav Organicke Chemie A Biochemie AV CR, V.V.I., Univerzita Karlova V Praze, Prirodovedecka Fukulta UKInventors: Petr Novak, David Sedlak, Petr Bartunek, Martin Kotora
-
Publication number: 20120282331Abstract: Described herein, in certain embodiments, are steroidal derivatives, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions.Type: ApplicationFiled: November 9, 2010Publication date: November 8, 2012Applicant: TOKAI PHARMACEUTICALS, INC.Inventors: Scott C. Chappel, David S. Casebier
-
Patent number: 8236946Abstract: Process for the preparation of a compound of formula (I) as defined herein by (i) triflating a ketone of formula (II) as defined herein to form a triflate of formula (III) as defined herein and (ii) reacting the compound of the formula (III) to form a compound of the formula (I) or a pharmaceutically-acceptable salt thereof. The triflating step is conducted in the presence of a base comprising a tertiary or heterocyclic amine such that the pKa of the conjugate acid at 25° C. is within the range 5.21 to 12. The base is selected from pyridine, 2,6-lutidine, N-methylmorpholine, 1,4-diazabicyclo[2.2.2]octane (DABCO), trimethylamine, triethylamine, N,N-diisopropylethylamine (DIPEA), quinuclidine and 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU).Type: GrantFiled: August 23, 2005Date of Patent: August 7, 2012Assignee: BTG International LimitedInventor: Paul S Bury
-
Publication number: 20120190659Abstract: Compounds of Structural Formula I or pharmaceutically acceptable salts thereof, are effective inhibitors of angiogenesis:Type: ApplicationFiled: April 16, 2010Publication date: July 26, 2012Applicants: Children's Medical Center Corporation, President and Fellows of Harvard CollegeInventors: Elias James Corey, Barbara Czakó, László Kürti, Akiko Mammoto, Donald E. Ingber
-
Publication number: 20120053162Abstract: Chemical entities that are bufalin derivatives, pharmaceutical compositions and methods of treatment of cancer are described.Type: ApplicationFiled: August 26, 2011Publication date: March 1, 2012Inventor: Xiangping Qian
-
Publication number: 20110312926Abstract: Novel chemical agents are described herein. More specifically, 2-(N-substituted piperazinyl) pregnane and 2-(N-substituted piperazinyl) androstane derivatives exhibiting cytotoxicity on a variety of cancer cell lines are disclosed herein.Type: ApplicationFiled: November 25, 2009Publication date: December 22, 2011Applicant: UNIVERSITE LAVALInventors: Donald Poirier, Jenny Roy, Rene Maltais
-
Publication number: 20110312924Abstract: Steroidal C-17 nitrogen-containing heterocycles of Formula I: wherein: the ABCD ring structure is the nucleus of a steroid, or an analog thereof; X is a group capable of coordinating a heme group of CYP17, and Y is an hydroxyl functionality, a suitable ester, or a prodrug group, for the treatment of urogenital and/or androgen-related cancers, such as castration-resistant prostate cancer. The invention provides methods of synthesizing new chemical entities and methods of using the same in treating urogenital and/or androgen-related cancers.Type: ApplicationFiled: February 5, 2010Publication date: December 22, 2011Applicant: TOKAI PHARMACEUTICALS, INC.Inventor: David Casebier
-
Publication number: 20110312916Abstract: Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and pharmacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.Type: ApplicationFiled: February 5, 2010Publication date: December 22, 2011Applicant: TOKAI PHARMACEUTICALS, INC.Inventor: David Casebier
-
Publication number: 20110288288Abstract: A compound of formula (I) or a pharmaceutically-acceptable salt thereof, may be made by a process including a triflating step by which a ketone of formula (II) is converted into a triflate of formula (III) in the presence of a base comprising a tertiary or heterocyclic amine such that the pKa of the conjugate acid at 25° C. is within the range 5.21 to 12.Type: ApplicationFiled: July 27, 2011Publication date: November 24, 2011Applicant: BTG International LimitedInventor: Paul S. Bury
-
Publication number: 20110275604Abstract: Sterol derivatives of formula (I) and a method for the production of the compounds, a medicament using one of the compounds and a pharmaceutical composition comprising the medicament.Type: ApplicationFiled: April 1, 2011Publication date: November 10, 2011Applicant: INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM)Inventors: Marc POIROT, Philippe De Medina, Sandrine Poirot
-
Publication number: 20110212935Abstract: The invention relates to the use of compounds to ameliorate or treat an condition such as a cystic fibrosis, neutropenia or other exemplified conditions. Exemplary compounds that can be used include 3?-hydroxy-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 3?-hydroxy-16?-fluoro-17?-aminoandrost-5-ene, 1?,3?-dihydroxy-4?-fluoroandrost-5-ene-17-one, 1?,3?,17?-trihydroxy-4?-fluoroandrost-5-ene, 1?,3?-dihydroxy-6?-bromoandrost-5-ene, 1?-fluoro-3?,12?-dihydroxyandrost-5-ene-17-one, 1?-fluoro-3?,4?-dihydroxyandrost-5-ene and 4?-fluoro-3?,6?,17?-trihydroxyandrostane.Type: ApplicationFiled: April 27, 2011Publication date: September 1, 2011Applicant: Harbor BioSciences, Inc.Inventor: James M. Frincke
-
Publication number: 20110034428Abstract: Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions. The present invention provides therapies and therapeutic regimens for the treatment of prostate cancer.Type: ApplicationFiled: August 5, 2010Publication date: February 10, 2011Applicant: TOKAI PHARMACEUTICALS, INC.Inventors: Jodie Pope Morrison, Cy Aaron Stein, David Scott Casebier
-
Publication number: 20100152437Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).Type: ApplicationFiled: February 4, 2010Publication date: June 17, 2010Applicant: BTG International LimitedInventor: Neil John Hunt
-
Patent number: 7700766Abstract: A salt of a compound of formula (I) may be made with methanesulfonic acid. The salt and salts with other acids may be prepared by recovering from methyl tert-butyl ether (MTBE).Type: GrantFiled: August 23, 2005Date of Patent: April 20, 2010Assignee: BTG International LimitedInventor: Neil John Hunt
-
Publication number: 20100047338Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.Type: ApplicationFiled: October 9, 2009Publication date: February 25, 2010Inventors: Angela Brodie, Vincent Njar
-
Publication number: 20100036115Abstract: This invention features permeability enhancer molecules, and methods, to increase membrane permeability of various molecules, such as nucleic acids, polynucleotides, oligonucleotides, enzymatic nucleic acid molecules, antisense nucleic acid molecules, 2-5A antisense chimeras, triplex forming oligonucleotides, decoy RNAs, dsRNAs, siRNAs, aptamers, or antisense nucleic acids containing nucleic acid cleaving chemical groups, peptides, polypeptides, proteins, carbohydrates, steroids, metals and small molecules, thereby facilitating cellular uptake of such molecules.Type: ApplicationFiled: May 21, 2009Publication date: February 11, 2010Applicant: Sirna Therapeutics, Inc.Inventors: Leonid Beigelman, Nilabh Chaudhary, Peter Haeberli, Alexander Karpeisky, Jasenka Matulic-Adamic, John Min, Mark Reynolds, David Sweedler
-
Publication number: 20080280864Abstract: Described are steroidal C-17 benzoazoles, pyrimidinoazoles (azabenzoazoles) and diazines. Methods for their synthesis are also described, which include methods having a step of nucleophilic vinylic “addition-elimination” substitution reaction of 3?-acetoxy-17-chloro-16-formylandrosta-5,16-diene or analogs thereof and benzoazole or pyrimidinoazole nucleophiles and methods having a palladium catalyzed cross-coupling reaction of 17-iodoandrosta-5,16-dien-3?-ol or analogs thereof with tributylstannyl diazines. The compounds are potent inhibitors of human CYP 17 enzyme as well as potent antagonists of both wild type and mutant androgen receptors (AR). The compounds are useful for the treatment of human prostate cancer.Type: ApplicationFiled: March 2, 2006Publication date: November 13, 2008Inventors: Angela Brodie, Vincent Njar
-
Publication number: 20030096799Abstract: The application discloses novel 2-alkoxyestradiol analogs which exhibit anti-proliferative properties, and methods of making and using such compounds to inhibit undesired cell proliferation and tumor growth. Additionally, methods are disclosed of treating diseases associated with undesired angiogenesis and undesired proliferation, and methods of treating infectious disease wherein the infectious agent is particularly susceptible to inhibition by agents that disrupt microtubule organization and function.Type: ApplicationFiled: June 11, 2002Publication date: May 22, 2003Inventors: Pemmaraju Narasimha Rao, Susan L. Mooberry, James W. Cessac, Tina L. Tinley