ZA200202947B - Methods of asymmetrically synthesizing enantiomers of casodex, its derivatives and intermediates thereof. - Google Patents
Methods of asymmetrically synthesizing enantiomers of casodex, its derivatives and intermediates thereof.Info
- Publication number
- ZA200202947B ZA200202947B ZA200202947A ZA200202947A ZA200202947B ZA 200202947 B ZA200202947 B ZA 200202947B ZA 200202947 A ZA200202947 A ZA 200202947A ZA 200202947 A ZA200202947 A ZA 200202947A ZA 200202947 B ZA200202947 B ZA 200202947B
- Authority
- ZA
- South Africa
- Prior art keywords
- casodex
- intermediates
- derivatives
- methods
- asymmetrically synthesizing
- Prior art date
Links
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 title 1
- LKJPYSCBVHEWIU-UHFFFAOYSA-N N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide Chemical compound C=1C=C(C#N)C(C(F)(F)F)=CC=1NC(=O)C(O)(C)CS(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-UHFFFAOYSA-N 0.000 title 1
- 229940097647 casodex Drugs 0.000 title 1
- 239000000543 intermediate Substances 0.000 title 1
- 230000002194 synthesizing effect Effects 0.000 title 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C315/00—Preparation of sulfones; Preparation of sulfoxides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
- C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
- C07C319/20—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides by reactions not involving the formation of sulfide groups
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C315/00—Preparation of sulfones; Preparation of sulfoxides
- C07C315/02—Preparation of sulfones; Preparation of sulfoxides by formation of sulfone or sulfoxide groups by oxidation of sulfides, or by formation of sulfone groups by oxidation of sulfoxides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
- C07C319/14—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of sulfides
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
- C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
- C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
- C07D317/32—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D317/34—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/07—Optical isomers
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16041299P | 1999-10-19 | 1999-10-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ZA200202947B true ZA200202947B (en) | 2003-09-23 |
Family
ID=22576803
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ZA200202947A ZA200202947B (en) | 1999-10-19 | 2002-04-15 | Methods of asymmetrically synthesizing enantiomers of casodex, its derivatives and intermediates thereof. |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US6583306B1 (xx) |
| EP (1) | EP1222165A2 (xx) |
| JP (1) | JP5112583B2 (xx) |
| KR (1) | KR20020091047A (xx) |
| CN (1) | CN1409702A (xx) |
| AU (1) | AU1968601A (xx) |
| BR (1) | BR0014889A (xx) |
| CA (1) | CA2387570A1 (xx) |
| CZ (1) | CZ20021340A3 (xx) |
| HK (1) | HK1048298A1 (xx) |
| HU (1) | HUP0203785A2 (xx) |
| IL (2) | IL149056A0 (xx) |
| MX (1) | MXPA02003884A (xx) |
| NO (1) | NO20021831L (xx) |
| NZ (1) | NZ518392A (xx) |
| PL (1) | PL354620A1 (xx) |
| WO (1) | WO2001028990A2 (xx) |
| ZA (1) | ZA200202947B (xx) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6995284B2 (en) | 2000-08-24 | 2006-02-07 | The University Of Tennessee Research Foundation | Synthesis of selective androgen receptor modulators |
| US7759520B2 (en) | 1996-11-27 | 2010-07-20 | University Of Tennessee Research Foundation | Synthesis of selective androgen receptor modulators |
| US6071957A (en) | 1996-11-27 | 2000-06-06 | The University Of Tennessee Research Corporation | Irreversible non-steroidal antagonist compound and its use in the treatment of prostate cancer |
| US8445534B2 (en) | 2000-08-24 | 2013-05-21 | University Of Tennessee Research Foundation | Treating androgen decline in aging male (ADAM)-associated conditions with SARMs |
| US6838484B2 (en) | 2000-08-24 | 2005-01-04 | University Of Tennessee Research Foundation | Formulations comprising selective androgen receptor modulators |
| US8008348B2 (en) | 2001-12-06 | 2011-08-30 | University Of Tennessee Research Foundation | Treating muscle wasting with selective androgen receptor modulators |
| US6998500B2 (en) | 2000-08-24 | 2006-02-14 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| US7026500B2 (en) | 2000-08-24 | 2006-04-11 | University Of Tennessee Research Foundation | Halogenated selective androgen receptor modulators and methods of use thereof |
| US7622503B2 (en) | 2000-08-24 | 2009-11-24 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| US6737550B2 (en) * | 2001-06-13 | 2004-05-18 | Biogal Gryogyszergyar Rt. | Process for preparing rac-bicalutamide and its intermediates |
| US8853266B2 (en) | 2001-12-06 | 2014-10-07 | University Of Tennessee Research Foundation | Selective androgen receptor modulators for treating diabetes |
| IL162340A0 (en) | 2001-12-06 | 2005-11-20 | Gtx Inc | Treating muscle wasting with selective androgen receptor modulators |
| JP4255381B2 (ja) | 2001-12-13 | 2009-04-15 | 住友化学株式会社 | ビカルタミドの結晶およびその製造方法 |
| DK1480634T3 (da) | 2002-02-07 | 2011-11-14 | Univ Tennessee Res Foundation | Selektive androgenreceptormodulatorer (SARM) til behandling af benign prostatahyperplasi |
| ATE533494T1 (de) | 2002-02-28 | 2011-12-15 | Univ Tennessee Res Foundation | Mehrfach substituierte selektive androgen- rezeptor-modulatoren und anwendungsverfahren dafür |
| WO2003074450A2 (en) | 2002-02-28 | 2003-09-12 | The University Of Tennessee Research Corporation | Radiolabeled selective androgen receptor modulators and their use in prostate cancer imaging and therapy |
| US7803970B2 (en) | 2002-02-28 | 2010-09-28 | University Of Tennessee Research Foundation | Multi-substitued selective androgen receptor modulators and methods of use thereof |
| US7772433B2 (en) | 2002-02-28 | 2010-08-10 | University Of Tennessee Research Foundation | SARMS and method of use thereof |
| DE10222104A1 (de) | 2002-05-17 | 2003-12-04 | Helm Ag | Verfahren zur Herstellung von N-(4'-Cyano-3'-trifluormethyl)-3-(4"-fluorphenylsulfonyl)-2-hydroxy-2-methylpropionamid |
| US7741371B2 (en) | 2002-06-17 | 2010-06-22 | University Of Tennessee Research Foundation | Selective androgen receptor modulators and methods of use thereof |
| CN100537520C (zh) | 2002-06-17 | 2009-09-09 | 田纳西大学研究基金会 | N-桥连选择性雄激素受体调节剂及其使用方法 |
| EP1402924B1 (de) * | 2002-09-04 | 2008-12-31 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Verwendung eines Mittel zur Therapie der Herzhypertrophie |
| US20040063782A1 (en) * | 2002-09-27 | 2004-04-01 | Westheim Raymond J.H. | Bicalutamide forms |
| US6818766B2 (en) * | 2002-10-02 | 2004-11-16 | Synthon Bv | Process for making bicalutamide and intermediates thereof |
| AU2003287077B2 (en) | 2002-10-15 | 2007-09-20 | University Of Tennessee Research Foundation | Methylene-bridged selective androgen receptor modulators and methods of use thereof |
| US8309603B2 (en) | 2004-06-07 | 2012-11-13 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| JP4322621B2 (ja) | 2003-10-16 | 2009-09-02 | 住友化学株式会社 | 4’−シアノ−3−[(4−フルオロフェニル)スルホニル]−2−ヒドロキシ−2−メチル−3’−トリフルオロメチルプロピオンアニリドの製造方法 |
| EP1631540A4 (en) | 2003-12-16 | 2006-10-04 | Gtx Inc | PRODRUGS OF SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHOD OF USE THEREOF |
| US9884038B2 (en) | 2004-06-07 | 2018-02-06 | University Of Tennessee Research Foundation | Selective androgen receptor modulator and methods of use thereof |
| US9889110B2 (en) | 2004-06-07 | 2018-02-13 | University Of Tennessee Research Foundation | Selective androgen receptor modulator for treating hormone-related conditions |
| WO2008013791A2 (en) * | 2006-07-24 | 2008-01-31 | University Of Delaware | Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal |
| US9844528B2 (en) | 2006-08-24 | 2017-12-19 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US10010521B2 (en) | 2006-08-24 | 2018-07-03 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| PT2054049E (pt) | 2006-08-24 | 2016-06-02 | Univ Tennessee Res Found | Acilanilidas substituídas e métodos de utilização das mesmas |
| US9730908B2 (en) | 2006-08-24 | 2017-08-15 | University Of Tennessee Research Foundation | SARMs and method of use thereof |
| US7968603B2 (en) | 2007-09-11 | 2011-06-28 | University Of Tennessee Research Foundation | Solid forms of selective androgen receptor modulators |
| WO2010116342A2 (en) * | 2009-04-10 | 2010-10-14 | Consiglio Nazionale Delle Ricerche | Non-steroidal compounds for androgen receptor modulation |
| ITBO20090236A1 (it) * | 2009-04-10 | 2010-10-11 | Consiglio Nazionale Ricerche | Procedimento per la sintesi di composti per il trattamento del tumore alla prostata |
| WO2011008543A2 (en) * | 2009-06-29 | 2011-01-20 | University Of Delaware | Pan-antagonists for the androgen receptor and androgen receptor mutants associated with anti-androgen withdrawal |
| CN103539710A (zh) * | 2012-07-02 | 2014-01-29 | 国药一心制药有限公司 | 一种(r)-比卡鲁胺的合成方法 |
| US9744149B2 (en) | 2012-07-13 | 2017-08-29 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US10987334B2 (en) | 2012-07-13 | 2021-04-27 | University Of Tennessee Research Foundation | Method of treating ER mutant expressing breast cancers with selective androgen receptor modulators (SARMs) |
| US9622992B2 (en) | 2012-07-13 | 2017-04-18 | Gtx, Inc. | Method of treating androgen receptor (AR)-positive breast cancers with selective androgen receptor modulator (SARMs) |
| US9969683B2 (en) | 2012-07-13 | 2018-05-15 | Gtx, Inc. | Method of treating estrogen receptor (ER)-positive breast cancers with selective androgen receptor modulator (SARMS) |
| US10258596B2 (en) | 2012-07-13 | 2019-04-16 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| US10314807B2 (en) | 2012-07-13 | 2019-06-11 | Gtx, Inc. | Method of treating HER2-positive breast cancers with selective androgen receptor modulators (SARMS) |
| IN2015DN01046A (xx) | 2012-07-13 | 2015-06-26 | Gtx Inc |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LU88769I2 (fr) * | 1982-07-23 | 1996-11-05 | Zeneca Ltd | Bicalutamide et ses sels et esters pharmaceutiquement acceptables (Casodex (R)) |
| GB8617652D0 (en) | 1986-07-18 | 1986-08-28 | Ici Plc | Acylanilide derivatives |
| WO1995019770A1 (en) * | 1994-01-21 | 1995-07-27 | Sepracor, Inc. | Methods and compositions for treating androgen-dependent diseases using optically pure r-(-)-casodex |
| AU7723198A (en) | 1997-06-04 | 1998-12-21 | University Of Tennessee Research Corporation, The | Non-steroidal radiolabeled agonist/antagonist compounds and their use in prostate cancer imaging |
| US6186674B1 (en) * | 1998-09-15 | 2001-02-13 | Lucent Technologies, Inc. | Optical sub-assembly package mount |
| US6252762B1 (en) * | 1999-04-21 | 2001-06-26 | Telcordia Technologies, Inc. | Rechargeable hybrid battery/supercapacitor system |
| US6331992B1 (en) * | 2000-04-07 | 2001-12-18 | Stratos Lightwave, Inc. | Small format optical subassembly |
| AU2002231027A1 (en) * | 2000-12-13 | 2002-06-24 | Teraconnect, Inc. | A packaging system for two-dimensional optoelectronic arrays |
| US6821032B2 (en) * | 2002-05-28 | 2004-11-23 | Intel Corporation | Methods of sealing electronic, optical and electro-optical packages and related package and substrate designs |
-
2000
- 2000-10-18 NZ NZ518392A patent/NZ518392A/en unknown
- 2000-10-18 CN CN00817022A patent/CN1409702A/zh active Pending
- 2000-10-18 US US09/691,621 patent/US6583306B1/en not_active Expired - Lifetime
- 2000-10-18 WO PCT/US2000/041233 patent/WO2001028990A2/en not_active Ceased
- 2000-10-18 KR KR1020027004966A patent/KR20020091047A/ko not_active Withdrawn
- 2000-10-18 JP JP2001531790A patent/JP5112583B2/ja not_active Expired - Fee Related
- 2000-10-18 CZ CZ20021340A patent/CZ20021340A3/cs unknown
- 2000-10-18 PL PL00354620A patent/PL354620A1/xx not_active Application Discontinuation
- 2000-10-18 IL IL14905600A patent/IL149056A0/xx unknown
- 2000-10-18 BR BR0014889-0A patent/BR0014889A/pt not_active Application Discontinuation
- 2000-10-18 CA CA002387570A patent/CA2387570A1/en not_active Abandoned
- 2000-10-18 HK HK03100367.2A patent/HK1048298A1/zh unknown
- 2000-10-18 MX MXPA02003884A patent/MXPA02003884A/es active IP Right Grant
- 2000-10-18 EP EP00982690A patent/EP1222165A2/en not_active Withdrawn
- 2000-10-18 HU HU0203785A patent/HUP0203785A2/hu unknown
- 2000-10-18 AU AU19686/01A patent/AU1968601A/en not_active Abandoned
-
2002
- 2002-04-09 IL IL149056A patent/IL149056A/en not_active IP Right Cessation
- 2002-04-15 ZA ZA200202947A patent/ZA200202947B/xx unknown
- 2002-04-18 NO NO20021831A patent/NO20021831L/no not_active Application Discontinuation
-
2003
- 2003-05-23 US US10/444,343 patent/US7022869B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| CN1409702A (zh) | 2003-04-09 |
| US6583306B1 (en) | 2003-06-24 |
| IL149056A0 (en) | 2002-11-10 |
| EP1222165A2 (en) | 2002-07-17 |
| CZ20021340A3 (cs) | 2002-08-14 |
| BR0014889A (pt) | 2002-12-31 |
| NO20021831L (no) | 2002-06-19 |
| NZ518392A (en) | 2004-02-27 |
| IL149056A (en) | 2011-05-31 |
| MXPA02003884A (es) | 2004-09-06 |
| US7022869B2 (en) | 2006-04-04 |
| AU1968601A (en) | 2001-04-30 |
| PL354620A1 (en) | 2004-02-09 |
| WO2001028990A2 (en) | 2001-04-26 |
| NO20021831D0 (no) | 2002-04-18 |
| CA2387570A1 (en) | 2001-04-26 |
| HUP0203785A2 (hu) | 2003-04-28 |
| HK1048298A1 (zh) | 2003-03-28 |
| JP5112583B2 (ja) | 2013-01-09 |
| KR20020091047A (ko) | 2002-12-05 |
| US20040030130A1 (en) | 2004-02-12 |
| JP2003512351A (ja) | 2003-04-02 |
| WO2001028990A3 (en) | 2001-09-07 |
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