ES2072848T3 - Nuevo procedimiento de preparacion de finasterida. - Google Patents

Nuevo procedimiento de preparacion de finasterida.

Info

Publication number
ES2072848T3
ES2072848T3 ES95200270T ES95200270T ES2072848T3 ES 2072848 T3 ES2072848 T3 ES 2072848T3 ES 95200270 T ES95200270 T ES 95200270T ES 95200270 T ES95200270 T ES 95200270T ES 2072848 T3 ES2072848 T3 ES 2072848T3
Authority
ES
Spain
Prior art keywords
finasteride
magnesium halide
disclosed
preparation
new procedure
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES95200270T
Other languages
English (en)
Other versions
ES2072848T1 (es
Inventor
Ulf H Dolling
James A Mccauley
Richard J Varsolona
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26681536&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2072848(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of ES2072848T1 publication Critical patent/ES2072848T1/es
Application granted granted Critical
Publication of ES2072848T3 publication Critical patent/ES2072848T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F3/00—Compounds containing elements of Groups 2 or 12 of the Periodic Table
    • C07F3/003—Compounds containing elements of Groups 2 or 12 of the Periodic Table without C-Metal linkages
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • H—ELECTRICITY
    • H04—ELECTRIC COMMUNICATION TECHNIQUE
    • H04N—PICTORIAL COMMUNICATION, e.g. TELEVISION
    • H04N5/00—Details of television systems
    • H04N5/74—Projection arrangements for image reproduction, e.g. using eidophor
    • H04N5/7416—Projection arrangements for image reproduction, e.g. using eidophor involving the use of a spatial light modulator, e.g. a light valve, controlled by a video signal
    • H04N5/7458—Projection arrangements for image reproduction, e.g. using eidophor involving the use of a spatial light modulator, e.g. a light valve, controlled by a video signal the modulator being an array of deformable mirrors, e.g. digital micromirror device [DMD]

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Multimedia (AREA)
  • Signal Processing (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Steroid Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Confectionery (AREA)
  • Dental Preparations (AREA)
  • Seasonings (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

SE DESCUBRE UN NUEVO PROCESO PARA PRODUCIR FINASTERURO QUE IMPLICA HACER REACCIONAR LA SAL DE MAGNESIO HALURO DE 17BETA-CARBOALCOXI-4AZA-5ALFA-ANDROST-1-EN-3-ONA CON HALURO DE MAGNESIO T-BUTILAMINO, PRESENTE EN AL MENOS UNA PROPORCION MOLAR DE 2:1 EN EL ESTER, FORMADO A PARTIR DE T-BUTIL AMINO Y UN HALURO DE MAGNESIO ALIFATICO/ARIL A TEMPERATURA AMBIENTE EN UN SOLVENTE ORGANICO INERTE BAJO UNA ATMOSFERA INERTE SEGUIDO POR EL CALENTAMIENTO Y RECUPERACION DEL PRODUCTO FINASTERURO. TAMBIEN SE DESCUBREN DOS FORMAS I Y II POLIMORFICAS CRISTALINAS DE FINASTERURO Y METODOS PARA SU PRODUCCION.
ES95200270T 1992-11-19 1993-11-12 Nuevo procedimiento de preparacion de finasterida. Expired - Lifetime ES2072848T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US97853592A 1992-11-19 1992-11-19
US08/010,734 US5468860A (en) 1992-11-19 1993-01-29 New finasteride processes

Publications (2)

Publication Number Publication Date
ES2072848T1 ES2072848T1 (es) 1995-08-01
ES2072848T3 true ES2072848T3 (es) 1999-05-01

Family

ID=26681536

Family Applications (2)

Application Number Title Priority Date Filing Date
ES93203163T Expired - Lifetime ES2052476T5 (es) 1992-11-19 1993-11-12 Un procedimiento para la produccion de finasterida.
ES95200270T Expired - Lifetime ES2072848T3 (es) 1992-11-19 1993-11-12 Nuevo procedimiento de preparacion de finasterida.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES93203163T Expired - Lifetime ES2052476T5 (es) 1992-11-19 1993-11-12 Un procedimiento para la produccion de finasterida.

Country Status (33)

Country Link
US (3) US5468860A (es)
EP (3) EP0599376B2 (es)
JP (2) JPH07110875B2 (es)
CN (1) CN1058018C (es)
AT (2) ATE177112T1 (es)
AU (1) AU658774B2 (es)
BG (2) BG62362B1 (es)
CA (1) CA2103107C (es)
CY (1) CY2135B1 (es)
CZ (3) CZ301160B6 (es)
DE (4) DE69317856T2 (es)
DK (2) DK0599376T4 (es)
DZ (1) DZ1733A1 (es)
ES (2) ES2052476T5 (es)
FI (4) FI107450B (es)
GR (4) GR940300045T1 (es)
HK (1) HK1008338A1 (es)
HR (2) HRP931410B1 (es)
HU (2) HU216195B (es)
IL (1) IL107574A (es)
IS (2) IS1692B (es)
LV (2) LV12212B (es)
MX (1) MX9307222A (es)
MY (2) MY110410A (es)
NO (3) NO305912B1 (es)
PH (1) PH31120A (es)
RO (2) RO115164B1 (es)
RU (1) RU2120445C1 (es)
SI (1) SI9300603B (es)
SK (2) SK286488B6 (es)
TW (1) TW257766B (es)
UA (1) UA41341C2 (es)
WO (1) WO1994011387A2 (es)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes
IT1270660B (it) * 1994-10-13 1997-05-07 Poli Ind Chimica Spa Procedimento microbiologico per la preparazione di 3-oxo-4-azasteroidi-17beta-carbossi sostituiti e uso dei prodotti come inibitori dell'enzima 5alfa-riduttasi
US5670643A (en) * 1995-03-16 1997-09-23 Glaxo Wellcome Inc. Method for preparing finasteride
US5585383A (en) * 1995-05-03 1996-12-17 Merck & Co., Inc. Process for crystallizing a 4-azasteroid 5alpha-reductase inhibitor
WO1997010217A1 (en) * 1995-09-15 1997-03-20 Merck & Co., Inc. 4-azasteroids for treatment of hyperandrogenic conditions
GB2338234B (en) * 1998-06-10 2000-05-03 Torcan Chemical Ltd Preparation of finasteride
ES2153789B1 (es) * 1999-07-05 2001-10-16 Raga Consultores S L Procedimiento para la obtencion de 178-(n-terc-butlcarbamoil)-3-ona-4-aza-esteroides
EP1228084A1 (en) * 1999-11-01 2002-08-07 TORCAN CHEMICAL Ltd Production of polymorphic forms i and ii of finasteride by complexation with group i or ii metal salts
SK2732003A3 (en) * 2000-09-07 2004-01-08 Reddys Lab Ltd Dr Novel polymorphic form of 17-beta-(N-ter.butyl carbamoyl)-4-aza- 5-alpha-androst-1-en-3-one and a process for preparing it
MXPA03002031A (es) * 2000-09-07 2004-12-13 Reddys Lab Ltd Dr Forma polimorfica novedosa de 17-beta-(n-tercbutil carbamoil)-4-aza-5-alfa-androst-1-en-3-ona y proceso para preparar la misma.
NZ525116A (en) * 2000-09-07 2004-11-26 Dr Novel polymorphic form of 17- beta -(N-ter.butyl carbamoyl)-4-AZA-5- alpha -androst-1-en-3-one and a process for preparing it
KR100415858B1 (ko) * 2001-09-22 2004-01-24 한미약품 주식회사 17베타-(엔-3차-부틸카바모일)-3-온 스테로이드 화합물의제조방법
CN100428897C (zh) * 2002-08-16 2008-10-29 浙江寿峰堂生物工程有限公司 抗疲劳改善亚健康的保健食品及其制备方法
ES2206065B1 (es) * 2002-10-31 2005-08-16 Ragactives, S.L. Procedimiento para la obtencion de la forma polimorfica i de finasterida.
WO2004083230A1 (en) * 2003-03-19 2004-09-30 Hetero Drugs Limited Novel crystalline forms of finasteride
ATE406376T1 (de) * 2003-07-03 2008-09-15 Cipla Ltd Verfahren zur herstellung von finasterid form i
US20050136015A1 (en) * 2003-12-17 2005-06-23 McKie Derrick B. Topical use of halosalicylic acid derivatives
US20070167477A1 (en) * 2006-01-13 2007-07-19 Mandava Venkata Naga Brahmeswa Processes to prepare finasteride polymorphs
US7531658B2 (en) * 2006-01-20 2009-05-12 Apotex Pharmachem Inc. Process for the preparation of 17-N-substituted-carbamoyl-4-aza-androst-1-en-3-ones
US7897800B2 (en) 2006-02-03 2011-03-01 Jr Chem, Llc Chemical compositions and methods of making them
WO2007089267A1 (en) 2006-02-03 2007-08-09 Jr Chem, Llc Anti-aging treatment using copper and zinc compositions
US7687650B2 (en) 2006-02-03 2010-03-30 Jr Chem, Llc Chemical compositions and methods of making them
US7867522B2 (en) 2006-09-28 2011-01-11 Jr Chem, Llc Method of wound/burn healing using copper-zinc compositions
US20090076058A1 (en) * 2007-09-17 2009-03-19 Protia, Llc Deuterium-enriched finasteride
US8273791B2 (en) 2008-01-04 2012-09-25 Jr Chem, Llc Compositions, kits and regimens for the treatment of skin, especially décolletage
US9004752B2 (en) * 2008-05-05 2015-04-14 Abbvie, Inc. Method for evaluating the solubility of a crystalline substance in a polymer
CA2750636C (en) 2009-01-23 2017-07-25 Jr Chem, Llc Rosacea treatments and kits for performing them
US8952057B2 (en) 2011-01-11 2015-02-10 Jr Chem, Llc Compositions for anorectal use and methods for treating anorectal disorders

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ211145A (en) * 1984-02-27 1988-10-28 Merck & Co Inc 4-aza-5-alpha-androst-1-en-3-ones and pharmaceutical compositions
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
DE3888378T2 (de) * 1987-04-03 1994-09-29 Merck & Co Inc Behandlung von Prostatacarcinoma mit 17-beta-n-monosubstituierten-Carbamoyl-4-aza-5-alpha-Androst-1-en-3-onen.
NZ225100A (en) * 1987-06-29 1991-09-25 Merck & Co Inc Reaction of steroids (including 4-azasteroids) with a silylating agent in the presence of a quinone to introduce a delta' double bond and silylated intermediates
US5084574A (en) * 1988-04-18 1992-01-28 Merck & Co., Inc. Dehydrogenation process
US5237061A (en) * 1988-10-31 1993-08-17 Merck & Co., Inc. Methods of synthesizing benign prostatic hypertropic agents and their intermediates
US5021575A (en) * 1989-11-13 1991-06-04 Merck & Co., Inc. Method for introducing a 1,2 double bond into azasteroids
EP0461930B1 (en) * 1990-06-15 1995-09-13 Merck & Co. Inc. A crystallization method to improve crystal structure and size
EP0462662A3 (en) * 1990-06-20 1992-08-19 Merck & Co. Inc. 17beta-n-monosubstituted adamantyl/norbornanyl carbamoyl-4-aza-5alpha-androst-1-en-3-ones and androstan-3-ones
US5120847A (en) † 1990-08-27 1992-06-09 Merck & Co., Inc. Process for iodinating or brominating the α-methylenic carbon of a secondary amide
US5091534A (en) 1990-08-27 1992-02-25 Merck & Co., Inc. Trialkylsilyl trifluoromethanesulfonate mediated α-methylenic carbon functionalization of 4-AZA-5α-androstan-3-one steroids
CA2050824A1 (en) * 1990-09-24 1992-03-25 John M. Williams Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones
US5061801A (en) * 1990-09-24 1991-10-29 Merck & Co., Inc. Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-ketones
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes

Also Published As

Publication number Publication date
ES2052476T5 (es) 2008-11-01
DZ1733A1 (fr) 2002-02-17
IS1671B (is) 1997-12-19
PH31120A (en) 1998-02-23
NO307888B1 (no) 2000-06-13
SK65995A3 (en) 1995-10-11
IS4286A (is) 1994-05-20
LV12460A (lv) 2000-04-20
NO990468D0 (no) 1999-02-01
CN1090583A (zh) 1994-08-10
SK286488B6 (sk) 2008-11-06
TW257766B (es) 1995-09-21
LV12212A (lv) 1999-01-20
RU95112521A (ru) 1997-02-10
CA2103107A1 (en) 1994-05-20
WO1994011387A3 (en) 1994-09-29
NO307609B1 (no) 2000-05-02
US5886184A (en) 1999-03-23
GR950300043T1 (en) 1995-07-31
EP0823436A3 (en) 1998-11-25
ES2052476T3 (es) 1998-06-16
NO990468L (no) 1995-05-19
JPH07110875B2 (ja) 1995-11-29
NO305912B1 (no) 1999-08-16
GR940300045T1 (en) 1994-07-29
ATE164850T1 (de) 1998-04-15
WO1994011387A2 (en) 1994-05-26
ES2072848T1 (es) 1995-08-01
HRP20000295A2 (en) 2000-08-31
GR3029554T3 (en) 1999-06-30
IL107574A0 (en) 1994-02-27
DK0599376T4 (da) 2008-07-28
BG99637A (bg) 1996-04-30
DE69323754T2 (de) 1999-10-07
EP0655458A2 (en) 1995-05-31
AU658774B2 (en) 1995-04-27
NO992580D0 (no) 1999-05-28
ATE177112T1 (de) 1999-03-15
HU216195B (hu) 1999-05-28
CZ287842B6 (en) 2001-02-14
NO951986D0 (no) 1995-05-19
CA2103107C (en) 2010-09-28
EP0655458A3 (en) 1996-07-10
US5652365A (en) 1997-07-29
EP0599376A2 (en) 1994-06-01
CY2135B1 (en) 2002-05-21
FI20040559A (fi) 2004-04-21
BG103170A (en) 1999-09-30
SK281765B6 (sk) 2001-07-10
DE69317856D1 (de) 1998-05-14
IS4094A (is) 1994-05-20
FI107450B (fi) 2001-08-15
HU210535A9 (en) 1995-04-28
BG62362B1 (bg) 1999-09-30
RU2120445C1 (ru) 1998-10-20
DE69317856T2 (de) 1998-11-05
EP0599376A3 (en) 1994-09-28
BG64464B1 (bg) 2005-03-31
LV12212B (en) 1999-03-20
FI114215B (fi) 2004-09-15
JP2742409B2 (ja) 1998-04-22
GR3026577T3 (en) 1998-07-31
MY110411A (en) 1998-05-30
AU5078793A (en) 1994-06-16
CN1058018C (zh) 2000-11-01
DE655458T1 (de) 1995-11-30
EP0655458B1 (en) 1999-03-03
CZ301160B6 (cs) 2009-11-18
EP0599376B1 (en) 1998-04-08
JPH06199889A (ja) 1994-07-19
SI9300603B (sl) 2004-06-30
FI20010289A (fi) 2001-02-15
UA41341C2 (uk) 2001-09-17
RO115164B1 (ro) 1999-11-30
HK1008338A1 (en) 1999-05-07
DE69323754D1 (de) 1999-04-08
LV12460B (en) 2000-09-20
IL107574A (en) 2000-07-16
RO115165B1 (ro) 1999-11-30
MY110410A (en) 1998-05-30
CZ126895A3 (en) 1995-12-13
FI952422A (fi) 1995-05-18
MX9307222A (es) 1994-07-29
HRP931410B1 (en) 2000-06-30
NO951986L (no) 1995-05-19
CZ301191B6 (cs) 2009-12-02
ES2052476T1 (es) 1994-07-16
EP0823436A2 (en) 1998-02-11
SI9300603A (en) 1994-06-30
HRP20000295B1 (en) 2002-08-31
IS1692B (is) 1998-04-20
HUT66973A (en) 1995-01-30
EP0599376B2 (en) 2008-04-16
FI114800B (fi) 2004-12-31
FI116941B (fi) 2006-04-13
HRP931410A2 (en) 1996-06-30
HU9303275D0 (en) 1994-03-28
JPH09235294A (ja) 1997-09-09
US5468860A (en) 1995-11-21
FI952422A0 (fi) 1995-05-18
FI20010290A (fi) 2001-02-15
DK0655458T3 (da) 1999-09-27
DE599376T1 (de) 1994-12-08
NO307888B3 (no) 2000-06-13
NO992580L (no) 1995-05-19

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ES2072848T3 (es) Nuevo procedimiento de preparacion de finasterida.

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