FI20010289A - Process for the preparation of a polymorphic form of finasteride - Google Patents

Process for the preparation of a polymorphic form of finasteride Download PDF

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Publication number
FI20010289A
FI20010289A FI20010289A FI20010289A FI20010289A FI 20010289 A FI20010289 A FI 20010289A FI 20010289 A FI20010289 A FI 20010289A FI 20010289 A FI20010289 A FI 20010289A FI 20010289 A FI20010289 A FI 20010289A
Authority
FI
Finland
Prior art keywords
finasteride
magnesium halide
disclosed
preparation
polymorphic form
Prior art date
Application number
FI20010289A
Other languages
Finnish (fi)
Swedish (sv)
Other versions
FI114800B (en
Inventor
Ulf H Dolling
James A Mccauley
Richard J Varsolona
Original Assignee
Merck & 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
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=26681536&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=FI20010289(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of FI20010289A publication Critical patent/FI20010289A/en
Application granted granted Critical
Publication of FI114800B publication Critical patent/FI114800B/en

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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]

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  • 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)
  • Urology & Nephrology (AREA)
  • Dermatology (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

Disclosed is a new process for producing finasteride which involves reacting the magnesium halide salt of 17β-carboalkoxy-4-aza-5α-androst-1-en-3-one with t-butylamino magnesium halide, present in at least a 2:1 molar ratio to the ester, formed from t-butyl amine and an aliphatic/aryl magnesium halide at ambient temperature in an inert organic solvent under an inert atmosphere followed by heating and recovering the product finasteride.Also disclosed are two polymorphic crystalline Forms I and II of finasteride, and methods of their production.
FI20010289A 1992-11-19 2001-02-15 A process for preparing a polymorphic form of finasteride FI114800B (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US97853592A 1992-11-19 1992-11-19
US97853592 1992-11-19
US08/010,734 US5468860A (en) 1992-11-19 1993-01-29 New finasteride processes
US1073493 1993-01-29
US9310659 1993-11-05
PCT/US1993/010659 WO1994011387A2 (en) 1992-11-19 1993-11-05 A process for the production of finasteride

Publications (2)

Publication Number Publication Date
FI20010289A true FI20010289A (en) 2001-02-15
FI114800B FI114800B (en) 2004-12-31

Family

ID=26681536

Family Applications (4)

Application Number Title Priority Date Filing Date
FI952422A FI107450B (en) 1992-11-19 1995-05-18 Process for the preparation of finasteride
FI20010290A FI114215B (en) 1992-11-19 2001-02-15 Process for the preparation of a polymorphic form of finasteride
FI20010289A FI114800B (en) 1992-11-19 2001-02-15 A process for preparing a polymorphic form of finasteride
FI20040559A FI116941B (en) 1992-11-19 2004-04-21 Process for the preparation of a polymorphic form of finasteride

Family Applications Before (2)

Application Number Title Priority Date Filing Date
FI952422A FI107450B (en) 1992-11-19 1995-05-18 Process for the preparation of finasteride
FI20010290A FI114215B (en) 1992-11-19 2001-02-15 Process for the preparation of a polymorphic form of finasteride

Family Applications After (1)

Application Number Title Priority Date Filing Date
FI20040559A FI116941B (en) 1992-11-19 2004-04-21 Process for the preparation of a polymorphic form of finasteride

Country Status (33)

Country Link
US (3) US5468860A (en)
EP (3) EP0823436A3 (en)
JP (2) JPH07110875B2 (en)
CN (1) CN1058018C (en)
AT (2) ATE177112T1 (en)
AU (1) AU658774B2 (en)
BG (2) BG62362B1 (en)
CA (1) CA2103107C (en)
CY (1) CY2135B1 (en)
CZ (3) CZ287842B6 (en)
DE (4) DE599376T1 (en)
DK (2) DK0655458T3 (en)
DZ (1) DZ1733A1 (en)
ES (2) ES2052476T5 (en)
FI (4) FI107450B (en)
GR (4) GR940300045T1 (en)
HK (1) HK1008338A1 (en)
HR (2) HRP931410B1 (en)
HU (2) HU216195B (en)
IL (1) IL107574A (en)
IS (2) IS1692B (en)
LV (2) LV12212B (en)
MX (1) MX9307222A (en)
MY (2) MY110411A (en)
NO (3) NO305912B1 (en)
PH (1) PH31120A (en)
RO (2) RO115164B1 (en)
RU (1) RU2120445C1 (en)
SI (1) SI9300603B (en)
SK (2) SK286488B6 (en)
TW (1) TW257766B (en)
UA (1) UA41341C2 (en)
WO (1) WO1994011387A2 (en)

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 (en) * 1994-10-13 1997-05-07 Poli Ind Chimica Spa MICROBIOLOGICAL PROCEDURE FOR THE PREPARATION OF 3-OXO-4-AZASTEROIDS-17BETA-CARBOSS REPLACED AND USE OF THE PRODUCTS AS INHIBITORS OF THE 5ALPAL-REDUCED ENZYME ENZYME
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
EP0859761A4 (en) * 1995-09-15 2000-01-26 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 (en) * 1999-07-05 2001-10-16 Raga Consultores S L PROCEDURE FOR OBTAINING 178- (N-TERC-BUTLCARBAMOIL) -3-ONA-4-AZA-STEROIDS
WO2001032683A1 (en) * 1999-11-01 2001-05-10 Torcan Chemical Ltd. Production of polymorphic forms i and ii of finasteride by complexation with group i or ii metal salts
JP2004508380A (en) * 2000-09-07 2004-03-18 ドクター・レディーズ・ラボラトリーズ・リミテッド Novel polymorph of 17-β- (N-ter-butylcarbamoyl) -4-aza-5-α-androst-1-en-3-one and method of preparing the same
AU2001269911B2 (en) * 2000-09-07 2006-09-21 Dr. Reddy's Laboratories Ltd. 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
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
KR100415858B1 (en) * 2001-09-22 2004-01-24 한미약품 주식회사 PROCESS FOR THE PREPARATION OF 17β-(N-TERT-BUTYLCARBAMOYL)-3-ONE STEROID COMPOUND
CN100428897C (en) * 2002-08-16 2008-10-29 浙江寿峰堂生物工程有限公司 Health care food for antifatigue and improving subhealthy and its preparation method
ES2206065B1 (en) * 2002-10-31 2005-08-16 Ragactives, S.L. PROCEDURE FOR OBTAINING THE POLYMORPHIC FORM I OF FINASTERIDA.
WO2004083230A1 (en) * 2003-03-19 2004-09-30 Hetero Drugs Limited Novel crystalline forms of finasteride
EP1651661B1 (en) * 2003-07-03 2008-08-27 Cipla Ltd. Process for the preparation of finasteride 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
US7687650B2 (en) 2006-02-03 2010-03-30 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
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
CA2723398C (en) * 2008-05-05 2017-07-04 Abbott Gmbh & Co. Kg 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

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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
IL74365A (en) 1984-02-27 1990-07-26 Merck & Co Inc 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it
DE3888378T2 (en) * 1987-04-03 1994-09-29 Merck & Co Inc Treatment of prostate carcinoma with 17-beta-n-monosubstituted-carbamoyl-4-aza-5-alpha-androst-1-en-3-ones.
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
JP3282731B2 (en) * 1990-06-15 2002-05-20 メルク エンド カムパニー インコーポレーテッド Crystallization method for improving 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
US5061801A (en) * 1990-09-24 1991-10-29 Merck & Co., Inc. Intermediate for making 3-oxo-4-aza-androst-1-ene 17β-ketones
CA2050824A1 (en) * 1990-09-24 1992-03-25 John M. Williams Process for making 3-oxo-4-aza-androst-1-ene 17-.beta.-ketones
US5468860A (en) * 1992-11-19 1995-11-21 Merck & Co., Inc. New finasteride processes

Also Published As

Publication number Publication date
NO992580D0 (en) 1999-05-28
CZ126895A3 (en) 1995-12-13
NO307888B3 (en) 2000-06-13
NO307609B1 (en) 2000-05-02
DE69317856D1 (en) 1998-05-14
IS4094A (en) 1994-05-20
JPH09235294A (en) 1997-09-09
RO115164B1 (en) 1999-11-30
CA2103107A1 (en) 1994-05-20
HU216195B (en) 1999-05-28
RU95112521A (en) 1997-02-10
SK281765B6 (en) 2001-07-10
NO307888B1 (en) 2000-06-13
JPH07110875B2 (en) 1995-11-29
EP0599376B1 (en) 1998-04-08
BG62362B1 (en) 1999-09-30
SI9300603B (en) 2004-06-30
SK286488B6 (en) 2008-11-06
RO115165B1 (en) 1999-11-30
EP0823436A2 (en) 1998-02-11
ES2072848T1 (en) 1995-08-01
NO992580L (en) 1995-05-19
FI952422A (en) 1995-05-18
ES2052476T3 (en) 1998-06-16
EP0823436A3 (en) 1998-11-25
ES2072848T3 (en) 1999-05-01
BG103170A (en) 1999-09-30
BG99637A (en) 1996-04-30
FI114215B (en) 2004-09-15
PH31120A (en) 1998-02-23
MX9307222A (en) 1994-07-29
CY2135B1 (en) 2002-05-21
MY110410A (en) 1998-05-30
FI20010290A (en) 2001-02-15
DE69323754T2 (en) 1999-10-07
IS4286A (en) 1994-05-20
HUT66973A (en) 1995-01-30
CN1090583A (en) 1994-08-10
LV12212A (en) 1999-01-20
LV12212B (en) 1999-03-20
WO1994011387A2 (en) 1994-05-26
GR940300045T1 (en) 1994-07-29
FI107450B (en) 2001-08-15
BG64464B1 (en) 2005-03-31
MY110411A (en) 1998-05-30
LV12460A (en) 2000-04-20
NO990468D0 (en) 1999-02-01
GR950300043T1 (en) 1995-07-31
SK65995A3 (en) 1995-10-11
FI952422A0 (en) 1995-05-18
HRP20000295A2 (en) 2000-08-31
EP0599376B2 (en) 2008-04-16
FI114800B (en) 2004-12-31
FI116941B (en) 2006-04-13
GR3026577T3 (en) 1998-07-31
CN1058018C (en) 2000-11-01
CZ301191B6 (en) 2009-12-02
AU658774B2 (en) 1995-04-27
EP0655458A2 (en) 1995-05-31
HU210535A9 (en) 1995-04-28
LV12460B (en) 2000-09-20
DE69317856T2 (en) 1998-11-05
CZ301160B6 (en) 2009-11-18
CA2103107C (en) 2010-09-28
US5886184A (en) 1999-03-23
EP0599376A2 (en) 1994-06-01
SI9300603A (en) 1994-06-30
ATE177112T1 (en) 1999-03-15
CZ287842B6 (en) 2001-02-14
AU5078793A (en) 1994-06-16
US5652365A (en) 1997-07-29
FI20040559A (en) 2004-04-21
JPH06199889A (en) 1994-07-19
DK0655458T3 (en) 1999-09-27
DE655458T1 (en) 1995-11-30
DE599376T1 (en) 1994-12-08
RU2120445C1 (en) 1998-10-20
IL107574A (en) 2000-07-16
HRP931410B1 (en) 2000-06-30
DZ1733A1 (en) 2002-02-17
IS1671B (en) 1997-12-19
IL107574A0 (en) 1994-02-27
ES2052476T5 (en) 2008-11-01
ATE164850T1 (en) 1998-04-15
GR3029554T3 (en) 1999-06-30
JP2742409B2 (en) 1998-04-22
HRP931410A2 (en) 1996-06-30
DK0599376T4 (en) 2008-07-28
DE69323754D1 (en) 1999-04-08
ES2052476T1 (en) 1994-07-16
WO1994011387A3 (en) 1994-09-29
EP0599376A3 (en) 1994-09-28
HU9303275D0 (en) 1994-03-28
NO305912B1 (en) 1999-08-16
TW257766B (en) 1995-09-21
HRP20000295B1 (en) 2002-08-31
IS1692B (en) 1998-04-20
NO990468L (en) 1995-05-19
US5468860A (en) 1995-11-21
EP0655458A3 (en) 1996-07-10
HK1008338A1 (en) 1999-05-07
EP0655458B1 (en) 1999-03-03
UA41341C2 (en) 2001-09-17
NO951986L (en) 1995-05-19
NO951986D0 (en) 1995-05-19

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FI114215B (en) Process for the preparation of a polymorphic form of finasteride

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Owner name: MERCK SHARP & DOHME CORP.

Free format text: MERCK SHARP & DOHME CORP.

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