HUP0101874A2 - Szelektív ösztrogén receptor modulátorok enzimatikus rezolválása - Google Patents

Szelektív ösztrogén receptor modulátorok enzimatikus rezolválása

Info

Publication number
HUP0101874A2
HUP0101874A2 HU0101874A HUP0101874A HUP0101874A2 HU P0101874 A2 HUP0101874 A2 HU P0101874A2 HU 0101874 A HU0101874 A HU 0101874A HU P0101874 A HUP0101874 A HU P0101874A HU P0101874 A2 HUP0101874 A2 HU P0101874A2
Authority
HU
Hungary
Prior art keywords
group
estrogen receptor
receptor modulators
selective estrogen
amino
Prior art date
Application number
HU0101874A
Other languages
English (en)
Inventor
Kevin Kun-Chin Liu
Original Assignee
Pfizer Products 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
Application filed by Pfizer Products Inc. filed Critical Pfizer Products Inc.
Publication of HU0101874D0 publication Critical patent/HU0101874D0/hu
Publication of HUP0101874A2 publication Critical patent/HUP0101874A2/hu
Publication of HUP0101874A3 publication Critical patent/HUP0101874A3/hu

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/16—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing two or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/16—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms containing two or more hetero rings
    • C12P17/165—Heterorings having nitrogen atoms as the only ring heteroatoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/10—Nitrogen as only ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
    • C12P17/10—Nitrogen as only ring hetero atom
    • C12P17/12—Nitrogen as only ring hetero atom containing a six-membered hetero ring
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
    • C12P41/00—Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture
    • C12P41/003—Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions
    • C12P41/004—Processes using enzymes or microorganisms to separate optical isomers from a racemic mixture by ester formation, lactone formation or the inverse reactions by esterification of alcohol- or thiol groups in the enantiomers or the inverse reaction
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y301/00—Hydrolases acting on ester bonds (3.1)
    • C12Y301/01—Carboxylic ester hydrolases (3.1.1)
    • C—CHEMISTRY; METALLURGY
    • C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
    • C12Y—ENZYMES
    • C12Y301/00—Hydrolases acting on ester bonds (3.1)
    • C12Y301/01—Carboxylic ester hydrolases (3.1.1)
    • C12Y301/01013—Sterol esterase (3.1.1.13)

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Wood Science & Technology (AREA)
  • Zoology (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biochemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Rheumatology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Analytical Chemistry (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (AREA)

Abstract

A találmány tárgya eljárás az (I) általános képletű vegyületek,valamint optikai és geometriai izomerjeik előállítására, ahol az (I)képletben A jelentése CH2 vagy NR csoport; B, D és E jelentéseegymástól függetlenül CH vagy N; Y jelentése fenil-, naftil-,cikloalkil-, cikloalkinilcsoport, öt- vagy hattagú heterociklusoscsoport, vagy öt- vagy hattagú, benzolgyűrűvel kondenzáltheterociklusos csoportból álló biciklusos gyűrűrendszer; Z1 jelentésealkil-, alkoxi- vagy alkiltiocsoport; G jelentése aminocsoport vagy 5-12 szénatomos, adott esetben szubsztituált biciklusos aminocsoport; Z1és G együtt gyűrűbe zárt amino-alkoxi-csoportot is képezhet; és eértéke 0, 1 vagy 2. A találmány szerint úgy járnak el, hogy egy (II)általános képletű vegyületet hidrolitikus enzim és vizes pufferoldatjelenlétében szelektíven dezacetilezik. A találmány szerintivegyületek ösztrogénagonista hatással rendelkeznek. Ó
HU0101874A 2000-05-08 2001-05-07 Enzymatic resolution of selective estrogen receptor modulators HUP0101874A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20241800P 2000-05-08 2000-05-08

Publications (3)

Publication Number Publication Date
HU0101874D0 HU0101874D0 (en) 2001-07-30
HUP0101874A2 true HUP0101874A2 (hu) 2002-03-28
HUP0101874A3 HUP0101874A3 (en) 2003-06-30

Family

ID=22749787

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0101874A HUP0101874A3 (en) 2000-05-08 2001-05-07 Enzymatic resolution of selective estrogen receptor modulators

Country Status (24)

Country Link
US (3) US6828134B2 (hu)
EP (1) EP1156120B1 (hu)
JP (1) JP2002000293A (hu)
KR (1) KR100488385B1 (hu)
CN (1) CN1322842A (hu)
AR (1) AR031844A1 (hu)
AT (1) ATE346159T1 (hu)
AU (1) AU782597B2 (hu)
BR (1) BR0101802A (hu)
CA (1) CA2346426C (hu)
CZ (1) CZ20011576A3 (hu)
DE (1) DE60124616T2 (hu)
ES (1) ES2274854T3 (hu)
HK (1) HK1040264A1 (hu)
HU (1) HUP0101874A3 (hu)
ID (1) ID30106A (hu)
IL (2) IL142881A (hu)
MX (1) MXPA01004626A (hu)
PL (1) PL347407A1 (hu)
RU (1) RU2213778C2 (hu)
SG (1) SG100688A1 (hu)
TW (1) TWI237059B (hu)
YU (1) YU31101A (hu)
ZA (1) ZA200103666B (hu)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011159769A2 (en) 2010-06-17 2011-12-22 Aragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof
CN109750013B (zh) * 2019-03-27 2023-01-13 云南师范大学 一种脂肪酶突变体及其制备方法和应用

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4814282A (en) * 1984-05-03 1989-03-21 Abbott Laboratories Centrifuge for two-dimensional centrifugation
DE3638762A1 (de) * 1986-11-13 1988-05-26 Schering Ag Racematspaltung von 7(alpha)-acyloxy-6ss-hydroxy-methyl-2-oxabicyclo (3.3.0)octan-3-onen durch stereospezifische enzymatische acylat-hydrolyse
US5248609A (en) 1986-11-13 1993-09-28 Schering Aktiengesellschaft Racemic separation of 7α-acyloxy-6β-hydroxymethyl-2-oxabicyclo[3.]-octan-3-ones by stereospecific enzymatic acylate hydrolysis
CA1319144C (en) 1986-11-14 1993-06-15 Quirico Branca Tetrahydronaphthalene derivatives
US5106750A (en) 1988-08-30 1992-04-21 G. D. Searle & Co. Enantio- and regioselective synthesis of organic compounds using enol esters as irreversible transacylation reagents
TW383306B (en) * 1992-12-22 2000-03-01 Lilly Co Eli New use of 2-phenyl-3-aroylbenzothiophenes in lowering serum cholesterol
FR2724184B1 (fr) * 1994-09-05 1997-01-03 Rhone Poulenc Chimie Procede de resolution d'un melange d'alcools stereoisomeres
US5589482A (en) * 1994-12-14 1996-12-31 Pfizer Inc. Benzo-thiophene estrogen agonists to treat prostatic hyperplasia
US5552412A (en) * 1995-01-09 1996-09-03 Pfizer Inc 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis
UA51676C2 (uk) 1995-11-02 2002-12-16 Пфайзер Інк. (-)цис-6(s)-феніл-5(r)[4-(2-піролідин-1-ілетокси)феніл]-5,6,7,8-тетрагідронафталін-2-ол d-тартрат, спосіб його одержання, спосіб лікування захворювань, що піддаються лікуванню агоністами естрогену, та фармацевтична композиція
IL120266A (en) * 1996-02-28 2005-05-17 Pfizer Use of estrogen antagonists and estrogen agonists in the preparation of medicaments for inhibiting pathological conditions
AU8058398A (en) * 1997-06-17 1999-01-04 Schering Corporation Enzymatic kinetic resolution of an intermediate useful for preparing substitutedtricyclics
PA8475901A1 (es) 1998-06-16 2000-05-24 Pfizer Prod Inc Terapia de combinacion para la fragilidad musculoesqueletica
ID23459A (id) 1998-08-28 2000-04-27 Pfizer Prod Inc Biotransformasi mikroba
US6180375B1 (en) 1999-08-27 2001-01-30 Pfizer Inc. Microbial biotransformation

Also Published As

Publication number Publication date
ID30106A (id) 2001-11-08
CA2346426A1 (en) 2001-11-08
JP2002000293A (ja) 2002-01-08
PL347407A1 (en) 2001-11-19
AU782597B2 (en) 2005-08-11
HK1040264A1 (zh) 2002-05-31
RU2213778C2 (ru) 2003-10-10
YU31101A (sh) 2005-07-19
EP1156120A3 (en) 2004-02-18
KR100488385B1 (ko) 2005-05-11
EP1156120B1 (en) 2006-11-22
CN1322842A (zh) 2001-11-21
IL168341A (en) 2006-08-01
HUP0101874A3 (en) 2003-06-30
US20070249025A1 (en) 2007-10-25
KR20010102942A (ko) 2001-11-17
CA2346426C (en) 2006-08-01
MXPA01004626A (es) 2004-09-10
ZA200103666B (en) 2002-11-07
AR031844A1 (es) 2003-10-08
ES2274854T3 (es) 2007-06-01
US7351567B2 (en) 2008-04-01
IL142881A0 (en) 2002-03-10
EP1156120A2 (en) 2001-11-21
DE60124616T2 (de) 2007-09-13
TWI237059B (en) 2005-08-01
US6828134B2 (en) 2004-12-07
AU4375801A (en) 2001-11-15
US20040176415A1 (en) 2004-09-09
US20020049219A1 (en) 2002-04-25
IL142881A (en) 2006-08-01
DE60124616D1 (de) 2007-01-04
SG100688A1 (en) 2003-12-26
HU0101874D0 (en) 2001-07-30
BR0101802A (pt) 2001-12-18
ATE346159T1 (de) 2006-12-15
CZ20011576A3 (cs) 2002-02-13

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Legal Events

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FD9A Lapse of provisional protection due to non-payment of fees