AR003930A1 - Procedimiento para preparar compuestos de 2-fenil-3-fenoxi o feniltio-benzotiofeno y sales farmaceuticamente aceptables, compuestos intermediarios de aplicación exclusiva en dicho procedimiento y metodo para preparar los compuestos intermediarios mencionados - Google Patents

Procedimiento para preparar compuestos de 2-fenil-3-fenoxi o feniltio-benzotiofeno y sales farmaceuticamente aceptables, compuestos intermediarios de aplicación exclusiva en dicho procedimiento y metodo para preparar los compuestos intermediarios mencionados

Info

Publication number
AR003930A1
AR003930A1 ARP960101537A ARP960101537A AR003930A1 AR 003930 A1 AR003930 A1 AR 003930A1 AR P960101537 A ARP960101537 A AR P960101537A AR P960101537 A ARP960101537 A AR P960101537A AR 003930 A1 AR003930 A1 AR 003930A1
Authority
AR
Argentina
Prior art keywords
procedure
compounds
preparing
intermediate compounds
pharmaceutically acceptable
Prior art date
Application number
ARP960101537A
Other languages
English (en)
Original Assignee
Lilly Co Eli
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
Priority claimed from US08/396,401 external-priority patent/US5510357A/en
Priority claimed from US08/552,890 external-priority patent/US5919800A/en
Priority claimed from US08/552,564 external-priority patent/US5998441A/en
Priority claimed from US08/552,679 external-priority patent/US5856339A/en
Priority claimed from US08/552,565 external-priority patent/US5977093A/en
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of AR003930A1 publication Critical patent/AR003930A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • 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
    • A61P5/30—Oestrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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 carbon atoms of the hetero ring
    • C07D333/64—Oxygen atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Epidemiology (AREA)
  • Diabetes (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

La presente invención proporciona compuestos farmacéuticamente activos de fórmula (I) en la que: R1 es -H, -OH, -O(alquilo de C1-C4), -OCOC6H5, -OCO(alquilo de C1-C6, ó -OSO2(alquilo de C2-C6); R2 es -H, -OH, -O(alquilo de C1-C4), -OCOC6H5, - OCO(alquilo de C1-C6), -OSO2(alquilo de C2-C6) ó halo; R3 es1-piperidinilo, 1-pirrolidinilo, metil-1-pirrolidinilo,dimetil-1-pirrolidinilo, 4-morfolino, dimetilamino, dietilamino, diisopropilamino ó 1-hexametilenimino;n es 2 ó 3; y z es -O- ó -S-;o una sal farmacéuticamente aceptable del mismo. Además se proporcionan composiciones farmacéuticas de los compuestos defórmula (I).
ARP960101537A 1995-02-28 1996-02-27 Procedimiento para preparar compuestos de 2-fenil-3-fenoxi o feniltio-benzotiofeno y sales farmaceuticamente aceptables, compuestos intermediarios de aplicación exclusiva en dicho procedimiento y metodo para preparar los compuestos intermediarios mencionados AR003930A1 (es)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US08/396,401 US5510357A (en) 1995-02-28 1995-02-28 Benzothiophene compounds as anti-estrogenic agents
US55276095A 1995-11-03 1995-11-03
US08/552,890 US5919800A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
US08/552,564 US5998441A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
US08/552,679 US5856339A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods
US08/552,565 US5977093A (en) 1995-02-28 1995-11-03 Benzothiophene compounds, intermediates, compositions, and methods

Publications (1)

Publication Number Publication Date
AR003930A1 true AR003930A1 (es) 1998-09-30

Family

ID=27559919

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP960101537A AR003930A1 (es) 1995-02-28 1996-02-27 Procedimiento para preparar compuestos de 2-fenil-3-fenoxi o feniltio-benzotiofeno y sales farmaceuticamente aceptables, compuestos intermediarios de aplicación exclusiva en dicho procedimiento y metodo para preparar los compuestos intermediarios mencionados

Country Status (16)

Country Link
EP (2) EP0729956B1 (es)
JP (2) JP3989569B2 (es)
AR (1) AR003930A1 (es)
AT (1) ATE207913T1 (es)
DE (1) DE69616396T2 (es)
DK (1) DK0729956T3 (es)
ES (1) ES2163587T3 (es)
FI (1) FI20095804A (es)
HK (1) HK1013991A1 (es)
IL (7) IL117276A (es)
PE (1) PE44597A1 (es)
PL (1) PL182493B1 (es)
PT (1) PT729956E (es)
SG (2) SG90193A1 (es)
SI (1) SI0729956T1 (es)
UA (1) UA44710C2 (es)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL182493B1 (pl) * 1995-02-28 2002-01-31 Lilly Co Eli Nowe pochodne benzotiofenu, nowe związki pośrednie i sposób wytwarzania nowych pochodnych benzotiofenu oraz środek farmaceutyczny
CA2214072C (en) * 1996-08-29 2006-11-14 Eli Lilly And Company Benzo [b] thiophene compounds, intermediates, processes, compositions, and methods
CA2216592C (en) * 1996-10-24 2006-07-18 Brian Stephen Muehl Benzothiophene compounds, intermediates, compositions, and methods
ZA982877B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment of central nervous system disorders with selective estrogen receptor modulators.
ZA982818B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Prevention of breast cancer using selective estrogen receptor modulators.
ZA982819B (en) * 1997-04-09 1999-10-04 Lilly Co Eli Treatment or prophylaxis of prostatic cancer and benign prostatic hyperplasia with selective estrogn receptor modulators.
WO1998055454A2 (en) * 1997-06-05 1998-12-10 Takeda Chemical Industries, Ltd. Benzofurans and benzothophenes as suppressors of neurodegeneration
US6653297B1 (en) * 1997-07-03 2003-11-25 Medical College Of Hampton Roads Control of selective estrogen receptor modulators
US6090843A (en) * 1997-08-11 2000-07-18 Eli Lilly And Company Benzothiophenes compounds which have useful pharmaceutical activity
ID24978A (id) * 1997-11-14 2000-08-31 Lilly Co Eli 2-ARYL-3-AROYLBENZO (b) THIOPHENES BERGUNA UNTUK PENGOBATAN SINDROM DEPRIVASI ESTROGEN
US6096781A (en) * 1997-11-14 2000-08-01 Eli Lilly And Company 2-arylbenzo[B]thiophenes useful for the treatment of estrogen deprivation syndrome
US6288108B1 (en) 1998-06-16 2001-09-11 Eli Lilly And Company Methods for increasing levels of acetylcholine
HUP0103834A2 (hu) * 1998-06-16 2002-05-29 Eli Lilly And Co. Eljárás az acetil-kolin-szint növelésére
CN1305377A (zh) 1998-06-16 2001-07-25 伊莱利利公司 提高乙酰胆碱水平的方法
US6087378A (en) * 1998-10-13 2000-07-11 Eli Lilly And Company Pharmaceutical formulations and applications thereof for the treatment of estrogen deprivation syndrome
PT1140888E (pt) * 1998-12-14 2003-09-30 Vertex Pharma San Diego Llc Sensores opticos moleculares para a actividade do citocromo p450
AU3964400A (en) * 1999-04-06 2000-10-23 Akzo Nobel N.V. Selective estrogenic compounds
DE60005693T2 (de) * 1999-07-29 2004-07-29 Eli Lilly And Co., Indianapolis Eine kristalline form von 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophen-hydrochlorid
EP1204656A2 (en) * 1999-07-29 2002-05-15 Eli Lilly And Company A crystalline form of 6-hydroxy-3-(4-[2-(piperidin-1-yl) ethoxy] phenoxy)-2-(4-methoxyphenyl) benzo[b]thiophene hydrochloride
ATE368046T1 (de) * 2000-03-10 2007-08-15 Univ Baylor Tubulin bindende liganden
EP1757291A3 (en) * 2000-05-08 2009-07-15 Eli Lilly & Company Stabilized formulations of 6-hydroxy-3-(4-[2-(piperidin-1-YL)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene and salts thereof
WO2001085147A2 (en) * 2000-05-08 2001-11-15 Eli Lilly And Company STABILIZED FORMULATIONS OF 6-HYDROXY-3-(4-[2-(PIPERIDIN-1-YL) ETHOXY]PHENOXY)-2-(4-METHOXYPHENYL) BENZO[b]THIOPHENE AND SALTS THEREOF
AR029538A1 (es) 2000-07-06 2003-07-02 Wyeth Corp Composiciones farmaceuticas de agentes estrogenicos
KR20030037690A (ko) * 2000-10-20 2003-05-14 일라이 릴리 앤드 캄파니 6-히드록시-3-(4-[2-(피페리딘-1-일)에톡시]페녹시)-2-(4-메톡시페닐)벤조[ｂ]티오펜 히드로클로라이드의 신규 결정형
JP4656939B2 (ja) 2002-07-22 2011-03-23 イーライ リリー アンド カンパニー フェニルスルホニル基を含む選択的エストロゲン受容体モジュレーター
CN1548434B (zh) * 2003-05-16 2010-07-28 中国科学院上海药物研究所 一类苯并噻吩类化合物、及制备和它的医药用途
EP1709022A1 (en) * 2004-01-22 2006-10-11 Eli Lilly And Company Selective estrogen receptor modulators
WO2006088648A1 (en) * 2005-02-11 2006-08-24 Eli Lilly And Company Compositions and methods for treating dyslipidemia
FR2913017A1 (fr) * 2007-02-23 2008-08-29 Cerep Sa Derives de piperidine et piperazine comme agents anti-neoplasiques ou inhibiteurs de proliferation cellulaire
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US4133814A (en) * 1975-10-28 1979-01-09 Eli Lilly And Company 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
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CA2145614A1 (en) * 1994-03-31 1995-10-01 Jeffrey A. Dodge Intermediates and processes for preparing benzothiophene compounds
US5484798A (en) * 1994-09-20 1996-01-16 Eli Lilly And Company Benzothiopene compounds, compositions, and method of inhibiting restenosis
PL182493B1 (pl) * 1995-02-28 2002-01-31 Lilly Co Eli Nowe pochodne benzotiofenu, nowe związki pośrednie i sposób wytwarzania nowych pochodnych benzotiofenu oraz środek farmaceutyczny

Also Published As

Publication number Publication date
DE69616396T2 (de) 2002-07-11
IL132954A0 (en) 2001-03-19
UA44710C2 (uk) 2002-03-15
JPH09183776A (ja) 1997-07-15
ATE207913T1 (de) 2001-11-15
ES2163587T3 (es) 2002-02-01
EP0729956B1 (en) 2001-10-31
IL132953A (en) 2002-02-10
IL117276A (en) 2001-10-31
DE69616396D1 (de) 2001-12-06
HK1013991A1 (en) 1999-09-17
DK0729956T3 (da) 2001-11-26
IL132954A (en) 2002-02-10
IL117276A0 (en) 1996-06-18
JP2007238626A (ja) 2007-09-20
PT729956E (pt) 2002-03-28
FI20095804A (fi) 2009-07-23
PL182493B1 (pl) 2002-01-31
SI0729956T1 (en) 2002-04-30
SG90193A1 (en) 2002-07-23
PL312955A1 (en) 1996-09-02
PE44597A1 (es) 1997-10-13
JP3989569B2 (ja) 2007-10-10
SG64896A1 (en) 1999-05-25
EP0729956A1 (en) 1996-09-04
IL132952A0 (en) 2001-03-19
EP1113013A1 (en) 2001-07-04
IL132952A (en) 2002-02-10
IL132953A0 (en) 2001-03-19

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