PE20011012A1 - Benzoxa y benzotiazoles como inhibidores de sulfatasa de esteroide - Google Patents

Benzoxa y benzotiazoles como inhibidores de sulfatasa de esteroide

Info

Publication number
PE20011012A1
PE20011012A1 PE2000001233A PE0012332000A PE20011012A1 PE 20011012 A1 PE20011012 A1 PE 20011012A1 PE 2000001233 A PE2000001233 A PE 2000001233A PE 0012332000 A PE0012332000 A PE 0012332000A PE 20011012 A1 PE20011012 A1 PE 20011012A1
Authority
PE
Peru
Prior art keywords
benzoxa
benzothiazoles
compound
steroid sulfatase
ester
Prior art date
Application number
PE2000001233A
Other languages
English (en)
Inventor
Andreas Billich
Barbara Wolff-Winiski
Erwin Paul Schreiner
Original Assignee
Novartis Ag
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 GBGB9927439.1A external-priority patent/GB9927439D0/en
Priority claimed from GB0007511A external-priority patent/GB0007511D0/en
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of PE20011012A1 publication Critical patent/PE20011012A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—Antipsoriatics
    • 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
    • A61P17/08—Antiseborrheics
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
    • 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
    • A61P5/28—Antiandrogens
    • 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
    • A61P5/32—Antioestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D263/57—Aryl or substituted aryl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Dermatology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Neurosurgery (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Transplantation (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)

Abstract

SE REFIERE A BENZOXA O BENZOTIAZOLES SUSTITUDOS EN POSICION 2 Y CON UN ESTER DEL ACIDO SULFAMICO ENLAZADO POR OXIGENO AL FENILO DEL COMPUESTO DE FORMULA I; DONDE X ES O, S; R1 Y R2 SON H, ALQUILO; O UNO ES H Y EL OTRO ES ACILO, ALCOXICARBONILO; R3 ES ALQUILO, ALQUENILO, ALQUINILO, CICLOALQUILO, ENTRE OTROS. UN COMPUESTO PREFERIDO ES 2-(ADAMANTAN-2-ILIDENMETIL)BENZOXAZOL-6-IL-ESTER DEL ACIDO SULFAMICO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION, A COMPUESTOS INTERMEDIOS. EL COMPUESTO I INHIBE A ESTEROIDE SULFATASA REDUCIENDO LOS NIVELES ENDOGENOS DE ANDROGENOS, ESTROGENOS EN LA PIEL Y PUEDE SER UTIL EN EL TRATAMIENTO DEL ACNE, SEBORREA, ALOPECIA ANDROGENICA, HIRSUTISMO, CARCINOMA DE CELULAS ESCAMOSAS
PE2000001233A 1999-11-19 2000-11-17 Benzoxa y benzotiazoles como inhibidores de sulfatasa de esteroide PE20011012A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9927439.1A GB9927439D0 (en) 1999-11-19 1999-11-19 Organic compounds
GB0007511A GB0007511D0 (en) 2000-03-28 2000-03-28 Organic compounds

Publications (1)

Publication Number Publication Date
PE20011012A1 true PE20011012A1 (es) 2001-10-02

Family

ID=26243976

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001233A PE20011012A1 (es) 1999-11-19 2000-11-17 Benzoxa y benzotiazoles como inhibidores de sulfatasa de esteroide

Country Status (15)

Country Link
US (1) US6716865B1 (es)
EP (1) EP1230227B1 (es)
JP (1) JP2003514806A (es)
AR (1) AR026504A1 (es)
AT (1) ATE269853T1 (es)
AU (1) AU1857701A (es)
CO (1) CO5261573A1 (es)
DE (1) DE60011801T2 (es)
DK (1) DK1230227T3 (es)
ES (1) ES2223620T3 (es)
HK (1) HK1049329B (es)
PE (1) PE20011012A1 (es)
PT (1) PT1230227E (es)
TR (1) TR200402432T4 (es)
WO (1) WO2001036398A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR041952A1 (es) * 2002-11-14 2005-06-01 Novartis Ag N-sulfonilaminotiazol
DE10260955A1 (de) * 2002-12-20 2004-07-08 Henkel Kgaa Verwendung von Steroidsulfatase-Inhibitoren zur Verminderung von Haarausfall
ES2655028T3 (es) * 2007-08-02 2018-02-16 Millennium Pharmaceuticals, Inc. Proceso para la síntesis de inhibidores de enzima de activación de E1
BRPI0817045A2 (pt) 2007-09-17 2015-03-24 Preglem Sa Tratamento de condições estrogênio-dependentes em mulheres pré-menopáusicas
CN104926730B (zh) * 2014-03-21 2017-07-21 中国科学院武汉岩土力学研究所 一种松香基咪唑啉类化合物及其合成方法和应用
US11001564B2 (en) * 2016-09-13 2021-05-11 Arbutus Biopharma Corporation Substituted chromane-8-carboxamide compounds and analogues thereof, and methods using same

Family Cites Families (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2868800A (en) 1954-10-13 1959-01-13 Upjohn Co 6-ethoxybenzothiazole-2-sulfonamide
US4472418A (en) * 1983-04-22 1984-09-18 Merck & Co., Inc. Benzothiazolesulfonamide derivatives for the topical treatment of elevated intraocular pressure
FI91869C (fi) 1987-03-18 1994-08-25 Tanabe Seiyaku Co Menetelmä antidiabeettisena aineena käytettävien bensoksatsolijohdannaisten valmistamiseksi
US5273993A (en) 1989-06-12 1993-12-28 A. H. Robins Company, Incorporated Compounds having one or more aminosulfonyloxy radicals useful as pharmaceuticals
PT94305B (pt) * 1989-06-12 1997-02-28 Robins Co Inc A H Processo para a preparacao de compostos tendo um ou mais radicais aminossulfoniloxi uteis como produtos farmaceuticos
US5194446A (en) 1989-06-12 1993-03-16 A. H. Robins Company, Incorporated Compounds having one or more aminosulfaonyloxy radicals useful as pharmaceuticals
US5192785A (en) 1989-09-03 1993-03-09 A. H. Robins Company, Incorporated Sulfamates as antiglaucoma agents
US5409930A (en) 1991-05-10 1995-04-25 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
CA2124329C (en) 1991-11-27 2008-11-18 Gregory A. Kopia Compounds, compositions and methods for binding bio-affecting substances to surface membranes of bio-particles
ATE188379T1 (de) 1992-10-14 2000-01-15 Merck & Co Inc Fibrinogenrezeptor-antagonisten
ATE248153T1 (de) 1994-10-12 2003-09-15 Euro Celtique Sa Neue benzoxazole
US6169085B1 (en) * 1995-03-10 2001-01-02 G. D. Searle & Company Sulfonylalkanoylamino hydroxyethylamino sulfonamide retroviral protease inhibitors
US5677321A (en) 1996-02-29 1997-10-14 Synaptic Pharmaceutical Corporation 5- and 6-(2-imidazolin-2-ylamino) and -(2-thiazolin-2-ylamino)-benzothiazoles as alpha-2 adrenergic ligands
US5709845A (en) 1996-05-13 1998-01-20 Rajagopalan; Raghavan Tricyclic functional dyes for contrast enhancement in optical imaging
DE19653647A1 (de) 1996-12-20 1998-06-25 Hoechst Ag Vitronectin - Rezeptorantagonisten, deren Herstellung sowie deren Verwendung
JPH10237053A (ja) 1997-02-24 1998-09-08 Sumitomo Chem Co Ltd ベンゾチアゾール類の製造方法
US6140051A (en) 1997-07-21 2000-10-31 Promega Biosciences, Inc. Fluorescent dibenzazole derivatives and methods related thereto
GB2331988B (en) * 1997-12-04 2003-04-16 Imperial College Polycyclic sulphamate inhibitors or oestrone sulphatase
GB9807779D0 (en) 1998-04-09 1998-06-10 Ciba Geigy Ag Organic compounds
AR019678A1 (es) 1998-06-18 2002-03-13 Novartis Ag Compuestos organicos

Also Published As

Publication number Publication date
HK1049329A1 (en) 2003-05-09
TR200402432T4 (tr) 2004-12-21
AR026504A1 (es) 2003-02-12
AU1857701A (en) 2001-05-30
EP1230227B1 (en) 2004-06-23
WO2001036398A1 (en) 2001-05-25
US6716865B1 (en) 2004-04-06
HK1049329B (zh) 2005-03-24
JP2003514806A (ja) 2003-04-22
DK1230227T3 (da) 2004-08-16
ATE269853T1 (de) 2004-07-15
DE60011801T2 (de) 2005-07-14
EP1230227A1 (en) 2002-08-14
ES2223620T3 (es) 2005-03-01
CO5261573A1 (es) 2003-03-31
PT1230227E (pt) 2004-10-29
DE60011801D1 (de) 2004-07-29

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