BRPI0408697A - composto - Google Patents

composto

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Publication number
BRPI0408697A
BRPI0408697A BRPI0408697-0A BRPI0408697A BRPI0408697A BR PI0408697 A BRPI0408697 A BR PI0408697A BR PI0408697 A BRPI0408697 A BR PI0408697A BR PI0408697 A BRPI0408697 A BR PI0408697A
Authority
BR
Brazil
Prior art keywords
group
alkyl
heteroaryl
substituted
amide
Prior art date
Application number
BRPI0408697-0A
Other languages
English (en)
Inventor
Nigel Vicker
Harshani Rithma Ruchi Lawrence
Gillian Margaret Allan
Christian Bubert
Delphine Sophie Marion Fisher
Alan Purohit
Michael John Reed
Barry Victor Lloyd Potter
Original Assignee
Sterix Ltd
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 Sterix Ltd filed Critical Sterix Ltd
Publication of BRPI0408697A publication Critical patent/BRPI0408697A/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • 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
    • A61P11/02—Nasal agents, e.g. decongestants
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
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    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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    • 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
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    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • 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
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P35/00—Antineoplastic agents
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
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    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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    • 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
    • A61P5/30—Oestrogens
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J41/00—Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Oncology (AREA)
  • Pulmonology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Reproductive Health (AREA)
  • Psychology (AREA)
  • Virology (AREA)
  • Psychiatry (AREA)
  • AIDS & HIV (AREA)
  • Transplantation (AREA)
  • Molecular Biology (AREA)
  • Vascular Medicine (AREA)
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  • Tropical Medicine & Parasitology (AREA)

Abstract

"COMPOSTO". é proporcionado um composto tendo a Fórmula I em que (I) R¬ 1¬ é selecionado de (i) um grupo alquiloxialquil (ii) um grupo nitrila, e em que R¬ 2¬ é capaz de formar uma ligação de hidrogênio (iii) grupo alquilaril em que o grupo aril é substituído por outro do que o grupo C1-10 (iv) grupo alquenilaril em que o grupo aril é substituído (v) grupo alquil heteroaril em que quando o grupo heteroaril compreende somente C e N no anel, o grupo aril é substituído por outro do que o grupo metil (vi) grupo alquenil heteroaríl (vii) grupo = N-O-alquil ou = N-O-H (viii) alquenil ramificado (ix) grupo álcool-alquil (x) amida ou alquilamida em que (a) o alquil da alquilamida é o -CH~ 2~ ou o -CH~ 2~CH~ 2~-, (b) a amida é di-substituída e/ou (c) a amida é substituída com pelo menos um dos grupos ~lquil heterociclo,grupo alquenil heterociclo, grupo alquil heteroaril, grupo alquenil heteroaril, grupo heteroaril,grupo alquilamina,grupo alquiloxialquil, grupo alquilaril, grupo alquil ramificado ou linear, (xi) -CHO de modo que R~ 1~, junto com o R~ 3~ proporciona um tautómero enol ou R~ 1~ junto com a forma R¬ 3¬ (xii ) um pirazol em que (a) R¬ 4¬ é um grupo = N-O-alquil ou = N-O-H, (b) o pirazol é substituído com um dos grupos alquil-OH, grupo alquil éster, grupo alquiloxialquil, grupo alquil ramificado, e uma amida e/ou (c) a posição 2 é substituída por um grupo selecionado de OH e -O-hidrocarbil (xiii) um anel heteroaril que proporciona um composto de fórmula (II) R¬ 2¬ é selecionado de grupos capazes de formar uma ligação de hidrogênio, um grupo sulfamato, um grupo fosfanata, um grupo tiofosfanato, um grupo sulfonato e um grupo sulfonamida; e (III) R¬ 3¬ é selecionado de -OH, = O, ou um -C ( = O) mimético.
BRPI0408697-0A 2003-03-24 2004-03-22 composto BRPI0408697A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0306718.8A GB0306718D0 (en) 2003-03-24 2003-03-24 Compound
PCT/GB2004/001234 WO2004085457A2 (en) 2003-03-24 2004-03-22 17beta-hydroxysteroid dehydrogenase inhibitors

Publications (1)

Publication Number Publication Date
BRPI0408697A true BRPI0408697A (pt) 2006-03-28

Family

ID=9955403

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0408697-0A BRPI0408697A (pt) 2003-03-24 2004-03-22 composto

Country Status (10)

Country Link
US (1) US8003783B2 (pt)
EP (2) EP2336146A1 (pt)
JP (1) JP5000294B2 (pt)
CN (1) CN100526328C (pt)
AU (1) AU2004224061B2 (pt)
BR (1) BRPI0408697A (pt)
CA (1) CA2519956C (pt)
GB (1) GB0306718D0 (pt)
MX (1) MXPA05010340A (pt)
WO (1) WO2004085457A2 (pt)

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MY145464A (en) * 2005-08-31 2012-02-15 Hoffmann La Roche Pyrazolone derivatives as 11-beta hsd1 inhibitors
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WO2012099904A1 (en) 2011-01-18 2012-07-26 General Atomics Hydrolase enzyme substrates and uses thereof
HUP1100453A2 (en) * 2011-08-19 2013-02-28 Richter Gedeon Nyrt Carboxamides with sterane skeleton as h3 antagonists
CN102952168A (zh) * 2012-12-12 2013-03-06 中国药科大学 一类作为血管抑制剂的雌甾衍生物、其制备方法和医药用途
JP6556125B2 (ja) * 2013-06-25 2019-08-07 フォレンド ファーマ リミテッド １７β−ヒドロキシステロイドデヒドロゲナーゼの阻害剤としての治療的に活性な１７−窒素置換エストラトリエンチアゾール誘導体
TW201512215A (zh) 2013-06-25 2015-04-01 Forendo Pharma Ltd 治療活性雌三烯噻唑衍生物
JP6456373B2 (ja) * 2013-06-25 2019-01-23 フォレンド ファーマ リミテッド １７β−ヒドロキシステロイドデヒドロゲナーゼ タイプ１の阻害剤として治療活性のあるエストラトリエンチアゾール誘導体
CN107207561B (zh) * 2014-12-23 2020-03-31 佛恩多制药有限公司 17β-HSD1–抑制剂的前药
JP6545266B2 (ja) * 2014-12-23 2019-07-17 フォレンド ファーマ リミテッド １７β‐ＨＳＤ１抑制剤のプロドラッグ
CZ307437B6 (cs) 2016-06-07 2018-08-22 Ăšstav organickĂ© chemie a biochemie AV ÄŚR, v.v.i. 15β-substituované deriváty estronu jako selektivní inhibitory 17β-hydroxysteoiddehydrogenáz
MA45599A (fr) * 2016-07-11 2019-05-15 Sage Therapeutics Inc Stéroïdes neuroactifs substitués en c17, c20 et c21 et leurs procédés d'utilisation
EP3500265B1 (en) * 2016-08-22 2023-10-04 Or-Genix Therapeutics, Inc. Estrogen receptor beta selective ligands
HRP20240679T1 (hr) 2017-06-08 2024-08-16 Organon R&D Finland Ltd 17-oksimi 15.beta.-[3-propanamido]-supstituiranih etera-1,3,5(10)-trien-17-ona za uporabu u inhibiciji 17.beta.-hidroksisteroid dehidrogenaza
JP7417608B2 (ja) 2018-12-05 2024-01-18 フォレンド ファーマ リミテッド １７－ｈｓｄ１阻害剤としての１６（１７）位でピラゾール環と縮合しているエストラ－１，３，５（１０）－トリエン化合物
CN114085216B (zh) * 2021-11-15 2025-06-24 兰州大学 一类烯基吲哚衍生物的合成方法

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US6046186A (en) * 1997-12-24 2000-04-04 Sri International Estrone sulfamate inhibitors of estrone sulfatase, and associated pharmaceutical compositions and methods of use
GB0020498D0 (en) 2000-08-18 2000-10-11 Sterix Ltd Compound
GB0025788D0 (en) * 2000-10-20 2000-12-06 Sterix Ltd Use
US6476012B2 (en) 2001-01-25 2002-11-05 Yale University Estradiol-16α-carboxylic acid esters as locally active estrogens

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US8003783B2 (en) 2011-08-23
WO2004085457A3 (en) 2005-02-03
EP2336146A1 (en) 2011-06-22
EP1631579A2 (en) 2006-03-08
JP5000294B2 (ja) 2012-08-15
AU2004224061B2 (en) 2011-06-16
JP2006521338A (ja) 2006-09-21
CN100526328C (zh) 2009-08-12
WO2004085457A2 (en) 2004-10-07
CN1791611A (zh) 2006-06-21
GB0306718D0 (en) 2003-04-30
MXPA05010340A (es) 2006-04-18
US20060074060A1 (en) 2006-04-06
CA2519956C (en) 2012-12-18
AU2004224061A1 (en) 2004-10-07
CA2519956A1 (en) 2004-10-07

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