BR112015031846A2 - derivados de estratrientiazol substituído por 17-nitrogênio terapeuticamente ativos como inibidores de 17.beta-hidroxiesteroide desidrogenase - Google Patents

derivados de estratrientiazol substituído por 17-nitrogênio terapeuticamente ativos como inibidores de 17.beta-hidroxiesteroide desidrogenase

Info

Publication number
BR112015031846A2
BR112015031846A2 BR112015031846A BR112015031846A BR112015031846A2 BR 112015031846 A2 BR112015031846 A2 BR 112015031846A2 BR 112015031846 A BR112015031846 A BR 112015031846A BR 112015031846 A BR112015031846 A BR 112015031846A BR 112015031846 A2 BR112015031846 A2 BR 112015031846A2
Authority
BR
Brazil
Prior art keywords
stratrientiazole
derivatives
therapeutically active
dehydrogenase inhibitors
nitrogen substituted
Prior art date
Application number
BR112015031846A
Other languages
English (en)
Other versions
BR112015031846A8 (pt
Inventor
Kangas Lauri
HIRVELÄ Leena
Eloranta Maire
Unkila Mikko
Koskimies Pasi
Lammintausta Risto
Original Assignee
Forendo Pharma 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 Forendo Pharma Ltd filed Critical Forendo Pharma Ltd
Publication of BR112015031846A2 publication Critical patent/BR112015031846A2/pt
Publication of BR112015031846A8 publication Critical patent/BR112015031846A8/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J43/00—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton
    • C07J43/003—Normal steroids having a nitrogen-containing hetero ring spiro-condensed or not condensed with the cyclopenta(a)hydrophenanthrene skeleton not condensed
    • 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
    • A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
    • 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
    • A61P13/00—Drugs for disorders of the urinary system
    • 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
    • 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
    • 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
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/12—Ophthalmic agents for cataracts
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0042—Nitrogen only
    • C07J71/0052—Nitrogen only at position 16(17)
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J71/00—Steroids in which the cyclopenta(a)hydrophenanthrene skeleton is condensed with a heterocyclic ring
    • C07J71/0036—Nitrogen-containing hetero ring
    • C07J71/0057—Nitrogen and oxygen
    • C07J71/0068—Nitrogen and oxygen at position 16(17)

Abstract

a invenção refere-se a compostos de fórmula (i) e sais farmaceuticamente aceitáveis dos mesmos em que r2 a r7 são como definidos nas reivindicações. a invenção também se refere a seu uso como inibidores de 17ß-hsd e em tratamento ou prevenção de doenças ou distúrbios dependentes de hormônio esteroide, tais como doenças ou distúrbios dependentes de hormônio esteroide requerendo a inibição da enzima 17ß-hsd1 e/ou requerendo a redução da concentração de estradiol endógeno. a presente invenção também se refere à preparação dos compostos anteriormente mencionados e às composições farmacêuticas compreendendo, como um ingrediente ativo, um ou mais dos compostos anteriormente mencionados ou sais farmaceuticamente aceitáveis dos mesmos.
BR112015031846A 2013-06-25 2014-06-25 derivados de estratrientiazol, seus usos, e composição farmacêutica BR112015031846A8 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
FI20135694 2013-06-25
PCT/FI2014/050518 WO2014207310A1 (en) 2013-06-25 2014-06-25 Therapeutically active 17-nitrogen substituted estratrienthiazole derivatives as inhibitors of 17.beta.-hydroxysteroid dehydrogenase

Publications (2)

Publication Number Publication Date
BR112015031846A2 true BR112015031846A2 (pt) 2017-07-25
BR112015031846A8 BR112015031846A8 (pt) 2018-03-06

Family

ID=51220584

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112015031846A BR112015031846A8 (pt) 2013-06-25 2014-06-25 derivados de estratrientiazol, seus usos, e composição farmacêutica

Country Status (18)

Country Link
US (1) US9663549B2 (pt)
EP (1) EP3013846B1 (pt)
JP (1) JP6556125B2 (pt)
KR (1) KR20160042873A (pt)
CN (1) CN105518015B (pt)
AR (1) AR096729A1 (pt)
AU (1) AU2014300894A1 (pt)
BR (1) BR112015031846A8 (pt)
CA (1) CA2914667A1 (pt)
EA (1) EA201690077A1 (pt)
HK (1) HK1217495A1 (pt)
IL (1) IL242968A0 (pt)
MA (1) MA38694B1 (pt)
MX (1) MX2015017879A (pt)
SG (1) SG11201510251TA (pt)
TN (1) TN2015000555A1 (pt)
TW (1) TW201534612A (pt)
WO (1) WO2014207310A1 (pt)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
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
CN110945007B (zh) 2017-06-08 2022-11-18 佛恩多制药有限公司 用于抑制17β-羟基类固醇脱氢酶的15β-[3-丙酰氨基]-取代的雌-1,3,5(10)-三烯-17-酮化合物及其17-肟
CN113412269A (zh) * 2018-12-05 2021-09-17 佛恩多制药有限公司 作为17-hsd1抑制剂的在位置16(17)具有缩合的吡唑环的雌甾-1,3,5(10)-三烯化合物
CN114644673B (zh) * 2020-12-19 2023-12-26 上海喀露蓝科技有限公司 一种雌二醇衍生物、其制备方法及其在医药上的用途

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JP2002506077A (ja) 1998-03-11 2002-02-26 アンドルシェルシュ・インコーポレイテッド タイプ５およびタイプ３１７β−ヒドロキシステロイドデヒドロゲナーゼのインヒビターおよびその使用法
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GB9929302D0 (en) 1999-12-11 2000-02-02 Univ Cardiff Benzyl tetralins compositions and uses thereof
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MXPA05006485A (es) 2002-12-17 2005-08-26 Schering Corp Inhibidores de la 17 beta-hidroxiesteroide deshidrogenasa tipo 3 para el tratamiento de enfermedades dependientes de androgeno.
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Also Published As

Publication number Publication date
WO2014207310A1 (en) 2014-12-31
AU2014300894A1 (en) 2016-01-28
IL242968A0 (en) 2016-02-01
US20170081357A1 (en) 2017-03-23
CN105518015A (zh) 2016-04-20
MX2015017879A (es) 2017-03-01
TN2015000555A1 (en) 2017-04-06
EP3013846B1 (en) 2017-08-09
EP3013846A1 (en) 2016-05-04
KR20160042873A (ko) 2016-04-20
MA38694A2 (fr) 2017-12-29
JP6556125B2 (ja) 2019-08-07
AR096729A1 (es) 2016-01-27
JP2016523886A (ja) 2016-08-12
MA38694B1 (fr) 2020-01-31
SG11201510251TA (en) 2016-01-28
EA201690077A1 (ru) 2016-09-30
BR112015031846A8 (pt) 2018-03-06
US9663549B2 (en) 2017-05-30
HK1217495A1 (zh) 2017-01-13
CA2914667A1 (en) 2014-12-31
CN105518015B (zh) 2017-09-15
TW201534612A (zh) 2015-09-16

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Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

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B350 Update of information on the portal [chapter 15.35 patent gazette]