[go: up one dir, main page]

BR0012489A - Composto, composição farmacêutica, uso de um composto, e, kit para a contracepção masculina - Google Patents

Composto, composição farmacêutica, uso de um composto, e, kit para a contracepção masculina

Info

Publication number
BR0012489A
BR0012489A BR0012489-3A BR0012489A BR0012489A BR 0012489 A BR0012489 A BR 0012489A BR 0012489 A BR0012489 A BR 0012489A BR 0012489 A BR0012489 A BR 0012489A
Authority
BR
Brazil
Prior art keywords
compound
alkyl
kit
pharmaceutical composition
hydrogen
Prior art date
Application number
BR0012489-3A
Other languages
English (en)
Inventor
Hubert Jan Jozef Loozen
Dirk Leysen
Jaap Van Der Louw
Original Assignee
Akzo Nobel Nv
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 Akzo Nobel Nv filed Critical Akzo Nobel Nv
Publication of BR0012489A publication Critical patent/BR0012489A/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified
    • C07J1/0074Esters
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/16Masculine contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/26Androgens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07JSTEROIDS
    • C07J1/00Normal steroids containing carbon, hydrogen, halogen or oxygen, not substituted in position 17 beta by a carbon atom, e.g. estrane, androstane
    • C07J1/0051Estrane derivatives
    • C07J1/0066Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa
    • C07J1/007Estrane derivatives substituted in position 17 beta not substituted in position 17 alfa the substituent being an OH group free esterified or etherified

Landscapes

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

Abstract

"COMPOSTO, COMPOSIçãO FARMACêUTICA, USO DE UM COMPOSTO, E, KIT PARA A CONTRACEPçãO MASCULINA". Andrógenos oralmente ativos, novos, são derivados de <30>^ 14^-nandrolona 7<244> substituídos. Os compostos satisfazem à fórmula (I) em que R~ 1~ é O, (H, H), (H,OR), NOR, com R sendo hidrogênio, alquila (C~ 1-6~) ou acila (C~ 1-6~); R~ 2~ é selecionado a partir do grupo, que consiste em alquila (C~ 2-4~), alquenila (C~ 2-4~), ou alquinila (C~ 2-4~), cada qual opcionalmente substituido por halogênio; ou R~ 2~ é ciclopropila, ou ciclopropenila, cada qual opcionalmente substituído por alquila (C~ 1-2~), ou halogênio; R~ 3~ é hidrogênio, alquila (C~ 1-2~), ou etenila; R~ 4~ é alquila (C~ 1-2~); R~ 5~ é hidrogênio, ou acila (C~ 1-15~); e as linhas pontilhadas indicam ligações opcionais.
BR0012489-3A 1999-07-16 2000-07-10 Composto, composição farmacêutica, uso de um composto, e, kit para a contracepção masculina BR0012489A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP99202348 1999-07-16
PCT/EP2000/006544 WO2001005806A1 (en) 1999-07-16 2000-07-10 Orally active androgens

Publications (1)

Publication Number Publication Date
BR0012489A true BR0012489A (pt) 2002-04-02

Family

ID=8240463

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0012489-3A BR0012489A (pt) 1999-07-16 2000-07-10 Composto, composição farmacêutica, uso de um composto, e, kit para a contracepção masculina

Country Status (28)

Country Link
US (3) US6313108B1 (pt)
EP (1) EP1203011B1 (pt)
JP (1) JP2003505394A (pt)
KR (1) KR20020092890A (pt)
CN (1) CN1360589A (pt)
AR (1) AR024746A1 (pt)
AT (1) ATE257159T1 (pt)
AU (1) AU770412B2 (pt)
BR (1) BR0012489A (pt)
CA (1) CA2379223A1 (pt)
CO (1) CO5200765A1 (pt)
CZ (1) CZ2002192A3 (pt)
DE (1) DE60007530T2 (pt)
ES (1) ES2213596T3 (pt)
HK (1) HK1043797A1 (pt)
HU (1) HUP0201952A3 (pt)
IL (1) IL147332A0 (pt)
MX (1) MXPA02000601A (pt)
NO (1) NO20020222L (pt)
NZ (1) NZ516525A (pt)
PE (1) PE20010330A1 (pt)
PL (1) PL353007A1 (pt)
RU (1) RU2002103883A (pt)
SK (1) SK712002A3 (pt)
TR (1) TR200200076T2 (pt)
TW (1) TW548277B (pt)
WO (1) WO2001005806A1 (pt)
ZA (1) ZA200200106B (pt)

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6756366B1 (en) * 1999-04-06 2004-06-29 Akzo Nobel N.V. Orally active androgens
US20030069215A1 (en) * 2001-03-30 2003-04-10 The Government Of The United States Of America, Methods of making and using 7a,11b-dimethyl-17b-hydroxy-4-estren-3-one 17b-trans-4-n-butylcyclohexane carboxylate and 7a,11b-dimethyl-17b-hydroxyestr-4-en-3-one 17-undecanoate
CA2402524C (en) * 2000-03-31 2009-11-17 Richard P. Blye Methods of making and using 7.alpha.,11.beta.-dimethyl-17.beta.-hydroxy-4-estren-3-one 17.beta.-trans-4-n-butylcyclohexane carboxylate and 7.alpha.,11.beta.-dimethyl-17.beta.-hydroxyestr-4-en-3-one 17-undecanoate
MXPA03000845A (es) * 2000-07-28 2004-04-05 Akzo Nobel Nv Estrogenos substituidos por 16alfa-metilo o etilo.
JP2005510541A (ja) * 2001-03-30 2005-04-21 アメリカ合衆国 7α,11β−ジメチル−17β−ヒドロキシエストラ−4,14−ジエン−3−オン及びその17エステルの製造方法及びそれらを含有する医薬製剤
TWI322813B (en) * 2002-01-21 2010-04-01 Organon Nv Process for the preparation of 7alpha-methylsteroids
GB0304927D0 (en) * 2003-03-04 2003-04-09 Resolution Chemicals Ltd Process for the production of tibolone
PE20050677A1 (es) 2003-12-22 2005-10-04 Akzo Nobel Nv Esteroides con perfil androgenico y progestagenico mixto
UA89964C2 (ru) 2004-09-08 2010-03-25 Н.В. Органон 15β-ЗАМЕЩЕННЫЕ СТЕРОИДЫ, КОТОРЫЕ ИМЕЮТ СЕЛЕКТИВНУЮ ЭСТРОГЕННУЮ АКТИВНОСТЬ
EP2350111A1 (en) * 2008-10-15 2011-08-03 Synthon B.V. Processes and intermediates for the production of fulvestrant
CN107266514A (zh) 2011-06-01 2017-10-20 埃斯特拉私人有限责任公司 用于产生雌四醇中间体的方法
BR112013030833B1 (pt) * 2011-06-01 2019-09-03 Estetra S A processo para a preparação de um composto de fórmula (i) e processo para a preparação de estetrol
EP2383279A1 (en) 2011-07-19 2011-11-02 Pantarhei Bioscience B.V. Process for the preparation of estetrol
PT2764008T (pt) * 2011-10-07 2016-11-10 Estetra Sprl Processo para a produção de estetrol
WO2015181116A1 (en) 2014-05-26 2015-12-03 Crystal Pharma, S.A.U. Process and intermediades for the preparation of 7-alkylated steroids
WO2016203009A1 (en) 2015-06-18 2016-12-22 Mithra Pharmaceuticals S.A. Orodispersible tablet containing estetrol
US20160367567A1 (en) 2015-06-18 2016-12-22 Mithra Pharmaceuticals S.A. Orodispersible dosage unit containing an estetrol component
EP3310346B1 (en) 2015-06-18 2021-03-24 Estetra SPRL Orodispersible tablet containing estetrol
PL3310333T3 (pl) 2015-06-18 2020-07-13 Estetra Sprl Ulegająca rozpadowi w jamie ustnej jednostka dawkowana zawierająca składnik estetrolowy
CA3178291A1 (en) 2016-08-05 2018-04-12 Estetra Srl Method for the management of dysmenorrhea and menstrual pain
ES2906117T3 (es) * 2017-02-23 2022-04-13 Siemens Healthcare Diagnostics Inc Conjugados de androstenodiona quimioluminiscente
JOP20200260A1 (ar) 2018-04-19 2019-10-19 Estetra Sprl مركبات واستخداماتها للتخفيف من الأعراض المصاحبة لانقطاع الطمث
TWI801561B (zh) 2018-04-19 2023-05-11 比利時商依思特拉私人有限責任公司 化合物及其用於緩解絕經相關症狀的用途
TWI893101B (zh) 2020-04-16 2025-08-11 比利時商埃斯特拉有限責任公司 具有降低之副作用之避孕組成物

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA712312B (en) * 1970-04-28 1972-01-26 Ochsner Med Found Alton 4,14-estradiene compounds

Also Published As

Publication number Publication date
HUP0201952A3 (en) 2003-10-28
US20020022609A1 (en) 2002-02-21
ZA200200106B (en) 2003-06-25
WO2001005806A1 (en) 2001-01-25
PL353007A1 (en) 2003-09-22
AU770412B2 (en) 2004-02-19
US6780854B2 (en) 2004-08-24
AR024746A1 (es) 2002-10-23
DE60007530T2 (de) 2004-12-23
EP1203011B1 (en) 2004-01-02
ATE257159T1 (de) 2004-01-15
DE60007530D1 (de) 2004-02-05
CN1360589A (zh) 2002-07-24
AU6562900A (en) 2001-02-05
TR200200076T2 (tr) 2002-04-22
US6541465B2 (en) 2003-04-01
US6313108B1 (en) 2001-11-06
SK712002A3 (en) 2002-06-04
EP1203011A1 (en) 2002-05-08
NO20020222L (no) 2002-01-25
CA2379223A1 (en) 2001-01-25
HK1043797A1 (zh) 2002-09-27
MXPA02000601A (es) 2002-07-30
JP2003505394A (ja) 2003-02-12
NZ516525A (en) 2003-06-30
IL147332A0 (en) 2002-08-14
CO5200765A1 (es) 2002-09-27
TW548277B (en) 2003-08-21
RU2002103883A (ru) 2004-02-27
CZ2002192A3 (cs) 2002-06-12
US20030087886A1 (en) 2003-05-08
ES2213596T3 (es) 2004-09-01
HUP0201952A2 (en) 2002-10-28
PE20010330A1 (es) 2001-03-22
NO20020222D0 (no) 2002-01-15
KR20020092890A (ko) 2002-12-12

Similar Documents

Publication Publication Date Title
BR0012489A (pt) Composto, composição farmacêutica, uso de um composto, e, kit para a contracepção masculina
MX222092B (es) Derivados de n2-fenil-amidina.
BR0012434A (pt) Composto, processo para a preparação do mesmo, uso de um composto, composição farmacêutica.
BR0207216A (pt) Derivados de tieno 2,3-d-pirimidindiona como inibidores de metaloproteinase matriz
DK1177176T3 (da) Triarylsyrederivater som PPAR-receptorligander
BR9813989A (pt) Composto, processo para prepará-lo, uso do mesmo, composição farmacêutica, e, processo para o tratamento de um paciente sofrendo de uma condição
BR0309534A (pt) Composto, composição farmacêutica, e, uso de um composto
BRPI0408284B8 (pt) compostos derivados de ftalazinona, seu uso e composição farmacêutica compreendendo os mesmos
DK1392714T3 (da) Steroider som agonister for FXR
BR0214023A (pt) Derivados de 1,2,4-tiadiazólio como moduladores de receptor de melanocortina
BR0014060A (pt) Derivado de quinolil propil piperidina, processo para preparação do mesmo, e, composição farmacêutica
BR9803179A (pt) Antagonistas receptores de ccr-3.
BR0115580A (pt) Derivados de 3-aroilindol e a utilizaçao dos mesmos como agonistas dos receptores cb2
AR005706A1 (es) Inhibidores egfr de 4-aminoquinzolina, procedimiento para su obtencion, composicion farmaceutica que los contiene, uso de los mismos para lapreparacion de un medicamento util como agente antineoplasico
BR9915403A (pt) Antagonistas receptores iii de 4-aroil-piperidin-ccr-3
PE20020473A1 (es) USO COMBINADO DE INHIBIDORES DE ACETILCOLINESTERASA Y AGONISTAS INVERSOS DE GABAa PARA EL TRATAMIENTO DE TRASTORNOS COGNITIVOS
HRP20090162T1 (en) Quinolinone-carboxamide compounds as 5-ht4 receptor agonists
BR9915735A (pt) Antagonistas receptores de ccr-3 de piperidina
BR0212353A (pt) Composto, composição farmacêutica, e, uso de um composto
DK1204658T3 (da) Benzofurylpiperazin-serotoninagonister
BR0211425A (pt) Método para a preparação de compostos, e, uso de uma composição
BRPI0510397A (pt) compostos, composições farmacêuticas contendo os mesmos, e métodos de uso dos mesmos
BR0013769A (pt) Esteróides estrogênicos não aromáticos, composição farmacêutica, e, uso de um composto esteróide
BR0308890A (pt) Composto
MX9101948A (es) Composicion farmaceutica que contiene derivados de tiazoloisoindolinona

Legal Events

Date Code Title Description
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 5A, 6A E 7A ANUIDADES.

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

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 1927 DE 11/12/2007.