BRPI0920459B1 - Compostos antagonistas de receptor de mineralocorticoide, composição farmacêutica e método in vitro de inibição da atividade do receptor de mineralocorticoide - Google Patents

Compostos antagonistas de receptor de mineralocorticoide, composição farmacêutica e método in vitro de inibição da atividade do receptor de mineralocorticoide Download PDF

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Publication number
BRPI0920459B1
BRPI0920459B1 BRPI0920459-8A BRPI0920459A BRPI0920459B1 BR PI0920459 B1 BRPI0920459 B1 BR PI0920459B1 BR PI0920459 A BRPI0920459 A BR PI0920459A BR PI0920459 B1 BRPI0920459 B1 BR PI0920459B1
Authority
BR
Brazil
Prior art keywords
group
phenyl
methyl
compound
hydroxy
Prior art date
Application number
BRPI0920459-8A
Other languages
English (en)
Portuguese (pt)
Inventor
John Nuss
Matthew Williams
Tie-Lin Wang
Kazumasa Aoki
Raju Mohan
Richard Martin
Hiroyuki Tsuruoka
Noriyuki Hayashi
Tsuyoshi Homma
Original Assignee
Exelixis, Inc
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 Exelixis, Inc filed Critical Exelixis, Inc
Publication of BRPI0920459A2 publication Critical patent/BRPI0920459A2/pt
Publication of BRPI0920459B1 publication Critical patent/BRPI0920459B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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 ring carbon atoms
    • 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • 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
    • A61P5/38—Drugs for disorders of the endocrine system of the suprarenal hormones
    • A61P5/42—Drugs for disorders of the endocrine system of the suprarenal hormones for decreasing, blocking or antagonising the activity of mineralocorticosteroids
    • 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
    • A61P7/10—Antioedematous agents; Diuretics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/325—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with substituted hydrocarbon radicals directly attached to the ring nitrogen atom

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Biomedical Technology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
BRPI0920459-8A 2008-10-08 2009-10-07 Compostos antagonistas de receptor de mineralocorticoide, composição farmacêutica e método in vitro de inibição da atividade do receptor de mineralocorticoide BRPI0920459B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US10371508P 2008-10-08 2008-10-08
US61/103,715 2008-10-08
PCT/US2009/059847 WO2010042622A1 (en) 2008-10-08 2009-10-07 Atropisomers of (hydroxyalkyl) pyrrole derivatives

Publications (2)

Publication Number Publication Date
BRPI0920459A2 BRPI0920459A2 (pt) 2020-08-11
BRPI0920459B1 true BRPI0920459B1 (pt) 2021-12-14

Family

ID=41360127

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0920459-8A BRPI0920459B1 (pt) 2008-10-08 2009-10-07 Compostos antagonistas de receptor de mineralocorticoide, composição farmacêutica e método in vitro de inibição da atividade do receptor de mineralocorticoide

Country Status (12)

Country Link
US (1) US8487117B2 (Direct)
EP (1) EP2349997B1 (Direct)
JP (2) JP5767586B2 (Direct)
KR (1) KR101643285B1 (Direct)
CN (1) CN102186817B (Direct)
AU (1) AU2009302371B2 (Direct)
BR (1) BRPI0920459B1 (Direct)
CA (1) CA2736923C (Direct)
ES (1) ES2547697T3 (Direct)
IL (1) IL212170A (Direct)
TW (2) TWI593674B (Direct)
WO (1) WO2010042622A1 (Direct)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105473552B (zh) * 2013-08-27 2017-11-10 第一三共株式会社 用于产生吡咯衍生物及其中间体的方法
CN112707854B (zh) * 2019-10-25 2022-03-15 年衍药业(珠海)有限公司 吡咯酰胺类化合物及其用途
CA3213094A1 (en) * 2021-03-30 2022-10-06 Qiao ZONG Crystalline form of pyrrole amide compound, preparation method therefor and use thereof
CN115784961B (zh) * 2021-09-10 2026-03-31 上海鼎雅药物化学科技有限公司 埃沙西林酮及其中间体的合成方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8026237B2 (en) * 2004-07-30 2011-09-27 Exelixis, Inc. Pyrrole derivatives as pharmaceutical agents
ES2448498T3 (es) * 2007-04-09 2014-03-14 Daiichi Sankyo Company, Limited Atropisómero de derivado de pirrol

Also Published As

Publication number Publication date
TW201028377A (en) 2010-08-01
AU2009302371B2 (en) 2015-02-12
BRPI0920459A2 (pt) 2020-08-11
JP6121952B2 (ja) 2017-04-26
IL212170A (en) 2016-03-31
AU2009302371A1 (en) 2010-04-15
US8487117B2 (en) 2013-07-16
TWI547479B (zh) 2016-09-01
ES2547697T3 (es) 2015-10-08
EP2349997A1 (en) 2011-08-03
HK1155163A1 (zh) 2012-05-11
TW201627283A (zh) 2016-08-01
JP2012505225A (ja) 2012-03-01
KR101643285B1 (ko) 2016-07-29
EP2349997B1 (en) 2015-08-12
CA2736923C (en) 2016-11-22
IL212170A0 (en) 2011-06-30
CA2736923A1 (en) 2010-04-15
TWI593674B (zh) 2017-08-01
JP5767586B2 (ja) 2015-08-19
US20110263673A1 (en) 2011-10-27
WO2010042622A1 (en) 2010-04-15
KR20110091663A (ko) 2011-08-12
CN102186817A (zh) 2011-09-14
JP2014196365A (ja) 2014-10-16
CN102186817B (zh) 2017-05-17

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B25G Requested change of headquarter approved

Owner name: EXELIXIS, INC. (US) ; DAIICHI SANKYO COMPANY, LIMITED (JP)

B25G Requested change of headquarter approved

Owner name: EXELIXIS, INC. (US) ; DAIICHI SANKYO COMPANY, LIMITED (JP)

B25A Requested transfer of rights approved

Owner name: EXELIXIS, INC. (US)

B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 07/10/2009, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF, QUE DETERMINA A ALTERACAO DO PRAZO DE CONCESSAO.