BRPI0519443A2 - composto orgÂnicos - Google Patents

composto orgÂnicos

Info

Publication number
BRPI0519443A2
BRPI0519443A2 BRPI0519443-1A BRPI0519443A BRPI0519443A2 BR PI0519443 A2 BRPI0519443 A2 BR PI0519443A2 BR PI0519443 A BRPI0519443 A BR PI0519443A BR PI0519443 A2 BRPI0519443 A2 BR PI0519443A2
Authority
BR
Brazil
Prior art keywords
treatment
substituted pyrrolidine
compound
compounds
renin
Prior art date
Application number
BRPI0519443-1A
Other languages
English (en)
Inventor
Werner Breitenstein
Sylvain Cottens
Claus Ehrhardt
Edgar Jacoby
Edwige Liliane Jeann Lorthiois
Juergen Klaus Maibaum
Nils Ostermann
Holger Sellner
Oliver Simic
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
Application filed by Novartis Ag filed Critical Novartis Ag
Publication of BRPI0519443A2 publication Critical patent/BRPI0519443A2/pt

Links

Classifications

    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, 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
    • 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
    • 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
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • A61P5/38—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
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—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 no 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
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychiatry (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

COMPOSTOS ORGÂNICOS. A presente invenção refere-se a compostos de pirrolidina 3-mono-, 3,4-di- e 3,4,4-trissubstituída, estes compostos para o uso no tratamento diagnóstico e terapêutico de um animal de sangue quente, especialmente para o tratamento de uma doença (=distúrbio) que depende da atividade inapropriada de renina; o uso de um composto desta classe para a preparação de uma formulação farmacêutica para o tratamento de uma doença que depende da atividade inapropriada de renina; o uso de um composto desta classe no tratamento de uma doença que depende da atividade inapropriada de renina; formulações farmacêuticas compreendendo um dito composto de pirrolidina substituida, e/ou um método de tratamento compreendendo administrar um dito composto de pirrolidina substituida, um método para a fabricação dos ditos compostos de pirrolidina substituida, e intermediários novos e etapas parciais para sua síntese são descritos. Os compostos de pirrolidina substituida são especialmente da fórmula 1 em que os substituintes são como descritos no relatório descritivo.
BRPI0519443-1A 2004-12-23 2005-12-21 composto orgÂnicos BRPI0519443A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0428250.5A GB0428250D0 (en) 2004-12-23 2004-12-23 Organic compounds
PCT/EP2005/013786 WO2006066896A2 (en) 2004-12-23 2005-12-21 Pyrrolidine derivatives for the treatment of a disease depending on the activity of renin

Publications (1)

Publication Number Publication Date
BRPI0519443A2 true BRPI0519443A2 (pt) 2009-01-27

Family

ID=34113181

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0519443-1A BRPI0519443A2 (pt) 2004-12-23 2005-12-21 composto orgÂnicos

Country Status (14)

Country Link
US (1) US20100087427A1 (pt)
EP (1) EP1836163B1 (pt)
JP (1) JP2008525350A (pt)
KR (1) KR20070088806A (pt)
CN (1) CN101115715A (pt)
AT (1) ATE482192T1 (pt)
AU (1) AU2005318392B2 (pt)
BR (1) BRPI0519443A2 (pt)
CA (1) CA2589331A1 (pt)
DE (1) DE602005023782D1 (pt)
GB (1) GB0428250D0 (pt)
MX (1) MX2007007772A (pt)
RU (1) RU2007128074A (pt)
WO (1) WO2006066896A2 (pt)

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GB0428526D0 (en) 2004-12-30 2005-02-09 Novartis Ag Organic compounds
US7820699B2 (en) 2005-04-27 2010-10-26 Hoffmann-La Roche Inc. Cyclic amines
GB0514203D0 (en) 2005-07-11 2005-08-17 Novartis Ag Organic compounds
BRPI0620736A2 (pt) 2005-12-30 2011-12-20 Novartis Ag compostos orgánicos
GB0611697D0 (en) * 2006-06-13 2006-07-26 Novartis Ag Organic compounds
GB0611696D0 (en) * 2006-06-13 2006-07-26 Novartis Ag Organic compounds
EP2119702A4 (en) * 2007-01-31 2010-12-08 Dainippon Sumitomo Pharma Co amide derivative
JP2010189275A (ja) * 2007-06-14 2010-09-02 Dainippon Sumitomo Pharma Co Ltd ナフタレン誘導体
SG182223A1 (en) 2007-06-25 2012-07-30 Novartis Ag N5-(2-ethoxyethyl)-n3-(2-pyridinyl)-3,5-piperidinedicarboxamide derivatives for use as renin inhibitors
JP5484069B2 (ja) 2007-12-19 2014-05-07 大日本住友製薬株式会社 二環性へテロ環誘導体
KR20120109292A (ko) 2009-06-24 2012-10-08 다이닛본 스미토모 세이야꾸 가부시끼가이샤 Ｎ-치환-시클릭 아미노 유도체
US8426414B2 (en) * 2009-10-09 2013-04-23 Bristol-Myers Squibb Company Modulators of G protein-coupled receptor 88
TWI562977B (en) 2010-11-05 2016-12-21 Bayer Ip Gmbh Process for the preparation of substituted n-(benzyl)cyclopropanamines by imine hydrogenation
RU2698697C2 (ru) 2013-12-23 2019-08-29 Байер Фарма Акциенгезельшафт Конъюгаты связующего (ADC) с ингибиторами KSP
CA2970565A1 (en) 2014-12-15 2016-06-23 Bayer Pharma Aktiengesellschaft Antibody-drug conjugates (adcs) of ksp inhibitors with aglycosylated anti-tweakr antibodies
JP6971858B2 (ja) 2015-06-22 2021-11-24 バイエル ファーマ アクチエンゲゼルシャフト 酵素開裂性基を有する抗体薬物複合体（ａｄｃ）および抗体プロドラッグ複合体（ａｐｄｃ）
WO2016207104A1 (de) 2015-06-23 2016-12-29 Bayer Pharma Aktiengesellschaft Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit anti-b7h3-antikörpern
EP3313521A1 (de) 2015-06-23 2018-05-02 Bayer Pharma Aktiengesellschaft Antikörper-wirkstoff-konjugate (adcs) von ksp-inhibitoren mit anti-tweakr-antikörpern
EP3919518A1 (en) 2016-06-15 2021-12-08 Bayer Pharma Aktiengesellschaft Specific antibody-drug-conjugates (adcs) with ksp inhibitors and anti-cd123-antibodies
CN110312534B (zh) 2016-12-21 2023-04-04 拜耳制药股份公司 具有酶促可裂解基团的抗体-药物-缀合物(adc)
CN110072556B (zh) 2016-12-21 2023-05-02 拜耳制药股份公司 具有ksp抑制剂的特异性抗体药物缀合物(adc)
CN110256305B (zh) * 2019-07-24 2020-05-26 中国药科大学 一种萘磺酰胺类化合物、制备方法和应用
CN121609673A (zh) * 2026-02-02 2026-03-06 五邑大学 一种pde4抑制剂及其制备方法和应用

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Also Published As

Publication number Publication date
AU2005318392B2 (en) 2009-11-05
ATE482192T1 (de) 2010-10-15
GB0428250D0 (en) 2005-01-26
JP2008525350A (ja) 2008-07-17
MX2007007772A (es) 2007-08-08
CA2589331A1 (en) 2006-06-29
DE602005023782D1 (de) 2010-11-04
EP1836163B1 (en) 2010-09-22
AU2005318392A1 (en) 2006-06-29
EP1836163A2 (en) 2007-09-26
KR20070088806A (ko) 2007-08-29
WO2006066896A2 (en) 2006-06-29
CN101115715A (zh) 2008-01-30
US20100087427A1 (en) 2010-04-08
WO2006066896A3 (en) 2006-08-31
RU2007128074A (ru) 2009-01-27

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