AR070473A2 - Compuestos inhibidores de la renina, un procedimiento de preparacion del compuesto, una composicion farmaceutica, uso del compuesto para preparar un medicamento y compuesto intermediario - Google Patents

Compuestos inhibidores de la renina, un procedimiento de preparacion del compuesto, una composicion farmaceutica, uso del compuesto para preparar un medicamento y compuesto intermediario

Info

Publication number
AR070473A2
AR070473A2 ARP090100634A ARP090100634A AR070473A2 AR 070473 A2 AR070473 A2 AR 070473A2 AR P090100634 A ARP090100634 A AR P090100634A AR P090100634 A ARP090100634 A AR P090100634A AR 070473 A2 AR070473 A2 AR 070473A2
Authority
AR
Argentina
Prior art keywords
compound
compounds
rhinine
prepare
pharmaceutical composition
Prior art date
Application number
ARP090100634A
Other languages
English (en)
Inventor
Volker Breu
Wolfgang Wostl
Eric Vieira
Hans Peter Marki
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR070473A2 publication Critical patent/AR070473A2/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three 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
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61P13/12—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
    • 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
    • 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
    • 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
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/40—Oxygen atoms
    • C07D211/42—Oxygen atoms attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Pyridine Compounds (AREA)

Abstract

Los compuestos son utiles para el tratamiento de enfermedades que están asociadas con la restenosis, glaucoma, infarto cardíaco, presion sanguínea elevada y lesiones en el organo final. Por ej., insuficiencia cardíaca e insuficiencia renal. Reivindicacion 1: Compuestos de formula (1) en donde R1 es naftilo opcionalmente sustituido por uno a tres grupos alcoxilo C1-5; R2 es fenilo o bencilo, opcionalmente sustituido por sustituyentes seleccionados independientemente entre uno a tres grupos halogeno, ciano, alcoxilo C1-3 y nitro; R3 es H-[CH(OR4)]2-CH2-O-CH2- o R3a-(CH2)k-[CH(OR4)]l-CH2-O-; R3a es hidroxilo o alcoxilo C1-3; R4 es hidrogeno o C1-3-alquilo; k es 1 o 2; l es 1 o 2; y sales farmacéuticamente aceptables de los mismos. Reivindicacion 31: Los compuestos de formula (2) en donde P1 representa un grupo protector de NH usual tal como tert-butoxicarbonilo, benciloxicarbonilo, aliloxicarbonilo, viniloxicarbonilo, alquilsililalquiloxicarbonilo tal como 2-(trimetilsilil)etoxicarbonilo, y tricloroetoxicarbonilo; y R1, R2 y R3 son como se ha definido en la reivindicacion 1.
ARP090100634A 1999-04-27 2009-02-25 Compuestos inhibidores de la renina, un procedimiento de preparacion del compuesto, una composicion farmaceutica, uso del compuesto para preparar un medicamento y compuesto intermediario AR070473A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP99108199 1999-04-27

Publications (1)

Publication Number Publication Date
AR070473A2 true AR070473A2 (es) 2010-04-07

Family

ID=8238050

Family Applications (2)

Application Number Title Priority Date Filing Date
ARP000101954A AR018719A1 (es) 1999-04-27 2000-04-26 Inhibidores de renina.
ARP090100634A AR070473A2 (es) 1999-04-27 2009-02-25 Compuestos inhibidores de la renina, un procedimiento de preparacion del compuesto, una composicion farmaceutica, uso del compuesto para preparar un medicamento y compuesto intermediario

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ARP000101954A AR018719A1 (es) 1999-04-27 2000-04-26 Inhibidores de renina.

Country Status (35)

Country Link
US (2) US6376672B1 (es)
EP (1) EP1175400B1 (es)
JP (1) JP3808706B2 (es)
KR (1) KR100443684B1 (es)
CN (1) CN1147471C (es)
AR (2) AR018719A1 (es)
AT (1) ATE512949T1 (es)
AU (1) AU763718B2 (es)
BR (1) BR0010080B1 (es)
CA (1) CA2370888C (es)
CO (1) CO5170513A1 (es)
CZ (1) CZ302012B6 (es)
DK (1) DK1175400T3 (es)
EG (1) EG23979A (es)
ES (1) ES2366668T3 (es)
GC (1) GC0000251A (es)
HK (1) HK1045999B (es)
HR (1) HRP20010762A2 (es)
HU (1) HU227764B1 (es)
IL (2) IL146002A0 (es)
JO (1) JO2256B1 (es)
MA (1) MA26787A1 (es)
MX (1) MXPA01010934A (es)
MY (1) MY127894A (es)
NO (1) NO320803B1 (es)
NZ (1) NZ514981A (es)
PE (1) PE20010069A1 (es)
PL (1) PL199895B1 (es)
PT (1) PT1175400E (es)
RS (1) RS51156B (es)
RU (1) RU2213731C2 (es)
TR (1) TR200103095T2 (es)
TW (1) TWI224593B (es)
WO (1) WO2000064873A1 (es)
ZA (1) ZA200108735B (es)

Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6376672B1 (en) * 1999-04-27 2002-04-23 Hoffmann-La Roche Inc. Naphthalenylmethoxypiperidines as renin inhibitors
US6835686B2 (en) * 2001-07-05 2004-12-28 Millennium Specialty Chemicals Catalyst system and process for rearrangement of epoxides to allylic alcohols
BR0312000A (pt) * 2002-06-27 2005-03-22 Actelion Pharmaceuticals Ltd Compostos, composições farmacêuticas, método para o tratamento ou profilaxia de doenças, e, uso dos compostos
US20040214832A1 (en) * 2003-04-10 2004-10-28 Cuiman Cai Piperazine derivative renin inhibitors
DE602004010385D1 (de) * 2003-04-29 2008-01-10 Actelion Pharmaceuticals Ltd 3,4-disubstituierte 1,2,3,4-tetrahydropyridinderivate
TW200900399A (en) * 2003-10-01 2009-01-01 Speedel Experimenta Ag Organic compounds
AR045950A1 (es) * 2003-10-09 2005-11-16 Speedel Experimenta Ag Compuestos derivados de piperazina, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos.
WO2005037317A2 (en) * 2003-10-17 2005-04-28 Cornell Research Foundation, Inc. Mast cell-derived renin
CA2546264A1 (en) * 2003-11-26 2005-06-09 Novartis Ag 4-phenylpiperidine derivatives as renin inhibitors
AR053406A1 (es) * 2004-07-09 2007-05-09 Speedel Experimenta Ag Derivados de piperidina como inhibidores de renina. composiciones farmaceuticas
EP1799199B1 (en) 2004-10-08 2012-03-28 Novartis AG Use of renin inhibitors for the prevention or treatment of diastolic dysfunction or diastolic heart failure
GB0428526D0 (en) 2004-12-30 2005-02-09 Novartis Ag Organic compounds
GB0500784D0 (en) * 2005-01-14 2005-02-23 Novartis Ag Organic compounds
EP1707202A1 (de) * 2005-03-31 2006-10-04 Speedel Experimenta AG Organische Verbindungen
AR055756A1 (es) * 2005-03-31 2007-09-05 Speedel Experimenta Ag Piperidinas sustituidas; procesos de preparacion y su uso como medicamentos
TW200722424A (en) * 2005-03-31 2007-06-16 Speedel Experimenta Ag Substituted piperidines
EP1897879A3 (en) * 2005-03-31 2008-06-11 Speedel Experimenta AG 2,4,5-substituted piperidines as renin inhibitors
BRPI0609534A2 (pt) * 2005-03-31 2010-04-13 Speedel Experimenta Ag piperidinas 3,4,5-substituìdas
ES2352564T3 (es) * 2005-03-31 2011-02-21 Novartis Ag Piperidinas sustituidas.
JP4297972B2 (ja) 2005-05-27 2009-07-15 アクテリオン ファーマシューティカルズ リミテッド 新規なピペリジンカルボン酸アミド誘導体
GB0514203D0 (en) * 2005-07-11 2005-08-17 Novartis Ag Organic compounds
BRPI0617621A2 (pt) * 2005-10-21 2011-08-02 Novartis Ag combinação de compostos orgánicos
CN101356156B (zh) * 2005-11-14 2012-12-05 生命医药公司 天冬氨酸蛋白酶抑制剂
PT2420491E (pt) * 2005-12-30 2013-10-14 Novartis Ag Compostos de piperidina 3,5-substituída como inibidores de renina
TW200804359A (en) 2006-01-19 2008-01-16 Speedel Experimenta Ag Substituted 4-phenylpiperidines
EP1816122A3 (en) * 2006-01-19 2007-09-19 Speedel Experimenta AG 3,4,5-substituted piperidines as therapeutic compounds
TW200821303A (en) * 2006-08-08 2008-05-16 Speedel Experimenta Ag Organic compounds
WO2008021552A2 (en) * 2006-08-18 2008-02-21 Duke University Biased ligands and methods of identifying same
EP1908761A1 (en) * 2006-10-04 2008-04-09 Speedel Experimenta AG Organic compounds
EP1911758A1 (en) * 2006-10-04 2008-04-16 Speedel Experimenta AG Phenyl piperidine derivatives for use as renin inhibitors
ES2541107T3 (es) 2007-06-25 2015-07-16 Novartis Ag Derivados de N5-(2-etoxietil)-N3-(2-piridinil)-3,5-piperidindicarboxamida para su uso como inhibidores de renina
JP2011503022A (ja) * 2007-11-02 2011-01-27 ノバルティス アーゲー レニン阻害剤としての４，４−二置換ピペリジン
US10517839B2 (en) 2008-06-09 2019-12-31 Cornell University Mast cell inhibition in diseases of the retina and vitreous
WO2011045244A1 (en) 2009-10-14 2011-04-21 Rainer Oberbauer Acute kidney injury risk testing
WO2013045505A1 (en) 2011-09-28 2013-04-04 Novartis Ag Biomarkers for raas combination therapy
EP2810644A1 (en) 2013-06-06 2014-12-10 Ferrer Internacional, S.A. Oral formulation for the treatment of cardiovascular diseases
WO2018002673A1 (en) 2016-07-01 2018-01-04 N4 Pharma Uk Limited Novel formulations of angiotensin ii receptor antagonists

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DK231088D0 (da) 1988-04-28 1988-04-28 Ferrosan As Piperidinforbindelser, deres fremstilling og anvendelse
DE3640475A1 (de) 1986-11-27 1988-06-09 Hoechst Sa Lab Arzneimittel auf basis von derivaten des 3,4-diphenylpiperidins, die verwendung der derivate als arzneimittel sowie neue 3,4-diphenylpiperidinderivate und verfahren zu ihrer herstellung
WO1993000042A1 (en) 1991-06-24 1993-01-07 B.V. Optische Industrie 'de Oude Delft' Device for measuring the respiration of a person
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US6376672B1 (en) * 1999-04-27 2002-04-23 Hoffmann-La Roche Inc. Naphthalenylmethoxypiperidines as renin inhibitors

Also Published As

Publication number Publication date
HU227764B1 (en) 2012-02-28
CZ302012B6 (cs) 2010-09-08
MXPA01010934A (es) 2002-05-06
HK1045999B (zh) 2004-10-21
US6673931B2 (en) 2004-01-06
NO20015206L (no) 2001-10-25
AR018719A1 (es) 2001-11-28
CN1147471C (zh) 2004-04-28
YU77101A (sh) 2004-09-03
EG23979A (en) 2008-02-27
HUP0203669A2 (hu) 2003-02-28
HRP20010762A2 (en) 2005-02-28
HK1045999A1 (en) 2002-12-20
IL146002A0 (en) 2002-07-25
EP1175400B1 (en) 2011-06-15
CO5170513A1 (es) 2002-06-27
ATE512949T1 (de) 2011-07-15
HUP0203669A3 (en) 2003-12-29
NZ514981A (en) 2004-02-27
JO2256B1 (en) 2004-10-07
CN1349503A (zh) 2002-05-15
MA26787A1 (fr) 2004-12-20
KR20010109529A (ko) 2001-12-10
IL146002A (en) 2007-03-08
CA2370888C (en) 2005-08-23
JP3808706B2 (ja) 2006-08-16
NO20015206D0 (no) 2001-10-25
AU4296800A (en) 2000-11-10
CA2370888A1 (en) 2000-11-02
US20020087002A1 (en) 2002-07-04
DK1175400T3 (da) 2011-07-18
MY127894A (en) 2006-12-29
WO2000064873A1 (en) 2000-11-02
EP1175400A1 (en) 2002-01-30
TWI224593B (en) 2004-12-01
PT1175400E (pt) 2011-08-11
TR200103095T2 (tr) 2002-04-22
PL199895B1 (pl) 2008-11-28
PE20010069A1 (es) 2001-03-03
CZ20013854A3 (cs) 2002-04-17
RS51156B (sr) 2010-10-31
BR0010080B1 (pt) 2012-03-20
US6376672B1 (en) 2002-04-23
BR0010080A (pt) 2002-01-15
GC0000251A (en) 2006-11-01
PL353442A1 (en) 2003-11-17
JP2002543063A (ja) 2002-12-17
ES2366668T3 (es) 2011-10-24
KR100443684B1 (ko) 2004-08-09
ZA200108735B (en) 2003-01-23
RU2213731C2 (ru) 2003-10-10
NO320803B1 (no) 2006-01-30
AU763718B2 (en) 2003-07-31

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