PE20120229A1 - Compuestos heterociclicos como inhibidores de proteasa aspartica - Google Patents

Compuestos heterociclicos como inhibidores de proteasa aspartica

Info

Publication number
PE20120229A1
PE20120229A1 PE2010000496A PE2010000496A PE20120229A1 PE 20120229 A1 PE20120229 A1 PE 20120229A1 PE 2010000496 A PE2010000496 A PE 2010000496A PE 2010000496 A PE2010000496 A PE 2010000496A PE 20120229 A1 PE20120229 A1 PE 20120229A1
Authority
PE
Peru
Prior art keywords
alkyl
inhibitors
heterocyclic compounds
ilcarbamoyl
propan
Prior art date
Application number
PE2010000496A
Other languages
English (en)
Inventor
John J Baldwin
David A Claremon
Colin Tice
Salvation Cacatian
Lawrence W Dillard
Alexey V Ishchenko
Jing Yuan
Zhenrong Xu
Gerard Mcgeehan
Wei Zhao
Robert D Simpson
Suresh B Singh
Patrick T Flaherty
Original Assignee
Vitae Pharmaceuticals 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 Vitae Pharmaceuticals Inc filed Critical Vitae Pharmaceuticals Inc
Publication of PE20120229A1 publication Critical patent/PE20120229A1/es

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Classifications

    • 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
    • C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/26—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by nitrogen 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
    • A61K31/435—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
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • 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
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • 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
    • A61P9/10—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
    • C07D211/08—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms
    • C07D211/18—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D211/20—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms
    • C07D211/22—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 hydrocarbon or substituted hydrocarbon radicals directly attached to ring carbon atoms with substituted hydrocarbon radicals attached to ring carbon atoms with hydrocarbon radicals, substituted by singly bound oxygen or sulphur atoms by oxygen atoms
    • 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
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 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
    • C07D409/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE Z ES O, -CH2-; X1 ES ENLACE COVALENTE, -O-, -S-, -S(O)-, -S(O)2-; Y1 ES EN LACE COVALENTE, ALQUILENO C1-C10, ALQUENILENO C2-C10 SUSTITUIDO O NO, ENTRE OTROS; R1 ES CICLOALQUILO C3-C7, FENILO, HETEROARILO SUSTITUIDO O NO, ENTRE OTROS; R2 ES -OCO(NH2), -OCS(NH2), -SC(S)(NH2), ENTRE OTROS; R3 ES H, -F, ALQUILO C1-C5, -OH, ENTRE OTROS; R4 ES -H, ALQUILO C1-C3; R5 Y R6 SON CADA UNO H, ALQUILO C1-C10, CICLOALQUILO C4-C10, HALOALQUILO C1-C10, ENTRE OTROS; G ES OH, NH2, NH(ALQUILO C1-C6), ENTRE OTROS; Q ES -C0-, -CS-, -C=CNO2-, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 4-(1-(1-CICLOHEXIL-3-(METILAMINO)PROPAN-2-ILCARBAMOIL)PIPERIDIN-3-IL)-4-(2-FLUOROFENIL)-4-HIDROXIBUTILCARBAMATO DE METILO; 4-ACETAMIDO-4-(3-CLOROFENIL)-4-(1-(1-CICLOHEXIL-3-(METILAMINO)PROPAN-2-ILCARBAMOIL)PIPERIDIN-3-IL)BUTILCABAMATO DE METILO; ENTRE OTROS. DICHOS COMPUESTOS SON INHIBIDORES DE LA PROTEASA ASPARTICA UTILES EN EL TRATAMIENTO DE HIPERTENSION
PE2010000496A 2005-11-14 2010-08-06 Compuestos heterociclicos como inhibidores de proteasa aspartica PE20120229A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US73656405P 2005-11-14 2005-11-14
US84529106P 2006-09-18 2006-09-18
US84533106P 2006-09-18 2006-09-18

Publications (1)

Publication Number Publication Date
PE20120229A1 true PE20120229A1 (es) 2012-04-04

Family

ID=37812974

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2006001432A PE20070804A1 (es) 2005-11-14 2006-11-13 Compuestos heterociclicos como inhibidores de proteasa aspartica
PE2010000496A PE20120229A1 (es) 2005-11-14 2010-08-06 Compuestos heterociclicos como inhibidores de proteasa aspartica

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2006001432A PE20070804A1 (es) 2005-11-14 2006-11-13 Compuestos heterociclicos como inhibidores de proteasa aspartica

Country Status (16)

Country Link
US (1) US8487108B2 (es)
EP (1) EP1966139B1 (es)
JP (1) JP2009515893A (es)
KR (1) KR101379663B1 (es)
AR (1) AR057890A1 (es)
AT (1) ATE538092T1 (es)
AU (1) AU2006325322B2 (es)
BR (1) BRPI0618585A2 (es)
CA (1) CA2628952C (es)
HK (1) HK1121459A1 (es)
NO (1) NO20082108L (es)
NZ (1) NZ568042A (es)
PE (2) PE20070804A1 (es)
SG (1) SG169983A1 (es)
TW (1) TWI411607B (es)
WO (1) WO2007070201A1 (es)

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Publication number Publication date
TWI411607B (zh) 2013-10-11
JP2009515893A (ja) 2009-04-16
KR101379663B1 (ko) 2014-04-14
TW200800893A (en) 2008-01-01
AR057890A1 (es) 2007-12-26
WO2007070201A1 (en) 2007-06-21
EP1966139A1 (en) 2008-09-10
AU2006325322A1 (en) 2007-06-21
BRPI0618585A2 (pt) 2011-09-27
CA2628952C (en) 2014-04-01
US8487108B2 (en) 2013-07-16
NO20082108L (no) 2008-08-06
CA2628952A1 (en) 2007-06-21
NZ568042A (en) 2010-12-24
AU2006325322B2 (en) 2011-08-04
HK1121459A1 (en) 2009-04-24
KR20080069685A (ko) 2008-07-28
PE20070804A1 (es) 2007-09-06
ATE538092T1 (de) 2012-01-15
EP1966139B1 (en) 2011-12-21
SG169983A1 (en) 2011-04-29
US20100048636A1 (en) 2010-02-25

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