AR076666A1 - Derivados azabiciclicos como inhibidor de hsl (lipasa sensible a las hormonas) - Google Patents

Derivados azabiciclicos como inhibidor de hsl (lipasa sensible a las hormonas)

Info

Publication number
AR076666A1
AR076666A1 ARP100101584A ARP100101584A AR076666A1 AR 076666 A1 AR076666 A1 AR 076666A1 AR P100101584 A ARP100101584 A AR P100101584A AR P100101584 A ARP100101584 A AR P100101584A AR 076666 A1 AR076666 A1 AR 076666A1
Authority
AR
Argentina
Prior art keywords
substituted
alkyl
pyrimidylalkyl
pyrazinyl
cycloalkyl
Prior art date
Application number
ARP100101584A
Other languages
English (en)
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 AR076666A1 publication Critical patent/AR076666A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10—Spiro-condensed systems
    • 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
    • A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
    • 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
    • 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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

Abstract

utiles para tratamiento de diabetes, dislipidemia, aterosclerosis u obesidad. Reivindicacion 1: Compuesto de la formula (1)en la que m es el numero 1 o 2; n es el numero cero, 1 o 2, en el caso de que n sea cero, entonces m es 1; A es -S(O)2- o carbonilo; R1 es alquilo, aminoalquilo, cicloalquilo, cicloalquilalquilo, haloalquilo, haloalquilcicloalquilo, hidroxicicloalquilalquilo, (cicloalquil)(hidroxi)alquilo, (cicloalquil)(alcoxi)alquilo, alcoxicicloalquilalquilo, hidroxicicloalquilo, cicloalcoxialquilo, hidroxialquilo, alcoxialquilo, benciloxialquilo, feniloxialquilo, dihidro-furanilidenometilo, tetrahidro-furanilmetilo, dihidro-isoindolilo, dihidro quinolinilo, -NR4R5, azepanilo, morfolinilo, piperidinilo, pirrolidinilo, pirazolilo, imidazolilo, isoxazolilo, oxazolilo, tiofenilo, tiazolilo, piridinilo, piridinilalquilo, piridazinilo, piridazinilalquilo, pirazinilo, pirazinilalquilo, pirimidilo, pirimidilalquilo, fenilo, fenilalquilo, piperidinilo sustituido, pirrolidinilo sustituido, pirazolilo sustituido, imidazolilo sustituido, isoxazolilo sustituido, oxazolilo sustituido, tiofenilo sustituido, tiazolilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazinilo sustituido, pirazinilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, fenilo sustituido o fenilalquilo sustituido, dichos piperidinilo sustituido, pirrolidinilo sustituido, pirazolilo sustituido, imidazolilo sustituido, isoxazolilo sustituido, oxazolilo sustituido, tiofenilo sustituido, tiazolilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazinilo sustituido, pirazinilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, fenilo sustituido y fenilalquilo sustituido están sustituidos con uno a tres sustituyentes elegidos con independencia entre alquilo, haloalquilo, halogeno, hidroxi, alcoxi, haloalcoxi, feniloxi, alquilfeniloxi, alquilsulfonilo, oxopirrolidinilo, alcoxicarbonilo, benciloxi y -NR6R7; R2 es imidazolilo, imidazolilalquilo, fenilo, fenilalquilo, piridinilo, piridinilalquilo, piridazinilo, piridazinilalquilo, pirazolilo, pirazolilalquilo, alquilindazolilo, alquilbenzotiazolilo, difluorbenzo[1,3}dioxolilo, pirimidilo, pirimidilalquilo, pirazinilo, pirazinilalquilo, imidazolilo sustituido, imidazolilalquilo sustituido, fenilo sustituido, fenilalquilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazolilo sustituido, pirazolilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, pirazinilo sustituido o pirazinilalquilo sustituido, dichos imidazolilo sustituido, imidazolilalquilo sustituido, fenilo sustituido, fenilalquilo sustituido, piridinilo sustituido, piridinilalquilo sustituido, piridazinilo sustituido, piridazinilalquilo sustituido, pirazolilo sustituido, pirazolilalquilo sustituido, pirimidilo sustituido, pirimidilalquilo sustituido, pirazinilo sustituido y pirazinilalquilo sustituido están sustituidos con uno a tres sustituyentes elegidos con independencia entre alquilo, haloalquilo, cicloalquilo, cicloalquilalquilo, halogeno, haloalcoxi, alcoxi, hidroxi, alcoxialquilo, hidroxialquilo, alquilsulfonilo, alquilsulfoniloxi, alquilsulfanilo, cicloalquilsulfoniloxi, cicloalcoxi, alquenilo, cicloalquilalcoxi, alcoxialcoxi, tetrahidrofuraniloxi, piridiniloxi, alcoxicarbonilalquilo, cianoalquilo, alquiloxazodiazolilalquilo, haloalquiloxazodiazolilalquilo, alcoxialquenilo, cicloalquilalquenilo, cicloalquilalcoxialquilo, alcoxicarbonilo, alquilcarbonilo, haloalquilhidroxialquilo, alquilaminocarbonilo, dialquilaminocarbonilo, hidroxioxetanilo, fluoroxetanilo e hidroxicicloalquilo; uno de R4 y R5 es hidrogeno o alquilo y el otro es hidrogeno, alquilo, hidroxialquilo, alcoxialquilo, cicloalquilo, fenilo, alquilfenilo, haloalcoxifenilo, fenilalquilo, halofenilo, halofenilalquilo, haloalquilfenilo o piridinilalquilo; uno de R6 y R7 es hidrogeno, alquilo, cicloalquilo o hidroxialquilo y el otro es hidrogeno, alquilo, cicloalquilo o hidroxialquilo; o sus sales farmacéuticamente aceptables.
ARP100101584A 2009-05-12 2010-05-10 Derivados azabiciclicos como inhibidor de hsl (lipasa sensible a las hormonas) AR076666A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09160026 2009-05-12

Publications (1)

Publication Number Publication Date
AR076666A1 true AR076666A1 (es) 2011-06-29

Family

ID=42269304

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101584A AR076666A1 (es) 2009-05-12 2010-05-10 Derivados azabiciclicos como inhibidor de hsl (lipasa sensible a las hormonas)

Country Status (15)

Country Link
US (1) US8329904B2 (es)
EP (1) EP2430023B1 (es)
JP (1) JP5542916B2 (es)
KR (1) KR101438263B1 (es)
CN (1) CN102421777A (es)
AR (1) AR076666A1 (es)
AU (1) AU2010247472A1 (es)
BR (1) BRPI1015038A2 (es)
CA (1) CA2760340A1 (es)
ES (1) ES2450119T3 (es)
IL (1) IL214352A0 (es)
MX (1) MX2011012017A (es)
SG (1) SG175298A1 (es)
TW (1) TW201043629A (es)
WO (1) WO2010130665A1 (es)

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WO2011009059A2 (en) * 2009-07-17 2011-01-20 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Method of treating or preventing cancer
US8258158B2 (en) * 2009-09-11 2012-09-04 Hoffmann-La Roche Inc. HSL inhibitors useful in the treatment of diabetes
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GB201007789D0 (en) * 2010-05-10 2010-06-23 Glaxo Group Ltd Novel Compound
GB201007791D0 (en) * 2010-05-10 2010-06-23 Glaxo Group Ltd Novel compounds
US8552024B2 (en) * 2010-08-13 2013-10-08 Hoffman-La Roche Inc. Azacyclic compounds
US8722721B2 (en) * 2011-03-16 2014-05-13 Hoffmann-La Roche Inc. SEC-hydroxycyclohexyl derivatives
US8703807B2 (en) * 2011-03-17 2014-04-22 Hoffmann-La Roche Inc. Azaspirodecanone compounds
US8809384B2 (en) * 2011-03-25 2014-08-19 Hoffmann-La Roche Inc. Azaspirodecanone compounds
US8497288B2 (en) * 2011-05-09 2013-07-30 Hoffmann-La Roche Inc. Hexahydropyrroloimidazolone compounds
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CN103408573B (zh) * 2013-07-12 2015-12-23 上海工程技术大学 硼酸衍生物及其制备方法和应用
HUE054960T2 (hu) 2015-03-31 2021-10-28 Enanta Pharm Inc Epesav származékok, mint az FXR/TGR5 agonista és annak felhasználási módszerei
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MX2019001318A (es) 2016-08-01 2019-07-01 Aptinyx Inc Moduladores del receptor nmda espiro-lactam y uso de los mismos.
JP2019527232A (ja) 2016-08-01 2019-09-26 アプティニックス インコーポレイテッド スピロ−ラクタムｎｍｄａ修飾因子及びこれを用いた方法
EP3490992B1 (en) * 2016-08-01 2023-03-22 Aptinyx Inc. Spiro-lactam nmda receptor modulators and uses thereof
KR20190056436A (ko) 2016-10-04 2019-05-24 이난타 파마슈티칼스, 인코포레이티드 Fxr 작용제로서의 이속사졸 유사체 및 그의 사용 방법
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Also Published As

Publication number Publication date
AU2010247472A1 (en) 2011-09-29
CN102421777A (zh) 2012-04-18
CA2760340A1 (en) 2010-11-18
US8329904B2 (en) 2012-12-11
EP2430023A1 (en) 2012-03-21
JP5542916B2 (ja) 2014-07-09
WO2010130665A1 (en) 2010-11-18
EP2430023B1 (en) 2013-12-11
TW201043629A (en) 2010-12-16
ES2450119T3 (es) 2014-03-24
SG175298A1 (en) 2011-11-28
KR101438263B1 (ko) 2014-09-05
KR20120035160A (ko) 2012-04-13
JP2012526154A (ja) 2012-10-25
IL214352A0 (en) 2011-09-27
US20100292212A1 (en) 2010-11-18
MX2011012017A (es) 2011-12-06
BRPI1015038A2 (pt) 2016-04-12

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