ES2490266T3 - Derivados azacíclicos como inhibidores de HSL - Google Patents

Derivados azacíclicos como inhibidores de HSL Download PDF

Info

Publication number
ES2490266T3
ES2490266T3 ES11715201.7T ES11715201T ES2490266T3 ES 2490266 T3 ES2490266 T3 ES 2490266T3 ES 11715201 T ES11715201 T ES 11715201T ES 2490266 T3 ES2490266 T3 ES 2490266T3
Authority
ES
Spain
Prior art keywords
haloalkyl
pyrimidyl
pyridazinyl
pyridinyl
pyrazinyl
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
ES11715201.7T
Other languages
English (en)
Inventor
Jean Ackermann
Aurelia Conte
Daniel Hunziker
Werner Neidhart
Matthias Nettekoven
Tanja Schulz-Gasch
Stanley Wertheimer
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche 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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of ES2490266T3 publication Critical patent/ES2490266T3/es
Active legal-status Critical Current
Anticipated expiration legal-status Critical

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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Child & Adolescent Psychology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Compuestos de la fórmula (I)**Fórmula** en la que: R1 es alquilo, cicloalquilo, haloalquilo, piperidinilo, piperazinilo, morfolinilo, imidazolilo, pirazolilo, triazolilo, tetrazolilo, oxazolilo, isoxazolilo, tiazolilo, fenilo, piridinilo, pirazinilo, pirimidilo o piridazinilo o en la que piperidinilo, piperazinilo, morfolinilo, imidazolilo, pirazolilo, triazolilo, tetrazolilo, oxazolilo, isoxazolilo, tiazolilo, fenilo, piridinilo, pirazinilo, pirimidilo y piridazinilo están sustituidos de una a tres veces por sustituyentes elegidos con independencia entre alquilo, cicloalquilo, cicloalquilalquilo, halógeno, haloalquilo, hidroxi, hidroxialquilo, alcoxi, alcoxialquilo, haloalcoxi e hidroxi-haloalquilo; R2 es fenilo, piridinilo, pirazinilo, pirimidilo o piridazinilo o en la que fenilo, piridinilo, pirazinilo, pirimidilo y piridazinilo están sustituidos de una a tres veces por sustituyentes elegidos con independencia entre alquilo, cicloalquilo, cicloalquilalquilo, halógeno, haloalquilo, hidroxi, hidroxialquilo, alcoxi, alcoxialquilo, haloalcoxi e hidroxi-haloalquilo; A es -(CH2)n-, -C(O)- o -S(O)2-; n es el número cero, 1 ó 2; o sus sales farmacéuticamente aceptables.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
imagen6
imagen7
imagen8
imagen9
imagen10
imagen11
imagen12
imagen13
imagen14
imagen15

Claims (1)

  1. imagen1
    imagen2
ES11715201.7T 2010-04-15 2011-04-12 Derivados azacíclicos como inhibidores de HSL Active ES2490266T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP10160030 2010-04-15
EP10160030 2010-04-15
PCT/EP2011/055670 WO2011128316A1 (en) 2010-04-15 2011-04-12 Azacyclic spiroderivatives as hsl inhibitors

Publications (1)

Publication Number Publication Date
ES2490266T3 true ES2490266T3 (es) 2014-09-03

Family

ID=44010146

Family Applications (1)

Application Number Title Priority Date Filing Date
ES11715201.7T Active ES2490266T3 (es) 2010-04-15 2011-04-12 Derivados azacíclicos como inhibidores de HSL

Country Status (14)

Country Link
US (1) US8097634B2 (es)
EP (1) EP2558464B1 (es)
JP (1) JP5956423B2 (es)
KR (1) KR20130098153A (es)
CN (1) CN102844316B (es)
AR (1) AR080894A1 (es)
BR (1) BR112012026147A2 (es)
CA (1) CA2795101A1 (es)
ES (1) ES2490266T3 (es)
HK (1) HK1176607A1 (es)
MX (1) MX2012010826A (es)
RU (1) RU2567395C2 (es)
TW (1) TW201202237A (es)
WO (1) WO2011128316A1 (es)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8389539B2 (en) * 2009-12-01 2013-03-05 Hoffman-La Roche Inc. Azacyclic derivatives
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
WO2013134562A1 (en) 2012-03-09 2013-09-12 Inception 2, Inc. Triazolone compounds and uses thereof
BR112015013350B1 (pt) 2012-12-20 2022-04-05 Tempest Therapeutics, Inc Composto ou sal farmaceuticamente aceitável do mesmo, composição farmacêutica e respectivos usos
PE20160880A1 (es) 2013-09-06 2016-09-22 Inception 2 Inc Compuestos de triazolona y usos de los mismos
KR102503590B1 (ko) 2016-08-01 2023-02-24 앱티닉스 인크. 스피로-락탐 nmda 수용체 조정제 및 그의 용도
US11028095B2 (en) 2016-08-01 2021-06-08 Aptinyx Inc. Spiro-lactam and bis-spiro-lactam NMDA receptor modulators and uses thereof
JP2019527233A (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受容体修飾因子及びその使用
PE20190501A1 (es) 2016-08-01 2019-04-10 Aptinyx Inc Moduladores nmda espiro-lactam y metodos de uso de los mismos
EA201990428A1 (ru) 2016-08-01 2019-08-30 Аптиникс Инк. Спиролактамовые модуляторы nmda-рецептора и их применение
KR20200115611A (ko) 2018-01-31 2020-10-07 앱티닉스 인크. 스피로-락탐 nmda 수용체 조정제 및 그의 용도

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR100974901B1 (ko) * 2001-12-28 2010-08-10 아카디아 파마슈티칼스 인코포레이티드 모노아민 수용체 조정자로서의 스피로아자사이클릭 화합물
DE10247680B4 (de) * 2002-10-12 2005-09-01 Aventis Pharma Deutschland Gmbh Neue bicyclische Inhibitoren der Hormon Sensitiven Lipase
CN101115741A (zh) * 2005-02-15 2008-01-30 诺和诺德公司 3,4-二氢-1h-异喹啉-2-羧酸5-氨基吡啶-2-基酯
BRPI0607545A2 (pt) 2005-02-15 2016-11-01 Novo Nordisk As composto, uso de um composto de fórmula i ou um sal farmaceuticamente aceitável do mesmo, e, composição farmacêutica
JP5475288B2 (ja) 2005-12-05 2014-04-16 インサイト・コーポレイション ラクタム化合物およびそれを用いる方法
CN101336243A (zh) * 2005-12-05 2008-12-31 因塞特公司 内酰胺化合物和其使用方法
US8329904B2 (en) * 2009-05-12 2012-12-11 Hoffmann-La Roche Inc. Azacyclic derivatives
US8440710B2 (en) * 2009-10-15 2013-05-14 Hoffmann-La Roche Inc. HSL inhibitors useful in the treatment of diabetes
US8389539B2 (en) * 2009-12-01 2013-03-05 Hoffman-La Roche Inc. Azacyclic derivatives
RU2603263C2 (ru) * 2010-07-13 2016-11-27 Ф. Хоффманн-Ля Рош Аг Новые азациклические соединения
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

Also Published As

Publication number Publication date
US8097634B2 (en) 2012-01-17
WO2011128316A1 (en) 2011-10-20
BR112012026147A2 (pt) 2016-06-28
KR20130098153A (ko) 2013-09-04
US20110257212A1 (en) 2011-10-20
RU2012146875A (ru) 2014-05-20
EP2558464A1 (en) 2013-02-20
HK1176607A1 (en) 2013-08-02
JP5956423B2 (ja) 2016-07-27
AR080894A1 (es) 2012-05-16
MX2012010826A (es) 2012-10-10
EP2558464B1 (en) 2014-06-18
CN102844316B (zh) 2015-02-25
JP2013523859A (ja) 2013-06-17
CN102844316A (zh) 2012-12-26
RU2567395C2 (ru) 2015-11-10
CA2795101A1 (en) 2011-10-20
TW201202237A (en) 2012-01-16

Similar Documents

Publication Publication Date Title
ES2490266T3 (es) Derivados azacíclicos como inhibidores de HSL
DOP2017000081A (es) NUEVOS COMPUESTOS ANTAGONISTAS DE INTEGRINA aVß6
DK2300459T3 (da) Nye fenylpyrazinoner som kinasehæmmere
CY1118212T1 (el) Παραγοντες οι οποιοι τροποποιουν την s1p
ES2524966T3 (es) Derivados de tieno[3,2-c]piridina como inhibidores de quinasas para uso en el tratamiento del cáncer
ZA201203771B (en) 4-[2-[5-methyl-1-(2-naphtalenyl)-1h-pyrazol-3-yl)oxy)ethyl)morpholine salts
PH12015502232A1 (en) Naphthyridine derivatives useful as alpha-v-beta-6 integrin antagonists
UA111725C2 (uk) Кристалічний (r)-(e)-2-(4-(2-(5-(1-(3,5-дихлорпіридин-4-іл)етоксі)-1h-індазол-3-іл)вініл)-1h-піразол-1-іл)етанол
UY33883A (es) Novedosos derivados heterocíclicos
AR084001A1 (es) Monobactamas y su uso en el tratamiento de infecciones bacterianas
MX371353B (es) Compuestos heterociclicos aromaticos como compuestos antiinflamatorios.
PL3290414T3 (pl) Sposób otrzymywania n-[5-(3,5-difluorobenzylo)-1h-indazol-3-ilo]-4-(4-metylopiperazyn-1-ylo)-2-(tetrahydropiran-4-yloamino)benzamidu
CR11757A (es) Compuestos de triazina como inhibidores mtor y quinasa pi3
IL231025A (en) 1-pyrazolyl-3 - (4 - ((2-anilinopyrimidine-4-yl) oxy) methylated-1-yl) Oriase for use as kinase inhibitors map 38p
AR078166A1 (es) (heteroarilmetil) tiohidantoinas sustituidas
CR20120130A (es) Compuestos de benzoxepina inhibidores de la pi3k y métodos de uso
AR094978A1 (es) Derivados de pirazol agonistas de receptores canabinoides
DK2751973T3 (da) Fremgangsmåde til styring af tilgangen af en brugers personlige data
CR9432A (es) Derivado de bencimidazol y uso como antagonista de angiotensina ii
HK1205457A1 (en) N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridin yl)oxy)phenyl)-4-(4- methyl-2-thienyl)-1-phthalazinamine for use in the treatment of antimitotic agent resistant cancer n-4(-((3-(2--4-)-2-)))-4- (4--2-)- 1-
AR076692A1 (es) Piperidinas sustituidas
AR082631A1 (es) Derivados de 2,8-diaza-espiro[4,5]decan-1-ona, composiciones farmaceuticas que los contienen, proceso para prepararlos y uso de los mismos para tratar diabetes, obesidad, dislipemia y sindrome metabolico
AR092772A1 (es) Derivado de 7-azaindol
AR082151A1 (es) Compuestos azaciclicos
AR085909A1 (es) Derivados de azaespirodecanona, composiciones farmaceuticas que los contienen, procedimiento para prepararlos y uso de los mismos para el tratamiento de diabetes, obesidad y enfermedades cardiovasculares, entre otras