AR082968A1 - Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto - Google Patents

Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto

Info

Publication number
AR082968A1
AR082968A1 ARP110103323A ARP110103323A AR082968A1 AR 082968 A1 AR082968 A1 AR 082968A1 AR P110103323 A ARP110103323 A AR P110103323A AR P110103323 A ARP110103323 A AR P110103323A AR 082968 A1 AR082968 A1 AR 082968A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
heterocycle
aryl
heteroalkyl
hydrogen
Prior art date
Application number
ARP110103323A
Other languages
English (en)
Inventor
Victoria Lombardo
Praveen Pabba
Wei He
Joseph Barbosa
Kenneth Gordon Carson
Michael Walter Gardyan
James Tarver Jr
Original Assignee
Lexicon 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 Lexicon Pharmaceuticals Inc filed Critical Lexicon Pharmaceuticals Inc
Publication of AR082968A1 publication Critical patent/AR082968A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Se describen compuestos que se pueden utilizar para inhibir la Notum pectinacetilesterasa, como también composiciones que los comprenden. Estos compuestos son útiles para tratar las enfermedades y los trastornos que afectan a los huesos, en particular la osteoporosis.Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: R1B es hidrógeno o alquilo, arilo, heteroalquilo o heterociclo opcionalmente sustituidos; R2 es hidrógeno, halo, -CO2R2A, -C(O)N(R2A)2, -SR2A, -OR2A o -N(R2A)2, alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; cada R2A es, de manera independiente, hidrógeno o alquilo, arilo, heteroalquilo, o heterociclo, opcionalmente sustituidos; R3 es hidrógeno, halo, ciano, -CO2R3A, -C(O)N(R3A)2, -SR3A, -OR3A, -N(R3A)2, o alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; cada R3A es, de manera independiente, hidrógeno, alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; R4 es hidrógeno, halo o alquilo, arilo, heteroalquilo o heterociclo, opcionalmente sustituidos; R5 es hidrógeno, halo, -CO2R5A, -C(O)N(R5A)2, -SR5A, -OR5A, -N(R5A)2 o arilo, heteroalquilo, o heterociclo, opcionalmente sustituidos; cada R5A es, de manera independiente, hidrógeno, alquilo, arilo, heteroalquilo, o heterociclo, opcionalmente sustituidos; y n es 0, 1 ó 2; en donde “opcionalmente sustituido” significa opcionalmente sustituido con uno o más de alcoxi, alquilo, amino (incluyendo alquilamino, dialquilamino), arilo, ácido carboxílico, ciano, halo, heterociclo o hidroxilo.
ARP110103323A 2010-09-14 2011-09-13 Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto AR082968A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US38252610P 2010-09-14 2010-09-14

Publications (1)

Publication Number Publication Date
AR082968A1 true AR082968A1 (es) 2013-01-23

Family

ID=44678054

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110103323A AR082968A1 (es) 2010-09-14 2011-09-13 Inhibidores biciclicos de notum pectinacetilesterasa y una composicion farmaceutica en base al compuesto

Country Status (22)

Country Link
US (2) US20120065200A1 (es)
EP (1) EP2616471B1 (es)
JP (1) JP2013537202A (es)
KR (1) KR20130112888A (es)
CN (1) CN103328481A (es)
AR (1) AR082968A1 (es)
AU (1) AU2011302225A1 (es)
BR (1) BR112013006131A2 (es)
CA (1) CA2811005A1 (es)
CL (1) CL2013000682A1 (es)
CO (1) CO6710916A2 (es)
DK (1) DK2616471T3 (es)
ES (1) ES2536078T3 (es)
MX (1) MX2013002851A (es)
NZ (1) NZ608031A (es)
PL (1) PL2616471T3 (es)
PT (1) PT2616471E (es)
RU (1) RU2013116801A (es)
SG (1) SG188530A1 (es)
TW (1) TW201219401A (es)
WO (1) WO2012037141A1 (es)
ZA (1) ZA201301795B (es)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2808432C (en) 2010-07-23 2019-06-04 President And Fellows Of Harvard College Tricyclic proteasome activity enhancing compounds with thieno[2,3-d]pyrimidine core
AR090037A1 (es) * 2011-11-15 2014-10-15 Xention Ltd Derivados de tieno y/o furo-pirimidinas y piridinas inhibidores de los canales de potasio
WO2013112706A1 (en) 2012-01-25 2013-08-01 Proteostasis Therapeutics, Inc. Proteasome activity modulating compounds
CN110337437B (zh) 2016-12-28 2023-02-03 达特神经科学有限公司 作为pde2抑制剂的取代的吡唑并嘧啶酮化合物
AU2018373258B2 (en) 2017-11-27 2023-03-02 Dart Neuroscience, Llc Substituted furanopyrimidine compounds as PDE1 inhibitors
GB201814151D0 (en) 2018-08-31 2018-10-17 Ucl Business Plc Compounds
CN111171044B (zh) * 2018-11-13 2022-06-24 沈阳化工研究院有限公司 一种噻吩并嘧啶类化合物及其医药用途
WO2020132384A1 (en) 2018-12-21 2020-06-25 Celgene Corporation Thienopyridine inhibitors of ripk2
PE20220281A1 (es) 2019-03-19 2022-02-25 Boehringer Ingelheim Animal Health Usa Inc Compuestos de aza-benzotiofeno y aza-benzofurano como antihelminticos
JP2023528822A (ja) 2020-05-29 2023-07-06 ベーリンガー インゲルハイム アニマル ヘルス ユーエスエイ インコーポレイテッド 駆虫性複素環式化合物
WO2022251343A2 (en) * 2021-05-27 2022-12-01 National Health Research Institutes Cdgsh iron sulfur domain 2 activators and use thereof
WO2023073641A1 (en) 2021-11-01 2023-05-04 Boehringer Ingelheim Vetmedica Gmbh Anthelmintic pyrrolopyridazine compounds

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4008726A1 (de) 1990-03-19 1991-09-26 Basf Ag Thieno(2,3-d)pyrimidinderivate
US6080576A (en) 1998-03-27 2000-06-27 Lexicon Genetics Incorporated Vectors for gene trapping and gene activation
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
WO2007146284A2 (en) * 2006-06-12 2007-12-21 Vertex Pharmaceuticals Incorporated Thienopyrimidines useful as modulators of ion channels
WO2009001214A2 (en) * 2007-06-28 2008-12-31 Pfizer Products Inc. Thieno[2,3-d]pyrimidin-4(3h)-one, isoxazolo[5,4-d]pyrimidin-4(5h)-one and isothiazolo[5,4-d]pyrimidin-4(5h)-one derivatives as calcium receptor antagonists

Also Published As

Publication number Publication date
CO6710916A2 (es) 2013-07-15
PL2616471T3 (pl) 2015-07-31
JP2013537202A (ja) 2013-09-30
PT2616471E (pt) 2015-04-20
WO2012037141A1 (en) 2012-03-22
CA2811005A1 (en) 2012-03-22
BR112013006131A2 (pt) 2016-06-07
CL2013000682A1 (es) 2013-11-08
ZA201301795B (en) 2014-05-28
EP2616471A1 (en) 2013-07-24
CN103328481A (zh) 2013-09-25
NZ608031A (en) 2015-01-30
US20120065200A1 (en) 2012-03-15
SG188530A1 (en) 2013-04-30
TW201219401A (en) 2012-05-16
AU2011302225A1 (en) 2013-03-21
DK2616471T3 (en) 2015-04-07
MX2013002851A (es) 2013-05-28
ES2536078T3 (es) 2015-05-20
EP2616471B1 (en) 2014-12-31
KR20130112888A (ko) 2013-10-14
RU2013116801A (ru) 2014-10-20
US20140288071A1 (en) 2014-09-25

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