AR075534A1 - Derivados de piridazinona sustituida por heteroarilo - Google Patents

Derivados de piridazinona sustituida por heteroarilo

Info

Publication number
AR075534A1
AR075534A1 ARP100100503A ARP100100503A AR075534A1 AR 075534 A1 AR075534 A1 AR 075534A1 AR P100100503 A ARP100100503 A AR P100100503A AR P100100503 A ARP100100503 A AR P100100503A AR 075534 A1 AR075534 A1 AR 075534A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
alkyl
alkylene
alkoxy
fluor
Prior art date
Application number
ARP100100503A
Other languages
English (en)
Inventor
Daniela Alberati
Matthias Koerner
Sarmiento Rosa Maria Rodriguez
Mark Rogers-Evans
Markus Rudolph
Jens-Uwe Peters
Bernd Kuhn
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 AR075534A1 publication Critical patent/AR075534A1/es

Links

Classifications

    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Diabetes (AREA)
  • Psychology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Composicion farmacéutica, proceso de preparacion, y usos como inhibidores de PDE10A, como medicamentos. Reivindicacion 1: Compuestos de la formula (1) en la que R1 es heteroarilo que puede estar opcionalmente sustituido de 1 a 4 veces por sustituyentes elegidos con independencia entre el grupo formado por alquilo inferior, alcoxi inferior, fluor-alquilo inferior, fluor-alcoxi inferior, (alquilo inferior)-SO2, fluor-(alquilo inferior)-SO2, halogeno, (alcoxi inferior)-alquilo inferior, ciano, NO2, morfolinilo, NH2-SO2, N(H,alquilo inferior)-SO2, N(alquilo inferior)2-SO2, pirrolidinil-SO2, piperidinil-SO2, morfolinil-So2, hidroxi, COOH, COO-alquilo inferior, (alquilo inferior)-C(O)O, CO-alquilo inferior, CONH2, CON(H,alquilo inferior), CON(alquilo inferior)2, (alquilo inferior)-CO-NH, (alquilo inferior)-CO-N(alquilo inferior), NH2-CO-alquilo inferior, NH(alquilo inferior)-CO-alquilo inferior, N(alquilo inferior)2-CO-alquilo inferior, NH2, N(H,alquilo inferior), N(alquilo inferior)2, NH2-alquilo inferior, N(H,alquilo inferior)-alquilo inferior, N(alquilo inferior)2-alquilo inferior, cicloalquilo, piperidinilo, piperazinilo y (N-alquilo inferior)-piperazinilo; R2 es arilo o heteroarilo, dichos arilo o heteroarilo pueden estar opcionalmente sustituidos de 1 a 4 veces por sustituyente elegidos con independencia entre el grupo formado por halogeno, ciano, alquilo inferior, alcoxi inferior, fluor-alquilo inferior, alquinilo inferior, (alquilo inferior)-SO2, COOH, CONH2, NH2-SO2, COO-alquilo inferior, (alcoxi inferior)-alquilo inferior, CON-(H, alquilo inferior), CON(alquilo inferior)2, N(H,alquilo inferior)-SO2, N(alquilo inferior)2-SO2, alquenilo inferior, hidroxi, NO2, morfolinilo, piperidinilo, piperazinilo, (N-alquilo inferior)-piperazinilo, pirrolidinilo, (alquilo inferior)-C(O)O, (alquilo inferior)-CO-NH, (alquilo inferior)-CO-N (alquilo inferior), NH2-CO-alquilo inferior, NH(alquilo inferior)-CO-alquilo inferior, N-(alquilo inferior)2-CO-alquilo inferior, CO-alquilo inferior, NH2, N(H,alquilo inferior), N(alquilo inferior) 2, NH2-alquilo inferior, N(H,alquilo inferior)-alquilo inferior, N(alquilo inferior)2-alquilo inferior, tri(alquilo inferior)silil-alquinilo inferior y cicloalquilo, o en la que dos sustituyentes de posiciones adyacentes del arilo o heteroarilo están unidos entre sí para formar un anillo y dichos dos sustituyentes unidos son alquileno inferior, dioxo-alquileno inferior, dioxo-fluor-alquileno inferior, NH-alquileno inferior, N(alquilo inferior)-alquileno inferior, alquileno inferior-NH-alquileno inferior, alquileno inferior-N-(alquilo inferior)-alquileno inferior, NH-C(O)-alquileno inferior, N(alquilo inferior)-C(O)-alquileno inferior, alquileno inferior-NH-C(O)-alquileno inferior, alquileno inferior-N-(alquilo inferior)-C(O)-alquileno inferior, C(O)-NH-alquileno inferior o C(O)-N(alquilo inferior)-alquileno inferior; R3 es hidrogeno, alquilo inferior, fluor-alquilo inferior, alcoxi inferior, fluor-alcoxi inferior, halogeno, hidroxi o fenilo; R4 es hidrogeno, alquilo inferior, fluor-alquilo inferior, alcoxi inferior, fluor-alcoxi inferior, halogeno, hidroxi o fenilo; y sus sales y ésteres farmacéuticamente aceptables.
ARP100100503A 2009-02-23 2010-02-22 Derivados de piridazinona sustituida por heteroarilo AR075534A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09153391 2009-02-23

Publications (1)

Publication Number Publication Date
AR075534A1 true AR075534A1 (es) 2011-04-06

Family

ID=42312870

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100503A AR075534A1 (es) 2009-02-23 2010-02-22 Derivados de piridazinona sustituida por heteroarilo

Country Status (15)

Country Link
US (1) US9187455B2 (es)
EP (1) EP2398795B1 (es)
JP (1) JP5518902B2 (es)
KR (1) KR101363091B1 (es)
CN (1) CN102325766B (es)
AR (1) AR075534A1 (es)
AU (1) AU2010215428B2 (es)
BR (1) BRPI1008007A2 (es)
CA (1) CA2749867C (es)
ES (1) ES2526251T3 (es)
IL (1) IL213983A (es)
MX (1) MX2011008360A (es)
SG (1) SG173671A1 (es)
TW (1) TW201033193A (es)
WO (1) WO2010094762A1 (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2393360T1 (sl) * 2009-02-05 2016-02-29 Takeda Pharmaceutical Company Limited Piridazinonske spojine
JP5800814B2 (ja) 2010-08-10 2015-10-28 武田薬品工業株式会社 複素環化合物およびその用途
BR112013021180A2 (pt) 2011-02-18 2019-09-24 Allergan Inc derivados de 6,7-dialcóxi-3-isoquinolinol substituído como inibidores de fosfodiesterase 10 (pde10a)
WO2014071044A1 (en) 2012-11-01 2014-05-08 Allergan, Inc. Substituted 6,7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (pde10a)
MX2015010940A (es) 2013-02-21 2015-10-29 Takeda Pharmaceutical Metodo de produccion de compuestos de piridazinona.
SG11201602387RA (en) * 2013-10-21 2016-05-30 Merck Patent Gmbh Heteroaryl compounds as btk inhibitors and uses thereof
US9200016B2 (en) 2013-12-05 2015-12-01 Allergan, Inc. Substituted 6, 7-dialkoxy-3-isoquinoline derivatives as inhibitors of phosphodiesterase 10 (PDE 10A)
CN103772352B (zh) * 2014-01-16 2017-01-18 四川百利药业有限责任公司 哒嗪酮类衍生物及其制备方法和用途
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
KR20230090078A (ko) 2021-12-14 2023-06-21 안희철 무선태그 장치

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL379544A1 (pl) * 2002-09-09 2006-10-02 Amgen Inc. 1,4,5-podstawione pochodne 1,2-dihydro-pirazol-3-onu i 3-alkoksy 1H-pirazolu jako środki obniżające poziom TNF-alfa oraz interleukin do leczenia stanów zapalnych
US7294625B2 (en) 2002-09-25 2007-11-13 Ube Industries, Ltd. Pyrazole compounds
CA2534432A1 (en) 2003-07-31 2005-02-10 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors
CA2650976A1 (en) 2006-05-02 2007-11-15 Pfizer Products Inc. Bicyclic heteroaryl compounds as pde10 inhibitors
US8716308B2 (en) * 2008-01-11 2014-05-06 Albany Molecular Research, Inc. (1-azinone)-substituted pyridoindoles
CN102239162B (zh) * 2008-12-04 2014-05-28 弗·哈夫曼-拉罗切有限公司 哒嗪酮衍生物

Also Published As

Publication number Publication date
US9187455B2 (en) 2015-11-17
WO2010094762A1 (en) 2010-08-26
JP2012518619A (ja) 2012-08-16
CA2749867A1 (en) 2010-08-26
US20100216793A1 (en) 2010-08-26
SG173671A1 (en) 2011-09-29
ES2526251T3 (es) 2015-01-08
CN102325766B (zh) 2015-03-18
KR20110111495A (ko) 2011-10-11
CA2749867C (en) 2017-06-06
AU2010215428A1 (en) 2011-08-11
JP5518902B2 (ja) 2014-06-11
IL213983A (en) 2016-07-31
EP2398795B1 (en) 2014-10-15
CN102325766A (zh) 2012-01-18
BRPI1008007A2 (pt) 2016-03-15
IL213983A0 (en) 2011-08-31
MX2011008360A (es) 2011-08-24
AU2010215428B2 (en) 2016-06-23
EP2398795A1 (en) 2011-12-28
KR101363091B1 (ko) 2014-02-13
TW201033193A (en) 2010-09-16

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