AR084152A1 - Compuestos de triazolopirimidina como inhibidores de pde10a, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades del snc - Google Patents

Compuestos de triazolopirimidina como inhibidores de pde10a, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades del snc

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Publication number
AR084152A1
AR084152A1 ARP110104533A ARP110104533A AR084152A1 AR 084152 A1 AR084152 A1 AR 084152A1 AR P110104533 A ARP110104533 A AR P110104533A AR P110104533 A ARP110104533 A AR P110104533A AR 084152 A1 AR084152 A1 AR 084152A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
lower alkyl
haloalkyl
heterocyclyl
Prior art date
Application number
ARP110104533A
Other languages
English (en)
Inventor
Alexander Flohr
Luca Gobbi
Matthias Koerner
Jens Peters
Zbinden Katrin Uwe-Groebke
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 AR084152A1 publication Critical patent/AR084152A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16Anti-Parkinson drugs
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Abstract

Estos compuestos inhiben la PDE10A y pueden utilizarse como medicamentos para el tratamiento de enfermedades mentales y proliferativas.Reivindicación 1: Un compuesto de la fórmula (1) en la que: R1 es halógeno, alquilo inferior, haloalquilo inferior, hidroxialquilo inferior, alcoxi inferior, (alcoxi inferior)-alquilo inferior, -C(O)-NR9R10, arilo, heteroarilo o NR7R8, dichos arilo y heteroarilo pueden estar sustituidos por 1 - 3 sustituyentes elegidos con independencia entre el grupo formado por hidroxilo, halógeno, alquilo inferior, alcoxi inferior, (alcoxi inferior)-alquilo inferior, haloalquilo inferior y haloalcoxi inferior; R2 es hidrógeno, halógeno, alquilo inferior, haloalquilo inferior, hidroxialquilo inferior, alcoxi inferior o (alcoxi inferior)-alquilo inferior; R3 es hidrógeno, alquilo inferior, haloalquilo inferior, hidroxialquilo inferior, alcoxi inferior o (alcoxi inferior)-alquilo inferior; R4 es hidroxilo, alcoxi inferior o NR5R6; R5 y R6 son con independencia hidrógeno, alquilo inferior, haloalquilo inferior, hidroxialquilo inferior, (alcoxi inferior)-alquilo inferior, cicloalquilo o heterociclilo, o R5 y/o R6 son alquilo inferior sustituido por un sustituyente elegido entre el grupo formado por heteroarilo, (alquilo inferior)-heteroarilo y alcoxi inferior-C(O)- o R5 y R6, junto con el átomo de nitrógeno al que están unidos, forman un heterociclilo, biciclo-heterociclilo o espiro-heterociclilo, dicho heterociclilo puede estar sustituido por 1 - 3 sustituyentes elegidos con independencia entre el grupo formado por hidroxilo, halógeno, alquilo inferior, alcoxi inferior, (alcoxi inferior)-alquilo inferior, haloalquilo inferior y oxo; R7 y R8 son con independencia hidrógeno, alquilo inferior, haloalquilo inferior, hidroxialquilo inferior, (alcoxi inferior)-alquilo inferior o cicloalquilo o R7 y R8, junto con el átomo de nitrógeno al que están unidos, forman un heterociclilo opcionalmente sustituido por un sustituyente elegido entre el grupo formado por hidroxilo, halógeno y oxo; y R9 y R10 son con independencia hidrógeno, alquilo inferior, haloalquilo inferior, hidroxialquilo inferior o (alcoxi inferior)-alquilo inferior; o una sal farmacéuticamente aceptable del mismo.
ARP110104533A 2010-12-07 2011-12-05 Compuestos de triazolopirimidina como inhibidores de pde10a, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades del snc AR084152A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10194014 2010-12-07

Publications (1)

Publication Number Publication Date
AR084152A1 true AR084152A1 (es) 2013-04-24

Family

ID=45099086

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110104533A AR084152A1 (es) 2010-12-07 2011-12-05 Compuestos de triazolopirimidina como inhibidores de pde10a, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades del snc

Country Status (30)

Country Link
US (1) US8349824B2 (es)
EP (1) EP2649070B1 (es)
JP (1) JP5932828B2 (es)
KR (1) KR20130128426A (es)
CN (1) CN103237803B (es)
AR (1) AR084152A1 (es)
AU (1) AU2011340685A1 (es)
BR (1) BR112013013912A2 (es)
CA (1) CA2816829C (es)
CL (1) CL2013001591A1 (es)
CO (1) CO6741154A2 (es)
CR (1) CR20130239A (es)
CY (1) CY1115863T1 (es)
DK (1) DK2649070T3 (es)
EA (1) EA022607B1 (es)
EC (1) ECSP13012667A (es)
ES (1) ES2520647T3 (es)
HR (1) HRP20141200T1 (es)
IL (1) IL225969A0 (es)
MA (1) MA35086B1 (es)
MX (1) MX2013006054A (es)
PE (1) PE20140226A1 (es)
PL (1) PL2649070T3 (es)
PT (1) PT2649070E (es)
RS (1) RS53677B1 (es)
SG (1) SG190305A1 (es)
SI (1) SI2649070T1 (es)
UA (1) UA109037C2 (es)
WO (1) WO2012076430A1 (es)
ZA (1) ZA201303811B (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013043518A1 (en) 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Imidazopyridyl compounds as aldosterone synthase inhibitors
WO2013043520A1 (en) 2011-09-22 2013-03-28 Merck Sharp & Dohme Corp. Triazolopyridyl compounds as aldosterone synthase inhibitors
KR20140128998A (ko) 2012-02-09 2014-11-06 에프. 호프만-라 로슈 아게 2-페닐-[1,2,4]트라이아졸로[1,5-a]피리딘 유도체의 제조 방법
JP2016513083A (ja) * 2013-01-31 2016-05-12 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 放射標識された化合物
CA2902781C (en) * 2013-02-27 2020-12-29 Mochida Pharmaceutical Co., Ltd. Novel pyrazole derivative
DK2991984T3 (en) 2013-04-30 2017-05-08 Hoffmann La Roche PALLADIUM-CATALYST COUPLING OF PYRAZOLAMIDES
CN105229005B (zh) * 2013-05-31 2018-01-02 日产化学工业株式会社 杂环酰胺化合物
US10039764B2 (en) 2013-07-12 2018-08-07 University Of South Alabama Treatment and diagnosis of cancer and precancerous conditions using PDE10A inhibitors and methods to measure PDE10A expression
KR20170032328A (ko) 2014-07-30 2017-03-22 모찌다 세이야쿠 가부시끼가이샤 피라졸 유도체의 제조 방법
KR20170032329A (ko) 2014-07-30 2017-03-22 모찌다 세이야쿠 가부시끼가이샤 피라졸 유도체의 제조 방법
WO2020021024A1 (en) * 2018-07-26 2020-01-30 Phenex Pharmaceuticals Ag Substituted bicyclic compounds as modulators of the aryl hydrocarbon receptor (ahr)
BR112022024751A2 (pt) 2020-06-05 2023-03-07 Noema Pharma Ag Uso de um inibidor de fosfodiesterase 10 para o tratamento da síndrome de tourette
JP2024505515A (ja) 2021-01-28 2024-02-06 ノエマ ファーマ アクツィエンゲゼルシャフト 小児期発症流暢症の治療のための方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2534432A1 (en) 2003-07-31 2005-02-10 Bayer Pharmaceuticals Corporation Methods for treating diabetes and related disorders using pde10a inhibitors
TWI501965B (zh) 2008-06-20 2015-10-01 Lundbeck & Co As H 作為pde10a酵素抑制劑之新穎苯基咪唑衍生物

Also Published As

Publication number Publication date
DK2649070T3 (da) 2014-10-13
JP5932828B2 (ja) 2016-06-08
BR112013013912A2 (pt) 2016-09-13
CN103237803A (zh) 2013-08-07
US8349824B2 (en) 2013-01-08
PL2649070T3 (pl) 2015-03-31
EP2649070A1 (en) 2013-10-16
SI2649070T1 (sl) 2014-12-31
SG190305A1 (en) 2013-06-28
IL225969A0 (en) 2013-06-27
ECSP13012667A (es) 2013-08-30
CN103237803B (zh) 2016-04-13
CO6741154A2 (es) 2013-08-30
HRP20141200T1 (hr) 2015-02-13
ES2520647T3 (es) 2014-11-11
MX2013006054A (es) 2013-06-18
PE20140226A1 (es) 2014-03-08
RS53677B1 (en) 2015-04-30
KR20130128426A (ko) 2013-11-26
ZA201303811B (en) 2014-04-30
EA201390799A1 (ru) 2013-12-30
CR20130239A (es) 2013-06-27
CY1115863T1 (el) 2017-01-25
JP2013544859A (ja) 2013-12-19
EA022607B1 (ru) 2016-01-29
UA109037C2 (uk) 2015-07-10
US20120142665A1 (en) 2012-06-07
CA2816829C (en) 2018-12-04
MA35086B1 (fr) 2014-05-02
AU2011340685A1 (en) 2013-05-23
CA2816829A1 (en) 2012-06-14
EP2649070B1 (en) 2014-09-17
CL2013001591A1 (es) 2013-12-27
WO2012076430A1 (en) 2012-06-14
PT2649070E (pt) 2014-11-21

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