AR078437A1 - Derivados de imidazopiridina, procesos de obtencion y composiciones farmaceuticas - Google Patents

Derivados de imidazopiridina, procesos de obtencion y composiciones farmaceuticas

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Publication number
AR078437A1
AR078437A1 ARP100103465A ARP100103465A AR078437A1 AR 078437 A1 AR078437 A1 AR 078437A1 AR P100103465 A ARP100103465 A AR P100103465A AR P100103465 A ARP100103465 A AR P100103465A AR 078437 A1 AR078437 A1 AR 078437A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
alkyl
alkoxy
fluoroalkyl
fluoro
Prior art date
Application number
ARP100103465A
Other languages
English (en)
Inventor
Alexander Flohr
Markus Rudolph
Katrin Groebke Zbinden
Jens-Uwe Peters
Konrad Bleicher
Daniela Alberati
Bernd Kuhn
Sanchez Ruben Alvarez
Matthias Koerner
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 AR078437A1 publication Critical patent/AR078437A1/es

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    • 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
    • C07D471/04—Ortho-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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • 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
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Abstract

Estos compuestos inhiben PDE1OA y pueden utilizarse como medicamentos. Reivindicacion 1: Compuestos de formula (1) en los que A es N o C(R6); R1 es hidrogeno, alquilo inferior o fluoroalquilo inferior; R2 es halogeno, C(O)NR7R8 o C(O)OR9; R3 es hidrogeno, NR10R11, alquilo inferior, alcoxi inferior, fluoro-alquilo inferior o fluoro-alcoxi inferior; R4 es hidrogeno, alquilo inferior, fluoroalquilo inferior, alcoxi inferior o fluoro-alcoxi inferior; R5 es arilo o heteroarilo, que puede estar sustituido opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halogeno, alquilo inferior, alcoxi inferior, fluoroalquilo inferior, fluoro-alcoxi inferior e hidroxi; R6 es hidrogeno, halogeno, CN, cicloalquilo, alquilo inferior, cicloalquil-alquilo inferior, alcoxi inferior, fluoro-alquilo inferior o fluoro-alcoxi inferior; R7 y R8 independientemente el uno del otro se selecciona del grupo que consiste en hidrogeno, alquilo inferior, alcoxi inferior-alquilo inferior, fluoroalquilo inferior, cicloalquilo, cicloalquil-alquilo inferior, NH2-alquilo inferior, N(H,alquilo inferior)-alquilo inferior, N(alquilo inferior2)-alquilo inferior, hidroxi-alquilo inferior, hidroxi-alcoxi inferior-alquilo inferior, NH2C(O)-alquilo inferior, N(H,alquilo inferior)C(O)-alquilo inferior, N(alquilo inferior2)C(O)-alquilo inferior, alcoxi inferior, hidroxi-alquilo inferior-oxetanil-alquilo inferior, oxotetrahidrofuranilo, tetrahidrofuranil-alquilo inferior, oxo-tetrahidrofuranil-alquilo inferior, hidroxifluoroalquilo inferior, tetrahidrofuranilo, arilo y heteroarilo, dicho arilo o heteroarilo pueden estar sustituidos opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halogeno, alquilo inferior, alcoxi inferior, fluoroalquilo inferior, fluoroalcoxi inferior e hidroxi, o R7 y R8, junto con el átomo de nitrogeno al que están unidos, forman un heterociclilo seleccionado de entre el grupo que consiste en pirrolidinilo, azetidinilo, morfolinilo, 5,6-dihidro-8-H-[1,2,4]triazolo[4,3-a]pirazinilo, 3,4-dihidro-1H-pirrolo[1,2-a]pirazinilo, 2-oxa-6-aza-spiro[3,3]heptilo, 5,6-dihidro-8H-imidazo[1,2-a]pirazinilo, [1,4]oxazepanilo, piperazinilo, tiomorfolinilo y 2-oxa-5-aza-biciclo[2,2,1]heptilo, dicho heterociclilo puede estar sustituidos opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halogeno, alquilo inferior, alquilo inferior-C(O), alcoxi inferior-alquilo inferior, oxo, hidroxi, hidroxialquilo inferior, N(alquilo inferior2), NH2, N(H,alquilo inferior), fluoroalquilo inferior, fluoroalquilo inferior-C(O), alcoxi inferior y fluoro-alcoxi inferior; R9 es hidrogeno, alquilo inferior, o fluoroalquilo inferior; R10 y R11 independientemente el uno del otro son hidrogeno, alquilo inferior o fluoroalquilo inferior, o R10 y R11, junto con el átomo de nitrogeno al que están unidos, forman un heterociclilo seleccionado de entre el grupo que consiste en piperidinilo, morfolinilo, pirrolidinilo, azetidinilo y piperazinilo, dicho heterociclilo puede estar sustituido opcionalmente por 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halogeno, alquilo inferior, alcoxi inferior, fluoro-alquilo inferior y fluoro-alcoxi inferior; y sales farmacéuticamente aceptables y ésteres de los mismos.
ARP100103465A 2009-09-24 2010-09-23 Derivados de imidazopiridina, procesos de obtencion y composiciones farmaceuticas AR078437A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09171253 2009-09-24

Publications (1)

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AR078437A1 true AR078437A1 (es) 2011-11-09

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US (2) US8017604B2 (es)
EP (1) EP2480546B1 (es)
JP (1) JP5629322B2 (es)
KR (1) KR101426624B1 (es)
CN (1) CN102548991B (es)
AR (1) AR078437A1 (es)
BR (1) BR112012006531A2 (es)
CA (1) CA2770087C (es)
CL (1) CL2012000708A1 (es)
CY (1) CY1116120T1 (es)
DK (1) DK2480546T3 (es)
ES (1) ES2530884T3 (es)
HR (1) HRP20150345T1 (es)
IL (1) IL218032A (es)
MX (1) MX2012003469A (es)
PE (1) PE20121438A1 (es)
PL (1) PL2480546T3 (es)
PT (1) PT2480546E (es)
RU (1) RU2502737C2 (es)
SI (1) SI2480546T1 (es)
TW (1) TWI402268B (es)
WO (1) WO2011036127A1 (es)

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CR20190101A (es) 2016-09-02 2019-07-04 Ironwood Pharmaceuticals Inc Estimuladores de sgc
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CA2770087C (en) 2014-09-09
RU2502737C2 (ru) 2013-12-27
US20110294779A1 (en) 2011-12-01
KR101426624B1 (ko) 2014-08-05
CY1116120T1 (el) 2017-02-08
IL218032A (en) 2014-06-30
ES2530884T3 (es) 2015-03-06
EP2480546A1 (en) 2012-08-01
JP2013505911A (ja) 2013-02-21
IL218032A0 (en) 2012-04-30
US20110071128A1 (en) 2011-03-24
WO2011036127A1 (en) 2011-03-31
US8263584B2 (en) 2012-09-11
SI2480546T1 (sl) 2015-03-31
CL2012000708A1 (es) 2012-09-07
EP2480546B1 (en) 2014-12-31
HRP20150345T1 (hr) 2015-05-08
CN102548991A (zh) 2012-07-04
PT2480546E (pt) 2015-02-09
CA2770087A1 (en) 2011-03-31
DK2480546T3 (en) 2015-02-02
CN102548991B (zh) 2015-03-25
MX2012003469A (es) 2012-04-19
TW201116530A (en) 2011-05-16
AU2010299927A1 (en) 2012-03-15
US8017604B2 (en) 2011-09-13
TWI402268B (zh) 2013-07-21
PL2480546T3 (pl) 2015-05-29
RU2012113128A (ru) 2013-11-10
JP5629322B2 (ja) 2014-11-19
KR20120068943A (ko) 2012-06-27
BR112012006531A2 (pt) 2016-11-22
PE20121438A1 (es) 2012-10-26

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