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PE20110906A1 - Compuestos de arilo con sustituyentes heterociclicos como inhibidores hif - Google Patents

Compuestos de arilo con sustituyentes heterociclicos como inhibidores hif

Info

Publication number
PE20110906A1
PE20110906A1 PE2011000986A PE2011000986A PE20110906A1 PE 20110906 A1 PE20110906 A1 PE 20110906A1 PE 2011000986 A PE2011000986 A PE 2011000986A PE 2011000986 A PE2011000986 A PE 2011000986A PE 20110906 A1 PE20110906 A1 PE 20110906A1
Authority
PE
Peru
Prior art keywords
pyrazole
phenyl
methyl
aryl compounds
pyridyl
Prior art date
Application number
PE2011000986A
Other languages
English (en)
Inventor
Michael Harter
Hartmut Beck
Peter Ellinghaus
Kerstin Berhoerster
Susanne Greschat
Karl-Heinz Thierauch
Frank Sussmeier
Original Assignee
Bayer Ip Gmbh
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
Priority claimed from DE102008057343A external-priority patent/DE102008057343A1/de
Priority claimed from DE102009041242A external-priority patent/DE102009041242A1/de
Application filed by Bayer Ip Gmbh filed Critical Bayer Ip Gmbh
Publication of PE20110906A1 publication Critical patent/PE20110906A1/es

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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4245—Oxadiazoles
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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 or sparfloxacin
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    • 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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • A—HUMAN NECESSITIES
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    • 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
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    • A61K31/54—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 sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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    • 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
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
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    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
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    • 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
    • C07D471/08—Bridged systems
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    • 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
    • C07D487/08—Bridged systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Vascular Medicine (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

REFERIDA A UN COMPUESTO DE FORMULA I, DONDE A ES FENILO, PIRIDILO; B-R3 ES PIRAZOL-3-R3, PIRAZOL-1-R3, ENTRE OTROS; R3 ES CH3-, C2H5-, CF3-; D ES DE PREFERENCIA 1,2,4-OXADIAZOL; E ES FENILO, PIRIDILO; N ES UN ANILLO AZAHETEROCICLO DE 4-10 MIEMBROS SATURADO, QUE CONTIENE AL MENOS UN ATOMO DE N COMO MIEMBROS DEL ANILLO; X ES UN ENLACE, -O-, -S-, -C(=O)-, ENTRE OTROS; R1 ES ES F, CN, HIDROXI, ENTRE OTROS; m ES 0-4; R2 ES ALQUILO C1-C6, ALQUILCARBONILO C1-C6, ALCOXICARBONILO C1-C6, ENTRE OTROS; n ES 0-1; R4 ES H, HALOGENO, CN, ENTRE OTROS; R5 ES F, Cl, METILO HIDROXILO, ENTRE OTROS; p ES 0-2. UN COMPUESTO PREFERIDO ES 2-CLORO-5-[(3-{3-[4-(2-FLUOROPROPAN-2-IL)FENIL]-1,2,4-OXADIAZOL-5-IL}-5-METIL-1H-PIRAZOL-1-IL)METIL]PIRIDINA. DICHOS COMPUESTOS SON INHIBIDORES DE LA TRANSACTIVACION DEL FACTOR DE TRANSCRIPCION HIF UTILES EN EL TRATAMIENTO DE ENFERMEDADES HIPERPROLIFERATIVAS Y ANGIOGENICAS
PE2011000986A 2008-11-14 2009-10-31 Compuestos de arilo con sustituyentes heterociclicos como inhibidores hif PE20110906A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE102008057343A DE102008057343A1 (de) 2008-11-14 2008-11-14 Heterocyclisch substituierte Aryl-Verbindungen und ihre Verwendung
DE102009041242A DE102009041242A1 (de) 2009-09-11 2009-09-11 Heterocyclisch substituierte Aryl-Verbindungen und ihre Verwendung

Publications (1)

Publication Number Publication Date
PE20110906A1 true PE20110906A1 (es) 2011-12-21

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PE2011000986A PE20110906A1 (es) 2008-11-14 2009-10-31 Compuestos de arilo con sustituyentes heterociclicos como inhibidores hif

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US (1) US20130196964A1 (es)
EP (1) EP2356113B1 (es)
JP (1) JP5829915B2 (es)
KR (1) KR20110082569A (es)
CN (1) CN102282143A (es)
AR (1) AR074336A1 (es)
AU (1) AU2009316019A1 (es)
BR (1) BRPI0921257A2 (es)
CA (1) CA2743536A1 (es)
CL (1) CL2011001060A1 (es)
CO (1) CO6361923A2 (es)
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CU (1) CU24067B1 (es)
DK (1) DK2356113T3 (es)
DO (1) DOP2011000132A (es)
EA (1) EA022271B1 (es)
EC (1) ECSP11011042A (es)
ES (1) ES2538301T3 (es)
GT (1) GT201100118A (es)
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MX (1) MX2011005025A (es)
MY (1) MY160004A (es)
NZ (1) NZ592792A (es)
PE (1) PE20110906A1 (es)
PL (1) PL2356113T3 (es)
PT (1) PT2356113E (es)
SA (1) SA109300677B1 (es)
SV (1) SV2011003901A (es)
TN (1) TN2011000234A1 (es)
TW (1) TW201031656A (es)
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US10793515B2 (en) 2008-03-19 2020-10-06 Aurimmed Pharma, Inc. Compounds advantageous in the treatment of central nervous system diseases and disorders
RU2010142655A (ru) * 2008-03-19 2012-04-27 Ауриммед Фарма, Инк. (Us) Соединение, пригодное для лечения болезней и нарушений центральной нервной системы, и способ его получения
CN102905527B (zh) 2010-01-11 2016-08-24 阿斯特来亚治疗有限责任公司 烟碱型乙酰胆碱受体调节剂
WO2011141325A1 (de) * 2010-05-08 2011-11-17 Bayer Pharma Aktiengesellschaft Hydroxyalkylbenzyl- pyrazole und ihre verwendung zur behandlung von hyperproliferativen und angiogenen erkrankungen
MA34939B1 (fr) * 2010-05-08 2014-03-01 Bayer Ip Gmbh Hétérocyclylbenzyle-pyrazoles substituées et leur utilisation
CN103313976B (zh) 2010-06-30 2016-11-23 铁木医药有限公司 sGC刺激物
US9061030B2 (en) 2010-11-09 2015-06-23 Ironwood Pharmaceuticals, Inc. sGC stimulators
UY34200A (es) 2011-07-21 2013-02-28 Bayer Ip Gmbh 3-(fluorovinil)pirazoles y su uso
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