PE20170662A1 - Compuestos de aminopiridiloxipirazol - Google Patents

Compuestos de aminopiridiloxipirazol

Info

Publication number
PE20170662A1
PE20170662A1 PE2017000536A PE2017000536A PE20170662A1 PE 20170662 A1 PE20170662 A1 PE 20170662A1 PE 2017000536 A PE2017000536 A PE 2017000536A PE 2017000536 A PE2017000536 A PE 2017000536A PE 20170662 A1 PE20170662 A1 PE 20170662A1
Authority
PE
Peru
Prior art keywords
pyridin
compounds
pyrazol
propan
pyran
Prior art date
Application number
PE2017000536A
Other languages
English (en)
Inventor
Douglas W Beight
David A Coates
Sajan Joseph
William T Mcmillen
Saravanan Parthasarathy
Huaxing Pei
Jason Scott Sawyer
Craig D Wolfangel
Gaiying Zhao
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20170662A1 publication Critical patent/PE20170662A1/es

Links

Classifications

    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non 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
    • 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P19/04Drugs for skeletal disorders for non-specific disorders of the connective tissue
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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 two hetero rings
    • C07D401/12Heterocyclic 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 two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Biomedical Technology (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Se refiere a un compuesto de formula I, donde: R1 es hidrogeno, isopropilo, entre otros; R2 es etilo, terc-butilo, entre otros; R3 es carbamoilfenilo, piridin-2-ilo, entre otros. Son compuestos preferidos: 2-{4-[(4-{[1-ciclopropil-3-(tetrahidro-2H-piran-4-il)-1H-pirazol-4-il]oxi}piridin-2-il)amino]piridin-2-il}propan-2-ol; 4-metilbencesulfonato de 2-{4-[(4-{[1-ciclopropil-3-(tetrahidro-2H-piran-4-il)-1H-pirazol-4-il]oxi}piridin-2-il)amino]piridin-2-il}propan-2-ol; entre otros. Tambien se refiere a una composicion farmaceutica. Dichos compuestos son derivados de aminopiridiloxipirazol que inhiben la actividad del receptor 1 del factor del crecimiento transformante beta (TGFBETAR1), siendo utiles en el tratamiento del cancer, preferentemente cancer de colon, melanoma, carcinoma, entre otros
PE2017000536A 2014-10-07 2015-09-30 Compuestos de aminopiridiloxipirazol PE20170662A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201462060724P 2014-10-07 2014-10-07

Publications (1)

Publication Number Publication Date
PE20170662A1 true PE20170662A1 (es) 2017-05-26

Family

ID=54266692

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2017000536A PE20170662A1 (es) 2014-10-07 2015-09-30 Compuestos de aminopiridiloxipirazol

Country Status (42)

Country Link
US (1) US9617243B2 (es)
EP (1) EP3204377B1 (es)
JP (1) JP6043894B2 (es)
KR (1) KR101921847B1 (es)
CN (1) CN106795139B (es)
AP (1) AP2017009836A0 (es)
AR (1) AR102003A1 (es)
AU (1) AU2015328553C1 (es)
BR (1) BR112017005453B1 (es)
CA (1) CA2961262C (es)
CL (1) CL2017000765A1 (es)
CO (1) CO2017002233A2 (es)
CR (1) CR20170072A (es)
CY (1) CY1120903T1 (es)
DK (1) DK3204377T3 (es)
DO (1) DOP2017000090A (es)
EA (1) EA031830B1 (es)
EC (1) ECSP17021097A (es)
ES (1) ES2700376T3 (es)
GT (1) GT201700067A (es)
HR (1) HRP20181797T1 (es)
IL (1) IL250543B (es)
JO (1) JO3336B1 (es)
LT (1) LT3204377T (es)
MA (1) MA41038B1 (es)
MX (1) MX367360B (es)
MY (1) MY190541A (es)
NZ (1) NZ729800A (es)
PE (1) PE20170662A1 (es)
PH (1) PH12017500635B1 (es)
PL (1) PL3204377T3 (es)
PT (1) PT3204377T (es)
RS (1) RS58094B1 (es)
SG (1) SG11201702481UA (es)
SI (1) SI3204377T1 (es)
SV (1) SV2017005411A (es)
TN (1) TN2017000046A1 (es)
TR (1) TR201816415T4 (es)
TW (1) TWI582083B (es)
UA (1) UA118807C2 (es)
WO (1) WO2016057278A1 (es)
ZA (1) ZA201701175B (es)

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PL3089971T3 (pl) 2014-01-01 2021-01-25 Medivation Technologies Llc Związki i sposoby ich zastosowania
CN106795120B (zh) * 2014-10-31 2020-09-01 豪夫迈·罗氏有限公司 新的吡啶基氧基-和苯基氧基-吡唑基化合物
EP3518926A1 (en) * 2016-09-30 2019-08-07 Eli Lilly and Company USE OF 2-{4-[(4-{[1-CYCLOPROPYL-3-TETRAHYDRO-2H-PYRAN-4-yl)-1H-PYRAZOL-4-yl]OXY}PYRIDINE-2-yl)AMINO]PYRIDIN-2-yl}PROPAN-2-OL IN THE TREATMENT OF CANCER
JOP20190080A1 (ar) * 2016-10-14 2019-04-11 Bayer Pharma AG مركبات مشتقة من 6-(1h-بيرازول-1-يل) بيريميدين-4- أمين مستبدل واستخداماتها
US11124509B2 (en) 2017-03-23 2021-09-21 Clavius Pharmaceuticals, LLC. Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment
WO2019013790A1 (en) * 2017-07-12 2019-01-17 Curza Global, Llc ANTIMICROBIAL COMPOUNDS AND USES THEREOF
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CN108912103A (zh) * 2018-01-21 2018-11-30 吕迎春 一种2-乙酸酯咪唑类化合物及其在防治骨质疏松药物中的应用
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CN112867724A (zh) 2018-07-23 2021-05-28 广州噢斯荣医药技术有限公司 二膦酸盐药物缀合物
CA3103995A1 (en) 2018-07-26 2020-01-30 Sumitomo Dainippon Pharma Oncology, Inc. Methods for treating diseases associated with abnormal acvr1 expression and acvr1 inhibitors for use in the same
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EP3868755A4 (en) * 2018-10-18 2022-05-25 Nanjing Sanhome Pharmaceutical Co., Ltd. TGF-BETA R1 INHIBITOR COMPOUND AND USE THEREOF
CN112839946B (zh) * 2018-10-31 2022-04-12 江苏奥赛康药业有限公司 作为TGF-βR1激酶抑制剂的双环吡唑类化合物
WO2020103817A1 (zh) * 2018-11-20 2020-05-28 南京圣和药业股份有限公司 TGF-βR1抑制剂及其应用
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CN113272281A (zh) * 2019-01-10 2021-08-17 大日本住友制药肿瘤公司 用于治疗骨髓增生异常综合征的alk5抑制剂
WO2020151749A1 (zh) 2019-01-24 2020-07-30 南京明德新药研发有限公司 作为TGF-βR1激酶抑制剂的5-(4-吡啶氧基)吡唑类化合物
WO2020258006A1 (en) * 2019-06-25 2020-12-30 Inventisbio Shanghai Ltd. Heterocyclic compounds, preparation methods therefor, and methods of uses thereof
CN112694477B (zh) * 2019-10-22 2024-02-06 四川科伦博泰生物医药股份有限公司 吡唑并环类化合物,包含其的药物组合物,其制备方法及其用途
CN114728980A (zh) * 2019-12-23 2022-07-08 江苏先声药业有限公司 吡唑类化合物
CN111303135A (zh) * 2020-04-01 2020-06-19 中科利健制药(广州)有限公司 4-(4-吡唑氧基)喹啉类化合物、其制备方法、药物组合物与应用
CN111116565B (zh) * 2020-04-01 2020-07-14 中科利健制药(广州)有限公司 2-芳基-4-(4-吡唑氧基)吡啶类化合物、其制备方法、药物组合物与应用
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Also Published As

Publication number Publication date
BR112017005453A8 (pt) 2018-04-24
MY190541A (en) 2022-04-27
US20160096823A1 (en) 2016-04-07
DK3204377T3 (en) 2018-11-26
JP6043894B2 (ja) 2016-12-14
SI3204377T1 (sl) 2018-11-30
JP2016535745A (ja) 2016-11-17
MA41038B1 (fr) 2018-10-31
CA2961262A1 (en) 2016-04-14
MA41038A (fr) 2017-08-16
CO2017002233A2 (es) 2017-05-31
ES2700376T3 (es) 2019-02-15
WO2016057278A1 (en) 2016-04-14
KR101921847B1 (ko) 2018-11-23
PH12017500635A1 (en) 2017-09-25
AU2015328553A1 (en) 2017-03-09
LT3204377T (lt) 2018-12-27
SG11201702481UA (en) 2017-04-27
AR102003A1 (es) 2017-01-25
CA2961262C (en) 2019-10-22
IL250543A0 (en) 2017-03-30
GT201700067A (es) 2019-10-10
TR201816415T4 (tr) 2018-11-21
EP3204377B1 (en) 2018-09-26
JO3336B1 (ar) 2019-03-13
PL3204377T3 (pl) 2019-02-28
CR20170072A (es) 2017-05-12
MX2017004457A (es) 2017-06-19
HRP20181797T1 (hr) 2018-12-28
EP3204377A1 (en) 2017-08-16
BR112017005453B1 (pt) 2022-12-06
DOP2017000090A (es) 2017-04-30
AU2015328553B2 (en) 2018-04-12
UA118807C2 (uk) 2019-03-11
IL250543B (en) 2020-06-30
EA201790476A1 (ru) 2017-08-31
TN2017000046A1 (en) 2018-07-04
CY1120903T1 (el) 2020-05-29
CL2017000765A1 (es) 2017-12-15
RS58094B1 (sr) 2019-02-28
BR112017005453A2 (pt) 2017-12-12
SV2017005411A (es) 2017-04-21
ECSP17021097A (es) 2018-02-28
AU2015328553C1 (en) 2018-11-15
MX367360B (es) 2019-08-16
CN106795139A (zh) 2017-05-31
TW201623282A (zh) 2016-07-01
PT3204377T (pt) 2018-12-19
ZA201701175B (en) 2019-01-30
CN106795139B (zh) 2019-08-09
NZ729800A (en) 2018-07-27
US9617243B2 (en) 2017-04-11
TWI582083B (zh) 2017-05-11
PH12017500635B1 (en) 2017-09-25
AP2017009836A0 (en) 2017-03-31
KR20170045348A (ko) 2017-04-26
EA031830B1 (ru) 2019-02-28

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