AR102003A1 - Compuestos de aminopiridiloxipirazol - Google Patents

Compuestos de aminopiridiloxipirazol

Info

Publication number
AR102003A1
AR102003A1 ARP150103058A ARP150103058A AR102003A1 AR 102003 A1 AR102003 A1 AR 102003A1 AR P150103058 A ARP150103058 A AR P150103058A AR P150103058 A ARP150103058 A AR P150103058A AR 102003 A1 AR102003 A1 AR 102003A1
Authority
AR
Argentina
Prior art keywords
cancer
pyridin
compounds
methyl
cyclopropyl
Prior art date
Application number
ARP150103058A
Other languages
English (en)
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 AR102003A1 publication Critical patent/AR102003A1/es

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Classifications

    • 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
    • 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
    • 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
    • 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (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

Que inhiben la actividad del receptor 1 del factor del crecimiento transformante b (TGFbR1), composiciones farmacéuticas que comprenden los compuestos y métodos para utilizar los compuestos para tratar cáncer, preferentemente cáncer de colon, melanoma, carcinoma hepatocelular, cáncer renal, glioblastoma, cáncer de páncreas, síndrome mielodisplásico, cáncer de plumón y cáncer gástrico y/o fibrosis, preferentemente fibrosis hepática y enfermedad renal crónica. Reivindicación 1: Un compuesto de la fórmula (1) en el cual: R¹ es hidrógeno, isopropilo, difluorometilo, difluoroetilo o ciclopropilo; R² es etilo, terc-butilo, piridin-2-ilo, tetrahidropiran-4-ilo, tetrahidrofuran-3-ilo, ciclopropilo o ciclobutilo; y R³ es carbamoilfenilo, piridin-2-ilo, (1-hidroxi-1-metiletil)piridinilo, 1-metil-2-oxo-1H-piridin-4-ilo, 1-metilpirazolilo, pirazin-2-ilo, 2-metoxipirimidin-4-ilo, 1-metil-2-oxo-1H-pirimidin-4-ilo, piridazin-3-ilo, 6-cloropiridazin-3-ilo, 6-metilpiridazin-3-ilo, o 6-metoxipiridazin-3-ilo; o una sal de ellos aceptable desde el punto de vista farmacéutico.
ARP150103058A 2014-10-07 2015-09-23 Compuestos de aminopiridiloxipirazol AR102003A1 (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
AR102003A1 true AR102003A1 (es) 2017-01-25

Family

ID=54266692

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP150103058A AR102003A1 (es) 2014-10-07 2015-09-23 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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WO2015089800A1 (en) 2013-12-19 2015-06-25 Eli Lilly And Company Fluorophenyl pyrazol compounds
AU2014373773C1 (en) 2014-01-01 2019-06-27 Medivation Technologies Llc Compounds and methods of use
JP6626885B2 (ja) * 2014-10-31 2019-12-25 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft 新しいピリジニルオキシ及びフェニルオキシピラゾリル化合物
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
CN107540672A (zh) * 2017-10-10 2018-01-05 牡丹江医学院 一种治疗肝硬化的药物及其合成方法
CN107892687B (zh) * 2018-01-21 2018-08-24 广东莱恩医药研究院有限公司 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
CA3103771A1 (en) * 2018-06-18 2019-12-26 Janssen Pharmaceutica Nv 6-aminopyridin-3-yl pyrazoles as modulators of roryt
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
CN112512597A (zh) 2018-07-26 2021-03-16 大日本住友制药肿瘤公司 用于治疗与acvr1表达异常相关的疾病的方法以及用于此的acvr1抑制剂
WO2020041562A1 (en) * 2018-08-22 2020-02-27 Clavius Pharmaceuticals, Llc Substituted imidazoles for the inhibition of tgf-beta and methods of treatment
WO2020078402A1 (zh) * 2018-10-18 2020-04-23 南京圣和药业股份有限公司 作为TGF-βR1抑制剂的化合物及其应用
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
BR112021007006A2 (pt) * 2018-12-27 2021-08-10 Nexys Therapeutics, Inc. derivados de (piridin-2-il)amina como inibidores de tgf-beta r1(alk5) para o tratamento de câncer
US20200323851A1 (en) * 2019-01-10 2020-10-15 Tolero Pharmaceuticals, Inc. Alk5 inhibitors for treating myelodysplastic syndrome
KR20210118891A (ko) 2019-01-24 2021-10-01 지앙수 아오사이캉 파마수티칼 씨오., 엘티디. TGF-β R1 키나아제 억제제로서의 5-(4-피리딜옥시)피라졸 화합물
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
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
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
WO2021204626A1 (en) 2020-04-06 2021-10-14 Almirall, S.A. Aryl and heteroaryl-carboxamide substituted heteroaryl compounds as tyk2 inhibitors
CN113698395B (zh) * 2020-05-22 2023-12-08 赛诺哈勃药业(成都)有限公司 转化生长因子受体拮抗剂、其制备方法和应用
CN114867723B (zh) * 2020-07-23 2023-05-30 江苏奥赛康药业有限公司 作为TGF-βR1抑制剂的吡啶氧基连吡唑类化合物的盐型、晶型以及其药物组合物
WO2023182780A1 (ko) * 2022-03-22 2023-09-28 오토텔릭바이오 주식회사 티아졸 유도체 화합물 및 이의 용도

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Also Published As

Publication number Publication date
MA41038B1 (fr) 2018-10-31
NZ729800A (en) 2018-07-27
TR201816415T4 (tr) 2018-11-21
US9617243B2 (en) 2017-04-11
EP3204377A1 (en) 2017-08-16
CO2017002233A2 (es) 2017-05-31
CY1120903T1 (el) 2020-05-29
WO2016057278A1 (en) 2016-04-14
BR112017005453A2 (pt) 2017-12-12
KR20170045348A (ko) 2017-04-26
KR101921847B1 (ko) 2018-11-23
TWI582083B (zh) 2017-05-11
BR112017005453A8 (pt) 2018-04-24
SV2017005411A (es) 2017-04-21
JP2016535745A (ja) 2016-11-17
HRP20181797T1 (hr) 2018-12-28
JP6043894B2 (ja) 2016-12-14
TW201623282A (zh) 2016-07-01
TN2017000046A1 (en) 2018-07-04
MA41038A (fr) 2017-08-16
AU2015328553A1 (en) 2017-03-09
CL2017000765A1 (es) 2017-12-15
CN106795139A (zh) 2017-05-31
CR20170072A (es) 2017-05-12
JO3336B1 (ar) 2019-03-13
PH12017500635A1 (en) 2017-09-25
AP2017009836A0 (en) 2017-03-31
SG11201702481UA (en) 2017-04-27
ES2700376T3 (es) 2019-02-15
MX2017004457A (es) 2017-06-19
EP3204377B1 (en) 2018-09-26
MY190541A (en) 2022-04-27
CA2961262A1 (en) 2016-04-14
UA118807C2 (uk) 2019-03-11
GT201700067A (es) 2019-10-10
LT3204377T (lt) 2018-12-27
AU2015328553B2 (en) 2018-04-12
RS58094B1 (sr) 2019-02-28
EA201790476A1 (ru) 2017-08-31
PT3204377T (pt) 2018-12-19
CN106795139B (zh) 2019-08-09
DOP2017000090A (es) 2017-04-30
DK3204377T3 (en) 2018-11-26
IL250543A0 (en) 2017-03-30
PE20170662A1 (es) 2017-05-26
MX367360B (es) 2019-08-16
SI3204377T1 (sl) 2018-11-30
ECSP17021097A (es) 2018-02-28
BR112017005453B1 (pt) 2022-12-06
IL250543B (en) 2020-06-30
US20160096823A1 (en) 2016-04-07
EA031830B1 (ru) 2019-02-28
CA2961262C (en) 2019-10-22
PH12017500635B1 (en) 2017-09-25
PL3204377T3 (pl) 2019-02-28
ZA201701175B (en) 2019-01-30
AU2015328553C1 (en) 2018-11-15

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