[go: up one dir, main page]

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)
  • Gastroenterology & Hepatology (AREA)
  • Urology & Nephrology (AREA)
  • Biomedical Technology (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)

Families Citing this family (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015089800A1 (en) 2013-12-19 2015-06-25 Eli Lilly And Company Fluorophenyl pyrazol compounds
CN109045032A (zh) 2014-01-01 2018-12-21 麦迪威森技术有限责任公司 氨基吡啶类化合物和使用方法
ES2968785T3 (es) * 2014-10-31 2024-05-14 Hoffmann La Roche Nuevos compuestos de piridiniloxi- y feniloxipirazolilo
CA3038749A1 (en) 2016-09-30 2018-04-05 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
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
US10975057B2 (en) * 2018-06-18 2021-04-13 Janssen Pharmaceutica Nv 6-aminopyridin-3-yl pyrazoles as modulators of RORgT
US12049475B2 (en) 2018-07-23 2024-07-30 Brise Pharmaceuticals Co., Ltd. Bisphosphonate drug conjugates
US11040038B2 (en) 2018-07-26 2021-06-22 Sumitomo Dainippon Pharma Oncology, Inc. Methods for treating diseases associated with abnormal ACVR1 expression and ACVR1 inhibitors for use in the same
WO2020041562A1 (en) * 2018-08-22 2020-02-27 Clavius Pharmaceuticals, Llc Substituted imidazoles for the inhibition of tgf-beta and methods of treatment
KR20210076069A (ko) * 2018-10-18 2021-06-23 난징 산홈 팔마세우티칼 컴퍼니 리미티드 TGF-βR1 억제제로서의 화합물 및 이의 적용
WO2020088526A1 (zh) * 2018-10-31 2020-05-07 南京明德新药研发有限公司 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
JP7515049B2 (ja) 2018-12-27 2024-07-12 ネクサス セラピューティクス, インコーポレイテッド がんの処置のためのtgf-ベータr1(alk5)阻害剤としての(ピリジン-2-イル)アミン誘導体
US20200323851A1 (en) * 2019-01-10 2020-10-15 Tolero Pharmaceuticals, Inc. Alk5 inhibitors for treating myelodysplastic syndrome
EP3922631A4 (en) * 2019-01-24 2022-10-26 Jiangsu AoSaiKang Pharmaceutical Co., Ltd. 5-(4-PYRIDYLOXY)PYRAZOLE COMPOUNDS AS A TGF-BETA R1 KINASE INHIBITOR
EP3990445A4 (en) 2019-06-25 2023-07-05 InventisBio Co., Ltd. HETEROCYCLIC COMPOUNDS, METHODS FOR THEIR PREPARATION AND THEIR METHODS OF USE
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
WO2021129621A1 (zh) * 2019-12-23 2021-07-01 江苏先声药业有限公司 吡唑类化合物
CN112812105B (zh) * 2020-03-24 2025-04-01 苏州阿尔脉生物科技有限公司 一种氨基吡啶基氧基吡唑类衍生物及其制备方法和应用
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
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
AU2023239988A1 (en) * 2022-03-22 2024-10-10 Autotelic Bio Inc. Thiazole derivative compound and uses thereof
CN119330934A (zh) * 2023-07-21 2025-01-21 中国人民解放军军事科学院军事医学研究院 一种靶向Smurf1蛋白的降解剂、制备方法及用途
WO2025063819A1 (ko) * 2023-09-21 2025-03-27 오토텔릭바이오 주식회사 티아졸 유도체 화합물을 포함하는 장섬유화증 치료용 조성물
WO2025063820A1 (ko) * 2023-09-21 2025-03-27 오토텔릭바이오 주식회사 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1269820C (zh) 2001-05-24 2006-08-16 伊莱利利公司 作为药物的新的吡咯衍生物
UA80571C2 (en) 2002-11-22 2007-10-10 Lilly Co Eli Quinolinyl-pyrrolopyrazoles
GB0313915D0 (en) * 2003-06-16 2003-07-23 Smithkline Beecham Corp Compounds
WO2009022171A1 (en) * 2007-08-13 2009-02-19 Astrazeneca Ab Pyridinyiioxy pyridines as alk5 inhibitors
US8080568B1 (en) 2010-06-29 2011-12-20 Ewha University - Industry Collaboration Foundation 2-pyridyl substituted imidazoles as therapeutic ALK5 and/or ALK4 inhibitors
AU2012240240A1 (en) 2011-04-04 2013-05-09 Netherlands Cancer Institute Methods and compositions for predicting resistance to anticancer treatment with protein kinase inhibitors
WO2013086397A1 (en) * 2011-12-08 2013-06-13 Array Biopharma Inc. Urea compounds as gka activators
WO2015089800A1 (en) 2013-12-19 2015-06-25 Eli Lilly And Company Fluorophenyl pyrazol compounds

Also Published As

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

Similar Documents

Publication Publication Date Title
PE20170662A1 (es) Compuestos de aminopiridiloxipirazol
MX2021011209A (es) Novedosos inhibidores de molécula pequeña de factores de transcripción tead.
PE20160874A1 (es) Compuestos quimicos
CO2020002961A2 (es) Activadores de piruvato quinasas para usar en el tratamiento de trastornos en la sangre
PE20142098A1 (es) Compuestos terapeuticamente activos y sus metodos de uso
UY35242A (es) Inhibidores de fosfatidilinositol 3-quinasa
SV2016005229A (es) Inhibidores de syk
MY192521A (en) Bicyclic-fused heteroaryl or aryl compounds and their use as irak4 inhibitors
PE20170666A1 (es) 2-(morfolin-4-il)-1,7-naftiridinas
PE20161236A1 (es) Compuesto de triazina y su uso para fines medicos
NZ726108A (en) Substituted dihydroisoquinolinone compounds
PE20141855A1 (es) Benzotienilo-pirrolotriazinas disustituidas y sus usos
PE20160664A1 (es) Compuestos heteroaromaticos y su uso como ligandos d1 de dopamina
PE20211782A1 (es) Compuestos de 5-cloro-2-difluorometoxifenil pirazolopirimidina, composiciones y metodos de uso de los mismos
PE20141408A1 (es) Aminoquinazolinas como inhibidores de quinasa
CL2016000816A1 (es) Forma de dosificación que comprende al compuesto (s)-3-(4-((4-morfolinometil)bencil)oxi)-1-oxoisoindolin-2-il)piperidin-2,6-diona, una cantidad de 90 hasta 99,9 por ciento en peso del peso total de una mezcla de almidón y lactosa como portador o excipiente, y acido esteárico como lubricante; su uso en el tratamiento de cáncer y enfermedades autoinmunes, entre otras.
MX2016016530A (es) Inhibidores de fosfatidilinositol 3-quinasa.
MD20160053A2 (ro) Derivaţi ai purinei 2,6-substituite şi utilizarea acestora în tratamentul tulburărilor proliferative
AR100431A1 (es) Compuestos de pladienolida piridina y métodos de uso
CL2011001860A1 (es) Compuestos derivados de indol; procedimiento de preparacion de dichos compuestos; composicion y combinacion farmaceutica; y uso en el tratamiento del cancer.
CY1117565T1 (el) Συνενωμενο δικυκλικο παραγωγο 2,4-διαμινοπυριδινης ως διπλος αναστολεας alk και fak
CO2017003969A2 (es) Derivado de isoxazol como inhibidor de isocitrato deshidrogenasa 1 mutante
TR201819805T4 (tr) Flavaglin türevleri̇.
CO2019002517A2 (es) Inhibidores de dopamina–β–hidroxilasa
ECSP13012548A (es) Inhibidores de oxadiazol de la producción de leucotrienos.