PE20170662A1 - Compuestos de aminopiridiloxipirazol - Google Patents
Compuestos de aminopiridiloxipirazolInfo
- 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
Links
Classifications
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- 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
- A61K31/445—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
- 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
- A61K31/445—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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- 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
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/02—Heterocyclic 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
- C07D401/12—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic 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
- C07D401/14—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/14—Heterocyclic 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
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)
Families Citing this family (28)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2015089800A1 (en) | 2013-12-19 | 2015-06-25 | Eli Lilly And Company | Fluorophenyl pyrazol compounds |
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 |
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 |
EP3806958B1 (en) * | 2018-06-18 | 2022-09-07 | 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 |
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 |
US20220064187A1 (en) * | 2018-08-22 | 2022-03-03 | Clavius Pharmaceuticals, Llc | Substituted imidazoles for the inhibition of tgf-beta and methods of treatment |
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 |
MX2021007738A (es) * | 2018-12-27 | 2021-08-05 | Nexys Therapeutics Inc | Derivados de (piridin-2-il)amina como inhibidores de tgf-beta r1 (alk5) para el tratamiento de cancer. |
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 |
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 |
WO2022017208A1 (zh) * | 2020-07-23 | 2022-01-27 | 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 |
Family Cites Families (8)
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UA76461C2 (en) | 2001-05-24 | 2006-08-15 | Lilly Co Eli | Pyrrazole derivatives as pharmaceutical agents, use thereof, a pharmaceutical composition on their basis |
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 |
US20140296248A1 (en) | 2011-04-04 | 2014-10-02 | Stichting het Nederlands Kanker Instiuut-Antoni van Leeuwenhoek ziekenhuis | Methods and compositions for predicting resistance to anticancer treatment |
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 |
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2015
- 2015-09-22 JO JOP/2015/0235A patent/JO3336B1/ar active
- 2015-09-22 TW TW104131319A patent/TWI582083B/zh not_active IP Right Cessation
- 2015-09-23 AR ARP150103058A patent/AR102003A1/es unknown
- 2015-09-30 UA UAA201702921A patent/UA118807C2/uk unknown
- 2015-09-30 MY MYPI2017701190A patent/MY190541A/en unknown
- 2015-09-30 EP EP15777845.7A patent/EP3204377B1/en active Active
- 2015-09-30 SG SG11201702481UA patent/SG11201702481UA/en unknown
- 2015-09-30 RS RS20181372A patent/RS58094B1/sr unknown
- 2015-09-30 TR TR2018/16415T patent/TR201816415T4/tr unknown
- 2015-09-30 PE PE2017000536A patent/PE20170662A1/es unknown
- 2015-09-30 MA MA41038A patent/MA41038B1/fr unknown
- 2015-09-30 SI SI201530417T patent/SI3204377T1/sl unknown
- 2015-09-30 CR CR20170072A patent/CR20170072A/es unknown
- 2015-09-30 AU AU2015328553A patent/AU2015328553C1/en not_active Ceased
- 2015-09-30 CA CA2961262A patent/CA2961262C/en active Active
- 2015-09-30 ES ES15777845T patent/ES2700376T3/es active Active
- 2015-09-30 TN TN2017000046A patent/TN2017000046A1/en unknown
- 2015-09-30 NZ NZ729800A patent/NZ729800A/en unknown
- 2015-09-30 KR KR1020177009123A patent/KR101921847B1/ko active IP Right Grant
- 2015-09-30 AP AP2017009836A patent/AP2017009836A0/en unknown
- 2015-09-30 JP JP2016526891A patent/JP6043894B2/ja active Active
- 2015-09-30 LT LTEP15777845.7T patent/LT3204377T/lt unknown
- 2015-09-30 EA EA201790476A patent/EA031830B1/ru not_active IP Right Cessation
- 2015-09-30 BR BR112017005453-1A patent/BR112017005453B1/pt active IP Right Grant
- 2015-09-30 PT PT15777845T patent/PT3204377T/pt unknown
- 2015-09-30 US US14/870,033 patent/US9617243B2/en active Active
- 2015-09-30 CN CN201580054343.9A patent/CN106795139B/zh active Active
- 2015-09-30 WO PCT/US2015/053098 patent/WO2016057278A1/en active Application Filing
- 2015-09-30 DK DK15777845.7T patent/DK3204377T3/en active
- 2015-09-30 MX MX2017004457A patent/MX367360B/es active IP Right Grant
- 2015-09-30 PL PL15777845T patent/PL3204377T3/pl unknown
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2017
- 2017-02-09 IL IL250543A patent/IL250543B/en active IP Right Grant
- 2017-02-16 ZA ZA2017/01175A patent/ZA201701175B/en unknown
- 2017-03-10 CO CONC2017/0002233A patent/CO2017002233A2/es unknown
- 2017-03-24 SV SV2017005411A patent/SV2017005411A/es unknown
- 2017-03-30 DO DO2017000090A patent/DOP2017000090A/es unknown
- 2017-03-30 CL CL2017000765A patent/CL2017000765A1/es unknown
- 2017-04-04 GT GT201700067A patent/GT201700067A/es unknown
- 2017-04-06 EC ECIEPI201721097A patent/ECSP17021097A/es unknown
- 2017-04-06 PH PH12017500635A patent/PH12017500635B1/en unknown
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2018
- 2018-10-30 HR HRP20181797TT patent/HRP20181797T1/hr unknown
- 2018-11-13 CY CY20181101193T patent/CY1120903T1/el unknown
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