ECSP17021097A - Compuestos de aminopiridiloxipirazol - Google Patents
Compuestos de aminopiridiloxipirazolInfo
- Publication number
- ECSP17021097A ECSP17021097A ECIEPI201721097A ECPI201721097A ECSP17021097A EC SP17021097 A ECSP17021097 A EC SP17021097A EC IEPI201721097 A ECIEPI201721097 A EC IEPI201721097A EC PI201721097 A ECPI201721097 A EC PI201721097A EC SP17021097 A ECSP17021097 A EC SP17021097A
- Authority
- EC
- Ecuador
- Prior art keywords
- cancer
- compounds
- aminopyridyloxipyrazole
- fibrosis
- tgfβr1
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- ZXKYDXVZUAQZIQ-UHFFFAOYSA-N 5-pyridin-2-yloxy-1H-pyrazol-4-amine Chemical class NC=1C(=NNC=1)OC1=NC=CC=C1 ZXKYDXVZUAQZIQ-UHFFFAOYSA-N 0.000 abstract 1
- 206010009944 Colon cancer Diseases 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 101000712674 Homo sapiens TGF-beta receptor type-1 Proteins 0.000 abstract 1
- 208000008839 Kidney Neoplasms Diseases 0.000 abstract 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 abstract 1
- 201000003793 Myelodysplastic syndrome Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 abstract 1
- 206010038389 Renal cancer Diseases 0.000 abstract 1
- 208000005718 Stomach Neoplasms Diseases 0.000 abstract 1
- 102100033456 TGF-beta receptor type-1 Human genes 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000020832 chronic kidney disease Diseases 0.000 abstract 1
- 208000019425 cirrhosis of liver Diseases 0.000 abstract 1
- 208000029742 colonic neoplasm Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 206010017758 gastric cancer Diseases 0.000 abstract 1
- 208000005017 glioblastoma Diseases 0.000 abstract 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 abstract 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 abstract 1
- 201000010982 kidney cancer Diseases 0.000 abstract 1
- 201000005202 lung cancer Diseases 0.000 abstract 1
- 208000020816 lung neoplasm Diseases 0.000 abstract 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 abstract 1
- 201000001441 melanoma Diseases 0.000 abstract 1
- 201000002528 pancreatic cancer Diseases 0.000 abstract 1
- 208000008443 pancreatic carcinoma Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 201000011549 stomach cancer Diseases 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
-
- 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
- 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)
- 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
La presente invención se refiere a compuestos novedosos de aminopiridiloxipirazol que inhiben la actividad del receptor 1 del factor del crecimiento transformante beta (TGFβR1), 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 pulmón y cáncer gástrico y/o fibrosis, preferentemente fibrosis hepática y enfermedad renal crónica.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462060724P | 2014-10-07 | 2014-10-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP17021097A true ECSP17021097A (es) | 2018-02-28 |
Family
ID=54266692
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECIEPI201721097A ECSP17021097A (es) | 2014-10-07 | 2017-04-06 | Compuestos de aminopiridiloxipirazol |
Country Status (42)
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015089800A1 (en) | 2013-12-19 | 2015-06-25 | Eli Lilly And Company | Fluorophenyl pyrazol compounds |
| CA2935392C (en) | 2014-01-01 | 2022-07-26 | Medivation Technologies, Inc. | Amino pyridine derivatives for the treatment of conditions associated with excessive tgf.beta activity |
| WO2016066664A1 (en) * | 2014-10-31 | 2016-05-06 | F. Hoffmann-La Roche Ag | New pyridinyloxy- and phenyloxy-pyrazolyl compounds |
| CN109831907A (zh) * | 2016-09-30 | 2019-05-31 | 伊莱利利公司 | 2-{4-[(4-{[1-环丙基-3-四氢-2h-吡喃-4-基)-1h-吡唑-4-基]氧基}吡啶-2-基)氨基]吡啶-2-基}丙-2-醇治疗癌症的用途 |
| JOP20190080A1 (ar) | 2016-10-14 | 2019-04-11 | Bayer Pharma AG | مركبات مشتقة من 6-(1h-بيرازول-1-يل) بيريميدين-4- أمين مستبدل واستخداماتها |
| JP2020512400A (ja) * | 2017-03-23 | 2020-04-23 | クラヴィウス ファーマシューティカルズ，エルエルシー | ＴＧＦβの阻害のための三置換イミダゾールおよび治療方法 |
| 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 |
| WO2019244001A1 (en) * | 2018-06-18 | 2019-12-26 | Janssen Pharmaceutica Nv | 6-aminopyridin-3-yl pyrazoles as modulators of roryt |
| CN112867724B (zh) | 2018-07-23 | 2024-06-04 | 熙源安健医药(北京)有限公司 | 二膦酸盐药物缀合物 |
| WO2020023910A1 (en) | 2018-07-26 | 2020-01-30 | Tolero Pharmaceuticals, 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 |
| US20210395235A1 (en) * | 2018-10-18 | 2021-12-23 | Nanjing Sanhome Pharmaceutical Co., Ltd. | COMPOUND AS TGF-beta R1 INHIBITOR AND APPLICATION THEREOF |
| 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 |
| CA3117838A1 (en) | 2018-12-27 | 2020-07-02 | Nexys Therapeutics, Inc. | (pyridin-2-yl)amine derivatives as tgf-beta r1 (alk5) inhibitors for the treatment of cancer |
| JP2022517951A (ja) * | 2019-01-10 | 2022-03-11 | スミトモ ダイニッポン ファーマ オンコロジー， インコーポレイテッド | 骨髄異形成症候群を処置するためのａｌｋ５阻害剤 |
| KR102740196B1 (ko) | 2019-01-24 | 2024-12-10 | 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 |
| 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 |
| CN119330934B (zh) * | 2023-07-21 | 2025-12-05 | 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 |
| WO2025063820A1 (ko) * | 2023-09-21 | 2025-03-27 | 오토텔릭바이오 주식회사 | 티아졸 유도체 화합물을 포함하는 폐섬유화증 치료용 조성물 |
| WO2025063819A1 (ko) * | 2023-09-21 | 2025-03-27 | 오토텔릭바이오 주식회사 | 티아졸 유도체 화합물을 포함하는 장섬유화증 치료용 조성물 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2289116T3 (es) | 2001-05-24 | 2008-02-01 | Eli Lilly And Company | Nuevos derivados de pirrol como agentes farmaceuticos. |
| 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 |
| UY31281A1 (es) * | 2007-08-13 | 2009-03-31 | Aminas, benzamidas y sulfonamidas {[4-(5,6-dimetil-2-piridin-2-il-piridin-3-il) oxipiridin-2-il]amino} sustituidas, sus sales farmacéuticamente aceptables, composiciones contenniéndolas y aplicaciones. | |
| 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 |
| TW201329067A (zh) * | 2011-12-08 | 2013-07-16 | Amgen Inc | 作為ｇｋａ活化劑之脲化合物 |
| WO2015089800A1 (en) | 2013-12-19 | 2015-06-25 | Eli Lilly And Company | Fluorophenyl pyrazol compounds |
-
2015
- 2015-09-22 TW TW104131319A patent/TWI582083B/zh not_active IP Right Cessation
- 2015-09-22 JO JOP/2015/0235A patent/JO3336B1/ar active
- 2015-09-23 AR ARP150103058A patent/AR102003A1/es unknown
- 2015-09-30 SI SI201530417T patent/SI3204377T1/sl unknown
- 2015-09-30 CN CN201580054343.9A patent/CN106795139B/zh not_active Expired - Fee Related
- 2015-09-30 US US14/870,033 patent/US9617243B2/en not_active Expired - Fee Related
- 2015-09-30 MX MX2017004457A patent/MX367360B/es active IP Right Grant
- 2015-09-30 MA MA41038A patent/MA41038B1/fr unknown
- 2015-09-30 EP EP15777845.7A patent/EP3204377B1/en active Active
- 2015-09-30 SG SG11201702481UA patent/SG11201702481UA/en unknown
- 2015-09-30 MY MYPI2017701190A patent/MY190541A/en unknown
- 2015-09-30 DK DK15777845.7T patent/DK3204377T3/en active
- 2015-09-30 PE PE2017000536A patent/PE20170662A1/es unknown
- 2015-09-30 BR BR112017005453-1A patent/BR112017005453B1/pt not_active IP Right Cessation
- 2015-09-30 UA UAA201702921A patent/UA118807C2/uk unknown
- 2015-09-30 LT LTEP15777845.7T patent/LT3204377T/lt unknown
- 2015-09-30 TN TN2017000046A patent/TN2017000046A1/en unknown
- 2015-09-30 JP JP2016526891A patent/JP6043894B2/ja not_active Expired - Fee Related
- 2015-09-30 NZ NZ729800A patent/NZ729800A/en not_active IP Right Cessation
- 2015-09-30 ES ES15777845T patent/ES2700376T3/es active Active
- 2015-09-30 CA CA2961262A patent/CA2961262C/en active Active
- 2015-09-30 RS RS20181372A patent/RS58094B1/sr unknown
- 2015-09-30 TR TR2018/16415T patent/TR201816415T4/tr unknown
- 2015-09-30 PT PT15777845T patent/PT3204377T/pt unknown
- 2015-09-30 WO PCT/US2015/053098 patent/WO2016057278A1/en not_active Ceased
- 2015-09-30 EA EA201790476A patent/EA031830B1/ru not_active IP Right Cessation
- 2015-09-30 CR CR20170072A patent/CR20170072A/es unknown
- 2015-09-30 PL PL15777845T patent/PL3204377T3/pl unknown
- 2015-09-30 AU AU2015328553A patent/AU2015328553C1/en not_active Ceased
- 2015-09-30 HR HRP20181797TT patent/HRP20181797T1/hr unknown
- 2015-09-30 AP AP2017009836A patent/AP2017009836A0/en unknown
- 2015-09-30 KR KR1020177009123A patent/KR101921847B1/ko not_active Expired - Fee Related
-
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 CL CL2017000765A patent/CL2017000765A1/es unknown
- 2017-03-30 DO DO2017000090A patent/DOP2017000090A/es unknown
- 2017-04-04 GT GT201700067A patent/GT201700067A/es unknown
- 2017-04-06 PH PH12017500635A patent/PH12017500635B1/en unknown
- 2017-04-06 EC ECIEPI201721097A patent/ECSP17021097A/es unknown
-
2018
- 2018-11-13 CY CY20181101193T patent/CY1120903T1/el unknown
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