JO3336B1 - مركبات أمينو بيريديلوكسي بيرازول - Google Patents
مركبات أمينو بيريديلوكسي بيرازولInfo
- Publication number
- JO3336B1 JO3336B1 JOP/2015/0235A JOP20150235A JO3336B1 JO 3336 B1 JO3336 B1 JO 3336B1 JO P20150235 A JOP20150235 A JO P20150235A JO 3336 B1 JO3336 B1 JO 3336B1
- Authority
- JO
- Jordan
- Prior art keywords
- cancer
- compounds
- aminopyridyloxypyrazole
- fibrosis
- glioblastoma
- Prior art date
Links
- 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 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 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
- 102000009618 Transforming Growth Factors Human genes 0.000 abstract 1
- 108010009583 Transforming Growth Factors Proteins 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)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biomedical Technology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
يتعلق الاختراع الحالي بمركبات أمينو بيريديلوكسي بيرازول جديدة تثبط نشاط مستقبل بيتا لعامل النمو المتحول 1 (TGF?R1)، وتركيبات صيدلية تشتمل على المركبات، وطرق استخدام المركبات لعلاج السرطان، وبشكل مفضل، سرطان القولون، الميلانوما، كارسينوما الخلايا الكبدية، السرطان الكلوي، الورم الأرومي النخاعي، سرطان البنكرياس، متلازمة خلل التنسج النخاعي، سرطان الرئة، وسرطان معدي، و/أو التليف، وبشكل مفضل، تليف الكبد وداء الكلى المزمن.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462060724P | 2014-10-07 | 2014-10-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3336B1 true JO3336B1 (ar) | 2019-03-13 |
Family
ID=54266692
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2015/0235A JO3336B1 (ar) | 2014-10-07 | 2015-09-22 | مركبات أمينو بيريديلوكسي بيرازول |
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 |
| WO2015103355A1 (en) | 2014-01-01 | 2015-07-09 | Medivation Technologies, Inc. | Compounds and methods of use |
| 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 |
| 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 |
| 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 |
| 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 |
| EP3806958B1 (en) * | 2018-06-18 | 2022-09-07 | Janssen Pharmaceutica NV | 6-aminopyridin-3-yl pyrazoles as modulators of roryt |
| US12049475B2 (en) | 2018-07-23 | 2024-07-30 | Brise Pharmaceuticals Co., Ltd. | Bisphosphonate drug conjugates |
| MX2021000977A (es) | 2018-07-26 | 2021-04-12 | Sumitomo Pharma Oncology Inc | Metodos para tratar enfermedades asociadas con expresion anormal de receptor de activina a tipo 1 (acvr1) e inhibidores de acvr1 para uso en los mismos. |
| 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 |
| 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 |
| US12102626B2 (en) * | 2018-12-27 | 2024-10-01 | Nexys Therapeutics, Inc. | (Pyridin-2-yl)amine derivatives as TGF-BETA R1 (ALK5) inhibitors for the treatment of cancer |
| EP3908575A4 (en) * | 2019-01-10 | 2022-09-14 | Sumitomo Pharma Oncology, 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 |
| 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 |
| 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 |
| 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)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1397364E (pt) | 2001-05-24 | 2007-10-22 | Lilly Co Eli | Novos derivados de pirrole como agentes farmacêuticos |
| 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 |
| 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 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 RS RS20181372A patent/RS58094B1/sr unknown
- 2015-09-30 JP JP2016526891A patent/JP6043894B2/ja not_active Expired - Fee Related
- 2015-09-30 MX MX2017004457A patent/MX367360B/es active IP Right Grant
- 2015-09-30 DK DK15777845.7T patent/DK3204377T3/en active
- 2015-09-30 US US14/870,033 patent/US9617243B2/en not_active Expired - Fee Related
- 2015-09-30 KR KR1020177009123A patent/KR101921847B1/ko not_active Expired - Fee Related
- 2015-09-30 BR BR112017005453-1A patent/BR112017005453B1/pt not_active IP Right Cessation
- 2015-09-30 CA CA2961262A patent/CA2961262C/en active Active
- 2015-09-30 WO PCT/US2015/053098 patent/WO2016057278A1/en not_active Ceased
- 2015-09-30 LT LTEP15777845.7T patent/LT3204377T/lt unknown
- 2015-09-30 SI SI201530417T patent/SI3204377T1/sl unknown
- 2015-09-30 AU AU2015328553A patent/AU2015328553C1/en not_active Ceased
- 2015-09-30 CN CN201580054343.9A patent/CN106795139B/zh not_active Expired - Fee Related
- 2015-09-30 TR TR2018/16415T patent/TR201816415T4/tr unknown
- 2015-09-30 MA MA41038A patent/MA41038B1/fr unknown
- 2015-09-30 TN TN2017000046A patent/TN2017000046A1/en unknown
- 2015-09-30 ES ES15777845T patent/ES2700376T3/es active Active
- 2015-09-30 PE PE2017000536A patent/PE20170662A1/es unknown
- 2015-09-30 NZ NZ729800A patent/NZ729800A/en not_active IP Right Cessation
- 2015-09-30 AP AP2017009836A patent/AP2017009836A0/en unknown
- 2015-09-30 EA EA201790476A patent/EA031830B1/ru not_active IP Right Cessation
- 2015-09-30 PT PT15777845T patent/PT3204377T/pt unknown
- 2015-09-30 UA UAA201702921A patent/UA118807C2/uk unknown
- 2015-09-30 MY MYPI2017701190A patent/MY190541A/en unknown
- 2015-09-30 CR CR20170072A patent/CR20170072A/es unknown
- 2015-09-30 HR HRP20181797TT patent/HRP20181797T1/hr unknown
- 2015-09-30 SG SG11201702481UA patent/SG11201702481UA/en unknown
- 2015-09-30 EP EP15777845.7A patent/EP3204377B1/en active Active
- 2015-09-30 PL PL15777845T patent/PL3204377T3/pl unknown
-
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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