BR112017005453A2 - compostos de aminopiridiloxipirazol - Google Patents
compostos de aminopiridiloxipirazolInfo
- Publication number
- BR112017005453A2 BR112017005453A2 BR112017005453A BR112017005453A BR112017005453A2 BR 112017005453 A2 BR112017005453 A2 BR 112017005453A2 BR 112017005453 A BR112017005453 A BR 112017005453A BR 112017005453 A BR112017005453 A BR 112017005453A BR 112017005453 A2 BR112017005453 A2 BR 112017005453A2
- Authority
- BR
- Brazil
- Prior art keywords
- cancer
- compounds
- aminopyridyloxypyrazole
- fibrosis
- tgfßr1
- Prior art date
Links
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
- C07D401/02—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
-
- 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
- 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
a presente invenção refere-se a compostos de aminopiridiloxipirazol que inibem a atividade do receptor 1 do fator de transformação do crescimento beta (tgfßr1), composições farmacêuticas compreendendo os compostos, e métodos de uso dos compostos para tratar câncer, preferivelmente câncer de cólon, melanoma, carcinoma hepatocelular, câncer renal, glioblastoma, câncer pancreático, síndrome mielodisplásica, câncer de pulmão, e câncer gástrico, e/ou fibrose, preferivelmente fibrose do fígado e doença renal crônica.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462060724P | 2014-10-07 | 2014-10-07 | |
| US62/060,724 | 2014-10-07 | ||
| PCT/US2015/053098 WO2016057278A1 (en) | 2014-10-07 | 2015-09-30 | Aminopyridyloxypyrazole compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| BR112017005453A2 true BR112017005453A2 (pt) | 2017-12-12 |
| BR112017005453A8 BR112017005453A8 (pt) | 2018-04-24 |
| BR112017005453B1 BR112017005453B1 (pt) | 2022-12-06 |
Family
ID=54266692
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112017005453-1A BR112017005453B1 (pt) | 2014-10-07 | 2015-09-30 | Compostos de aminopiridiloxipirazol, seus usos, e composição farmacêutica |
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 |
| 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 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA03010630A (es) | 2001-05-24 | 2004-03-09 | Lilly Co Eli | 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 |
| 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 |
| 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 TR TR2018/16415T patent/TR201816415T4/tr unknown
- 2015-09-30 LT LTEP15777845.7T patent/LT3204377T/lt unknown
- 2015-09-30 PL PL15777845T patent/PL3204377T3/pl unknown
- 2015-09-30 TN TN2017000046A patent/TN2017000046A1/en unknown
- 2015-09-30 PT PT15777845T patent/PT3204377T/pt unknown
- 2015-09-30 AU AU2015328553A patent/AU2015328553C1/en not_active Ceased
- 2015-09-30 JP JP2016526891A patent/JP6043894B2/ja active Active
- 2015-09-30 AP AP2017009836A patent/AP2017009836A0/en unknown
- 2015-09-30 EP EP15777845.7A patent/EP3204377B1/en active Active
- 2015-09-30 CA CA2961262A patent/CA2961262C/en active Active
- 2015-09-30 PE PE2017000536A patent/PE20170662A1/es unknown
- 2015-09-30 US US14/870,033 patent/US9617243B2/en active Active
- 2015-09-30 KR KR1020177009123A patent/KR101921847B1/ko active IP Right Grant
- 2015-09-30 CR CR20170072A patent/CR20170072A/es unknown
- 2015-09-30 MX MX2017004457A patent/MX367360B/es active IP Right Grant
- 2015-09-30 SG SG11201702481UA patent/SG11201702481UA/en unknown
- 2015-09-30 MY MYPI2017701190A patent/MY190541A/en unknown
- 2015-09-30 UA UAA201702921A patent/UA118807C2/uk unknown
- 2015-09-30 BR BR112017005453-1A patent/BR112017005453B1/pt active IP Right Grant
- 2015-09-30 SI SI201530417T patent/SI3204377T1/sl unknown
- 2015-09-30 ES ES15777845T patent/ES2700376T3/es active Active
- 2015-09-30 RS RS20181372A patent/RS58094B1/sr unknown
- 2015-09-30 CN CN201580054343.9A patent/CN106795139B/zh active Active
- 2015-09-30 DK DK15777845.7T patent/DK3204377T3/en active
- 2015-09-30 MA MA41038A patent/MA41038B1/fr unknown
- 2015-09-30 WO PCT/US2015/053098 patent/WO2016057278A1/en active Application Filing
- 2015-09-30 NZ NZ729800A patent/NZ729800A/en unknown
- 2015-09-30 EA EA201790476A patent/EA031830B1/ru not_active IP Right Cessation
-
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
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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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| B07D | Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette] | ||
| B07E | Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette] | ||
| B06U | Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette] | ||
| B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
| B350 | Update of information on the portal [chapter 15.35 patent gazette] | ||
| B06A | Patent application procedure suspended [chapter 6.1 patent gazette] | ||
| B09A | Decision: intention to grant [chapter 9.1 patent gazette] | ||
| B16A | Patent or certificate of addition of invention granted [chapter 16.1 patent gazette] |
Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 30/09/2015, OBSERVADAS AS CONDICOES LEGAIS |