KR20180032611A - Tgf 베타 수용체 길항제 - Google Patents
Tgf 베타 수용체 길항제 Download PDFInfo
- Publication number
- KR20180032611A KR20180032611A KR1020187004934A KR20187004934A KR20180032611A KR 20180032611 A KR20180032611 A KR 20180032611A KR 1020187004934 A KR1020187004934 A KR 1020187004934A KR 20187004934 A KR20187004934 A KR 20187004934A KR 20180032611 A KR20180032611 A KR 20180032611A
- Authority
- KR
- South Korea
- Prior art keywords
- pyrrolo
- pyridin
- amino
- triazin
- amine
- Prior art date
- Legal status (The legal status 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 status listed.)
- Ceased
Links
- 0 CCP*(P(c1ccccc1)(c1ccccc1)c1ccccc1)=CC Chemical compound CCP*(P(c1ccccc1)(c1ccccc1)c1ccccc1)=CC 0.000 description 21
- BMGCIYPWZVRMRW-UHFFFAOYSA-N CC(C)(C)OC(Nc(cc(nc1)Cl)c1F)=O Chemical compound CC(C)(C)OC(Nc(cc(nc1)Cl)c1F)=O BMGCIYPWZVRMRW-UHFFFAOYSA-N 0.000 description 1
- KWLOIDOKWUESNM-UHFFFAOYSA-N CC1(C)OB(c2n[nH]cc2)OC1(C)C Chemical compound CC1(C)OB(c2n[nH]cc2)OC1(C)C KWLOIDOKWUESNM-UHFFFAOYSA-N 0.000 description 1
- VYWCRVNLPOVYJH-UHFFFAOYSA-N CC1(C)OB(c2nc(OC)ccc2)OC1(C)C Chemical compound CC1(C)OB(c2nc(OC)ccc2)OC1(C)C VYWCRVNLPOVYJH-UHFFFAOYSA-N 0.000 description 1
- MUTMWVFVVJDTOE-UHFFFAOYSA-N CC1=CC=CC(c(nc2Nc(ccnc3)c3Cl)n[n]3c2ccc3)=C[IH]1 Chemical compound CC1=CC=CC(c(nc2Nc(ccnc3)c3Cl)n[n]3c2ccc3)=C[IH]1 MUTMWVFVVJDTOE-UHFFFAOYSA-N 0.000 description 1
- JWSUIGWPCWRVBT-UHFFFAOYSA-N CCOC(C1=C2C(Oc3ccccc3)=NC(Cl)=NC(C)C2CC=C1)=O Chemical compound CCOC(C1=C2C(Oc3ccccc3)=NC(Cl)=NC(C)C2CC=C1)=O JWSUIGWPCWRVBT-UHFFFAOYSA-N 0.000 description 1
- UPTMIXQQEKBKKK-UHFFFAOYSA-N CCc1c(C)c(F)ccc1C Chemical compound CCc1c(C)c(F)ccc1C UPTMIXQQEKBKKK-UHFFFAOYSA-N 0.000 description 1
- GBZKXUCZHRYTNP-UHFFFAOYSA-N CCc1nc(C(N=C2Nc(ccnc3)c3F)=NC(C)C3C2=CC(C=C)=CC3)ccc1 Chemical compound CCc1nc(C(N=C2Nc(ccnc3)c3F)=NC(C)C3C2=CC(C=C)=CC3)ccc1 GBZKXUCZHRYTNP-UHFFFAOYSA-N 0.000 description 1
- PYYYHARFWAZDEA-UHFFFAOYSA-N CN(C)CCCCOc(cncc1)c1N Chemical compound CN(C)CCCCOc(cncc1)c1N PYYYHARFWAZDEA-UHFFFAOYSA-N 0.000 description 1
- BRZNAATZQZPGBQ-UHFFFAOYSA-N COC(c1cc([N+]([O-])=O)c[nH]1)=O Chemical compound COC(c1cc([N+]([O-])=O)c[nH]1)=O BRZNAATZQZPGBQ-UHFFFAOYSA-N 0.000 description 1
- RCEOLIZDOQWYMQ-UHFFFAOYSA-N COc1nc(C(N=C2Nc3ccncc3)=NC(CCC=C3)C2=C3Cl)ccc1 Chemical compound COc1nc(C(N=C2Nc3ccncc3)=NC(CCC=C3)C2=C3Cl)ccc1 RCEOLIZDOQWYMQ-UHFFFAOYSA-N 0.000 description 1
- VVABXULUCBLYRJ-UHFFFAOYSA-N Cc1c[s]c(C(N=C2Nc3ccncc3)=NC3C2=CC=CCC3)n1 Chemical compound Cc1c[s]c(C(N=C2Nc3ccncc3)=NC3C2=CC=CCC3)n1 VVABXULUCBLYRJ-UHFFFAOYSA-N 0.000 description 1
- CWJIRGBBVBLEAT-UHFFFAOYSA-N Cc1nc(-c(nc2Nc3cc(N)ncc3)n[n]3c2ccc3)ccc1F Chemical compound Cc1nc(-c(nc2Nc3cc(N)ncc3)n[n]3c2ccc3)ccc1F CWJIRGBBVBLEAT-UHFFFAOYSA-N 0.000 description 1
- RXAXXPSLZPTWET-UHFFFAOYSA-N Cc1nc(-c(nc2Nc3cc(NC(C4CC4)=O)ncc3)n[n]3c2ccc3)ccc1F Chemical compound Cc1nc(-c(nc2Nc3cc(NC(C4CC4)=O)ncc3)n[n]3c2ccc3)ccc1F RXAXXPSLZPTWET-UHFFFAOYSA-N 0.000 description 1
- KJBKPRMEMJKXDV-UHFFFAOYSA-N Nc(ccnc1)c1Cl Chemical compound Nc(ccnc1)c1Cl KJBKPRMEMJKXDV-UHFFFAOYSA-N 0.000 description 1
- BLBDTBCGPHPIJK-UHFFFAOYSA-N Nc1cc(Cl)ncc1 Chemical compound Nc1cc(Cl)ncc1 BLBDTBCGPHPIJK-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562195854P | 2015-07-23 | 2015-07-23 | |
| US62/195,854 | 2015-07-23 | ||
| PCT/US2016/043252 WO2017015425A1 (en) | 2015-07-23 | 2016-07-21 | Tgf beta receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20180032611A true KR20180032611A (ko) | 2018-03-30 |
Family
ID=56609944
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187004934A Ceased KR20180032611A (ko) | 2015-07-23 | 2016-07-21 | Tgf 베타 수용체 길항제 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10336761B2 (https=) |
| EP (1) | EP3325484A1 (https=) |
| JP (1) | JP2018520201A (https=) |
| KR (1) | KR20180032611A (https=) |
| CN (1) | CN108026105B (https=) |
| WO (1) | WO2017015425A1 (https=) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7114076B2 (ja) | 2015-12-22 | 2022-08-08 | シャイ・セラピューティクス・エルエルシー | がん及び炎症性疾患の処置のための化合物 |
| JP7514005B2 (ja) | 2017-06-21 | 2024-07-10 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物 |
| CN111655260A (zh) * | 2017-10-26 | 2020-09-11 | 南方研究院 | 作为TGF-β抑制剂的噁二唑和噻二唑 |
| JP7407461B2 (ja) | 2018-12-19 | 2024-01-04 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ｒａｓ病、及び線維性疾患の処置のためのｒａｓスーパーファミリーと相互作用する化合物 |
| 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 |
| CN111825675B (zh) * | 2019-04-15 | 2023-08-01 | 武汉朗来科技发展有限公司 | Rock抑制剂及其制备方法和用途 |
| 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 |
| WO2021147699A1 (zh) * | 2020-01-21 | 2021-07-29 | 四川科伦博泰生物医药股份有限公司 | 吡啶并杂环类化合物、其制备方法及用途 |
| CN113620956B (zh) * | 2020-05-06 | 2023-06-13 | 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 |
| AU2023249795A1 (en) * | 2022-04-08 | 2024-10-17 | Shy Therapeutics, Llc | Compounds that interact with ras superfamily proteins for treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| US20260028365A1 (en) * | 2022-07-14 | 2026-01-29 | Biogen Ma Inc. | Tyrosine kinase 2 inhibitors and uses thereof |
| EP4651950A1 (en) * | 2023-01-19 | 2025-11-26 | Skyhawk Therapeutics, Inc. | Compositions useful for modulating splicing |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2497444C (en) * | 2002-09-04 | 2010-11-30 | Schering Corporation | Pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| WO2004065392A1 (en) * | 2003-01-24 | 2004-08-05 | Smithkline Beecham Corporation | Condensed pyridines and pyrimidines and their use as alk-5 receptor ligands |
| JP2006521398A (ja) * | 2003-03-28 | 2006-09-21 | サイオス・インコーポレーテツド | ＴＧＦβの二−環式ピリミジン阻害剤 |
| MX2013010163A (es) * | 2011-03-09 | 2013-10-30 | Merck Patent Gmbh | Derivados de pirido[2,3-b] pirazina y sus usos terapeuticos. |
| CN103450204B (zh) * | 2012-05-31 | 2016-08-17 | 中国科学院上海药物研究所 | 吡咯[2，1-f][1，2，4]并三嗪类化合物，其制备方法及用途 |
-
2016
- 2016-07-21 KR KR1020187004934A patent/KR20180032611A/ko not_active Ceased
- 2016-07-21 US US15/746,597 patent/US10336761B2/en active Active
- 2016-07-21 JP JP2018503142A patent/JP2018520201A/ja active Pending
- 2016-07-21 EP EP16747941.9A patent/EP3325484A1/en not_active Withdrawn
- 2016-07-21 CN CN201680055202.3A patent/CN108026105B/zh active Active
- 2016-07-21 WO PCT/US2016/043252 patent/WO2017015425A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| JP2018520201A (ja) | 2018-07-26 |
| EP3325484A1 (en) | 2018-05-30 |
| US10336761B2 (en) | 2019-07-02 |
| US20180215761A1 (en) | 2018-08-02 |
| CN108026105B (zh) | 2020-10-16 |
| CN108026105A (zh) | 2018-05-11 |
| WO2017015425A1 (en) | 2017-01-26 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20180220 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| A201 | Request for examination | ||
| PA0201 | Request for examination |
Patent event code: PA02012R01D Patent event date: 20210721 Comment text: Request for Examination of Application |
|
| E902 | Notification of reason for refusal | ||
| PE0902 | Notice of grounds for rejection |
Comment text: Notification of reason for refusal Patent event date: 20230725 Patent event code: PE09021S01D |
|
| E601 | Decision to refuse application | ||
| PE0601 | Decision on rejection of patent |
Patent event date: 20231006 Comment text: Decision to Refuse Application Patent event code: PE06012S01D Patent event date: 20230725 Comment text: Notification of reason for refusal Patent event code: PE06011S01I |