KR20180034548A - Tgf 베타 수용체 길항제 - Google Patents
Tgf 베타 수용체 길항제 Download PDFInfo
- Publication number
- KR20180034548A KR20180034548A KR1020187005403A KR20187005403A KR20180034548A KR 20180034548 A KR20180034548 A KR 20180034548A KR 1020187005403 A KR1020187005403 A KR 1020187005403A KR 20187005403 A KR20187005403 A KR 20187005403A KR 20180034548 A KR20180034548 A KR 20180034548A
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- South Korea
- Prior art keywords
- alkyl
- hydrogen
- heterocyclic ring
- heteroatoms selected
- membered heterocyclic
- 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.)
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- 201000000849 skin cancer Diseases 0.000 description 1
- 229940126586 small molecule drug Drugs 0.000 description 1
- WBHQBSYUUJJSRZ-UHFFFAOYSA-M sodium bisulfate Chemical compound [Na+].OS([O-])(=O)=O WBHQBSYUUJJSRZ-UHFFFAOYSA-M 0.000 description 1
- 229910000342 sodium bisulfate Inorganic materials 0.000 description 1
- 229940100996 sodium bisulfate Drugs 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
- BEOOHQFXGBMRKU-UHFFFAOYSA-N sodium cyanoborohydride Chemical compound [Na+].[B-]C#N BEOOHQFXGBMRKU-UHFFFAOYSA-N 0.000 description 1
- HRZFUMHJMZEROT-UHFFFAOYSA-L sodium disulfite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])(=O)=O HRZFUMHJMZEROT-UHFFFAOYSA-L 0.000 description 1
- 229940001584 sodium metabisulfite Drugs 0.000 description 1
- 235000010262 sodium metabisulphite Nutrition 0.000 description 1
- RYYKJJJTJZKILX-UHFFFAOYSA-M sodium octadecanoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCC([O-])=O RYYKJJJTJZKILX-UHFFFAOYSA-M 0.000 description 1
- NESLWCLHZZISNB-UHFFFAOYSA-M sodium phenolate Chemical compound [Na+].[O-]C1=CC=CC=C1 NESLWCLHZZISNB-UHFFFAOYSA-M 0.000 description 1
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- 229940075582 sorbic acid Drugs 0.000 description 1
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- 125000003638 stannyl group Chemical group [H][Sn]([H])([H])* 0.000 description 1
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- 201000000596 systemic lupus erythematosus Diseases 0.000 description 1
- 230000008685 targeting Effects 0.000 description 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 230000002381 testicular Effects 0.000 description 1
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- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
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- 125000001425 triazolyl group Chemical group 0.000 description 1
- USKQYZHWJZDNCM-UHFFFAOYSA-N tributyl-(6-methylpyridin-2-yl)stannane Chemical compound CCCC[Sn](CCCC)(CCCC)C1=CC=CC(C)=N1 USKQYZHWJZDNCM-UHFFFAOYSA-N 0.000 description 1
- 125000003866 trichloromethyl group Chemical group ClC(Cl)(Cl)* 0.000 description 1
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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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic 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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562197667P | 2015-07-28 | 2015-07-28 | |
| US62/197,667 | 2015-07-28 | ||
| PCT/US2016/044233 WO2017019757A1 (en) | 2015-07-28 | 2016-07-27 | Tgf beta receptor antagonists |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20180034548A true KR20180034548A (ko) | 2018-04-04 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020187005403A Withdrawn KR20180034548A (ko) | 2015-07-28 | 2016-07-27 | Tgf 베타 수용체 길항제 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10399987B2 (enExample) |
| EP (1) | EP3328861A1 (enExample) |
| JP (1) | JP2018526344A (enExample) |
| KR (1) | KR20180034548A (enExample) |
| CN (1) | CN108137597A (enExample) |
| WO (1) | WO2017019757A1 (enExample) |
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| CN111825674A (zh) * | 2019-04-22 | 2020-10-27 | 上海仕谱生物科技有限公司 | 嘧啶并五元杂环类化合物及其作为突变型idh2抑制剂的用途 |
| CN116621843B (zh) * | 2022-06-13 | 2024-05-24 | 四川大学华西医院 | 一种dna甲基转移酶1抑制剂及其制备方法和用途 |
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| WO2004021979A2 (en) * | 2002-09-06 | 2004-03-18 | Smithkline Beecham Corporation | PYRROLO[2, 3-d]PYRIMIDINE-4-YL AND PURIN-6-YL UREA COMPOUNDS |
| DE602004014347D1 (de) * | 2003-03-12 | 2008-07-24 | Millennium Pharm Inc | Chinazolin-derivate als tgf-beta-inhibitoren |
| EP1608631A4 (en) * | 2003-03-28 | 2008-08-20 | Scios Inc | BICYCLIC PYRIMIDININHIBITORS OF TGF BETA |
| TWI309240B (en) | 2004-09-17 | 2009-05-01 | Hoffmann La Roche | Anti-ox40l antibodies |
| JP5238936B2 (ja) | 2005-03-25 | 2013-07-17 | ジーアイティーアール，インク． | Ｇｉｔｒ結合分子およびその使用 |
| DK1879573T3 (da) | 2005-05-10 | 2013-02-25 | Incyte Corp | Modulatorer af indolamin 2,3-dioxygenase og fremgangsmåder til anvendelse deraf |
| KR101704734B1 (ko) | 2005-07-01 | 2017-02-09 | 이. 알. 스퀴부 앤드 선즈, 엘.엘.씨. | 예정 사멸 리간드 1 (피디-엘1)에 대한 인간 모노클로날 항체 |
| ES2540561T3 (es) | 2005-12-20 | 2015-07-10 | Incyte Corporation | N-hidroxiamidinoheterociclos como moduladores de indolamina 2,3-dioxigenasa |
| CA2663057C (en) | 2006-09-19 | 2015-12-08 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| CL2007002650A1 (es) | 2006-09-19 | 2008-02-08 | Incyte Corp | Compuestos derivados de heterociclo n-hidroxiamino; composicion farmaceutica, util para tratar cancer, infecciones virales y desordenes neurodegenerativos entre otras. |
| EP1987839A1 (en) | 2007-04-30 | 2008-11-05 | I.N.S.E.R.M. Institut National de la Sante et de la Recherche Medicale | Cytotoxic anti-LAG-3 monoclonal antibody and its use in the treatment or prevention of organ transplant rejection and autoimmune disease |
| PT2175884T (pt) | 2007-07-12 | 2016-09-21 | Gitr Inc | Terapias de combinação empregando moléculas de ligação a gitr |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| WO2009073620A2 (en) | 2007-11-30 | 2009-06-11 | Newlink Genetics | Ido inhibitors |
| FR2927330B1 (fr) | 2008-02-07 | 2010-02-19 | Sanofi Aventis | Derives de 5,6-bisaryl-2-pyridine-carboxamide, leur preparation et leur application en therapeutique comme antagonistes des recepteurs a l'urotensine ii |
| AR072999A1 (es) | 2008-08-11 | 2010-10-06 | Medarex Inc | Anticuerpos humanos que se unen al gen 3 de activacion linfocitaria (lag-3) y los usos de estos |
| MX356367B (es) | 2008-12-09 | 2018-05-25 | Genentech Inc | Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t. |
| IN2015DN02826A (enExample) | 2009-09-03 | 2015-09-11 | Merck Sharp & Dohme | |
| EP2493862B1 (en) | 2009-10-28 | 2016-10-05 | Newlink Genetics Corporation | Imidazole derivatives as ido inhibitors |
| DK2510010T3 (en) | 2009-12-10 | 2015-12-14 | Hoffmann La Roche | Antibodies that bind to human CSF1R extracellular domain 4 and their use |
| DK2542256T3 (da) | 2010-03-04 | 2019-08-26 | Macrogenics Inc | Antistoffer reagerende med b7-h3, immunologisk aktive fragmenter deraf og anvendelser deraf |
| CN102918061B (zh) | 2010-03-05 | 2016-06-08 | 霍夫曼-拉罗奇有限公司 | 针对人csf-1r的抗体及其用途 |
| RU2617971C2 (ru) | 2010-03-05 | 2017-04-28 | Ф.Хоффманн-Ля Рош Аг | Антитела против csf-1r человека и их применение |
| EP3943154A1 (en) | 2010-05-04 | 2022-01-26 | Five Prime Therapeutics, Inc. | Antibodies that bind csf1r |
| NZ729044A (en) | 2010-09-09 | 2020-07-31 | Pfizer | 4-1bb binding molecules |
| NO2694640T3 (enExample) | 2011-04-15 | 2018-03-17 | ||
| CA2833636A1 (en) | 2011-04-20 | 2012-10-26 | Amplimmune, Inc. | Antibodies and other molecules that bind b7-h1 and pd-1 |
| BR112014012819B1 (pt) | 2011-11-28 | 2022-08-16 | Merck Patent Gmbh | Anticorpo anti-pd-l1 ou fragmento de ligação ao antígeno do mesmo e composição |
| MX356337B (es) | 2011-12-15 | 2018-05-23 | Hoffmann La Roche | Anticuerpos contra csf-1r humano y sus usos. |
| MX2014008961A (es) | 2012-02-06 | 2014-10-14 | Genentech Inc | Composiciones y metodos para utilizar inhibidores de csf1r. |
| AR090263A1 (es) | 2012-03-08 | 2014-10-29 | Hoffmann La Roche | Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma |
| KR20150018533A (ko) | 2012-05-11 | 2015-02-23 | 파이브 프라임 테라퓨틱스, 인크. | 콜로니 자극 인자 1 수용체(csf1r)에 결속하는 항체들에 의한 질병 상태의 치료 방법 |
| AR091649A1 (es) | 2012-07-02 | 2015-02-18 | Bristol Myers Squibb Co | Optimizacion de anticuerpos que se fijan al gen de activacion de linfocitos 3 (lag-3) y sus usos |
| CN107759690A (zh) | 2012-08-31 | 2018-03-06 | 戊瑞治疗有限公司 | 用结合群落刺激因子1受体(csf1r)的抗体治疗病状的方法 |
-
2016
- 2016-07-27 US US15/747,843 patent/US10399987B2/en active Active
- 2016-07-27 EP EP16747979.9A patent/EP3328861A1/en not_active Withdrawn
- 2016-07-27 CN CN201680056221.8A patent/CN108137597A/zh active Pending
- 2016-07-27 WO PCT/US2016/044233 patent/WO2017019757A1/en not_active Ceased
- 2016-07-27 JP JP2018504171A patent/JP2018526344A/ja not_active Withdrawn
- 2016-07-27 KR KR1020187005403A patent/KR20180034548A/ko not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| US10399987B2 (en) | 2019-09-03 |
| CN108137597A (zh) | 2018-06-08 |
| US20180215762A1 (en) | 2018-08-02 |
| EP3328861A1 (en) | 2018-06-06 |
| JP2018526344A (ja) | 2018-09-13 |
| WO2017019757A1 (en) | 2017-02-02 |
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Legal Events
| Date | Code | Title | Description |
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| PA0105 | International application |
Patent event date: 20180223 Patent event code: PA01051R01D Comment text: International Patent Application |
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| PG1501 | Laying open of application | ||
| PC1203 | Withdrawal of no request for examination |