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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- 230000007017 scission Effects 0.000 description 1
- 238000007493 shaping process Methods 0.000 description 1
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- 229910001923 silver oxide Inorganic materials 0.000 description 1
- 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
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
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- 235000010265 sodium sulphite Nutrition 0.000 description 1
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- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000003549 soybean oil Substances 0.000 description 1
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- 150000003413 spiro compounds Chemical class 0.000 description 1
- 125000003638 stannyl group Chemical group [H][Sn]([H])([H])* 0.000 description 1
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- 229940124530 sulfonamide Drugs 0.000 description 1
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- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 description 1
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- 150000003462 sulfoxides Chemical class 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
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- 238000013268 sustained release Methods 0.000 description 1
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- 230000002195 synergetic effect Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 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
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
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- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
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- 125000005309 thioalkoxy group Chemical group 0.000 description 1
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- 208000030901 thyroid gland follicular carcinoma Diseases 0.000 description 1
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- 231100000331 toxic Toxicity 0.000 description 1
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- 231100000419 toxicity Toxicity 0.000 description 1
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- 230000002103 transcriptional effect Effects 0.000 description 1
- 125000004306 triazinyl group Chemical group 0.000 description 1
- 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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- 230000004614 tumor growth Effects 0.000 description 1
- 102000003298 tumor necrosis factor receptor Human genes 0.000 description 1
- 230000005751 tumor progression Effects 0.000 description 1
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- 206010046766 uterine cancer Diseases 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 235000019871 vegetable fat Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
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- 235000004835 α-tocopherol Nutrition 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
- A61K31/495—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
ID=56609982
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 (https=) |
| EP (1) | EP3328861A1 (https=) |
| JP (1) | JP2018526344A (https=) |
| KR (1) | KR20180034548A (https=) |
| CN (1) | CN108137597A (https=) |
| WO (1) | WO2017019757A1 (https=) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| US7223766B2 (en) * | 2003-03-28 | 2007-05-29 | Scios, Inc. | Bi-cyclic pyrimidine inhibitors of TGFβ |
| TWI380996B (zh) | 2004-09-17 | 2013-01-01 | Hoffmann La Roche | 抗ｏｘ４０ｌ抗體 |
| PT2343320T (pt) | 2005-03-25 | 2018-01-23 | Gitr Inc | Anticorpos anti-gitr e as suas utilizações |
| PL1879573T3 (pl) | 2005-05-10 | 2013-05-31 | Incyte Holdings Corp | Modulatory 2,3-dioksygenazy indoloaminy i sposoby ich zastosowania |
| PT1907424E (pt) | 2005-07-01 | 2015-10-09 | Squibb & Sons Llc | Anticorpos monoclonais humanos para o ligando 1 de morte programada (pd-l1) |
| US8450351B2 (en) | 2005-12-20 | 2013-05-28 | Incyte Corporation | N-hydroxyamidinoheterocycles as modulators of indoleamine 2,3-dioxygenase |
| WO2008036642A2 (en) | 2006-09-19 | 2008-03-27 | 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 |
| US8591886B2 (en) | 2007-07-12 | 2013-11-26 | Gitr, Inc. | Combination therapies employing GITR binding molecules |
| EP2044949A1 (en) | 2007-10-05 | 2009-04-08 | Immutep | Use of recombinant lag-3 or the derivatives thereof for eliciting monocyte immune response |
| US10047066B2 (en) | 2007-11-30 | 2018-08-14 | Newlink Genetics Corporation | 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 |
| EP3255060A1 (en) | 2008-12-09 | 2017-12-13 | F. Hoffmann-La Roche AG | Anti-pd-l1 antibodies and their use to enhance t-cell function |
| KR101790802B1 (ko) | 2009-09-03 | 2017-10-27 | 머크 샤프 앤드 돔 코포레이션 | 항-ｇｉｔｒ 항체 |
| EP2493862B1 (en) | 2009-10-28 | 2016-10-05 | Newlink Genetics Corporation | Imidazole derivatives as ido inhibitors |
| ES2722300T3 (es) | 2009-12-10 | 2019-08-09 | Hoffmann La Roche | Anticuerpos que se unen preferentemente al dominio extracelular 4 de CSF1R y su uso |
| EP2542256B1 (en) | 2010-03-04 | 2019-05-22 | MacroGenics, Inc. | Antibodies reactive with b7-h3, immunologically active fragments thereof and uses thereof |
| US9169323B2 (en) | 2010-03-05 | 2015-10-27 | Hoffmann-La Roche Inc. | Antibodies against human CSF-1R |
| JP5989547B2 (ja) | 2010-03-05 | 2016-09-07 | エフ・ホフマン−ラ・ロシュ・アクチェンゲゼルシャフト | ヒトｃｓｆ−１ｒに対する抗体及びその使用 |
| HRP20190047T1 (hr) | 2010-05-04 | 2019-02-22 | Five Prime Therapeutics, Inc. | Protutijela koja se vežu na csf1r |
| MX337040B (es) | 2010-09-09 | 2016-02-09 | Pfizer | Moleculas de union a 4-1bb. |
| NO2694640T3 (https=) | 2011-04-15 | 2018-03-17 | ||
| JP6072771B2 (ja) | 2011-04-20 | 2017-02-01 | メディミューン，エルエルシー | Ｂ７−ｈ１およびｐｄ−１に結合する抗体およびその他の分子 |
| KR101764096B1 (ko) | 2011-11-28 | 2017-08-02 | 메르크 파텐트 게엠베하 | 항-ｐｄ-ｌ1 항체 및 그의 용도 |
| RU2658603C2 (ru) | 2011-12-15 | 2018-06-21 | Ф.Хоффманн-Ля Рош Аг | Антитела против человеческого csf-1r и их применения |
| KR20140127855A (ko) | 2012-02-06 | 2014-11-04 | 제넨테크, 인크. | Csf1r 억제제를 사용하는 조성물 및 방법 |
| 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 |
| RU2670743C9 (ru) | 2012-05-11 | 2018-12-19 | Файв Прайм Терапьютикс, Инк. | Способы лечения состояний антителами, которые связывают рецептор колониестимулирующего фактора 1 (csf1r) |
| UY34887A (es) | 2012-07-02 | 2013-12-31 | Bristol Myers Squibb Company Una Corporacion Del Estado De Delaware | Optimización de anticuerpos que se fijan al gen de activación 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 KR KR1020187005403A patent/KR20180034548A/ko 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 EP EP16747979.9A patent/EP3328861A1/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| CN108137597A (zh) | 2018-06-08 |
| US10399987B2 (en) | 2019-09-03 |
| WO2017019757A1 (en) | 2017-02-02 |
| EP3328861A1 (en) | 2018-06-06 |
| JP2018526344A (ja) | 2018-09-13 |
| US20180215762A1 (en) | 2018-08-02 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| PA0105 | International application |
Patent event date: 20180223 Patent event code: PA01051R01D Comment text: International Patent Application |
|
| PG1501 | Laying open of application | ||
| PC1203 | Withdrawal of no request for examination |