CN108137597A - TGFβ受体拮抗剂 - Google Patents

TGFβ受体拮抗剂 Download PDF

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Publication number
CN108137597A
CN108137597A CN201680056221.8A CN201680056221A CN108137597A CN 108137597 A CN108137597 A CN 108137597A CN 201680056221 A CN201680056221 A CN 201680056221A CN 108137597 A CN108137597 A CN 108137597A
Authority
CN
China
Prior art keywords
alkyl
hydrogen
heteroatoms selected
ring containing
alkoxy
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.)
Pending
Application number
CN201680056221.8A
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English (en)
Chinese (zh)
Inventor
L·S·卡里克里斯南
B·E·芬克
R·M·博尔齐莱里
G·特奴库奴如
J·S·瓦里尔
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Bristol Myers Squibb Co
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of CN108137597A publication Critical patent/CN108137597A/zh
Pending legal-status Critical Current

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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

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  • 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)
CN201680056221.8A 2015-07-28 2016-07-27 TGFβ受体拮抗剂 Pending CN108137597A (zh)

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
CN108137597A true CN108137597A (zh) 2018-06-08

Family

ID=56609982

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201680056221.8A Pending CN108137597A (zh) 2015-07-28 2016-07-27 TGFβ受体拮抗剂

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=)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
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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WO2004081009A1 (en) * 2003-03-12 2004-09-23 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as tgf-beta inhibitors
WO2004087056A2 (en) * 2003-03-28 2004-10-14 Scios Inc. BI-CYCLIC PYRIMIDINE INHIBITORS OF TGFβ

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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

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004021979A2 (en) * 2002-09-06 2004-03-18 Smithkline Beecham Corporation PYRROLO[2, 3-d]PYRIMIDINE-4-YL AND PURIN-6-YL UREA COMPOUNDS
WO2004081009A1 (en) * 2003-03-12 2004-09-23 Millennium Pharmaceuticals, Inc. Quinazoline derivatives as tgf-beta inhibitors
WO2004087056A2 (en) * 2003-03-28 2004-10-14 Scios Inc. BI-CYCLIC PYRIMIDINE INHIBITORS OF TGFβ

Also Published As

Publication number Publication date
US10399987B2 (en) 2019-09-03
WO2017019757A1 (en) 2017-02-02
KR20180034548A (ko) 2018-04-04
EP3328861A1 (en) 2018-06-06
JP2018526344A (ja) 2018-09-13
US20180215762A1 (en) 2018-08-02

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Application publication date: 20180608