KR101937495B1 - Ｊａｋ 경로의 억제를 위한 조성물 및 방법 - Google Patents

Ｊａｋ 경로의 억제를 위한 조성물 및 방법 Download PDF

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Publication number
KR101937495B1
KR101937495B1 KR1020137004970A KR20137004970A KR101937495B1 KR 101937495 B1 KR101937495 B1 KR 101937495B1 KR 1020137004970 A KR1020137004970 A KR 1020137004970A KR 20137004970 A KR20137004970 A KR 20137004970A KR 101937495 B1 KR101937495 B1 KR 101937495B1
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South Korea
Prior art keywords
ylamino
methyl
benzo
pyrimidin
fluoro
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Expired - Fee Related
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KR1020137004970A
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Korean (ko)
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KR20130132406A (ko
Inventor
후이 리
틸로 제이. 헤크로트
얀 첸
다렌 존 맥무르트리
바네사 테일러
라진더 싱
핑위 딩
로즈 옌
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리겔 파마슈티칼스, 인크.
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/04—Artificial tears; Irrigation solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/14—Decongestants or antiallergics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002—Heterocyclic compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05—Isotopically modified compounds, e.g. labelled

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Epidemiology (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
KR1020137004970A 2010-07-28 2011-07-27 Ｊａｋ 경로의 억제를 위한 조성물 및 방법 Expired - Fee Related KR101937495B1 (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36857010P 2010-07-28 2010-07-28
US61/368,570 2010-07-28
PCT/US2011/045609 WO2012015972A1 (en) 2010-07-28 2011-07-27 Compositions and methods for inhibition of the jak pathway

Publications (2)

Publication Number Publication Date
KR20130132406A KR20130132406A (ko) 2013-12-04
KR101937495B1 true KR101937495B1 (ko) 2019-01-10

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Country Status (20)

Country Link
US (8) US8343954B2 (enExample)
EP (1) EP2598500B1 (enExample)
JP (2) JP6073221B2 (enExample)
KR (1) KR101937495B1 (enExample)
CN (1) CN103201280B (enExample)
AR (2) AR082408A1 (enExample)
AU (1) AU2011282742B2 (enExample)
BR (1) BR112013001632B1 (enExample)
CA (1) CA2804199C (enExample)
DK (1) DK2598500T3 (enExample)
EA (1) EA201390015A1 (enExample)
ES (1) ES2880622T3 (enExample)
IL (1) IL223855A (enExample)
MX (2) MX347331B (enExample)
PL (1) PL2598500T3 (enExample)
PT (1) PT2598500T (enExample)
RU (1) RU2672100C2 (enExample)
TW (1) TWI582090B (enExample)
WO (1) WO2012015972A1 (enExample)
ZA (1) ZA201300388B (enExample)

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US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
HRP20151325T1 (hr) * 2009-01-23 2016-01-01 Rigel Pharmaceuticals, Inc. Pripravci i postupci za inhibiciju jak puta
WO2012015972A1 (en) * 2010-07-28 2012-02-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
EP2833889B1 (en) 2012-04-04 2017-11-01 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
WO2013173506A2 (en) * 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
EP2948150A1 (en) * 2013-01-25 2015-12-02 Rigel Pharmaceuticals, Inc. Compounds and methods for treating inflammatory bowel diseases
EP2970275B1 (en) 2013-03-14 2018-05-09 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
US20160159774A1 (en) * 2014-12-05 2016-06-09 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2016100452A2 (en) * 2014-12-17 2016-06-23 Celgene Avilomics Research, Inc. Heteroaryl compounds and uses thereof
WO2017007658A1 (en) * 2015-07-07 2017-01-12 Rigel Pharmaceuticals, Inc. A combination for immune mediated cancer treatment
US20190060311A1 (en) * 2017-08-24 2019-02-28 Aclaris Therapeutics, Inc. Compositions and methods for treatment of vitiligo
ES2925450T3 (es) * 2017-11-06 2022-10-18 Bristol Myers Squibb Co Compuestos de isofuranona útiles como inhibidores de HPK1
JP2021524458A (ja) * 2018-05-24 2021-09-13 アストラゼネカ・アクチエボラーグＡｓｔｒａｚｅｎｅｃａ Ａｋｔｉｅｂｏｌａｇ ５−（（５−メチル−２−（（３，４，５−トリメチルフェニル）アミノ）ピリミジン−４−イル）アミノ）−ベンゾ［ｄ］オキサゾール−２（３Ｈ）−オンのフマル酸塩
WO2020092015A1 (en) 2018-11-02 2020-05-07 University Of Rochester Therapeutic mitigation of epithelial infection
CN110078633B (zh) * 2019-05-24 2021-05-11 爱斯特（成都）生物制药股份有限公司 一种4-氟-3-甲氧基-5-甲基苯胺盐酸盐制备方法
AU2021280113B2 (en) * 2020-05-29 2023-12-21 Nanjing Chia Tai Tianqing Pharmaceutical Co., Ltd. Pyrimidine compound as AXL inhibitor
KR20250053739A (ko) * 2023-10-13 2025-04-22 주식회사유한양행 7,7-다이메틸푸로[3,4-b]피리딘-5(7H)-온 유도체 또는 이의 염 및 이를 포함하는 약학 조성물
WO2025109026A1 (en) * 2023-11-21 2025-05-30 Intervet International B.V. Process for the preparation of 4-fluoro-3-methoxyaniline

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WO2008118822A1 (en) * 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
KR101762967B1 (ko) * 2009-01-23 2017-07-28 리겔 파마슈티칼스, 인크. Ｊａｋ 경로의 억제를 위한 조성물 및 방법

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US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
WO2008118822A1 (en) * 2007-03-23 2008-10-02 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
KR101762967B1 (ko) * 2009-01-23 2017-07-28 리겔 파마슈티칼스, 인크. Ｊａｋ 경로의 억제를 위한 조성물 및 방법

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EA201390015A1 (ru) 2013-07-30
EP2598500B1 (en) 2021-05-19
US20220024907A1 (en) 2022-01-27
US20130090310A1 (en) 2013-04-11
AU2011282742B2 (en) 2015-08-27
AR119882A2 (es) 2022-01-19
US9920041B2 (en) 2018-03-20
WO2012015972A1 (en) 2012-02-02
US20180162848A1 (en) 2018-06-14
AR082408A1 (es) 2012-12-05
US10479783B2 (en) 2019-11-19
JP2017061518A (ja) 2017-03-30
PT2598500T (pt) 2021-07-22
JP2013536179A (ja) 2013-09-19
JP6073221B2 (ja) 2017-02-01
IL223855A (en) 2016-05-31
EP2598500A1 (en) 2013-06-05
BR112013001632B1 (pt) 2021-05-25
US8343954B2 (en) 2013-01-01
CA2804199A1 (en) 2012-02-02
ZA201300388B (en) 2013-09-25
MX2020009397A (es) 2020-12-03
US20150259332A1 (en) 2015-09-17
US9611260B2 (en) 2017-04-04
MX347331B (es) 2017-04-21
MX2013000757A (es) 2013-04-29
CN103201280A (zh) 2013-07-10
BR112013001632A2 (pt) 2016-05-24
US20120028923A1 (en) 2012-02-02
US20200115371A1 (en) 2020-04-16
ES2880622T3 (es) 2021-11-25
AU2011282742A1 (en) 2013-02-07
AU2011282742A2 (en) 2013-04-04
USRE47396E1 (en) 2019-05-21
PL2598500T3 (pl) 2021-11-29
US20170158683A1 (en) 2017-06-08
RU2015122016A (ru) 2016-12-27
TW201209053A (en) 2012-03-01
CN103201280B (zh) 2016-08-10
US9067925B2 (en) 2015-06-30
TWI582090B (zh) 2017-05-11
DK2598500T3 (da) 2021-07-26
US11174251B2 (en) 2021-11-16
KR20130132406A (ko) 2013-12-04
RU2672100C2 (ru) 2018-11-12
CA2804199C (en) 2020-05-12

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