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)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • Transplantation (AREA)
  • Epidemiology (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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KR1020137004970A Expired - Fee Related KR101937495B1 (ko) 2010-07-28 2011-07-27 Ｊａｋ 경로의 억제를 위한 조성물 및 방법

Country Status (20)

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

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US20070203161A1 (en) * 2006-02-24 2007-08-30 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the jak pathway
PL2565193T3 (pl) * 2009-01-23 2014-07-31 Rigel Pharmaceuticals Inc Kompozycje i sposoby hamowania szlaku JAK
AU2011282742B2 (en) 2010-07-28 2015-08-27 Rigel Pharmaceuticals, Inc. Compositions and methods for inhibition of the JAK pathway
ES2658395T3 (es) 2012-04-04 2018-03-09 Rigel Pharmaceuticals, Inc. Inhibidores de proteína cinasa C y usos de los mismos
US20130310340A1 (en) * 2012-05-16 2013-11-21 Rigel Pharmaceuticals, Inc. Method of treating muscular degradation
CA2899281C (en) * 2013-01-25 2022-05-31 Rigel Pharmaceuticals, Inc. Pyrimidinediamine compounds for use in treating or preventing autoimmune alopecia
CA2904610A1 (en) * 2013-03-14 2014-09-25 Rigel Pharmaceuticals, Inc. Protein kinase c inhibitors and uses thereof
WO2016090079A1 (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
WO2019040706A1 (en) * 2017-08-24 2019-02-28 Aclaris Therapeutics, Inc. COMPOSITIONS AND METHODS FOR TREATING VITILIGO
JP7167146B2 (ja) * 2017-11-06 2022-11-08 ブリストル－マイヤーズ スクイブ カンパニー Ｈｐｋ１阻害剤として有用なイソフラノン化合物
US20210198248A1 (en) * 2018-05-24 2021-07-01 Astrazeneca Ab Fumarate salt of 5-((5-methyl-2-((3,4,5-trimethylphenyl)amino)pyrimidin-4-yl)amino)-benzo[d]oxazol-2(3h)-one
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
JP2023527242A (ja) * 2020-05-29 2023-06-27 南京正大天晴制薬有限公司 Ａｘｌ阻害剤であるピリミジン系化合物
WO2025080099A1 (ko) * 2023-10-13 2025-04-17 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

Also Published As

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

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