BR112014022790B1 - Sais de um inibidor de quinase de receptor de fator do crescimento epidermal, composição farmacêutica e usos do mesmo - Google Patents

Sais de um inibidor de quinase de receptor de fator do crescimento epidermal, composição farmacêutica e usos do mesmo Download PDF

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BR112014022790B1
BR112014022790B1 BR112014022790-0A BR112014022790A BR112014022790B1 BR 112014022790 B1 BR112014022790 B1 BR 112014022790B1 BR 112014022790 A BR112014022790 A BR 112014022790A BR 112014022790 B1 BR112014022790 B1 BR 112014022790B1
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compound
acid
salt
peaks
ray powder
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BR112014022790-0A
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Portuguese (pt)
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BR112014022790A2 (enExample
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Mei Lai
Steven Richard Witowski
Richland Wayne Tester
Kwangho Lee
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Celgene Car Llc
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/02—Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/05—Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing at least two sulfo groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/25—Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton
    • C07C309/27—Sulfonic acids having sulfo groups bound to carbon atoms of rings other than six-membered aromatic rings of a carbon skeleton containing carboxyl groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/29—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings
    • C07C309/30—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of non-condensed six-membered aromatic rings of six-membered aromatic rings substituted by alkyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00—Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01—Sulfonic acids
    • C07C309/28—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C309/33—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems
    • C07C309/34—Sulfonic acids having sulfo groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton of six-membered aromatic rings being part of condensed ring systems formed by two rings
    • C07C309/35—Naphthalene sulfonic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/06—Oxalic acid
    • C07C55/07—Salts thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C62/00—Compounds having carboxyl groups bound to carbon atoms of rings other than six—membered aromatic rings and containing any of the groups OH, O—metal, —CHO, keto, ether, groups, groups, or groups
    • C07C62/02—Saturated compounds containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)
  • Air-Conditioning For Vehicles (AREA)
  • Electric Connection Of Electric Components To Printed Circuits (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
BR112014022790-0A 2012-03-15 2013-03-13 Sais de um inibidor de quinase de receptor de fator do crescimento epidermal, composição farmacêutica e usos do mesmo BR112014022790B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201261611400P 2012-03-15 2012-03-15
US61/611,400 2012-03-15
PCT/US2013/030996 WO2013138502A1 (en) 2012-03-15 2013-03-13 Salts of an epidermal growth factor receptor kinase inhibitor

Publications (2)

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BR112014022790A2 BR112014022790A2 (enExample) 2017-06-20
BR112014022790B1 true BR112014022790B1 (pt) 2022-04-19

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US (5) US9108927B2 (enExample)
EP (1) EP2825042B1 (enExample)
JP (2) JP6317320B2 (enExample)
KR (1) KR102090453B1 (enExample)
CN (2) CN104284584B (enExample)
AR (1) AR090357A1 (enExample)
AU (3) AU2013201519C1 (enExample)
BR (1) BR112014022790B1 (enExample)
CA (1) CA2866857C (enExample)
CY (1) CY1122176T1 (enExample)
DK (1) DK2825042T3 (enExample)
ES (1) ES2698298T3 (enExample)
HR (1) HRP20181784T1 (enExample)
IL (1) IL234426B (enExample)
LT (1) LT2825042T (enExample)
MX (1) MX356179B (enExample)
MY (1) MY185243A (enExample)
PH (1) PH12014502037B1 (enExample)
PL (1) PL2825042T3 (enExample)
PT (1) PT2825042T (enExample)
RS (1) RS57901B1 (enExample)
RU (1) RU2711077C9 (enExample)
SG (2) SG11201405692UA (enExample)
SI (1) SI2825042T1 (enExample)
SM (1) SMT201800571T1 (enExample)
TR (1) TR201816244T4 (enExample)
TW (1) TWI591060B (enExample)
WO (1) WO2013138502A1 (enExample)

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US11351168B1 (en) 2008-06-27 2022-06-07 Celgene Car Llc 2,4-disubstituted pyrimidines useful as kinase inhibitors
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BR112014022789B1 (pt) 2012-03-15 2022-04-19 Celgene Car Llc Formas sólidas de um inibidor de quinase de receptor do fator de crescimento epidérmico, composição farmacêutica e usos do mesmo
RU2711077C9 (ru) 2012-03-15 2020-08-11 Селджен Кар Ллс Соли ингибитора киназы рецептора эпидермального фактора роста
EP2953457B1 (en) 2013-02-08 2020-04-08 Celgene CAR LLC Erk inhibitors and uses thereof
JP2016518408A (ja) * 2013-05-06 2016-06-23 クロヴィス・オンコロジー，インコーポレーテッド 上皮増殖因子受容体キナーゼ阻害剤の塩
NO2718543T3 (enExample) * 2014-02-04 2018-01-06
EP3179858B1 (en) 2014-08-13 2019-05-15 Celgene Car Llc Forms and compositions of an erk inhibitor
CN104961688A (zh) * 2014-12-25 2015-10-07 苏州晶云药物科技有限公司 一种表皮生长因子受体激酶抑制剂的磷酸盐及其制备方法
WO2016101912A1 (zh) * 2014-12-25 2016-06-30 苏州晶云药物科技有限公司 一种表皮生长因子受体激酶抑制剂的盐的晶型及其制备方法
WO2017016463A1 (zh) * 2015-07-24 2017-02-02 上海海雁医药科技有限公司 Egfr抑制剂及其药学上可接受的盐和多晶型物及其应用
CN105461640B (zh) * 2015-12-02 2017-11-21 芷威（上海）化学科技有限公司 一种酪氨酸激酶抑制剂的制备方法
CN105481779B (zh) * 2015-12-24 2019-01-25 南京华威医药科技集团有限公司 抗癌药物Rociletinib及其中间体制备
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JOP20190281A1 (ar) * 2017-06-13 2019-12-02 Korea Res Inst Chemical Tech مشتق n2، n4 ثنائي فينيل بيريميدين -2، 4- ثنائي أمين، وطريقة لتحضيره، وتركيبة صيدلانية تحتوي على المشتق بوصفه مكون فعال للوقاية من السرطان أو علاجه
TWI798334B (zh) * 2018-01-31 2023-04-11 大陸商迪哲（江蘇）醫藥股份有限公司 Ｅｒｂｂ／ｂｔｋ抑制劑
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BR112022009031A2 (pt) * 2019-11-11 2022-10-11 Incyte Corp Sais e formas cristalinas de um inibidor de pd-1/pd-l1
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