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PE20240236A1 - Formas solidas cristalinas de un inhibidor de bet - Google Patents

Formas solidas cristalinas de un inhibidor de bet

Info

Publication number
PE20240236A1
PE20240236A1 PE2023002468A PE2023002468A PE20240236A1 PE 20240236 A1 PE20240236 A1 PE 20240236A1 PE 2023002468 A PE2023002468 A PE 2023002468A PE 2023002468 A PE2023002468 A PE 2023002468A PE 20240236 A1 PE20240236 A1 PE 20240236A1
Authority
PE
Peru
Prior art keywords
compound
crystalline solid
solid forms
bet inhibitor
oxazin
Prior art date
Application number
PE2023002468A
Other languages
English (en)
Inventor
Zhongjiang Jia
Pingli Liu
Lei Qiao
Yongzhong Wu
Jiacheng Zhou
Qun Li
Shili Chen
Original Assignee
Incyte Corp
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=59258384&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20240236(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of PE20240236A1 publication Critical patent/PE20240236A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—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
    • A61K31/535—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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A01—AGRICULTURE; FORESTRY; ANIMAL HUSBANDRY; HUNTING; TRAPPING; FISHING
    • A01M—CATCHING, TRAPPING OR SCARING OF ANIMALS; APPARATUS FOR THE DESTRUCTION OF NOXIOUS ANIMALS OR NOXIOUS PLANTS
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    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P11/02—Nasal agents, e.g. decongestants
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    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
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    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
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    • A—HUMAN NECESSITIES
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    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
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  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
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  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
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  • Neurosurgery (AREA)
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  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)

Abstract

La invencion se refiere a un proceso para preparar el compuesto 2,2,4-trimetil-8-(6-metil-7-oxo-1-tosil-6,7-dihidro-1H-pirrolo[2,3-c]piridin-4-il)-6-(metilsulfonil)-2H-benzo[b][1,4]oxazin-3(4H)-ona (compuesto 8), que comprende en la reaccion del compuesto 7 con un compuesto 9 en presencia de P2 y B2, donde P2 es un catalizador de metal de transicion, tal como paladio y B2 es una base de bicarbonato de metal alcalino. Tambien proporciona un proceso de preparacion del compuesto 7 intermediario. El citado compuesto 8 es un compuesto intermediario en la obtencion del compuesto 2,2,4-trimetil-8-(6-metil-7-oxo-6,7-dihidro-1H-pirrolo[2,3-c]piridin-4-il)-6-(metilsulfonil)-2H-benzo[b][1,4]oxazin-3(4H)-ona (compuesto 1), el cual es un inhibidor de proteinas BET, tales como 5 BRD2, BRD3, BRD4 y BRD-t, siendo util para el tratamiento del cancer.
PE2023002468A 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet PE20240236A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662352220P 2016-06-20 2016-06-20
US201662397575P 2016-09-21 2016-09-21
PCT/US2017/038121 WO2017222977A1 (en) 2016-06-20 2017-06-19 Crystalline solid forms of a bet inhibitor

Publications (1)

Publication Number Publication Date
PE20240236A1 true PE20240236A1 (es) 2024-02-16

Family

ID=59258384

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2018003269A PE20190623A1 (es) 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet
PE2023002468A PE20240236A1 (es) 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2018003269A PE20190623A1 (es) 2016-06-20 2017-06-19 Formas solidas cristalinas de un inhibidor de bet

Country Status (33)

Country Link
US (6) US10189832B2 (es)
EP (2) EP3472157B1 (es)
JP (6) JP7096170B2 (es)
KR (4) KR102888132B1 (es)
CN (3) CN109715625B (es)
AU (3) AU2017281286B2 (es)
CA (3) CA3220975A1 (es)
CL (3) CL2018003702A1 (es)
CO (1) CO2018014339A2 (es)
CR (2) CR20190027A (es)
CY (1) CY1126092T1 (es)
DK (1) DK3472157T3 (es)
EC (1) ECSP19001982A (es)
ES (1) ES2945063T3 (es)
FI (1) FI3472157T3 (es)
HR (1) HRP20230466T1 (es)
HU (1) HUE062234T2 (es)
IL (3) IL302528A (es)
LT (1) LT3472157T (es)
MD (1) MD3472157T2 (es)
MX (3) MX389145B (es)
MY (2) MY198892A (es)
PE (2) PE20190623A1 (es)
PH (3) PH12021551887A1 (es)
PL (1) PL3472157T3 (es)
PT (1) PT3472157T (es)
RS (1) RS64274B1 (es)
SG (2) SG11201811416VA (es)
SI (1) SI3472157T1 (es)
SM (1) SMT202300155T1 (es)
TW (3) TWI854936B (es)
UA (2) UA124106C2 (es)
WO (1) WO2017222977A1 (es)

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EP3581576B1 (en) 2013-03-15 2022-01-26 Incyte Holdings Corporation Tricyclic heterocycles as bet protein inhibitors for use in the treatment of a proliferative disease in combination with a janus kinase inhibitor
WO2015095492A1 (en) 2013-12-19 2015-06-25 Incyte Corporation Tricyclic heterocycles as bet protein inhibitors
NZ763740A (en) 2014-04-23 2023-06-30 Incyte Holdings Corp 1h-pyrrolo[2,3-c]pyridin-7(6h)-ones and pyrazolo[3,4-c]pyridin-7(6h)-ones as inhibitors of bet proteins
ES2855225T3 (es) 2014-09-15 2021-09-23 Incyte Corp Heterociclos tricíclicos para su uso como inhibidores de proteínas BET
TW201722966A (zh) 2015-10-29 2017-07-01 英塞特公司 Bet蛋白質抑制劑之非晶固體形式
MD3472157T2 (ro) * 2016-06-20 2023-10-31 Incyte Corp Forme cristaline solide ale unui inhibitor BET
TWI882964B (zh) * 2018-09-13 2025-05-11 大陸商恒翼生物醫藥（上海）股份有限公司 Bet 溴結構域(bromodomain)抑制劑之固體形式之製備方法
WO2021217117A1 (en) * 2020-04-24 2021-10-28 Memorial Sloan Kettering Cancer Center Targeted therapy for the treatment & prevention of life-threatening complications of infection
EP4161528B1 (en) * 2020-06-03 2025-11-05 Incyte Corporation Combination of ruxolitinib with incb057643 for use in the treatment of myeloproliferative neoplasms
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN112137961A (zh) * 2020-09-30 2020-12-29 严鹏科 一种雷帕霉素组合物及其制备方法
JP2024500975A (ja) * 2020-12-23 2024-01-10 カスケード プロドラッグ インコーポレイテッド ビンカアルカロイドｎ－オキシドと免疫チェックポイント阻害剤との併用療法
TW202508595A (zh) 2023-05-04 2025-03-01 美商銳新醫藥公司 用於ｒａｓ相關疾病或病症之組合療法
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