FI3377484T3 - Menetelmiä multippeliskleroosin hoitoon käyttämällä pyrimidiini- ja pyridiiniyhdisteitä, joilla on BTK inhiboiva vaikutus - Google Patents

Menetelmiä multippeliskleroosin hoitoon käyttämällä pyrimidiini- ja pyridiiniyhdisteitä, joilla on BTK inhiboiva vaikutus Download PDF

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Publication number
FI3377484T3
FI3377484T3 FIEP16805251.2T FI16805251T FI3377484T3 FI 3377484 T3 FI3377484 T3 FI 3377484T3 FI 16805251 T FI16805251 T FI 16805251T FI 3377484 T3 FI3377484 T3 FI 3377484T3
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Prior art keywords
multiple sclerosis
compound
pyrimidine
phenoxyphenyl
methyl
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FIEP16805251.2T
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English (en)
Finnish (fi)
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Tammy Dellovade
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Merck Patent Gmbh
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4418Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/455Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00Drugs for disorders of the muscular or neuromuscular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
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  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
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  • Pharmacology & Pharmacy (AREA)
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  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biomedical Technology (AREA)
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  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
FIEP16805251.2T 2015-11-17 2016-11-16 Menetelmiä multippeliskleroosin hoitoon käyttämällä pyrimidiini- ja pyridiiniyhdisteitä, joilla on BTK inhiboiva vaikutus FI3377484T3 (fi)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562256199P 2015-11-17 2015-11-17
PCT/US2016/062154 WO2017087445A1 (en) 2015-11-17 2016-11-16 Methods for treating multiple sclerosis using pyrimidine and pyridine compounds with btk inhibitory activity

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Publication Number Publication Date
FI3377484T3 true FI3377484T3 (fi) 2023-11-30

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FIEP16805251.2T FI3377484T3 (fi) 2015-11-17 2016-11-16 Menetelmiä multippeliskleroosin hoitoon käyttämällä pyrimidiini- ja pyridiiniyhdisteitä, joilla on BTK inhiboiva vaikutus

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US (2) US10716788B2 (enExample)
EP (2) EP3377484B1 (enExample)
JP (1) JP6891173B2 (enExample)
KR (1) KR102780243B1 (enExample)
CN (1) CN108884076B (enExample)
AU (1) AU2016357735B2 (enExample)
BR (1) BR112018007517B1 (enExample)
CL (1) CL2018001252A1 (enExample)
DK (1) DK3377484T3 (enExample)
ES (1) ES2964946T3 (enExample)
FI (1) FI3377484T3 (enExample)
HR (1) HRP20231547T1 (enExample)
HU (1) HUE064244T2 (enExample)
IL (1) IL258978B (enExample)
LT (1) LT3377484T (enExample)
MX (1) MX386146B (enExample)
MY (1) MY199473A (enExample)
NZ (1) NZ741294A (enExample)
PH (1) PH12018500736A1 (enExample)
PL (1) PL3377484T3 (enExample)
PT (1) PT3377484T (enExample)
RS (1) RS64908B1 (enExample)
SI (1) SI3377484T1 (enExample)
UA (1) UA123159C2 (enExample)
WO (1) WO2017087445A1 (enExample)
ZA (1) ZA201802348B (enExample)

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CA3001735A1 (en) * 2015-11-04 2017-05-11 Merck Patent Gmbh Methods for treating cancer using pyrimidine and pyridine compounds with btk inhibitory activity
CN108884076B (zh) * 2015-11-17 2021-07-30 默克专利有限公司 使用具有btk抑制活性的嘧啶和吡啶化合物治疗多发性硬化症的方法
KR20210022674A (ko) * 2018-06-19 2021-03-03 메르크 파텐트 게엠베하 1-(4-{[6-아미노-5-(4-페녹시-페닐)-피리미딘-4-일아미노]-메틸}-4-플루오로-피페리딘-1-일)-프로펜온의 신규한 결정 형태, 이의 염 형태, 및 이를 수득하는 방법
HRP20241737T1 (hr) * 2018-07-20 2025-02-28 Merck Patent Gmbh Supstituirani amino-pirimidinski spoj za upotrebu u postupku za liječenje i prevenciju multiple skleroze
IL294560A (en) 2020-01-20 2022-09-01 Genzyme Corp Medicinal tyrosine kinase inhibitors for relapsing multiple sclerosis
CN112250666B (zh) * 2020-10-09 2022-01-14 广东东阳光药业有限公司 取代的嘧啶类化合物及其用途
CA3200332A1 (en) * 2020-12-02 2022-06-09 Telios Pharma, Inc. Methods and compositions for treating an ophthalmic condition
WO2022121670A1 (zh) 2020-12-10 2022-06-16 苏州科睿思制药有限公司 Tolebrutinib的晶型及其制备方法和用途
US11866421B2 (en) 2021-05-31 2024-01-09 Epigen Biosciences, Inc. Pyrimidine and pyridine amine compounds and usage thereof in disease treatment
CN119744171A (zh) 2022-06-24 2025-04-01 默克专利股份公司 自身免疫病和炎性疾病的治疗方案
WO2024099241A1 (zh) * 2022-11-07 2024-05-16 天津征程医药科技有限公司 氘代的嘧啶衍生物以及包含该化合物的药物组合物
WO2025096900A1 (en) * 2023-11-03 2025-05-08 Board Of Regents, The University Of Texas System Synthetic network materials and methods of making and use thereof

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GB0512844D0 (en) * 2005-06-23 2005-08-03 Novartis Ag Organic compounds
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KR101301533B1 (ko) 2010-02-09 2013-09-04 한미사이언스 주식회사 암세포 성장 억제 효과를 갖는 신규 피리미딘 유도체
PT2718270T (pt) 2011-06-10 2022-07-29 Merck Patent Gmbh Composições e métodos para a produção de compostos de pirimidina e piridina com atividade inibidora de btk
TW201414734A (zh) * 2012-07-10 2014-04-16 Takeda Pharmaceutical 氮雜吲哚衍生物
GEP201606597B (en) * 2012-11-02 2017-01-10 Pfizer Bruton's tyrosine kinase inhibitors
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BR112015032330B1 (pt) * 2013-06-26 2019-01-22 Abbvie Inc. carboxamidas primárias como inibidores de bkt
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CA3001735A1 (en) * 2015-11-04 2017-05-11 Merck Patent Gmbh Methods for treating cancer using pyrimidine and pyridine compounds with btk inhibitory activity
CN108884076B (zh) * 2015-11-17 2021-07-30 默克专利有限公司 使用具有btk抑制活性的嘧啶和吡啶化合物治疗多发性硬化症的方法

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LT3377484T (lt) 2023-12-27
PT3377484T (pt) 2023-12-14
IL258978B (en) 2021-04-29
US10716788B2 (en) 2020-07-21
BR112018007517A2 (pt) 2018-10-23
CA3002224A1 (en) 2017-05-26
CN108884076A (zh) 2018-11-23
EP4295910A2 (en) 2023-12-27
EP4295910A3 (en) 2024-03-20
BR112018007517B1 (pt) 2023-09-26
KR20180080243A (ko) 2018-07-11
JP2018538264A (ja) 2018-12-27
PL3377484T3 (pl) 2024-04-08
US20170136018A1 (en) 2017-05-18
DK3377484T3 (da) 2023-11-27
JP6891173B2 (ja) 2021-06-18
MX386146B (es) 2025-03-18
ES2964946T3 (es) 2024-04-10
MY199473A (en) 2023-10-31
EP3377484B1 (en) 2023-09-06
UA123159C2 (uk) 2021-02-24
HRP20231547T1 (hr) 2024-03-15
AU2016357735A1 (en) 2018-04-26
PH12018500736A1 (en) 2018-10-01
RS64908B1 (sr) 2023-12-29
WO2017087445A1 (en) 2017-05-26
MX2018005463A (es) 2018-08-01
AU2016357735B2 (en) 2021-01-14
KR102780243B1 (ko) 2025-03-14
EP3377484A1 (en) 2018-09-26
ZA201802348B (en) 2020-08-26
US20200316068A1 (en) 2020-10-08
CL2018001252A1 (es) 2018-08-17
SI3377484T1 (sl) 2024-02-29
NZ741294A (en) 2023-07-28
IL258978A (en) 2018-07-31
CN108884076B (zh) 2021-07-30
RU2018120151A3 (enExample) 2020-03-24
RU2018120151A (ru) 2019-12-18
HUE064244T2 (hu) 2024-02-28

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