ME02119B - Spojevi korisni za inhibiranje chk1 - Google Patents

Spojevi korisni za inhibiranje chk1

Info

Publication number
ME02119B
ME02119B MEP-2015-69A MEP6915A ME02119B ME 02119 B ME02119 B ME 02119B ME P6915 A MEP6915 A ME P6915A ME 02119 B ME02119 B ME 02119B
Authority
ME
Montenegro
Prior art keywords
cancer
salt
compound
methylpyridin
pyrazin
Prior art date
Application number
MEP-2015-69A
Other languages
English (en)
Inventor
Sajan Joseph
Susanta Samajdar
Original Assignee
Lilly Co Eli
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
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of ME02119B publication Critical patent/ME02119B/me

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Classifications

    • 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
    • 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
    • A61K31/4965Non-condensed pyrazines
    • A61K31/497Non-condensed pyrazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C309/00Sulfonic acids; Halides, esters, or anhydrides thereof
    • C07C309/01Sulfonic acids
    • C07C309/02Sulfonic acids having sulfo groups bound to acyclic carbon atoms
    • C07C309/03Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C309/04Sulfonic acids having sulfo groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton containing only one sulfo group
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C53/00Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/08Acetic acid
    • C07C53/10Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/06Oxalic acid
    • C07C55/07Salts thereof
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C55/00Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02Dicarboxylic acids
    • C07C55/10Succinic acid

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (13)

1.Spoj, naznačen time što je (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amin, ili njegova farmaceutski prihvatljiva sol.
2.Spoj u skladu s patentnim zahtjevom 1, naznačen time što je (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amin.
3.Spoj u skladu s patentnim zahtjevom 1, naznačen time što je sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina s metansulfonskom kiselinom.
4.Spoj u skladu s patentnim zahtjevom 1, naznačen time što je sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina s octenom kiselinom.
5.Spoj u skladu s patentnim zahtjevom 1, naznačen time što je hemioksalatna sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina.
6.Spoj u skladu s patentnim zahtjevom 1, naznačen time što je hemisukcinatna sol (R)-[5-(2-metoksi-6-metilpiridin-3-il)-2H-pirazol-3-il][6-(piperidin-3-iloksi)pirazin-2-il]amina.
7.Farmaceutski pripravak, naznačen time što sadrži spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, kao i farmaceutski prihvatljivu podlogu, razrjeđivač ili pomoćnu tvar.
8.Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u terapiji.
9.Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u liječenju raka.
10.Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u istodobnoj, odvojenoj ili uzastopnoj kombinaciji s ionizirajućim zračenjem u liječenju raka.
11.Spoj ili sol u skladu bilo kojim od patentnih zahtjeva 1-6, naznačeni time što su namijenjeni upotrebi u istodobnoj, odvojenoj ili uzastopnoj kombinaciji s jednim ili više kemoterapijskih sredstava u liječenju raka.
12.Spoj ili sol namijenjeni upotrebi u skladu s patentnim zahtjevom 11, naznačeni time što se jedno ili više kemoterapijskih sredstava bira iz skupine koju čine 5-fluoruracil, hidroksiurea, gemcitabin, metotreksat, pemetreksed, doksorubicin, etopozid, cisplatin i taksol.
13.Spoj ili sol namijenjeni upotrebi u skladu bilo kojim od patentnih zahtjeva 9-12, naznačeni time što se rak bira iz skupine koju čine rak mokraćnog mjehura, rak debelog crijeva, rak želuca, rak jetre, rak pluća, rak dojke, melanom, rak jajnika, rak gušterače, mezoteliom, rak bubrega i rak maternice.
MEP-2015-69A 2010-11-08 2011-11-01 Spojevi korisni za inhibiranje chk1 ME02119B (me)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US41113710P 2010-11-08 2010-11-08
PCT/US2011/058692 WO2012064548A1 (en) 2010-11-08 2011-11-01 Compounds useful for inhibiting chk1
EP11788263.9A EP2638033B1 (en) 2010-11-08 2011-11-01 Compounds useful for inhibiting chk1

Publications (1)

Publication Number Publication Date
ME02119B true ME02119B (me) 2015-10-20

Family

ID=45044707

Family Applications (1)

Application Number Title Priority Date Filing Date
MEP-2015-69A ME02119B (me) 2010-11-08 2011-11-01 Spojevi korisni za inhibiranje chk1

Country Status (22)

Country Link
US (1) US9067920B2 (me)
EP (1) EP2638033B1 (me)
JP (1) JP5792316B2 (me)
KR (1) KR101533166B1 (me)
CN (1) CN103180311B (me)
AR (1) AR083575A1 (me)
AU (1) AU2011326230B2 (me)
BR (1) BR112013010009B1 (me)
CA (1) CA2816944C (me)
DK (1) DK2638033T3 (me)
EA (1) EA022096B1 (me)
ES (1) ES2541414T3 (me)
HR (1) HRP20150530T1 (me)
JO (1) JO3145B1 (me)
ME (1) ME02119B (me)
MX (1) MX2013005181A (me)
PL (1) PL2638033T3 (me)
PT (1) PT2638033E (me)
RS (1) RS54012B1 (me)
SI (1) SI2638033T1 (me)
TW (1) TWI501956B (me)
WO (1) WO2012064548A1 (me)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201402277D0 (en) 2014-02-10 2014-03-26 Sentinel Oncology Ltd Pharmaceutical compounds
CN108601781B (zh) 2016-02-04 2019-11-22 广州必贝特医药技术有限公司 作为检测点激酶1(chk1)抑制剂的3,5-二取代吡唑及其制备及应用
EP3461480A1 (en) 2017-09-27 2019-04-03 Onxeo Combination of a dna damage response cell cycle checkpoint inhibitors and belinostat for treating cancer
CN112457306A (zh) 2019-09-06 2021-03-09 上海瑛派药业有限公司 3,5-二取代吡唑化合物作为激酶抑制剂及其应用
CA3200498A1 (en) 2020-11-30 2022-06-02 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1h-pyrazol-3-amine derivative
US11564920B2 (en) 2020-11-30 2023-01-31 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1H-pyrazol-3-amine derivative
UY39832A (es) 2021-06-28 2023-01-31 Blueprint Medicines Corp Inhibidores de cdk2
TW202333680A (zh) 2021-12-24 2023-09-01 日商住友製藥股份有限公司 具有二環性骨架之1h-吡唑-3-胺衍生物
EP4534100A1 (en) * 2022-05-27 2025-04-09 Sumitomo Pharma Co., Ltd. Therapeutic for cancer refractory to immune checkpoint inhibitor
CN121311482A (zh) * 2023-04-14 2026-01-09 缆图药品公司 Cdk2抑制剂

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006528661A (ja) * 2003-07-25 2006-12-21 ファイザー・インク アミノピラゾール化合物およびchk1阻害剤としての使用
DE602004031777D1 (en) * 2004-01-05 2011-04-21 Astrazeneca Ab Thiophenderivate als chk-1-inhibitoren
WO2005121121A2 (en) 2004-06-04 2005-12-22 Arena Pharmaceuticals, Inc. Substituted aryl and heteroaryl derivatives as modulators of metabolism and the prophylaxis and treatment of disorders related thereto
WO2006117560A1 (en) * 2005-05-05 2006-11-09 Astrazeneca Ab Pyrazolyl-amino- substituted pyrimidines and their use in the treatment of cancer
CA2610884A1 (en) * 2005-06-09 2006-12-21 Merck & Co., Inc. Inhibitors of checkpoint kinases
WO2008117050A1 (en) * 2007-03-27 2008-10-02 Astrazeneca Ab Pyrazolyl-amino-substituted pyrazines and their use for the treatment of cancer
PA8850801A1 (es) * 2008-12-17 2010-07-27 Lilly Co Eli Compuestos útiles para inhibir chk1

Also Published As

Publication number Publication date
EA022096B1 (ru) 2015-10-30
KR101533166B1 (ko) 2015-07-01
BR112013010009B1 (pt) 2021-10-19
HRP20150530T1 (hr) 2015-06-19
TWI501956B (zh) 2015-10-01
EP2638033B1 (en) 2015-04-08
PT2638033E (pt) 2015-06-01
AR083575A1 (es) 2013-03-06
MX2013005181A (es) 2013-10-17
RS54012B1 (sr) 2015-10-30
CA2816944A1 (en) 2012-05-18
SI2638033T1 (sl) 2015-05-29
AU2011326230A1 (en) 2013-05-09
CN103180311A (zh) 2013-06-26
CN103180311B (zh) 2014-08-20
DK2638033T3 (en) 2015-04-27
ES2541414T3 (es) 2015-07-20
AU2011326230B2 (en) 2015-02-19
JO3145B1 (ar) 2017-09-20
US9067920B2 (en) 2015-06-30
KR20130099146A (ko) 2013-09-05
EA201390499A1 (ru) 2013-08-30
WO2012064548A1 (en) 2012-05-18
EP2638033A1 (en) 2013-09-18
JP5792316B2 (ja) 2015-10-07
PL2638033T3 (pl) 2015-09-30
TW201305138A (zh) 2013-02-01
JP2013541586A (ja) 2013-11-14
CA2816944C (en) 2015-12-22
US20130190262A1 (en) 2013-07-25
BR112013010009A2 (pt) 2020-09-29

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