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

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/14—Heterocyclic 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
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
    • A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
    • A61K31/704—Compounds 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
    • 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
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds 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
    • A61K31/7064—Compounds 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
    • A61K31/7068—Compounds 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
    • 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
    • C07C53/00—Saturated compounds having only one carboxyl group bound to an acyclic carbon atom or hydrogen
    • C07C53/08—Acetic acid
    • C07C53/10—Salts thereof
    • 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
    • C07C55/00—Saturated compounds having more than one carboxyl group bound to acyclic carbon atoms
    • C07C55/02—Dicarboxylic acids
    • C07C55/10—Succinic 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
EP11788263.9A EP2638033B1 (en) 2010-11-08 2011-11-01 Compounds useful for inhibiting chk1
PCT/US2011/058692 WO2012064548A1 (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 (11)

* 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
CA3013514C (en) 2016-02-04 2021-11-23 Pharmaengine, Inc. 3,5-disubstituted pyrazoles useful as checkpoint kinase 1 (chk1) inhibitors, and their preparations and applications
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
MX2023006364A (es) * 2020-11-30 2023-06-13 Sumitomo Pharma Co Ltd Derivado de 5-heteroaril-1h-pirazol-3-amina.
US11564920B2 (en) 2020-11-30 2023-01-31 Sumitomo Pharma Co., Ltd. 5-heteroaryl-1H-pyrazol-3-amine derivative
WO2022266190A1 (en) 2021-06-16 2022-12-22 Blueprint Medicines Corporation Substituted pyrimidinyl-pyrazoles as cdk2 inhibitors
CN117897384A (zh) 2021-06-28 2024-04-16 缆图药品公司 Cdk2抑制剂
CA3241992A1 (en) 2021-12-24 2023-06-29 Seiji Kamioka 1h-pyrazole-3-amine derivative having bicyclic backbone
JPWO2023229032A1 (me) * 2022-05-27 2023-11-30
AU2024255916A1 (en) * 2023-04-14 2025-11-13 Blueprint Medicines Corporation Cdk2 inhibitors

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
JP2007517843A (ja) * 2004-01-05 2007-07-05 アストラゼネカ アクチボラグ Chk1阻害剤であるチオフェン誘導体
EA011671B1 (ru) 2004-06-04 2009-04-28 Арена Фармасьютикалз, Инк. Замещенные производные арила и гетероарила в качестве модуляторов метаболизма и для профилактики и лечения связанных с ним расстройств
JP2008540391A (ja) * 2005-05-05 2008-11-20 アストラゼネカ アクチボラグ ピラゾリルアミノ置換ピリミジン、および癌の処置におけるそれらの使用
JP2008543754A (ja) * 2005-06-09 2008-12-04 メルク エンド カムパニー インコーポレーテッド チェックポイントキナーゼの阻害剤
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
EP2638033B1 (en) 2015-04-08
EA022096B1 (ru) 2015-10-30
CA2816944C (en) 2015-12-22
JO3145B1 (ar) 2017-09-20
PT2638033E (pt) 2015-06-01
BR112013010009A2 (pt) 2020-09-29
US9067920B2 (en) 2015-06-30
WO2012064548A1 (en) 2012-05-18
RS54012B1 (sr) 2015-10-30
US20130190262A1 (en) 2013-07-25
TWI501956B (zh) 2015-10-01
MX2013005181A (es) 2013-10-17
AU2011326230A1 (en) 2013-05-09
ES2541414T3 (es) 2015-07-20
PL2638033T3 (pl) 2015-09-30
KR101533166B1 (ko) 2015-07-01
CN103180311A (zh) 2013-06-26
JP2013541586A (ja) 2013-11-14
CA2816944A1 (en) 2012-05-18
SI2638033T1 (sl) 2015-05-29
EA201390499A1 (ru) 2013-08-30
DK2638033T3 (en) 2015-04-27
BR112013010009B1 (pt) 2021-10-19
EP2638033A1 (en) 2013-09-18
KR20130099146A (ko) 2013-09-05
JP5792316B2 (ja) 2015-10-07
CN103180311B (zh) 2014-08-20
AR083575A1 (es) 2013-03-06
AU2011326230B2 (en) 2015-02-19
TW201305138A (zh) 2013-02-01
HRP20150530T1 (hr) 2015-06-19

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