CA2994644A1 - Pyrazole pyrimidine derivative and uses thereof - Google Patents
Pyrazole pyrimidine derivative and uses thereof Download PDFInfo
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- CA2994644A1 CA2994644A1 CA2994644A CA2994644A CA2994644A1 CA 2994644 A1 CA2994644 A1 CA 2994644A1 CA 2994644 A CA2994644 A CA 2994644A CA 2994644 A CA2994644 A CA 2994644A CA 2994644 A1 CA2994644 A1 CA 2994644A1
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- branched
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- compound
- alkyl
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- FEYLUKDSKVSMSZ-UHFFFAOYSA-N tert-butyl n-(4-aminocyclohexyl)carbamate Chemical compound CC(C)(C)OC(=O)NC1CCC(N)CC1 FEYLUKDSKVSMSZ-UHFFFAOYSA-N 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 239000003104 tissue culture media Substances 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 238000013518 transcription Methods 0.000 description 1
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- 230000002103 transcriptional effect Effects 0.000 description 1
- 230000026683 transduction Effects 0.000 description 1
- 238000010361 transduction Methods 0.000 description 1
- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 description 1
- 229910000404 tripotassium phosphate Inorganic materials 0.000 description 1
- 235000019798 tripotassium phosphate Nutrition 0.000 description 1
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- 239000008158 vegetable oil Substances 0.000 description 1
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Classifications
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- 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
- 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
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/08—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 carbon chain containing alicyclic rings
-
- 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
- C07D403/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic 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
- C07D405/14—Heterocyclic 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 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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| US62/200,846 | 2015-08-04 | ||
| US201562268750P | 2015-12-17 | 2015-12-17 | |
| US62/268,750 | 2015-12-17 | ||
| PCT/IL2016/050852 WO2017021969A1 (en) | 2015-08-04 | 2016-08-04 | Pyrazole pyrimidine derivative and uses thereof |
Publications (1)
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| CA2994644A1 true CA2994644A1 (en) | 2017-02-09 |
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| SM (1) | SMT202100720T1 (enExample) |
| WO (1) | WO2017021969A1 (enExample) |
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| US10376511B2 (en) * | 2015-08-04 | 2019-08-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Pyrazole pyrimidine derivative and uses thereof |
| MX394556B (es) * | 2017-02-01 | 2025-03-24 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer. |
| JOP20180011A1 (ar) | 2017-02-16 | 2019-01-30 | Gilead Sciences Inc | مشتقات بيرولو [1، 2-b]بيريدازين |
| WO2019155468A1 (en) | 2018-02-08 | 2019-08-15 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use |
| TWI898556B (zh) | 2018-07-13 | 2025-09-21 | 美商基利科學股份有限公司 | 吡咯并[1,2-b]嗒衍生物 |
| US11066404B2 (en) | 2018-10-11 | 2021-07-20 | Incyte Corporation | Dihydropyrido[2,3-d]pyrimidinone compounds as CDK2 inhibitors |
| WO2020168197A1 (en) | 2019-02-15 | 2020-08-20 | Incyte Corporation | Pyrrolo[2,3-d]pyrimidinone compounds as cdk2 inhibitors |
| US11472791B2 (en) | 2019-03-05 | 2022-10-18 | Incyte Corporation | Pyrazolyl pyrimidinylamine compounds as CDK2 inhibitors |
| WO2020205560A1 (en) | 2019-03-29 | 2020-10-08 | Incyte Corporation | Sulfonylamide compounds as cdk2 inhibitors |
| US11447494B2 (en) | 2019-05-01 | 2022-09-20 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| US11440914B2 (en) | 2019-05-01 | 2022-09-13 | Incyte Corporation | Tricyclic amine compounds as CDK2 inhibitors |
| SG11202113211PA (en) * | 2019-06-03 | 2021-12-30 | Biotheryx Inc | Non-hygroscopic crystalline salts of a pyrazole compound, and pharmaceutical compositions and use thereof |
| WO2021000957A1 (zh) * | 2019-07-04 | 2021-01-07 | 北京国鸿生物医药科技有限公司 | 一种杂环化合物、其药物组合物及用途 |
| BR112022002698A2 (pt) | 2019-08-14 | 2022-07-19 | Incyte Corp | Compostos de imidazolil pirimidinilamina como inibidores de cdk2 |
| AU2020364007A1 (en) | 2019-10-11 | 2022-04-28 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| AU2021209057A1 (en) * | 2020-01-13 | 2022-06-30 | Yissum Research Development Company Of The Hebrew University Of Jerusalem, Ltd. | Pyrazolylpyrimidines and use thereof |
| WO2021155050A1 (en) * | 2020-01-29 | 2021-08-05 | Biotheryx, Inc. | Kinase modulators, pharmaceutical compositions, and therapeutic applications |
| WO2021191384A1 (en) * | 2020-03-26 | 2021-09-30 | Janssen Pharmaceutica Nv | Aryl piperidines as monoacylglycerol lipase modulators |
| US20240207268A1 (en) * | 2021-03-24 | 2024-06-27 | Biotheryx, Inc. | Pyrazolylpyrimidines for treating malignant solid tumor |
| US11981671B2 (en) | 2021-06-21 | 2024-05-14 | Incyte Corporation | Bicyclic pyrazolyl amines as CDK2 inhibitors |
| US11752151B2 (en) * | 2021-07-12 | 2023-09-12 | Buddhist Tzu Chi Medical Foundation | Method for enhancing hair growth |
| US20230053307A1 (en) * | 2021-07-19 | 2023-02-16 | Buddhist Tzu Chi Medical Foundation | Method for preventing or treating skin disorders and conditions |
| US11976073B2 (en) | 2021-12-10 | 2024-05-07 | Incyte Corporation | Bicyclic amines as CDK2 inhibitors |
| WO2025199440A1 (en) * | 2024-03-21 | 2025-09-25 | Edgewood Oncology | Methods of treating liposarcoma using a pyrazole compound |
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| EP1343781B1 (en) | 2000-12-05 | 2008-09-03 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| US6884804B2 (en) | 2001-05-16 | 2005-04-26 | Vertex Pharmaceuticals Incorporated | Inhibitors of Src and other protein kinases |
| GB0215844D0 (en) | 2002-07-09 | 2002-08-14 | Novartis Ag | Organic compounds |
| US20090036448A1 (en) | 2004-03-30 | 2009-02-05 | Taisho Pharmecutical Co., Ltd. | Pyrimidine derivatives and methods of treatment related to the use thereof |
| JP2007145819A (ja) | 2005-10-28 | 2007-06-14 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
| WO2007129195A2 (en) * | 2006-05-04 | 2007-11-15 | Pfizer Products Inc. | 4-pyrimidine-5-amino-pyrazole compounds |
| JP2009538352A (ja) | 2006-05-26 | 2009-11-05 | アストラゼネカ アクチボラグ | 細胞増殖を阻害するための薬剤としての２−カルボシクロアミノ−４−イミダゾリルピリミジン類 |
| EP2231636B1 (en) | 2007-12-07 | 2011-09-14 | Novartis AG | Pyrazole derivatives and use thereof as inhibitors of cyclin dependent kinases |
| WO2013066684A1 (en) | 2011-11-04 | 2013-05-10 | Jasco Pharmaceuticals, LLC | Aminopyrimidine kinase inhibitors |
| CA2925211A1 (en) | 2013-09-27 | 2015-04-02 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| EP3057956B1 (en) * | 2013-10-18 | 2021-05-05 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (cdk7) |
| US10376511B2 (en) | 2015-08-04 | 2019-08-13 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Pyrazole pyrimidine derivative and uses thereof |
| MX394556B (es) * | 2017-02-01 | 2025-03-24 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Derivados de n1-(4-(5-(ciclopropilmetil)-1-metil-1h-pirazol-4-il) piridin-2-il) ciclohexano-1,4-diamina y compuestos relacionados como inhibidores de ck1 y/o irak1 para tratar cáncer. |
| WO2019155468A1 (en) | 2018-02-08 | 2019-08-15 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use |
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2016
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- 2016-08-04 PT PT167537091T patent/PT3331877T/pt unknown
- 2016-08-04 RU RU2018107668A patent/RU2735522C2/ru active
- 2016-08-04 MX MX2018001395A patent/MX384172B/es unknown
- 2016-08-04 CN CN201680059148.XA patent/CN108137562B/zh active Active
- 2016-08-04 SI SI201631426T patent/SI3331877T1/sl unknown
- 2016-08-04 ES ES16753709T patent/ES2901349T3/es active Active
- 2016-08-04 WO PCT/IL2016/050852 patent/WO2017021969A1/en not_active Ceased
- 2016-08-04 KR KR1020187006128A patent/KR102698366B1/ko active Active
- 2016-08-04 AU AU2016304464A patent/AU2016304464B2/en active Active
- 2016-08-04 PL PL16753709T patent/PL3331877T3/pl unknown
- 2016-08-04 DK DK16753709.1T patent/DK3331877T3/da active
- 2016-08-04 RS RS20211558A patent/RS62728B1/sr unknown
- 2016-08-04 SM SM20210720T patent/SMT202100720T1/it unknown
- 2016-08-04 EP EP16753709.1A patent/EP3331877B1/en active Active
- 2016-08-04 HR HRP20211949TT patent/HRP20211949T1/hr unknown
- 2016-08-04 LT LTEPPCT/IL2016/050852T patent/LT3331877T/lt unknown
- 2016-08-04 CA CA2994644A patent/CA2994644A1/en active Pending
- 2016-08-04 HU HUE16753709A patent/HUE057607T2/hu unknown
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2018
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- 2018-01-31 ZA ZA2018/00671A patent/ZA201800671B/en unknown
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2019
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2021
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- 2021-03-29 US US17/215,959 patent/US11925641B2/en active Active
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2024
- 2024-02-05 US US18/432,931 patent/US20250049793A1/en active Pending
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