SG11201906681PA - N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer - Google Patents
N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancerInfo
- Publication number
- SG11201906681PA SG11201906681PA SG11201906681PA SG11201906681PA SG11201906681PA SG 11201906681P A SG11201906681P A SG 11201906681PA SG 11201906681P A SG11201906681P A SG 11201906681PA SG 11201906681P A SG11201906681P A SG 11201906681PA SG 11201906681P A SG11201906681P A SG 11201906681PA
- Authority
- SG
- Singapore
- Prior art keywords
- international
- cyclopropylmethyl
- pyrazol
- pyridin
- cyclohexane
- Prior art date
Links
- 206010028980 Neoplasm Diseases 0.000 title abstract 3
- 201000011510 cancer Diseases 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 239000003112 inhibitor Substances 0.000 title abstract 3
- XREIADPMSAUOHY-UHFFFAOYSA-N 4-N-[4-[5-(cyclopropylmethyl)-1-methylpyrazol-4-yl]pyridin-2-yl]cyclohexane-1,4-diamine Chemical class C1(CC1)CC1=C(C=NN1C)C1=CC(=NC=C1)NC1CCC(CC1)N XREIADPMSAUOHY-UHFFFAOYSA-N 0.000 title abstract 2
- 102000008122 Casein Kinase I Human genes 0.000 abstract 3
- 108010049812 Casein Kinase I Proteins 0.000 abstract 3
- 102000006940 Interleukin-1 Receptor-Associated Kinases Human genes 0.000 abstract 3
- 108010072621 Interleukin-1 Receptor-Associated Kinases Proteins 0.000 abstract 3
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 241000234282 Allium Species 0.000 abstract 1
- 235000002732 Allium cepa var. cepa Nutrition 0.000 abstract 1
- FNFMQIWXTYFRKA-UHFFFAOYSA-N cyclohexane-1,4-diamine Chemical class NC1[CH]CC(N)CC1 FNFMQIWXTYFRKA-UHFFFAOYSA-N 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- VIKNJXKGJWUCNN-XGXHKTLJSA-N norethisterone Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](C)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 VIKNJXKGJWUCNN-XGXHKTLJSA-N 0.000 abstract 1
- 230000008520 organization Effects 0.000 abstract 1
- 150000003217 pyrazoles Chemical class 0.000 abstract 1
- 102220240796 rs553605556 Human genes 0.000 abstract 1
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
- C07D401/02—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 two hetero rings
- C07D401/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/425—Thiazoles
- A61K31/427—Thiazoles 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
- A61K31/435—Heterocyclic 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- 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
- 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
- C07D403/14—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
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
International Patent Classification: CO7D 401/04 (2006.01) A61K 31/506 (2006.01) CO7D 403/04 (2006.01) A61K 31/4155 (2006.01) C07D 417/04 (2006.01) A61K 31/427 (2006.01) A61K 31/4439 (2006.01) A61P 35/00 (2006.01) (21) International Application Number: (12) INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property Organization International Bureau (43) International Publication Date 09 August 2018 (09.08.2018) WIPO I PCT omit °nolo milli offi onion° oimIE (10) International Publication Number WO 2018/142393 Al PCT/IL2018/050100 (22) International Filing Date: 30 January 2018 (30.01.2018) (25) Filing Language: English (26) Publication Language: English (30) Priority Data: 62/453,192 01 February 2017 (01.02.2017) US (71) Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW [IL/IL]; Hi Tech Park, Edmond J. Safra Campus, Givat Ram, 9139002 Jerusalem (IL). (72) Inventors: LI, Dansu; 2690 Fawn Lane, Warrington, Pennsylvania 18976 (US). SNIR-ALKALAY, Irit; 63/3 Habosem St., 9076901 Mevasseret Zion (IL). VACCA, Joseph; 733 Indian Creek Road, Telford, Pennsylvania 18969 (US). BEN-NERIAH, Yinon; 5 Mevo Duvdevan St., POB 1691, 9071923 Mevasseret Zion (IL). VENKAT- AC-IALAM, Avanthika; Jerusalem (IL). (74) Agent: VOLMAN, Gail; Dr. Shlomo Cohen & Co., B. S. R Tower 3, 5 Kineret St., 5126237 Bnei Brak (IL). (81) Designated States (unless otherwise indicated, for every kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW. (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, TJ, TM), European (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Published: — with international search report (Art. 21(3)) (54) Title: N1 -(4-(5-(CYCLOPROPYLMETHYL)-1 -METHYL-1 H-PYRAZOL-4-YL)PYRIDIN-2-YL)CYCLOHEXANE-1,4- DIAMINE DERIVATIVES AND RELATED COMPOUNDS AS CK1 AND/OR IRAKI INHIBITORS FOR TREATING CANCER W O 20 18/ 142393 Al R2 (57) : The present invention provides pyra- zole derivatives of Formula (I), and in par- ticular N1 -(4-(5-(cyclopropylmethyl)-1 -methy1-1H-pyrazol-4-y1) pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related com- pounds as casein kinase 1 (CK1) and/or interleukin 1 receptor asso- ciated kinase 1 (IRAKI) inhibitors for treating cancer, inflammatory and immune related disorders. (I)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762453192P | 2017-02-01 | 2017-02-01 | |
| PCT/IL2018/050100 WO2018142393A1 (en) | 2017-02-01 | 2018-01-30 | N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SG11201906681PA true SG11201906681PA (en) | 2019-08-27 |
Family
ID=61198874
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SG11201906681PA SG11201906681PA (en) | 2017-02-01 | 2018-01-30 | N1 -(4-(5-(cyclopropylmethyl)-1 -methyl-1 h-pyrazol-4-yl)pyridin-2-yl)cyclohexane-1,4-diamine derivatives and related compounds as ck1 and/or iraki inhibitors for treating cancer |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US11072599B2 (en) |
| EP (1) | EP3577108B1 (en) |
| JP (1) | JP7142646B2 (en) |
| KR (1) | KR20190115017A (en) |
| CN (1) | CN110475771B (en) |
| AU (1) | AU2018215809B2 (en) |
| CA (1) | CA3052247A1 (en) |
| ES (1) | ES2902885T3 (en) |
| IL (1) | IL268128B2 (en) |
| MX (1) | MX394556B (en) |
| NZ (1) | NZ755447A (en) |
| RU (1) | RU2761457C2 (en) |
| SG (1) | SG11201906681PA (en) |
| TW (1) | TW201837027A (en) |
| WO (1) | WO2018142393A1 (en) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2901349T3 (en) * | 2015-08-04 | 2022-03-22 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Pyrazole pyrimidine derivative and uses thereof |
| AU2019219678A1 (en) * | 2018-02-08 | 2020-08-27 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd. | Heteroaryl compounds, pharmaceutical compositions thereof, and their therapeutic use |
| CN114127058B (en) * | 2019-07-04 | 2024-06-25 | 深圳国顺康医药科技有限公司 | A heterocyclic compound, its pharmaceutical composition and use |
| KR20230069169A (en) * | 2020-09-17 | 2023-05-18 | 얀센 파마슈티카 엔.브이. | casein kinase 1 delta modulator |
| JP2024517792A (en) * | 2021-04-28 | 2024-04-23 | コーネル・ユニバーシティー | Soluble adenylyl cyclase (sAC) inhibitors and uses thereof |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007129195A2 (en) | 2006-05-04 | 2007-11-15 | Pfizer Products Inc. | 4-pyrimidine-5-amino-pyrazole compounds |
| MX340490B (en) * | 2010-07-13 | 2016-07-11 | F Hoffmann-La Roche Ag * | Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators. |
| ES2650744T3 (en) | 2010-12-14 | 2018-01-22 | Electrophoretics Limited | Casein kinase 1 delta inhibitors (CK1delta) |
| RU2674017C2 (en) | 2011-11-04 | 2018-12-04 | ДЖАСКО ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Aminopyrimidine kinase inhibitors |
| BR112016006319A2 (en) | 2013-09-27 | 2017-08-01 | Nimbus Iris Inc | irak inhibitors and uses thereof |
| JP6491202B2 (en) * | 2013-10-18 | 2019-03-27 | デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド | Polycyclic inhibitors of cyclin dependent kinase 7 (CDK 7) |
| NZ730728A (en) * | 2014-11-20 | 2022-04-29 | Merck Patent Gmbh | Heteroaryl compounds as irak inhibitors and uses thereof |
| JP6827948B2 (en) | 2015-03-23 | 2021-02-10 | ザ ユニヴァーシティー オブ メルボルン | Treatment of respiratory diseases |
| ES2901349T3 (en) * | 2015-08-04 | 2022-03-22 | Yissum Res Dev Co Of Hebrew Univ Jerusalem Ltd | Pyrazole pyrimidine derivative and uses thereof |
-
2018
- 2018-01-30 US US16/482,199 patent/US11072599B2/en active Active
- 2018-01-30 IL IL268128A patent/IL268128B2/en unknown
- 2018-01-30 MX MX2019009083A patent/MX394556B/en unknown
- 2018-01-30 ES ES18705024T patent/ES2902885T3/en active Active
- 2018-01-30 TW TW107103255A patent/TW201837027A/en unknown
- 2018-01-30 AU AU2018215809A patent/AU2018215809B2/en not_active Ceased
- 2018-01-30 KR KR1020197025024A patent/KR20190115017A/en not_active Ceased
- 2018-01-30 CN CN201880022829.8A patent/CN110475771B/en not_active Expired - Fee Related
- 2018-01-30 JP JP2019561389A patent/JP7142646B2/en active Active
- 2018-01-30 NZ NZ755447A patent/NZ755447A/en unknown
- 2018-01-30 WO PCT/IL2018/050100 patent/WO2018142393A1/en not_active Ceased
- 2018-01-30 SG SG11201906681PA patent/SG11201906681PA/en unknown
- 2018-01-30 CA CA3052247A patent/CA3052247A1/en active Pending
- 2018-01-30 EP EP18705024.0A patent/EP3577108B1/en active Active
- 2018-01-30 RU RU2019127038A patent/RU2761457C2/en active
-
2021
- 2021-07-26 US US17/384,922 patent/US11999721B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| NZ755447A (en) | 2023-05-26 |
| JP7142646B2 (en) | 2022-09-27 |
| ES2902885T8 (en) | 2022-04-06 |
| RU2019127038A (en) | 2021-03-02 |
| IL268128B2 (en) | 2023-03-01 |
| MX394556B (en) | 2025-03-24 |
| IL268128A (en) | 2019-09-26 |
| JP2020505468A (en) | 2020-02-20 |
| WO2018142393A1 (en) | 2018-08-09 |
| EP3577108B1 (en) | 2021-10-20 |
| AU2018215809B2 (en) | 2021-12-23 |
| EP3577108A1 (en) | 2019-12-11 |
| CN110475771B (en) | 2022-09-02 |
| KR20190115017A (en) | 2019-10-10 |
| IL268128B (en) | 2022-11-01 |
| CA3052247A1 (en) | 2018-08-09 |
| TW201837027A (en) | 2018-10-16 |
| US20200354340A1 (en) | 2020-11-12 |
| US11072599B2 (en) | 2021-07-27 |
| US20220017493A1 (en) | 2022-01-20 |
| CN110475771A (en) | 2019-11-19 |
| US11999721B2 (en) | 2024-06-04 |
| AU2018215809A1 (en) | 2019-08-15 |
| ES2902885T3 (en) | 2022-03-30 |
| RU2019127038A3 (en) | 2021-03-17 |
| MX2019009083A (en) | 2019-09-10 |
| RU2761457C2 (en) | 2021-12-08 |
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