JP2018510135A - RORγT阻害剤としての置換ピラゾール化合物及びその使用 - Google Patents
RORγT阻害剤としての置換ピラゾール化合物及びその使用 Download PDFInfo
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- JP2018510135A JP2018510135A JP2017541959A JP2017541959A JP2018510135A JP 2018510135 A JP2018510135 A JP 2018510135A JP 2017541959 A JP2017541959 A JP 2017541959A JP 2017541959 A JP2017541959 A JP 2017541959A JP 2018510135 A JP2018510135 A JP 2018510135A
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- Prior art keywords
- chloro
- alkyl
- tetrahydro
- mmol
- cyclopropylbenzoyl
- Prior art date
- Legal status (The legal status 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 status listed.)
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- UYPAVTZCVXPFAQ-UHFFFAOYSA-N CC(C)(C)OC(NC(CC1)Cc2c1c(-c(c(F)c1)ccc1C(O)=O)n[n]2C(c(c(C1CC1)ccc1)c1Cl)=O)=O Chemical compound CC(C)(C)OC(NC(CC1)Cc2c1c(-c(c(F)c1)ccc1C(O)=O)n[n]2C(c(c(C1CC1)ccc1)c1Cl)=O)=O UYPAVTZCVXPFAQ-UHFFFAOYSA-N 0.000 description 1
- BCSXUVZTKVXBSD-UHFFFAOYSA-N CC(CNCC1)C1N Chemical compound CC(CNCC1)C1N BCSXUVZTKVXBSD-UHFFFAOYSA-N 0.000 description 1
- XBIUTTXWWURGHK-UHFFFAOYSA-N CCc1n[n](C(c2c(C3CC3)cccc2Cl)=O)c(C2)c1CCC2NC(OC(C)(C)C)=O Chemical compound CCc1n[n](C(c2c(C3CC3)cccc2Cl)=O)c(C2)c1CCC2NC(OC(C)(C)C)=O XBIUTTXWWURGHK-UHFFFAOYSA-N 0.000 description 1
- IUAVAKAEXAAZAL-UHFFFAOYSA-N COC(C(CC1)Cc2c1c(I)n[n]2C(c1c(C2CC2)cccc1Cl)=O)=O Chemical compound COC(C(CC1)Cc2c1c(I)n[n]2C(c1c(C2CC2)cccc1Cl)=O)=O IUAVAKAEXAAZAL-UHFFFAOYSA-N 0.000 description 1
- BKWRLCIYMAYFPA-UHFFFAOYSA-N COC(c1cc(F)c(B(O)O)cc1)=O Chemical compound COC(c1cc(F)c(B(O)O)cc1)=O BKWRLCIYMAYFPA-UHFFFAOYSA-N 0.000 description 1
- AZHMCMMGUMQQHX-UHFFFAOYSA-N Ic1n[nH]c2c1CCCC2 Chemical compound Ic1n[nH]c2c1CCCC2 AZHMCMMGUMQQHX-UHFFFAOYSA-N 0.000 description 1
- ZKHDOWBUYPIKLV-UHFFFAOYSA-N O=C(c1c(C2CC2)cccc1Cl)Cl Chemical compound O=C(c1c(C2CC2)cccc1Cl)Cl ZKHDOWBUYPIKLV-UHFFFAOYSA-N 0.000 description 1
- ZNZLEMZPQHWNBS-UHFFFAOYSA-N O=C(c1c(C2CC2)cccc1Cl)[n](c1c2CCCC1)nc2I Chemical compound O=C(c1c(C2CC2)cccc1Cl)[n](c1c2CCCC1)nc2I ZNZLEMZPQHWNBS-UHFFFAOYSA-N 0.000 description 1
- HCYXHSKXTROMDM-UHFFFAOYSA-N O=C(c1c(C2CCC2)cccc1Cl)[n](c1c2CCCC1)nc2I Chemical compound O=C(c1c(C2CCC2)cccc1Cl)[n](c1c2CCCC1)nc2I HCYXHSKXTROMDM-UHFFFAOYSA-N 0.000 description 1
- RTLRDIAWRKKVFT-UHFFFAOYSA-N OC(c1c(C2CC2)cccc1Cl)=O Chemical compound OC(c1c(C2CC2)cccc1Cl)=O RTLRDIAWRKKVFT-UHFFFAOYSA-N 0.000 description 1
- OUGLIVSISBKMIE-UHFFFAOYSA-N OCC(CC1)Cc2c1c(-c(ccc(C(O)=O)c1)c1F)n[n]2C(c(c(C1CC1)ccc1)c1Cl)=O Chemical compound OCC(CC1)Cc2c1c(-c(ccc(C(O)=O)c1)c1F)n[n]2C(c(c(C1CC1)ccc1)c1Cl)=O OUGLIVSISBKMIE-UHFFFAOYSA-N 0.000 description 1
- GORQVVQHYIPFBT-UHFFFAOYSA-N OCC(CC1)Cc2c1c(I)n[n]2C(c1c(C2CC2)cccc1Cl)=O Chemical compound OCC(CC1)Cc2c1c(I)n[n]2C(c1c(C2CC2)cccc1Cl)=O GORQVVQHYIPFBT-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
- C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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- 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
- A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- 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
- C07D403/12—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 chain containing hetero atoms as chain links
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- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
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- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Neurology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Physical Education & Sports Medicine (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Hospice & Palliative Care (AREA)
- Tropical Medicine & Parasitology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562114854P | 2015-02-11 | 2015-02-11 | |
| US62/114,854 | 2015-02-11 | ||
| PCT/US2016/017566 WO2016130818A1 (en) | 2015-02-11 | 2016-02-11 | SUBSTITUTED PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018510135A true JP2018510135A (ja) | 2018-04-12 |
| JP2018510135A5 JP2018510135A5 (https=) | 2019-03-07 |
Family
ID=56614908
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017541959A Pending JP2018510135A (ja) | 2015-02-11 | 2016-02-11 | RORγT阻害剤としての置換ピラゾール化合物及びその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10221142B2 (https=) |
| EP (1) | EP3256450B1 (https=) |
| JP (1) | JP2018510135A (https=) |
| AU (1) | AU2016219183B2 (https=) |
| CA (1) | CA2975997A1 (https=) |
| WO (1) | WO2016130818A1 (https=) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2021527650A (ja) * | 2018-06-15 | 2021-10-14 | リアタ ファーマシューティカルズ インコーポレイテッド | IL−17およびRORγの阻害用のピラゾール化合物およびイミダゾール化合物 |
| JP2024501520A (ja) * | 2020-12-22 | 2024-01-12 | メルク・シャープ・アンド・ドーム・エルエルシー | 新規ジアシルグリセリドo-アシルトランスフェラーゼ2阻害薬としてのテトラヒドロインダゾール誘導体の調製 |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015095795A1 (en) | 2013-12-20 | 2015-06-25 | Merck Sharp & Dohme Corp. | TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE |
| EP3256450B1 (en) | 2015-02-11 | 2020-12-02 | Merck Sharp & Dohme Corp. | Substituted pyrazole compounds as ror-gamma-t inhibitors and uses thereof |
| WO2017075178A1 (en) * | 2015-10-27 | 2017-05-04 | Merck Sharp & Dohme Corp. | SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| AU2016344118A1 (en) | 2015-10-27 | 2018-05-10 | Merck Sharp & Dohme Corp. | Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof |
| RU2018117503A (ru) * | 2015-10-27 | 2019-11-28 | Мерк Шарп И Доум Корп. | ЗАМЕЩЕННЫЕ ИНДАЗОЛЬНЫЕ СОЕДИНЕНИЯ В КАЧЕСТВЕ ИНГИБИТОРОВ RORγТ И ИХ ПРИМЕНЕНИЕ |
| EP3806958B1 (en) * | 2018-06-18 | 2022-09-07 | Janssen Pharmaceutica NV | 6-aminopyridin-3-yl pyrazoles as modulators of roryt |
| WO2020117715A1 (en) | 2018-12-03 | 2020-06-11 | Board Of Regents, The University Of Texas System | Oligo-benzamide analogs and their use in cancer treatment |
| US12398097B2 (en) | 2019-07-29 | 2025-08-26 | Vanderbilt University | WDR5-MYC inhibitors |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2007505908A (ja) * | 2003-09-17 | 2007-03-15 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | 縮合複素環式化合物 |
| WO2014028591A2 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | N-ALKYLATED INDOLE AND INDAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
| WO2014028589A2 (en) * | 2012-08-15 | 2014-02-20 | Merck Sharp & Dohme Corp. | 4-HETEROARYL SUBSTITUTED BENZOIC ACID COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF |
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| WO2015139621A1 (zh) * | 2014-03-18 | 2015-09-24 | 北京韩美药品有限公司 | 4-杂芳基取代的苯甲酸或苯甲酰胺类化合物 |
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| US10221142B2 (en) | 2019-03-05 |
| EP3256450A4 (en) | 2018-05-30 |
| AU2016219183B2 (en) | 2020-06-11 |
| US20180016239A1 (en) | 2018-01-18 |
| CA2975997A1 (en) | 2016-08-18 |
| EP3256450A1 (en) | 2017-12-20 |
| EP3256450B1 (en) | 2020-12-02 |
| WO2016130818A1 (en) | 2016-08-18 |
| AU2016219183A1 (en) | 2017-08-24 |
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