JP5735526B2 - 三環式ピラゾールアミン誘導体 - Google Patents
三環式ピラゾールアミン誘導体 Download PDFInfo
- Publication number
- JP5735526B2 JP5735526B2 JP2012538350A JP2012538350A JP5735526B2 JP 5735526 B2 JP5735526 B2 JP 5735526B2 JP 2012538350 A JP2012538350 A JP 2012538350A JP 2012538350 A JP2012538350 A JP 2012538350A JP 5735526 B2 JP5735526 B2 JP 5735526B2
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- JP
- Japan
- Prior art keywords
- het
- formula
- nhso
- pyrazole
- compound
- 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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- 0 C*(*)C1=CC=C2I(C)CC(C(C(*3C*(*)COCC3)=O)=**3*)=C3C2=CC1 Chemical compound C*(*)C1=CC=C2I(C)CC(C(C(*3C*(*)COCC3)=O)=**3*)=C3C2=CC1 0.000 description 11
- CSCGUYSWGSJUJN-ARTHODIWSA-N CC(/C=C(/C)\[C@H](C1)SCC=C1N(C)N)N=O Chemical compound CC(/C=C(/C)\[C@H](C1)SCC=C1N(C)N)N=O CSCGUYSWGSJUJN-ARTHODIWSA-N 0.000 description 1
- DWHSASWNVZSFMT-UHFFFAOYSA-N CC(C)(c1c(C2=C3C=CCC2)[n](-c2ccccc2)nc1C(N1CCOCC1)=O)S3(=O)=O Chemical compound CC(C)(c1c(C2=C3C=CCC2)[n](-c2ccccc2)nc1C(N1CCOCC1)=O)S3(=O)=O DWHSASWNVZSFMT-UHFFFAOYSA-N 0.000 description 1
- CFHVJWPSKFYAKY-UHFFFAOYSA-N CC(C)C(C(S(C1)(=O)=O)=C(C(C)=C)c2c1c(C(O)=O)n[n]2C)F Chemical compound CC(C)C(C(S(C1)(=O)=O)=C(C(C)=C)c2c1c(C(O)=O)n[n]2C)F CFHVJWPSKFYAKY-UHFFFAOYSA-N 0.000 description 1
- NWZVZHGLMDYDOP-UHFFFAOYSA-N CCCOCCNC Chemical compound CCCOCCNC NWZVZHGLMDYDOP-UHFFFAOYSA-N 0.000 description 1
- CILFXFVAUNMKFI-UHFFFAOYSA-N CCN(CCOC)C(c1n[n](CCNC)c(C2=C3C=CCC2)c1CS3(COC)=O)=O Chemical compound CCN(CCOC)C(c1n[n](CCNC)c(C2=C3C=CCC2)c1CS3(COC)=O)=O CILFXFVAUNMKFI-UHFFFAOYSA-N 0.000 description 1
- QQGMORONNSQQAO-CLTKARDFSA-N CCOC(c(c(C1)c2C=C(/C=C\C)S1(=O)=O)n[n]2-c(cccc1)c1F)=O Chemical compound CCOC(c(c(C1)c2C=C(/C=C\C)S1(=O)=O)n[n]2-c(cccc1)c1F)=O QQGMORONNSQQAO-CLTKARDFSA-N 0.000 description 1
- QTQPSEDAPBJFFD-UHFFFAOYSA-N CCOC(c(c1c2-c(cccc3)c3SC1)n[n]2-c1ccc(C)cc1)=O Chemical compound CCOC(c(c1c2-c(cccc3)c3SC1)n[n]2-c1ccc(C)cc1)=O QTQPSEDAPBJFFD-UHFFFAOYSA-N 0.000 description 1
- BLJJFMCTIXBXGP-UHFFFAOYSA-O CCOC(c(c1c2-c(cccc3)c3[SH+]C1)n[n]2-c1ccc(CO)cc1)=O Chemical compound CCOC(c(c1c2-c(cccc3)c3[SH+]C1)n[n]2-c1ccc(CO)cc1)=O BLJJFMCTIXBXGP-UHFFFAOYSA-O 0.000 description 1
- YWRCZVNEAYSLAB-UHFFFAOYSA-N CCOC(c(c1c2-c3ccccc3SC1)n[n]2-c(cc1)cc2c1nc(C)[s]2)=O Chemical compound CCOC(c(c1c2-c3ccccc3SC1)n[n]2-c(cc1)cc2c1nc(C)[s]2)=O YWRCZVNEAYSLAB-UHFFFAOYSA-N 0.000 description 1
- HZOOVSDCIIZYPU-UHFFFAOYSA-N CCOC(c(nc1)c2[n]1-c(cccc1)c1SC2)=O Chemical compound CCOC(c(nc1)c2[n]1-c(cccc1)c1SC2)=O HZOOVSDCIIZYPU-UHFFFAOYSA-N 0.000 description 1
- NRULIRPKJVMPDY-UHFFFAOYSA-N C[n]1nc(C(N2CCOCC2)=O)c(CS(c2c3)(=O)=O)c1-c2ccc3OC Chemical compound C[n]1nc(C(N2CCOCC2)=O)c(CS(c2c3)(=O)=O)c1-c2ccc3OC NRULIRPKJVMPDY-UHFFFAOYSA-N 0.000 description 1
- LMHALRWGVJFYLA-UHFFFAOYSA-N Oc1cc(-[n]2nc(C(N3CCOCC3)=O)c3c2-c(cccc2)c2SC3)ccc1 Chemical compound Oc1cc(-[n]2nc(C(N3CCOCC3)=O)c3c2-c(cccc2)c2SC3)ccc1 LMHALRWGVJFYLA-UHFFFAOYSA-N 0.000 description 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
-
- 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
-
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A61P19/04—Drugs for skeletal disorders for non-specific disorders of the connective tissue
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- A—HUMAN NECESSITIES
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- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P5/14—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4
- A61P5/16—Drugs for disorders of the endocrine system of the thyroid hormones, e.g. T3, T4 for decreasing, blocking or antagonising the activity of the thyroid hormones
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- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Immunology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Neurosurgery (AREA)
- Virology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Communicable Diseases (AREA)
- Emergency Medicine (AREA)
- Oncology (AREA)
- Molecular Biology (AREA)
- Transplantation (AREA)
- Obesity (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Reproductive Health (AREA)
- Gastroenterology & Hepatology (AREA)
- Epidemiology (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09175933 | 2009-11-13 | ||
| EP09175933.2 | 2009-11-13 | ||
| US26185409P | 2009-11-17 | 2009-11-17 | |
| US61/261,854 | 2009-11-17 | ||
| PCT/EP2010/067412 WO2011058149A1 (en) | 2009-11-13 | 2010-11-12 | Tricyclic pyrazol amine derivatives |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013510825A JP2013510825A (ja) | 2013-03-28 |
| JP2013510825A5 JP2013510825A5 (enExample) | 2014-01-09 |
| JP5735526B2 true JP5735526B2 (ja) | 2015-06-17 |
Family
ID=41796476
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2012538350A Active JP5735526B2 (ja) | 2009-11-13 | 2010-11-12 | 三環式ピラゾールアミン誘導体 |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US9073940B2 (enExample) |
| EP (1) | EP2499146B1 (enExample) |
| JP (1) | JP5735526B2 (enExample) |
| KR (1) | KR20130049766A (enExample) |
| CN (1) | CN102695710B (enExample) |
| AR (1) | AR078979A1 (enExample) |
| AU (1) | AU2010317883B2 (enExample) |
| CA (1) | CA2778174C (enExample) |
| EA (1) | EA201290305A1 (enExample) |
| ES (1) | ES2607952T3 (enExample) |
| IL (1) | IL219602A (enExample) |
| MX (1) | MX2012005518A (enExample) |
| WO (1) | WO2011058149A1 (enExample) |
| ZA (1) | ZA201202641B (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9044451B2 (en) | 2010-07-19 | 2015-06-02 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Use of delta tocopherol for the treatment of lysosomal storage disorders |
| DE102011055815A1 (de) | 2011-11-29 | 2013-05-29 | Aicuris Gmbh & Co. Kg | Carboxamid-substituierte Heteroaryl-Pyrazole und ihre Verwendung |
| ES2661510T3 (es) | 2011-12-15 | 2018-04-02 | Novartis Ag | Uso de inhibidores de la actividad o función de PI3K |
| DE102012016908A1 (de) | 2012-08-17 | 2014-02-20 | Aicuris Gmbh & Co. Kg | Tris-(Hetero)Aryl-Pyrazole und ihre Verwendung |
| JP6367211B2 (ja) * | 2012-11-16 | 2018-08-01 | ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ | リソソーム蓄積症の改善物質としてのトコフェロール誘導体およびトコフェリルキノン誘導体 |
| WO2014121901A1 (en) | 2013-02-07 | 2014-08-14 | Merck Patent Gmbh | Polymorphic forms |
| RU2663898C2 (ru) * | 2013-06-24 | 2018-08-13 | Мерк Патент Гмбх | Пиразольные соединения в качестве модуляторов fshr и их применение |
| WO2015196335A1 (en) * | 2014-06-23 | 2015-12-30 | Tocopherx, Inc. | Pyrazole compounds as modulators of fshr and uses thereof |
| AU2016313263B2 (en) | 2015-08-26 | 2021-02-04 | Fundación Del Sector Público Estatal Centro Nacional De Investigaciones Oncológicas Carlos III (F.S.P. CNIO) | Condensed tricyclic compounds as protein kinase inhibitors |
| TW201837026A (zh) | 2017-01-10 | 2018-10-16 | 德商拜耳廠股份有限公司 | 作為除害劑之雜環衍生物（二） |
| KR102515694B1 (ko) | 2017-01-10 | 2023-03-29 | 바이엘 악티엔게젤샤프트 | 해충 방제제로서의 헤테로사이클 유도체 |
| CN108434150B (zh) * | 2018-02-09 | 2020-03-10 | 天津医科大学总医院 | Zstk474用于制备ean治疗药物的应用 |
| EP3608326A1 (en) * | 2018-08-10 | 2020-02-12 | Irbm S.P.A. | Tricyclic inhibitors of hepatitis b virus |
| CN113754678B (zh) * | 2020-06-02 | 2023-03-10 | 江苏恒瑞医药股份有限公司 | 二氢硫代色烯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| CN113754685B (zh) * | 2020-06-02 | 2023-06-16 | 江苏恒瑞医药股份有限公司 | 二氢硫代色烯并吡唑类衍生物、其制备方法及其在医药上的应用 |
| BR112022026904A2 (pt) | 2020-07-02 | 2023-01-24 | Bayer Ag | Derivados de heterocicleno como agentes de controle de pragas |
| WO2022007924A1 (zh) * | 2020-07-09 | 2022-01-13 | 江苏恒瑞医药股份有限公司 | 氧杂氮杂双环类衍生物、其制备方法及其在医药上的应用 |
| WO2022022630A1 (zh) | 2020-07-29 | 2022-02-03 | 江苏恒瑞医药股份有限公司 | 氧杂氮杂螺环类衍生物、其制备方法及其在医药上的应用 |
| GB202117511D0 (en) * | 2021-12-03 | 2022-01-19 | Ionctura Sa | Treatment regimens |
| FI4313058T3 (fi) * | 2021-03-29 | 2025-04-30 | Ionctura Sa | Roginolisibia käsittävä koostumus ja annosteluohjelma syövän tai tulehdus- tai autoimmunisairauden hoitoon |
| JP2024511836A (ja) * | 2021-03-29 | 2024-03-15 | アイオンクチュラ・ソシエテ・アノニム | 膵臓癌の治療のためのｐｉ３ｋ－デルタ阻害剤 |
| CN114524827B (zh) * | 2022-02-22 | 2024-07-09 | 深圳市儿童医院 | 一种用于治疗神经重症的吡唑衍生物及其应用 |
| CN114524828B (zh) * | 2022-02-22 | 2024-07-09 | 深圳市儿童医院 | 一种用于治疗神经重症的噻唑衍生物及其应用 |
| CN115491252B (zh) * | 2022-09-29 | 2023-05-02 | 江苏四新界面剂科技有限公司 | 一种宝石切割用低泡润湿剂及其制备方法 |
| WO2024184266A1 (en) | 2023-03-03 | 2024-09-12 | Ionctura Sa | Combination of roginolisib and hdac inhibitor in the treatment of haematological malignancy |
| JP2026510567A (ja) | 2023-03-03 | 2026-04-08 | アイオンクチュラ・ソシエテ・アノニム | 血液悪性腫瘍の治療におけるロギノリシブ及びｂｃｌ－２阻害剤の組み合わせ |
| GB202308807D0 (en) | 2023-06-13 | 2023-07-26 | Ionctura Sa | Combinations |
| AU2024357109A1 (en) | 2023-10-06 | 2026-03-12 | Ionctura Sa | Combination of roginolisib with a malt1-gls inhibitor |
| WO2025195504A1 (zh) * | 2024-03-22 | 2025-09-25 | 复旦大学附属中山医院 | 三环骨架化合物及其在制备抗肿瘤药物中的应用 |
| TWI926701B (zh) * | 2024-03-22 | 2026-05-21 | 復旦大學附屬中山醫院 | 三環骨架化合物及其在製備抗腫瘤藥物的應用 |
| GB202418087D0 (en) | 2024-12-10 | 2025-01-22 | Ionctura Sa | Biomarkers |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4816467A (en) | 1987-01-09 | 1989-03-28 | Farmitalia Carlo Erba S.R.L | Heteroaryl 3-oxo-propanenitrile derivatives, pharmaceutical compositions and use |
| GB8814586D0 (en) * | 1988-06-20 | 1988-07-27 | Erba Carlo Spa | Tricyclic 3-oxo-propanenitrile derivatives & process for their preparation |
| GB8907799D0 (en) * | 1989-04-06 | 1989-05-17 | Erba Carlo Spa | Heteroaryl-3-oxo-propanenitrile derivatives useful in the treatment of rheumatoid arthritis and other autoimmune diseases |
| GB8916290D0 (en) * | 1989-07-17 | 1989-08-31 | Erba Carlo Spa | Heteroaryl-3-oxo-propanenitrile derivatives useful in stimulating myelopoiesis |
| JP3542826B2 (ja) | 1994-07-11 | 2004-07-14 | 帝国臓器製薬株式会社 | 新規な二環式化合物縮合［２，１−ｄ］イソキサゾール−３−カルボン酸誘導体 |
| GB9720901D0 (en) * | 1997-10-01 | 1997-12-03 | Pharmacia & Upjohn Spa | Condensed benzothiopyranic compounds |
| FR2800375B1 (fr) * | 1999-11-03 | 2004-07-23 | Sanofi Synthelabo | Derives tricycliques d'acide pyrazolecarboxylique, leur preparation, les compositions pharmaceutiques en contenant |
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| MXPA05000453A (es) | 2002-07-10 | 2005-03-23 | Applied Research Systems | Derivados de benceno fusionados a azolidinona-vinilo. |
| WO2004056820A1 (en) | 2002-12-20 | 2004-07-08 | Warner-Lambert Company Llc | Benzoxazines and derivatives thereof as inhibitors of pi3ks |
| GB0305152D0 (en) | 2003-03-06 | 2003-04-09 | Novartis Ag | Organic compounds |
| GB0320197D0 (en) | 2003-08-28 | 2003-10-01 | Novartis Ag | Organic compounds |
| US7691888B2 (en) | 2004-10-07 | 2010-04-06 | Boehringer Ingelheim International Gmbh | Thiazolyl-dihydro-indazole |
| CA2633500A1 (en) | 2005-12-20 | 2007-07-05 | President And Fellows Of Harvard College | Compounds, screens, and methods of treatment |
| WO2008035356A2 (en) | 2006-09-20 | 2008-03-27 | Glenmark Pharmaceuticals Limited | Novel cannabinoid receptor ligands, pharmaceutical compositions containing them, and process for their preparation |
| WO2009010824A1 (en) | 2007-07-13 | 2009-01-22 | Glenmark Pharmaceuticals, S.A. | Dihydrochromenopyrazole derivatives as vanilloid receptor ligands |
| WO2009071895A1 (en) * | 2007-12-04 | 2009-06-11 | Ucb Pharma S.A. | Fused thiazole and thiophene derivatives as kinase inhibitors |
| ES2480994T3 (es) | 2008-03-31 | 2014-07-29 | Genentech, Inc. | Compuestos de tipo benzopirano y benzoxepina inhibidores de PI3K y métodos de uso |
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- 2010-11-12 KR KR1020127015183A patent/KR20130049766A/ko not_active Withdrawn
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| CA2778174A1 (en) | 2011-05-19 |
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| US20120238545A1 (en) | 2012-09-20 |
| AU2010317883A1 (en) | 2012-05-03 |
| IL219602A0 (en) | 2012-07-31 |
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| EP2499146B1 (en) | 2016-09-21 |
| CN102695710A (zh) | 2012-09-26 |
| AU2010317883B2 (en) | 2015-08-06 |
| WO2011058149A1 (en) | 2011-05-19 |
| MX2012005518A (es) | 2012-06-19 |
| CN102695710B (zh) | 2015-08-19 |
| IL219602A (en) | 2017-04-30 |
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