JP6505682B2 - ヘテロ環式化合物およびそれらの使用方法 - Google Patents
ヘテロ環式化合物およびそれらの使用方法 Download PDFInfo
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- JP6505682B2 JP6505682B2 JP2016524633A JP2016524633A JP6505682B2 JP 6505682 B2 JP6505682 B2 JP 6505682B2 JP 2016524633 A JP2016524633 A JP 2016524633A JP 2016524633 A JP2016524633 A JP 2016524633A JP 6505682 B2 JP6505682 B2 JP 6505682B2
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- Prior art keywords
- nhc
- phenyl
- alkyl
- alkynyl
- aryl
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- 229960001052 streptozocin Drugs 0.000 description 1
- 229910052712 strontium Inorganic materials 0.000 description 1
- CIOAGBVUUVVLOB-UHFFFAOYSA-N strontium atom Chemical compound [Sr] CIOAGBVUUVVLOB-UHFFFAOYSA-N 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 239000001384 succinic acid Substances 0.000 description 1
- 235000011044 succinic acid Nutrition 0.000 description 1
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- 150000008163 sugars Chemical class 0.000 description 1
- 229950000244 sulfanilic acid Drugs 0.000 description 1
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- YROXIXLRRCOBKF-UHFFFAOYSA-N sulfonylurea Chemical class OC(=N)N=S(=O)=O YROXIXLRRCOBKF-UHFFFAOYSA-N 0.000 description 1
- MLKXDPUZXIRXEP-MFOYZWKCSA-N sulindac Chemical compound CC1=C(CC(O)=O)C2=CC(F)=CC=C2\C1=C/C1=CC=C(S(C)=O)C=C1 MLKXDPUZXIRXEP-MFOYZWKCSA-N 0.000 description 1
- 229960000894 sulindac Drugs 0.000 description 1
- 229960001796 sunitinib Drugs 0.000 description 1
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 description 1
- 239000006228 supernatant Substances 0.000 description 1
- 230000009469 supplementation Effects 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
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- 230000035900 sweating Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229960001603 tamoxifen Drugs 0.000 description 1
- 229940033123 tannic acid Drugs 0.000 description 1
- 229920002258 tannic acid Polymers 0.000 description 1
- 235000015523 tannic acid Nutrition 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 description 1
- OGBMKVWORPGQRR-UMXFMPSGSA-N teriparatide Chemical compound C([C@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@@H](N)CO)C(C)C)[C@@H](C)CC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)C1=CNC=N1 OGBMKVWORPGQRR-UMXFMPSGSA-N 0.000 description 1
- 229960005460 teriparatide Drugs 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 150000003526 tetrahydroisoquinolines Chemical class 0.000 description 1
- 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 description 1
- 125000001712 tetrahydronaphthyl group Chemical group C1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000000147 tetrahydroquinolinyl group Chemical group N1(CCCC2=CC=CC=C12)* 0.000 description 1
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 description 1
- 150000003536 tetrazoles Chemical class 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 230000004797 therapeutic response Effects 0.000 description 1
- 230000036575 thermal burns Effects 0.000 description 1
- 125000002769 thiazolinyl group Chemical group 0.000 description 1
- 230000008719 thickening Effects 0.000 description 1
- 125000003777 thiepinyl group Chemical group 0.000 description 1
- 230000000451 tissue damage Effects 0.000 description 1
- 231100000827 tissue damage Toxicity 0.000 description 1
- 208000037816 tissue injury Diseases 0.000 description 1
- 229960002905 tolfenamic acid Drugs 0.000 description 1
- YEZNLOUZAIOMLT-UHFFFAOYSA-N tolfenamic acid Chemical compound CC1=C(Cl)C=CC=C1NC1=CC=CC=C1C(O)=O YEZNLOUZAIOMLT-UHFFFAOYSA-N 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 description 1
- 229960000303 topotecan Drugs 0.000 description 1
- 231100000331 toxic Toxicity 0.000 description 1
- 230000002588 toxic effect Effects 0.000 description 1
- LLPOLZWFYMWNKH-UHFFFAOYSA-N trans-dihydrocodeinone Natural products C1C(N(CCC234)C)C2CCC(=O)C3OC2=C4C1=CC=C2OC LLPOLZWFYMWNKH-UHFFFAOYSA-N 0.000 description 1
- 230000001052 transient effect Effects 0.000 description 1
- 238000003146 transient transfection Methods 0.000 description 1
- 229960000575 trastuzumab Drugs 0.000 description 1
- 230000008733 trauma Effects 0.000 description 1
- 230000000472 traumatic effect Effects 0.000 description 1
- 150000003852 triazoles Chemical class 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 description 1
- 125000005455 trithianyl group Chemical group 0.000 description 1
- 201000008827 tuberculosis Diseases 0.000 description 1
- 208000009852 uremia Diseases 0.000 description 1
- 125000005500 uronium group Chemical group 0.000 description 1
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- 239000003981 vehicle Substances 0.000 description 1
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- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 description 1
- 238000005406 washing Methods 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
- 230000003442 weekly effect Effects 0.000 description 1
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 description 1
- 229960000523 zalcitabine Drugs 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
- C07D217/26—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
- C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
- C07H13/04—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals attached to acyclic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H13/00—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids
- C07H13/02—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids
- C07H13/10—Compounds containing saccharide radicals esterified by carbonic acid or derivatives thereof, or by organic acids, e.g. phosphonic acids by carboxylic acids having the esterifying carboxyl radicals directly attached to heterocyclic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H17/00—Compounds containing heterocyclic radicals directly attached to hetero atoms of saccharide radicals
- C07H17/02—Heterocyclic radicals containing only nitrogen as ring hetero atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Biotechnology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Pain & Pain Management (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Other In-Based Heterocyclic Compounds (AREA)
- Saccharide Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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| Application Number | Priority Date | Filing Date | Title |
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| AU2013902513 | 2013-07-08 | ||
| AU2013902513A AU2013902513A0 (en) | 2013-07-08 | Method of treatment or prophylaxis | |
| PCT/AU2014/050116 WO2015003223A1 (en) | 2013-07-08 | 2014-07-08 | Heterocyclic compounds and methods of their use |
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| JP2016525093A JP2016525093A (ja) | 2016-08-22 |
| JP2016525093A5 JP2016525093A5 (enExample) | 2017-08-17 |
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| US (1) | US9714224B2 (enExample) |
| EP (1) | EP3019477B1 (enExample) |
| JP (1) | JP6505682B2 (enExample) |
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| PT2800738T (pt) | 2012-01-06 | 2020-06-23 | Novartis Ag | Compostos heterocíclicos e métodos para a utilização dos mesmos |
| US10308628B2 (en) * | 2015-03-12 | 2019-06-04 | Novartis Ag | Heterocyclic compounds and methods for their use |
| CN106478502B (zh) * | 2015-08-29 | 2021-04-27 | 上海翰森生物医药科技有限公司 | 1,2,3,4-四氢异喹啉衍生物、其制备方法和应用 |
| PT3620454T (pt) | 2017-06-09 | 2021-09-10 | Shandong Danhong Pharmaceutical Co Ltd | Derivado de ácido carboxílico como antagonista do recetor at2r |
| US11485725B2 (en) | 2017-12-15 | 2022-11-01 | Auransa Inc. | Derivatives of piperlongumine and uses thereof |
| US11384097B2 (en) | 2018-06-19 | 2022-07-12 | Zhejiang Hisun Pharmaceutical Co., Ltd. | Tetrahydroisoquinoline derivative, preparation method therefor and use thereof |
| WO2020012266A1 (en) * | 2018-07-12 | 2020-01-16 | Novartis Ag | Biocatalytic synthesis of olodanrigan (ema401) from 3-(2-(benzyloxy)-3-methoxyphenyl)propenoic acid with phenylalanine ammonia lyase |
| CN111620816B (zh) * | 2020-05-27 | 2023-06-02 | 上海赛默罗生物科技有限公司 | 螺桨烷类衍生物、其制备方法、药物组合物和用途 |
| CN113880825B (zh) * | 2020-07-01 | 2025-03-14 | 浙江海正药业股份有限公司 | 四氢异喹啉类衍生物的盐、其制备方法及其医药应用 |
| CN111777555B (zh) * | 2020-09-04 | 2020-12-01 | 上海赛默罗生物科技有限公司 | 脂肪环烷衍生物、其制备方法、药物组合物和其应用 |
| MX2024001155A (es) | 2021-07-30 | 2024-07-01 | Confo Therapeutics N V | Compuestos para el tratamiento del dolor, en particular el dolor neuropatico, y/u otras enfermedades o trastornos que se asocian con at2r y/o se?alizacion mediada por at2r. |
| CN117603088A (zh) * | 2023-10-28 | 2024-02-27 | 广东工业大学 | 一种基于氨基酸乙酯的芳香醛席夫碱及其在不对称烷基化中的应用 |
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| JPS55127373A (en) * | 1979-03-26 | 1980-10-02 | Takeda Chem Ind Ltd | Tetrahydroisoquinoline compound and its preparation |
| US5246943A (en) * | 1992-05-19 | 1993-09-21 | Warner-Lambert Company | Substituted 1,2,3,4-tetahydroisoquinolines with angiotensin II receptor antagonist properties |
| US5236934A (en) * | 1992-08-26 | 1993-08-17 | E. I. Du Pont De Nemours And Company | 1,2,3,4-tetrahydroisoquinolines useful in the treatment of CNS disorders |
| WO2003041641A2 (en) * | 2001-11-09 | 2003-05-22 | Bristol-Myers Squibb Company | Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity |
| WO2006055951A2 (en) | 2004-11-19 | 2006-05-26 | Portola Pharmaceuticals, Inc. | Tetrahydroisoquinolines as factor xa inhibitors |
| NZ555334A (en) | 2004-12-24 | 2010-05-28 | Spinifex Pharm Pty Ltd | Method of treatment or prophylaxis of a neuropathic condition using AT2 receptor antagonist |
| AU2007229322B2 (en) * | 2006-03-20 | 2012-04-05 | Novartis Ag | Method of treatment or prophylaxis inflammatory pain |
| CA2787173C (en) * | 2010-01-19 | 2018-05-01 | Spinifex Pharmaceuticals Pty Ltd | Methods and compositions for improved nerve conduction velocity |
| CN103003244B (zh) * | 2010-07-21 | 2016-04-20 | 诺华股份有限公司 | 四氢异喹啉衍生物的盐和溶剂合物 |
| PT2800738T (pt) | 2012-01-06 | 2020-06-23 | Novartis Ag | Compostos heterocíclicos e métodos para a utilização dos mesmos |
| US20150011565A1 (en) | 2012-01-25 | 2015-01-08 | Spinifex Pharmaceuticals Pty Ltd | Heterocyclic Compounds and Methods For Their Use |
| CN104470930B (zh) | 2012-01-25 | 2017-02-22 | 诺华股份有限公司 | 杂环化合物和它们的使用方法 |
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- 2014-07-08 WO PCT/AU2014/050116 patent/WO2015003223A1/en not_active Ceased
- 2014-07-08 CN CN201480038866.XA patent/CN105358532B/zh active Active
Also Published As
| Publication number | Publication date |
|---|---|
| JP2016525093A (ja) | 2016-08-22 |
| EP3019477A1 (en) | 2016-05-18 |
| PL3019477T3 (pl) | 2021-11-22 |
| CN105358532B (zh) | 2019-07-23 |
| US20160145213A1 (en) | 2016-05-26 |
| EP3019477A4 (en) | 2017-01-11 |
| PT3019477T (pt) | 2021-08-20 |
| CN105358532A (zh) | 2016-02-24 |
| WO2015003223A1 (en) | 2015-01-15 |
| ES2883155T3 (es) | 2021-12-07 |
| NZ630908A (en) | 2017-08-25 |
| EP3019477B1 (en) | 2021-05-26 |
| US9714224B2 (en) | 2017-07-25 |
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