TW202019408A - 稠合三環雜環化合物及其治療用途 - Google Patents
稠合三環雜環化合物及其治療用途 Download PDFInfo
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- TW202019408A TW202019408A TW108123007A TW108123007A TW202019408A TW 202019408 A TW202019408 A TW 202019408A TW 108123007 A TW108123007 A TW 108123007A TW 108123007 A TW108123007 A TW 108123007A TW 202019408 A TW202019408 A TW 202019408A
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- cycloalkyl
- aryl
- heteroaryl
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- 125000000169 tricyclic heterocycle group Chemical group 0.000 title abstract 2
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- 239000007901 soft capsule Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 210000000130 stem cell Anatomy 0.000 description 1
- 125000000547 substituted alkyl group Chemical group 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000010189 synthetic method Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000000037 tert-butyldiphenylsilyl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1[Si]([H])([*]C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 description 1
- 150000003512 tertiary amines Chemical class 0.000 description 1
- CBXCPBUEXACCNR-UHFFFAOYSA-N tetraethylammonium Chemical compound CC[N+](CC)(CC)CC CBXCPBUEXACCNR-UHFFFAOYSA-N 0.000 description 1
- CXWXQJXEFPUFDZ-UHFFFAOYSA-N tetralin Chemical compound C1=CC=C2CCCCC2=C1 CXWXQJXEFPUFDZ-UHFFFAOYSA-N 0.000 description 1
- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
- CZDYPVPMEAXLPK-UHFFFAOYSA-N tetramethylsilane Chemical compound C[Si](C)(C)C CZDYPVPMEAXLPK-UHFFFAOYSA-N 0.000 description 1
- 150000003536 tetrazoles Chemical class 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 210000001519 tissue Anatomy 0.000 description 1
- 230000000451 tissue damage Effects 0.000 description 1
- 231100000827 tissue damage Toxicity 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000005945 translocation Effects 0.000 description 1
- 238000011277 treatment modality Methods 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
- IMFACGCPASFAPR-UHFFFAOYSA-N tributylamine Chemical compound CCCCN(CCCC)CCCC IMFACGCPASFAPR-UHFFFAOYSA-N 0.000 description 1
- TUQOTMZNTHZOKS-UHFFFAOYSA-N tributylphosphine Chemical compound CCCCP(CCCC)CCCC TUQOTMZNTHZOKS-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- 230000001960 triggered effect Effects 0.000 description 1
- 108700026220 vif Genes Proteins 0.000 description 1
- 230000003612 virological effect Effects 0.000 description 1
- BFDBKMOZYNOTPK-UHFFFAOYSA-N vonoprazan Chemical compound C=1C=CN=CC=1S(=O)(=O)N1C=C(CNC)C=C1C1=CC=CC=C1F BFDBKMOZYNOTPK-UHFFFAOYSA-N 0.000 description 1
- 239000003643 water by type Substances 0.000 description 1
Classifications
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-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
-
- 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
- A61K31/5365—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 ortho- or peri-condensed with heterocyclic ring 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
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/06—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/16—Peri-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Virology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Rheumatology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862691208P | 2018-06-28 | 2018-06-28 | |
| US62/691,208 | 2018-06-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW202019408A true TW202019408A (zh) | 2020-06-01 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW108123007A TW202019408A (zh) | 2018-06-28 | 2019-06-28 | 稠合三環雜環化合物及其治療用途 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US11535633B2 (https=) |
| EP (1) | EP3813827A4 (https=) |
| JP (1) | JP2021530442A (https=) |
| KR (1) | KR20210025016A (https=) |
| CN (1) | CN112351778B (https=) |
| TW (1) | TW202019408A (https=) |
| WO (1) | WO2020006432A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7570235B2 (ja) | 2018-05-25 | 2024-10-21 | インサイト・コーポレイション | Ｓｔｉｎｇ活性化剤としての三環式複素環式化合物 |
| WO2020028566A1 (en) | 2018-07-31 | 2020-02-06 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
| US11008344B2 (en) | 2018-07-31 | 2021-05-18 | Incyte Corporation | Tricyclic heteroaryl compounds as STING activators |
| AU2019326633B2 (en) * | 2018-08-24 | 2022-09-08 | Adlai Nortye Biopharma Co., Ltd. | High activity sting protein agonist |
| CN111655682B (zh) * | 2018-08-29 | 2024-05-31 | 杭州阿诺生物医药科技有限公司 | 一种高活性sting蛋白激动剂化合物 |
| US11596692B1 (en) | 2018-11-21 | 2023-03-07 | Incyte Corporation | PD-L1/STING conjugates and methods of use |
| US20220056044A1 (en) * | 2018-12-14 | 2022-02-24 | Jiangsu Hengrui Medicine Co., Ltd. | Tricyclic compounds as sting agonists, and preparation methods and medicinal uses thereof |
| WO2020146237A1 (en) | 2019-01-07 | 2020-07-16 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
| JP7843695B2 (ja) | 2019-08-02 | 2026-04-10 | メルサナ セラピューティクス インコーポレイテッド | がんの処置用のＳＴＩＮＧ（インターフェロン遺伝子刺激因子）アゴニストとしてのビス－［Ｎ－（（５－カルバモイル）－１Ｈ－ベンゾ［ｄ］イミダゾール－２－イル）－ピラゾール－５－カルボキサミド］誘導体および関連化合物 |
| IL296901A (en) | 2020-04-02 | 2022-12-01 | Mersana Therapeutics Inc | Antibody-drug conjugates comprising sting agonists |
| TW202200136A (zh) | 2020-04-10 | 2022-01-01 | 日商小野藥品工業股份有限公司 | 癌治療方法 |
| CN115554303B (zh) * | 2021-09-18 | 2024-07-09 | 上海科技大学 | 一种三环类化合物、其制备方法及其应用 |
| US20250171461A1 (en) * | 2022-02-21 | 2025-05-29 | Geode Therapeutics Inc. | Stimulator of interferon genes (sting) modulators, and compositions and methods thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR2731708B1 (fr) * | 1995-03-13 | 1997-04-30 | Synthelabo | Derives de piperidine, leur procede de preparation et leur application en therapeutique |
| FR2747678B1 (fr) * | 1996-04-22 | 1998-05-22 | Synthelabo | Composes derives d'imidazobenzoxazine, leurs procedes de preparation et leurs utilisations en therapeutique |
| AU9298798A (en) * | 1998-05-15 | 1999-12-06 | Guilford Pharmaceuticals Inc. | Fused tricyclic compounds which inhibit parp activity |
| ECSP003637A (es) | 1999-08-31 | 2002-03-25 | Agouron Pharma | Inhibidores triciclicos de poli (adp-ribosa) polimerasas |
| CA2324090A1 (en) | 1999-10-25 | 2001-04-25 | Leviton Manufacturing Co., Inc. | Electrical wiring device with multiple types of wire terminations |
| US20070032469A1 (en) | 2005-08-05 | 2007-02-08 | Astrazeneca Ab | Tricyclic benzimidazoles and their use as metabotropic glutamate receptor modulators |
| JP2011529708A (ja) | 2008-08-04 | 2011-12-15 | ユニバーシティ オブ マイアミ | 自然免疫応答の調節因子ｓｔｉｎｇ（インターフェロン遺伝子の刺激因子） |
| RU2013138835A (ru) * | 2011-02-09 | 2015-03-20 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения в качестве ингибиторов pi3 киназы |
| KR20150004416A (ko) | 2012-04-30 | 2015-01-12 | 글렌 엔. 바버 | 면역 반응의 조절 |
| JP6599979B2 (ja) * | 2014-09-15 | 2019-10-30 | インサイト・コーポレイション | Ｂｅｔタンパク質阻害剤として用いるための三環式複素環化合物 |
| PT3440076T (pt) | 2016-04-07 | 2022-07-29 | Glaxosmithkline Ip Dev Ltd | Amidas heterocíclicas úteis como modeladores de proteína |
| JP2019510802A (ja) | 2016-04-07 | 2019-04-18 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | タンパク質調節物質として有用な複素環アミド |
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- 2019-06-28 JP JP2020570791A patent/JP2021530442A/ja active Pending
- 2019-06-28 KR KR1020207037227A patent/KR20210025016A/ko not_active Ceased
- 2019-06-28 EP EP19825637.2A patent/EP3813827A4/en not_active Withdrawn
- 2019-06-28 WO PCT/US2019/039860 patent/WO2020006432A1/en not_active Ceased
- 2019-06-28 CN CN201980043105.6A patent/CN112351778B/zh active Active
- 2019-06-28 TW TW108123007A patent/TW202019408A/zh unknown
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| CN112351778B (zh) | 2023-04-04 |
| EP3813827A4 (en) | 2022-04-13 |
| JP2021530442A (ja) | 2021-11-11 |
| US20210300944A1 (en) | 2021-09-30 |
| KR20210025016A (ko) | 2021-03-08 |
| US11535633B2 (en) | 2022-12-27 |
| WO2020006432A1 (en) | 2020-01-02 |
| EP3813827A1 (en) | 2021-05-05 |
| CN112351778A (zh) | 2021-02-09 |
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