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)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (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)
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|---|---|
| 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 (enExample) |
| EP (1) | EP3813827A4 (enExample) |
| JP (1) | JP2021530442A (enExample) |
| KR (1) | KR20210025016A (enExample) |
| CN (1) | CN112351778B (enExample) |
| TW (1) | TW202019408A (enExample) |
| WO (1) | WO2020006432A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3802534B1 (en) | 2018-05-25 | 2022-07-13 | Incyte Corporation | Tricyclic heterocyclic compounds as sting activators |
| US10875872B2 (en) | 2018-07-31 | 2020-12-29 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
| WO2020028565A1 (en) | 2018-07-31 | 2020-02-06 | Incyte Corporation | Tricyclic heteraryl compounds as sting activators |
| AU2019326633B2 (en) * | 2018-08-24 | 2022-09-08 | Adlai Nortye Biopharma Co., Ltd. | High activity sting protein agonist |
| CA3110474C (en) * | 2018-08-29 | 2024-04-23 | Adlai Nortye Biopharma Co., Ltd. | Highly active sting protein agonist compound |
| US11596692B1 (en) | 2018-11-21 | 2023-03-07 | Incyte Corporation | PD-L1/STING conjugates and methods of use |
| CN113195473B (zh) * | 2018-12-14 | 2022-11-22 | 江苏恒瑞医药股份有限公司 | 三环化合物作为sting激动剂及其制备方法和医药用途 |
| WO2020146237A1 (en) | 2019-01-07 | 2020-07-16 | Incyte Corporation | Heteroaryl amide compounds as sting activators |
| KR20220056176A (ko) | 2019-08-02 | 2022-05-04 | 메르사나 테라퓨틱스, 인코포레이티드 | 암 치료를 위한 sting(인터페론 유전자의 자극인자) 작용제로서의 비스-[n-((5-카바모일)-1h-벤조[d]이미다졸-2-일)-피라졸-5-카복사미드] 유도체 및 관련 화합물 |
| CN116196435B (zh) | 2020-04-02 | 2025-12-02 | 梅尔莎纳医疗公司 | 包含sting激动剂的抗体药物缀合物 |
| US20230141284A1 (en) | 2020-04-10 | 2023-05-11 | Ono Pharmaceutical Co., Ltd. | Cancer therapeutic method |
| 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 |
| WO2023158862A2 (en) * | 2022-02-21 | 2023-08-24 | 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 |
| CA2332239A1 (en) * | 1998-05-15 | 1999-11-25 | 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 |
| MX2008001152A (es) * | 2005-08-05 | 2008-04-02 | Astrazeneca Ab | Benzimidazoles triciclicos y su uso como moduladores del receptor de glutamato metabotropico. |
| EP2324044A4 (en) | 2008-08-04 | 2012-04-25 | Univ Miami | STING (STIMULATOR OF INTERFERON GENES) AS A REGULATOR OF BORROWING IMMUNE REACTIONS |
| US8653089B2 (en) * | 2011-02-09 | 2014-02-18 | F. Hoffmann-La Roche Ag | Heterocyclic compounds and methods of use |
| AU2013256468A1 (en) | 2012-04-30 | 2014-12-04 | Glen N. Barber | Modulating immune responses |
| 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 |
| SG10201900628RA (en) | 2016-04-07 | 2019-02-27 | Glaxosmithkline Ip Dev Ltd | Heterocyclic amides useful as protein modulators |
| WO2017175156A1 (en) * | 2016-04-07 | 2017-10-12 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides useful as protein modulators |
-
2019
- 2019-06-28 CN CN201980043105.6A patent/CN112351778B/zh active Active
- 2019-06-28 WO PCT/US2019/039860 patent/WO2020006432A1/en not_active Ceased
- 2019-06-28 US US17/255,712 patent/US11535633B2/en active Active
- 2019-06-28 JP JP2020570791A patent/JP2021530442A/ja active Pending
- 2019-06-28 KR KR1020207037227A patent/KR20210025016A/ko not_active Ceased
- 2019-06-28 TW TW108123007A patent/TW202019408A/zh unknown
- 2019-06-28 EP EP19825637.2A patent/EP3813827A4/en not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| EP3813827A1 (en) | 2021-05-05 |
| US20210300944A1 (en) | 2021-09-30 |
| US11535633B2 (en) | 2022-12-27 |
| KR20210025016A (ko) | 2021-03-08 |
| EP3813827A4 (en) | 2022-04-13 |
| WO2020006432A1 (en) | 2020-01-02 |
| CN112351778A (zh) | 2021-02-09 |
| CN112351778B (zh) | 2023-04-04 |
| JP2021530442A (ja) | 2021-11-11 |
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