JPWO2019173380A5 - - Google Patents
Download PDFInfo
- Publication number
- JPWO2019173380A5 JPWO2019173380A5 JP2020570407A JP2020570407A JPWO2019173380A5 JP WO2019173380 A5 JPWO2019173380 A5 JP WO2019173380A5 JP 2020570407 A JP2020570407 A JP 2020570407A JP 2020570407 A JP2020570407 A JP 2020570407A JP WO2019173380 A5 JPWO2019173380 A5 JP WO2019173380A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- pharmaceutically acceptable
- acceptable salt
- alkyl
- 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.)
- Pending
Links
- 150000001875 compounds Chemical class 0.000 claims description 90
- 150000003839 salts Chemical class 0.000 claims description 84
- 239000011780 sodium chloride Substances 0.000 claims description 84
- 239000012453 solvate Substances 0.000 claims description 68
- 125000000217 alkyl group Chemical group 0.000 claims description 67
- 229910052739 hydrogen Inorganic materials 0.000 claims description 43
- 239000001257 hydrogen Substances 0.000 claims description 43
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 34
- -1 2,3-dimethylbutyl Chemical group 0.000 claims description 26
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 25
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 22
- 150000002431 hydrogen Chemical class 0.000 claims description 21
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 21
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 13
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 9
- 238000006467 substitution reaction Methods 0.000 claims description 6
- 125000003709 fluoroalkyl group Chemical group 0.000 claims description 5
- 229910052736 halogen Inorganic materials 0.000 claims description 5
- 150000002367 halogens Chemical class 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 4
- 125000005917 3-methylpentyl group Chemical group 0.000 claims description 3
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 3
- 125000004491 isohexyl group Chemical group C(CCC(C)C)* 0.000 claims description 3
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 125000001280 n-hexyl group Chemical group C(CCCCC)* 0.000 claims description 3
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 125000005244 neohexyl group Chemical group [H]C([H])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims description 3
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- 125000003538 pentan-3-yl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])C([H])([H])[H] 0.000 claims description 3
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 3
- 102000009346 Adenosine receptors Human genes 0.000 claims description 2
- 108050000203 Adenosine receptors Proteins 0.000 claims description 2
- 208000008787 Cardiovascular Disease Diseases 0.000 claims description 2
- 206010012601 Diabetes mellitus Diseases 0.000 claims description 2
- 206010016654 Fibrosis Diseases 0.000 claims description 2
- 208000001718 Immediate Hypersensitivity Diseases 0.000 claims description 2
- 208000001083 Kidney Disease Diseases 0.000 claims description 2
- 208000009856 Lung Disease Diseases 0.000 claims description 2
- 208000008589 Obesity Diseases 0.000 claims description 2
- 206010045240 Type I hypersensitivity Diseases 0.000 claims description 2
- 230000001154 acute Effects 0.000 claims description 2
- 230000001684 chronic Effects 0.000 claims description 2
- 230000004761 fibrosis Effects 0.000 claims description 2
- 201000009673 liver disease Diseases 0.000 claims description 2
- 230000000926 neurological Effects 0.000 claims description 2
- 235000020824 obesity Nutrition 0.000 claims description 2
- 239000000546 pharmaceutic aid Substances 0.000 claims description 2
- 239000000825 pharmaceutical preparation Substances 0.000 claims description 2
- 230000009959 type I hypersensitivity Effects 0.000 claims description 2
- 238000009472 formulation Methods 0.000 claims 4
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 1
- 230000001105 regulatory Effects 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 description 27
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 description 13
- 125000004404 heteroalkyl group Chemical group 0.000 description 12
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 description 8
- 125000004432 carbon atoms Chemical group C* 0.000 description 6
- 241000124008 Mammalia Species 0.000 description 5
- 125000003545 alkoxy group Chemical group 0.000 description 4
- 125000002619 bicyclic group Chemical group 0.000 description 4
- 125000006580 bicyclic heterocycloalkyl group Chemical group 0.000 description 4
- 229910052799 carbon Inorganic materials 0.000 description 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 description 4
- 125000004428 fluoroalkoxy group Chemical group 0.000 description 4
- 239000008194 pharmaceutical composition Substances 0.000 description 4
- 125000002393 azetidinyl group Chemical group 0.000 description 3
- 229910052760 oxygen Inorganic materials 0.000 description 3
- 125000004430 oxygen atoms Chemical group O* 0.000 description 3
- 125000003386 piperidinyl group Chemical group 0.000 description 3
- 229910052717 sulfur Inorganic materials 0.000 description 3
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 description 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 description 2
- 150000001345 alkine derivatives Chemical class 0.000 description 2
- 125000005360 alkyl sulfoxide group Chemical group 0.000 description 2
- 125000004414 alkyl thio group Chemical group 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 125000005362 aryl sulfone group Chemical group 0.000 description 2
- 125000005361 aryl sulfoxide group Chemical group 0.000 description 2
- 125000005110 aryl thio group Chemical group 0.000 description 2
- 125000004104 aryloxy group Chemical group 0.000 description 2
- 125000004429 atoms Chemical group 0.000 description 2
- BVCRERJDOOBZOH-UHFFFAOYSA-N bicyclo[2.2.1]heptanyl Chemical group C1C[C+]2CC[C-]1C2 BVCRERJDOOBZOH-UHFFFAOYSA-N 0.000 description 2
- 125000002950 monocyclic group Chemical group 0.000 description 2
- 125000002757 morpholinyl group Chemical group 0.000 description 2
- 125000003566 oxetanyl group Chemical group 0.000 description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 description 2
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 2
- 125000004306 triazinyl group Chemical group 0.000 description 2
- 239000002775 capsule Substances 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000004855 decalinyl group Chemical group C1(CCCC2CCCCC12)* 0.000 description 1
- 125000004852 dihydrofuranyl group Chemical group O1C(CC=C1)* 0.000 description 1
- 125000005043 dihydropyranyl group Chemical group O1C(CCC=C1)* 0.000 description 1
- 125000000532 dioxanyl group Chemical group 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 239000000839 emulsion Substances 0.000 description 1
- 125000002541 furyl group Chemical group 0.000 description 1
- 125000002883 imidazolyl group Chemical group 0.000 description 1
- 238000001990 intravenous administration Methods 0.000 description 1
- 125000001786 isothiazolyl group Chemical group 0.000 description 1
- 125000000842 isoxazolyl group Chemical group 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 description 1
- 125000001715 oxadiazolyl group Chemical group 0.000 description 1
- 125000002971 oxazolyl group Chemical group 0.000 description 1
- 125000003551 oxepanyl group Chemical group 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 125000003373 pyrazinyl group Chemical group 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 150000003457 sulfones Chemical class 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 description 1
- 125000003831 tetrazolyl group Chemical group 0.000 description 1
- 125000001113 thiadiazolyl group Chemical group 0.000 description 1
- 125000000335 thiazolyl group Chemical group 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 1
- 125000001425 triazolyl group Chemical group 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024014959A JP2024032976A (ja) | 2018-03-05 | 2024-02-02 | アデノシン受容体アンタゴニストおよびその使用 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862638737P | 2018-03-05 | 2018-03-05 | |
| US62/638,737 | 2018-03-05 | ||
| US201862688088P | 2018-06-21 | 2018-06-21 | |
| US62/688,088 | 2018-06-21 | ||
| PCT/US2019/020810 WO2019173380A1 (en) | 2018-03-05 | 2019-03-05 | Adenosine receptor antagonists and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024014959A Division JP2024032976A (ja) | 2018-03-05 | 2024-02-02 | アデノシン受容体アンタゴニストおよびその使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2021517164A JP2021517164A (ja) | 2021-07-15 |
| JPWO2019173380A5 true JPWO2019173380A5 (he) | 2022-04-01 |
Family
ID=67847428
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020570407A Pending JP2021517164A (ja) | 2018-03-05 | 2019-03-05 | アデノシン受容体アンタゴニストおよびその使用 |
| JP2024014959A Pending JP2024032976A (ja) | 2018-03-05 | 2024-02-02 | アデノシン受容体アンタゴニストおよびその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024014959A Pending JP2024032976A (ja) | 2018-03-05 | 2024-02-02 | アデノシン受容体アンタゴニストおよびその使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US20210040097A1 (he) |
| EP (2) | EP4364727A3 (he) |
| JP (2) | JP2021517164A (he) |
| KR (1) | KR20200132901A (he) |
| CN (1) | CN112218867B (he) |
| AU (1) | AU2019232736B2 (he) |
| BR (1) | BR112020018158A2 (he) |
| CA (1) | CA3093234A1 (he) |
| IL (1) | IL277144B1 (he) |
| MX (1) | MX2020009286A (he) |
| SG (1) | SG11202008611UA (he) |
| WO (1) | WO2019173380A1 (he) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3093234A1 (en) | 2018-03-05 | 2019-09-12 | Teon Therapeutics, Inc. | Adenosine receptor antagonists and uses thereof |
| CN116194537A (zh) * | 2020-08-07 | 2023-05-30 | 泰昂治疗公司 | 与腺苷受体拮抗剂的组合疗法 |
| MX2023002676A (es) * | 2020-09-04 | 2023-05-10 | Teon Therapeutics Inc | Cocristales de un antagonista del receptor de adenosina a2b. |
| TW202313612A (zh) | 2021-06-04 | 2023-04-01 | 美商天恩治療有限公司 | 腺苷ａｂ受體拮抗劑的固體形式 |
| TW202327612A (zh) * | 2021-09-10 | 2023-07-16 | 美商天恩治療有限公司 | 使用腺苷受體拮抗劑之改良療法 |
| WO2024015372A1 (en) * | 2022-07-14 | 2024-01-18 | Teon Therapeutics, Inc. | Adenosine receptor antagonists and uses thereof |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5466811A (en) * | 1994-07-18 | 1995-11-14 | Merck & Co., Inc. | Dioxolenylmethyl carbamates pro moieties for amine drugs |
| EP1075472A1 (en) * | 1998-04-15 | 2001-02-14 | Warner-Lambert Company | Prodrugs of benzofuranylmethyl carbamate nk 1? antagonists |
| US7304070B2 (en) | 2001-11-09 | 2007-12-04 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US20080318983A1 (en) | 2001-11-09 | 2008-12-25 | Rao Kalla | A2b adenosine receptor antagonists |
| US7317017B2 (en) | 2002-11-08 | 2008-01-08 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US7125993B2 (en) | 2001-11-09 | 2006-10-24 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| US6977300B2 (en) | 2001-11-09 | 2005-12-20 | Cv Therapeutics, Inc. | A2B adenosine receptor antagonists |
| CN100467469C (zh) | 2001-11-09 | 2009-03-11 | Cv医药有限公司 | A2b腺苷受体拮抗剂 |
| BR0308737A (pt) * | 2002-03-20 | 2005-01-11 | Bristol Myers Squibb Co | Pró-drogas de fosfato de fluoroxindóis |
| DK1622908T3 (da) * | 2003-05-06 | 2008-11-17 | Cv Therapeutics Inc | Xanthin-derivater som A2B adenosin-receptor-antagonister |
| SI1789053T1 (sl) | 2004-09-01 | 2012-09-28 | Gilead Sciences Inc | Postopek celjenja rane z uporabo antagonistov A2B adenozinskih receptorjev |
| NZ589657A (en) | 2004-10-15 | 2012-06-29 | Gilead Palo Alto Inc | Method of preventing and treating airway remodeling and pulmonary inflammation using A2B adenosine receptor antagonists |
| EP2301937A1 (en) * | 2005-06-16 | 2011-03-30 | Cv Therapeutics, Inc. | Prodrugs of A2b adenosine receptor antagonists |
| US7795268B2 (en) | 2006-03-17 | 2010-09-14 | Gilead Palo Alto, Inc. | Method of treating hepatic disease using A2B adenosine receptor antagonists |
| US20100254965A1 (en) | 2006-10-24 | 2010-10-07 | Board Of Regents ,The University Of Texas System | Adenosine Signaling in Diagnosis, Treatment, and Prevention of Priapism and Erectile Dysfunction |
| WO2009088518A1 (en) | 2008-01-11 | 2009-07-16 | Cv Therapeutics, Inc. | A2b adenosine receptor antagonists for the treatment of cancer |
| CN102015712A (zh) * | 2008-03-26 | 2011-04-13 | 阿德维纳斯治疗私人有限公司 | 作为腺苷受体拮抗剂的杂环化合物 |
| WO2009157938A1 (en) | 2008-06-26 | 2009-12-30 | Cv Therapeutics, Inc. | A2b adenosine receptor antagonists for treating cancer |
| AU2011270701B2 (en) * | 2010-06-24 | 2015-05-14 | Alkermes Pharma Ireland Limited | Prodrugs of NH-acidic compounds: ester, carbonate, carbamate and phosphonate derivatives |
| CN103237548A (zh) * | 2010-06-30 | 2013-08-07 | 吉利德科学股份有限公司 | A2b腺苷受体拮抗剂用于治疗肺高血压的应用 |
| EP2616470B1 (en) * | 2010-09-13 | 2016-10-12 | Advinus Therapeutics Limited | Purine compounds as prodrugs of a2b adenosine receptor antagonists, their process and medicinal applications |
| AR085942A1 (es) | 2011-04-07 | 2013-11-06 | Gilead Sciences Inc | Uso de receptor de aadenosina para tratar la insuficiencia cardiaca y la arritmia en pacientes posinfarto de miocardio |
| WO2012170209A2 (en) * | 2011-05-23 | 2012-12-13 | Nectid, Inc. | Benzofuran-2 carboxamide compounds |
| US10117868B2 (en) | 2011-10-25 | 2018-11-06 | Case Western Reserve University | Systems pharmacology for treating ocular disorders |
| AU2018317390A1 (en) | 2017-08-14 | 2020-04-02 | Cytodigm, Inc. | Microparticle formulations of adenosine receptor antagonists for treating cancer |
| US10709763B2 (en) | 2017-12-19 | 2020-07-14 | Gpcr Therapeutics, Inc. | GPCR heteromer inhibitors and uses thereof |
| CA3093234A1 (en) | 2018-03-05 | 2019-09-12 | Teon Therapeutics, Inc. | Adenosine receptor antagonists and uses thereof |
-
2019
- 2019-03-05 CA CA3093234A patent/CA3093234A1/en active Pending
- 2019-03-05 BR BR112020018158-7A patent/BR112020018158A2/pt unknown
- 2019-03-05 EP EP24152200.2A patent/EP4364727A3/en active Pending
- 2019-03-05 IL IL277144A patent/IL277144B1/he unknown
- 2019-03-05 KR KR1020207028522A patent/KR20200132901A/ko not_active Application Discontinuation
- 2019-03-05 JP JP2020570407A patent/JP2021517164A/ja active Pending
- 2019-03-05 WO PCT/US2019/020810 patent/WO2019173380A1/en unknown
- 2019-03-05 SG SG11202008611UA patent/SG11202008611UA/en unknown
- 2019-03-05 MX MX2020009286A patent/MX2020009286A/es unknown
- 2019-03-05 AU AU2019232736A patent/AU2019232736B2/en active Active
- 2019-03-05 EP EP19764343.0A patent/EP3762386B1/en active Active
- 2019-03-05 CN CN201980030563.6A patent/CN112218867B/zh active Active
- 2019-03-05 US US16/978,040 patent/US20210040097A1/en not_active Abandoned
-
2021
- 2021-02-02 US US17/165,736 patent/US11124515B2/en active Active
- 2021-08-02 US US17/391,245 patent/US20220056033A1/en not_active Abandoned
-
2024
- 2024-02-02 JP JP2024014959A patent/JP2024032976A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP6524081B2 (ja) | ジヒドロピリミジン化合物及び医薬におけるその適用 | |
| RU2745431C1 (ru) | Гетероарильное производное пиперазина, способ его получения и применение в медицине | |
| KR102559499B1 (ko) | 삼환성 스피로 화합물 | |
| JP2010506854A5 (he) | ||
| TW201408662A (zh) | 二氫嘧啶類化合物及其在藥物中的應用 | |
| CA2662242A1 (en) | Benzo-fused compounds for use in treating metabolic disorders | |
| JP7485701B2 (ja) | Ａｔｒキナーゼ阻害剤としての２，４，６－三置換ピリミジン化合物 | |
| EP3912975A1 (en) | Lysophosphatidic acid receptor antagonists and preparation method therefor | |
| JP7159440B2 (ja) | ジカチオン化合物及びその製造方法と使用 | |
| KR20200081381A (ko) | P2x3 및/또는 p2x2/3 수용체 길항제, 이를 포함하는 약학적 조성물 및 이의 용도 | |
| JPWO2019173380A5 (he) | ||
| JP2019535644A (ja) | ジヒドロピリミジン化合物並びにその調製方法及び使用 | |
| WO2019205979A1 (zh) | 非天然氨基酸类衍生物、包含其的药物组合物及其制备方法和用途 | |
| EP4050008A1 (en) | Pyridazinone or pyridazine compound and derivative and pharmaceutical composition thereof | |
| ES2548683T3 (es) | Amidas del ácido 4-(5-isoxazolil o 5-pirrazolil-1,2,4-oxadiazol-3-il)-mandélico como agonistas de receptor de esfingosina-1-fosfato 1 | |
| AU2021341258A1 (en) | CD73 inhibitor and application thereof in medicine | |
| HU198199B (en) | Process for production of derivatives of imidasolidinon and medical compositions containing these substances | |
| CN116583501A (zh) | 用于治疗与lpa受体活性相关的病症的化合物和组合物 | |
| KR20230027161A (ko) | 비시클릭 화합물 및 이의 응용 | |
| JP2006515867A (ja) | 鉄含有量が非常に低いリセドロン酸ナトリウム | |
| CN111051326A (zh) | 核苷磷酸类化合物及其制备方法和用途 | |
| EP4342532A2 (en) | Antiplatelet drugs and uses thereof | |
| JPWO2021003310A5 (he) | ||
| AU2021302146A1 (en) | ATR inhibitors and uses thereof | |
| CN108299465B (zh) | 一种治疗胰腺炎的药物及其制备方法 |