JP2020037585A5 - - Google Patents
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- JP2020037585A5 JP2020037585A5 JP2019206852A JP2019206852A JP2020037585A5 JP 2020037585 A5 JP2020037585 A5 JP 2020037585A5 JP 2019206852 A JP2019206852 A JP 2019206852A JP 2019206852 A JP2019206852 A JP 2019206852A JP 2020037585 A5 JP2020037585 A5 JP 2020037585A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- orally acceptable
- acceptable dosage
- formulation
- heterocyclyl
- 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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- 239000002552 dosage form Substances 0.000 claims 15
- 238000009472 formulation Methods 0.000 claims 15
- 239000000203 mixture Substances 0.000 claims 15
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 125000002947 alkylene group Chemical group 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 229910052739 hydrogen Inorganic materials 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 239000001257 hydrogen Substances 0.000 claims 5
- -1 hydroxy piperidinylmethyl Chemical group 0.000 claims 5
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 150000001875 compounds Chemical class 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 206010053643 Neurodegenerative disease Diseases 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 206010003816 Autoimmune disease Diseases 0.000 claims 1
- 206010070976 Craniocerebral injury Diseases 0.000 claims 1
- 206010020751 Hypersensitivity Diseases 0.000 claims 1
- 206010038683 Respiratory disease Diseases 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 208000005765 Traumatic Brain Injury Diseases 0.000 claims 1
- 206010047461 Viral infection Diseases 0.000 claims 1
- 208000001756 Virus Disease Diseases 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 230000002491 angiogenic Effects 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000037406 food intake Effects 0.000 claims 1
- 235000012631 food intake Nutrition 0.000 claims 1
- 200000000028 growth disorder Diseases 0.000 claims 1
- 200000000018 inflammatory disease Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 210000001519 tissues Anatomy 0.000 claims 1
- 230000017613 viral reproduction Effects 0.000 claims 1
- 200000000019 wound Diseases 0.000 claims 1
- 0 CN(C(*)=*)NC(C=C[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O Chemical compound CN(C(*)=*)NC(C=C[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O 0.000 description 4
- BGUKCLNXSXSYCZ-PLNGDYQASA-N CC(C)(C)C(NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)=O Chemical compound CC(C)(C)C(NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)=O BGUKCLNXSXSYCZ-PLNGDYQASA-N 0.000 description 1
- XDEHMKQLKPZERH-BYPYZUCNSA-N CC(C)[C@@H](C(N)=O)N Chemical compound CC(C)[C@@H](C(N)=O)N XDEHMKQLKPZERH-BYPYZUCNSA-N 0.000 description 1
- QZXFTDAXYQVJOG-ARJAWSKDSA-N CC1N(CC(NNC2OC2/C=C\[n]2nc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2)=O)C(C)COC1 Chemical compound CC1N(CC(NNC2OC2/C=C\[n]2nc(-c3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc2)=O)C(C)COC1 QZXFTDAXYQVJOG-ARJAWSKDSA-N 0.000 description 1
- JGZRCCPXJBIBJL-PLNGDYQASA-N CN(C(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)[N](C)(C)C(C(N1CCOCC1)=O)=O Chemical compound CN(C(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)[N](C)(C)C(C(N1CCOCC1)=O)=O JGZRCCPXJBIBJL-PLNGDYQASA-N 0.000 description 1
- WPZLXGTWFVZICP-XQRVVYSFSA-N CNC(CN(CC1)CC[O]1/[O]=C(\C1CNCCC1)/NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)=O Chemical compound CNC(CN(CC1)CC[O]1/[O]=C(\C1CNCCC1)/NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)=O WPZLXGTWFVZICP-XQRVVYSFSA-N 0.000 description 1
- ODDMRWATJPOZIC-IHWYPQMZSA-N Cc([nH]nc1)c1C(NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)=O Chemical compound Cc([nH]nc1)c1C(NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O)=O ODDMRWATJPOZIC-IHWYPQMZSA-N 0.000 description 1
- CSDUVPJWQLJHGC-UHFFFAOYSA-O O=C(C=C[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)N[NH2+]C(c1nccnc1)=O Chemical compound O=C(C=C[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)N[NH2+]C(c1nccnc1)=O CSDUVPJWQLJHGC-UHFFFAOYSA-O 0.000 description 1
- OVOIZHFSFHOUPO-UPHRSURJSA-N O=C(CN1CCOCC1)NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O Chemical compound O=C(CN1CCOCC1)NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O OVOIZHFSFHOUPO-UPHRSURJSA-N 0.000 description 1
- FEWZCLGKEHFXRY-RJRFIUFISA-N O=C(Cc1cnccn1)NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O Chemical compound O=C(Cc1cnccn1)NNC(/C=C\[n]1nc(-c2cc(C(F)(F)F)cc(C(F)(F)F)c2)nc1)=O FEWZCLGKEHFXRY-RJRFIUFISA-N 0.000 description 1
Claims (15)
- 式I:
の化合物
(式中、
R1は、水素およびC1〜C4アルキルから選択され;
R2は、OおよびSから選択され;
R3は、−N(R4)−(C3〜C6シクロアルキル)、−C 3 〜C6アルキル、−(C0〜C 1 アルキレン)−ヘテロシクリル、および−(C0〜C4アルキレン)−ヘテロアリールから選択され、R3のあらゆるアルキルまたはアルキレン部分は、−N(R 5 ) 2 (式中、各R 5 は水素およびC 1 〜C 4 アルキルから独立して選択される)で任意に置換され;
R 3 のあらゆるヘテロシクリルおよびヘテロアリール部分が、環内に少なくとも1つの窒素原子を含んでなり;
R 3 のあらゆるヘテロシクリルおよびヘテロアリール部分が、C 1 〜C 4 アルキルで任意に置換され;
R4は、水素である)
またはその薬学的に許容可能な塩、溶媒和物もしくは水和物、ならびに
薬学的に許容可能な担体
を含んでなる、経口的に許容可能な剤形の製剤。 - R1が、水素およびメチルから選択される、請求項1に記載の経口的に許容可能な剤形の製剤。
- R1が、水素である、請求項2に記載の経口的に許容可能な剤形の製剤。
- R2がOである、請求項1〜3のいずれか一項に記載の経口的に許容可能な剤形の製剤。
- R3が、−(C0〜C1アルキレン)−ヘテロシクリルである、請求項1に記載の経口的に許容可能な剤形の製剤。
- R3が、−(C1アルキレン)−ヘテロシクリルである、請求項5に記載の経口的に許容可能な剤形の製剤。
- 前記ヘテロシクリルが、ピラジニル、ピペリジニル、モルホリニル、およびピラゾリルから選択される、請求項5または請求項6に記載の経口的に許容可能な剤形の製剤。
- 前記ヘテロシクリルが、モルホリニルである、請求項7に記載の経口的に許容可能な剤形の製剤。
- R3が、−C(CH3)3、−CH(NH2)−CH(CH3)2、−NH−シクロプロピル、−(CH2)0〜1−ピラジニル、ピペリジニル、ヒドロキシピペリジニル、N−メチルピペリジニル、−CH2−モルホリン−4−イル、およびメチルピラゾリルから選択される、請求項1に記載の経口的に許容可能な剤形の製剤。
- R3が、−C(CH3)3、−CH(NH2)−CH(CH3)2、−NH−シクロプロピル、−(CH2)0〜1−ピラジン−2−イル、ピペリジン−3−イル、−CH2−モルホリン−4−イル、および5−メチル−1−H−ピラゾール−4−イルから選択される、請求項9に記載の経口的に許容可能な剤形の製剤。
- R3が、−C(CH3)3、−NH−シクロプロピル、−CH2−ピラジン−2−イル、−ピラジン−2−イル、−CH2−モルホリン−4−イル、および5−メチル−1−H−ピラゾール−4−イルから選択される、請求項10に記載の経口的に許容可能な剤形の製剤。
- 前記化合物が、化合物1、2、3、4、8、11、12、および13のいずれか1つから選択される、請求項12に記載の経口的に許容可能な剤形の製剤。
- 増殖性疾患、血管新生疾患、炎症性疾患、自己免疫障害、ウイルス感染症、創傷、眼科疾患、神経変性疾患、異常な組織成長障害、食物摂取量関連障害、アレルギー、脳卒中、外傷性脳損傷および呼吸器疾患から選択される疾患の治療のための、請求項1に記載の経口的に許容可能な剤形の製剤。
- 神経変性疾患の治療のための、請求項1に記載の経口的に許容可能な剤形の製剤。
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201261644802P | 2012-05-09 | 2012-05-09 | |
US61/644,802 | 2012-05-09 | ||
US201361798188P | 2013-03-15 | 2013-03-15 | |
US61/798,188 | 2013-03-15 |
Related Parent Applications (1)
Application Number | Title | Priority Date | Filing Date |
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JP2018154275A Division JP2018172444A (ja) | 2012-05-09 | 2018-08-20 | 核内輸送調節因子およびその使用 |
Related Child Applications (1)
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JP2020218700A Division JP2021063104A (ja) | 2012-05-09 | 2020-12-28 | 核内輸送調節因子およびその使用 |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2020037585A JP2020037585A (ja) | 2020-03-12 |
JP2020037585A5 true JP2020037585A5 (ja) | 2020-05-14 |
JP6818849B2 JP6818849B2 (ja) | 2021-01-20 |
Family
ID=49448240
Family Applications (5)
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JP2015511713A Active JP6195909B2 (ja) | 2012-05-09 | 2013-05-09 | 核内輸送調節因子およびその使用 |
JP2017160341A Withdrawn JP2018012715A (ja) | 2012-05-09 | 2017-08-23 | 核内輸送調節因子およびその使用 |
JP2018154275A Withdrawn JP2018172444A (ja) | 2012-05-09 | 2018-08-20 | 核内輸送調節因子およびその使用 |
JP2019206852A Active JP6818849B2 (ja) | 2012-05-09 | 2019-11-15 | 核内輸送調節因子およびその使用 |
JP2020218700A Withdrawn JP2021063104A (ja) | 2012-05-09 | 2020-12-28 | 核内輸送調節因子およびその使用 |
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JP2015511713A Active JP6195909B2 (ja) | 2012-05-09 | 2013-05-09 | 核内輸送調節因子およびその使用 |
JP2017160341A Withdrawn JP2018012715A (ja) | 2012-05-09 | 2017-08-23 | 核内輸送調節因子およびその使用 |
JP2018154275A Withdrawn JP2018172444A (ja) | 2012-05-09 | 2018-08-20 | 核内輸送調節因子およびその使用 |
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JP2020218700A Withdrawn JP2021063104A (ja) | 2012-05-09 | 2020-12-28 | 核内輸送調節因子およびその使用 |
Country Status (32)
Country | Link |
---|---|
US (10) | US9096543B2 (ja) |
EP (3) | EP2858991B1 (ja) |
JP (5) | JP6195909B2 (ja) |
KR (5) | KR102163377B1 (ja) |
CN (1) | CN104428295B (ja) |
AU (5) | AU2013259384B2 (ja) |
BR (1) | BR112014027860B8 (ja) |
CA (1) | CA2872190A1 (ja) |
CL (1) | CL2014003054A1 (ja) |
CO (1) | CO7190242A2 (ja) |
CY (2) | CY1120832T1 (ja) |
DK (2) | DK3404027T3 (ja) |
EA (1) | EA036639B1 (ja) |
ES (2) | ES2702279T3 (ja) |
GE (1) | GEP20237477B (ja) |
HK (1) | HK1209420A1 (ja) |
HR (2) | HRP20181838T1 (ja) |
HU (2) | HUE050452T2 (ja) |
IN (1) | IN2014DN09434A (ja) |
LT (2) | LT3404027T (ja) |
ME (1) | ME03795B (ja) |
MX (1) | MX364992B (ja) |
NZ (1) | NZ702663A (ja) |
PE (1) | PE20150128A1 (ja) |
PL (2) | PL2858991T3 (ja) |
PT (2) | PT3404027T (ja) |
RS (2) | RS58058B1 (ja) |
SG (1) | SG11201407268SA (ja) |
SI (2) | SI2858991T1 (ja) |
UA (1) | UA118085C2 (ja) |
WO (1) | WO2013170068A2 (ja) |
ZA (1) | ZA202004892B (ja) |
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