JP2020530832A5 - - Google Patents
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- Publication number
- JP2020530832A5 JP2020530832A5 JP2019572820A JP2019572820A JP2020530832A5 JP 2020530832 A5 JP2020530832 A5 JP 2020530832A5 JP 2019572820 A JP2019572820 A JP 2019572820A JP 2019572820 A JP2019572820 A JP 2019572820A JP 2020530832 A5 JP2020530832 A5 JP 2020530832A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical preparation
- preparation according
- weight
- pharmaceutical
- diluent
- 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.)
- Granted
Links
- 239000000825 pharmaceutical preparation Substances 0.000 claims 40
- -1 4-chloro-2- (morpholin-4-yl) thiazole-5-yl Chemical group 0.000 claims 13
- 239000003085 diluting agent Substances 0.000 claims 8
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 7
- 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 7
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims 6
- 229960001021 lactose monohydrate Drugs 0.000 claims 6
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 6
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 5
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 5
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 5
- 239000000314 lubricant Substances 0.000 claims 5
- 229940127557 pharmaceutical product Drugs 0.000 claims 5
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 4
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 4
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims 4
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 239000011230 binding agent Substances 0.000 claims 3
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 claims 3
- 239000008187 granular material Substances 0.000 claims 3
- 235000019359 magnesium stearate Nutrition 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 239000004094 surface-active agent Substances 0.000 claims 3
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims 2
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims 2
- 229920003171 Poly (ethylene oxide) Chemical class 0.000 claims 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical group O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 2
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical class [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 2
- 239000007884 disintegrant Substances 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 2
- 229920005862 polyol Polymers 0.000 claims 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 2
- 239000007909 solid dosage form Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 229940032147 starch Drugs 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 1
- 229920002261 Corn starch Polymers 0.000 claims 1
- 229920002785 Croscarmellose sodium Polymers 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- SNRUBQQJIBEYMU-UHFFFAOYSA-N Dodecane Natural products CCCCCCCCCCCC SNRUBQQJIBEYMU-UHFFFAOYSA-N 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920000881 Modified starch Polymers 0.000 claims 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 235000021355 Stearic acid Nutrition 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229930006000 Sucrose Natural products 0.000 claims 1
- NQIWTFFSXXTCBM-UHFFFAOYSA-M [Br-].C(CCCCCCCCCCCCCCC)C[N+](C)(C)CCCCCCCCCCCCCC Chemical compound [Br-].C(CCCCCCCCCCCCCCC)C[N+](C)(C)CCCCCCCCCCCCCC NQIWTFFSXXTCBM-UHFFFAOYSA-M 0.000 claims 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims 1
- 239000000783 alginic acid Substances 0.000 claims 1
- 235000010443 alginic acid Nutrition 0.000 claims 1
- 229920000615 alginic acid Polymers 0.000 claims 1
- 229960001126 alginic acid Drugs 0.000 claims 1
- 150000004781 alginic acids Chemical class 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 150000008051 alkyl sulfates Chemical class 0.000 claims 1
- 229910000019 calcium carbonate Inorganic materials 0.000 claims 1
- 229960003563 calcium carbonate Drugs 0.000 claims 1
- 235000010216 calcium carbonate Nutrition 0.000 claims 1
- 239000001506 calcium phosphate Substances 0.000 claims 1
- 229910000389 calcium phosphate Inorganic materials 0.000 claims 1
- 229960001714 calcium phosphate Drugs 0.000 claims 1
- 235000011010 calcium phosphates Nutrition 0.000 claims 1
- 229960001927 cetylpyridinium chloride Drugs 0.000 claims 1
- YMKDRGPMQRFJGP-UHFFFAOYSA-M cetylpyridinium chloride Chemical compound [Cl-].CCCCCCCCCCCCCCCC[N+]1=CC=CC=C1 YMKDRGPMQRFJGP-UHFFFAOYSA-M 0.000 claims 1
- 239000008120 corn starch Substances 0.000 claims 1
- 229940099112 cornstarch Drugs 0.000 claims 1
- 229960001681 croscarmellose sodium Drugs 0.000 claims 1
- 229960000913 crospovidone Drugs 0.000 claims 1
- 125000003438 dodecyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- MVPICKVDHDWCJQ-UHFFFAOYSA-N ethyl 3-pyrrolidin-1-ylpropanoate Chemical compound CCOC(=O)CCN1CCCC1 MVPICKVDHDWCJQ-UHFFFAOYSA-N 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 229960001855 mannitol Drugs 0.000 claims 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 claims 1
- 229960000502 poloxamer Drugs 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 150000003077 polyols Chemical class 0.000 claims 1
- 229920001451 polypropylene glycol Polymers 0.000 claims 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 1
- 229920001592 potato starch Polymers 0.000 claims 1
- 239000000344 soap Chemical class 0.000 claims 1
- 229910000029 sodium carbonate Inorganic materials 0.000 claims 1
- 229940001593 sodium carbonate Drugs 0.000 claims 1
- 235000017550 sodium carbonate Nutrition 0.000 claims 1
- 239000008109 sodium starch glycolate Substances 0.000 claims 1
- 229920003109 sodium starch glycolate Polymers 0.000 claims 1
- 229940079832 sodium starch glycolate Drugs 0.000 claims 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000008117 stearic acid Substances 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 239000000454 talc Substances 0.000 claims 1
- 229910052623 talc Inorganic materials 0.000 claims 1
- 235000012222 talc Nutrition 0.000 claims 1
- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023084119A JP7720354B2 (ja) | 2017-08-14 | 2023-05-22 | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762545393P | 2017-08-14 | 2017-08-14 | |
| US62/545,393 | 2017-08-14 | ||
| PCT/US2018/046707 WO2019036472A1 (en) | 2017-08-14 | 2018-08-14 | CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023084119A Division JP7720354B2 (ja) | 2017-08-14 | 2023-05-22 | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020530832A JP2020530832A (ja) | 2020-10-29 |
| JP2020530832A5 true JP2020530832A5 (https=) | 2021-09-24 |
| JP7285222B2 JP7285222B2 (ja) | 2023-06-01 |
Family
ID=65362465
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019572820A Active JP7285222B2 (ja) | 2017-08-14 | 2018-08-14 | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
| JP2023084119A Active JP7720354B2 (ja) | 2017-08-14 | 2023-05-22 | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023084119A Active JP7720354B2 (ja) | 2017-08-14 | 2023-05-22 | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20210137935A1 (https=) |
| EP (1) | EP3630763A4 (https=) |
| JP (2) | JP7285222B2 (https=) |
| KR (1) | KR102644781B1 (https=) |
| CN (1) | CN110997667A (https=) |
| AR (1) | AR112471A1 (https=) |
| AU (3) | AU2018318990B2 (https=) |
| BR (1) | BR112020002966A2 (https=) |
| CA (1) | CA3064445A1 (https=) |
| EA (1) | EA202090321A1 (https=) |
| MX (2) | MX2019015318A (https=) |
| TW (2) | TW202400179A (https=) |
| WO (1) | WO2019036472A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS65839B1 (sr) | 2014-01-21 | 2024-09-30 | Neurocrine Biosciences Inc | Crf1 receptor antagonisti za tretman kongenitalne adrenalne hiperplazije |
| JP7285222B2 (ja) * | 2017-08-14 | 2023-06-01 | スプルース バイオサイエンシズ インコーポレイテッド | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
| WO2019036503A1 (en) | 2017-08-14 | 2019-02-21 | Spruce Biosciences, Inc. | CORTICOTROPIN RELEASE FACTOR RECEPTOR ANTAGONISTS |
| EP4643950A3 (en) * | 2018-04-27 | 2026-01-14 | Spruce Biosciences, Inc. | Methods for treating testicular and ovarian adrenal rest tumors |
| US20220023266A1 (en) | 2018-12-07 | 2022-01-27 | Neurocrine Biosciences, Inc. | Crf1 receptor antagonist, pharmaceutical formulations and solid forms thereof for the treatment of congenital adrenal hyperplasia |
| JP2022541550A (ja) * | 2019-07-19 | 2022-09-26 | スプルース バイオサイエンシーズ，インク． | 先天性副腎過形成を処置する方法 |
| JP7623365B2 (ja) | 2019-09-27 | 2025-01-28 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | Ｃｒｆ受容体アンタゴニストおよび使用方法 |
| KR20240023691A (ko) | 2020-08-12 | 2024-02-22 | 스프루스 바이오사이언시스 인코포레이티드 | 다낭성 난소 증후군을 치료하기 위한 방법 및 조성물 |
| US20240024330A1 (en) * | 2020-08-26 | 2024-01-25 | Neurocrine Biosciences, Inc. | Crf receptor antagonists and methods of use |
| US11708372B2 (en) | 2021-11-19 | 2023-07-25 | Spruce Biosciences, Inc. | Crystalline composition of tildacerfont and methods of use and preparation thereof |
| WO2025188842A1 (en) * | 2024-03-08 | 2025-09-12 | Spruce Biosciences, Inc. | Amorphous solid dispersion of tildacerfont formulations |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU713673B2 (en) | 1996-02-07 | 1999-12-09 | Neurocrine Biosciences Inc. | Pyrazolopyrimidines as crf receptor antagonists |
| ATE301657T1 (de) | 1998-01-28 | 2005-08-15 | Bristol Myers Squibb Pharma Co | Azolo-pyrimidine |
| IL137019A (en) * | 1998-01-28 | 2010-11-30 | Du Pont Pharm Co | 2,7 - dimethyl - 4 - (substituted amino) - 8 - arylpyrazolo [1,5-a] triazine derivatives and pharmaceutical compositions containing them |
| PL351069A1 (en) * | 1999-12-08 | 2003-03-10 | Pharmacia Corp | Valdecoxib compositions |
| EP1722826A2 (en) * | 2004-02-13 | 2006-11-22 | SB Pharmco Puerto Rico Inc. | Crf receptor antagonists, their preparations, their pharmaceutical composition and their uses |
| EP1869049B1 (en) * | 2005-03-21 | 2009-03-04 | Eli Lilly And Company | Imidazopyridazine compounds |
| HRP20100516T1 (hr) * | 2006-09-20 | 2010-10-31 | Eli Lilly And Company | Tiazolpirazolopirimidini kao antagonisti receptora crf1 |
| JP5184536B2 (ja) * | 2006-09-20 | 2013-04-17 | イーライ リリー アンド カンパニー | チオフェンピラゾロピリミジン化合物 |
| DK2350079T3 (da) * | 2008-10-02 | 2012-12-17 | Lilly Co Eli | Thiazolylpyrazolopyrimidinforbindelser som syntetiske mellemprodukter og dertil relaterede syntetiske fremgangsmåder |
| JP7285222B2 (ja) | 2017-08-14 | 2023-06-01 | スプルース バイオサイエンシズ インコーポレイテッド | 副腎皮質刺激ホルモン放出因子受容体拮抗薬 |
-
2018
- 2018-08-14 JP JP2019572820A patent/JP7285222B2/ja active Active
- 2018-08-14 BR BR112020002966-1A patent/BR112020002966A2/pt not_active Application Discontinuation
- 2018-08-14 MX MX2019015318A patent/MX2019015318A/es unknown
- 2018-08-14 EP EP18846043.0A patent/EP3630763A4/en active Pending
- 2018-08-14 TW TW112117030A patent/TW202400179A/zh unknown
- 2018-08-14 KR KR1020207005534A patent/KR102644781B1/ko active Active
- 2018-08-14 CA CA3064445A patent/CA3064445A1/en active Pending
- 2018-08-14 AU AU2018318990A patent/AU2018318990B2/en not_active Ceased
- 2018-08-14 TW TW107128345A patent/TWI803504B/zh active
- 2018-08-14 WO PCT/US2018/046707 patent/WO2019036472A1/en not_active Ceased
- 2018-08-14 US US16/639,540 patent/US20210137935A1/en not_active Abandoned
- 2018-08-14 EA EA202090321A patent/EA202090321A1/ru unknown
- 2018-08-14 CN CN201880038596.0A patent/CN110997667A/zh active Pending
- 2018-08-14 AR ARP180102314 patent/AR112471A1/es unknown
-
2019
- 2019-12-16 MX MX2022015858A patent/MX2022015858A/es unknown
-
2023
- 2023-03-20 AU AU2023201703A patent/AU2023201703B2/en not_active Ceased
- 2023-05-22 JP JP2023084119A patent/JP7720354B2/ja active Active
-
2024
- 2024-12-16 AU AU2024278470A patent/AU2024278470A1/en not_active Abandoned
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