JP2020510661A5 - - Google Patents
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- JP2020510661A5 JP2020510661A5 JP2019547093A JP2019547093A JP2020510661A5 JP 2020510661 A5 JP2020510661 A5 JP 2020510661A5 JP 2019547093 A JP2019547093 A JP 2019547093A JP 2019547093 A JP2019547093 A JP 2019547093A JP 2020510661 A5 JP2020510661 A5 JP 2020510661A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- xrpd
- anhydrous
- ray powder
- powder diffraction
- 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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- 238000000634 powder X-ray diffraction Methods 0.000 claims 14
- 239000008194 pharmaceutical composition Substances 0.000 claims 13
- 150000004682 monohydrates Chemical class 0.000 claims 6
- HVFLCNVBZFFHBT-ZKDACBOMSA-N Cefepime Chemical compound S([C@@H]1[C@@H](C(N1C=1C([O-])=O)=O)NC(=O)\C(=N/OC)C=2N=C(N)SC=2)CC=1C[N+]1(C)CCCC1 HVFLCNVBZFFHBT-ZKDACBOMSA-N 0.000 claims 4
- 229960002100 cefepime Drugs 0.000 claims 4
- ODKSFYDXXFIFQN-BYPYZUCNSA-N L-arginine Chemical compound OC(=O)[C@@H](N)CCCN=C(N)N ODKSFYDXXFIFQN-BYPYZUCNSA-N 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 2
- -1 (Trans-4- (2-aminoethylamino) cyclohexyl) acetamide Chemical compound 0.000 claims 1
- 206010060945 Bacterial infection Diseases 0.000 claims 1
- 235000014852 L-arginine Nutrition 0.000 claims 1
- 125000005605 benzo group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drugs Drugs 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- PFZUWUXKQPRWAL-NOLJZWGESA-N NCCN[C@H]1CC[C@H](CC(N[C@H]2Cc3cccc(C(O)=O)c3OB2O)=O)CC1 Chemical compound NCCN[C@H]1CC[C@H](CC(N[C@H]2Cc3cccc(C(O)=O)c3OB2O)=O)CC1 PFZUWUXKQPRWAL-NOLJZWGESA-N 0.000 description 1
Claims (15)
- （Ｒ）−３−（２−（トランス−４−（２−アミノエチルアミノ）シクロヘキシル）アセトアミド）−２−ヒドロキシ−３，４−ジヒドロ−２Ｈ−ベンゾ［ｅ］［１，２］オキサボリニン−８−カルボン酸であるジヒドロクロリドの、無水結晶形態：
- 無水結晶形態は、約７．３°±０．１°２θ、約１４．５°±０．１°２θ、約１８．０°±０．１°２θ、約１９．７°±０．１°２θ、約２４．０°±０．１°２θ、及び約２７．３°±０．１°２θで特徴ピークを含むＸ線粉末回折（ＸＲＰＤ）パターンを有する、ことを特徴とする請求項１に記載の無水結晶形態。
- Ｘ線粉末回折（ＸＲＰＤ）パターンはさらに、約１０．８°±０．１°２θ、約１６．６°±０．１°２θ、約１９．６°±０．１°２θ、約２３．３°±０．１°２θ、約２４．３°±０．１°２θ、及び約２９．３°±０．１°２θで特徴ピークを含む、ことを特徴とする請求項１または２に記載の無水結晶形態。
- Ｘ線粉末回折（ＸＲＰＤ）パターンは、約７．３°±０．１°２θ、約１０．８°±０．１°２θ、約１４．５°±０．１°２θ、約１６．６°±０．１°２θ、約１８．０°±０．１°２θ、約１９．６°±０．１°２θ、約１９．７°±０．１°２θ、約２３．３°±０．１°２θ、約２４．０°±０．１°２θ、約２４．３°±０．１°２θ、約２７．３°±０．１°２θ、及び約２９．３°±０．１°２θから選択される少なくとも３つの特徴ピークを有する、ことを特徴とする請求項１または２に記載の無水結晶形態。
- （Ｒ）−３−（２−（トランス−４−（２−アミノエチルアミノ）シクロヘキシル）アセトアミド）−２−ヒドロキシ−３，４−ジヒドロ−２Ｈ−ベンゾ［ｅ］［１，２］オキサボリニン−８−カルボン酸であるジヒドロクロリドの、一水和物結晶形態：
- 一水和物結晶形態は、約７．０°±０．１°２θ、約１４．１°±０．１°２θ、約２０．２°±０．１°２θ、約２４．６°±０．１°２θ、及び約２７．７°±０．１°２θで特徴ピークを含むＸ線粉末回折（ＸＲＰＤ）パターンを有する、ことを特徴とする請求項５に記載の一水和物結晶形態。
- Ｘ線粉末回折（ＸＲＰＤ）パターンはさらに、約１０．５°±０．１°２θ、約１８．９°±０．１°２θ、約２３．７°±０．１°２θ、約２５．６°±０．１°２θ、及び約２９．６°±０．１°２θで特徴ピークを含む、ことを特徴とする請求項６に記載の一水和物結晶形態。
- 一水和物結晶形態は、約７．０°±０．１°２θ、約１０．５°±０．１°２θ、約１４．１°±０．１°２θ、約１８．９°±０．１°２θ、約２０．２°±０．１°２θ、約２３．７°±０．１°２θ、約２４．６°±０．１°２θ、約２５．６°±０．１°２θ、約２７．７°±０．１°２θ、及び約２９．６°±０．１°２θから選択される少なくとも３つの特徴ピークを有するＸ線粉末回折（ＸＲＰＤ）パターンを有する、ことを特徴とする請求項５に記載の一水和物結晶形態。
- 医薬組成物であって、該医薬組成物は：
（ｉ）無水（Ｒ）−３−（２−（トランス−４−（２−アミノエチルアミノ）シクロヘキシル）アセトアミド）−２−ヒドロキシ−３，４−ジヒドロ−２Ｈ−ベンゾ［ｅ］［１，２］オキサボリニン−８−カルボン酸であるジヒドロクロリド；及び
（ｉｉ）セフェピム
を含む、医薬組成物。 - （ｉ）（Ｒ）−３−（２−（トランス−４−（２−アミノエチルアミノ）シクロヘキシル）アセトアミド）−２−ヒドロキシ−３，４−ジヒドロ−２Ｈ−ベンゾ［ｅ］［１，２］オキサボリニン−８−カルボン酸であるジヒドロクロリドの無水結晶形態；及び
（ｉｉ）セフェピム
を含む、ことを特徴とする請求項９に記載の医薬組成物。 - （ｉ）約７．３°±０．１°２θ、約１４．５°±０．１°２θ、約１８．０°±０．１°２θ、約１９．７°±０．１°２θ、約２４．０°±０．１°２θ、及び約２７．３°±０．１°２θで特徴ピークを含むＸ線粉末回折（ＸＲＰＤ）パターンを有する、（Ｒ）−３−（２−（トランス−４−（２−アミノエチルアミノ）シクロヘキシル）アセトアミド）−２−ヒドロキシ−３，４−ジヒドロ−２Ｈ−ベンゾ［ｅ］［１，２］オキサボリニン−８−カルボン酸であるジヒドロクロリドの無水結晶形態；及び
（ｉｉ）セフェピム
を含む、ことを特徴とする請求項９に記載の医薬組成物。 - 前記医薬組成物は注射に適している均質の液体として製剤される、ことを特徴とする請求項９から１１のいずれか１つに記載の医薬組成物。
- Ｌ−アルギニンをさらに含む、ことを特徴とする請求項９から１２のいずれか１つに記載の医薬組成物。
- 前記医薬組成物は、約５００ｍｇまたは約７５０ｍｇの（Ｒ）−３−（２−（トランス−４−（２−アミノエチルアミノ）シクロヘキシル）アセトアミド）−２−ヒドロキシ−３，４−ジヒドロ−２Ｈ−ベンゾ［ｅ］［１，２］オキサボリニン−８−カルボン酸と、約２ｇのセフェピムとを含む、ことを特徴とする請求項９から１３のいずれか１つに記載の医薬組成物。
- 必要としている被験体の細菌感染を処置するための薬剤の製造における、請求項９から１４のいずれか１つに記載の医薬組成物の使用。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023007546A JP2023061946A (ja) | 2017-03-06 | 2023-01-20 | β－ラクタマーゼ阻害剤を含む固体形態及び組み合わせ組成物並びにその使用 |
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762467752P | 2017-03-06 | 2017-03-06 | |
| US201762467750P | 2017-03-06 | 2017-03-06 | |
| US62/467,750 | 2017-03-06 | ||
| US62/467,752 | 2017-03-06 | ||
| US201762564990P | 2017-09-28 | 2017-09-28 | |
| US201762564989P | 2017-09-28 | 2017-09-28 | |
| US62/564,990 | 2017-09-28 | ||
| US62/564,989 | 2017-09-28 | ||
| PCT/US2018/020968 WO2018165048A1 (en) | 2017-03-06 | 2018-03-05 | Solid forms and combination compositions comprising a beta-lactamase inhibitor and uses thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023007546A Division JP2023061946A (ja) | 2017-03-06 | 2023-01-20 | β－ラクタマーゼ阻害剤を含む固体形態及び組み合わせ組成物並びにその使用 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020510661A JP2020510661A (ja) | 2020-04-09 |
| JP2020510661A5 true JP2020510661A5 (ja) | 2021-04-08 |
Family
ID=63448038
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019547093A Pending JP2020510661A (ja) | 2017-03-06 | 2018-03-05 | β−ラクタマーゼ阻害剤を含む固体形態及び組み合わせ組成物並びにその使用 |
| JP2023007546A Pending JP2023061946A (ja) | 2017-03-06 | 2023-01-20 | β－ラクタマーゼ阻害剤を含む固体形態及び組み合わせ組成物並びにその使用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023007546A Pending JP2023061946A (ja) | 2017-03-06 | 2023-01-20 | β－ラクタマーゼ阻害剤を含む固体形態及び組み合わせ組成物並びにその使用 |
Country Status (14)
| Country | Link |
|---|---|
| US (3) | US11091505B2 (ja) |
| EP (1) | EP3592362A4 (ja) |
| JP (2) | JP2020510661A (ja) |
| KR (1) | KR102603489B1 (ja) |
| CN (2) | CN117398398A (ja) |
| AU (1) | AU2018230991B2 (ja) |
| BR (1) | BR112019018447A2 (ja) |
| CA (1) | CA3055253A1 (ja) |
| IL (2) | IL301591A (ja) |
| MA (1) | MA47743A (ja) |
| MY (1) | MY196966A (ja) |
| PH (1) | PH12019502037A1 (ja) |
| SG (1) | SG11201908181XA (ja) |
| WO (1) | WO2018165048A1 (ja) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105026407B (zh) | 2012-12-07 | 2017-09-08 | 维纳拓尔斯制药公司 | β‑内酰胺酶抑制剂 |
| WO2014110442A1 (en) | 2013-01-10 | 2014-07-17 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| EP2970340B1 (en) | 2013-03-14 | 2020-02-12 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| EP3882252A1 (en) | 2014-06-11 | 2021-09-22 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| US9511142B2 (en) | 2014-06-11 | 2016-12-06 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| EP3347008B1 (en) | 2015-09-11 | 2022-03-09 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| WO2017100537A1 (en) | 2015-12-10 | 2017-06-15 | VenatoRx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
| WO2018027062A1 (en) | 2016-08-04 | 2018-02-08 | VenatoRx Pharmaceuticals, Inc. | Boron-containing compounds |
| US11091505B2 (en) | 2017-03-06 | 2021-08-17 | VenatoRx Pharmaceuticals, Inc. | Solid forms and combination compositions comprising a beta-lactamase inhibitor and uses thereof |
| EP3630783A4 (en) | 2017-05-26 | 2021-03-03 | Venatorx Pharmaceuticals, Inc. | PENICILLIN BINDING PROTEIN INHIBITORS |
| CN110959008A (zh) | 2017-05-26 | 2020-04-03 | 维纳拓尔斯制药公司 | 青霉素结合蛋白抑制剂 |
| EP3849562A4 (en) * | 2018-09-12 | 2022-05-18 | Venatorx Pharmaceuticals, Inc. | COMPOSITIONS IN THE FORM OF COMBINATIONS COMPRISING A BETA-LACTAMASE INHIBITOR |
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| US1021454A (en) | 1911-01-23 | 1912-03-26 | Thomas Ernest Davis | Serving-table. |
| US7271186B1 (en) | 2002-12-09 | 2007-09-18 | Northwestern University | Nanomolar β-lactamase inhibitors |
| ME01975B (me) | 2004-03-30 | 2015-05-20 | Millennium Pharm Inc | Sinteza jedinjenja estra organoborne kiseline i organoborne kiseline |
| CN1965838A (zh) | 2005-11-17 | 2007-05-23 | 李海超 | 含头孢匹胺和β－内酰胺酶抑制剂的药物组合物 |
| CN101129382B (zh) | 2006-08-25 | 2013-12-25 | 天津和美生物技术有限公司 | 含β-内酰胺类抗生素和缓冲组分的抗生素复方 |
| EA201000774A1 (ru) | 2007-11-13 | 2010-12-30 | Новартис Интернэшнл Фармасьютикл Лтд. | Ингибиторы бета-лактамазы |
| US20100120715A1 (en) | 2007-11-13 | 2010-05-13 | Burns Christopher J | Beta-lactamase inhibitors |
| PT2666774E (pt) | 2008-01-18 | 2015-04-13 | Merck Sharp & Dohme | Inibidores de beta-lactamase |
| US20100292185A1 (en) | 2009-05-12 | 2010-11-18 | Burns Christopher J | Beta-lactamase inhibitors |
| AU2011289615B2 (en) | 2010-08-10 | 2015-05-07 | Melinta Therapeutics, Inc. | Cyclic boronic acid ester derivatives and therapeutic uses thereof |
| AU2011373912B2 (en) | 2011-07-26 | 2016-09-29 | Wockhardt Limited | Pharmaceutical compositions comprising beta-lactam antibiotic, sulbactam and beta-lactamase inhibitor |
| WO2013053372A1 (en) | 2011-10-13 | 2013-04-18 | Therabor Pharmaceuticals | Boronic acid inhibitors of beta-lactamases |
| KR101288157B1 (ko) | 2011-12-07 | 2013-07-19 | 백병하 | 기존 세파계 항생제 및 베타 락타마제 저해제로 배합된 내성균주에 기인한 감염증의 치료 및 예방을 위한 복합항생제 |
| JP5798495B2 (ja) | 2012-01-13 | 2015-10-21 | 住友理工株式会社 | 配線体接続構造体 |
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| EP2970340B1 (en) | 2013-03-14 | 2020-02-12 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
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| US20150361107A1 (en) | 2014-06-11 | 2015-12-17 | VenatoRx Pharmaceuticals, Inc. | Orally bioavailable beta-lactamase inhibitors |
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| KR101935186B1 (ko) | 2014-09-04 | 2019-01-03 | 시오노기세야쿠 가부시키가이샤 | 카테콜기를 갖는 세팔로스포린류를 함유하는 제제 |
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| EP3347008B1 (en) | 2015-09-11 | 2022-03-09 | Venatorx Pharmaceuticals, Inc. | Beta-lactamase inhibitors |
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| WO2018027062A1 (en) | 2016-08-04 | 2018-02-08 | VenatoRx Pharmaceuticals, Inc. | Boron-containing compounds |
| US11091505B2 (en) | 2017-03-06 | 2021-08-17 | VenatoRx Pharmaceuticals, Inc. | Solid forms and combination compositions comprising a beta-lactamase inhibitor and uses thereof |
| EP3802551A4 (en) | 2018-05-25 | 2022-03-02 | Venatorx Pharmaceuticals, Inc. | PENICILLIN-BINDING PROTEIN INHIBITORS |
| EP3849562A4 (en) | 2018-09-12 | 2022-05-18 | Venatorx Pharmaceuticals, Inc. | COMPOSITIONS IN THE FORM OF COMBINATIONS COMPRISING A BETA-LACTAMASE INHIBITOR |
| CA3121130A1 (en) | 2018-11-29 | 2020-06-04 | VenatoRx Pharmaceuticals, Inc. | Combination compositions comprising a beta-lactamase inhibitor and uses thereof |
-
2018
- 2018-03-05 US US16/491,116 patent/US11091505B2/en active Active
- 2018-03-05 IL IL301591A patent/IL301591A/en unknown
- 2018-03-05 AU AU2018230991A patent/AU2018230991B2/en active Active
- 2018-03-05 SG SG11201908181X patent/SG11201908181XA/en unknown
- 2018-03-05 WO PCT/US2018/020968 patent/WO2018165048A1/en unknown
- 2018-03-05 IL IL268981A patent/IL268981B2/en unknown
- 2018-03-05 EP EP18763383.9A patent/EP3592362A4/en active Pending
- 2018-03-05 MA MA047743A patent/MA47743A/fr unknown
- 2018-03-05 MY MYPI2019005139A patent/MY196966A/en unknown
- 2018-03-05 CA CA3055253A patent/CA3055253A1/en active Pending
- 2018-03-05 JP JP2019547093A patent/JP2020510661A/ja active Pending
- 2018-03-05 CN CN202311312855.3A patent/CN117398398A/zh active Pending
- 2018-03-05 CN CN201880030083.5A patent/CN110678186A/zh active Pending
- 2018-03-05 KR KR1020197029086A patent/KR102603489B1/ko active IP Right Grant
- 2018-03-05 BR BR112019018447A patent/BR112019018447A2/pt unknown
-
2019
- 2019-09-06 PH PH12019502037A patent/PH12019502037A1/en unknown
-
2021
- 2021-06-21 US US17/353,377 patent/US11820784B2/en active Active
-
2023
- 2023-01-20 JP JP2023007546A patent/JP2023061946A/ja active Pending
- 2023-09-27 US US18/476,050 patent/US20240101580A1/en active Pending
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