RU2020121150A - Твердые формы ингибитора калликреина плазмы и его солей - Google Patents
Твердые формы ингибитора калликреина плазмы и его солей Download PDFInfo
- Publication number
- RU2020121150A RU2020121150A RU2020121150A RU2020121150A RU2020121150A RU 2020121150 A RU2020121150 A RU 2020121150A RU 2020121150 A RU2020121150 A RU 2020121150A RU 2020121150 A RU2020121150 A RU 2020121150A RU 2020121150 A RU2020121150 A RU 2020121150A
- Authority
- RU
- Russia
- Prior art keywords
- solid form
- ray powder
- powder diffraction
- compound
- formula
- Prior art date
Links
- 239000007787 solid Substances 0.000 title claims 46
- 229940126155 plasma kallikrein inhibitor Drugs 0.000 title 1
- 238000000634 powder X-ray diffraction Methods 0.000 claims 21
- 150000001875 compounds Chemical class 0.000 claims 18
- 238000000034 method Methods 0.000 claims 15
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims 12
- 239000002904 solvent Substances 0.000 claims 12
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 8
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 8
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 230000001404 mediated effect Effects 0.000 claims 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- 230000005855 radiation Effects 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 5
- 238000001757 thermogravimetry curve Methods 0.000 claims 5
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims 4
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 4
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 4
- 201000011190 diabetic macular edema Diseases 0.000 claims 4
- 238000001938 differential scanning calorimetry curve Methods 0.000 claims 4
- 239000011877 solvent mixture Substances 0.000 claims 4
- ZWEHNKRNPOVVGH-UHFFFAOYSA-N 2-Butanone Chemical compound CCC(C)=O ZWEHNKRNPOVVGH-UHFFFAOYSA-N 0.000 claims 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims 3
- 206010019860 Hereditary angioedema Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 230000002207 retinal effect Effects 0.000 claims 3
- 230000008728 vascular permeability Effects 0.000 claims 3
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical class CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N Tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 238000001356 surgical procedure Methods 0.000 claims 2
- 206010001052 Acute respiratory distress syndrome Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 206010008111 Cerebral haemorrhage Diseases 0.000 claims 1
- 208000032843 Hemorrhage Diseases 0.000 claims 1
- 208000001953 Hypotension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 208000013616 Respiratory Distress Syndrome Diseases 0.000 claims 1
- 206010040070 Septic Shock Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 208000011341 adult acute respiratory distress syndrome Diseases 0.000 claims 1
- 201000000028 adult respiratory distress syndrome Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical class OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 claims 1
- 230000000740 bleeding effect Effects 0.000 claims 1
- 239000008280 blood Substances 0.000 claims 1
- 210000004369 blood Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000002612 cardiopulmonary effect Effects 0.000 claims 1
- 230000015271 coagulation Effects 0.000 claims 1
- 238000005345 coagulation Methods 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 230000036543 hypotension Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000002467 phosphate group Chemical class [H]OP(=O)(O[H])O[*] 0.000 claims 1
- 208000004644 retinal vein occlusion Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000036303 septic shock Effects 0.000 claims 1
- 239000000243 solution Substances 0.000 claims 1
- 150000003467 sulfuric acid derivatives Chemical class 0.000 claims 1
- YLQBMQCUIZJEEH-UHFFFAOYSA-N tetrahydrofuran Natural products C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000005490 tosylate group Chemical class 0.000 claims 1
- 230000004304 visual acuity Effects 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0048—Eye, e.g. artificial tears
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Ophthalmology & Optometry (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762592140P | 2017-11-29 | 2017-11-29 | |
| GB1719881.3 | 2017-11-29 | ||
| GBGB1719881.3A GB201719881D0 (en) | 2017-11-29 | 2017-11-29 | Solid forms of plasma kallikrein inhibitor and salts thereof |
| US62/592,140 | 2017-11-29 | ||
| PCT/GB2018/053466 WO2019106377A1 (en) | 2017-11-29 | 2018-11-29 | Solid forms of a plasma kallikrein inhibitor and salts thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2020121150A true RU2020121150A (ru) | 2021-12-29 |
Family
ID=60950492
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2020121150A RU2020121150A (ru) | 2017-11-29 | 2018-11-29 | Твердые формы ингибитора калликреина плазмы и его солей |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11584735B2 (enExample) |
| EP (1) | EP3717469A1 (enExample) |
| JP (1) | JP2021504310A (enExample) |
| KR (1) | KR20200094142A (enExample) |
| CN (1) | CN111433197A (enExample) |
| AU (1) | AU2018374541B2 (enExample) |
| BR (1) | BR112020010064A2 (enExample) |
| CA (1) | CA3082304A1 (enExample) |
| GB (1) | GB201719881D0 (enExample) |
| IL (1) | IL274555A (enExample) |
| MX (1) | MX2020005422A (enExample) |
| RU (1) | RU2020121150A (enExample) |
| WO (1) | WO2019106377A1 (enExample) |
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| TWI636047B (zh) | 2013-08-14 | 2018-09-21 | 英商卡爾維斯塔製藥有限公司 | 雜環衍生物 |
| GB201421085D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | New enzyme inhibitors |
| GB201421083D0 (en) | 2014-11-27 | 2015-01-14 | Kalvista Pharmaceuticals Ltd | Enzyme inhibitors |
| JP6884801B2 (ja) | 2016-05-31 | 2021-06-09 | カルビスタ・ファーマシューティカルズ・リミテッド | 血漿カリクレインインヒビターとしてのピラゾール誘導体 |
| GB201609607D0 (en) | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts |
| GB201609603D0 (en) * | 2016-06-01 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide |
| GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
| MX2020005168A (es) | 2017-11-29 | 2020-08-20 | Kalvista Pharmaceuticals Ltd | Formas de dosificacion que contienen un inhibidor calicreina de plasma. |
| CN112135825A (zh) | 2018-03-13 | 2020-12-25 | 夏尔人类遗传性治疗公司 | 血浆激肽释放酶抑制剂及其用途 |
| US11306061B2 (en) * | 2019-07-08 | 2022-04-19 | Rezolute, Inc. | Crystalline forms of plasma kallikrein inhibitors |
| EP4010333A1 (en) | 2019-08-09 | 2022-06-15 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
| JP7695232B2 (ja) | 2019-09-18 | 2025-06-18 | 武田薬品工業株式会社 | ヘテロアリール血漿カリクレインインヒビター |
| ES2987744T3 (es) | 2019-09-18 | 2024-11-18 | Takeda Pharmaceuticals Co | Inhibidores de calicreína plasmática y usos de los mismos |
| WO2022079446A1 (en) | 2020-10-15 | 2022-04-21 | Kalvista Pharmaceuticals Limited | Treatments of angioedema |
| WO2022172006A1 (en) | 2021-02-09 | 2022-08-18 | Kalvista Pharmaceuticals Limited | Treatments of hereditary angioedema |
| WO2023002219A1 (en) | 2021-07-23 | 2023-01-26 | Kalvista Pharmaceuticals Limited | Treatments of hereditary angioedema |
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-
2017
- 2017-11-29 GB GBGB1719881.3A patent/GB201719881D0/en not_active Ceased
-
2018
- 2018-11-29 JP JP2020526923A patent/JP2021504310A/ja not_active Ceased
- 2018-11-29 RU RU2020121150A patent/RU2020121150A/ru unknown
- 2018-11-29 EP EP18815306.8A patent/EP3717469A1/en not_active Withdrawn
- 2018-11-29 CA CA3082304A patent/CA3082304A1/en active Pending
- 2018-11-29 MX MX2020005422A patent/MX2020005422A/es unknown
- 2018-11-29 WO PCT/GB2018/053466 patent/WO2019106377A1/en not_active Ceased
- 2018-11-29 CN CN201880077596.1A patent/CN111433197A/zh active Pending
- 2018-11-29 KR KR1020207015220A patent/KR20200094142A/ko not_active Withdrawn
- 2018-11-29 BR BR112020010064-1A patent/BR112020010064A2/pt not_active IP Right Cessation
- 2018-11-29 AU AU2018374541A patent/AU2018374541B2/en not_active Withdrawn - After Issue
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2020
- 2020-05-10 IL IL274555A patent/IL274555A/en unknown
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2023
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| US20210171496A1 (en) | 2021-06-10 |
| US20230203012A1 (en) | 2023-06-29 |
| IL274555A (en) | 2020-06-30 |
| GB201719881D0 (en) | 2018-01-10 |
| JP2021504310A (ja) | 2021-02-15 |
| MX2020005422A (es) | 2020-08-27 |
| US11584735B2 (en) | 2023-02-21 |
| CA3082304A1 (en) | 2019-06-06 |
| CN111433197A (zh) | 2020-07-17 |
| KR20200094142A (ko) | 2020-08-06 |
| WO2019106377A1 (en) | 2019-06-06 |
| EP3717469A1 (en) | 2020-10-07 |
| AU2018374541A1 (en) | 2020-05-28 |
| BR112020010064A2 (pt) | 2020-11-03 |
| AU2018374541B2 (en) | 2022-12-22 |
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