BR112017010882B8 - Compostos de n-((het)-arilmetil)-heteroaril-carboxamidas como inibidores de calicreína plasmática e seus usos - Google Patents
Compostos de n-((het)-arilmetil)-heteroaril-carboxamidas como inibidores de calicreína plasmática e seus usosInfo
- Publication number
- BR112017010882B8 BR112017010882B8 BR112017010882A BR112017010882A BR112017010882B8 BR 112017010882 B8 BR112017010882 B8 BR 112017010882B8 BR 112017010882 A BR112017010882 A BR 112017010882A BR 112017010882 A BR112017010882 A BR 112017010882A BR 112017010882 B8 BR112017010882 B8 BR 112017010882B8
- Authority
- BR
- Brazil
- Prior art keywords
- compounds
- plasma kallikrein
- arylmethyl
- het
- heteroaryl
- Prior art date
Links
- 102000003827 Plasma Kallikrein Human genes 0.000 title abstract 3
- 108090000113 Plasma Kallikrein Proteins 0.000 title abstract 3
- 229940127379 Kallikrein Inhibitors Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
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- 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
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/10—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 two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
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- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- 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
- C07D401/02—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 two hetero rings
- C07D401/06—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 two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Urology & Nephrology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Vascular Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
compostos de n-((het)-arilmetil)- heteroaril-carboxamidas como inibidores de calicreína plasmática. a presente invenção refere-se a compostos de fórmula (i): composições compreendendo tais compostos; o uso de tais compostos em terapia (por exemplo, no tratamento ou prevenção de uma doença ou condição em que a atividade de calicreína plasmática está implicada); e métodos de tratamento de pacientes com tais compostos; em que r5, r6, r7, a, b, w, x, y e z são como definidos aqui.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB1421083.5 | 2014-11-27 | ||
GBGB1421083.5A GB201421083D0 (en) | 2014-11-27 | 2014-11-27 | Enzyme inhibitors |
PCT/GB2015/053615 WO2016083820A1 (en) | 2014-11-27 | 2015-11-26 | N-((het)arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors, |
Publications (3)
Publication Number | Publication Date |
---|---|
BR112017010882A2 BR112017010882A2 (pt) | 2017-12-26 |
BR112017010882B8 true BR112017010882B8 (pt) | 2023-10-31 |
BR112017010882B1 BR112017010882B1 (pt) | 2023-10-31 |
Family
ID=52349552
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BR112017010882-8A BR112017010882B1 (pt) | 2014-11-27 | 2015-11-26 | Compostos de n-((het)-arilmetil)-heteroaril-carboxamidas como inibidores de calicreína plasmática |
Country Status (37)
Country | Link |
---|---|
US (6) | US10364238B2 (pt) |
EP (4) | EP4039681A1 (pt) |
JP (4) | JP6653702B2 (pt) |
KR (2) | KR102267623B1 (pt) |
CN (2) | CN107108576B (pt) |
AR (2) | AR102850A1 (pt) |
AU (2) | AU2015352193B2 (pt) |
BR (1) | BR112017010882B1 (pt) |
CA (1) | CA2967894C (pt) |
CL (1) | CL2017001362A1 (pt) |
CO (1) | CO2017006230A2 (pt) |
CY (3) | CY1122255T1 (pt) |
DK (3) | DK3224256T3 (pt) |
EC (1) | ECSP17039127A (pt) |
ES (3) | ES2908303T3 (pt) |
GB (1) | GB201421083D0 (pt) |
HK (1) | HK1244268A1 (pt) |
HR (3) | HRP20220314T1 (pt) |
HU (3) | HUE053317T2 (pt) |
IL (2) | IL278182B (pt) |
LT (3) | LT3224256T (pt) |
MA (3) | MA41014B1 (pt) |
MD (3) | MD3567037T2 (pt) |
ME (1) | ME03514B (pt) |
MX (2) | MX2020013038A (pt) |
MY (1) | MY176853A (pt) |
NZ (1) | NZ731945A (pt) |
PH (1) | PH12017500901A1 (pt) |
PL (3) | PL3224256T3 (pt) |
PT (3) | PT3556752T (pt) |
RS (3) | RS59395B1 (pt) |
RU (2) | RU2707870C2 (pt) |
SG (2) | SG10201907819WA (pt) |
SI (3) | SI3224256T1 (pt) |
TW (2) | TWI741377B (pt) |
UA (1) | UA123087C2 (pt) |
WO (1) | WO2016083820A1 (pt) |
Families Citing this family (31)
Publication number | Priority date | Publication date | Assignee | Title |
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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 |
RS62807B1 (sr) | 2015-10-01 | 2022-02-28 | Biocryst Pharm Inc | Inhibitori humanog kalikreina plazme |
GB201609519D0 (en) * | 2016-05-31 | 2016-07-13 | Kalvista Pharmaceuticals Ltd | Polymorphs of n-[(2,6-difluoro-3-methoxyphenyl)methyl]-3-(methoxymethyl)-1-({4-[(2-oxopyr idin-1-yl)methyl]phenyl}methyl)pyrazole-4-carboxamide |
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 |
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 |
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 |
WO2018200674A1 (en) * | 2017-04-26 | 2018-11-01 | Mitobridge, Inc. | Dynamin-1-like protein inhibitors |
GB201721515D0 (en) * | 2017-12-21 | 2018-02-07 | Kalvista Pharmaceuticals Ltd | Dosage forms comprising a plasma kallikrein inhibtor |
WO2019106359A1 (en) * | 2017-11-29 | 2019-06-06 | Kalvista Pharmaceuticals Limited | Enzyme inhibitors |
IL274557B1 (en) * | 2017-11-29 | 2024-05-01 | Kalvista Pharmaceuticals Ltd | Dosage forms containing a plasma kallikrein inhibitor |
GB201719882D0 (en) * | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of a plasma kallikrein inhibitor and salts thereof |
GB201719881D0 (en) * | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
EP3765459A1 (en) | 2018-03-13 | 2021-01-20 | Shire Human Genetic Therapies, Inc. | Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof |
CA3121202A1 (en) | 2018-11-30 | 2020-06-04 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
GB201910116D0 (en) | 2019-07-15 | 2019-08-28 | Kalvista Pharmaceuticals Ltd | Treatments of hereditary angioedema |
GB201910125D0 (en) * | 2019-07-15 | 2019-08-28 | Kalvista Pharmaceuticals Ltd | Treatments of angioedema |
WO2021028645A1 (en) | 2019-08-09 | 2021-02-18 | Kalvista Pharmaceuticals Limited | Plasma kallikrein inhibitors |
EP4031547A1 (en) | 2019-09-18 | 2022-07-27 | Takeda Pharmaceutical Company Limited | Plasma kallikrein inhibitors and uses thereof |
JP2022549601A (ja) | 2019-09-18 | 2022-11-28 | 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 |
CN113004286B (zh) * | 2019-12-20 | 2022-08-12 | 成都康弘药业集团股份有限公司 | 作为血浆激肽释放酶抑制剂的三环类化合物及其用途 |
TW202144331A (zh) * | 2020-02-13 | 2021-12-01 | 德商百靈佳殷格翰國際股份有限公司 | 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物 |
EP4116299A4 (en) * | 2020-03-04 | 2024-03-27 | Medshine Discovery Inc | HETEROCYCLIC COMPOUND |
TW202228686A (zh) | 2020-10-15 | 2022-08-01 | 英商卡爾維斯塔製藥有限公司 | 血管性水腫之治療 |
WO2022084693A1 (en) | 2020-10-23 | 2022-04-28 | 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 |
WO2023185634A1 (zh) * | 2022-03-30 | 2023-10-05 | 南京明德新药研发有限公司 | 作为血浆激肽释放酶抑制剂的杂环类化合物 |
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