RU2019101889A - Полизамещенные ароматические соединения в качестве ингибиторов сериновых протеаз - Google Patents
Полизамещенные ароматические соединения в качестве ингибиторов сериновых протеаз Download PDFInfo
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- RU2019101889A RU2019101889A RU2019101889A RU2019101889A RU2019101889A RU 2019101889 A RU2019101889 A RU 2019101889A RU 2019101889 A RU2019101889 A RU 2019101889A RU 2019101889 A RU2019101889 A RU 2019101889A RU 2019101889 A RU2019101889 A RU 2019101889A
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- Prior art keywords
- substituted
- unsubstituted
- compound
- aryl
- disease
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- 102000012479 Serine Proteases Human genes 0.000 title 1
- 108010022999 Serine Proteases Proteins 0.000 title 1
- 150000001491 aromatic compounds Chemical class 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 238000000034 method Methods 0.000 claims 72
- 150000001875 compounds Chemical class 0.000 claims 41
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 36
- 125000003118 aryl group Chemical group 0.000 claims 35
- 125000001072 heteroaryl group Chemical group 0.000 claims 25
- 125000000217 alkyl group Chemical group 0.000 claims 22
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 21
- 201000010099 disease Diseases 0.000 claims 19
- 208000035475 disorder Diseases 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 16
- 125000002947 alkylene group Chemical group 0.000 claims 15
- 125000001544 thienyl group Chemical group 0.000 claims 13
- 150000002431 hydrogen Chemical class 0.000 claims 12
- 125000002541 furyl group Chemical group 0.000 claims 10
- 125000001624 naphthyl group Chemical group 0.000 claims 10
- 125000002098 pyridazinyl group Chemical group 0.000 claims 10
- 125000004076 pyridyl group Chemical group 0.000 claims 10
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 10
- 102000001399 Kallikrein Human genes 0.000 claims 9
- 108060005987 Kallikrein Proteins 0.000 claims 9
- 125000000928 benzodioxinyl group Chemical group O1C(=COC2=C1C=CC=C2)* 0.000 claims 9
- 125000004474 heteroalkylene group Chemical group 0.000 claims 9
- 125000002757 morpholinyl group Chemical group 0.000 claims 9
- 125000003566 oxetanyl group Chemical group 0.000 claims 9
- 125000004404 heteroalkyl group Chemical group 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 230000002401 inhibitory effect Effects 0.000 claims 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- 125000004366 heterocycloalkenyl group Chemical group 0.000 claims 6
- 239000000203 mixture Substances 0.000 claims 6
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 208000007536 Thrombosis Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 230000004968 inflammatory condition Effects 0.000 claims 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims 3
- 206010012438 Dermatitis atopic Diseases 0.000 claims 2
- 206010012688 Diabetic retinal oedema Diseases 0.000 claims 2
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 102100038297 Kallikrein-1 Human genes 0.000 claims 2
- 101710176219 Kallikrein-1 Proteins 0.000 claims 2
- 208000011219 Netherton syndrome Diseases 0.000 claims 2
- 102000003827 Plasma Kallikrein Human genes 0.000 claims 2
- 108090000113 Plasma Kallikrein Proteins 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 206010040047 Sepsis Diseases 0.000 claims 2
- 206010051379 Systemic Inflammatory Response Syndrome Diseases 0.000 claims 2
- 201000008937 atopic dermatitis Diseases 0.000 claims 2
- 201000011190 diabetic macular edema Diseases 0.000 claims 2
- 239000003889 eye drop Substances 0.000 claims 2
- 229940012356 eye drops Drugs 0.000 claims 2
- 239000003527 fibrinolytic agent Substances 0.000 claims 2
- 230000003480 fibrinolytic effect Effects 0.000 claims 2
- 239000007924 injection Substances 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 2
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 2
- 208000002780 macular degeneration Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 230000002381 testicular Effects 0.000 claims 2
- 230000000699 topical effect Effects 0.000 claims 2
- 208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 208000005189 Embolism Diseases 0.000 claims 1
- 206010014513 Embolism arterial Diseases 0.000 claims 1
- 206010014522 Embolism venous Diseases 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 208000035719 Maculopathy Diseases 0.000 claims 1
- 108090000190 Thrombin Proteins 0.000 claims 1
- 208000001435 Thromboembolism Diseases 0.000 claims 1
- 206010064930 age-related macular degeneration Diseases 0.000 claims 1
- 230000001269 cardiogenic effect Effects 0.000 claims 1
- 208000009190 disseminated intravascular coagulation Diseases 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 229960004072 thrombin Drugs 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
- 208000004043 venous thromboembolism Diseases 0.000 claims 1
- 210000004127 vitreous body Anatomy 0.000 claims 1
Classifications
-
- 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
-
- 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
- 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
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D231/38—Nitrogen 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Ophthalmology & Optometry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicinal Preparation (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361789358P | 2013-03-15 | 2013-03-15 | |
| US61/789,358 | 2013-03-15 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015144151A Division RU2678830C2 (ru) | 2013-03-15 | 2014-03-17 | Полизамещенные ароматические соединения в качестве ингибиторов сериновых протеаз |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2019101889A true RU2019101889A (ru) | 2019-03-28 |
Family
ID=51538152
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015144151A RU2678830C2 (ru) | 2013-03-15 | 2014-03-17 | Полизамещенные ароматические соединения в качестве ингибиторов сериновых протеаз |
| RU2019101889A RU2019101889A (ru) | 2013-03-15 | 2014-03-17 | Полизамещенные ароматические соединения в качестве ингибиторов сериновых протеаз |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2015144151A RU2678830C2 (ru) | 2013-03-15 | 2014-03-17 | Полизамещенные ароматические соединения в качестве ингибиторов сериновых протеаз |
Country Status (25)
| Country | Link |
|---|---|
| US (5) | US9533970B2 (OSRAM) |
| EP (2) | EP3421036B8 (OSRAM) |
| JP (3) | JP6388634B2 (OSRAM) |
| KR (1) | KR20150132148A (OSRAM) |
| CN (5) | CN110101700A (OSRAM) |
| AU (5) | AU2014232308B2 (OSRAM) |
| BR (1) | BR112015022340A2 (OSRAM) |
| CA (2) | CA2901637C (OSRAM) |
| DK (1) | DK2968297T3 (OSRAM) |
| ES (2) | ES2702182T3 (OSRAM) |
| HK (1) | HK1257685A1 (OSRAM) |
| HR (1) | HRP20182081T1 (OSRAM) |
| HU (1) | HUE042393T2 (OSRAM) |
| IL (2) | IL240691B (OSRAM) |
| LT (1) | LT2968297T (OSRAM) |
| MX (2) | MX373964B (OSRAM) |
| NZ (1) | NZ711064A (OSRAM) |
| PL (2) | PL2968297T3 (OSRAM) |
| PT (1) | PT2968297T (OSRAM) |
| RU (2) | RU2678830C2 (OSRAM) |
| SG (2) | SG10201707480PA (OSRAM) |
| SI (1) | SI2968297T1 (OSRAM) |
| TR (1) | TR201819092T4 (OSRAM) |
| WO (1) | WO2014145986A1 (OSRAM) |
| ZA (1) | ZA201506295B (OSRAM) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2017144535A (ru) * | 2010-03-30 | 2019-02-18 | Версеон Корпорейшн | Мультизамещенные ароматические соединения в качестве ингибиторов тромбина |
| BR112015023214A8 (pt) | 2013-03-15 | 2019-12-24 | Verseon Corp | composto, composição farmacêutica, e, uso de um composto ou composição farmacêutica |
| PL2968297T3 (pl) | 2013-03-15 | 2019-04-30 | Verseon Corp | Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej |
| 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 |
| US10681909B2 (en) | 2014-08-29 | 2020-06-16 | Fmc Corporation | Herbicidal triazoles |
| EP3194369A4 (en) * | 2014-09-17 | 2018-02-28 | Verseon Corporation | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
| 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 |
| JP6836996B2 (ja) * | 2015-02-25 | 2021-03-03 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | 新しいトリフルオロメチルプロパンアミド誘導体 |
| CA2977993A1 (en) * | 2015-02-27 | 2016-09-01 | Verseon Corporation | Substituted pyrazole compounds as serine protease inhibitors |
| CN106518868B (zh) * | 2015-11-04 | 2018-02-23 | 衡阳师范学院 | 激肽释放酶7小分子抑制剂及其制备方法、用途 |
| CN105218545A (zh) * | 2015-11-04 | 2016-01-06 | 衡阳师范学院 | 激肽释放酶7小分子抑制剂及其制备方法、用途 |
| CN108602787A (zh) | 2015-11-09 | 2018-09-28 | 库特克希米公司 | 精氨酸牙龈卟啉菌蛋白酶的抑制剂 |
| WO2017152842A1 (en) * | 2016-03-10 | 2017-09-14 | National Institute Of Biological Sciences, Beijing | Kinase inhibitors |
| SG11201809922YA (en) | 2016-05-31 | 2018-12-28 | Kalvista Pharmaceuticals Ltd | Pyrazole derivatives as plasma kallikrein inhibitors |
| 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 |
| RS63069B1 (sr) | 2017-11-29 | 2022-04-29 | Kalvista Pharmaceuticals Ltd | Dozni oblici koji sadrže inhibitor kalikreina plazme |
| WO2020014669A1 (en) * | 2018-07-13 | 2020-01-16 | Verseon Corporation | Thrombin inhibitors, formulations, and uses thereof |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| CA3133803A1 (en) | 2019-04-11 | 2020-10-15 | Angion Biomedica Corp. | Solid forms of (e)-3-[2-(2-thienyl)vinyl]-1h-pyrazole |
| CN114206852A (zh) | 2019-08-09 | 2022-03-18 | 卡尔维斯塔制药有限公司 | 血浆激肽释放酶抑制剂 |
| BR102020009679A2 (pt) | 2020-05-14 | 2021-11-23 | Fundação Universidade Federal Do Abc - Ufabc | Anticorpos recombinantes humanos para inibição da calicreína tecidual humana 7 (klk7) e uso em doenças relacionadas ao processo de descamação da pele |
| WO2023064458A1 (en) * | 2021-10-13 | 2023-04-20 | Yale University | Selective jak2 inhibitors and methods of use |
Family Cites Families (119)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE627393A (OSRAM) | 1962-01-23 | |||
| BE793955A (fr) | 1972-01-15 | 1973-07-12 | Merck Patent Gmbh | Arylpiperazines et leur procede de preparation |
| DE2409753A1 (de) | 1974-03-01 | 1975-09-11 | Basf Ag | Substituierte pyrazole |
| US4256108A (en) | 1977-04-07 | 1981-03-17 | Alza Corporation | Microporous-semipermeable laminated osmotic system |
| US4160452A (en) | 1977-04-07 | 1979-07-10 | Alza Corporation | Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina |
| US4265874A (en) | 1980-04-25 | 1981-05-05 | Alza Corporation | Method of delivering drug with aid of effervescent activity generated in environment of use |
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