TR201819092T4 - Serin proteaz inhibitörleri olarak multi-sübstüte edilmiş aromatik bileşikler. - Google Patents
Serin proteaz inhibitörleri olarak multi-sübstüte edilmiş aromatik bileşikler. Download PDFInfo
- Publication number
- TR201819092T4 TR201819092T4 TR2018/19092T TR201819092T TR201819092T4 TR 201819092 T4 TR201819092 T4 TR 201819092T4 TR 2018/19092 T TR2018/19092 T TR 2018/19092T TR 201819092 T TR201819092 T TR 201819092T TR 201819092 T4 TR201819092 T4 TR 201819092T4
- Authority
- TR
- Turkey
- Prior art keywords
- aromatic compounds
- substituted aromatic
- protease inhibitors
- serine protease
- kallikrein
- Prior art date
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- 150000001491 aromatic compounds Chemical class 0.000 title abstract 2
- 239000003001 serine protease inhibitor Substances 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 4
- 102000001399 Kallikrein Human genes 0.000 abstract 2
- 108060005987 Kallikrein Proteins 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 230000005764 inhibitory process Effects 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 125000003226 pyrazolyl group Chemical group 0.000 abstract 1
- 125000001425 triazolyl group Chemical group 0.000 abstract 1
Classifications
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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
- A61K31/4427—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
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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
- A61K31/41—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
- A61K31/4427—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
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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
- A61K31/535—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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
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- 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
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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
- C07D231/38—Nitrogen atoms
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- 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
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- 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
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- 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
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- 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
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (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)
Abstract
Burada, kallikreinin inhibisyonu için kullanışlı olan, inter alia, multi-sübstüte edilmiş aromatik bileşikler sağlanır, bu bileşikler sübstüte edilmiş pirazolili veya sübstüte edilmiş triazolili içerir. İlave olarak, burada farmasötik bileşimler sağlanır. Ek olarak, burada belirli hastalıkları veya bozuklukları tedavi etmenin ve önlemenin yöntemleri sağlanır, bu hastalık veya bozukluk kallikreinin inhibisyonu ile tedavi veya önlenme için uygundur.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361789358P | 2013-03-15 | 2013-03-15 |
Publications (1)
Publication Number | Publication Date |
---|---|
TR201819092T4 true TR201819092T4 (tr) | 2019-01-21 |
Family
ID=51538152
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
TR2018/19092T TR201819092T4 (tr) | 2013-03-15 | 2014-03-17 | Serin proteaz inhibitörleri olarak multi-sübstüte edilmiş aromatik bileşikler. |
Country Status (25)
Country | Link |
---|---|
US (5) | US9533970B2 (tr) |
EP (2) | EP3421036B8 (tr) |
JP (3) | JP6388634B2 (tr) |
KR (1) | KR20150132148A (tr) |
CN (5) | CN108354933A (tr) |
AU (5) | AU2014232308B2 (tr) |
BR (1) | BR112015022340A2 (tr) |
CA (2) | CA3051327A1 (tr) |
DK (1) | DK2968297T3 (tr) |
ES (2) | ES2853483T3 (tr) |
HK (2) | HK1214142A1 (tr) |
HR (1) | HRP20182081T1 (tr) |
HU (1) | HUE042393T2 (tr) |
IL (2) | IL240691B (tr) |
LT (1) | LT2968297T (tr) |
MX (2) | MX2015012867A (tr) |
NZ (1) | NZ711064A (tr) |
PL (2) | PL3421036T3 (tr) |
PT (1) | PT2968297T (tr) |
RU (2) | RU2678830C2 (tr) |
SG (2) | SG10201707480PA (tr) |
SI (1) | SI2968297T1 (tr) |
TR (1) | TR201819092T4 (tr) |
WO (1) | WO2014145986A1 (tr) |
ZA (1) | ZA201506295B (tr) |
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CN110423221A (zh) | 2013-03-15 | 2019-11-08 | 维颂公司 | 作为凝血酶抑制剂的卤代吡唑 |
NZ711064A (en) * | 2013-03-15 | 2019-06-28 | Verseon Corp | Pyridone-substituted pyrazolyl compounds as serine protease inhibitors |
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 |
BR112017003918B1 (pt) | 2014-08-29 | 2022-05-03 | Fmc Corporation | Composto, composições e mistura herbicida e método para o controle do crescimento da vegetação |
WO2016044662A1 (en) * | 2014-09-17 | 2016-03-24 | 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 |
WO2016135070A1 (en) * | 2015-02-25 | 2016-09-01 | F. Hoffmann-La Roche Ag | New trifluoromethylpropanamide derivatives |
HUE060104T2 (hu) | 2015-02-27 | 2023-01-28 | Verseon Int Corporation | Szubsztituált pirazol vegyületek mint szerinproteázinhibitorok |
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 |
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 |
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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 |
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GB201719881D0 (en) | 2017-11-29 | 2018-01-10 | Kalvista Pharmaceuticals Ltd | Solid forms of plasma kallikrein inhibitor and salts thereof |
JP2021531338A (ja) * | 2018-07-13 | 2021-11-18 | ヴァーセオン インターナショナル コーポレイション | トロンビン阻害薬、製剤、及びそれらの使用 |
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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 |
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