CA2920815C - Inhibitors of plasma kallikrein - Google Patents

Inhibitors of plasma kallikrein Download PDF

Info

Publication number
CA2920815C
CA2920815C CA2920815A CA2920815A CA2920815C CA 2920815 C CA2920815 C CA 2920815C CA 2920815 A CA2920815 A CA 2920815A CA 2920815 A CA2920815 A CA 2920815A CA 2920815 C CA2920815 C CA 2920815C
Authority
CA
Canada
Prior art keywords
carboxamide
aminoisoquinolin
formula
yomethyl
group
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.)
Active
Application number
CA2920815A
Other languages
English (en)
French (fr)
Other versions
CA2920815A1 (en
Inventor
Hannah Joy EDWARDS
David Michael Evans
Premji Meghani
Andrew Richard NOVAK
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Kalvista Pharmaceuticals Ltd
Original Assignee
Kalvista Pharmaceuticals Ltd
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Kalvista Pharmaceuticals Ltd filed Critical Kalvista Pharmaceuticals Ltd
Publication of CA2920815A1 publication Critical patent/CA2920815A1/en
Application granted granted Critical
Publication of CA2920815C publication Critical patent/CA2920815C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • 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
    • A61K31/455—Nicotinic acids, e.g. niacin; Derivatives thereof, e.g. esters, amides
    • 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
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/495—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
    • 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
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • 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
    • 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
    • A61P9/12—Antihypertensives
    • 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
    • C07D401/12—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 chain containing hetero atoms as chain links
    • 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
    • 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
    • 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
    • C07D403/14—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 three or more hetero 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Obesity (AREA)
  • Ophthalmology & Optometry (AREA)
  • Endocrinology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CA2920815A 2013-08-14 2014-08-14 Inhibitors of plasma kallikrein Active CA2920815C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361865756P 2013-08-14 2013-08-14
US201361865732P 2013-08-14 2013-08-14
US61/865,756 2013-08-14
US61/865,732 2013-08-14
PCT/GB2014/052510 WO2015022546A1 (en) 2013-08-14 2014-08-14 Inhibitors of plasma kallikrein

Publications (2)

Publication Number Publication Date
CA2920815A1 CA2920815A1 (en) 2015-02-19
CA2920815C true CA2920815C (en) 2021-09-21

Family

ID=51392282

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2920815A Active CA2920815C (en) 2013-08-14 2014-08-14 Inhibitors of plasma kallikrein

Country Status (11)

Country Link
US (1) US10221161B2 (enExample)
EP (1) EP3033336B1 (enExample)
JP (1) JP6527147B2 (enExample)
CN (1) CN105683179B (enExample)
CA (1) CA2920815C (enExample)
ES (1) ES2674088T3 (enExample)
HU (1) HUE14755117T2 (enExample)
MX (1) MX366498B (enExample)
PL (1) PL3033336T3 (enExample)
RU (1) RU2674028C2 (enExample)
WO (1) WO2015022546A1 (enExample)

Families Citing this family (30)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US9611252B2 (en) 2013-12-30 2017-04-04 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
KR20160106627A (ko) * 2013-12-30 2016-09-12 라이프에스씨아이 파마슈티컬스, 인크. 치료적 억제 화합물
JP6951970B2 (ja) * 2014-07-16 2021-10-20 ライフサイ ファーマシューティカルズ，インク． 治療用阻害化合物
US9463201B2 (en) 2014-10-19 2016-10-11 M.G. Therapeutics Ltd Compositions and methods for the treatment of meibomian gland dysfunction
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
US9815853B2 (en) 2015-06-12 2017-11-14 Global Blood Therapeutics, Inc. Bridged bicyclic kallikrein inhibitors
US10981893B2 (en) 2015-07-01 2021-04-20 Attune Pharmaceuticals, Inc. Therapeutic inhibitory compounds
US20190263818A1 (en) * 2015-07-01 2019-08-29 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
CA3000088A1 (en) 2015-09-28 2017-04-06 Azura Ophthalmics Ltd. Thiol and disulfide-containing agents for increasing meibomian gland lipid secretion
US11040062B2 (en) 2016-04-14 2021-06-22 Azura Ophthalmics Ltd. Selenium disulfide compositions for use in treating meibomian gland dysfunction
RS60600B1 (sr) 2016-05-31 2020-08-31 Kalvista Pharmaceuticals Ltd Derivati pirazola kao inhibitori kalikreina plazme
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
WO2018011628A1 (en) 2016-07-11 2018-01-18 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
GB201721515D0 (en) * 2017-12-21 2018-02-07 Kalvista Pharmaceuticals Ltd Dosage forms comprising a plasma kallikrein inhibtor
PL3716952T3 (pl) 2017-11-29 2022-05-02 Kalvista Pharmaceuticals Limited Postacie dawkowania zawierające inhibitor kalikreiny osoczowej
EP3758702A4 (en) * 2018-02-28 2021-11-10 Attune Pharmaceuticals, Inc. TREATMENT OF HEREDITARY ANGIOEDEMA
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
EP3837252B1 (en) * 2018-08-16 2025-12-10 Boehringer Ingelheim International GmbH Heteroaromatic carboxamide derivatives as plasma kallikrein inhibitors
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
DK4031547T3 (da) 2019-09-18 2024-09-09 Takeda Pharmaceuticals Co Plasmakallikreininhibitorer og anvendelser deraf
CN114667289B (zh) 2019-09-18 2025-08-26 武田药品工业有限公司 杂芳基血浆激肽释放酶抑制剂
WO2021121396A1 (zh) * 2019-12-20 2021-06-24 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
WO2021138540A1 (en) 2020-01-03 2021-07-08 Berg Llc Polycyclic amides as ube2k modulators for treating cancer
CA3166357A1 (en) 2020-01-10 2021-07-15 Azura Ophthalmics Ltd. Instructions for composition and sensitivity
TW202448473A (zh) * 2023-02-16 2024-12-16 南韓商治納輔醫藥科技有限公司 包含ｓｏｓ１抑制劑及抗癌藥物的用於治療癌症之藥學組成物
WO2025153806A1 (en) 2024-01-15 2025-07-24 Kalvista Pharmaceuticals Limited Methods for determining amidolytic activity

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5187157A (en) 1987-06-05 1993-02-16 Du Pont Merck Pharmaceutical Company Peptide boronic acid inhibitors of trypsin-like proteases
GB9019558D0 (en) 1990-09-07 1990-10-24 Szelke Michael Enzyme inhibitors
SE9301911D0 (sv) 1993-06-03 1993-06-03 Ab Astra New peptide derivatives
US5589467A (en) 1993-09-17 1996-12-31 Novo Nordisk A/S 2,5',N6-trisubstituted adenosine derivatives
SI1441734T1 (sl) 2001-10-26 2007-08-31 Angeletti P Ist Richerche Bio Dihidropirimidin karboksamidni inhibitorji HIV-integraze
GB0205527D0 (en) 2002-03-08 2002-04-24 Ferring Bv Inhibitors
ATE551324T1 (de) * 2003-02-03 2012-04-15 Janssen Pharmaceutica Nv Chinolin-amid-derivate als modulatoren von vanilloid-vr1-rezeptoren
KR101471732B1 (ko) 2003-08-27 2014-12-16 옵쏘테크 코포레이션 안구의 혈관신생성 장애를 치료하기 위한 조합 치료법
GB0403155D0 (en) * 2004-02-12 2004-03-17 Vernalis Res Ltd Chemical compounds
US7417063B2 (en) * 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
US7429604B2 (en) * 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
US20070254894A1 (en) * 2006-01-10 2007-11-01 Kane John L Jr Novel small molecules with selective cytotoxicity against human microvascular endothelial cell proliferation
JP5322935B2 (ja) 2006-07-31 2013-10-23 アクティベサイト ファーマシューティカルズ インコーポレイティッド 血漿カリクレインの阻害薬
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
KR20150090281A (ko) 2006-12-29 2015-08-05 아비에 도이치란트 게엠베하 운트 콤파니 카게 카복스아미드 화합물 및 칼페인 억제제로서의 이의 용도
WO2008109180A2 (en) * 2007-03-07 2008-09-12 Alantos Pharmaceuticals Holding, Inc. Metalloprotease inhibitors containing a heterocyclic moiety
EP2142516B1 (en) * 2007-03-30 2012-12-26 Sanofi Pyrimidine hydrazide compounds as pgds inhibitors
WO2009083553A1 (en) 2007-12-31 2009-07-09 Rheoscience A/S Azine compounds as glucokinase activators
US8324385B2 (en) * 2008-10-30 2012-12-04 Madrigal Pharmaceuticals, Inc. Diacylglycerol acyltransferase inhibitors
GB0910003D0 (en) 2009-06-11 2009-07-22 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
SG10201408429UA (en) 2009-12-18 2015-02-27 Activesite Pharmaceuticals Inc Prodrugs of inhibitors of plasma kallikrein
JP2013121919A (ja) 2010-03-25 2013-06-20 Astellas Pharma Inc 血漿カリクレイン阻害剤
WO2012004678A2 (en) 2010-07-07 2012-01-12 The Medicines Company (Leipzig) Gmbh Serine protease inhibitors
US9290485B2 (en) 2010-08-04 2016-03-22 Novartis Ag N-((6-amino-pyridin-3-yl)methyl)-heteroaryl-carboxamides
EP2458315B1 (de) 2010-11-25 2017-01-04 Balcke-Dürr GmbH Regenerativer Wärmetauscher mit zwangsgeführter Rotordichtung
EP2697196A1 (en) 2011-04-13 2014-02-19 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
US20140378474A1 (en) * 2012-01-27 2014-12-25 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
US20140350034A1 (en) 2012-01-27 2014-11-27 Novartis Ag Aminopyridine derivatives as plasma kallikrein inhibitors
GB201300304D0 (en) * 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
EP3305778B1 (en) * 2013-05-23 2022-01-19 Kalvista Pharmaceuticals Limited Inhibitors of plasma kallikrein
KR20160106627A (ko) 2013-12-30 2016-09-12 라이프에스씨아이 파마슈티컬스, 인크. 치료적 억제 화합물
WO2015171526A2 (en) 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Tricyclic pyrazolopyridine compounds
US9695166B2 (en) 2014-05-05 2017-07-04 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
JP6951970B2 (ja) 2014-07-16 2021-10-20 ライフサイ ファーマシューティカルズ，インク． 治療用阻害化合物

Also Published As

Publication number Publication date
MX366498B (es) 2019-07-11
WO2015022546A1 (en) 2015-02-19
ES2674088T3 (es) 2018-06-27
JP2016530262A (ja) 2016-09-29
JP6527147B2 (ja) 2019-06-05
PL3033336T3 (pl) 2018-11-30
CN105683179A (zh) 2016-06-15
EP3033336B1 (en) 2018-05-30
RU2016108753A3 (enExample) 2018-05-03
EP3033336A1 (en) 2016-06-22
CN105683179B (zh) 2018-10-26
HUE14755117T2 (hu) 2018-12-28
RU2016108753A (ru) 2017-09-19
RU2674028C2 (ru) 2018-12-04
US20160168123A1 (en) 2016-06-16
CA2920815A1 (en) 2015-02-19
US10221161B2 (en) 2019-03-05
MX2016001864A (es) 2016-05-24

Similar Documents

Publication Publication Date Title
CA2920815C (en) Inhibitors of plasma kallikrein
AU2021200140B2 (en) Pyrazole derivatives as plasma kallikrein inhibitors
AU2014270152B2 (en) Heterocyclic derivates
CA2967894C (en) N-((het)arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors
CA2920817C (en) Bicyclic inhibitors of plasma kallikrein
CA2967737C (en) N-((het)arylmethyl)-heteroaryl-carboxamides compounds as plasma kallikrein inhibitors
WO2019106359A1 (en) Enzyme inhibitors
EP4017849A1 (en) Enzyme inhibitors
US20220153724A1 (en) Inhibitors Of Plasma Kallikrein
NZ788182A (en) Pyrazole derivatives as plasma kallikrein inhibitors
NZ714027B2 (en) Heterocyclic derivates

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20190808