BR112018074395A2 - derivados de pirazol como inibidores de calicreína plasmática - Google Patents

derivados de pirazol como inibidores de calicreína plasmática

Info

Publication number
BR112018074395A2
BR112018074395A2 BR112018074395-0A BR112018074395A BR112018074395A2 BR 112018074395 A2 BR112018074395 A2 BR 112018074395A2 BR 112018074395 A BR112018074395 A BR 112018074395A BR 112018074395 A2 BR112018074395 A2 BR 112018074395A2
Authority
BR
Brazil
Prior art keywords
plasma kallikrein
inhibitors
pyrazole derivatives
compounds
implicated
Prior art date
Application number
BR112018074395-0A
Other languages
English (en)
Inventor
Louise Davie Rebecca
Joy Edwards Hannah
Michael Evans David
Teanby Hodgson Simon
John Pethen Stephen
Philip Rooker David
Original Assignee
Kalvista Pharmaceuticals Limited
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=60478506&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112018074395(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from GBGB1609517.6A external-priority patent/GB201609517D0/en
Priority claimed from GBGB1702044.7A external-priority patent/GB201702044D0/en
Application filed by Kalvista Pharmaceuticals Limited filed Critical Kalvista Pharmaceuticals Limited
Publication of BR112018074395A2 publication Critical patent/BR112018074395A2/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/04Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/08Plasma substitutes; Perfusion solutions; Dialytics or haemodialytics; Drugs for electrolytic or acid-base disorders, e.g. hypovolemic shock
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/10Antioedematous agents; Diuretics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/02Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/06Heterocyclic 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 only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/10Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Epidemiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

a presente invenção provê uma seleção de compostos de fórmula (i): (i) (i) composições compreendendo tais compostos; o uso de tais compostos em terapia (por exemplo no tratamento ou prevenção de uma doença ou condição na qual a atividade da 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 conforme definidos no presente documento.
BR112018074395-0A 2016-05-31 2017-05-31 derivados de pirazol como inibidores de calicreína plasmática BR112018074395A2 (pt)

Applications Claiming Priority (9)

Application Number Priority Date Filing Date Title
US201662343363P 2016-05-31 2016-05-31
GB1609517.6 2016-05-31
GBGB1609517.6A GB201609517D0 (en) 2016-05-31 2016-05-31 Enzyme inhibitors
US62/343,363 2016-05-31
US201762456219P 2017-02-08 2017-02-08
US62/456,219 2017-02-08
GB1702044.7 2017-02-08
GBGB1702044.7A GB201702044D0 (en) 2017-02-08 2017-02-08 Enzyme inhibitors
PCT/GB2017/051546 WO2017207983A1 (en) 2016-05-31 2017-05-31 Pyrazole derivatives as plasma kallikrein inhibitors

Publications (1)

Publication Number Publication Date
BR112018074395A2 true BR112018074395A2 (pt) 2019-03-06

Family

ID=60478506

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018074395-0A BR112018074395A2 (pt) 2016-05-31 2017-05-31 derivados de pirazol como inibidores de calicreína plasmática

Country Status (31)

Country Link
US (2) US11180484B2 (pt)
EP (2) EP3464271B1 (pt)
JP (2) JP6884801B2 (pt)
KR (2) KR20220107319A (pt)
CN (2) CN113387933A (pt)
AU (2) AU2017275820B2 (pt)
BR (1) BR112018074395A2 (pt)
CA (1) CA3025718A1 (pt)
CL (1) CL2018003213A1 (pt)
CO (1) CO2018012894A2 (pt)
CY (1) CY1123223T1 (pt)
DK (1) DK3464271T3 (pt)
EC (1) ECSP18094983A (pt)
ES (1) ES2805027T3 (pt)
HR (1) HRP20201131T1 (pt)
HU (1) HUE049918T2 (pt)
IL (2) IL293304A (pt)
LT (1) LT3464271T (pt)
MD (1) MD3464271T2 (pt)
ME (1) ME03794B (pt)
MX (2) MX2018014188A (pt)
PH (1) PH12018502355A1 (pt)
PL (1) PL3464271T3 (pt)
PT (1) PT3464271T (pt)
RS (1) RS60600B1 (pt)
RU (2) RU2020140891A (pt)
SG (2) SG11201809922YA (pt)
SI (1) SI3464271T1 (pt)
UA (1) UA123735C2 (pt)
WO (1) WO2017207983A1 (pt)
ZA (1) ZA201808639B (pt)

Families Citing this family (25)

* 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
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
SI3464271T1 (sl) 2016-05-31 2020-10-30 Kalvista Pharmaceuticals Limited Derivati pirazola kot inhibitorji plazemskega kalikreina
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
TW201925188A (zh) * 2017-11-29 2019-07-01 英商卡爾維斯塔製藥有限公司 酶抑制劑
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
DK3716952T3 (da) 2017-11-29 2022-03-14 Kalvista Pharmaceuticals Ltd Doseringsformer omfattende en plasmakallikrein-inhibitor
EP3765459A1 (en) 2018-03-13 2021-01-20 Shire Human Genetic Therapies, Inc. Substituted imidazopyridines as inhibitors of plasma kallikrein and uses thereof
US20210387963A1 (en) 2018-10-10 2021-12-16 Boehringer Ingelheim International Gmbh Phenyltetrazole derivatives as plasma kallikrein inhibitors
US11034669B2 (en) 2018-11-30 2021-06-15 Nuvation Bio Inc. Pyrrole and pyrazole compounds and methods of use thereof
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
WO2021055589A1 (en) 2019-09-18 2021-03-25 Shire Human Genetic Therapies, Inc. Heteroaryl plasma kallikrein inhibitors
CN114728962A (zh) 2019-09-18 2022-07-08 武田药品工业有限公司 血浆激肽释放酶抑制剂及其用途
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
TW202144330A (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
WO2021175290A1 (zh) * 2020-03-04 2021-09-10 南京明德新药研发有限公司 杂环类化合物
JP2023531411A (ja) * 2020-06-16 2023-07-24 メルク・シャープ・アンド・ドーム・エルエルシー 血漿カリクレイン阻害剤
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
JP2024505596A (ja) 2021-02-09 2024-02-06 カルビスタ・ファーマシューティカルズ・リミテッド 遺伝性血管性浮腫の治療
EP4308228A1 (en) 2021-03-17 2024-01-24 Takeda Pharmaceutical Company Limited Plasma kallikrein inhibitors
WO2023002219A1 (en) 2021-07-23 2023-01-26 Kalvista Pharmaceuticals Limited Treatments of hereditary angioedema
CN116003386B (zh) * 2022-11-20 2024-03-26 药康众拓(北京)医药科技有限公司 一种氘代n-苄基吡啶酮吡唑甲酰胺类化合物、药物组合物和用途

Family Cites Families (97)

* 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
US5786328A (en) 1995-06-05 1998-07-28 Genentech, Inc. Use of kunitz type plasma kallikrein inhibitors
US7101878B1 (en) 1998-08-20 2006-09-05 Agouron Pharmaceuticals, Inc. Non-peptide GNRH agents, methods and intermediates for their preparation
IL144910A0 (en) 1999-04-15 2002-06-30 Bristol Myers Squibb Co Cyclic compounds and pharmaceutical compositions containing the same
DE60218511T2 (de) 2001-10-26 2007-10-25 Istituto Di Richerche Di Biologia Molecolare P. Angeletti S.P.A. Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
EP1451160B1 (en) 2001-11-01 2010-01-13 Icagen, Inc. Pyrazole-amides for use in the treatment of pain
GB0205527D0 (en) 2002-03-08 2002-04-24 Ferring Bv Inhibitors
ES2298513T3 (es) 2002-04-26 2008-05-16 Eli Lilly And Company Derivados de tiazol como antagonistas del receptor de taquicinina.
EP1426364A1 (en) 2002-12-04 2004-06-09 Aventis Pharma Deutschland GmbH Imidazole-derivatives as factor Xa inhibitors
DE10301300B4 (de) 2003-01-15 2009-07-16 Curacyte Chemistry Gmbh Verwendung von acylierten 4-Amidino- und 4-Guanidinobenzylaminen zur Inhibierung von Plasmakallikrein
TW200505450A (en) 2003-02-03 2005-02-16 Janssen Pharmaceutica Nv Quinoline-derived amide modulators of vanilloid VR1 receptor
JP4951339B2 (ja) 2003-08-27 2012-06-13 オプソテツク・コーポレイシヨン 眼血管新生疾患の治療のための併用療法
TW200526588A (en) 2003-11-17 2005-08-16 Smithkline Beecham Corp Chemical compounds
GB0403155D0 (en) 2004-02-12 2004-03-17 Vernalis Res Ltd Chemical compounds
EP1568698A1 (en) 2004-02-27 2005-08-31 Aventis Pharma Deutschland GmbH Pyrrole-derivatives as factor Xa inhibitors
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
BRPI0514843A (pt) 2004-09-03 2008-06-24 Yuhan Corp derivados de pirrolo[3,2-c] piridina e processos para a preparação dos mesmos
EP2500031A3 (en) 2005-02-24 2012-12-26 Joslin Diabetes Center, Inc. Compositions and Methods for Treating Vascular Permeability
GB0508472D0 (en) 2005-04-26 2005-06-01 Glaxo Group Ltd Compounds
KR101142363B1 (ko) 2005-06-27 2012-05-21 주식회사유한양행 피롤로피리딘 유도체를 포함하는 항암제 조성물
AU2006270322A1 (en) 2005-07-14 2007-01-25 Takeda San Diego, Inc. Histone deacetylase 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
GB0606876D0 (en) 2006-04-05 2006-05-17 Glaxo Group Ltd Compounds
US20070258976A1 (en) 2006-05-04 2007-11-08 Ward Keith W Combination Therapy for Diseases Involving Angiogenesis
SI2049478T1 (sl) 2006-07-06 2012-08-31 Glaxo Group Ltd Substituirani N-fenilmetil-5-okso-prolin-2-amidi kot antagonisti receptorja P2X7 in postopki za njihovo uporabo
CA2658523C (en) 2006-07-31 2012-06-12 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
DE102006050672A1 (de) 2006-10-24 2008-04-30 Curacyte Discovery Gmbh Hemmstoffe des Plasmins und des Plasmakallikreins
BRPI0721298A2 (pt) 2006-12-29 2014-03-25 Abbott Gmbh & Co Kg Composto de carboxamida e seus usos como inibidores de calpaína
US20100119512A1 (en) 2007-01-25 2010-05-13 Joslin Diabetes Center Methods of diagnosing, treating, and preventing increased vascular permeability
US20080221093A1 (en) 2007-03-07 2008-09-11 Christian Gege Metalloprotease inhibitors containing a heterocyclic moiety
MX2009009443A (es) 2007-03-30 2009-09-14 Sanofi Aventis Compuestos de pirimidina hidrazida como inhibidores de pgds.
JP2010523524A (ja) 2007-04-03 2010-07-15 グラクソ グループ リミテッド P2x7調節因子としてのイミダゾリジンカルボキサミド誘導体
RU2010106393A (ru) 2007-07-26 2011-09-10 Зингента Партисипейшнс Аг (Ch) Новые микробиоциды
JP2010536871A (ja) 2007-08-22 2010-12-02 アラーガン、インコーポレイテッド スフィンゴシン−1−リン酸受容体アゴニストまたはアンタゴニスト生物学的活性を有するピロール化合物
AU2008345225A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009083553A1 (en) 2007-12-31 2009-07-09 Rheoscience A/S Azine compounds as glucokinase activators
US8658685B2 (en) 2008-01-31 2014-02-25 Activesite Pharmaceuticals, Inc. Methods for treatment of kallikrein-related disorders
WO2009106980A2 (en) 2008-02-29 2009-09-03 Pfizer Inc. Indazole derivatives
JP5537442B2 (ja) 2008-03-13 2014-07-02 ブリストル−マイヤーズ スクイブ カンパニー 第xia因子阻害剤としてのピリダジン誘導体
CN102149680B (zh) 2008-07-08 2014-12-10 第一三共株式会社 含氮芳族杂环化合物
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
MX2012006913A (es) 2009-12-18 2012-08-23 Activesite Pharmaceuticals Inc Profarmacos de inhibidores de calicreina plasmatica.
JP2011157349A (ja) 2010-01-07 2011-08-18 Daiichi Sankyo Co Ltd 含窒素芳香族ヘテロシクリル化合物を含有する医薬組成物
ES2569983T3 (es) 2010-01-28 2016-05-13 The Medicines Company (Leipzig) Gmbh Inhibidores de serinproteasa de tipo tripsina y su preparación y uso
JP2013121919A (ja) 2010-03-25 2013-06-20 Astellas Pharma Inc 血漿カリクレイン阻害剤
ES2483802T3 (es) 2010-07-07 2014-08-07 The Medicines Company (Leipzig) Gmbh Inhibidores de serina proteasa
EP2595986A2 (en) 2010-07-14 2013-05-29 Addex Pharma SA Novel 2-amino-4-pyrazolyl-thiazole derivatives and their use as allosteric modulators of metabotropic glutamate receptors
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
WO2012142308A1 (en) 2011-04-13 2012-10-18 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
US9133128B2 (en) 2011-06-17 2015-09-15 Research Triangle Institute Pyrazole derivatives as cannabinoid receptor 1 antagonists
GB2494851A (en) 2011-07-07 2013-03-27 Kalvista Pharmaceuticals Ltd Plasma kallikrein inhibitors
US9249096B2 (en) 2011-09-27 2016-02-02 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
US8952180B2 (en) 2011-09-27 2015-02-10 Bristol-Myers Squibb Company Pyrrolinone carboxamide compounds useful as endothelial lipase inhibitors
EP2807156A1 (en) 2012-01-27 2014-12-03 Novartis AG Aminopyridine derivatives as plasma kallikrein inhibitors
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
AU2013216721B2 (en) 2012-02-10 2017-09-28 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013130603A1 (en) 2012-02-27 2013-09-06 Board Of Regents, The University Of Texas System Ganglioside gd2 as a marker and target on cancer stem cells
GB201212081D0 (en) 2012-07-06 2012-08-22 Kalvista Pharmaceuticals Ltd New polymorph
CN104918942A (zh) 2013-01-08 2015-09-16 萨维拉制药有限公司 嘧啶酮衍生物和它们用于治疗、改善或预防病毒疾病的用途
GB201300304D0 (en) * 2013-01-08 2013-02-20 Kalvista Pharmaceuticals Ltd Benzylamine derivatives
GB2510407A (en) 2013-02-04 2014-08-06 Kalvista Pharmaceuticals Ltd Aqueous suspensions of kallikrein inhibitors for parenteral administration
CA2897336C (en) 2013-01-20 2023-10-17 Dyax Corp. Evaluation and treatment of pkal-mediated disorders
EP2968297B1 (en) 2013-03-15 2018-09-26 Verseon Corporation Multisubstituted aromatic compounds as serine protease inhibitors
AU2014270152B9 (en) 2013-05-23 2018-03-08 Kalvista Pharmaceuticals Limited Heterocyclic derivates
GB2517908A (en) 2013-08-14 2015-03-11 Kalvista Pharmaceuticals Ltd Bicyclic inhibitors
CA2920815C (en) 2013-08-14 2021-09-21 Kalvista Pharmaceuticals Limited Inhibitors of plasma kallikrein
CN106061480B (zh) 2013-12-30 2020-02-28 莱福斯希医药公司 治疗性抑制性化合物
US9611252B2 (en) 2013-12-30 2017-04-04 Lifesci Pharmaceuticals, Inc. Therapeutic inhibitory compounds
LT3828173T (lt) 2014-03-07 2022-11-10 Biocryst Pharmaceuticals, Inc. Pakeistieji pirazolai kaip žmogaus plazmos kalikreino inhibitoriai
WO2015171527A1 (en) 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Pyrazolopyridine pyrazolopyrimidine and related compounds
WO2015171526A2 (en) 2014-05-05 2015-11-12 Global Blood Therapeutics, Inc. Tricyclic pyrazolopyridine compounds
BR112017000816A2 (pt) 2014-07-16 2017-12-05 Lifesci Pharmaceuticals Inc compostos inibitórios terapêuticos
WO2016029214A1 (en) 2014-08-22 2016-02-25 Biocryst Pharmaceuticals, Inc. Compositions and uses of amidine derivatives
JP2017528486A (ja) 2014-09-17 2017-09-28 ヴァーセオン コーポレイション セリンプロテアーゼ阻害剤としてのピラゾリル置換ピリドン化合物
GB201421083D0 (en) * 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421088D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
HUE060104T2 (hu) 2015-02-27 2023-01-28 Verseon Int Corporation Szubsztituált pirazol vegyületek mint szerinproteázinhibitorok
EP3317241A4 (en) 2015-07-01 2019-01-23 Lifesci Pharmaceuticals, Inc. THERAPEUTIC INHIBITOR COMPOUNDS
EP3317259A4 (en) 2015-07-01 2019-06-12 Lifesci Pharmaceuticals, Inc. THERAPEUTIC INHIBITING COMPOUNDS
US10640486B2 (en) 2015-10-27 2020-05-05 Boehringer Ingelheim International Gmbh Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
EP3368529B1 (en) 2015-10-27 2022-04-06 Boehringer Ingelheim International GmbH Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
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
SI3464271T1 (sl) 2016-05-31 2020-10-30 Kalvista Pharmaceuticals Limited Derivati pirazola kot inhibitorji plazemskega kalikreina
GB201609602D0 (en) 2016-06-01 2016-07-13 Nucuna Biomed Ltd Chemical compounds
GB201609601D0 (en) 2016-06-01 2016-07-13 Nucana Biomed Ltd Phosphoramidate compounds
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
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
TW201925188A (zh) 2017-11-29 2019-07-01 英商卡爾維斯塔製藥有限公司 酶抑制劑

Also Published As

Publication number Publication date
AU2021200140B2 (en) 2022-06-02
CO2018012894A2 (es) 2019-04-30
EP3464271A1 (en) 2019-04-10
IL293304A (en) 2022-07-01
HUE049918T2 (hu) 2020-11-30
RS60600B1 (sr) 2020-08-31
AU2021200140A1 (en) 2021-03-18
SI3464271T1 (sl) 2020-10-30
EP3464271B1 (en) 2020-05-13
PL3464271T3 (pl) 2021-01-25
JP6884801B2 (ja) 2021-06-09
RU2018141881A (ru) 2020-07-13
US20220002275A1 (en) 2022-01-06
WO2017207983A1 (en) 2017-12-07
RU2018141881A3 (pt) 2020-07-13
HRP20201131T1 (hr) 2020-10-30
LT3464271T (lt) 2020-09-10
JP2021119196A (ja) 2021-08-12
IL263235A (en) 2018-12-31
ES2805027T3 (es) 2021-02-10
JP7109012B2 (ja) 2022-07-29
EP3760622A1 (en) 2021-01-06
ZA201808639B (en) 2023-01-25
MX2018014188A (es) 2019-08-12
RU2739447C2 (ru) 2020-12-24
CN109311847A (zh) 2019-02-05
DK3464271T3 (da) 2020-06-15
ECSP18094983A (es) 2019-01-31
AU2017275820B2 (en) 2020-10-22
MX2021008342A (es) 2021-08-05
CN109311847B (zh) 2021-07-06
ME03794B (me) 2021-04-20
US20190218205A1 (en) 2019-07-18
PT3464271T (pt) 2020-07-20
KR102424709B1 (ko) 2022-07-22
KR20190033487A (ko) 2019-03-29
JP2019517464A (ja) 2019-06-24
CN113387933A (zh) 2021-09-14
IL263235B (en) 2022-07-01
CL2018003213A1 (es) 2019-04-26
PH12018502355A1 (en) 2019-10-07
CA3025718A1 (en) 2017-12-07
CY1123223T1 (el) 2021-10-29
MD3464271T2 (ro) 2020-08-31
UA123735C2 (uk) 2021-05-26
KR20220107319A (ko) 2022-08-02
AU2017275820A1 (en) 2018-11-29
SG10201913616UA (en) 2020-03-30
RU2020140891A (ru) 2021-02-10
SG11201809922YA (en) 2018-12-28
US11180484B2 (en) 2021-11-23

Similar Documents

Publication Publication Date Title
BR112018074395A2 (pt) derivados de pirazol como inibidores de calicreína plasmática
BR112017010882B8 (pt) Compostos de n-((het)-arilmetil)-heteroaril-carboxamidas como inibidores de calicreína plasmática e seus usos
BR112015028879A2 (pt) derivados heterocíclicos
MX2016001864A (es) Inhibidores de calicreina plasmatica.
BR112015016293A2 (pt) derivados de benzilamina
BR112014000240A2 (pt) derivados de benzilamina como inibidores de calicreína plasmática
BR112016020199A8 (pt) composto inibidor de calicreína plasmática de humano, composição farmacêutica compreendendo o referido composto, kit e seu uso
MX2016001865A (es) Inhibidores biciclicos.
BR112015026297A2 (pt) terapia combinada composta por um inibidor tor quinase e um composto de 5-quinazolinona substituído para o tratamento de câncer
BR112022001341A2 (pt) Inibidores de enzima
BR112017005242A2 (pt) composto, composição farmacêutica, e, composto para uso.
BR112022001025A2 (pt) Inibidores de calicreína plasmática
CO2022000270A2 (es) Inhibidores de enzimas
BR112018076821A2 (pt) derivados de ftalazina como inibidores de parp1, parp2 e/ou tubulina úteis para o tratamento contra câncer
PH12015501492A1 (en) Benzylamine derivatives
BR112016003039B8 (pt) Compostos inibidores de calicreína plasmática, composições farmacêuticas compreendendo os mesmos e seus usos

Legal Events

Date Code Title Description
B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06W Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette]
B350 Update of information on the portal [chapter 15.35 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B11B Dismissal acc. art. 36, par 1 of ipl - no reply within 90 days to fullfil the necessary requirements