PL3421036T3 - Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej - Google Patents

Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej

Info

Publication number
PL3421036T3
PL3421036T3 PL18189634T PL18189634T PL3421036T3 PL 3421036 T3 PL3421036 T3 PL 3421036T3 PL 18189634 T PL18189634 T PL 18189634T PL 18189634 T PL18189634 T PL 18189634T PL 3421036 T3 PL3421036 T3 PL 3421036T3
Authority
PL
Poland
Prior art keywords
aromatic compounds
protease inhibitors
serine protease
multisubstituted aromatic
multisubstituted
Prior art date
Application number
PL18189634T
Other languages
English (en)
Polish (pl)
Inventor
Kevin Michael Short
Son Minh Pham
David Charles Williams
David Ben Kita
Original Assignee
Verseon International Corporation
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 Verseon International Corporation filed Critical Verseon International Corporation
Publication of PL3421036T3 publication Critical patent/PL3421036T3/pl

Links

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)
  • 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)
PL18189634T 2013-03-15 2014-03-17 Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej PL3421036T3 (pl)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201361789358P 2013-03-15 2013-03-15
EP14764515.4A EP2968297B1 (en) 2013-03-15 2014-03-17 Multisubstituted aromatic compounds as serine protease inhibitors
PCT/US2014/030853 WO2014145986A1 (en) 2013-03-15 2014-03-17 Multisubstituted aromatic compounds as serine protease inhibitors
EP18189634.1A EP3421036B8 (en) 2013-03-15 2014-03-17 Multisubstituted aromatic compounds as serine protease inhibitors

Publications (1)

Publication Number Publication Date
PL3421036T3 true PL3421036T3 (pl) 2021-06-14

Family

ID=51538152

Family Applications (2)

Application Number Title Priority Date Filing Date
PL18189634T PL3421036T3 (pl) 2013-03-15 2014-03-17 Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej
PL14764515T PL2968297T3 (pl) 2013-03-15 2014-03-17 Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej

Family Applications After (1)

Application Number Title Priority Date Filing Date
PL14764515T PL2968297T3 (pl) 2013-03-15 2014-03-17 Wielopodstawione związki aromatyczne jako inhibitory protezy serynowej

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) PL3421036T3 (OSRAM)
PT (1) PT2968297T (OSRAM)
RU (2) RU2678830C2 (OSRAM)
SG (2) SG11201506449QA (OSRAM)
SI (1) SI2968297T1 (OSRAM)
TR (1) TR201819092T4 (OSRAM)
WO (1) WO2014145986A1 (OSRAM)
ZA (1) ZA201506295B (OSRAM)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2639876C2 (ru) * 2010-03-30 2017-12-25 Версеон Корпорейшн Мультизамещенные ароматические соединения в качестве ингибиторов тромбина
BR112015022340A2 (pt) * 2013-03-15 2017-07-18 Verseon Corp método para tratamento ou prevenção de uma doença ou distúrbio relacionado à calicreína em um sujeito, composto, e, composição farmacêutica
JP6479749B2 (ja) 2013-03-15 2019-03-06 ヴァーセオン コーポレイション トロンビン阻害剤としてのハロゲノピラゾール
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
MX2017003624A (es) * 2014-09-17 2017-07-13 Verseon Corp Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas.
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
AR103742A1 (es) * 2015-02-25 2017-05-31 Hoffmann La Roche Derivados de trifluorometilpropanamida
LT3261639T (lt) * 2015-02-27 2022-11-25 Verseon International Corporation Pakaitiniai pirazolo junginiai kaip serino proteazės inhibitoriai
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
WO2017083433A1 (en) * 2015-11-09 2017-05-18 Cortexyme, Inc. Inhibitors of arginine gingipain
WO2017152842A1 (en) * 2016-03-10 2017-09-14 National Institute Of Biological Sciences, Beijing Kinase inhibitors
SMT202000382T1 (it) 2016-05-31 2020-09-10 Kalvista Pharmaceuticals Ltd Derivati di pirazolo come inibitori di callicreina plasmatica
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
PL3716952T3 (pl) 2017-11-29 2022-05-02 Kalvista Pharmaceuticals Limited Postacie dawkowania zawierające inhibitor kalikreiny osoczowej
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
SG11202100247WA (en) * 2018-07-13 2021-02-25 Verseon Int 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
KR20220004083A (ko) 2019-04-11 2022-01-11 앤지온 바이오메디카 코포레이션 (e)-3-[2-(2-티에닐)비닐]-1h-피라졸의 고체 형태
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
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
US20250034112A1 (en) * 2021-10-13 2025-01-30 Yale University Improved selective jak2 inhibitors and methods of use

Family Cites Families (119)

* Cited by examiner, † Cited by third party
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
US4160452A (en) 1977-04-07 1979-07-10 Alza Corporation Osmotic system having laminated wall comprising semipermeable lamina and microporous lamina
US4256108A (en) 1977-04-07 1981-03-17 Alza Corporation Microporous-semipermeable laminated osmotic system
US4265874A (en) 1980-04-25 1981-05-05 Alza Corporation Method of delivering drug with aid of effervescent activity generated in environment of use
US4911920A (en) 1986-07-30 1990-03-27 Alcon Laboratories, Inc. Sustained release, comfort formulation for glaucoma therapy
FR2588189B1 (fr) 1985-10-03 1988-12-02 Merck Sharp & Dohme Composition pharmaceutique de type a transition de phase liquide-gel
IL82542A0 (en) 1986-05-23 1987-11-30 Smithkline Beckman Corp Triazole derivatives,their preparation and pharmaceutical compositions containing them
JPH089541B2 (ja) 1988-03-07 1996-01-31 三井東圧化学株式会社 ピラゾール類を主成分とする脳浮腫抑制剤
JP2784925B2 (ja) 1988-09-07 1998-08-13 日本農薬株式会社 ３又は５−フェニルピラゾール類又はその塩及び除草剤
DK0495421T3 (da) 1991-01-15 1996-12-09 Alcon Lab Inc Anvendelse af carragenaner i topiske ophthalmiske sammensætninger
US5212162A (en) 1991-03-27 1993-05-18 Alcon Laboratories, Inc. Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions
JP3810097B2 (ja) 1993-01-15 2006-08-16 明治製菓株式会社 ピロリジン−２−イルカルボニル複素環式化合物誘導体
KR100263817B1 (ko) 1993-11-30 2000-08-16 윌리암스 로저 에이 염증치료용 치환 피라졸일벤젠술폰아미드
US5466823A (en) 1993-11-30 1995-11-14 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides
US6309853B1 (en) 1994-08-17 2001-10-30 The Rockfeller University Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof
ATE262902T1 (de) 1994-11-10 2004-04-15 Millennium Pharm Inc Verwendung von pyrazole verbindungen zur behandlung von glomerulonephritis, krebs, atherosklerose oder restenose
US5733955A (en) 1995-02-10 1998-03-31 The Goodyear Tire & Rubber Company Asphalt cement modification
JP3663522B2 (ja) 1995-08-12 2005-06-22 日本農薬株式会社 植物生育調節用組成物及びその使用方法
US5756529A (en) 1995-09-29 1998-05-26 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides for use in veterinary therapies
US5739083A (en) 1995-10-13 1998-04-14 Otsuka Kagaku Kabushiki Kaisha Pyrazole derivatives and insecticidal compositions containing the derivative as active component
JPH1023173A (ja) 1996-07-02 1998-01-23 Nippon Telegr & Teleph Corp <Ntt> 移動体の遠隔制御システム及び遠隔制御方法
US5792761A (en) 1996-08-12 1998-08-11 Merck & Co., Inc. Thrombin inhibitors
DE19632773A1 (de) * 1996-08-14 1998-02-19 Basf Ag Neue Thrombininhibitoren
GB9622370D0 (en) 1996-10-28 1997-01-08 Merck Sharp & Dohme Therapeutic agents
US5869500A (en) 1996-12-13 1999-02-09 Hoffmann-La Roche Inc. Pyridone compounds useful in treating Alzheimer's disease
IL130286A0 (en) 1996-12-23 2000-06-01 Du Pont Pharm Co Nitrogen containing heteroaromatics as factor Xa inhibitors
CN1250446A (zh) 1997-03-21 2000-04-12 诺瓦提斯公司 作为除草剂的吡唑衍生物
AU5510799A (en) 1998-08-11 2000-03-06 Nihon Bayer Agrochem K.K. Nematicidal pyrazoles
KR20000047461A (ko) 1998-12-29 2000-07-25 성재갑 트롬빈 억제제
SE9900070D0 (sv) 1999-01-13 1999-01-13 Astra Ab New use
AR023510A1 (es) 1999-04-21 2002-09-04 Astrazeneca Ab Un equipo de partes, formulacion farmaceutica y uso de un inhibidor de trombina.
WO2000071536A1 (en) 1999-05-20 2000-11-30 E.I. Du Pont De Nemours And Company Heteroaryloxypyrimidine insecticides and acaricides
JP2003507329A (ja) 1999-08-12 2003-02-25 フアルマシア・イタリア・エツセ・ピー・アー ３（５）−アミノ−ピラゾール誘導体、それらの製造方法および抗腫瘍薬としてのそれらの使用
NZ517828A (en) 1999-09-17 2003-10-31 Millennium Pharm Inc Inhibitors having activity against mammalian factor Xa
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
US6673820B2 (en) 1999-12-02 2004-01-06 Novartis Animal Health Us, Inc. Aminoheterocyclylamides as pesticides and antiparasitic agents
AU2001273040A1 (en) 2000-06-27 2002-01-08 Du Pont Pharmaceuticals Company Factor xa inhibitors
US6884804B2 (en) 2001-05-16 2005-04-26 Vertex Pharmaceuticals Incorporated Inhibitors of Src and other protein kinases
US6589997B2 (en) 2001-06-29 2003-07-08 North Shore-Long Island Jewish Health System Small-molecule modulators of hepatocyte growth factor/scatter factor activities
SI21097A (sl) 2001-12-04 2003-06-30 Univerza V Ljubljani Inhibitorji trombina
WO2003062206A2 (en) 2002-01-23 2003-07-31 Arena Pharmaceuticals, Inc. Small molecule modulators of the 5-ht2a serotonin receptor useful for the prophylaxis and treatment of disorders related thereto
SE0200198D0 (sv) 2002-01-23 2002-01-23 Astrazeneca Ab New use
JP2003313103A (ja) 2002-02-20 2003-11-06 Sankyo Agro Kk ４−アシルアミノピラゾール誘導体を有効成分として含有する農薬
GB0214139D0 (en) 2002-06-19 2002-07-31 Glaxo Group Ltd Chemical compounds
DE10229070A1 (de) 2002-06-28 2004-01-15 Merck Patent Gmbh Phenylderivate 5
NZ538339A (en) 2002-08-09 2007-01-26 Astrazeneca Ab Oxadiazoles as modulators of metabotropic glutamate receptor-5
WO2004035564A1 (en) * 2002-10-17 2004-04-29 Syngenta Participations Ag Pyridine derivatives useful as herbicides
US7192976B2 (en) 2002-12-21 2007-03-20 Angion Biomedica Corporation Small molecule modulators of hepatocyte growth factor (scatter factor) activity
MXPA05006200A (es) * 2002-12-23 2005-08-19 Aventis Pharma Gmbh Derivados de pirazol como inhibidores del factor xa.
US20060229335A1 (en) 2002-12-24 2006-10-12 Bradley Teegarden Diarylamine and arylheteroarylamine pyrazole derivatives as modulators of 5ht2a
US20040147561A1 (en) 2002-12-27 2004-07-29 Wenge Zhong Pyrid-2-one derivatives and methods of use
JP2004231528A (ja) 2003-01-28 2004-08-19 Sankyo Agro Kk アミド誘導体
GB0308318D0 (en) 2003-04-10 2003-05-14 Merck Sharp & Dohme Therapeutic agents
PL1618092T3 (pl) 2003-05-01 2011-02-28 Bristol Myers Squibb Co Związki amidopirazolowe z podstawnikami arylowymi jako inhibitory kinazy
TW200509910A (en) 2003-05-02 2005-03-16 Elan Pharm Inc Substituted pyrazole derivatives and related compounds as bradykinin B1 receptor antagonists
US7223780B2 (en) * 2003-05-19 2007-05-29 Sanofi-Aventis Deutschland Gmbh Triazole-derivatives as blood clotting enzyme factor Xa inhibitors
EP1479679A1 (en) 2003-05-19 2004-11-24 Aventis Pharma Deutschland GmbH Triazole-derivatives as factor Xa inhibitors
JP2007513058A (ja) 2003-09-08 2007-05-24 武田薬品工業株式会社 ジペプチジルぺプチダーゼ阻害剤
JP4895811B2 (ja) 2003-09-11 2012-03-14 ケミア，インコーポレイテッド サイトカイン阻害剤
WO2005030128A2 (en) 2003-09-23 2005-04-07 Merck & Co., Inc. Pyrazole modulators of metabotropic glutamate receptors
TW200526588A (en) 2003-11-17 2005-08-16 Smithkline Beecham Corp Chemical compounds
WO2005066162A1 (en) * 2003-12-23 2005-07-21 Human Biomolecular Research Institute Synthetic compounds and derivatives as modulators of smoking or nicotine ingestion and lung cancer
JP5319113B2 (ja) 2004-03-26 2013-10-16 メチルジーン インコーポレイテッド ヒストンデアセチラーゼの阻害剤
US7235530B2 (en) * 2004-09-27 2007-06-26 Dyax Corporation Kallikrein inhibitors and anti-thrombolytic agents and uses thereof
JP2008526887A (ja) 2005-01-10 2008-07-24 ユニバーシティ オブ コネチカット カンナビノイド受容体に作用する新規なヘテロピロール類似体
EP1867331A4 (en) 2005-04-06 2009-04-08 Takeda Pharmaceutical TRIAZOLE DERIVATIVE AND USE THEREOF
GB0507577D0 (en) 2005-04-14 2005-05-18 Novartis Ag Organic compounds
CN100427481C (zh) 2005-05-26 2008-10-22 沈阳化工研究院 一种芳基醚类化合物及其制备与应用
WO2007067836A2 (en) 2005-12-05 2007-06-14 Boehringer Ingelheim International Gmbh Substituted pyrazole compounds useful as soluble epoxide hydrolase inhibitors
JP2009535388A (ja) 2006-05-03 2009-10-01 アストラゼネカ アクチボラグ ピラゾール誘導体、及びそのｐｉ３ｋ阻害薬としての使用
AU2007257959A1 (en) 2006-06-09 2007-12-21 Kemia, Inc. Therapy using cytokine inhibitors
DE102006032824A1 (de) 2006-07-14 2008-01-17 Bayer Healthcare Ag Substituierte Indazole
BRPI0715492A2 (pt) 2006-07-17 2013-03-19 Boehringer Ingelheim Int uso de inibidores diretos de trombina
CA2658523C (en) 2006-07-31 2012-06-12 Activesite Pharmaceuticals, Inc. Inhibitors of plasma kallikrein
CN101495468A (zh) * 2006-07-31 2009-07-29 艾克提弗赛特制药股份有限公司 血浆激肽释放酶抑制剂
WO2008023235A1 (en) 2006-08-25 2008-02-28 Pfizer Products Inc. Pyrazole derivatives as anti-platelet and anti-thrombotic agents
WO2008062739A1 (en) 2006-11-20 2008-05-29 Japan Tobacco Inc. Pyrazoles and use thereof as drugs
WO2008063888A2 (en) 2006-11-22 2008-05-29 Plexxikon, Inc. Compounds modulating c-fms and/or c-kit activity and uses therefor
US20100144793A1 (en) 2006-11-24 2010-06-10 Ac Immune Sa Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins
JP2010513519A (ja) 2006-12-22 2010-04-30 ミレニアム・ファーマシューティカルズ・インコーポレイテッド キナーゼインヒビター活性を有するある種のピラゾリン誘導体
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
WO2008105383A1 (ja) 2007-02-26 2008-09-04 Toray Industries, Inc. ピラゾール誘導体およびその医薬用途
GB0714129D0 (en) 2007-07-19 2007-08-29 Smithkline Beecham Corp compounds
BRPI0815112A2 (pt) 2007-08-06 2015-08-25 Dainippon Sumitomo Pharma Co Derivado de aminopirazol amida
US8334301B2 (en) 2007-09-28 2012-12-18 Takeda Pharmaceutical Company Limited 5-Membered heterocyclic compound
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009097141A1 (en) 2008-01-31 2009-08-06 Joslin Diabetes Center Methods for treatment of kallikrein-related disorders
WO2009100438A2 (en) 2008-02-07 2009-08-13 Massachusetts Eye & Ear Infirmary Compounds that enhance atoh-1 expression
EP2300004A4 (en) 2008-05-15 2012-05-30 Univ Duke COMPOSITIONS AND METHODS RELATED TO HEAT SHOCK TRANSCRIPTION FACTOR ACTIVATING CONNECTIONS AND OBJECTS THEREFOR
EP2300435A2 (en) * 2008-05-19 2011-03-30 Schering Corporation Heterocyclic compounds as factor ixa inhibitors
CA2767331A1 (en) 2008-07-10 2010-01-14 Angion Biomedica Corp. Methods and compositions of small molecule modulators of hepatocyte growth factor (scatter factor) activity
US8273900B2 (en) 2008-08-07 2012-09-25 Novartis Ag Organic compounds
WO2010017902A1 (de) 2008-08-14 2010-02-18 Bayer Cropscience Aktiengesellschaft Insektizide 4-phenyl-1h-pyrazole
EP2331096A1 (en) 2008-08-19 2011-06-15 Boehringer Ingelheim International GmbH Dabigatran in tumour therapy
EP2328581A1 (en) 2008-08-19 2011-06-08 Boehringer Ingelheim International GmbH Use of dabigatranetexilate for treating patients with pulmonary hypertension
NZ591108A (en) 2008-08-19 2012-11-30 Boehringer Ingelheim Int Dabigatran for percutaneous interventional cardiac catheterisation
AR076753A1 (es) 2009-05-07 2011-07-06 Gruenenthal Chemie Derivados de carboxamida y urea aromaticas sustituidas como ligandos del receptor de vanilloides.
RU2639876C2 (ru) 2010-03-30 2017-12-25 Версеон Корпорейшн Мультизамещенные ароматические соединения в качестве ингибиторов тромбина
CN101851207B (zh) 2010-06-11 2012-01-25 扬州康伊尔医药科技有限公司 抗病毒化合物中间体1-酰基-吡唑-3-羧酸及其制备方法
US8486938B2 (en) 2010-06-24 2013-07-16 Gilead Sciences, Inc. Pyrazolo[1,5-a]pyrimidines for antiviral treatment
EP2604602A4 (en) 2010-08-11 2013-12-18 Taisho Pharmaceutical Co Ltd HETEROARYL PYRAZOLE DERIVATIVE
AP3821A (en) 2010-11-03 2016-09-30 Dow Agrosciences Llc Pesticidal compositions and processes related thereto
WO2012065019A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
EP2688872A4 (en) 2011-03-22 2014-08-27 Merck Sharp & Dohme AMIDOPYRAZOLHEMMER OF INTERLEUKIN RECEPTOR-MEDIATED KINASES
WO2012142308A1 (en) 2011-04-13 2012-10-18 Activesite Pharmaceuticals, Inc. Prodrugs of inhibitors of plasma kallikrein
WO2012154880A1 (en) 2011-05-09 2012-11-15 Proteostasis Therapeutics, Inc. Proteostasis regulators for treating cystic fibrosis and other protein misfolding diseases
CN103917235A (zh) 2011-05-17 2014-07-09 普莱希科公司 激酶调节及其适应症
WO2013039985A2 (en) * 2011-09-12 2013-03-21 The Johns Hopkins University Serine protease inhibitors
WO2013049591A2 (en) 2011-09-29 2013-04-04 Verseon Corporation Dual inhibitor compounds and methods of use thereof
EP2797915B1 (en) 2011-12-27 2016-07-13 Ironwood Pharmaceuticals, Inc. 2-benzyl-3-(oxazole/thiazole)-5-(pyrimidin-2-yl)-1(H)-pyrazole derivatives as stimulators of the soluble guanylate cyclase (sGC) for the treatment of e.g. hypertension or heart failure
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
IN2014MN02512A (OSRAM) 2012-06-14 2015-07-17 Daiichi Sankyo Co Ltd
WO2014111496A1 (en) 2013-01-18 2014-07-24 F. Hoffmann-La Roche Ag 3-substituted pyrazoles and use as dlk inhibitors
JP6479749B2 (ja) 2013-03-15 2019-03-06 ヴァーセオン コーポレイション トロンビン阻害剤としてのハロゲノピラゾール
BR112015022340A2 (pt) * 2013-03-15 2017-07-18 Verseon Corp método para tratamento ou prevenção de uma doença ou distúrbio relacionado à calicreína em um sujeito, composto, e, composição farmacêutica
SMT202400446T1 (it) 2014-02-06 2024-11-15 Nxera Pharma Uk Ltd Composti aza biciclici come agonisti del recettore muscarinico
MX2017003624A (es) * 2014-09-17 2017-07-13 Verseon Corp Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas.

Also Published As

Publication number Publication date
ES2853483T3 (es) 2021-09-16
CA2901637C (en) 2019-09-24
US10251872B2 (en) 2019-04-09
JP2020121999A (ja) 2020-08-13
AU2014232308A1 (en) 2015-09-03
CN110179795A (zh) 2019-08-30
IL240691B (en) 2020-02-27
HRP20182081T1 (hr) 2019-02-08
TR201819092T4 (tr) 2019-01-21
US10058541B2 (en) 2018-08-28
US9687479B2 (en) 2017-06-27
US20170258775A1 (en) 2017-09-14
SG10201707480PA (en) 2017-10-30
EP2968297A1 (en) 2016-01-20
DK2968297T3 (en) 2019-01-07
RU2015144151A3 (OSRAM) 2018-03-28
MX373964B (es) 2020-07-13
US9533970B2 (en) 2017-01-03
CN110101700A (zh) 2019-08-09
RU2019101889A (ru) 2019-03-28
MX2020004183A (es) 2020-08-03
AU2018200736B2 (en) 2019-12-05
MX2015012867A (es) 2016-06-10
CA3051327A1 (en) 2014-09-18
US20190142813A1 (en) 2019-05-16
CN105324117B (zh) 2019-04-09
NZ749214A (en) 2021-04-30
IL240691A0 (en) 2015-10-29
EP2968297B1 (en) 2018-09-26
CN105324117A (zh) 2016-02-10
AU2017225000A1 (en) 2017-10-05
SG11201506449QA (en) 2015-09-29
AU2017258834A1 (en) 2017-11-30
KR20150132148A (ko) 2015-11-25
SI2968297T1 (sl) 2019-02-28
PL2968297T3 (pl) 2019-04-30
AU2018200736A1 (en) 2018-02-22
EP3421036A1 (en) 2019-01-02
US20180064698A1 (en) 2018-03-08
JP6388634B2 (ja) 2018-09-12
US20160024047A1 (en) 2016-01-28
BR112015022340A2 (pt) 2017-07-18
RU2015144151A (ru) 2017-04-24
EP3421036B8 (en) 2020-12-30
HUE042393T2 (hu) 2019-06-28
EP3421036B1 (en) 2020-11-18
EP2968297A4 (en) 2016-11-30
US20170065570A1 (en) 2017-03-09
PT2968297T (pt) 2019-01-10
ES2702182T3 (es) 2019-02-27
AU2017258834B2 (en) 2018-11-08
WO2014145986A1 (en) 2014-09-18
JP6694458B2 (ja) 2020-05-13
AU2020201668A1 (en) 2020-04-02
JP2016513714A (ja) 2016-05-16
CA2901637A1 (en) 2014-09-18
AU2017225000B2 (en) 2017-10-26
RU2678830C2 (ru) 2019-02-04
HK1257685A1 (en) 2019-10-25
NZ711064A (en) 2019-06-28
AU2014232308B2 (en) 2017-11-09
ZA201506295B (en) 2019-01-30
IL272474A (en) 2020-03-31
LT2968297T (lt) 2019-01-10
JP2018118979A (ja) 2018-08-02
HK1214142A1 (en) 2016-07-22
CN110101699A (zh) 2019-08-09
CN108354933A (zh) 2018-08-03

Similar Documents

Publication Publication Date Title
IL272474A (en) Polysubstituted aromatic compounds as serine protease inhibitors
ZA201701799B (en) Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
EP2948450A4 (en) METALLOENZYMINHIBITORVERBINDUNGEN
ZA201508847B (en) Serine/threonine kinase inhibitors
EP3008051A4 (en) Metalloenzyme inhibitor compounds
IL253876A0 (en) Converted pyrazole compounds as serine protease inhibitors
ZA201506156B (en) Novel inhibitors
PL3033332T3 (pl) Bicykliczne inhibitory kalikreiny osoczowej
GB201317609D0 (en) Inhibitor compounds
ZA201604461B (en) Serine/threonine kinase inhibitors
ZA201506440B (en) Halogenopyrazoles as inhibitors of thrombin
GB201321328D0 (en) Inhibitor compounds
GB201305503D0 (en) Inhibitor