UY35975A - Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia - Google Patents

Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia

Info

Publication number
UY35975A
UY35975A UY0001035975A UY35975A UY35975A UY 35975 A UY35975 A UY 35975A UY 0001035975 A UY0001035975 A UY 0001035975A UY 35975 A UY35975 A UY 35975A UY 35975 A UY35975 A UY 35975A
Authority
UY
Uruguay
Prior art keywords
inhibitors
macrociclos
heterocycles
groups
compounds
Prior art date
Application number
UY0001035975A
Other languages
English (en)
Inventor
Delucca Indawati
Kumar Balashanmuga Pabbisetty
Zhu Yeheng
Ruth R Wexler
Donald J Pinto
Michael J Orwat
Yang Wu
James R Corte
William R Ewing
Wang Yufeng
Andrew K Dilger
Fang Tianan
Leon M Smith Ii
Original Assignee
Bristol Myers Squibb Company Una Corporación Del Estado De Delaware
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=52484570&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=UY35975(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Company Una Corporación Del Estado De Delaware filed Critical Bristol Myers Squibb Company Una Corporación Del Estado De Delaware
Publication of UY35975A publication Critical patent/UY35975A/es

Links

Classifications

    • 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
    • C07D471/08—Bridged systems
    • 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
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D403/06—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 only aliphatic carbon atoms
    • 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
    • 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
    • C07D471/12—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 three hetero rings
    • C07D471/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/08—Bridged systems

Abstract

La presente invención proporciona compuestos de la Fórmula (I): o estereoisómeros, tautómeros o sales de aquellos aceptables desde el punto de vista farmacéutico, en donde todas las variables son como se definen en la presente. Estos compuestos son inhibidores selectivos del factor XIa o inhibidores duales de FXIa y calicreína plasmática. La prese nte invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos y a métodos para tratar trastornos tromboembólicos y/o inflamatorios mediante su uso.
UY0001035975A 2014-01-31 2015-01-30 Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia UY35975A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461933942P 2014-01-31 2014-01-31
US201462058293P 2014-10-01 2014-10-01

Publications (1)

Publication Number Publication Date
UY35975A true UY35975A (es) 2015-07-31

Family

ID=52484570

Family Applications (2)

Application Number Title Priority Date Filing Date
UY0001035975A UY35975A (es) 2014-01-31 2015-01-30 Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia
UY0001035971A UY35971A (es) 2014-01-31 2015-01-30 Macrociclos con grupos p2? aromáticos como inhibidores del factor xia

Family Applications After (1)

Application Number Title Priority Date Filing Date
UY0001035971A UY35971A (es) 2014-01-31 2015-01-30 Macrociclos con grupos p2? aromáticos como inhibidores del factor xia

Country Status (31)

Country Link
US (2) US20170002006A1 (es)
EP (4) EP3988549A1 (es)
JP (6) JP6464176B2 (es)
KR (3) KR102413453B1 (es)
CN (4) CN106132962B (es)
AU (4) AU2015210904C1 (es)
BR (1) BR112016015717B1 (es)
CA (1) CA2937739C (es)
CL (1) CL2016001933A1 (es)
CY (1) CY1120702T1 (es)
DK (1) DK3099687T3 (es)
EA (1) EA030222B1 (es)
ES (3) ES2893251T3 (es)
HR (1) HRP20181339T1 (es)
HU (1) HUE040226T2 (es)
IL (4) IL298983B2 (es)
LT (1) LT3099687T (es)
MX (2) MX2016009230A (es)
MY (1) MY190429A (es)
NZ (2) NZ723762A (es)
PE (2) PE20161069A1 (es)
PH (2) PH12016501249B1 (es)
PL (1) PL3099687T3 (es)
PT (1) PT3099687T (es)
RS (1) RS57659B1 (es)
SG (2) SG10201908467RA (es)
SI (1) SI3099687T1 (es)
TW (4) TWI790421B (es)
UY (2) UY35975A (es)
WO (2) WO2015116886A1 (es)
ZA (1) ZA201606011B (es)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB201116559D0 (en) 2011-09-26 2011-11-09 Univ Leuven Kath Novel viral replication inhibitors
LT2766346T (lt) 2011-10-14 2017-06-12 Bristol-Myers Squibb Company Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai
US9738655B2 (en) 2013-03-25 2017-08-22 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors
NZ723762A (en) * 2014-01-31 2023-03-31 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2’ groups as factor xia inhibitors
NO2760821T3 (es) 2014-01-31 2018-03-10
EP2913330A1 (en) 2014-02-27 2015-09-02 Laboratoire Biodim Condensed derivatives of imidazole useful as pharmaceuticals
CN107074821B (zh) 2014-09-04 2020-05-22 百时美施贵宝公司 为fxia抑制剂的二酰胺大环化合物
US9453018B2 (en) 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
MX2017003999A (es) 2014-10-01 2018-02-09 Merck Patent Gmbh Derivados de acido boronico.
NO2721243T3 (es) * 2014-10-01 2018-10-20
JOP20160086B1 (ar) 2015-05-08 2021-08-17 2 Katholieke Univ Leuven Ku Leuven Research And Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors
JO3703B1 (ar) 2015-07-09 2021-01-31 Bayer Pharma AG مشتقات أوكسوبيريدين مستبدلة
US10287288B2 (en) 2015-07-29 2019-05-14 Bristol-Myers Squibb Factor XIa macrocyclic inhibitors bearing alkyl or cycloalkyl P2' moieties
CN114805365A (zh) 2015-07-29 2022-07-29 百时美施贵宝公司 携带非芳族p2,基团的因子xia新大环
JOP20160198B1 (ar) 2015-09-16 2022-03-14 Janssen Pharmaceuticals Inc مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JO3633B1 (ar) 2015-09-16 2020-08-27 Katholieke Univ Leuven Ku Leuven Research & Development مشتقات اندول مستبدلة احاديا او ثنائيا بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
KR20180073602A (ko) * 2015-10-29 2018-07-02 머크 샤프 앤드 돔 코포레이션 인자 XIa 억제제
EP3371162B1 (en) 2015-10-29 2022-01-26 Merck Sharp & Dohme Corp. Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use
JP2019507167A (ja) 2016-03-02 2019-03-14 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ 第ｘｉａ因子阻害活性を有するジアミド大員環
CR20180495A (es) 2016-03-31 2018-12-06 Univ Leuven Kath Deribados de indol sustituidos como inhibidores de replicación viral del dengue
EP3436436B1 (en) 2016-03-31 2022-05-11 Janssen Pharmaceuticals, Inc. Substituted indoline derivatives as dengue viral replication inhibitors
CA3013408A1 (en) 2016-04-01 2017-10-05 Janssen Pharmaceuticals, Inc. Substituted indole compound derivatives as dengue viral replication inhibitors
JOP20170069B1 (ar) 2016-04-01 2021-08-17 1 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
AR109304A1 (es) 2016-08-10 2018-11-21 Sumitomo Chemical Co Compuesto de oxadiazol y su uso
US10143681B2 (en) 2016-08-22 2018-12-04 Merck Sharp & Dohme Corp. Factor XIa inhibitors
CN110062757B (zh) * 2017-01-18 2022-03-04 广东东阳光药业有限公司 凝血因子XIa抑制剂及其用途
JOP20180025B1 (ar) 2017-03-31 2021-08-17 Janssen Pharmaceuticals Inc مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
JOP20180026A1 (ar) 2017-03-31 2019-01-30 Univ Leuven Kath مشتقات اندولين مستبدلة بصفتها مانعات للتكاثر الفيروسي لحمى الفنك
KR102625991B1 (ko) 2017-05-22 2024-01-16 얀센 파마슈티칼즈, 인코포레이티드 뎅기 바이러스 복제 억제제로서의 치환 인돌린 유도체
CN110691773B (zh) 2017-05-22 2023-06-23 杨森制药公司 作为登革热病毒复制抑制剂的经取代的吲哚啉衍生物
WO2019011166A1 (zh) * 2017-07-14 2019-01-17 四川科伦博泰生物医药股份有限公司 大环酰胺化合物及其药物组合物和用途
AU2020272973A1 (en) 2019-04-11 2021-12-02 Bristol-Myers Squibb Company Novel synthetic options towards the manufacture of (6R,10S)-10- {4-[5-chloro-2-(4-chloro-1H-1,2,3-triazol-1-yl)phenyl]-6-oxo-1(6H)- pyrimidinyl}- 1-(difluoromethyl)-6-methyl-1,4,7,8,9,10-hexahydro-11,15 -(metheno)pyrazolo [4,3-b] [1,7] diazacyclotetradecin-5(6H)-one
EP3953355A1 (en) * 2019-04-11 2022-02-16 Bristol-Myers Squibb Company Enhanced performance of amorphous solid and solubilized formulations for achieving therapeutic plasma concentrations
US20220204508A1 (en) * 2019-04-16 2022-06-30 Medshine Discovery Inc. Macrocyclic derivatives acting as xia factor inhibitor
WO2021013209A1 (zh) 2019-07-23 2021-01-28 南京明德新药研发有限公司 作为XIa因子抑制剂的大环衍生物
TWI749881B (zh) * 2019-11-21 2021-12-11 大陸商深圳信立泰藥業股份有限公司 二氧代哌類衍生物、其製備方法及其在醫藥上的應用
CN112608274B (zh) * 2020-12-30 2022-09-06 西南大学 一种手性胺化合物的催化合成方法及其化合物
CN112876461B (zh) * 2021-01-20 2022-12-30 上海零诺生物科技有限公司 尼古丁及其中间体的制备方法
WO2022222960A1 (zh) * 2021-04-21 2022-10-27 上海美悦生物科技发展有限公司 FXIa抑制剂及其药物组合物、制备方法和用途
TW202339720A (zh) * 2022-02-03 2023-10-16 美商Ｄ Ｅ 蕭爾研究有限公司 作為trpa1抑制劑之噠嗪酮化合物
WO2023240140A1 (en) * 2022-06-08 2023-12-14 Blossomhill Therapeutics, Inc. Indazole macrocycles and their use

Family Cites Families (110)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1525186A (fr) 1967-03-29 1968-05-17 Roussel Uclaf Nouvelles pénicillines et procédé de préparation
DE3065190D1 (en) 1979-11-05 1983-11-10 Beecham Group Plc Enzyme derivatives, and their preparation
DE4034829A1 (de) 1990-11-02 1992-05-07 Merck Patent Gmbh Cyclopeptide
JP3190431B2 (ja) 1991-07-01 2001-07-23 三菱化学株式会社 ケトン誘導体
GB9206757D0 (en) 1992-03-27 1992-05-13 Ferring Bv Novel peptide receptor ligands
WO1996034010A2 (en) 1995-03-29 1996-10-31 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5624936A (en) 1995-03-29 1997-04-29 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
US5869682A (en) 1996-04-03 1999-02-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0891352A4 (en) 1996-04-03 2001-08-16 Merck & Co Inc INHIBITORS OF FARNESYL PROTEIN TRANSFERASE
PE121699A1 (es) 1997-02-18 1999-12-08 Boehringer Ingelheim Pharma Heterociclos biciclicos disustituidos como inhibidores de la trombina
ZA985247B (en) 1997-06-19 1999-12-17 Du Pont Merck Pharma Guanidine mimics as factor Xa inhibitors.
TW557297B (en) 1997-09-26 2003-10-11 Abbott Lab Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
NZ528282A (en) 1998-03-19 2005-05-27 Vertex Pharma Interleukin-1 beta converting enzyme inhibitors
ES2310039T3 (es) 1998-05-26 2008-12-16 Warner-Lambert Company Llc Pirimidinas biciclicas y 3,4-dihidropirimidinas biciclicas como inhibidores de la proliferacion celular.
US6307049B1 (en) 1998-09-30 2001-10-23 The Procter & Gamble Co. Heterocyclic 2-substituted ketoamides
CA2358578A1 (en) 1999-01-02 2000-07-13 Aventis Pharma Deutschland Gmbh Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor xa activity)
EP1016663A1 (en) 1999-01-02 2000-07-05 Aventis Pharma Deutschland GmbH Novel malonic acid derivatives, processes for their preparation, their use and pharmaceutical compositions containing them (inhibition of factor Xa activity)
DE50008510D1 (de) 1999-04-09 2004-12-09 Abbott Gmbh & Co Kg Niedermolekulare inhibitoren von komplementproteasen
AU5546000A (en) 1999-06-14 2001-01-02 Protherics Molecular Design Limited Compounds
DE19962924A1 (de) 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
EP1125925A1 (en) 2000-02-15 2001-08-22 Applied Research Systems ARS Holding N.V. Amine derivatives for the treatment of apoptosis
CN1244561C (zh) 2000-05-11 2006-03-08 布里斯托尔-迈尔斯斯奎布公司 可用作生长激素促分泌素的四氢异喹啉类似物
SV2003000617A (es) 2000-08-31 2003-01-13 Lilly Co Eli Inhibidores de la proteasa peptidomimetica ref. x-14912m
AR035216A1 (es) 2000-12-01 2004-05-05 Astrazeneca Ab Derivados de acido mandelico ,derivados farmaceuticamente aceptables, uso de estos derivados para la fabricacion de medicamentos, metodos de tratamiento ,procesos para la preparacion de estos derivados, y compuestos intermediarios
WO2003011222A2 (en) * 2001-07-27 2003-02-13 Merck & Co., Inc. Thrombin inhibitors
US6951840B2 (en) 2001-08-31 2005-10-04 Eli Lilly And Company Lipoglycopeptide antibiotics
AU2002341693B2 (en) 2001-09-21 2008-05-29 Bristol-Myers Squibb Holdings Ireland Unlimited Company Lactam-containing compounds and derivatives thereof as factor Xa inhibitors
US6649606B1 (en) 2001-11-09 2003-11-18 Bristol-Myers Squibb Co. Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
AU2002316317A1 (en) 2002-06-18 2003-12-31 The Scripps Research Institute Synthesis of diazonamide "a" core
US20040180855A1 (en) 2003-02-19 2004-09-16 Schumacher William A. Methods of treating thrombosis with reduced risk of increased bleeding times
US7138412B2 (en) 2003-03-11 2006-11-21 Bristol-Myers Squibb Company Tetrahydroquinoline derivatives useful as serine protease inhibitors
US7129264B2 (en) 2003-04-16 2006-10-31 Bristol-Myers Squibb Company Biarylmethyl indolines and indoles as antithromboembolic agents
US7544699B2 (en) 2003-08-08 2009-06-09 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
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
US7453002B2 (en) 2004-06-15 2008-11-18 Bristol-Myers Squibb Company Five-membered heterocycles useful as serine protease inhibitors
US20100190688A1 (en) 2004-07-12 2010-07-29 Bin Chao Tetrapeptide analogs
CN101137412B (zh) 2005-01-13 2012-11-07 布里斯托尔-迈尔斯·斯奎布公司 用作凝血因子XIa抑制剂的取代的二芳基化合物
WO2006089005A2 (en) 2005-02-17 2006-08-24 Bristol-Myers Squibb Company Combination of selective factor viia and/or xia and plasma kallikrein inhibitors
US20070111947A1 (en) 2005-10-14 2007-05-17 Mcmurry Thomas J Fibrin targeted therapeutics
EP1948639A2 (en) 2005-11-11 2008-07-30 F. Hoffmann-la Roche AG Novel carbocyclic fused cyclic amines
ATE511502T1 (de) 2005-12-14 2011-06-15 Bristol Myers Squibb Co Arylpropionamid-, arylacrylamid-, arylpropinamid- oder arylmethylharnstoffanaloge als faktor-xia- inhibitoren
WO2007070816A2 (en) 2005-12-14 2007-06-21 Bristol-Myers Squibb Company Thiophene derivatives as factor xia inhibitors
EP1966141A1 (en) 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
CN101389613B (zh) * 2005-12-23 2011-10-12 布里斯托尔-迈尔斯.斯奎布公司 用作抗凝血药的大环凝血因子viia抑制剂
PE20071132A1 (es) 2005-12-23 2007-12-14 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
US8410155B2 (en) 2006-12-15 2013-04-02 Bristol-Myers Squibb Company Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor XIA inhibitors
PE20081775A1 (es) 2006-12-20 2008-12-18 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
KR20100037600A (ko) 2007-06-13 2010-04-09 브리스톨-마이어스 스큅 컴퍼니 응고 인자 억제제로서의 디펩티드 유사체
EP2265601B1 (en) 2008-03-13 2012-02-01 Bristol-Myers Squibb Company Pyridazine derivatives as factor xia inhibitors
WO2010151317A1 (en) 2009-06-22 2010-12-29 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
WO2011002520A2 (en) 2009-07-02 2011-01-06 Angion Biomedica Corp. Small molecule inhibitors of parp activity
WO2011017296A1 (en) 2009-08-04 2011-02-10 Schering Corporation 4, 5, 6-trisubstituted pyrimidine derivatives as factor ixa inhibitors
WO2011031658A1 (en) * 2009-09-09 2011-03-17 E. I. Du Pont De Nemours And Company Herbicidal pyrimidone derivatives
AU2011215898B2 (en) 2010-02-11 2016-08-11 Bristol-Myers Squibb Company Macrocycles as Factor XIa inhibitors
US9161924B2 (en) 2011-07-08 2015-10-20 Merck Sharp & Dohme Corp. Factor IXa inhibitors
TW201319068A (zh) * 2011-08-05 2013-05-16 必治妥美雅史谷比公司 作為ｘｉａ因子抑制劑之環狀ｐ１接合劑
TW201311689A (zh) * 2011-08-05 2013-03-16 必治妥美雅史谷比公司 作為因子ｘｉａ抑制劑之新穎巨環化合物
CN103987697B (zh) 2011-10-14 2017-04-26 百时美施贵宝公司 作为因子xia抑制剂的取代的四氢异喹啉化合物
LT2766346T (lt) 2011-10-14 2017-06-12 Bristol-Myers Squibb Company Pakeistieji tetrahidroizochinolino junginiai, kaip faktoriaus xia inhibitoriai
IN2014CN02805A (es) 2011-10-14 2015-07-03 Bristol Myers Squibb Co
WO2013093484A1 (en) * 2011-12-21 2013-06-27 Ono Pharmaceutical Co., Ltd. Pyridinone and pyrimidinone derivatives as factor xia inhibitors
GB2497806A (en) 2011-12-21 2013-06-26 Ono Pharmaceutical Co Pyridinone and pyrimidinone derivatives as factor XIa inhibitors
WO2013111108A1 (en) 2012-01-27 2013-08-01 Novartis Ag 5-membered heteroarylcarboxamide derivatives as plasma kallikrein inhibitors
EP2807156A1 (en) 2012-01-27 2014-12-03 Novartis AG Aminopyridine derivatives as plasma kallikrein inhibitors
JP2015083542A (ja) 2012-02-08 2015-04-30 大日本住友製薬株式会社 ３位置換プロリン誘導体
US9783614B2 (en) 2012-05-10 2017-10-10 Bayer Pharma Aktiengesellschaft Antibodies capable of binding to the coagulation Factor XI and/or its activated form factor Xia and uses thereof
GB201209138D0 (en) 2012-05-24 2012-07-04 Ono Pharmaceutical Co Compounds
CN104640843A (zh) 2012-07-19 2015-05-20 大日本住友制药株式会社 1-(环烷基羰基)脯氨酸衍生物
RS55581B1 (sr) * 2012-08-03 2017-06-30 Bristol Myers Squibb Co Dihidropiridon kao inhibitor faktora xia
LT2880026T (lt) 2012-08-03 2017-04-25 Bristol-Myers Squibb Company Dihidropiridonai p1, kaip faktoriaus xia inhibitoriai
CN104837833B (zh) 2012-10-12 2017-07-14 百时美施贵宝公司 Xia因子抑制剂的晶型
US9315519B2 (en) 2012-10-12 2016-04-19 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor XIa inhibitors
EP2906541B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014120346A1 (en) 2012-12-19 2014-08-07 Merck Sharp & Dohme Corp. Factor ixa inhibitors
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
US9738655B2 (en) 2013-03-25 2017-08-22 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors
TWI633089B (zh) 2013-03-28 2018-08-21 拜耳製藥股份有限公司 經取代的酮基吡啶衍生物
WO2015011087A1 (de) 2013-07-23 2015-01-29 Bayer Pharma Aktiengesellschaft Substituierte oxopyridin-derivate und ihre verwendung als faktor xia / plasma
UY35746A (es) 2013-09-26 2015-04-30 Bayer Pharma AG Derivados de fenilalanina sustituidos
WO2015044170A1 (de) 2013-09-26 2015-04-02 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate und ihre verwendung zur behandlung von thrombotischen / thromboembolischen erkrankungen
WO2015044165A1 (de) 2013-09-26 2015-04-02 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate
EP3049410A1 (de) 2013-09-26 2016-08-03 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate als faktor xia modulatoren
EP3049403A1 (de) 2013-09-26 2016-08-03 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate
AR097755A1 (es) 2013-09-26 2016-04-13 Bayer Pharma AG Derivados sustituidos de fenilalanina como moduladores del factor xia
US20160244437A1 (en) 2013-09-26 2016-08-25 Bayer Pharma Aktiengesellschaft Substituted phenylalanine derivatives
WO2015044169A1 (de) 2013-09-26 2015-04-02 Bayer Pharma Aktiengesellschaft Substituierte phenylalanin-derivate
US20160229839A1 (en) 2013-09-27 2016-08-11 Merck Sharp & Dohme Corp. Factor XIa Inhibitors
EP3054944B1 (en) 2013-10-07 2019-12-04 Merck Sharp & Dohme Corp. Factor xia inhibitors
JP6337750B2 (ja) 2013-11-22 2018-06-06 小野薬品工業株式会社 化合物
WO2015107724A1 (ja) 2014-01-14 2015-07-23 大日本住友製薬株式会社 縮合５－オキサゾリジノン誘導体
NZ723762A (en) 2014-01-31 2023-03-31 Bristol Myers Squibb Co Macrocycles with hetrocyclic p2’ groups as factor xia inhibitors
NO2760821T3 (es) 2014-01-31 2018-03-10
EP4309653A1 (en) 2014-02-07 2024-01-24 Exithera Pharmaceuticals Inc. Therapeutic compounds and compositions
EP3104702B1 (en) 2014-02-11 2022-08-10 Merck Sharp & Dohme LLC Factor xia inhibitors
US9663527B2 (en) 2014-02-11 2017-05-30 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US9944643B2 (en) 2014-02-11 2018-04-17 Merck Sharp & Dohme Corp. Factor XIa inhibitors
EP3138839B1 (en) 2014-02-14 2020-10-28 Sichuan Haisco Pharmaceutical Co., Ltd. Pyridone or pyrimidone derivative, preparation method therefor and application thereof
AU2015226855C1 (en) 2014-03-07 2021-02-11 Biocryst Pharmaceuticals, Inc. Human plasma kallikrein inhibitors
WO2015160636A1 (en) 2014-04-16 2015-10-22 Merck Sharp & Dohme Corp. Factor ixa inhibitors
US9808445B2 (en) 2014-04-16 2017-11-07 Merck Sharp & Dohme Corp. Factor IXa inhibitors
GB201409202D0 (en) * 2014-05-23 2014-07-09 Ffei Ltd Improvements in imaging microscope samples
KR20150136294A (ko) 2014-05-27 2015-12-07 주식회사 레고켐 바이오사이언스 인자 ＸＩａ 억제 활성을 가지는 신규한 화합물
RU2016150410A (ru) 2014-05-28 2018-06-28 Мерк Шарп И Доум Корп. Ингибиторы фактора xia
EP3197891B1 (de) 2014-09-24 2018-11-21 Bayer Pharma Aktiengesellschaft Faktor xia hemmende pyridobenzazepin- und pyridobenzazocin-derivate
NO2721243T3 (es) 2014-10-01 2018-10-20
US9453018B2 (en) * 2014-10-01 2016-09-27 Bristol-Myers Squibb Company Pyrimidinones as factor XIa inhibitors
NZ733574A (en) 2014-12-10 2024-03-22 Ono Pharmaceutical Co Dihydroindolizinone derivative
US10160750B2 (en) 2015-06-19 2018-12-25 Bristol-Myers Squibb Company Diamide macrocycles as factor XIa inhibitors

Also Published As

Publication number Publication date
PH12016501249A1 (en) 2016-08-15
AU2021203968A1 (en) 2021-07-08
JP6464176B2 (ja) 2019-02-06
EA030222B1 (ru) 2018-07-31
AU2015210904A1 (en) 2016-09-15
CN105980384A (zh) 2016-09-28
UY35971A (es) 2015-07-31
EP3392249A1 (en) 2018-10-24
PH12016501249B1 (en) 2016-08-15
NZ723762A (en) 2023-03-31
JP6630004B2 (ja) 2020-01-15
ES2893251T3 (es) 2022-02-08
JP2017504641A (ja) 2017-02-09
CN106132962B (zh) 2018-09-07
SG10201908467RA (en) 2019-10-30
IL272377B2 (en) 2023-05-01
RS57659B1 (sr) 2018-11-30
CN110845498A (zh) 2020-02-28
TW201615639A (zh) 2016-05-01
PH12021550418A1 (en) 2021-11-15
KR102413453B1 (ko) 2022-06-28
ZA201606011B (en) 2018-05-30
SG11201606209PA (en) 2016-08-30
JP7325464B2 (ja) 2023-08-14
ES2687498T3 (es) 2018-10-25
PE20210470A1 (es) 2021-03-08
WO2015116886A1 (en) 2015-08-06
EP3099686A1 (en) 2016-12-07
CN110845498B (zh) 2023-02-17
SI3099687T1 (en) 2018-08-31
CN116987080A (zh) 2023-11-03
AU2015210904C1 (en) 2019-08-29
EP3099687A1 (en) 2016-12-07
EP3099686B1 (en) 2020-03-11
IL246964B (en) 2020-02-27
CA2937739C (en) 2024-04-16
CN105980384B (zh) 2019-11-15
CY1120702T1 (el) 2019-12-11
TW202340188A (zh) 2023-10-16
TW202037595A (zh) 2020-10-16
AU2015210904B2 (en) 2019-05-16
EP3099687B1 (en) 2018-07-04
AU2021203968B2 (en) 2023-03-30
PT3099687T (pt) 2018-10-19
JP6505727B2 (ja) 2019-04-24
JP2019077704A (ja) 2019-05-23
PL3099687T3 (pl) 2018-12-31
HUE040226T2 (hu) 2019-02-28
EP3392249B1 (en) 2021-08-25
IL272377A (en) 2020-03-31
KR20160113267A (ko) 2016-09-28
US9777001B2 (en) 2017-10-03
HRP20181339T1 (hr) 2018-12-28
DK3099687T3 (en) 2018-10-22
MX2020012520A (es) 2021-02-16
LT3099687T (lt) 2018-09-10
ES2784841T3 (es) 2020-10-01
TW201613922A (en) 2016-04-16
AU2019216617A1 (en) 2019-09-05
MX2016009230A (es) 2016-10-03
EA201691471A1 (ru) 2016-12-30
IL298983A (en) 2023-02-01
CL2016001933A1 (es) 2017-03-24
CA2937739A1 (en) 2015-08-06
IL272377B1 (en) 2023-01-01
MY190429A (en) 2022-04-21
KR20220093390A (ko) 2022-07-05
IL307212A (en) 2023-11-01
BR112016015717A2 (pt) 2017-08-08
PE20161069A1 (es) 2016-10-22
JP2023133468A (ja) 2023-09-22
CN106132962A (zh) 2016-11-16
TWI688564B (zh) 2020-03-21
US20170002006A1 (en) 2017-01-05
JP2019094354A (ja) 2019-06-20
JP2017504642A (ja) 2017-02-09
JP6854067B2 (ja) 2021-04-07
BR112016015717B1 (pt) 2023-04-04
TWI790421B (zh) 2023-01-21
AU2023203695A1 (en) 2023-07-06
US20170096429A1 (en) 2017-04-06
IL298983B2 (en) 2024-03-01
IL298983B1 (en) 2023-11-01
WO2015116885A1 (en) 2015-08-06
AU2019216617B2 (en) 2021-03-18
EP3988549A1 (en) 2022-04-27
JP2021088610A (ja) 2021-06-10
KR20240017118A (ko) 2024-02-06
IL246964A0 (en) 2016-09-29
KR102631769B1 (ko) 2024-02-01
BR112016015717A8 (pt) 2018-05-02
NZ761182A (en) 2023-04-28

Similar Documents

Publication Publication Date Title
UY35975A (es) Macrociclos con grupos p2? heterocíclicos como inhibidores del factor xia
CO2017003833A2 (es) Pirimidinonas como inhibidores del factor xia
UY34960A (es) Dihidropiridona p1 como inhibidores del factor xia
UY35972A (es) Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos
UY34959A (es) Dihidropiridona p1 como inhibidores del factor xia
CO2017001152A2 (es) Espirocicloheptanos como inhibidores de la cinasa rho (rock)
ECSP17070706A (es) Inhibidores de bromodominio
CU24605B1 (es) Pirimidin-2-il amino-1h-pirazoles útiles como inhibidores de lrrk2
CL2017001650A1 (es) Derivados de 5-[(piperazina-1-yl)-3-oxo-propilo]-imidazolidina-2,4-dionan como inhibidores adamts para el tratamiento oesteoartritis.
UY36170A (es) Compuestos de dihidroisoquinolinona sustituida
UY34657A (es) ?derivados macrocíclicos para el tratamiento de enfermedades?.
UY35513A (es) Inhibidores de la phd de 6-(5-hidroxi-1hpirazol-1-il)nicotinamida
AR103895A1 (es) Lactamas como inhibidores de rock
CU24263B1 (es) Derivados de imidazopiridazinas inhibidores de quinasa akt, útiles para el tratamiento del cáncer
CO2017000011A2 (es) Derivados de quinolizinona como inhibidores de pi3k
EA201790687A1 (ru) Хинолинкарбоксамиды для применения в лечении множественной миеломы
SV2016005310A (es) Derivados de diheterociclo enlazado a cicloalquilo
DOP2016000326A (es) Compuestos de dihidroisoquinolinona sustituida

Legal Events

Date Code Title Description
110 Patent granted

Effective date: 20230918