JP2017525744A5 - - Google Patents

Download PDF

Info

Publication number: JP2017525744A5
Authority: JP; Japan
Prior art keywords: alkyl; methyl; benzodiazacyclododecin; dioxo; nhco
Prior art date: 2015-09-03
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.): Granted

Application number

JP2017512780A

Other languages

English (en)

Japanese (ja)

Other versions

JP2017525744A (ja

JP6526796B2 (ja

Filing date

2015-09-03

Publication date

2018-10-11

2015-09-03 Application filed filed Critical

2015-09-03 Priority claimed from PCT/US2015/048212 external-priority patent/WO2016036893A1/en

2017-09-07 Publication of JP2017525744A publication Critical patent/JP2017525744A/ja

2018-10-11 Publication of JP2017525744A5 publication Critical patent/JP2017525744A5/ja

2019-06-05 Application granted granted Critical

2019-06-05 Publication of JP6526796B2 publication Critical patent/JP6526796B2/ja

Status Active legal-status Critical Current

2035-09-03 Anticipated expiration legal-status Critical

Links

125000000217 alkyl group Chemical group 0.000 claims 96
229910052739 hydrogen Inorganic materials 0.000 claims 24
229910052799 carbon Inorganic materials 0.000 claims 17
229910052736 halogen Inorganic materials 0.000 claims 14
150000002367 halogens Chemical class 0.000 claims 14
229910052757 nitrogen Chemical group 0.000 claims 13
-1 (±) -methyl Chemical group 0.000 claims 12
125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims 11
125000000623 heterocyclic group Chemical group 0.000 claims 11
150000003839 salts Chemical class 0.000 claims 9
150000001875 compounds Chemical class 0.000 claims 7
125000004432 carbon atom Chemical group C* 0.000 claims 6
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
208000035475 disorder Diseases 0.000 claims 6
125000005842 heteroatom Chemical group 0.000 claims 6
125000002887 hydroxy group Chemical group [H]O* 0.000 claims 6
230000009424 thromboembolic effect Effects 0.000 claims 6
125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 5
125000003545 alkoxy group Chemical group 0.000 claims 5
125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 4
KPPVNWGJXFMGAM-UUILKARUSA-N (e)-2-methyl-1-(6-methyl-3,4-dihydro-2h-quinolin-1-yl)but-2-en-1-one Chemical compound CC1=CC=C2N(C(=O)C(/C)=C/C)CCCC2=C1 KPPVNWGJXFMGAM-UUILKARUSA-N 0.000 claims 4
239000008194 pharmaceutical composition Substances 0.000 claims 4
125000004414 alkyl thio group Chemical group 0.000 claims 3
125000004433 nitrogen atom Chemical group N* 0.000 claims 3
208000007536 Thrombosis Diseases 0.000 claims 2
206010047249 Venous thrombosis Diseases 0.000 claims 2
125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 2
230000002526 effect on cardiovascular system Effects 0.000 claims 2
MTDWONZHWZACQI-FQEVSTJZSA-N methyl N-[(9S)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),13,15-trien-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)CCCCC[C@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 MTDWONZHWZACQI-FQEVSTJZSA-N 0.000 claims 2
229910052760 oxygen Inorganic materials 0.000 claims 2
229910052717 sulfur Inorganic materials 0.000 claims 2
UDJKQCZYNZIIJX-IUINOXSKSA-N (6E,9R)-N-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethyl]-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(16),6,12,14-tetraene-9-carboxamide Chemical compound Clc1ccc(c(CCNC(=O)[C@H]2C\C=C\CCC(=O)Nc3ccccc3C(=O)N2)c1)-n1cnnn1 UDJKQCZYNZIIJX-IUINOXSKSA-N 0.000 claims 1
208000004476 Acute Coronary Syndrome Diseases 0.000 claims 1
206010002388 Angina unstable Diseases 0.000 claims 1
201000001320 Atherosclerosis Diseases 0.000 claims 1
206010003658 Atrial Fibrillation Diseases 0.000 claims 1
QMLDERKCRDMXBF-OWOJBTEDSA-N C(N)(=N)N1CCC(CC1)NC(=O)C1C/C=C/CCC(NC2=C(C(N1)=O)C=CC=C2)=O Chemical compound C(N)(=N)N1CCC(CC1)NC(=O)C1C/C=C/CCC(NC2=C(C(N1)=O)C=CC=C2)=O QMLDERKCRDMXBF-OWOJBTEDSA-N 0.000 claims 1
KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
206010008088 Cerebral artery embolism Diseases 0.000 claims 1
206010008092 Cerebral artery thrombosis Diseases 0.000 claims 1
WMKDDDFZWIMAOE-UHFFFAOYSA-N ClC=1C=CC(=C(C=1)CCNC(=O)C1CCCCCC(NC2=C(C(N1)=O)C=CC=C2)=O)N1N=NN=C1 Chemical compound ClC=1C=CC(=C(C=1)CCNC(=O)C1CCCCCC(NC2=C(C(N1)=O)C=CC=C2)=O)N1N=NN=C1 WMKDDDFZWIMAOE-UHFFFAOYSA-N 0.000 claims 1
206010011091 Coronary artery thrombosis Diseases 0.000 claims 1
206010051055 Deep vein thrombosis Diseases 0.000 claims 1
206010014513 Embolism arterial Diseases 0.000 claims 1
208000032382 Ischaemic stroke Diseases 0.000 claims 1
208000010378 Pulmonary Embolism Diseases 0.000 claims 1
206010037437 Pulmonary thrombosis Diseases 0.000 claims 1
206010063544 Renal embolism Diseases 0.000 claims 1
208000006011 Stroke Diseases 0.000 claims 1
208000007814 Unstable Angina Diseases 0.000 claims 1
125000003118 aryl group Chemical group 0.000 claims 1
125000004429 atom Chemical group 0.000 claims 1
230000015572 biosynthetic process Effects 0.000 claims 1
239000008280 blood Substances 0.000 claims 1
210000004369 blood Anatomy 0.000 claims 1
210000005242 cardiac chamber Anatomy 0.000 claims 1
208000002528 coronary thrombosis Diseases 0.000 claims 1
239000003085 diluting agent Substances 0.000 claims 1
239000003814 drug Substances 0.000 claims 1
239000003937 drug carrier Substances 0.000 claims 1
201000004332 intermediate coronary syndrome Diseases 0.000 claims 1
201000010849 intracranial embolism Diseases 0.000 claims 1
ZWOVUXOCMLKLQV-IIBYNOLFSA-N methyl N-[(4R,9R)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-4-methyl-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),13,15-trien-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)[C@H](C)CCCC[C@@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 ZWOVUXOCMLKLQV-IIBYNOLFSA-N 0.000 claims 1
INAKQOFTONZECB-KKSFZXQISA-N methyl N-[(5S,9S)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-5-methyl-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),13,15-trien-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)C[C@@H](C)CCC[C@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 INAKQOFTONZECB-KKSFZXQISA-N 0.000 claims 1
ZDNIPUHFPCOYDW-ZOXCZHJPSA-N methyl N-[(6E,9R)-9-[2-[5-chloro-2-(tetrazol-1-yl)phenyl]ethylcarbamoyl]-3,11-dioxo-2,10-diazabicyclo[10.4.0]hexadeca-1(12),6,13,15-tetraen-15-yl]carbamate Chemical compound COC(=O)Nc1ccc2c(NC(=O)CC\C=C\C[C@@H](NC2=O)C(=O)NCCc2cc(Cl)ccc2-n2cnnn2)c1 ZDNIPUHFPCOYDW-ZOXCZHJPSA-N 0.000 claims 1
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
239000000203 mixture Substances 0.000 claims 1
208000010125 myocardial infarction Diseases 0.000 claims 1
230000000414 obstructive effect Effects 0.000 claims 1
230000003836 peripheral circulation Effects 0.000 claims 1
230000002093 peripheral effect Effects 0.000 claims 1
125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
230000002265 prevention Effects 0.000 claims 1
238000002560 therapeutic procedure Methods 0.000 claims 1
201000005060 thrombophlebitis Diseases 0.000 claims 1
230000001052 transient effect Effects 0.000 claims 1

JP2017512780A 2014-09-04 2015-09-03 Ｆｘｉａ阻害剤であるジアミドマクロ環 Active JP6526796B2 (ja)

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
US201462045589P	2014-09-04	2014-09-04
US62/045,589		2014-09-04
PCT/US2015/048212 WO2016036893A1 (en)	2014-09-04	2015-09-03	Diamide macrocycles that are fxia inhibitors

Publications (3)

Publication Number	Publication Date
JP2017525744A JP2017525744A (ja)	2017-09-07
JP2017525744A5 true JP2017525744A5 (2)	2018-10-11
JP6526796B2 JP6526796B2 (ja)	2019-06-05

Family

ID=54140704

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2017512780A Active JP6526796B2 (ja)	2014-09-04	2015-09-03	Ｆｘｉａ阻害剤であるジアミドマクロ環

Country Status (6)

Country	Link
US (1)	US10081623B2 (2)
EP (1)	EP3189047B1 (2)
JP (1)	JP6526796B2 (2)
CN (1)	CN107074821B (2)
ES (1)	ES2714283T3 (2)
WO (1)	WO2016036893A1 (2)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
ES2762987T3 (es)	2015-06-19	2020-05-26	Bristol Myers Squibb Co	Macrociclos de diamida como inhibidores del factor XIA
CN114874222B (zh)	2015-07-29	2025-06-06	百时美施贵宝公司	携带非芳族p2,基团的因子xia新大环
JP6629958B2 (ja)	2015-07-29	2020-01-15	ブリストル−マイヤーズスクイブカンパニーＢｒｉｓｔｏｌ−ＭｙｅｒｓＳｑｕｉｂｂＣｏｍｐａｎｙ	アルキルまたはシクロアルキルＰ２’基を担持する大員環の第ＸＩａ因子阻害剤
KR20180117156A (ko)	2016-03-02	2018-10-26	브리스톨-마이어스 스큅 컴퍼니	인자 XIa 억제 활성을 갖는 디아미드 마크로사이클
EP3426674A4 (en)	2016-03-09	2019-08-14	Blade Therapeutics, Inc.	CYCLIC KETO AMID COMPOUNDS AS CALPAIN MODULATORS AND METHOD FOR THE PRODUCTION AND USE THEREOF
AU2017292646A1 (en) *	2016-07-05	2019-02-07	Blade Therapeutics, Inc.	Calpain modulators and therapeutic uses thereof
WO2018039094A1 (en)	2016-08-22	2018-03-01	Merck Sharp & Dohme Corp.	Pyridine-1-oxide derivatives and their use as factor xia inhibitors
WO2018064119A1 (en)	2016-09-28	2018-04-05	Blade Therapeutics, Inc.	Calpain modulators and therapeutic uses thereof
CN112778273B (zh) *	2019-11-11	2022-08-23	江西济民可信集团有限公司	环酮并吡啶酮类化合物及其制备方法和用途
CN113135930B (zh) *	2020-01-17	2023-11-17	上海济煜医药科技有限公司	呋喃并吡啶酮咪唑化合物及其制备方法和用途
CN114085223B (zh) *	2020-08-25	2025-04-04	黄河科技学院	一类大环小分子pcsk9蛋白抑制剂

Family Cites Families (98)

* 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
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
US5624936A (en)	1995-03-29	1997-04-29	Merck & Co., Inc.	Inhibitors of farnesyl-protein transferase
WO1996034010A2 (en)	1995-03-29	1996-10-31	Merck & Co., Inc.	Inhibitors of farnesyl-protein transferase
US5869682A (en)	1996-04-03	1999-02-09	Merck & Co., Inc.	Inhibitors of farnesyl-protein transferase
CA2249617A1 (en)	1996-04-03	1997-10-09	S. Jane Desolms	Inhibitors of farnesyl-protein transferase
TW557297B (en)	1997-09-26	2003-10-11	Abbott Lab	Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
TWI243828B (en)	1998-03-19	2005-11-21	Vertex Pharma	Inhibitors of caspases
TR200003429T2 (tr)	1998-05-26	2001-07-23	Warner-Lambert Company	Hücresel çoğalma inhibitörleri olarak bisiklik pirimidinler ve bisiklik 3,4-dihidropirimidinler.
US6307049B1 (en)	1998-09-30	2001-10-23	The Procter & Gamble Co.	Heterocyclic 2-substituted ketoamides
TR200101903T2 (tr)	1999-01-02	2001-11-21	Aventis Pharma Deutschland Gmbh	Yeni malonik asit türevleri, bunların preparasyon işlemleri.
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)
JP4489976B2 (ja)	1999-04-09	2010-06-23	ビーエーエスエフソシエタス・ヨーロピア	補体プロテアーゼの低分子インヒビター
EP1125925A1 (en)	2000-02-15	2001-08-22	Applied Research Systems ARS Holding N.V.	Amine derivatives for the treatment of apoptosis
ATE310728T1 (de)	2000-05-11	2005-12-15	Bristol Myers Squibb Co	Tetrahydroisochinolin-analoga als wachstumshormon-sekretagoga
SV2003000617A (es)	2000-08-31	2003-01-13	Lilly Co Eli	Inhibidores de la proteasa peptidomimetica ref. x-14912m
AU2002322802A1 (en)	2001-07-27	2003-02-17	Merck And Co., Inc.	Thrombin inhibitors
US6951840B2 (en)	2001-08-31	2005-10-04	Eli Lilly And Company	Lipoglycopeptide antibiotics
WO2003041641A2 (en)	2001-11-09	2003-05-22	Bristol-Myers Squibb Company	Tetrahydroisoquinoline analogs as modulators of chemokine receptor activity
WO2003106438A1 (en)	2002-06-18	2003-12-24	The Scripps Research Institute	Synthesis of diazonamide "a" core
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
CA2573644A1 (en)	2004-07-12	2006-02-16	Idun Pharmaceuticals, Inc.	Tetrapeptide analogs
EP1841504B1 (en)	2005-01-13	2014-11-19	Bristol-Myers Squibb Company	Substituted biaryl compounds as factor xia inhibitors
US20060183771A1 (en)	2005-02-17	2006-08-17	Seiffert Dietmar A	Novel combination of selective factor VIIa and/or factor XIa inhibitors and selective plasma kallikrein inhibitors
WO2007008143A1 (en) *	2005-07-08	2007-01-18	Astrazeneca Ab	Heterocyclic sulfonamide derivatives as inhibitors of factor xa
WO2007047608A2 (en)	2005-10-14	2007-04-26	Epix Pharmaceuticals, Inc.	Fibrin targeted therapeutics
JP4955009B2 (ja)	2005-11-11	2012-06-20	エフ．ホフマン−ラロシュアーゲー	凝固因子Ｘａの阻害剤としての炭素環式縮合環アミン
EP1966141A1 (en)	2005-12-14	2008-09-10	Brystol-Myers Squibb Company	Six-membered heterocycles useful as serine protease inhibitors
WO2007070816A2 (en)	2005-12-14	2007-06-21	Bristol-Myers Squibb Company	Thiophene derivatives as factor xia inhibitors
NZ568595A (en)	2005-12-14	2010-04-30	Bristol Myers Squibb Co	Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor Xla inhibitors
PE20071132A1 (es)	2005-12-23	2007-12-14	Bristol Myers Squibb Co	Compuestos macrociclicos como inhibidores del factor viia
EP2102189B1 (en) *	2006-12-15	2015-07-29	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
CN101784516B (zh)	2007-06-13	2014-07-02	百时美施贵宝公司	作为凝血因子抑制剂的二肽类似物
US8324199B2 (en)	2008-03-13	2012-12-04	Bristol-Myers Squibb Company	Pyridazine derivatives as factor xia inhibitors
US8624040B2 (en)	2009-06-22	2014-01-07	Millennium Pharmaceuticals, Inc.	Substituted hydroxamic acids and uses thereof
US8513433B2 (en)	2009-07-02	2013-08-20	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
NZ602266A (en)	2010-02-11	2014-05-30	Bristol Myers Squibb Co	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
EP2766347B1 (en)	2011-10-14	2016-05-04	Bristol-Myers Squibb Company	Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2013055984A1 (en)	2011-10-14	2013-04-18	Bristol-Myers Squibb Company	Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
JP6033319B2 (ja)	2011-10-14	2016-11-30	ブリストル−マイヤーズスクイブカンパニーＢｒｉｓｔｏｌ−ＭｙｅｒｓＳｑｕｉｂｂＣｏｍｐａｎｙ	第ＸＩａ因子阻害剤としての置換テトラヒドロイソキノリン化合物
US9732085B2 (en)	2011-12-21	2017-08-15	Ono Pharmaceutical Co., Ltd.	Pyridinone and pyrimidinone derivatives as factor Xia
GB2497806A (en)	2011-12-21	2013-06-26	Ono Pharmaceutical Co	Pyridinone and pyrimidinone derivatives as factor XIa inhibitors
US20140378474A1 (en)	2012-01-27	2014-12-25	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
EP2847228B1 (en)	2012-05-10	2018-07-25	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
US9376444B2 (en)	2012-08-03	2016-06-28	Bristol-Myers Squibb Company	Dihydropyridone P1 as factor XIa inhibitors
AU2013296259A1 (en)	2012-08-03	2015-03-19	Bristol-Myers Squibb Company	Dihydropyridone P1 as factor XIa inhibitors
EP2906552B1 (en)	2012-10-12	2017-11-22	Bristol-Myers Squibb Company	Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
TR201807316T4 (tr)	2012-10-12	2018-06-21	Bristol Myers Squibb Co	Bir faktör XIa inhibitörünün kristalli formları.
US9403774B2 (en)	2012-10-12	2016-08-02	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
WO2014160668A1 (en)	2013-03-25	2014-10-02	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
CA2918814C (en)	2013-07-23	2021-10-12	Bayer Pharma Aktiengesellschaft	Substituted oxopyridine derivatives and use thereof as factor xia/plasma
EP3049403A1 (de)	2013-09-26	2016-08-03	Bayer Pharma Aktiengesellschaft	Substituierte phenylalanin-derivate
EP3049410A1 (de)	2013-09-26	2016-08-03	Bayer Pharma Aktiengesellschaft	Substituierte phenylalanin-derivate als faktor xia modulatoren
EP3049406A1 (de)	2013-09-26	2016-08-03	Bayer Pharma Aktiengesellschaft	Substituierte phenylalanin-derivate und ihre verwendung zur behandlung von thrombotischen / thromboembolischen erkrankungen
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
US20160272617A1 (en)	2013-09-26	2016-09-22	Bayer Pharma Aktiengesellschaft	Substituted phenylalanine derivatives
US20160280688A1 (en)	2013-09-26	2016-09-29	Bayer Pharma Aktiengesellschaft	Substituted phenylalanine derivatives
AR097754A1 (es)	2013-09-26	2016-04-13	Bayer Pharma AG	Derivados sustituidos de fenilalanina
EP3049435A4 (en)	2013-09-27	2017-03-29	Merck Sharp & Dohme Corp.	Factor xia inhibitors
WO2015054087A1 (en)	2013-10-07	2015-04-16	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
CA2939326A1 (en)	2014-01-14	2015-07-23	Sumitomo Dainippon Pharma Co., Ltd.	Condensed 5-oxazolidinone derivative
SG10201908467RA (en)	2014-01-31	2019-10-30	Bristol Myers Squibb Co	Macrocycles with hetrocyclic p2' groups as factor xia inhibitors
NO2760821T3 (2)	2014-01-31	2018-03-10
RU2733405C2 (ru)	2014-02-07	2020-10-01	Экзитера Фармасьютикалз Инк.	Терапевтические соединения и композиции
WO2015123093A1 (en)	2014-02-11	2015-08-20	Merck Sharp & Dohme Corp.	Factor xia inhibitors
US9663527B2 (en)	2014-02-11	2017-05-30	Merck Sharp & Dohme Corp.	Factor XIa inhibitors
WO2015123091A1 (en)	2014-02-11	2015-08-20	Merck Sharp & Dohme Corp.	Factor xia inhibitors
CN105829298B (zh)	2014-02-14	2019-02-01	四川海思科制药有限公司	一种吡啶酮或嘧啶酮衍生物、及其制备方法和应用
KR102736869B1 (ko)	2014-03-07	2024-12-02	바이오크리스트파마슈티컬즈,인코포레이티드	인간 혈장 칼리크레인 저해제
US9808445B2 (en)	2014-04-16	2017-11-07	Merck Sharp & Dohme Corp.	Factor IXa inhibitors
WO2015160636A1 (en)	2014-04-16	2015-10-22	Merck Sharp & Dohme Corp.	Factor ixa inhibitors
KR20150136294A (ko)	2014-05-27	2015-12-07	주식회사 레고켐 바이오사이언스	인자 ＸＩａ 억제 활성을 가지는 신규한 화합물
CA2947987A1 (en)	2014-05-28	2015-12-03	Merck Sharp & Dohme Corp.	Factor xia inhibitors
EP3197891B1 (de)	2014-09-24	2018-11-21	Bayer Pharma Aktiengesellschaft	Faktor xia hemmende pyridobenzazepin- und pyridobenzazocin-derivate
NO2721243T3 (2)	2014-10-01	2018-10-20
BR112017012146B1 (pt)	2014-12-10	2023-11-21	Ono Pharmaceutical Co., Ltd	Composto derivado de di-hidroindolizinona, seu uso, composição farmacêutica e inibidor de fxia

2015
- 2015-09-03 ES ES15763756T patent/ES2714283T3/es active Active
- 2015-09-03 US US15/508,122 patent/US10081623B2/en active Active
- 2015-09-03 WO PCT/US2015/048212 patent/WO2016036893A1/en not_active Ceased
- 2015-09-03 JP JP2017512780A patent/JP6526796B2/ja active Active
- 2015-09-03 EP EP15763756.2A patent/EP3189047B1/en active Active
- 2015-09-03 CN CN201580047665.0A patent/CN107074821B/zh active Active

Publication	Publication Date	Title
JP2017525744A5 (2)	2018-10-11
JP2014521701A5 (2)	2015-09-24
JP2019509978A5 (2)	2020-02-20
JP2014532070A5 (2)	2015-12-03
JP2017504642A5 (2)	2018-06-07
JP2020526565A5 (2)	2021-08-19
JP2017504640A5 (2)	2018-03-08
JP2014530240A5 (2)	2015-12-03
JP2011520967A5 (2)	2012-06-07
JP2011509309A5 (2)	2012-02-09
JP2017504641A5 (2)	2018-03-08
RU2005120146A (ru)	2006-05-10	Производные миндальной кислоты
JP2015524443A5 (2)	2016-04-14
JP2018525371A5 (2)	2019-08-15
IL298983A (en)	2023-02-01	Macrocyclines with P2' heterocyclic groups as factor XIA inhibitors
RU2020123151A (ru)	2022-01-20	Антагонисты tlr7/8 и их применение
HRP20170784T1 (hr)	2017-08-11	Supstituirani spojevi tetrahidroizohinolina kao inhbitori xia faktora
JP2019507167A5 (2)	2020-04-02
JP2014514360A5 (2)	2015-05-21
JP2016505042A5 (2)	2017-02-16
JP2013502431A5 (2)	2013-10-03
RU2014129797A (ru)	2016-02-10	Соединения
RU2012116877A (ru)	2013-11-10	Соединения 2-пиридона, применяемые в качестве ингибиторов нейтрофильной эластазы
JP2016531113A5 (2)	2017-09-28
JP2017513932A5 (2)	2018-05-17