AR088423A1 - Ligadores p1 ciclicos como inhibidores del factor xia - Google Patents
Ligadores p1 ciclicos como inhibidores del factor xiaInfo
- Publication number
- AR088423A1 AR088423A1 ARP120102879A ARP120102879A AR088423A1 AR 088423 A1 AR088423 A1 AR 088423A1 AR P120102879 A ARP120102879 A AR P120102879A AR P120102879 A ARP120102879 A AR P120102879A AR 088423 A1 AR088423 A1 AR 088423A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- nr9c
- alkylene
- halogen
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/08—Bridged systems
-
- 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
- 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
- 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
- C07D471/06—Peri-condensed systems
-
- 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
-
- 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
- C07D487/06—Peri-condensed 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-condensed systems
Abstract
Estos compuestos son inhibidores selectivos del factor Xla o inhibidores duales de FXIa y calicreína plasmática. También, composiciones farmacéuticas que comprenden estos compuestos y métodos para tratar trastornos tromboembólicos y/o inflamatorios mediante su uso. Reivindicación 1: Un compuesto de la fórmula (1) o un estereoisómero, un tautómero, una sal aceptable desde el punto de vista farmacéutico, un solvato de este, en donde: G¹ se selecciona del grupo que consiste en un arilo de 6 miembros y un heteroarilo de 5 a 6 miembros, en donde el arilo y el heteroarilo se sustituyen con 1 - 5 R⁸; el anillo A se selecciona del grupo que consiste en un arilo de 6 miembros y un heterociclo de 5 a 6 miembros, en donde el arilo y el heterociclo se sustituyen con 1 - 3 R¹³; X se selecciona del grupo que consiste en alquileno C₄₋₈ y alquenileno C₄₋₈, en donde el alquileno y el alquenileno se sustituyen con R¹, R² y R⁶; de manera alternativa, uno o más de los átomos de carbono del alquileno y alquenileno se pueden reemplazar por O, C=O, S(O)ₚ, NH y N(alquilo C₁₋₄); X² se selecciona del grupo que consiste en CHR¹¹, C=O, O, NH y N(alquilo C₁₋₄); X³ es CR¹² o N; siempre que X³ sea CR¹² cuando X² es O, NH o N(alquilo C₁₋₄); R¹ y R² se seleccionan independientemente del grupo que consiste en H, halógeno, alquilo C₁₋₆, OH, NH₂, -CH₂NH₂, haloalquilo C₁₋₄, -OCH₂F, -OCHF₂, -OCF₃, NH(alquilo C₁₋₄), N(alquilo C₁₋₄)₂, alcoxi C₁₋₄, -CH₂OH y -CH₂O(alquilo C₁₋₄); de manera alternativa, R¹ y R² se toman en forma conjunta con los átomos de carbono a los que están unidos para formar un carbociclo; R³ se selecciona del grupo que consiste en H, haloalquilo, -C(=O)OH, -C(=O)O-alquilo C₁₋₄ y -C(=O)NR⁹R¹⁰; R⁴ se selecciona del grupo que consiste en H y alquilo C₁₋₆; de manera alternativa, R³ y R⁴ son, en forma conjunta, =O; R⁵ se selecciona independientemente del grupo que consiste en H, halógeno, alquilo C₁₋₄, OH, CN, NR⁹R¹⁰, NO₂, alcoxi C₁₋₄, -C(=O)OH, -C(=O)O(alquilo C₁₋₄), -C(=O)NH₂, C(=O)NR⁹(alquilo C₁₋₄), -C(=O)NR⁹-alquilen C₁₋₄-O(alquilo C₁₋₄), -NR⁹C(=O)alquilo C₁₋₄, -NR⁹C(=O)O-alquilo C₁₋₄, -NR⁹C(=O)alquilen C₁₋₄-O(alquilo C₁₋₄), -NR⁹C(=O)O-alquilen C₁₋₄-O(alquilo C₁₋₄), -NR⁹C(=O)NH(alquilo C₁₋₄), R¹⁵, -C(=O)OR¹⁵, -C(=O)NR⁹R¹⁵, -NR⁹R¹⁵, -NR⁹C(=O)R¹⁵ y -NR⁹C(=O)OR¹⁵; R⁵ᵃ se selecciona del grupo que consiste en H, halógeno y metilo; R⁶ se selecciona del grupo que consiste en H, alquilo C₁₋₆ y OH; R⁷ se selecciona del grupo que consiste en H, ²H, F, =O, OH y alquilo C₁₋₄; R⁸ se selecciona del grupo que consiste en H, halógeno, OH, CN, alquilo C₁₋₆, haloalquilo, alcoxi, haloalcoxi y -C(=O)alquilo C₁₋₃; R⁹ se selecciona del grupo que consiste en H y alquilo C₁₋₆; R¹⁰ se selecciona del grupo que consiste en H y alquilo C₁₋₆; de manera alternativa, R⁹ y R¹⁰ se toman en forma conjunta con el átomo de nitrógeno al que están unidos para formar un heterociclo de 4- a 7- miembros sustituido con R¹⁴; R¹¹ se selecciona del grupo que consiste en H y alquilo C₁₋₆; R¹² se selecciona del grupo que consiste en H, ²H y alquilo C₁₋₆; R¹³ se selecciona del grupo que consiste en H, OH, halógeno, CN, alquilo C₁₋₆, alcoxi, haloalquilo, haloalcoxi y cicloalquilo C₃₋₆; R¹⁴ se selecciona del grupo que consiste en H, OH, halógeno y alquilo C₁₋₆; R¹⁵ se selecciona del grupo que consiste en: -(CH₂)ₙ-carbociclo C₃₋₁₀ y -(CH₂)ₙ-heterociclo de 4 - 10 miembros, en donde el carbociclo y heterocíclico se sustituyen opcionalmente con alquilo C₁₋₆, cicloalquilo C₃₋₆, -(CH₂)ₙ-C(=O)O-alquilo C₁₋₄, -(CH₂)ₙ-O-alquilo C₁₋₄ y =O; n, en cada caso, se selecciona de 0, 1, 2, 3 y 4; y; p, en cada caso, se selecciona de 0, 1 y 2.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161515404P | 2011-08-05 | 2011-08-05 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR088423A1 true AR088423A1 (es) | 2014-06-11 |
Family
ID=46964007
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP120102879A AR088423A1 (es) | 2011-08-05 | 2012-08-07 | Ligadores p1 ciclicos como inhibidores del factor xia |
Country Status (8)
Country | Link |
---|---|
US (2) | US8901115B2 (es) |
EP (2) | EP3070087B1 (es) |
JP (1) | JP6113727B2 (es) |
CN (2) | CN105294701B (es) |
AR (1) | AR088423A1 (es) |
ES (2) | ES2563445T3 (es) |
TW (1) | TW201319068A (es) |
WO (1) | WO2013022814A1 (es) |
Families Citing this family (38)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EA020528B1 (ru) | 2010-02-11 | 2014-11-28 | Бристол-Майерс Сквибб Компани | Макроциклы в качестве ингибиторов фактора xia |
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 |
ES2699226T3 (es) | 2011-10-14 | 2019-02-08 | Bristol Myers Squibb Co | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
RS56168B1 (sr) | 2011-10-14 | 2017-11-30 | Bristol Myers Squibb Co | Supstituisana jedinjenja tetrahidroizohinolina kao inhibitori xia faktora |
EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
HUE032622T2 (en) * | 2012-08-03 | 2017-10-30 | Bristol Myers Squibb Co | Dihydropyridone P1 as factor XIA inhibitors |
DK2882734T3 (en) * | 2012-08-03 | 2017-01-30 | Bristol Myers Squibb Co | DIHYDROPYRIDON AS FACTOR-XIA INHIBITORS |
LT2906551T (lt) | 2012-10-12 | 2018-04-25 | Bristol-Myers Squibb Company | Faktoriaus xia kristalinės formos |
US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
ES2712699T3 (es) | 2013-03-25 | 2019-05-14 | Bristol Myers Squibb Co | Tetrahidroisoquinolinas que contienen azoles sustituidos como inhibidores del factor XIa |
US9809545B2 (en) | 2013-03-27 | 2017-11-07 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
NO2760821T3 (es) * | 2014-01-31 | 2018-03-10 | ||
EP3392249B1 (en) * | 2014-01-31 | 2021-08-25 | Bristol-Myers Squibb Company | Macrocycles with heterocyclic p2' groups as 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 |
WO2015123093A1 (en) | 2014-02-11 | 2015-08-20 | Merck Sharp & Dohme Corp. | Factor xia inhibitors |
US10093683B2 (en) | 2014-04-22 | 2018-10-09 | Merck Sharp & Dohme Corp. | Factor XIa inhibitors |
EP3180317B1 (en) | 2014-07-28 | 2021-04-14 | Merck Sharp & Dohme Corp. | FACTOR XIa INHIBITORS |
EP3189047B1 (en) | 2014-09-04 | 2018-12-26 | Bristol-Myers Squibb Company | Diamide macrocycles that are fxia inhibitors |
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 |
WO2016093285A1 (ja) * | 2014-12-10 | 2016-06-16 | 小野薬品工業株式会社 | ジヒドロインドリジノン誘導体 |
WO2016205482A1 (en) * | 2015-06-19 | 2016-12-22 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
WO2017019819A1 (en) | 2015-07-29 | 2017-02-02 | Bristol-Myers Squibb Company | Factor xia macrocyclic inhibitors bearing alkyl or cycloalkyl p2' moieties |
ES2871111T3 (es) | 2015-07-29 | 2021-10-28 | Bristol Myers Squibb Co | Inhibidores macrocíclicos del factor XIa que contienen un grupo P2' no aromático |
WO2017074833A1 (en) | 2015-10-29 | 2017-05-04 | Merck Sharp & Dohme Corp. | Macrocyclic spirocarbamate derivatives as factor xia inhibitors, pharmaceutically acceptable compositions and their use |
AU2016344476B2 (en) * | 2015-10-29 | 2020-08-13 | Merck Sharp & Dohme Llc | Factor XIa inhibitors |
KR20180117156A (ko) | 2016-03-02 | 2018-10-26 | 브리스톨-마이어스 스큅 컴퍼니 | 인자 XIa 억제 활성을 갖는 디아미드 마크로사이클 |
EP3500556B1 (en) | 2016-08-22 | 2023-08-02 | Merck Sharp & Dohme LLC | Pyridine-1-oxide derivatives and their use as factor xia inhibitors |
EP3301094A1 (en) * | 2016-09-30 | 2018-04-04 | Mutabilis | Heterocyclic compounds and their use in preventing or treating bacterial infections |
WO2018133793A1 (zh) * | 2017-01-18 | 2018-07-26 | 广东东阳光药业有限公司 | 凝血因子XIa抑制剂及其用途 |
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 |
ES2942214T3 (es) * | 2018-04-17 | 2023-05-30 | Univ Michigan Regents | Inhibidores de la función plaquetaria y procedimientos de utilización de los mismos |
CA3136861A1 (en) | 2019-04-16 | 2020-10-22 | Medshine Discovery Inc. | Macrocyclic derivatives acting as xia factor inhibitor |
US20220281868A1 (en) * | 2019-07-23 | 2022-09-08 | Medshine Discovery Inc. | Macrocyclic derivatives as factor xia inhibitors |
CN115490708A (zh) * | 2021-06-18 | 2022-12-20 | 苏州亚盛药业有限公司 | 磺酰胺类大环衍生物及其制备方法和用途 |
Family Cites Families (37)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0028489B1 (en) | 1979-11-05 | 1983-10-05 | Beecham Group Plc | Enzyme derivatives, and their preparation |
JPH0987280A (ja) * | 1995-09-28 | 1997-03-31 | Yamanouchi Pharmaceut Co Ltd | オキソピペラジン誘導体又はその塩 |
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. |
CA2383008A1 (en) | 1999-06-14 | 2000-12-21 | Amanda Jane Lyons | Compounds |
DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
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 |
AU2002322802A1 (en) * | 2001-07-27 | 2003-02-17 | Merck And Co., Inc. | Thrombin inhibitors |
PL204263B1 (pl) | 2001-09-21 | 2009-12-31 | Bristol Myers Squibb Co | Pochodna 1H-pirazolo[3,4-c]pirydyny i jej zastosowanie oraz kompozycja farmaceutyczna i jej zastosowanie |
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 |
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 |
JP5236293B2 (ja) | 2005-01-13 | 2013-07-17 | ブリストル−マイヤーズ スクイブ カンパニー | Xia因子阻害剤としての置換ビアリール化合物 |
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 |
NZ568595A (en) | 2005-12-14 | 2010-04-30 | Bristol Myers Squibb Co | Arylpropionamide, arylacrylamide, arylpropynamide, or arylmethylurea analogs as factor Xla inhibitors |
CN101341124A (zh) | 2005-12-14 | 2009-01-07 | 布里斯托尔-迈尔斯斯奎布公司 | 可用作丝氨酸蛋白酶抑制剂的6元杂环 |
US8466295B2 (en) | 2005-12-14 | 2013-06-18 | Bristol-Myers Squibb Company | Thiophene derivatives as factor XIa inhibitors |
TW200745062A (en) * | 2005-12-23 | 2007-12-16 | Bristol Myers Squibb Co | Macrocyclic factor VIIA inhibitors useful as anticoagulants |
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 |
JP5342450B2 (ja) | 2006-12-15 | 2013-11-13 | ブリストル−マイヤーズ スクイブ カンパニー | 第XIa因子インヒビターとしてのアリールプロピオンアミド、アリールアクリルアミド、アリールプロピンアミド、またはアリールメチルウレアアナログ |
EP2152664B1 (en) | 2007-06-13 | 2014-09-03 | Bristol-Myers Squibb Company | Dipeptide analogs as coagulation factor inhibitors |
EP2070899A1 (en) | 2007-12-14 | 2009-06-17 | F. Hoffmann-La Roche Ag | Deprotection of N-BOC compounds |
ES2380648T3 (es) * | 2008-03-13 | 2012-05-17 | Bristol-Myers Squibb Company | Derivados de piridazina como inhibidores del factor XIA |
EA020528B1 (ru) | 2010-02-11 | 2014-11-28 | Бристол-Майерс Сквибб Компани | Макроциклы в качестве ингибиторов фактора xia |
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 |
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 |
EP2766347B1 (en) | 2011-10-14 | 2016-05-04 | Bristol-Myers Squibb Company | Substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
RS56168B1 (sr) | 2011-10-14 | 2017-11-30 | Bristol Myers Squibb Co | Supstituisana jedinjenja tetrahidroizohinolina kao inhibitori xia faktora |
ES2699226T3 (es) | 2011-10-14 | 2019-02-08 | Bristol Myers Squibb Co | Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa |
HUE032622T2 (en) | 2012-08-03 | 2017-10-30 | Bristol Myers Squibb Co | Dihydropyridone P1 as factor XIA inhibitors |
DK2882734T3 (en) | 2012-08-03 | 2017-01-30 | Bristol Myers Squibb Co | DIHYDROPYRIDON AS FACTOR-XIA INHIBITORS |
US9403774B2 (en) | 2012-10-12 | 2016-08-02 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
LT2906551T (lt) | 2012-10-12 | 2018-04-25 | Bristol-Myers Squibb Company | Faktoriaus xia kristalinės formos |
WO2014059202A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
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2012
- 2012-08-03 TW TW101128158A patent/TW201319068A/zh unknown
- 2012-08-06 ES ES12766737.6T patent/ES2563445T3/es active Active
- 2012-08-06 CN CN201510648908.8A patent/CN105294701B/zh active Active
- 2012-08-06 EP EP16151754.5A patent/EP3070087B1/en active Active
- 2012-08-06 WO PCT/US2012/049698 patent/WO2013022814A1/en active Application Filing
- 2012-08-06 CN CN201280037801.4A patent/CN103702999B/zh active Active
- 2012-08-06 ES ES16151754T patent/ES2733096T3/es active Active
- 2012-08-06 US US14/236,968 patent/US8901115B2/en active Active
- 2012-08-06 JP JP2014524151A patent/JP6113727B2/ja active Active
- 2012-08-06 EP EP12766737.6A patent/EP2739625B1/en active Active
- 2012-08-07 AR ARP120102879A patent/AR088423A1/es unknown
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JP2014521700A (ja) | 2014-08-28 |
CN103702999B (zh) | 2015-11-25 |
CN105294701B (zh) | 2017-10-24 |
US9108981B2 (en) | 2015-08-18 |
ES2563445T3 (es) | 2016-03-15 |
EP2739625A1 (en) | 2014-06-11 |
US20150057262A1 (en) | 2015-02-26 |
EP3070087A1 (en) | 2016-09-21 |
ES2733096T3 (es) | 2019-11-27 |
EP2739625B1 (en) | 2016-01-20 |
CN105294701A (zh) | 2016-02-03 |
TW201319068A (zh) | 2013-05-16 |
US20140163002A1 (en) | 2014-06-12 |
EP3070087B1 (en) | 2019-04-10 |
US8901115B2 (en) | 2014-12-02 |
WO2013022814A1 (en) | 2013-02-14 |
CN103702999A (zh) | 2014-04-02 |
JP6113727B2 (ja) | 2017-04-12 |
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