[go: up one dir, main page]

PE20121806A1 - Macrociclos como inhibidores del factor de coagulacion (fxia) - Google Patents

Macrociclos como inhibidores del factor de coagulacion (fxia)

Info

Publication number
PE20121806A1
PE20121806A1 PE2012001189A PE2012001189A PE20121806A1 PE 20121806 A1 PE20121806 A1 PE 20121806A1 PE 2012001189 A PE2012001189 A PE 2012001189A PE 2012001189 A PE2012001189 A PE 2012001189A PE 20121806 A1 PE20121806 A1 PE 20121806A1
Authority
PE
Peru
Prior art keywords
alkyl
halogen
members
inhibitors
macrocicles
Prior art date
Application number
PE2012001189A
Other languages
English (en)
Inventor
James R Corte
Tianan Fang
Carl P Decicco
Donald J P Pinto
Karen A Rossi
Zilun Hu
Yoon Jeon
Mimi L Quan
Joanne M Smalllheer
Yufeng Wang
Wu Yang
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20121806A1 publication Critical patent/PE20121806A1/es

Links

Classifications

    • 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
    • C07D487/04—Ortho-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
    • 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D225/00—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom
    • C07D225/04—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D225/08—Heterocyclic compounds containing rings of more than seven members having one nitrogen atom as the only ring hetero atom condensed with carbocyclic rings or ring systems condensed with two six-membered 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
    • C07D471/14—Ortho-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
    • C07D471/12—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
    • C07D487/06—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
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-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
    • C07D487/12—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 three hetero rings
    • C07D487/16—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
    • C07D487/12—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 three hetero rings
    • C07D487/18—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
    • C07D498/04—Ortho-condensed 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

REFERIDA A UN COMPUESTO DE FORMULA I, DONDE A ES UN CARBOCICLO C3-C10, CARBOCILO C5-C10; B ES BENCENO, HETEROARILO DE 5-6 MIEMBROS; C ES BENCENO, HETEROCICLO DE 5-10 MIEMBROS; L1 ES ENLACE, -CH2O--OCH2, -CN2NH-, ENTRE OTROS; L ES ALQUILENO C3-C8, ALQUINILENO C4-C8 SUSTITUIDO O NO, ENTRE OTROS; Y ES CH2, CH(ALQUILO C1-C4), C(ALQUILO C1-C4)2, CO, O, S, ENTRE OTROS; R1 ES HALOGENO,ALQUILO C1-C6, ALCOXI C1-C4, ALQUILTIO C1-C4, OH, ENTRE OTROS; R2 ES HETEROCICLO DE 5-7 MIEMBROS CON 1-4 HETEROATOMOS, ENTRE OTROS; R3 ES H, HALOGENO, OH, NH2, CN, ENTRE OTROS; R4 ES H, ALQUILO C1-C4; R6 ES HALOGENO, ALQUILO C1-C4, OH, CF3, CO2H, ENTRE OTROS. UN COMPUESTO PREFERIDO ES: ESTER TERC-BUTILICO DEL ACIDO {(S)-14-[(E)-3-(5-CLORO-2-TETRAZOL-1-IL-FENIL)-ACRILOILAMINO]-17-FLUORO-9-OXO-8,16,18-TRIAZA-TRICICLO[13.2.1.0]OCTADECA-1(17),2,4,6,15(18)-PENTAEN-5-IL}-CARBAMICO. DICHOS COMPUESTOS SON INHIBIDORES SELECTIVOS DEL FACTOR XIa UTILES EN EL TRATAMIENTO DE TRASTORNOS TROMBOEMBOLICOS Y/O INFLAMATORIOS
PE2012001189A 2010-02-11 2011-02-10 Macrociclos como inhibidores del factor de coagulacion (fxia) PE20121806A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US30342310P 2010-02-11 2010-02-11
US40533810P 2010-10-21 2010-10-21

Publications (1)

Publication Number Publication Date
PE20121806A1 true PE20121806A1 (es) 2013-01-02

Family

ID=43858008

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2016000777A PE20160841A1 (es) 2010-02-11 2011-02-10 Macrociclos como inhibidores del factor de coagulacion (fxia)
PE2012001189A PE20121806A1 (es) 2010-02-11 2011-02-10 Macrociclos como inhibidores del factor de coagulacion (fxia)

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PE2016000777A PE20160841A1 (es) 2010-02-11 2011-02-10 Macrociclos como inhibidores del factor de coagulacion (fxia)

Country Status (23)

Country Link
US (9) US8828983B2 (es)
EP (3) EP2534154B1 (es)
JP (3) JP5844287B2 (es)
KR (2) KR101901545B1 (es)
CN (3) CN107973809B (es)
AR (1) AR080167A1 (es)
AU (1) AU2011215898B2 (es)
BR (1) BR112012019925B1 (es)
CA (1) CA2789622C (es)
CL (1) CL2012002229A1 (es)
CO (1) CO6551666A2 (es)
EA (1) EA020528B1 (es)
ES (2) ES2674745T3 (es)
IL (1) IL221343B (es)
MX (1) MX2012008874A (es)
MY (1) MY162936A (es)
NZ (1) NZ602266A (es)
PE (2) PE20160841A1 (es)
PH (1) PH12012501589A1 (es)
SG (1) SG183153A1 (es)
TW (2) TWI577665B (es)
WO (2) WO2011100401A1 (es)
ZA (1) ZA201206758B (es)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2011215898B2 (en) * 2010-02-11 2016-08-11 Bristol-Myers Squibb Company Macrocycles as Factor XIa inhibitors
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
ES2572908T3 (es) 2011-10-14 2016-06-03 Bristol-Myers Squibb Company Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa
EP2766347B1 (en) 2011-10-14 2016-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
ES2625256T3 (es) 2011-10-14 2017-07-19 Bristol-Myers Squibb Company Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIA
AU2013296259A1 (en) * 2012-08-03 2015-03-19 Bristol-Myers Squibb Company Dihydropyridone P1 as factor XIa inhibitors
PT2882734T (pt) 2012-08-03 2016-12-09 Bristol Myers Squibb Co Di-hidropiridona pi como inibidores do fator xia
PE20150639A1 (es) 2012-10-12 2015-05-11 Bristol Myers Squibb Co Formas cristalinas de inhibidor del factor xia
EP2906552B1 (en) 2012-10-12 2017-11-22 Bristol-Myers Squibb Company Guanidine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
WO2014059214A1 (en) 2012-10-12 2014-04-17 Bristol-Myers Squibb Company Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors
US9738655B2 (en) 2013-03-25 2017-08-22 Bristol-Myers Squibb Company Tetrahydroisoquinolines containing substituted azoles as factor XIa inhibitors
CA2911259A1 (en) * 2013-05-06 2014-11-13 Merck Patent Gmbh Macrocycles as kinase inhibitors
WO2015054087A1 (en) * 2013-10-07 2015-04-16 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
RU2720237C2 (ru) 2013-11-18 2020-04-28 Форма Терапеутикс, Инк. Композиции, содержащие бензопиперазин, в качестве ингибиторов бромодоменов вет
HRP20210431T1 (hr) 2013-11-18 2021-05-14 Forma Therapeutics, Inc. Pripravci tetrahidrokinolina kao inhibitori bet bromodomene
PE20210470A1 (es) * 2014-01-31 2021-03-08 Bristol Myers Squibb Co Macrociclos con grupos p2' heterociclicos como inhibidores del factor xia
NO2760821T3 (es) * 2014-01-31 2018-03-10
RU2020131276A (ru) 2014-02-07 2020-11-03 Экзитера Фармасьютикалз Инк. Терапевтические соединения и композиции
US9944643B2 (en) 2014-02-11 2018-04-17 Merck Sharp & Dohme Corp. Factor XIa inhibitors
US9676723B2 (en) 2014-02-11 2017-06-13 Merck Sharp & Dohme Corp Factor XIa inhibitors
US10093683B2 (en) 2014-04-22 2018-10-09 Merck Sharp & Dohme Corp. Factor XIa inhibitors
WO2016015593A1 (en) 2014-07-28 2016-02-04 Merck Sharp & Dohme Corp. FACTOR XIa INHIBITORS
US10081623B2 (en) 2014-09-04 2018-09-25 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
CN107106548A (zh) * 2015-01-20 2017-08-29 默沙东公司 因子XIa抑制剂
TWI535452B (zh) * 2015-01-23 2016-06-01 長庚醫療財團法人 使用抗－ｃｄ４４中和抗體來治療和／或預防心房顫動
EP3310777B1 (en) 2015-06-19 2019-10-09 Bristol-Myers Squibb Company Diamide macrocycles as factor xia inhibitors
ES2803659T3 (es) * 2015-07-29 2021-01-28 Bristol Myers Squibb Co Inhibidores macrocíclicos del factor xia que contienen restos alquilo o cicloalquilo p2’
EP3868753B1 (en) * 2015-07-29 2022-12-21 Bristol-Myers Squibb Company Factor xia macrocyclic inhibitors bearing a non-aromatic p2' group
CN105085492A (zh) * 2015-09-29 2015-11-25 青岛友诚高新技术有限公司 一种可用于制备治疗冠状动脉粥样硬化药物的化合物及其制备方法、用途
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
EP3368036B1 (en) 2015-10-29 2022-07-20 Merck Sharp & Dohme LLC Macrocyclic pyridine-n-oxide derivatives as factor xia inhibitors
EP3423458A1 (en) * 2016-03-02 2019-01-09 Bristol-Myers Squibb Company Diamide macrocycles having factor xia inhibiting activity
AU2017242027B2 (en) * 2016-04-01 2020-10-08 Recurium Ip Holdings, Llc Estrogen receptor modulators
WO2018039094A1 (en) 2016-08-22 2018-03-01 Merck Sharp & Dohme Corp. Pyridine-1-oxide derivatives and their use as factor xia inhibitors
US20220235013A1 (en) 2017-03-21 2022-07-28 Bayer Pharma Aktiengesellschaft 2-methyl-quinazolines
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
CN109721539B (zh) * 2017-10-27 2021-07-09 天津药物研究院有限公司 吡唑酰胺类衍生物及其制备方法和用途
CN109721613B (zh) * 2017-10-27 2021-07-30 四川科伦博泰生物医药股份有限公司 含季铵离子的大环酰胺化合物及其药物组合物和用途
CN109867660A (zh) * 2017-12-01 2019-06-11 四川科伦博泰生物医药股份有限公司 含季铵离子的四氢异喹啉酰胺化合物及其药物用途
CA3089970A1 (en) 2018-02-07 2019-08-15 eXIthera Pharmaceuticals Inc. Therapeutic compounds and compositions
GB201805174D0 (en) * 2018-03-29 2018-05-16 Univ Leeds Innovations Ltd Compounds
EP3781565A1 (en) 2018-04-18 2021-02-24 Bayer Pharma Aktiengesellschaft 2-methyl-aza-quinazolines
CN109232259B (zh) * 2018-09-27 2021-05-28 浙江理工大学 一种硝基苯乙酮的制备方法
CN111138366B (zh) * 2018-11-06 2023-03-28 天津药物研究院有限公司 吡唑氨基甲酰类衍生物、及其制备方法和用途
WO2020211781A1 (zh) 2019-04-16 2020-10-22 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
JP7286001B2 (ja) 2019-07-23 2023-06-02 メッドシャイン ディスカバリー インコーポレイテッド 第ＸＩａ因子阻害剤としての大環状誘導体
CN113004284B (zh) * 2019-12-20 2022-08-12 成都康弘药业集团股份有限公司 作为血浆激肽释放酶抑制剂的四环类化合物及其用途
CN113004283B (zh) * 2019-12-20 2022-08-12 成都康弘药业集团股份有限公司 作为血浆激肽释放酶抑制剂的四环类化合物及其用途
CN113004286B (zh) * 2019-12-20 2022-08-12 成都康弘药业集团股份有限公司 作为血浆激肽释放酶抑制剂的三环类化合物及其用途
WO2021136390A1 (zh) * 2019-12-31 2021-07-08 上海京新生物医药有限公司 凝血因子XIa抑制剂
TWI873290B (zh) * 2020-02-13 2025-02-21 德商百靈佳殷格翰國際股份有限公司 作為血漿激肽釋放酶抑制劑之雜芳族甲醯胺衍生物
CN113943259A (zh) * 2020-07-17 2022-01-18 西安禾渼生物医药有限公司 一种氨基酸衍生物、其制备方法及应用
US12129265B2 (en) 2020-07-21 2024-10-29 Ankh Life Sciences Limited Therapeutic agents and uses thereof
CN118373832B (zh) * 2023-01-20 2025-01-28 深圳晶蛋生物医药科技有限公司 大环类化合物、其药物组合物及其应用
CN116813490B (zh) * 2023-06-30 2025-08-08 常州大学 可见光驱动非天然氨基酸及其衍生物的合成方法
WO2025117439A1 (en) * 2023-11-30 2025-06-05 Viva Star Biosciences (Us) Inc. Macrocycle compounds as inhibitors of nlrp3 activity and therapeutic uses thereof

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3065190D1 (en) 1979-11-05 1983-11-10 Beecham Group Plc Enzyme derivatives, and their preparation
JPS62103070A (ja) 1985-10-29 1987-05-13 Mitsui Toatsu Chem Inc イソオキサゾリン誘導体および植物生長調節剤
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.
WO2000077027A2 (en) 1999-06-14 2000-12-21 Tularik Limited Serine protease inhibitors
TW557297B (en) * 1997-09-26 2003-10-11 Abbott Lab Rapamycin analogs having immunomodulatory activity, and pharmaceutical compositions containing same
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
US6951840B2 (en) * 2001-08-31 2005-10-04 Eli Lilly And Company Lipoglycopeptide antibiotics
CN102617567A (zh) 2001-09-21 2012-08-01 百时美施贵宝公司 含有内酰胺的化合物及其衍生物作为Xa因子的抑制剂
WO2003106438A1 (en) * 2002-06-18 2003-12-24 The Scripps Research Institute Synthesis of diazonamide "a" core
CN1160358C (zh) * 2002-10-09 2004-08-04 武汉大学 （8s，18s）－1，4，10，13，16－五氮杂三环[16.3.0.04,8]二十一烷－9，17－二酮及其制备方法和用途
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
EP1654245A1 (en) 2003-08-07 2006-05-10 Bayer Pharmaceuticals Corporation Benzofuran derivatives useful for treating hyper-proliferative disorders
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic 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
CN101006063B (zh) * 2004-06-15 2013-07-17 布里斯托尔-迈尔斯斯奎布公司 用作丝氨酸蛋白酶抑制剂的五元杂环类化合物
US7429604B2 (en) 2004-06-15 2008-09-30 Bristol Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
EP1841504B1 (en) 2005-01-13 2014-11-19 Bristol-Myers Squibb Company Substituted biaryl compounds as factor xia inhibitors
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
KR20080087817A (ko) 2005-12-14 2008-10-01 브리스톨-마이어스 스큅 컴퍼니 인자 ｘｉａ 억제제로서 아릴프로피온아미드,아릴아크릴아미드, 아릴프로핀아미드 또는 아릴메틸우레아유사체
KR20080080173A (ko) * 2005-12-14 2008-09-02 브리스톨-마이어스 스큅 컴퍼니 세린 프로테아제 억제제로서 유용한 6-원 헤테로사이클
ES2365815T3 (es) * 2005-12-14 2011-10-11 Bristol-Myers Squibb Company Análogos de arilpropionamida, arilacrilamida, arilpropinamida o arilmetilurea como inhibidores del factor xia.
US8466295B2 (en) 2005-12-14 2013-06-18 Bristol-Myers Squibb Company Thiophene derivatives as factor XIa 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
CN101495480B (zh) * 2006-05-03 2013-07-10 百时美施贵宝公司 作为降钙素基因相关肽受体拮抗剂的受限化合物
US7605126B2 (en) * 2006-08-11 2009-10-20 Enanta Pharmaceuticals, Inc. Acylaminoheteroaryl hepatitis C virus protease inhibitors
WO2008031508A1 (de) * 2006-09-13 2008-03-20 Sanofi-Aventis Tartratderivate als inhibitoren des koagulationsfaktors ixa
CN101605779B (zh) * 2006-12-15 2013-11-20 百时美施贵宝公司 作为凝血因子xia抑制剂的芳基丙酰胺、芳基丙烯酰胺、芳基丙炔酰胺或芳基甲基脲类似物
CN101611019A (zh) * 2006-12-20 2009-12-23 百时美施贵宝公司 可用作抗凝血药的大环凝血因子Ⅶa抑制剂
PE20081775A1 (es) * 2006-12-20 2008-12-18 Bristol Myers Squibb Co Compuestos macrociclicos como inhibidores del factor viia
PE20091002A1 (es) 2007-06-13 2009-07-15 Bristol Myers Squibb Co Analogos dipeptidos como inhibidores del factor de coagulacion
EP2197873B1 (en) * 2007-09-20 2014-07-16 Irm Llc Compounds and compositions as modulators of gpr119 activity
EP2065382A1 (de) 2007-10-18 2009-06-03 Boehringer Ingelheim Pharma GmbH & Co. KG CGRP Antagonisten
GB0800035D0 (en) 2008-01-02 2008-02-13 Glaxo Group Ltd Compounds
CN102026996B (zh) * 2008-03-13 2015-01-07 百时美施贵宝公司 作为凝血因子xia抑制剂的哒嗪衍生物
AU2011215898B2 (en) * 2010-02-11 2016-08-11 Bristol-Myers Squibb Company Macrocycles as Factor XIa inhibitors
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
ES2625256T3 (es) 2011-10-14 2017-07-19 Bristol-Myers Squibb Company Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIA
EP2766347B1 (en) 2011-10-14 2016-05-04 Bristol-Myers Squibb Company Substituted tetrahydroisoquinoline compounds as factor xia inhibitors
ES2572908T3 (es) 2011-10-14 2016-06-03 Bristol-Myers Squibb Company Compuestos de tetrahidroisoquinolina sustituidos como inhibidores del factor XIa
RU2630677C2 (ru) 2011-12-21 2017-09-12 Оно Фармасьютикал Ко., Лтд. Соединения
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
GB201209138D0 (en) 2012-05-24 2012-07-04 Ono Pharmaceutical Co Compounds

Also Published As

Publication number Publication date
TWI520965B (zh) 2016-02-11
US20160362414A1 (en) 2016-12-15
CN102834397B (zh) 2016-02-03
ES2822130T3 (es) 2021-04-29
US20150266894A1 (en) 2015-09-24
IL221343A0 (en) 2012-10-31
AU2011215898A1 (en) 2012-09-27
AU2011215898B2 (en) 2016-08-11
WO2011100402A1 (en) 2011-08-18
CO6551666A2 (es) 2012-10-31
JP5841547B2 (ja) 2016-01-13
US10487086B2 (en) 2019-11-26
EA020528B1 (ru) 2014-11-28
EP2534152B1 (en) 2018-05-02
CA2789622A1 (en) 2011-08-18
TW201130847A (en) 2011-09-16
TWI577665B (zh) 2017-04-11
AR080167A1 (es) 2012-03-21
MX2012008874A (es) 2012-08-31
US20120309960A1 (en) 2012-12-06
JP6294286B2 (ja) 2018-03-14
ES2674745T3 (es) 2018-07-03
CN107973809A (zh) 2018-05-01
US20200087312A1 (en) 2020-03-19
US20180022753A1 (en) 2018-01-25
US11136327B2 (en) 2021-10-05
US20230058729A1 (en) 2023-02-23
JP2013519679A (ja) 2013-05-30
KR101843542B1 (ko) 2018-03-30
US9079918B2 (en) 2015-07-14
IL221343B (en) 2019-01-31
NZ602266A (en) 2014-05-30
WO2011100401A1 (en) 2011-08-18
SG183153A1 (en) 2012-09-27
CA2789622C (en) 2018-04-03
US8828983B2 (en) 2014-09-09
MY162936A (en) 2017-07-31
US20120041190A1 (en) 2012-02-16
PE20160841A1 (es) 2016-09-10
US9802939B2 (en) 2017-10-31
TW201605806A (zh) 2016-02-16
KR101901545B1 (ko) 2018-09-21
US20150112058A1 (en) 2015-04-23
BR112012019925B1 (pt) 2022-06-14
EP2534152A1 (en) 2012-12-19
CN102753555A (zh) 2012-10-24
US9745313B2 (en) 2017-08-29
KR20170135981A (ko) 2017-12-08
JP2016102114A (ja) 2016-06-02
PH12012501589A1 (en) 2012-10-22
CN102834397A (zh) 2012-12-19
CN107973809B (zh) 2023-06-30
EP3786165A1 (en) 2021-03-03
EA201270716A1 (ru) 2013-03-29
EP2534154B1 (en) 2020-08-05
CN102753555B (zh) 2018-01-12
EP2534154A1 (en) 2012-12-19
JP5844287B2 (ja) 2016-01-13
JP2013519678A (ja) 2013-05-30
KR20120134122A (ko) 2012-12-11
CL2012002229A1 (es) 2013-01-11
US9453029B2 (en) 2016-09-27
US8940720B2 (en) 2015-01-27
BR112012019925A2 (pt) 2021-04-20
ZA201206758B (en) 2014-02-26
US20140343276A1 (en) 2014-11-20
US12404274B2 (en) 2025-09-02

Similar Documents

Publication Publication Date Title
PE20121806A1 (es) Macrociclos como inhibidores del factor de coagulacion (fxia)
PE20121500A1 (es) 2-amino-5,5-difluor-5,6-dihidro-4h-oxazinas como inhibidores de bace 1 y/o bace 2
PE20091843A1 (es) Inhibidores de catepsina c
PE20091834A1 (es) Compuestos de 2-imino-3-metilpirrolopirimidinona tiofenilo-sustituida como inhibidores de bace-1 y composiciones que los contienen
PH12014500947B1 (en) 1,2,5-oxadiazoles as inhibitors of indoleamine 2,3-dioxygenase
PE20090770A1 (es) Derivados de benzoxazolona
PE20160654A1 (es) Compuestos de inhibidor de autotaxina
CO6680699A2 (es) Derivados de amina para el control de plagas
PE20121182A1 (es) Derivados arilo y heteroarilcarbonilo de hexahidroindenopiridina y octahidrobenzoquinolina
PE20141540A1 (es) Derivados de 2-amino-4-(piridin-2-il)-5,6-dihidro-4h-1,3-oxazina y su uso como inhibidores de bace-1 y/o bace-2
CR20110013A (es) Derivados de Heteroarilo como Inhibidores de DGAT1
PE20141726A1 (es) Heterociclilaminas como inhibidores de pi 3k
PE20161243A1 (es) Compuesto heterociclico fusionado
PE20091623A1 (es) DERIVADOS DE 1H-PIRAZOLO[3,4-b]PIRIDINA COMO INHIBIDORES DE RAF QUINASA
PE20091901A1 (es) Activadores de glucoquinasa
CO6311079A2 (es) Derivados de aminodihidrotiazina como inhibidores de la enzima bace para el tratamiento de la enfermedad de alzheimer
PE20121352A1 (es) Derivados de heteroarilo que contienen n como inhibidores de cinasa jak3
PE20121180A1 (es) (heteroarilmetil) tiohidantoinas sustituidas como drogas anticancer
CO6150181A2 (es) Compuesto 6-(bencilo sustituido con heterociclo)-4-oxoquinolina y su uso como inhibidor de integrasa vih
MX339252B (es) Derivados de acido carboxilico de pirrolidina o tiazolidina, composicion farmaceutica y metodos para su uso en el tratamiento de transtornos metabolicos, como agonistas del receptor 43 acoplado por proteina-g (gpr43).
AR084011A1 (es) Compuestos nitrogenados heterociclicos utiles para el tratamiento de infecciones por el virus sincitial respiratorio (rsv), proceso para prepararlos y composiciones farmaceuticas que los contienen
PE20140966A1 (es) Quinazolincarboxamida azetidinas
PE20150021A1 (es) 5-amino[1,4]tiazinas como inhibidores de bace1
MX383762B (es) Derivados de glutarimida, uso de los mismos, composición farmacéutica basada en los mismos y métodos para producir derivados de glutarimida.
AR087494A1 (es) Derivados de isoxazolina como compuestos insecticidas

Legal Events

Date Code Title Description
FG Grant, registration