PE20071132A1 - Compuestos macrociclicos como inhibidores del factor viia - Google Patents
Compuestos macrociclicos como inhibidores del factor viiaInfo
- Publication number
- PE20071132A1 PE20071132A1 PE2006001599A PE2006001599A PE20071132A1 PE 20071132 A1 PE20071132 A1 PE 20071132A1 PE 2006001599 A PE2006001599 A PE 2006001599A PE 2006001599 A PE2006001599 A PE 2006001599A PE 20071132 A1 PE20071132 A1 PE 20071132A1
- Authority
- PE
- Peru
- Prior art keywords
- halo
- alkyl
- independently
- factor viia
- macrocyclic compounds
- Prior art date
Links
- 150000002678 macrocyclic compounds Chemical class 0.000 title abstract 2
- 229940012414 factor viia Drugs 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 239000002253 acid Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 230000009424 thromboembolic effect Effects 0.000 abstract 2
- 108010054265 Factor VIIa Proteins 0.000 abstract 1
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical group [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000002526 effect on cardiovascular system Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
- C07D245/02—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms not condensed with other rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D245/00—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms
- C07D245/04—Heterocyclic compounds containing rings of more than seven members having two nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
- C07D255/02—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D255/00—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00
- C07D255/04—Heterocyclic compounds containing rings having three nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D249/00 - C07D253/00 condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D273/00—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00
- C07D273/02—Heterocyclic compounds containing rings having nitrogen and oxygen atoms as the only ring hetero atoms, not provided for by groups C07D261/00 - C07D271/00 having two nitrogen atoms and only one oxygen atom
-
- 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
- C07D403/12—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 chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Peptides Or Proteins (AREA)
Abstract
SE REFIERE A COMPUESTOS MACROCICLICOS DE FORMULA (I), EN DONDE A Y B INDEPENDIENTEMENTE ES FENILO O UN ISOMERO DE PIRIDILO; M ES -CONH-, -SO2NH-, -NHCO-, O -NHSO2-; Y CUANDO M ES -NHCO-, L ES -C(R12R13)C(R12R13)-, -C(R12R13)C(R12R13)C(R12R13)-, C(R12R13)C(R12R13)-, ENTRE OTROS; W ES a), b), ENTRE OTROS, SUSTITUIDOS CON R14; Z ES NH, O u S; R1 ES H, HALO, ALQUILO(C1-C4), ENTRE OTROS; R2 Y R3 SON INDEPENDIENTEMENTE H, HALO, -ORa-, -SRb, CF3, ENTRE OTROS; R4 ES H, ENTRE OTROS; R5 ES H, -(CH2)qORa, ALQUILO(C1-C6), ENTRE OTROS; R6 ES H, -(CH2)rORa, -(CH2)rSRb, ENTRE OTROS; R7 ES H O ALQUILO(C1-C6); R8 ES H, HALO, -SO2Rb, ENTRE OTROS; R9, R10 y R11 SON INDEPENDIENTEMENTE H, HALO, ALQUILO(C1-C4), O ALCOXI(C1-C4). SON SELECCIONADOS: SAL DEL ACIDO 2-(1-AMINO-ISOQUINOLIN-6-ILAMINO)-16-OXA-4,11-DIAZA-TRICICLO[15.2.2.16,10] DOCOSA-1(20),6,8,10(22),17(21),18-HEXAENO-3,12-DIONA TRIFLUOROACETICO, SAL DEL ACIDO 2-(1-AMINO-ISOQUINOLIN-6-ILAMINO)-4,11-DIAZA-TRICICLO[14.2.2.16,10]HENICOSA-1(19),6,8,10(21),16(20),17-HEXAENO-3,12-DIONA TRIFLUROACETICO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES SELECTIVOS DEL FACTOR VIIa DE COAGULACION DE SERINA PROTEASA Y SON UTILES PARA EL TRATAMIENTO DE TRASTORNO TROMBOEMBOLICO, TAL COMO TRASTORNO TROMBOEMBOLICO CARDIOVASCULAR ARTERIAL, VENOSOS Y DE CAVIDADES DEL CORAZON
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US75378605P | 2005-12-23 | 2005-12-23 | |
| US86547506P | 2006-11-13 | 2006-11-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20071132A1 true PE20071132A1 (es) | 2007-12-14 |
Family
ID=37897422
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2006001599A PE20071132A1 (es) | 2005-12-23 | 2006-12-13 | Compuestos macrociclicos como inhibidores del factor viia |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US7592331B2 (es) |
| EP (1) | EP1971582B1 (es) |
| JP (1) | JP5139999B2 (es) |
| KR (1) | KR20080087848A (es) |
| AR (1) | AR058380A1 (es) |
| AU (1) | AU2006330495A1 (es) |
| BR (1) | BRPI0620254A2 (es) |
| CA (1) | CA2634794A1 (es) |
| EA (1) | EA200801592A1 (es) |
| ES (1) | ES2395052T3 (es) |
| IL (1) | IL192105A0 (es) |
| NO (1) | NO20082629L (es) |
| NZ (1) | NZ568715A (es) |
| PE (1) | PE20071132A1 (es) |
| TW (1) | TW200745062A (es) |
| WO (1) | WO2007076431A1 (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PE20081775A1 (es) * | 2006-12-20 | 2008-12-18 | Bristol Myers Squibb Co | Compuestos macrociclicos como inhibidores del factor viia |
| CN101631784A (zh) * | 2006-12-20 | 2010-01-20 | 百时美施贵宝公司 | 用作抗凝血药的二环内酰胺凝血因子viia抑制剂 |
| 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 |
| EP2858977A1 (en) | 2012-06-08 | 2015-04-15 | Bristol-Myers Squibb Company | Macrocyclic factor viia inhibitors |
| PE20150639A1 (es) | 2012-10-12 | 2015-05-11 | Bristol Myers Squibb Co | Formas cristalinas de inhibidor del factor xia |
| WO2014059214A1 (en) | 2012-10-12 | 2014-04-17 | Bristol-Myers Squibb Company | Guanidine and amine substituted tetrahydroisoquinoline compounds as factor xia inhibitors |
| EP2906552B1 (en) | 2012-10-12 | 2017-11-22 | Bristol-Myers Squibb Company | Guanidine 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 |
| EP3008052A1 (en) * | 2013-06-13 | 2016-04-20 | Bristol-Myers Squibb Company | Macrocyclic factor viia inhibitors |
| 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 | ||
| US10081623B2 (en) | 2014-09-04 | 2018-09-25 | Bristol-Myers Squibb Company | Diamide macrocycles that are FXIa inhibitors |
| US9453018B2 (en) | 2014-10-01 | 2016-09-27 | Bristol-Myers Squibb Company | Pyrimidinones as factor XIa inhibitors |
| EP3310777B1 (en) * | 2015-06-19 | 2019-10-09 | Bristol-Myers Squibb Company | Diamide macrocycles as factor xia inhibitors |
| CN115404020B (zh) * | 2022-10-14 | 2023-06-30 | 深圳市高仁电子新材料有限公司 | 一种用于全贴合和柔性折叠屏的三层结构的丙烯酸类光学胶膜及其制备方法 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5843442A (en) | 1990-10-22 | 1998-12-01 | Corvas International, Inc. | Blood coagulation protein antagonists and uses therefor |
| US5866542A (en) | 1994-10-18 | 1999-02-02 | Corvas International, Inc. | Nematode-extracted anticoagulant protein |
| WO1999013063A1 (en) * | 1997-09-09 | 1999-03-18 | Nycomed Imaging As | Factor vii fragments and analogs thereof and their use in the treatment of blood clottng disorders |
| US6642252B2 (en) | 2000-11-07 | 2003-11-04 | Bristol-Myers Squibb Company | Acid derivatives useful as serine protease inhibitors |
| WO2003011222A2 (en) | 2001-07-27 | 2003-02-13 | Merck & Co., Inc. | Thrombin inhibitors |
| EP1594505A4 (en) | 2003-02-11 | 2008-08-13 | Bristol Myers Squibb Co | PHENYLGLYCIN DERIVATIVES USEFUL AS SERINE PROTEASE INHIBITORS |
| WO2004072102A2 (en) | 2003-02-11 | 2004-08-26 | Bristol-Myers Squibb Company | Benzene acetamide compounds useful as serine protease inhibitors |
| WO2006076246A2 (en) | 2005-01-10 | 2006-07-20 | Bristol-Myers Squibb Company | Phenylglycinamide derivatives useful as anticoagulants |
| ATE455103T1 (de) | 2005-06-24 | 2010-01-15 | Bristol Myers Squibb Co | Als antikoagulationsmittel geeignete phenylglycinamid- und pyridylglycinamidderivate |
-
2006
- 2006-12-13 AR ARP060105501A patent/AR058380A1/es unknown
- 2006-12-13 PE PE2006001599A patent/PE20071132A1/es not_active Application Discontinuation
- 2006-12-13 TW TW095146558A patent/TW200745062A/zh unknown
- 2006-12-21 EP EP06846746A patent/EP1971582B1/en active Active
- 2006-12-21 CA CA002634794A patent/CA2634794A1/en not_active Abandoned
- 2006-12-21 ES ES06846746T patent/ES2395052T3/es active Active
- 2006-12-21 EA EA200801592A patent/EA200801592A1/ru unknown
- 2006-12-21 NZ NZ568715A patent/NZ568715A/en not_active IP Right Cessation
- 2006-12-21 JP JP2008547767A patent/JP5139999B2/ja not_active Expired - Fee Related
- 2006-12-21 US US11/614,131 patent/US7592331B2/en active Active
- 2006-12-21 AU AU2006330495A patent/AU2006330495A1/en not_active Abandoned
- 2006-12-21 WO PCT/US2006/062469 patent/WO2007076431A1/en not_active Ceased
- 2006-12-21 KR KR1020087017981A patent/KR20080087848A/ko not_active Withdrawn
- 2006-12-21 BR BRPI0620254-3A patent/BRPI0620254A2/pt not_active IP Right Cessation
-
2008
- 2008-06-04 NO NO20082629A patent/NO20082629L/no not_active Application Discontinuation
- 2008-06-12 IL IL192105A patent/IL192105A0/en unknown
-
2009
- 2009-07-23 US US12/507,907 patent/US20090281139A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| ES2395052T3 (es) | 2013-02-07 |
| JP2009521505A (ja) | 2009-06-04 |
| KR20080087848A (ko) | 2008-10-01 |
| US7592331B2 (en) | 2009-09-22 |
| EP1971582B1 (en) | 2012-10-10 |
| IL192105A0 (en) | 2008-12-29 |
| BRPI0620254A2 (pt) | 2011-11-08 |
| US20070208054A1 (en) | 2007-09-06 |
| EP1971582A1 (en) | 2008-09-24 |
| WO2007076431A1 (en) | 2007-07-05 |
| NO20082629L (no) | 2008-09-05 |
| NZ568715A (en) | 2011-01-28 |
| EA200801592A1 (ru) | 2008-12-30 |
| AR058380A1 (es) | 2008-01-30 |
| CA2634794A1 (en) | 2007-07-05 |
| TW200745062A (en) | 2007-12-16 |
| AU2006330495A1 (en) | 2007-07-05 |
| JP5139999B2 (ja) | 2013-02-06 |
| US20090281139A1 (en) | 2009-11-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration | ||
| FD | Application declared void or lapsed |