AR036832A1 - Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos - Google Patents
Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentosInfo
- Publication number
- AR036832A1 AR036832A1 ARP020103876A ARP020103876A AR036832A1 AR 036832 A1 AR036832 A1 AR 036832A1 AR P020103876 A ARP020103876 A AR P020103876A AR P020103876 A ARP020103876 A AR P020103876A AR 036832 A1 AR036832 A1 AR 036832A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- aryl
- independently selected
- cycloalkyl
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
- C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
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- 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
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic 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
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- 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
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- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/06—Antiarrhythmics
-
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
- C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
- C07D493/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Abstract
Un compuesto derivado de himbacina representado por la fórmula estructural (1) o una sal farmacéuticamente aceptable de los mismos, en la cual R representa 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en H, alquilo C1-6, halógeno, hidroxi, amino, alquilo C1-6-amino, dialquilamino C1-6, alcoxi C1-6, -COR16, -COOR17, -SOR16, -SO2R16, -SO2NR17R18, -NR17SO2R18, -NR16COR16a, -NR16COOR16a, -NR16CONR4R5, flúor-alquilo C1-6, diflúor-alquilo C1-6, triflúor-alquilo C1-6, cicloalquilo C3-6, arilo-alquilo C1-6, hidroxi-alquilo C1-6, amino-alquilo C1-6, arilo y tio-alquilo C1-6; R1 y R2 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, flúor-alquilo C1-6, diflúor -alquilo C1-6, triflúor-alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, aril-alquilo C1-6, hidroxi-alquilo C1-6, amino-alquilo C1-6, arilo y tio-alquilo C1-6; ó R1 y R2 conjuntamente forman un grupo =O; R3 es H, hidroxi, alcoxi C1-6, ariloxi, aril-alquiloxi C1-6, heteroariloxi, heteroaril-alquiloxi C1-6, cicloalquiloxi C3-6, -SOR16, -SO2R17, -SO2NR18R19, -SR18, -SO3H, -C(O)OR17, -C(O)NR18R19, -OC(O)R32, -OC(O)NR33R34, -(CR33R34)nOR32, -NR4R5, -NR33COOR32, -NR33COR32, -NR33S(O)2R32, -NR33CONR33R34, -NR33S(O)2NR33R34, -(CR33R34)Nnr4r5, -(cr33r34)nNR33COOR32, -(CR33R34)nNR33COR32, -(CR33R34)nNR33S(O)R32, -(CR33R34)nNR33CONR33R34,-(CR33R34)nNR33S(O)2NR33R34, alquilo C1-6, halógeno, cicloalquilo C3-6, alquenilo C2-6, -CN, arilo, heteroarilo, heterocicloalquilo, -P(O)(OR7)2 ó alquilo C1-6 sustituido con 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en halógeno, -OH, -NH2, arilo, -COOH, -SO3H, tio y alquiltio C1-6; n es 1, 2, 3, ó 4; n1 y n2 son independientemente 0-3, con la condición de que ambos no sean 0; Het es un grupo heteroaromático mono-, bi- ó tricíclico C5-14 que comprende C1-13 y 1 a 4 heteroátomos independientemente seleccionados del grupo que consiste en N, O y S, donde un nitrógeno del anillo puede formar un N-óxido o un grupo cuaternario con un grupo alquilo C1-4, donde Het está adherido a B mediante un miembro de anillo de átomo de carbono y donde el grupo Het está sustituido con 1 a 4 sustituyentes, W, está independientemente seleccionado del grupo que consiste en alquilo C1-6; -NR4R5, -NHCOR26, -NHSO2R16, R21-arilo, arilo donde los átomos de carbono adyacentes forman un anillo con un grupo metilendioxi; y R21-heteroarilo; R4 y R5 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, fenilo, bencilo, y cicloalquilo C3-6, ó R4 y R5 conjuntamente son -(CH2)3-,-(CH2)4-,-(CH2)5- ó (CH2)2NR7-(CH2)2- y forman un anillo con el nitrógeno al cual están adheridos; R7 es H ó alquilo C1-6; R8, R10 y R11 están independientemente seleccionados del grupo que consiste en R1 y -OR1; R9 es H, OH, -NR4R5, alcoxi C1-6, halógeno o halo-alquilo C1-6; B es -(CH2)n3- ó cis ó trans -(CH2)n4CR12 =CR12a(CH2)n5, donde n3 es 0-5, n4 y n5 son independientemente 0-2, y R12 y R12a están independientemente seleccionados del grupo que consiste en H, alquilo C1-6 y halógeno; R16 y R16a están independientemente seleccionados del grupo que consiste en alquilo C1-6, fenilo y bencilo; R17, R18 y R19 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, fenilo y bencilo; R21 representa de 1 a 3 sustituyentes independientemente seleccionados del grupo que consiste en H, -CF3, -OCF3, halógeno, -NO2, alquilo C1-6, alcoxi C1-6, -NH2, alquiloC1-6-amino, di-(alquilo C1-6)amino, amino-alquilo C1-6, alquilamino C1-6 alquilo C1-6, di-(alquilo C1-6)-amino-alquilo C1-6, hidroxi-alquilo C1-6, -COOR17, -COR17, -CONR24R25, -NHCOR16, -NHSO2R16, NHSO2CH2CF3, -SO2NR24R25, -NR29C(O)NR24R25, -SO2R30, -P(O)(OR29)2, arilo, arilo-alquilo C1-6, heteroarilo, heterocicloalquilo, y -CR29(=NOR28); R22 es -COR23, -S(O)R31, -S(O)2R31, -SO2NR24R25 ó -COOR27; R23 es halo-alquilo C1-6, alquenilo C2-6, halo-alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquilo C3-7-alquilo C1-6, cicloalquilo C3-7 sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en halo, alcoxi C1-3-alquilo C1-3, hidroxi y alcoxi C1-6, arilo, aril-alquilo C2-6, heteroarilo, heterocicloalquilo, alquilo C1-6 sustituido con 1-3 sustituyentes independientemente seleccionados de -COOH y SO3H; ó fórmula (2) donde R35 y R36 están independientemente seleccionados del grupo que consiste en H, alquilo, o alquilo C1-6 sustituido con R37, donde R37 está seleccionado del grupo que consiste en HO-, HS-, -CH2S-, -NH2, fenilo, p-hidroxifenilo e indolilo; R24 y R25 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6, halo-alquilo C1-6, alquenilo C2-6, haloa-alquilo C2-6, alquinilo C2-6, arilo, aril-alquilo C1-6, cicloalquilo C3-7, halo-cicloalquilo C3-7, alcoxi C1-3-alquilo C1-3, hidroxi y alcoxi C1-6; R26 es cicloalquilo C3-7, arilo, aril-alquilo C1-6, heteroarilo, heteroaril-alquilo C1-6 ó alquilamino C1-6; R27 es alquilo C1-6, fenilo, bencilo, alcoxi C1-3-alquilo C1-3, cicloalquilo C3-7, carboxi-alquilo C1-6, sulfo-alquilo C1-6 ó alquilo C1-6 sustituido con NR18R19 y carboxi; R28 es H, alquilo C1-6, fenilo, bencilo ó alcoxi C1-3-alquilo C1-3; R29 y R30 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6; R31 es alquilo C1-6, halo-alquilo C1-6, alquenilo C2-6, halo-alquilo C2-6, alquinilo C2-6, cicloalquilo C3-7, cicloalquilo C3-7 sustituido con 1 a 3 sustituyentes seleccionados del grupo que consiste en halo, alcoxi C1-3-alquilo C1-3, hidroxi y alcoxi C1-6; arilo, aril-alquilo C1-6, heteroarilo, heterocicloalquilo, alquilo C1-6 sustituido con 1 a 3 sustituyentes independientemente seleccionados de -COOH y SO3H; ó alcoxi C1-6; R32 es R35-alquilo C1-6, R35-cicloalquilo C3-7, R35-alquenilo C2-6, R35-alquinilo C2-6 ó R35-arilo, donde R35 representa uno o dos sustituyentes independientemente seleccionados del grupo que consiste en H, -COOH, -NH2, -SO3H, =O y =NOR28; y R33 y R34 están independientemente seleccionados del grupo que consiste en H, alquilo C1-6 y cicloalquilo C3-7, así como también composiciones farmacéuticas que los contienen y un método para tratar enfermedades asociadas con trombosis, arteriosclerosis, restenosis, hipertensión, angina pectoris, arritmia, insuficiencia cardíaca y cáncer mediante la administración de dichos compuestos.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US33035901P | 2001-10-18 | 2001-10-18 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR036832A1 true AR036832A1 (es) | 2004-10-06 |
Family
ID=23289411
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP020103876A AR036832A1 (es) | 2001-10-18 | 2002-10-16 | Compuestos derivados de himbacina, agonistas receptores de trombina, composiciones farmaceuticas y el uso de dichos compuestos para la preparacion de medicamentos |
Country Status (23)
Country | Link |
---|---|
US (2) | US7037920B2 (es) |
EP (1) | EP1436298B1 (es) |
JP (2) | JP4307260B2 (es) |
KR (1) | KR100960170B1 (es) |
CN (1) | CN100369917C (es) |
AR (1) | AR036832A1 (es) |
AT (1) | ATE525378T1 (es) |
AU (1) | AU2002335031C1 (es) |
BR (1) | BR0213967A (es) |
CA (1) | CA2463628A1 (es) |
CO (1) | CO5570668A2 (es) |
EC (1) | ECSP045064A (es) |
HU (1) | HUP0500443A3 (es) |
IL (1) | IL160918A0 (es) |
MX (1) | MXPA04003610A (es) |
MY (1) | MY139335A (es) |
NO (1) | NO329349B1 (es) |
NZ (1) | NZ531869A (es) |
PE (1) | PE20030808A1 (es) |
PL (1) | PL371948A1 (es) |
RU (1) | RU2319704C9 (es) |
WO (1) | WO2003033501A1 (es) |
ZA (1) | ZA200402849B (es) |
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US9701669B2 (en) | 2013-08-22 | 2017-07-11 | Merck Sharp & Dohme Corp. | Preparation and use of 7a-amide substituted- 6,6-difluoro bicyclic himbacine derivatives as PAR-1 receptor antagonists |
WO2015026685A1 (en) | 2013-08-22 | 2015-02-26 | Merck Sharp & Dohme Corp. | 7a-heterocycle substituted- 6, 6-difluoro bicyclic himbacine derivatives |
US9969724B2 (en) | 2014-04-16 | 2018-05-15 | Merck Sharp & Dohme Corp. | Factor IXa inhibitors |
CN104610330A (zh) * | 2015-02-25 | 2015-05-13 | 成都安斯利生物医药有限公司 | 一种制备(e)-3-丙烯酸乙酯频呐硼酸酯的方法 |
WO2022018156A1 (en) | 2020-07-22 | 2022-01-27 | Janssen Pharmaceutica Nv | Compounds useful as factor xia inhibitors |
US11845748B2 (en) | 2021-03-18 | 2023-12-19 | Janssen Pharmaceutica Nv | Bicyclic pyridine N-oxide derivatives useful as a factor XIa inhibitors |
US11814364B2 (en) | 2021-03-18 | 2023-11-14 | Janssen Pharmaceutica Nv | Pyridine N-oxide derivatives useful as factor XIa inhibitors |
US11919881B2 (en) | 2021-03-18 | 2024-03-05 | Janssen Pharmaceutica Nv | Substituted pyridine N-oxide derivatives useful as a factor XIa inhibitors |
US11897880B2 (en) | 2021-04-30 | 2024-02-13 | Janssen Pharmaceutica Nv | 7,8-dihydrobenzo[e]pyrido[3,4-c]azocine-2,5(3H,6H)-dione derivatives useful as a factor XIa inhibitors |
US11958856B2 (en) | 2021-07-22 | 2024-04-16 | Janssen Pharmaceutica Nv | Substituted 1,2,3,8,9,9a-hexahydro-5H-pyrrolo[1,2-a]azepin-5-ones as factor XIa inhibitors |
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US5716952A (en) * | 1992-03-18 | 1998-02-10 | Allergan | Method for reducing intraocular pressure in the mammalian eye by administration of muscarinic antagonists |
IL106197A (en) | 1992-07-30 | 1999-11-30 | Cor Therapeutics Inc | Agagonists for the rhombin receptors and pharmaceutical preparations containing them |
JP2000229961A (ja) | 1998-12-11 | 2000-08-22 | Sagami Chem Res Center | ヒドロナフト[2,3−c]フラン誘導体およびその製造方法 |
US6063847A (en) * | 1997-11-25 | 2000-05-16 | Schering Corporation | Thrombin receptor antagonists |
DE19801636A1 (de) * | 1998-01-17 | 1999-07-22 | Bayer Ag | Substituierte bicyclische Lactone |
EP2301930B1 (en) | 2000-06-15 | 2016-01-06 | Merck Sharp & Dohme Corp. | Derivatives of hexahydrobenzofuranone useful for the treatment of (inter alia) auto-immune or inflammatory disorders |
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