AR043413A1 - Derivados de etinilo, un procedimiento para su preparacion, los medicamentos que los contienen, el empleo de estos derivados para preparar un medicamento, y un kit que los incluye - Google Patents
Derivados de etinilo, un procedimiento para su preparacion, los medicamentos que los contienen, el empleo de estos derivados para preparar un medicamento, y un kit que los incluyeInfo
- Publication number
- AR043413A1 AR043413A1 ARP040100613A ARP040100613A AR043413A1 AR 043413 A1 AR043413 A1 AR 043413A1 AR P040100613 A ARP040100613 A AR P040100613A AR P040100613 A ARP040100613 A AR P040100613A AR 043413 A1 AR043413 A1 AR 043413A1
- Authority
- AR
- Argentina
- Prior art keywords
- oxo
- derivatives
- imino
- formula
- diyl
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 4
- 229940126601 medicinal product Drugs 0.000 title 1
- -1 phenylene, pyridin-diyl Chemical group 0.000 abstract 25
- 206010028980 Neoplasm Diseases 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229940079593 drug Drugs 0.000 abstract 2
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 abstract 2
- 239000004615 ingredient Substances 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 239000000203 mixture Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 239000012453 solvate Substances 0.000 abstract 2
- 238000011282 treatment Methods 0.000 abstract 2
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 108010039209 Blood Coagulation Factors Proteins 0.000 abstract 1
- 102000015081 Blood Coagulation Factors Human genes 0.000 abstract 1
- 206010061218 Inflammation Diseases 0.000 abstract 1
- 206010022562 Intermittent claudication Diseases 0.000 abstract 1
- 206010027476 Metastases Diseases 0.000 abstract 1
- 208000031481 Pathologic Constriction Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 108090000190 Thrombin Proteins 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 208000007536 Thrombosis Diseases 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 abstract 1
- 238000002399 angioplasty Methods 0.000 abstract 1
- 230000023555 blood coagulation Effects 0.000 abstract 1
- 239000003114 blood coagulation factor Substances 0.000 abstract 1
- 230000015271 coagulation Effects 0.000 abstract 1
- 238000005345 coagulation Methods 0.000 abstract 1
- 230000004054 inflammatory process Effects 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 229940127557 pharmaceutical product Drugs 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 230000036262 stenosis Effects 0.000 abstract 1
- 208000037804 stenosis Diseases 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 229960004072 thrombin Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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 ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/06—Antimigraine agents
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- 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
- 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
- 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
- C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
- C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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 ring carbon atoms
- C07D233/44—Nitrogen atoms not forming part of a nitro radical
- C07D233/46—Nitrogen atoms not forming part of a nitro radical with only hydrogen atoms attached to said nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
- C07D265/32—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings with oxygen atoms directly attached to ring carbon atoms
-
- 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
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6527—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and oxygen atoms as the only ring hetero atoms
- C07F9/6533—Six-membered rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Diabetes (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
Los derivados de etinilo de fórmula (1) donde significan X fenileno, piridin-diílo, pirimidin-diílo o tiofen-diílo; R1 A, que puede estar mono, di o trisustituido por S(O)mA, Ar, NH2, NHA, NA2, OH, OA, PO(OA)2, etinilo u O(CH2)nPh, R2 H, Hal o A; R3 2-oxo-piperidin-1-ilo, 2-oxo-pirrolidin-1-ilo, 2-oxo-1H-piridin-1-ilo, 3-oxo-morfolin-4-ilo, 4-oxo-1H-piridin-1ilo, 2-oxo-1H-pirazin-1-ilo, 2-oxo-imidazolidin-1-ilo, 2-imino-piperidin-1-ilo, 2-imino-pirrolidin-1-ilo, 3-imino-morfolin-4-ilo, 2-imino-imidazolidin-1-ilo, 2-imino-1H-pirazin-1-ilo, 2,6dioxopiperidin-1-ilo, 2-oxo-piperazin-1-ilo, 2,6-dioxo-piperazin-1-ilo, 2,5-dioxo-pirrolidin-1-ilo, 2-oxo-1,3-oxazolidin-3-ilo, 3-oxo-2H-piridazin-2-ilo, 2-caprolactan-1-ilo (= 2-oxo-azepan-1-ilo), 2-aza-biciclo[2.2.2]-octan-3-on-2-ilo, 5,6-dihidro-1H-pirimidin-2-oxo-1-ilo, 2-oxo-[1,3]oxazinan-3-ilo o 4H-[1,4]oxazin-4-ilo, h fenilo, r NH u O, alquilo no ramificado o ramificado con 1-10 átomos de C, y también 1-7 átomos de H pueden estar reemplazados por F, a1 es F, Cl, Br o I, 0, 1 o 2, 0, 1 o 2, así como sus derivados, sales, solvatos y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, son inhibidores del actor de coagulación Xa y pueden ser utilizados para la profilaxis y/o la terapia de enfermedades tromboembólicas y para el tratamiento de tumores. Los compuestos de fórmula (1) también son inhibidores de los factores de coagulación VIIa y IXa y la trombina de la cascada de coagulación sanguínea. También se describen los productos farmacéuticos que contienen los compuestos de fórmula (1) y el uso de dichos compuestos para preparar un medicamento para el tratamiento de trombosis, infarto de miocardio, arterioesclerosis, inflamaciones, apoplejía, angina de pecho, estenosis post-angioplastia, claudicatio intermittens, migrana, tumores, enfermedades tumorales y/o metástasis tumorales, ya sea en forma individual o en combinación con al menos otro ingrediente activo medicamentoso. Finalmente se describe un Kit que consiste en envases separados de (a) una cantidad efectiva de un compuesto de la fórmula (1) y/o sus derivados, sales, solvatos y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones, y (b) una cantidad efectiva de otro ingrediente activo medicamentoso.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10308907A DE10308907A1 (de) | 2003-02-28 | 2003-02-28 | Ethynylderivate |
Publications (1)
Publication Number | Publication Date |
---|---|
AR043413A1 true AR043413A1 (es) | 2005-07-27 |
Family
ID=32842052
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040100613A AR043413A1 (es) | 2003-02-28 | 2004-02-27 | Derivados de etinilo, un procedimiento para su preparacion, los medicamentos que los contienen, el empleo de estos derivados para preparar un medicamento, y un kit que los incluye |
Country Status (15)
Country | Link |
---|---|
US (1) | US7427618B2 (es) |
EP (1) | EP1597244B1 (es) |
JP (1) | JP2006519188A (es) |
KR (1) | KR20050105493A (es) |
CN (1) | CN1753882A (es) |
AR (1) | AR043413A1 (es) |
AT (1) | ATE473217T1 (es) |
AU (1) | AU2004215708B2 (es) |
BR (1) | BRPI0407865A (es) |
CA (1) | CA2517391A1 (es) |
DE (2) | DE10308907A1 (es) |
MX (1) | MXPA05009002A (es) |
PL (1) | PL377531A1 (es) |
WO (1) | WO2004076429A1 (es) |
ZA (1) | ZA200507818B (es) |
Families Citing this family (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN105294669B (zh) * | 2014-10-24 | 2019-01-22 | 山东凯森制药有限公司 | 一种第十因子抑制剂及其制备方法和应用 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ZA928276B (en) | 1991-10-31 | 1993-05-06 | Daiichi Seiyaku Co | Aromatic amidine derivates and salts thereof. |
IL115420A0 (en) | 1994-09-26 | 1995-12-31 | Zeneca Ltd | Aminoheterocyclic derivatives |
DE19530996A1 (de) | 1995-08-23 | 1997-02-27 | Boehringer Mannheim Gmbh | Cyclische Guanidine, Verfahren zu ihrer Herstellung und Arzneimittel |
CA2294042A1 (en) | 1997-06-26 | 1999-01-07 | David Kent Herron | Antithrombotic agents |
US6956988B2 (en) * | 1998-08-21 | 2005-10-18 | Avanex Corporation | Optical interleaver |
US6635657B1 (en) | 1998-12-23 | 2003-10-21 | Eli Lilly And Company | Aromatic amides |
DE10063008A1 (de) * | 2000-12-16 | 2002-06-20 | Merck Patent Gmbh | Carbonsäureamidderivate |
DE10102322A1 (de) * | 2001-01-19 | 2002-07-25 | Merck Patent Gmbh | Phenylderivate |
DE60221505D1 (de) | 2001-03-30 | 2007-09-13 | Millennium Pharm Inc | FAKTOR Xa BENZAMIDIN INHIBITOREN |
US7312235B2 (en) * | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
-
2003
- 2003-02-28 DE DE10308907A patent/DE10308907A1/de not_active Withdrawn
-
2004
- 2004-01-30 KR KR1020057015881A patent/KR20050105493A/ko not_active Application Discontinuation
- 2004-01-30 DE DE502004011365T patent/DE502004011365D1/de not_active Expired - Lifetime
- 2004-01-30 MX MXPA05009002A patent/MXPA05009002A/es not_active Application Discontinuation
- 2004-01-30 CA CA002517391A patent/CA2517391A1/en not_active Abandoned
- 2004-01-30 JP JP2006501655A patent/JP2006519188A/ja active Pending
- 2004-01-30 AT AT04706669T patent/ATE473217T1/de not_active IP Right Cessation
- 2004-01-30 EP EP04706669A patent/EP1597244B1/de not_active Expired - Lifetime
- 2004-01-30 CN CNA2004800054434A patent/CN1753882A/zh active Pending
- 2004-01-30 US US10/547,130 patent/US7427618B2/en not_active Expired - Fee Related
- 2004-01-30 BR BRPI0407865-9A patent/BRPI0407865A/pt not_active Application Discontinuation
- 2004-01-30 AU AU2004215708A patent/AU2004215708B2/en not_active Ceased
- 2004-01-30 WO PCT/EP2004/000817 patent/WO2004076429A1/de active Application Filing
- 2004-01-30 PL PL377531A patent/PL377531A1/pl unknown
- 2004-02-27 AR ARP040100613A patent/AR043413A1/es not_active Application Discontinuation
-
2005
- 2005-09-27 ZA ZA200507818A patent/ZA200507818B/en unknown
Also Published As
Publication number | Publication date |
---|---|
ATE473217T1 (de) | 2010-07-15 |
WO2004076429A1 (de) | 2004-09-10 |
DE10308907A1 (de) | 2004-09-09 |
MXPA05009002A (es) | 2005-10-18 |
KR20050105493A (ko) | 2005-11-04 |
PL377531A1 (pl) | 2006-02-06 |
CA2517391A1 (en) | 2004-09-10 |
EP1597244A1 (de) | 2005-11-23 |
US7427618B2 (en) | 2008-09-23 |
ZA200507818B (en) | 2007-02-28 |
CN1753882A (zh) | 2006-03-29 |
DE502004011365D1 (de) | 2010-08-19 |
US20060084648A1 (en) | 2006-04-20 |
AU2004215708A1 (en) | 2004-09-10 |
BRPI0407865A (pt) | 2006-03-01 |
EP1597244B1 (de) | 2010-07-07 |
AU2004215708B2 (en) | 2010-03-11 |
JP2006519188A (ja) | 2006-08-24 |
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Legal Events
Date | Code | Title | Description |
---|---|---|---|
FB | Suspension of granting procedure | ||
FA | Abandonment or withdrawal | ||
FB | Suspension of granting procedure |