AR043833A1 - Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticas - Google Patents
Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticasInfo
- Publication number
- AR043833A1 AR043833A1 ARP040101115A ARP040101115A AR043833A1 AR 043833 A1 AR043833 A1 AR 043833A1 AR P040101115 A ARP040101115 A AR P040101115A AR P040101115 A ARP040101115 A AR P040101115A AR 043833 A1 AR043833 A1 AR 043833A1
- Authority
- AR
- Argentina
- Prior art keywords
- hal
- atoms
- coo
- derivatives
- cona
- Prior art date
Links
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical class C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 2
- 108010074860 Factor Xa Proteins 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001435 Thromboembolism Diseases 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000004429 atom Chemical group 0.000 abstract 1
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000000896 monocarboxylic acid group Chemical group 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
- 150000003839 salts Chemical class 0.000 abstract 1
- 229920006395 saturated elastomer Polymers 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
- 238000011282 treatment Methods 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
-
- 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
-
- 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
- A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
-
- 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
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/04—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
-
- 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
- C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
- C07D453/06—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing isoquinuclidine ring systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Rheumatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Los compuestos de la fórmula (1) en donde R es H, A, A-CO-, Hal, -C:::C-H, -C:::C-A o -C:::C-C(=O)-A; R1es H, =O, Hal, A, OH, OA, A-COO-, Ph-(CH2)n-COO-, cicloalquil-(CH2)n-COO-, A-CONH-, A-CONA-, Ph-CONA-, N3, NH2, NO2, CN, COOH, COOA, CO-NH2, CONHA, CON(A)2, O-alilo, O-propargilo, O-bencilo, =N-OH, =N-OA o =CF2; Ph es fenilo insustituido o mono, di o trisustituido con A, OA o Hal; R2 es H, Hal o A; R3n es un heterociclo monocíclico saturado, insaturado o aromático con 1 a 4 átomos de N, O y/o S, que puede estar insustituido o mono, di o trisustituido con Hal, A, OA, CN, (CH2)nOH, (CH2)nHal, NR4R5, =NH, =N-OH, =N-OA y/o el O del carbonilo (=O), o CONR4R5; R4, R5 son, de modo independiente entre sí, H o A, R4 y R5 también son juntos una cadena de alquileno con 3, 4 o 5 átomos de C que también puede estar sustituida con A, Hal, OA y/o el O del carbonilo (=CO); A es alquilo no ramificado, ramificado o cíclico con 1-10 átomos de C, donde también 1-7 átomos de H pueden estar reemplazados por F y/o Cl; Hal es F, Cl, Br o I; n es 0, 1, 2, 3, o 4; así como sus derivados, sales, solvatos y estereoisómeros de utilidad farmacéutica, incluyendo sus mezclas en todas las proporciones. Son inhibidores del factor de coagulación Xa y pueden emplearse para la profilaxis y/o la terapia de enfermedades tromboembólicas y para el tratamiento de tumores.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10315377A DE10315377A1 (de) | 2003-04-03 | 2003-04-03 | Carbonylverbindungen |
| DE2003129295 DE10329295A1 (de) | 2003-06-30 | 2003-06-30 | Carbonylverbindungen |
| DE10336570A DE10336570A1 (de) | 2003-08-08 | 2003-08-08 | Azaprolinderivate |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR043833A1 true AR043833A1 (es) | 2005-08-17 |
Family
ID=33135448
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP040101115A AR043833A1 (es) | 2003-04-03 | 2004-04-02 | Derivados de 1,2 diazol. metodo de preparacion y composiciones farmaceuticas |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US7557102B2 (es) |
| EP (1) | EP1608645B1 (es) |
| JP (1) | JP4624982B2 (es) |
| KR (1) | KR20050109617A (es) |
| AR (1) | AR043833A1 (es) |
| AT (1) | ATE361296T1 (es) |
| AU (1) | AU2004226281B2 (es) |
| BR (1) | BRPI0408444A (es) |
| CA (1) | CA2520894C (es) |
| DE (1) | DE502004003688D1 (es) |
| ES (1) | ES2285444T3 (es) |
| MX (1) | MXPA05010445A (es) |
| PL (1) | PL377864A1 (es) |
| WO (1) | WO2004087696A1 (es) |
Families Citing this family (24)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10358814A1 (de) | 2003-12-16 | 2005-07-21 | Merck Patent Gmbh | Prolinylarylacetamide |
| DE102004016605A1 (de) * | 2004-04-03 | 2005-10-20 | Merck Patent Gmbh | Thiocarbamoylproline |
| WO2007054453A2 (en) * | 2005-11-11 | 2007-05-18 | F. Hoffmann-La Roche Ag | Carbocyclic fused cyclic amines as inhibitors of the coagulation factor xa |
| KR101020440B1 (ko) | 2005-11-16 | 2011-03-08 | 에프. 호프만-라 로슈 아게 | 응고 인자 Ｘａ의 억제제로서의 피롤리딘 유도체 |
| US8673920B2 (en) * | 2009-05-06 | 2014-03-18 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9073882B2 (en) | 2010-10-27 | 2015-07-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9056859B2 (en) | 2010-10-29 | 2015-06-16 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| TW201249824A (en) * | 2011-03-09 | 2012-12-16 | Glaxosmithkline Llc | Peptide deformylase inhibitors |
| CA2844310A1 (en) | 2011-08-19 | 2013-02-28 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| TW201317213A (zh) | 2011-09-16 | 2013-05-01 | Merck Sharp & Dohme | 腎外髓質鉀通道抑制劑 |
| WO2013062900A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2013062892A1 (en) | 2011-10-25 | 2013-05-02 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2013066718A2 (en) | 2011-10-31 | 2013-05-10 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9108947B2 (en) | 2011-10-31 | 2015-08-18 | Merck Sharp & Dohme Corp. | Inhibitors of the Renal Outer Medullary Potassium channel |
| WO2013066714A1 (en) | 2011-10-31 | 2013-05-10 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9145368B2 (en) | 2011-12-15 | 2015-09-29 | Council Of Scientific & Industrial Research | Organocatalytic synthesis of chiral pyrazolidines and their analogues |
| WO2013090271A1 (en) | 2011-12-16 | 2013-06-20 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| AR092031A1 (es) | 2012-07-26 | 2015-03-18 | Merck Sharp & Dohme | Inhibidores del canal de potasio medular externo renal |
| EP2925322B1 (en) | 2012-11-29 | 2018-10-24 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2014099633A2 (en) | 2012-12-19 | 2014-06-26 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| WO2014126944A2 (en) | 2013-02-18 | 2014-08-21 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| US9765074B2 (en) | 2013-03-15 | 2017-09-19 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
| EP3027625B1 (en) | 2013-07-31 | 2018-05-30 | Merck Sharp & Dohme Corp. | Spiro-fused derivatives of piperidine useful for the treatment of inter alia hypertension and acute or chronic heart failure |
| WO2015065866A1 (en) | 2013-10-31 | 2015-05-07 | Merck Sharp & Dohme Corp. | Inhibitors of the renal outer medullary potassium channel |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2001245353A1 (en) * | 2000-02-29 | 2001-09-12 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| DE10113402A1 (de) * | 2001-03-20 | 2002-09-26 | Merck Patent Gmbh | Biurethanderivate |
| US6566357B1 (en) * | 2001-09-20 | 2003-05-20 | The Procter & Gamble Co. | Spirocyclic-6,7-dihydro-5H-pyrazolo[1,2-a]pyrazol-1-ones which control inflammatory cytokines |
-
2004
- 2004-03-09 PL PL377864A patent/PL377864A1/pl not_active Application Discontinuation
- 2004-03-09 JP JP2006504604A patent/JP4624982B2/ja not_active Expired - Fee Related
- 2004-03-09 DE DE502004003688T patent/DE502004003688D1/de not_active Expired - Lifetime
- 2004-03-09 CA CA2520894A patent/CA2520894C/en not_active Expired - Fee Related
- 2004-03-09 MX MXPA05010445A patent/MXPA05010445A/es not_active Application Discontinuation
- 2004-03-09 KR KR1020057018641A patent/KR20050109617A/ko not_active Withdrawn
- 2004-03-09 AT AT04718641T patent/ATE361296T1/de not_active IP Right Cessation
- 2004-03-09 EP EP04718641A patent/EP1608645B1/de not_active Expired - Lifetime
- 2004-03-09 AU AU2004226281A patent/AU2004226281B2/en not_active Ceased
- 2004-03-09 US US10/551,559 patent/US7557102B2/en not_active Expired - Fee Related
- 2004-03-09 WO PCT/EP2004/002407 patent/WO2004087696A1/de not_active Ceased
- 2004-03-09 BR BRPI0408444-6A patent/BRPI0408444A/pt not_active IP Right Cessation
- 2004-03-09 ES ES04718641T patent/ES2285444T3/es not_active Expired - Lifetime
- 2004-04-02 AR ARP040101115A patent/AR043833A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004087696A1 (de) | 2004-10-14 |
| KR20050109617A (ko) | 2005-11-21 |
| AU2004226281B2 (en) | 2010-06-10 |
| CA2520894C (en) | 2013-02-05 |
| PL377864A1 (pl) | 2006-02-20 |
| AU2004226281A1 (en) | 2004-10-14 |
| MXPA05010445A (es) | 2005-11-04 |
| JP4624982B2 (ja) | 2011-02-02 |
| ES2285444T3 (es) | 2007-11-16 |
| US7557102B2 (en) | 2009-07-07 |
| EP1608645B1 (de) | 2007-05-02 |
| US20060183742A1 (en) | 2006-08-17 |
| CA2520894A1 (en) | 2004-10-14 |
| BRPI0408444A (pt) | 2006-04-04 |
| EP1608645A1 (de) | 2005-12-28 |
| JP2006522038A (ja) | 2006-09-28 |
| DE502004003688D1 (de) | 2007-06-14 |
| ATE361296T1 (de) | 2007-05-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |