AR035805A1 - Compuestos de dihidropirimidina ciano sustituidos - Google Patents
Compuestos de dihidropirimidina ciano sustituidosInfo
- Publication number
- AR035805A1 AR035805A1 ARP020101175A ARP020101175A AR035805A1 AR 035805 A1 AR035805 A1 AR 035805A1 AR P020101175 A ARP020101175 A AR P020101175A AR P020101175 A ARP020101175 A AR P020101175A AR 035805 A1 AR035805 A1 AR 035805A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- compounds
- heteroarylalkyl
- arylalkyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 8
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 4
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 3
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 230000036456 mitotic arrest Effects 0.000 abstract 2
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- 101100134922 Gallus gallus COR5 gene Proteins 0.000 abstract 1
- -1 OR7 Chemical group 0.000 abstract 1
- 125000002877 alkyl aryl group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 239000002246 antineoplastic agent Substances 0.000 abstract 1
- 125000005418 aryl aryl group Chemical group 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 125000001188 haloalkyl group Chemical group 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 150000002431 hydrogen Chemical class 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 230000001939 inductive effect Effects 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 239000012453 solvate Substances 0.000 abstract 1
- 125000005420 sulfonamido group Chemical group S(=O)(=O)(N*)* 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/20—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
- C07D239/22—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to ring carbon atoms
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- 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
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- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
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- 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
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
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- 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
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
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- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
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- 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]
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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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
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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
- A61P9/06—Antiarrhythmics
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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
- 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
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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
- A61P9/14—Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
- C07D211/90—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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- 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
- C07D401/10—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 carbon chain containing aromatic rings
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- 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
- C07D403/10—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 carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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- 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
- C07D413/10—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 carbon chain containing aromatic rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Oncology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Urology & Nephrology (AREA)
- Physical Education & Sports Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Immunology (AREA)
- Communicable Diseases (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- Psychology (AREA)
- Rheumatology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Gastroenterology & Hepatology (AREA)
- AIDS & HIV (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Transplantation (AREA)
- Biotechnology (AREA)
- Tropical Medicine & Parasitology (AREA)
Abstract
Compuestos de la fórmula (1) sus enantiómeros, diastereómeros, sales farmacéuticamente aceptables, prodrogas y solvatos del mismo, donde R1 está seleccionado del grupo que consiste en hidrógeno, alquilo y cicloalquilo; Y1, Y2, Y3, Y4 e Y5 están independientemente seleccionados del grupo que consiste en H, halógeno, alquilo inferior, O alquilo, O arilo, NH alquilo, NH arilo, N alquilalquilo, N alquilarilo, N arilarilo con la condición de que al menos uno de Y1, Y2, Y3, Y4 e Y5 sea arilo o heteroarilo; R4 está seleccionado del grupo que consiste en alquilo, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, CN, COR5, CO2R5 y CONR5R6; R5 y R6 están independientemente seleccionados del grupo que consiste en H, alquilo, haloalquilo, cicloalquilo, aminoalquilo, arilalquilo, cicloalquilalquilo, heteroarilalquilo y heterocicloalquilalquilo; Z está seleccionado del grupo que consiste en O, S y NR8; R8 está seleccionado del grupo que consiste en H, CN, sulfonamido, OR7, alquilo, cicloalquilo, arilo, arilalquilo, heterociclilo, heteroarilo y heteroarilalquilo; y R7 está seleccionado del grupo que consiste en H, alquilo, arilalquilo, cicloalquilalquilo, heterocicloalquilalquilo y heteroarilalquilo. Los compuestos de fórmula (1) inducen al paro mitótico y por ello son útiles como agentes anticancerígenos y para el tratamiento de otras enfermedades que pueden ser tratadas induciendo el paro mitótico.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US27995601P | 2001-03-29 | 2001-03-29 | |
| US10/104,382 US6900214B2 (en) | 2001-03-29 | 2002-03-22 | Cyano-substituted dihydropyrimidine compounds and their use to treat diseases |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035805A1 true AR035805A1 (es) | 2004-07-14 |
Family
ID=26801480
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020101175A AR035805A1 (es) | 2001-03-29 | 2002-04-02 | Compuestos de dihidropirimidina ciano sustituidos |
Country Status (24)
| Country | Link |
|---|---|
| US (1) | US6900214B2 (es) |
| EP (1) | EP1373223A4 (es) |
| JP (1) | JP2004529139A (es) |
| KR (1) | KR20030086328A (es) |
| CN (1) | CN1500082A (es) |
| AR (1) | AR035805A1 (es) |
| BG (1) | BG108195A (es) |
| BR (1) | BR0208353A (es) |
| CA (1) | CA2442484A1 (es) |
| CZ (1) | CZ20032643A3 (es) |
| EE (1) | EE200300473A (es) |
| HR (1) | HRP20030874A2 (es) |
| HU (1) | HUP0400341A3 (es) |
| IL (1) | IL157442A0 (es) |
| IS (1) | IS6966A (es) |
| MX (1) | MXPA03008635A (es) |
| NO (1) | NO20034301L (es) |
| NZ (1) | NZ527617A (es) |
| PE (1) | PE20020997A1 (es) |
| PL (1) | PL364005A1 (es) |
| RU (1) | RU2003131975A (es) |
| SK (1) | SK11072003A3 (es) |
| WO (1) | WO2002079169A1 (es) |
| YU (1) | YU75603A (es) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69734362T2 (de) | 1996-12-03 | 2006-07-20 | Sloan-Kettering Institute For Cancer Research | Synthese von epothilonen, zwischenprodukte dazu, analoga und verwendungen davon |
| US6809102B2 (en) | 2001-03-29 | 2004-10-26 | Bristol-Myers Squibb Company | Cyano-substituted dihydropyrimidine compounds and their use to treat diseases |
| PT1454903E (pt) * | 2001-12-11 | 2010-11-09 | Kyowa Hakko Kirin Co Ltd | Derivados de tiadiazolina para tratamento do cancro |
| ES2281692T3 (es) | 2002-08-23 | 2007-10-01 | Sloan-Kettering Institute For Cancer Research | Sintesis de epotilones, sus intermediarios, sus analogos y sus usos. |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| CA2522594C (en) | 2003-04-18 | 2012-01-24 | Kyowa Hakko Kogyo Co., Ltd. | Mitotic kinesin inhibitor |
| CN1802361A (zh) * | 2003-06-10 | 2006-07-12 | 协和发酵工业株式会社 | 噻二唑啉衍生物 |
| WO2005007124A2 (en) | 2003-07-23 | 2005-01-27 | Bristol-Myers Squibb Company | Substituted dihydropyrimidine inhibitors of calcium channel function |
| US7166603B2 (en) | 2003-07-23 | 2007-01-23 | Bristol-Myers Squibb Co. | Dihydropyrimidone inhibitors of calcium channel function |
| WO2005037799A1 (en) * | 2003-10-16 | 2005-04-28 | Cytokinetics, Inc. | Compounds, compositions, and methods |
| RU2447077C2 (ru) | 2004-08-18 | 2012-04-10 | Астразенека Аб | Энантиомеры выбранных конденсированных пиримидинов и их применение для лечения и предотвращения злокачественного новообразования |
| FR2883284A1 (fr) * | 2005-03-15 | 2006-09-22 | Commissariat Energie Atomique | Nouveaux derives dihydropyrimidines et leur utilisation comme agents anti-cancereux |
| CA2602559A1 (en) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | Agent for treatment of hematopoietic tumor |
| CA2602397A1 (en) * | 2005-03-22 | 2006-09-28 | Kyowa Hakko Kogyo Co., Ltd. | Therapeutic agent for solid tumor |
| WO2006137490A1 (ja) * | 2005-06-24 | 2006-12-28 | Kyowa Hakko Kogyo Co., Ltd. | 再狭窄治療剤 |
| DE102006002065B4 (de) * | 2006-01-16 | 2007-11-29 | Infineon Technologies Austria Ag | Kompensationsbauelement mit reduziertem und einstellbarem Einschaltwiderstand |
| EP2455456A1 (en) | 2010-11-22 | 2012-05-23 | Institut Curie | Use of kinesin inhibitors in HIV infection treatment and a method for screening them |
| BR112014003989A2 (pt) * | 2011-08-26 | 2017-06-13 | Sanford-Burnham Medical Res Inst | composto, composições e métodos para inibir a replicação do hiv-1 em paciente, para tratar pacientes infectados com hiv/aids e para profilaxia de pré-exposição para tratar paciente e para prevenir a transmissão de pessoa infectada para pessoa não infectada |
| CN105237465B (zh) * | 2015-11-13 | 2017-07-21 | 吉林大学 | 一种具有神经保护作用的化合物及医用用途 |
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| JPS422265Y1 (es) | 1965-10-21 | 1967-02-10 | ||
| US6211198B1 (en) | 1993-04-05 | 2001-04-03 | Synaptic Pharmaceutical Corporation | Dihydropyridines and new uses thereof |
| HUT77941A (hu) | 1994-11-16 | 1998-12-28 | Synaptic Pharmaceutical Corporation | Dihidropirimidinszármazékok és ezek alkalmazása |
| WO1997017969A1 (en) | 1995-11-16 | 1997-05-22 | Synaptic Pharmaceutical Corporation | Dihydropyrimidines and uses thereof |
| US6172066B1 (en) | 1996-05-16 | 2001-01-09 | Synaptic Pharmaceutical Corporation | Dihydropyrimidines and uses thereof |
| JP2000506904A (ja) | 1996-05-16 | 2000-06-06 | シナプティック・ファーマスーティカル・コーポレーション | ジヒドロピリミジン類およびその使用 |
| US6080760A (en) | 1997-06-18 | 2000-06-27 | Merck & Co., Inc. | Alpha 1A adrenergic receptor antagonists |
| EP1003511A1 (en) | 1997-06-18 | 2000-05-31 | Merck & Co., Inc. | ALPHA 1aADRENERGIC RECEPTOR ANTAGONISTS |
| AU1403099A (en) | 1997-11-14 | 1999-06-07 | Merck & Co., Inc. | Alpha-1a adrenergic receptor antagonists |
| US6346389B1 (en) | 1998-04-01 | 2002-02-12 | Yale University | Method for selectively modulating the interactions between survivin and tubulin |
| US6300084B1 (en) | 1998-10-08 | 2001-10-09 | The Regents Of The University Of California | Anti-mitotic agent screening process |
| GB9914258D0 (en) * | 1999-06-18 | 1999-08-18 | Celltech Therapeutics Ltd | Chemical compounds |
| AUPQ171999A0 (en) | 1999-07-20 | 1999-08-12 | University Of Sydney, The | Neurotropic virus transport |
| DE19935303A1 (de) | 1999-07-28 | 2001-02-08 | Aventis Pharma Gmbh | Oligonukleotide zur Inhibierung der Expression von humanem eg5 |
| US6617115B1 (en) | 1999-10-27 | 2003-09-09 | Cytokinetics, Inc. | Methods of screening for modulators of cell proliferation |
| ES2263501T3 (es) | 1999-10-27 | 2006-12-16 | Cytokinetics, Inc. | Procedimiento y composiciones que utilizan quinazolinonas. |
| US6284480B1 (en) | 2000-04-03 | 2001-09-04 | Cytokinetics, Inc. | Antifungal assay |
| US6809102B2 (en) | 2001-03-29 | 2004-10-26 | Bristol-Myers Squibb Company | Cyano-substituted dihydropyrimidine compounds and their use to treat diseases |
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2002
- 2002-03-22 US US10/104,382 patent/US6900214B2/en not_active Expired - Lifetime
- 2002-03-26 EP EP02731175A patent/EP1373223A4/en not_active Withdrawn
- 2002-03-26 NZ NZ527617A patent/NZ527617A/en unknown
- 2002-03-26 HU HU0400341A patent/HUP0400341A3/hu unknown
- 2002-03-26 CN CNA028074564A patent/CN1500082A/zh active Pending
- 2002-03-26 PL PL02364005A patent/PL364005A1/xx not_active Application Discontinuation
- 2002-03-26 WO PCT/US2002/009494 patent/WO2002079169A1/en not_active Ceased
- 2002-03-26 RU RU2003131975/04A patent/RU2003131975A/ru not_active Application Discontinuation
- 2002-03-26 HR HR20030874A patent/HRP20030874A2/xx not_active Application Discontinuation
- 2002-03-26 CA CA002442484A patent/CA2442484A1/en not_active Abandoned
- 2002-03-26 BR BR0208353-1A patent/BR0208353A/pt not_active IP Right Cessation
- 2002-03-26 JP JP2002577796A patent/JP2004529139A/ja not_active Withdrawn
- 2002-03-26 MX MXPA03008635A patent/MXPA03008635A/es unknown
- 2002-03-26 YU YU75603A patent/YU75603A/sh unknown
- 2002-03-26 KR KR10-2003-7012607A patent/KR20030086328A/ko not_active Withdrawn
- 2002-03-26 SK SK1107-2003A patent/SK11072003A3/sk unknown
- 2002-03-26 EE EEP200300473A patent/EE200300473A/xx unknown
- 2002-03-26 CZ CZ20032643A patent/CZ20032643A3/cs unknown
- 2002-03-26 IL IL15744202A patent/IL157442A0/xx unknown
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- 2002-04-02 AR ARP020101175A patent/AR035805A1/es unknown
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2003
- 2003-09-24 BG BG108195A patent/BG108195A/bg unknown
- 2003-09-24 IS IS6966A patent/IS6966A/is unknown
- 2003-09-26 NO NO20034301A patent/NO20034301L/no not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| NO20034301D0 (no) | 2003-09-26 |
| NO20034301L (no) | 2003-11-10 |
| IL157442A0 (en) | 2004-03-28 |
| JP2004529139A (ja) | 2004-09-24 |
| HUP0400341A2 (hu) | 2004-10-28 |
| EP1373223A1 (en) | 2004-01-02 |
| PL364005A1 (en) | 2004-11-29 |
| KR20030086328A (ko) | 2003-11-07 |
| BR0208353A (pt) | 2004-03-23 |
| YU75603A (sh) | 2006-05-25 |
| CN1500082A (zh) | 2004-05-26 |
| NZ527617A (en) | 2005-02-25 |
| CA2442484A1 (en) | 2002-10-10 |
| PE20020997A1 (es) | 2002-11-08 |
| BG108195A (bg) | 2004-07-30 |
| IS6966A (is) | 2003-09-24 |
| EE200300473A (et) | 2004-02-16 |
| SK11072003A3 (sk) | 2004-06-08 |
| US6900214B2 (en) | 2005-05-31 |
| HRP20030874A2 (en) | 2004-04-30 |
| MXPA03008635A (es) | 2004-02-23 |
| US20020143026A1 (en) | 2002-10-03 |
| HUP0400341A3 (en) | 2004-11-29 |
| RU2003131975A (ru) | 2005-05-10 |
| EP1373223A4 (en) | 2004-09-29 |
| WO2002079169A8 (en) | 2004-04-29 |
| WO2002079169A1 (en) | 2002-10-10 |
| CZ20032643A3 (en) | 2004-06-16 |
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