AR066475A1 - Compuestos nitrogenados condensados, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de los mismos particularmente, en el tratamiento del dolor y/o la vejiga hiperactiva. - Google Patents
Compuestos nitrogenados condensados, composiciones farmaceuticas que los contienen, metodo de preparacion y uso de los mismos particularmente, en el tratamiento del dolor y/o la vejiga hiperactiva.Info
- Publication number
- AR066475A1 AR066475A1 ARP080101934A ARP080101934A AR066475A1 AR 066475 A1 AR066475 A1 AR 066475A1 AR P080101934 A ARP080101934 A AR P080101934A AR P080101934 A ARP080101934 A AR P080101934A AR 066475 A1 AR066475 A1 AR 066475A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- pyrrolo
- pyrimidin
- dihydro
- cycloalkyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title 1
- 229910017464 nitrogen compound Inorganic materials 0.000 title 1
- 150000002830 nitrogen compounds Chemical class 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 13
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 125000000623 heterocyclic group Chemical group 0.000 abstract 11
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 abstract 5
- 125000000041 C6-C10 aryl group Chemical group 0.000 abstract 5
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 4
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 abstract 3
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 abstract 3
- 125000006719 (C6-C10) aryl (C1-C6) alkyl group Chemical group 0.000 abstract 3
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- -1 methoxy, ethoxy Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 125000004043 oxo group Chemical group O=* 0.000 abstract 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 125000001831 (C6-C10) heteroaryl group Chemical group 0.000 abstract 1
- IBMLYCWUODNPQH-UHFFFAOYSA-N 2,4-dianilino-6-phenyl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound O=C1N(C=2C=CC=CC=2)CC(C(=N2)NC=3C=CC=CC=3)=C1N=C2NC1=CC=CC=C1 IBMLYCWUODNPQH-UHFFFAOYSA-N 0.000 abstract 1
- CGGWAVHWIKLVAB-UHFFFAOYSA-N 2,4-dimorpholin-4-yl-6-phenyl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound O=C1N(C=2C=CC=CC=2)CC2=C1N=C(N1CCOCC1)N=C2N1CCOCC1 CGGWAVHWIKLVAB-UHFFFAOYSA-N 0.000 abstract 1
- QCPCEZGIVYJBIX-UHFFFAOYSA-N 2-(2,4-dimorpholin-4-yl-7-oxo-5H-pyrrolo[3,4-d]pyrimidin-6-yl)acetic acid Chemical compound O=C1N(CC(=O)O)CC2=C1N=C(N1CCOCC1)N=C2N1CCOCC1 QCPCEZGIVYJBIX-UHFFFAOYSA-N 0.000 abstract 1
- QZGARANSYKTBDC-UHFFFAOYSA-N 2-amino-4-anilino-5,6-dihydropyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C(N)=NC=2C(=O)NCC=2C=1NC1=CC=CC=C1 QZGARANSYKTBDC-UHFFFAOYSA-N 0.000 abstract 1
- VXLXUJZNOAHCHX-UHFFFAOYSA-N 2-anilino-4-(4-hydroxyanilino)-6-phenyl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound C1=CC(O)=CC=C1NC1=NC(NC=2C=CC=CC=2)=NC2=C1CN(C=1C=CC=CC=1)C2=O VXLXUJZNOAHCHX-UHFFFAOYSA-N 0.000 abstract 1
- GURRVPHOIBFMGX-UHFFFAOYSA-N 2-anilino-5-(dimethylaminomethylidene)-6-phenyl-4-piperidin-1-ylpyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C(N2CCCCC2)=C2C(=CN(C)C)N(C=3C=CC=CC=3)C(=O)C2=NC=1NC1=CC=CC=C1 GURRVPHOIBFMGX-UHFFFAOYSA-N 0.000 abstract 1
- YUYTYNNYSUUASP-UHFFFAOYSA-N 2-anilino-6-phenyl-4-piperidin-1-yl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound O=C1N(C=2C=CC=CC=2)CC(C(=N2)N3CCCCC3)=C1N=C2NC1=CC=CC=C1 YUYTYNNYSUUASP-UHFFFAOYSA-N 0.000 abstract 1
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- CPNSTJAAYBDJOJ-UHFFFAOYSA-N 4,5-diamino-2-piperidin-1-ylpyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C(N)=C2C(N)=NC(=O)C2=NC=1N1CCCCC1 CPNSTJAAYBDJOJ-UHFFFAOYSA-N 0.000 abstract 1
- BNXMFXHWNIQJDY-UHFFFAOYSA-N 4,5-diamino-2-pyrrolidin-1-ylpyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C(N)=C2C(N)=NC(=O)C2=NC=1N1CCCC1 BNXMFXHWNIQJDY-UHFFFAOYSA-N 0.000 abstract 1
- XWWXTDVQJLFDFV-UHFFFAOYSA-N 4-(2-aminoanilino)-5-imino-6-propyl-2-pyrrolidin-1-ylpyrrolo[3,4-d]pyrimidin-7-one Chemical compound O=C1N(CCC)C(=N)C2=C1N=C(N1CCCC1)N=C2NC1=CC=CC=C1N XWWXTDVQJLFDFV-UHFFFAOYSA-N 0.000 abstract 1
- DKMPIQLANQBSAT-UHFFFAOYSA-N 4-(2-chloroethylamino)-6-phenyl-2-piperidin-1-yl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound C1C=2C(NCCCl)=NC(N3CCCCC3)=NC=2C(=O)N1C1=CC=CC=C1 DKMPIQLANQBSAT-UHFFFAOYSA-N 0.000 abstract 1
- RRLPSESHUJLSNV-UHFFFAOYSA-N 4-anilino-2-(4-methoxyanilino)-6-(4-methoxyphenyl)-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound C1=CC(OC)=CC=C1NC(N=C1NC=2C=CC=CC=2)=NC2=C1CN(C=1C=CC(OC)=CC=1)C2=O RRLPSESHUJLSNV-UHFFFAOYSA-N 0.000 abstract 1
- ILLWQROLXQJVLG-UHFFFAOYSA-N 4-anilino-6-(4-methoxyphenyl)-2-morpholin-4-yl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound C1=CC(OC)=CC=C1N1C(=O)C(N=C(N=C2NC=3C=CC=CC=3)N3CCOCC3)=C2C1 ILLWQROLXQJVLG-UHFFFAOYSA-N 0.000 abstract 1
- WDQHPGFOJZDBTR-UHFFFAOYSA-N 4-anilino-6-(4-methoxyphenyl)-2-piperidin-1-yl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound C1=CC(OC)=CC=C1N1C(=O)C(N=C(N=C2NC=3C=CC=CC=3)N3CCCCC3)=C2C1 WDQHPGFOJZDBTR-UHFFFAOYSA-N 0.000 abstract 1
- CQBVOMZAZMYVKM-UHFFFAOYSA-N 4-anilino-6-butyl-2-(butylamino)-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C(NCCCC)=NC=2C(=O)N(CCCC)CC=2C=1NC1=CC=CC=C1 CQBVOMZAZMYVKM-UHFFFAOYSA-N 0.000 abstract 1
- WNWVKZTYMQWFHE-UHFFFAOYSA-N 4-ethylmorpholine Chemical group [CH2]CN1CCOCC1 WNWVKZTYMQWFHE-UHFFFAOYSA-N 0.000 abstract 1
- HQIUVIJMAFBZCE-UHFFFAOYSA-N 5-[2-[4-[4-(4-chloroanilino)-7-oxo-6-propan-2-yl-5h-pyrrolo[3,4-d]pyrimidin-2-yl]piperazin-1-yl]-2-oxoethyl]imidazolidine-2,4-dione Chemical compound O=C1N(C(C)C)CC2=C1N=C(N1CCN(CC1)C(=O)CC1C(NC(=O)N1)=O)N=C2NC1=CC=C(Cl)C=C1 HQIUVIJMAFBZCE-UHFFFAOYSA-N 0.000 abstract 1
- XUQJFFZXBMLQAP-UHFFFAOYSA-N 5-amino-2-piperidin-1-yl-4-(propylamino)pyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C=2C(=O)N=C(N)C=2C(NCCC)=NC=1N1CCCCC1 XUQJFFZXBMLQAP-UHFFFAOYSA-N 0.000 abstract 1
- DEJGHFKEECGAPD-UHFFFAOYSA-N 5-amino-4-(propylamino)-2-pyrrolidin-1-ylpyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C=2C(=O)N=C(N)C=2C(NCCC)=NC=1N1CCCC1 DEJGHFKEECGAPD-UHFFFAOYSA-N 0.000 abstract 1
- BDBSQSXJHWQFNH-UHFFFAOYSA-N 5-amino-4-piperidin-1-yl-2-pyrrolidin-1-ylpyrrolo[3,4-d]pyrimidin-7-one Chemical compound C=12C(N)=NC(=O)C2=NC(N2CCCC2)=NC=1N1CCCCC1 BDBSQSXJHWQFNH-UHFFFAOYSA-N 0.000 abstract 1
- ZNSNEWNOEGDDAI-UHFFFAOYSA-N 5-imino-6-propyl-4-(propylamino)-2-pyrrolidin-1-ylpyrrolo[3,4-d]pyrimidin-7-one Chemical compound N=1C=2C(=O)N(CCC)C(=N)C=2C(NCCC)=NC=1N1CCCC1 ZNSNEWNOEGDDAI-UHFFFAOYSA-N 0.000 abstract 1
- PFCXLNRXHKDQIV-UHFFFAOYSA-N 6-(2-hydroxyethyl)-2,4-di(piperidin-1-yl)-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound O=C1N(CCO)CC2=C1N=C(N1CCCCC1)N=C2N1CCCCC1 PFCXLNRXHKDQIV-UHFFFAOYSA-N 0.000 abstract 1
- OLCOZECKMWCLNV-UHFFFAOYSA-N 6-benzyl-2,4-dimorpholin-4-yl-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound C1C(C(=NC(=N2)N3CCOCC3)N3CCOCC3)=C2C(=O)N1CC1=CC=CC=C1 OLCOZECKMWCLNV-UHFFFAOYSA-N 0.000 abstract 1
- AAHCHOHXTXNJAU-UHFFFAOYSA-N 6-phenyl-2,4-di(piperidin-1-yl)-5h-pyrrolo[3,4-d]pyrimidin-7-one Chemical compound O=C1N(C=2C=CC=CC=2)CC2=C1N=C(N1CCCCC1)N=C2N1CCCCC1 AAHCHOHXTXNJAU-UHFFFAOYSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- JHSUWHZTDYOHMS-UHFFFAOYSA-N n-(7-oxo-6-phenyl-4-piperidin-1-yl-5h-pyrrolo[3,4-d]pyrimidin-2-yl)-n-phenylbenzamide Chemical compound C=1C=CC=CC=1C(=O)N(C=1N=C(C=2CN(C(=O)C=2N=1)C=1C=CC=CC=1)N1CCCCC1)C1=CC=CC=C1 JHSUWHZTDYOHMS-UHFFFAOYSA-N 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000000286 phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 abstract 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61P13/10—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
- 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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
-
- 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
- A61P25/22—Anxiolytics
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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
- 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
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Psychology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Cardiology (AREA)
- Epidemiology (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Reivindicacion 1: Un compuesto de formula 1, una sal farmacéuticamente aceptable del mismo, un diastereomero, un enantiomero, o una mezcla del mismo, donde R1 y R2 son independientemente seleccionados de hidrogeno, alquiI C1-6-C(=O)-, alquil C1-6,alquenil C2-6, cicloalquil C3-7, cicloalquil C3-7-4alquil C1-6, cicloalquil C3-7 fusionado con un fenil, cicloalquil C3-7 fusionado con un fenil y heteroaril C2-6, heterociclil C1-14, heterociclil C1-14-alquiI C1-6, aril C6-10, aril C6-10-alquiI C1-6, o R1 y R2 juntos con el nitrogeno unido a estos forman un heterociclil C2-9; donde dichos alquiI C1-6-C(=O)-, alquil C1-6, alquenil C2-6, cicloalquil C3-7, cicloalquil C3-7-4alquil C1-6, cicloalquil C3-7 fusionado con un fenil, heterociclil C1-14, heterociclil C1-14-alquiI C1-6, aril C6-10, aril C6-10-alquiI C1-6 y heterociclil C2-9 son opcionalmente sustituidos por uno o más grupos seleccionados de, halogeno, ciano, nitro, alcoxi C1-6, haloalcoxi C1-4, alquil C1-6, alquil C1-6halogenado, cicioalquil C3-6, cicloalcoxi C3-6, cicloalquil C3-6-alcoxi C1-4, -(CH2)m-C(=O)NR7R8, -(CH2)m-S(=O)2NR7R8, -(CH2)mNH- C(=O)NR7R8, -(CH2)m-N(R7)C(=O)R8, -(CH2)m-N(R7)C(=O)-OR8, -(CH2)m-C(=O)-OR7, -(CH2)m-C(=O)R7, -(CH2)m-S(=O)2R7, -(CH2)m-S(=O)R7, -(CH2)m-SR7, -(CH2)m-O-C(=O)-R7, -(CH2)m-OR7, -(CH2)m-NR7R8, hidroxi, heterociclil C1-14-alquil C0-4, fenil, bencil, feniletil, donde dichos heterociclil C1-14-alquil C0-4, fenil, bencil o fenetil son opcionalmente sustituido por uno o másgrupos seleccionados de halogeno, ciano, nitro, oxo, alcoxi C1-6, haloalcoxi C1-4, alquil C1-6, alquil C1-6 halogenado, cicloalquil C3-6, cicloalcoxi C3-6, -(CH2)m-C(=O)NR7R8, -C(=O)-(CH2)m-NR7R8, -(CH2)m-S(=O)2NR7R8, -(CH2)mNH-C(=O)NR7R8, -(CH2)m-N(R7)C(=O)R8, -(CH2)m-N(R7)C(=O)-OR8, -(CH2)m-C(=O)-OR7, -(CH2)m-C(=O)R7, -(CH2)m-S(=O)2R7, -(CH2)m-S(=O)R7, -(CH2)m-SR7, -(CH2)m-O-C(=O)-R7, -(CH2)m-OR7, -(CH2)m-NR7R8 e hidroxi; R3 y R4 son independientemente seleccionados de hidrogeno, alquil C1-6, alquenil C2-6, cicloalquil C3-8, cicloalquil C3-8-alquil C1-6, aril C6-10, aril C6-10-alquiI C1-6, heterociclil C3-6 y heterociclil C3-6-alquiI C1-6; o R3 y R4 juntos con el nitrogeno unido a estos forman un heterociclil C2-9; donde dichos alquilC1-6, alquenil C2-6, cicloalquil C3-8, cicloalquil C3-8-alquil C1-6, aril C6-10, aril C6-10-alquiI C1-6, heterociclil C3-6, heterociclil C3-6-alquiI C1-6 y heterociclil C2-9 son opcionalmente sustituidos por uno o más grupos seleccionados de alquilC1-6, alquil C1-6 halogenado, carboxi, halogeno, ciano, nitro, oxo, alcoxi C1-4, haloalcoxi C1-4, hidroxi, cicloalquil C3-6-alcoxi C1-4, heterocicloalquil C3-6, -(CH2)m-C(=O)NR7R8, -C(=O)-(CH2)m-NR7R8, -(CH2)m-S(=O)2NR7R8, -(CH2)mNH-C(=O)NR7R8, -(CH2)m-N(R7)C(=O)R8, -(CH2)m-N(R7)C(=O)-OR8, -(CH2)m-C(=O)-OR7, -(CH2)m-C(=O)R7, -(CH2)m-S(=O)2R7, -(CH2)m-O-C(=O)-R7, -(CH2)m-OR7, y -(CH2)m-NR7R8; R5 es seleccionado de hidrogeno y alquil C1-6, cicloalquil C3-7, heterociclil C1-6, heteroaril yaril C6-10, son opcionalmente sustituidos con uno o más grupos seleccionados de OH, alcoxi C1-4, alcoxi C1-4 halogenado, y halogeno; R7 y R8 son independientemente seleccionados a partir de -H, alquil C1-6, aril C6-10, heterociclil C1-5, ycicloalquil C3-6-alquil C0-4, donde dichos alquil C1-6, aril C6-10, heterociclil C1-5, y cicloalquil C3-6-alquil C0-4 son opcionalmente sustituidos con uno o más grupos seleccionados de -OH, metoxi, etoxi y halogeno; y m es 0, 1, 2 o 3, con lacondicion de que al menos uno de R1, R2, R3 y R4 no sea hidrogeno con la condicion adicional de que el compuesto no sea seleccionado de 5-[2-(4-{4-[(4-clorofenil)amino]-6-isopropil-7-oxo-6,7-dihidro-5H-pirrolo[3,4-d]-pirimidin-2-il}piperazin-1-il)-2-oxoetil]imidazolidina-2,4-diona; 2-amino-4-anilino-5,6-dihidro-7H-pirrolo[3,4-d]pirimidin-7-ona; 1-[4-[4-clorofenil)amino]-6,7-dihidro-6-(1-metiletil)-7-oxo-5H-pirrolo[3,4-d]pirimidin-2-il]-4-[2-(hidroxiimino)-1-oxopropil]-piperazina; 4-[(4-clorofenil)amino]-5,6-dihidro-2-(4-morfolinil)-6-[2-(4-morfolinil)etil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 4-[(2-aminofenil)amino]-5,6-dihidro-5-imino-6-propil-2-(1-pirrolidinil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 5,6-dihidro-5-imino-6-propil-4-(propilamino)-2-(1-pirrolidinil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 5-amino-2-(1-piperidinil)-4-(propilamino)-7H-pirrolo[3,4-d]pirimidin-7-ona; 4,5-diamino-2-(1-piperidinil)-7H-Pirrolo[3,4-d]pirimidin-7-ona; 5-amino-4-(1-piperidinil)-2-(1-pirrolidinil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 5-amino-4-(propilamino)-2-(1-pirrolidinil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 4,5-diamino-2-(1-pirrolidinil)-7H-pirrolo[3,4-d]pirimidin-7-ona; N-[6,7-dihidro-7-oxo-6-fenil-4-(1-piperidinil)-5H-pirrolo[3,4-d]pirimidin-2-il]-N-fenil- benzamida; 5-[(dimetilamino)metileno]-5,6-dihidro-6-fenil-2-(fenilamino)-4-(1-piperidinil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 2,4-bis(dimetilamino)-5,6-dihidro-6-fenil-7H-pirrolo[3,4-d)pirimidin-7-ona; 5,6-dihidro-6-fenil-2-(fenilamino)-4-(1-piperidinil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 5,6-dihidro-6-metil-2,4-di-1-piperidinil-7H-pirrolo[3,4-d}pirimidin-7-ona; 4-anilino-6-butil-2-(butilamino)-5,6-dihidro-7H-pirrolo[3,4-d]pirimidin-7-ona; 4-anilino-2-p-anisidino-5,6-dihidro-6-(p-metoxifenil)-7H-pirrolo[3,4-d]pirimidin-7-ona; 2-anilino-5,6-dihidro-4-(p-hidroxianilino)-6-fenil-7H-pirrolo[3,4-d]pirimidin-7-ona; 2,4-dianilino-5,6-dihidro-6-fenil-7H-pirrolo[3,4-d]pirimidin-7-ona; 4-[(2-cloroetil)amino]-5,6-dihidro-6-fenil-2-piperidino-7H-pirrolo[3,4-d]pirimidin-7-ona; 4-anilino-5,6-dihidro-6-(p-metoxifenil)-2-morfolino-7H-pirrolo[3,4-d]pirimidin-7-ona; 4-anilino-5,6-dihidro-6-(p-metoxifenil)-2-piperidino-7H-pirrolo[3,4-d]pirimidin-7-ona; 2-hidroxietil éster del ácido 5,7-dihidro-2,4-dimorfolino-7-oxo-6H-pirrolo[3,4-d]pirimidina-6-acético; 6-bencil-5,6-dihidro-2,4-dimorfolino-7H-pirrolo[3,4-d]pirimidin-7-ona; 5,6-dihidro-2,4-dimorfolino-6-fenil-7H-pirrolo[3,4-d]pirimidin-7-ona; 5,6-dihidro-6-(2-hidroxietil)-2,4-dipiperidino-7H-pirrolo[3,4-d]pirimidin-7-ona; y 5,6-dihidro-6-fenil-2,4-di-1-piperidinil-7H-pirrolo[3,4-d]pirimidin-7-ona.
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| US91658807P | 2007-05-08 | 2007-05-08 |
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- 2008-05-07 KR KR1020097025526A patent/KR20100017688A/ko not_active Withdrawn
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| Publication number | Publication date |
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| PE20090816A1 (es) | 2009-07-25 |
| JP2010526138A (ja) | 2010-07-29 |
| CL2008001335A1 (es) | 2008-11-14 |
| US20090099195A1 (en) | 2009-04-16 |
| CA2686707A1 (en) | 2008-11-13 |
| MX2009011997A (es) | 2009-11-19 |
| TW200846001A (en) | 2008-12-01 |
| RU2009140469A (ru) | 2011-06-20 |
| CN101687875A (zh) | 2010-03-31 |
| KR20100017688A (ko) | 2010-02-16 |
| BRPI0811436A2 (pt) | 2014-12-16 |
| EP2155751A1 (en) | 2010-02-24 |
| UY31068A1 (es) | 2009-01-05 |
| AU2008246351A1 (en) | 2008-11-13 |
| WO2008136756A1 (en) | 2008-11-13 |
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