AR057107A2 - Uso de compuestos derivados de piperazina utiles como antagonistas ccr5, para la preparacion de medicamentos - Google Patents
Uso de compuestos derivados de piperazina utiles como antagonistas ccr5, para la preparacion de medicamentosInfo
- Publication number
- AR057107A2 AR057107A2 ARP060103794A ARP060103794A AR057107A2 AR 057107 A2 AR057107 A2 AR 057107A2 AR P060103794 A ARP060103794 A AR P060103794A AR P060103794 A ARP060103794 A AR P060103794A AR 057107 A2 AR057107 A2 AR 057107A2
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- group
- hydrogen
- phenyl
- independently selected
- Prior art date
Links
- 239000003814 drug Substances 0.000 title abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 title 2
- 102100035875 C-C chemokine receptor type 5 Human genes 0.000 title 1
- 101710149870 C-C chemokine receptor type 5 Proteins 0.000 title 1
- 239000005557 antagonist Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 22
- 229910052739 hydrogen Inorganic materials 0.000 abstract 9
- 239000001257 hydrogen Substances 0.000 abstract 8
- 150000002431 hydrogen Chemical group 0.000 abstract 5
- -1 -OSO2CF3 Chemical group 0.000 abstract 3
- 229910052736 halogen Inorganic materials 0.000 abstract 3
- 150000002367 halogens Chemical group 0.000 abstract 3
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 2
- 125000006163 5-membered heteroaryl group Chemical group 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 239000002777 nucleoside Substances 0.000 abstract 2
- 150000003833 nucleoside derivatives Chemical class 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 125000001424 substituent group Chemical group 0.000 abstract 2
- VSNHCAURESNICA-NJFSPNSNSA-N 1-oxidanylurea Chemical compound N[14C](=O)NO VSNHCAURESNICA-NJFSPNSNSA-N 0.000 abstract 1
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 abstract 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 abstract 1
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 108010032976 Enfuvirtide Proteins 0.000 abstract 1
- 241000725303 Human immunodeficiency virus Species 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 108010065805 Interleukin-12 Proteins 0.000 abstract 1
- 108010002350 Interleukin-2 Proteins 0.000 abstract 1
- IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 239000003443 antiviral agent Substances 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 239000003067 chemokine receptor CCR5 antagonist Substances 0.000 abstract 1
- 125000005982 diphenylmethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 abstract 1
- PEASPLKKXBYDKL-FXEVSJAOSA-N enfuvirtide Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(C)=O)[C@@H](C)O)[C@@H](C)CC)C1=CN=CN1 PEASPLKKXBYDKL-FXEVSJAOSA-N 0.000 abstract 1
- 229960002062 enfuvirtide Drugs 0.000 abstract 1
- 125000003983 fluorenyl group Chemical group C1(=CC=CC=2C3=CC=CC=C3CC12)* 0.000 abstract 1
- 125000004446 heteroarylalkyl group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- XSXHWVKGUXMUQE-UHFFFAOYSA-N osmium dioxide Inorganic materials O=[Os]=O XSXHWVKGUXMUQE-UHFFFAOYSA-N 0.000 abstract 1
- 239000000137 peptide hydrolase inhibitor Substances 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 229960000329 ribavirin Drugs 0.000 abstract 1
- HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000003003 spiro group Chemical group 0.000 abstract 1
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 abstract 1
- 125000001889 triflyl group Chemical group FC(F)(F)S(*)(=O)=O 0.000 abstract 1
Classifications
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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
-
- 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
-
- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
-
- 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
-
- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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]
-
- 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
-
- 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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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
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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
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/08—Antiallergic 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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- 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
- C07D211/06—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 no double bonds between ring members or between ring members and non-ring members
- C07D211/36—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 no 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D211/56—Nitrogen atoms
- C07D211/58—Nitrogen atoms attached in position 4
-
- 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
- C07D401/06—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 only aliphatic 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
- C07D401/10—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
-
- 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
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- C07D413/06—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 only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Biomedical Technology (AREA)
- Virology (AREA)
- Oncology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Communicable Diseases (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Uso de un antagonista CCR5 de la formula estructural (1) o una sal farmacéuticamente aceptable del mismo, en la cual R es R8-fenilo, R8-piridilo, R8-tiofenilo o R8-naftilo; R1 es hidrogeno o alquilo C1-6; R2 es heteroarilo de 6 miembros substituido con R9, R10 y R11; N-oxido de heteroarilo de 6 miembros substituido con R9, R10 y R11; heteroarilo de 5 miembros substituido con R12 y R13; naftilo; fluorenilo; difenilmetilo, grupo de formulas (2) o formula (3); heteroarilo R3 es hidrogeno, alquilo C1-6; alcoxi C1-6-alquilo C1-6, cicloalquilo C3-10, cicloalquilo C3-10-alquilo C1-6, R8-fenilo, R8-fenilalquilo C1-6, R8-naftilo, R8-naftilalquilo C1-6, R8-heteroarilo o R8-heteroarilo o R8-heteroarilalquilo C1-6; R4, R5, R7 y R13 están independientemente seleccionados del grupo que consiste en hidrogeno y alquilo C1-6; R6 es hidrogeno, alquilo C1-6 o alquenilo C2-6; R8 representa de 1 a 3 subtituyentes independientemente seleccionados del grupo que consiste en hidrogeno, halogeno, alquilo C1-6, alcoxi C1-6, -CF3, CF3O-, CH3C(O)-, -CN, CH3SO2-, CF3SO2-, R14-fenilo, R14-bencilo, CH3C(=NOCH3), CH3C(=NOCH2CH3), formula (4); -NH2, -NHCOCF3, -NHCONH(alquilo C1-6), -NHCO(C1-6 alquilo), -NHSO2(alquilo C1-6), heteroarilo de 5 miembros y formula (5) donde X es -O-, -NH- o -N(CH3)-; R9 y R10 están independientemente seleccionados del grupo que consiste en alquilo C1-6, halogeno, -NR17R18, -OH, -CF3, -OCH3, -O-acilo, -PCF3 y -Si(CH3)3; R11 es R9, hidrogeno, fenilo, -NO2, -CN, -CH2F, -CHO, -CH=NOR17, piridilo, N,-oxido de piridilo, pirimidinilo, pirazinilo, -N(R17)CONR18R19, -NHCONH(cloro-alquilo C1-6), NHCONH(cicloalquilo C3-10-alquilo C1-6), NHCOalquilo C1-6, -NHCOCF3, -NHSO2N(alquilo C1-6)2, -NHSO2alquilo C1-6, -N(SO2CF3)2, - NHCO2alquilo C1-6, cicloalquilo C3-10, -SR20, -SOR20, -SO2R20, -SO2NH(alquilo C1-6), -OSO2alquilo C1-6, -OSO2CF3, hidroxialquilo C1-6, CONR17R18, -CON(CH2CH2-O-CH3)2, -OCONHalquilo C1-6, -C=2R17, -Si(CH3)3 o -B(OC(CH3)2)2; R12 es alquilo C1-6, -NH2 o R14-fenilo; R14 representa de 1 a 3 substituyentes independientemente seleccionados del grupo que consiste en hidrogeno, alquilo C1-C6, -CF3, -CO2R17, -CN, alcoxi C1-6 y halogeno; R15 y R16 están independientemente seleccionados del grupo que consiste en hidrogeno alquilo C1-C6 o R15 y R16 conjuntamente son un grupo alquileno C2-C5 y con el carbono al cual están unidos forman un anillo espiro de 3 a 6 átomos de carbono; R17, R18 y R19 están independientemente seleccionados del grupo que consiste en H y alquilo C1-6; y R20 es alquilo C1-C6 o fenilo; y uno o más agentes antivirales seleccionados del grupo que consiste en inhibidores de retrotranscriptasa nucleosídica, inhibidores de retrotranscriptasa no nucleosídica, inhibidores de proteasa, hidroxiurea, ribavirina, IL-2, IL-12, pentafusida y Yissum N° 11607 para la preparacion de un medicamento para tratar el virus de inmunodeficiencia humana a un humano que necesite dicho tratamiento.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30522699A | 1999-05-04 | 1999-05-04 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR057107A2 true AR057107A2 (es) | 2007-11-14 |
Family
ID=23179892
Family Applications (5)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP000102096A AR023823A1 (es) | 1999-05-04 | 2000-05-02 | Compuestos derivados de piperazina utiles como antagonistas ccr5, composiciones farmaceuticas que los comprenden, y el uso de los mismos para la preparacion de medicamentos. |
| ARP060103793A AR057106A2 (es) | 1999-05-04 | 2006-08-30 | USO DE COMPUESTOS DERIVADOS DE PIPERAZINA UTILES COMO ANTAGONISTAS CCR5, PARA LA PREPARACIoN DE MEDICAMENTOS |
| ARP060103792A AR057786A2 (es) | 1999-05-04 | 2006-08-30 | Uso de compuestos derivados de piperazina utiles como antagonistas ccr5, para la preparacion de medicamentos |
| ARP060103794A AR057107A2 (es) | 1999-05-04 | 2006-08-30 | Uso de compuestos derivados de piperazina utiles como antagonistas ccr5, para la preparacion de medicamentos |
| ARP060104839A AR057873A2 (es) | 1999-05-04 | 2006-11-03 | Compuestos derivados de piperizina utiles como antagonistas ccr5, composiciones farmaceuticas que los comprenden, y el uso de los mismos para la preparacion de medicamentos |
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| Application Number | Title | Priority Date | Filing Date |
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| ARP000102096A AR023823A1 (es) | 1999-05-04 | 2000-05-02 | Compuestos derivados de piperazina utiles como antagonistas ccr5, composiciones farmaceuticas que los comprenden, y el uso de los mismos para la preparacion de medicamentos. |
| ARP060103793A AR057106A2 (es) | 1999-05-04 | 2006-08-30 | USO DE COMPUESTOS DERIVADOS DE PIPERAZINA UTILES COMO ANTAGONISTAS CCR5, PARA LA PREPARACIoN DE MEDICAMENTOS |
| ARP060103792A AR057786A2 (es) | 1999-05-04 | 2006-08-30 | Uso de compuestos derivados de piperazina utiles como antagonistas ccr5, para la preparacion de medicamentos |
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| Application Number | Title | Priority Date | Filing Date |
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| ARP060104839A AR057873A2 (es) | 1999-05-04 | 2006-11-03 | Compuestos derivados de piperizina utiles como antagonistas ccr5, composiciones farmaceuticas que los comprenden, y el uso de los mismos para la preparacion de medicamentos |
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| KR (1) | KR100439358B1 (es) |
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| AT (2) | ATE495154T1 (es) |
| AU (2) | AU780888B2 (es) |
| BR (1) | BR0010304A (es) |
| CA (1) | CA2371583C (es) |
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| CL (1) | CL2008002737A1 (es) |
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| IL (1) | IL145741A0 (es) |
| MY (1) | MY128367A (es) |
| NO (1) | NO322045B1 (es) |
| PE (1) | PE20010150A1 (es) |
| PL (1) | PL203116B1 (es) |
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| TW (1) | TWI285200B (es) |
| WO (1) | WO2000066558A1 (es) |
| ZA (1) | ZA200108868B (es) |
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| MX2021015133A (es) | 2019-06-10 | 2022-01-24 | Novartis Ag | Derivado de piridina y pirazina para el tratamiento de la fibrosis quistica, enfermedad pulmonar obstructiva cronica y bronquiectasia. |
| CR20220060A (es) | 2019-08-28 | 2022-03-01 | Novartis Ag | Derivados de 1,3-fenil heteroarilo sustituidos y su uso en el tratamiento de enfermedades |
| TW202140550A (zh) | 2020-01-29 | 2021-11-01 | 瑞士商諾華公司 | 使用抗tslp抗體治療炎性或阻塞性氣道疾病之方法 |
| US11629196B2 (en) | 2020-04-27 | 2023-04-18 | Incelldx, Inc. | Method of treating SARS-CoV-2-associated hypercytokinemia by administering a human monoclonal antibody (PRO-140) that inhibits CCR5/CCL5 binding interactions |
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|---|---|---|---|---|
| SE8803429D0 (sv) * | 1988-09-28 | 1988-09-28 | Pharmacia Ab | Novel pyridyl- and pyrimidyl derivatives |
| SE9201956D0 (sv) * | 1992-06-25 | 1992-06-25 | Kabi Pharmacia Ab | Novel nicotinicacid esters |
| US5889006A (en) * | 1995-02-23 | 1999-03-30 | Schering Corporation | Muscarinic antagonists |
| IL117149A0 (en) | 1995-02-23 | 1996-06-18 | Schering Corp | Muscarinic antagonists |
| EP1003514A4 (en) * | 1997-07-25 | 2000-10-11 | Merck & Co Inc | CYCLIC AMINE MODULATORS OF CHEMOKIN RECEPTORS |
| AR019167A1 (es) * | 1998-06-30 | 2001-12-26 | Schering Corp | Derivados heteroaromaticos de piperazinas di-n-sustituidas y piperidinas 1,4-disustituidas, composiciones farmaceuticas y el uso de los mismos para lapreparacion de medicamentos |
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2000
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