AR037742A1 - Compuestos derivados de piperazina, sus composiciones y su uso - Google Patents
Compuestos derivados de piperazina, sus composiciones y su usoInfo
- Publication number
- AR037742A1 AR037742A1 ARP020103961A ARP020103961A AR037742A1 AR 037742 A1 AR037742 A1 AR 037742A1 AR P020103961 A ARP020103961 A AR P020103961A AR P020103961 A ARP020103961 A AR P020103961A AR 037742 A1 AR037742 A1 AR 037742A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heteroaryl
- heterocyclyl
- aryl
- compositions
- Prior art date
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/74—Amino or imino radicals substituted by hydrocarbon or substituted hydrocarbon radicals
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- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
- C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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- 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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- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A61P37/00—Drugs for immunological or allergic disorders
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- A—HUMAN NECESSITIES
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- 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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- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/63—One oxygen atom
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/72—Nitrogen atoms
- C07D213/76—Nitrogen atoms to which a second hetero atom is attached
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/79—Acids; Esters
- C07D213/80—Acids; Esters in position 3
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- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D213/81—Amides; Imides
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- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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
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- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
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- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three 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
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- C07D295/00—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
- C07D295/16—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
- C07D295/18—Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
- C07D295/182—Radicals derived from carboxylic acids
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- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Un compuesto de fórmula (1) o una forma farmacéuticamente aceptable del mismo; a es 0, 1, 2, 3, 4, ó 5; b es 0, 1, ó 2; c es 0, 1, ó 2; d es 0, 1, 2, 3, ó 4; X es -O-, -S-, -CH2-, ó -NR6-; Y es arilo (C6-10) ó heteroarilo (C2-9); cada R1 es independientemente H-, HO-, halo-, alquil (C1-8)-, alquil (C1-8)-O-, HO-alquil (C1-8)-, NC-, H2N-, H2N-alquil (C1-8)-, HO-(C=O)-, alquil (C1-8)-(C=O)-, alquil (C1-8)-(C=O)-alquil (C1-8)-, H2N-(C=O)-, ó H2N-(C=O)-alquil (C1-8)-; cada R2 y R3 son independientemente H-, oxo, alquil (C1-8)-, cicloalquil (C3-8)-alquil (C1-8)-, aril (C6-10)-, aril (C6-10)-alquil (C1-8)-, HO-alquil (C1-8)-, alquil (C1-8)-O-alquil (C1-8)-, H2N-alquil (C1-8)-, alquil (C1-8)-NH-alquil (C1-8)-, [alquil (C1-8)]2N-alquil (C1-8)-, heterociclil (C2-9)-alquil (C1-8)-, cicloalquil (C3-8)-NH-alquil (C1-8)-, alquil (C1-8)-(C=O)-NH-alquil (C1-8)-, alquil (C1-8)-O-(C=O)-NH-alquil (C1-8)-, H2N-(C=O)-NH-alquil (C1-8)-, alquil (C1-8)-SO2-NH-alquil (C1-8)-, heteroaril (C2-9)-alquil (C1-8)-, H2N-(C=O)-, ó H2N-(C=O)-alquil (C1-8)-; R4 es [HO-(C=O)-][H2N-]alquil (C1-8)-, [HO-(C=O)-][alquil (C1-8)NH-]alquil (C1-8), [HO-(C=O)-][(alquil (C1-8))2N-]alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-NH-, HO-(C=O)-alquil (C1-8)-NH-alquil (C1-8)-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)]N-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)]N-alquil (C1-8)-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)-SO2]N-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)-SO2]N-alquil (C1-8)-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)-(C=O)-]N-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)-(C=O)-]N-alquil (C1-8)-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)-O-(C=O)-]N-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)-O-(C=O)-]N-alquil (C1-8)-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8) N-(C=O)-]N-, [HO-(C=O)-alquil (C1-8)][alquil (C1-8)-NH-(C=O)-]N-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-O-N=alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-SO2- , HO-(C=O)-alquil (C1-8)-SO2-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-SO2-NH-, HO-(C=O)-alquil (C1-8)-SO2-NH-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-NH-SO2-, HO-(C=O)-alquil (C1-8)-NH-SO2-alquil (C1-8)-, HO-(C=O)-(C=O)-NH-SO2-, HO-(C=O)-(C=O)-NH-SO2-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-NH-(C=O)-NH-, HO-(C=O)-alquil (C1-8)-NH-(C=O)-NH-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-O-, HO-(C=O)-alquil (C1-8)-O-alquil (C1-8)-, HO-(C=O)-alquil (C1-8) sustituido con hidroxi, HO-(C=O)-alquenil (C2-8)-, heterociclil (C1-9)-alquil (C1-8)-O-, heterociclil (C1-9)-alquil (C1-8)-O-alquil (C1-8)-, heteroaril (C1-9)-alquil (C1-8)-O-, heteroaril (C1-9)-alquil (C1-8)-O-alquil (C1-8)-, heterociclil (C1-9)-O-, heterociclil (C1-9)-O- alquil (C1-8)-, heteroaril (C1-9)-O-, heteroaril (C1-9)-O-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-S-, HO-(C=O)-alquil (C1-8)-S-alquil (C1-8)-, heterociclil (C1-9)-alquil (C1-8)-S-, heterociclil (C1-9)-alquil (C1-8)-S-alquil (C1-8)-, heteroaril (C1-9)-alquil (C1-8)-S-, heteroaril (C1-9)-alquil (C1-8)-S-alquil (C1-8)-, heterociclil (C1-9)-S-, heterociclil (C1-9)-S-alquil (C1-8)-, heteroaril (C1-9)-S-, heteroaril (C1-9)-S-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-NH-SO2-NH-, HO-(C=O)-alquil (C1-8)-NH-SO2-NH-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-SO2-NH-(C=O)-, HO-(C=O)-alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-(C=O)-NH-SO2-, HO-(C=O)-alquil (C1-8)-(C=O)-NH-SO2-alquil (C1-8)-, HO-(C=O)-(C=O)-, HO-(C=O)-(C=O)-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-(C=O)-, HO-(C=O)-alquil (C1-8)-(C=O)-alquil (C1-8)-, HO-(C=O)-heterociclil (C1-9)-(C=O)-, HO-(C=O)-heteroaril (C1-9)-(C=O)-, NC-NH-(C=O)-, NC-NH-(C=O)-alquil (C1-8), [alquil (C1-8)-SO2-NH-(C=O)-][H2N-]alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-NH-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-NH-alquil (C1-8)-, [alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)][alquil (C1-8)]N-, [alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)][alquil (C1-8)]N-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-NH-SO2-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-NH-SO2-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-SO2-NH-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-SO2-NH-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-SO2-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-SO2-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-(C=O)-, alquil (C1-8)-SO2-NH-(C=O)-(C=O)-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-(C=O)-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-(C=O)-alquil (C1-8)-, NH-alquil (C1-8)-SO2-NH-(C=O)-, NC-alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-, HO-alquil (C1-8)-SO2-NH-(C=O)-, HO-alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-alquenil (C2-8)-, heterociclil (C1-9)-SO2-NH-(C=O)-, heterociclil (C1-9)-SO2-NH-(C=O)-alquil (C1-8)-, heterociclil (C1-9)-alquil (C1-8)-SO2-NH-(C=O)-, heterociclil (C1-9)-alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-, aril (C6-10)-SO2-NH-(C=O)-, aril (C6-10)-SO2-NH-(C=O)-alquil (C1-8)-, heteroaril (C1-9)-SO2-NH-(C=O)-, heteroaril (C1-9)-SO2-NH-(C=O)-alquil (C1-8)-, H2N-SO2-NH-(C=O)-, H2N-SO2-NH-(C=O)-alquil (C1-8)-, alquil (C1-8)-NH-SO2-NH-(C=O)-, alquil (C1-8)-NH-SO2-NH-(C=O)-alquil (C1-8)-, [alquil (C1-8)]2N-SO2-NH-(C=O)-, [alquil (C1-8)]2N-SO2-NH-(C=O)-alquil (C1-8), alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-O-, alquil (C1-8)-SO2-NH-(C=O)-alquil (C1-8)-O-alquil (C1-8)-, alquil (C1-8)-(C=O)-NH-SO2-, H2N-SO2-alquil (C1-8)-, alquil (C1-8)-(C=O)-NH-SO2-alquil (C1-8)-, NC-alquil (C1-8)-(C=O)-NH-SO2-alquil (C1-8)-, HO-(alquil C1-C8)-(C=O)-NH-SO2-alquil (C1-8)-, aril (C6-10)-(C=O)-NH-SO2-, aril (C6-10)-(C=O)-NH-SO2-alquil (C1-8)-, heteroaril (C1-9)-(C=O)-NH-SO2-, heteroaril (C1-9)-(C=O)-NH-SO2-alquil (C1-8)-, heterociclil (C1-9)-(C=O)-NH-SO2-, heterociclil (C1-9)-(C=O)-NH-SO2-alquil (C1-8)-, H2N-(C=O)-NH-SO2-, H2N-(C=O)-NH-SO2-alquil (C1-8)-, alquil (C1-8)-NH-(C=O)-NH-SO2-, alquil (C1-8)-NH-(C=O)-NH-SO2-alquil (C1-8)-, [alquil (C1-8)]2-N-(C=O)-NH-SO2-, [alquil (C1-8)]2-N-(C=O)-NH-SO2-alquil (C1-8)-, aril (C6-10)-NH-(C=O)-NH-SO2-, aril (C6-10)-NH-(C=O)-NH-SO2-alquil (C1-8)-, heteroaril (C1-9)-NH-(C=O)-NH-SO2-, heteroaril (C1-9)-NH-(C=O)-NH-SO2-alquil (C1-8)-, alquil (C1-8)-O-(C=O)-NH-SO2-, alquil (C1-8)-O-(C=O)-NH-SO2-alquil (C1-8)-, aril (C6-10)-oxi-(C=O)-NH-SO2-, aril (C6-10)-oxi-(C=O)-NH-SO2-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-O-, alquil (C1-8)-SO2-NH-(C=O)-O-alquil (C1-8)-, alquil (C1-8)-SO2-NH-(C=O)-NH-, alquil (C1-8)-SO2-NH-(C=O)-NH-alquil (C1-8)-, aril (C6-10)-SO2-NH-(C=O)-O-, aril (C6-10)-SO2-NH-(C=O)-O-alquil (C1-8)-, aril (C6-10)-SO2-NH-(C=O)-NH-, aril (C6-10)-SO2-NH-(C=O)-NH-alquil (C1-8)-, heteroaril (C1-9)-SO2-NH-(C=O)-O-, heteroaril (C1-9)-SO2-NH-(C=O)-O-alquil (C1-8)-, NH2-SO2-NH-(C=O)-O-, NH2-SO2-NH-(C=O)-O-alquil (C1-8)-, heteroaril (C1-9)-SO2-NH-(C=O)-NH-, heteroaril (C1-9)-SO2-NH-(C=O)-NH-alquil (C1-8)-, NH2-SO2-NH-(C=O)-NH-, NH2-SO2-NH-(C=O)-NH-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-NH-(C=O)-O-, HO-(C=O)-alquil (C1-8)-NH-(C=O)-O-alquil (C1-8)-, HO-(C=O)-alquil (C1-8)-O-(C=O)-NH-, HO-(C=O)-alquil (C1-8)-O-(C=O)-NH-alquil (C1-8)-, alquil (C1-8)-(C=O)-NH-SO2-NH-, alquil (C1-8)-(C=O)-NH-SO2-NH-alquil (C1-8), aril (C6-10)-(C=O)-NH-SO2-NH-, aril (C6-10)-(C=O)-NH-SO2-NH-alquil (C1-8), heteroaril (C1-9)-(C=O)-NH-SO2-NH-, heteroaril (C1-9)-(C=O)-NH-SO2-NH-alquil (C1-8), NH2-(C=O)-NH-SO2-NH-, NH2-(C=O)-NH-SO2-NH-alquil (C1-8), heteroaril (C1-9)-alquil (C1-8)-(C=O)-, heterociclil (C1-9)-alquil (C1-8)-(C=O)-, heteroaril (C1-9)-alquil (C1-8)-(C=O)-alquil (C1-8)-, heterociclil (C1-9)-alquil (C1-8)-(C=O)-alquil (C1-8)-, heteroaril (C1-9)-(C=O)-alquil (C1-8)-, ó heterociclil (C1-9)-(C=O)-alquil (C1-8); ó, si Y es un grupo heteroarilo (C2-9), entonces R4 puede ser también HO-(C=O)-alquil (C1-8)-, heteroaril (C1-9)-, heterociclil (C1-9)-, heteroaril (C1-9)-alquil (C1-8), ó heterociclil (C1-9)-alquil (C1-8); cada R5 es independientemente H-, HO-, halo-, NC-, HO-(C=O)-, H2N-, alquil (C1-8)-NH-, [alquil (C1-8)]2N-, alquil (C1-8)-, alquil (C1-8)-O-, HO-alquil (C1-8)-, alquil (C1-8)-O-alquil (C1-8)-, H2N-alquil (C1-8)-, alquil (C1-8)-NH-alquil (C1-8)-, [alquil (C1-8)]2N-alquil (C1-8)-, alquil (C1-8)-(C=O)-, alquil (C1-8)-(C=O)-alquil (C1-8)-, aril (C6-10)-, heteroaril (C2-9)-, aril (C6-10)-oxi-, H2N-(C=O)-, H2N-(C=O)-alquil (C1-8)-, alquil (C1-8)-NH-(C=O)-, alquil (C1-8)-NH-(C=O)-alquil (C1-8)-, [alquil (C1-8)]2N-(C=O)-, [alquil (C1-8)]2-N-(C=O)-alquil (C1-8)-, cicloalquil (C3-8)-, alquil (C1-8)-SO2-, NC-alquil (C1-8)-, alquil (C1-8)-(C=O)-NH-, H2N-(C=O)-NH-, ó H2N-(C=O)-NH-alquil (C1-8)-; y R6 es H, alquil (C1-8)-, alquil (C1-8)-(C=O)-, aril (C6-10)-(C=O)-, heteroaril (C2-9)-(C=O)-, H2N-(C=O)-, alquil (C1-8)-NH-(C=O)-, [alquil (C1-8)]2N-(C=O)-, alquil (C1-8)-O-(C=O)-, ó alquil (C1-8)-SO2-. Composiciones farmacéuticas que comprenden un compuesto de fórmula (1) y un vehículo farmacéuticamente aceptable, y procedimientos de uso de los compuestos y composiciones descriptos en este documento para el tratamiento o prevención de un trastorno o afección que puede tratarse o prevenirse por antagonización del receptor CCR1 en un mamífero.
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IL110040A (en) | 1993-06-29 | 2000-07-16 | Nissan Chemical Ind Ltd | Pyridazinone derivatives their preparation and pharmaceutical compositions comprising them |
HUP9602489A3 (en) | 1995-01-11 | 1998-01-28 | Samjin Pharm Co Ltd | Piperazine derivatives, process for producing them and pharmaceutical compositions containing them |
US6207665B1 (en) * | 1997-06-12 | 2001-03-27 | Schering Aktiengesellschaft | Piperazine derivatives and their use as anti-inflammatory agents |
CA2404626A1 (en) * | 2000-03-31 | 2001-10-04 | Pfizer Products Inc. | Novel piperazine derivatives |
WO2002032901A2 (en) | 2000-10-19 | 2002-04-25 | Pfizer Products Inc. | Bridged piperazine derivatives |
UY27003A1 (es) | 2000-11-06 | 2002-07-31 | Schering Ag | Productos radiofarmacéuticos para el diagnóstico de la enfermedad de alzheimer |
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2002
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- 2002-09-26 JP JP2003538143A patent/JP2005507923A/ja not_active Ceased
- 2002-09-26 WO PCT/IB2002/003989 patent/WO2003035627A1/en not_active Application Discontinuation
- 2002-09-26 CZ CZ2004519A patent/CZ2004519A3/cs unknown
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- 2002-09-26 CN CNA028208889A patent/CN1575283A/zh active Pending
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