SK286968B6 - Piperidín-piperidinyl ako CCR5 antagonista, farmaceutický prostriedok s jeho obsahom a jeho použitie - Google Patents
Piperidín-piperidinyl ako CCR5 antagonista, farmaceutický prostriedok s jeho obsahom a jeho použitie Download PDFInfo
- Publication number
- SK286968B6 SK286968B6 SK1567-2001A SK15672001A SK286968B6 SK 286968 B6 SK286968 B6 SK 286968B6 SK 15672001 A SK15672001 A SK 15672001A SK 286968 B6 SK286968 B6 SK 286968B6
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- Prior art keywords
- alkyl
- mmol
- formula
- phenyl
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- 239000002798 polar solvent Substances 0.000 description 1
- 229920000573 polyethylene Polymers 0.000 description 1
- 239000011591 potassium Substances 0.000 description 1
- 229910052700 potassium Inorganic materials 0.000 description 1
- 235000015320 potassium carbonate Nutrition 0.000 description 1
- 235000011181 potassium carbonates Nutrition 0.000 description 1
- LPNYRYFBWFDTMA-UHFFFAOYSA-N potassium tert-butoxide Chemical compound [K+].CC(C)(C)[O-] LPNYRYFBWFDTMA-UHFFFAOYSA-N 0.000 description 1
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- 238000012910 preclinical development Methods 0.000 description 1
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- RZWZRACFZGVKFM-UHFFFAOYSA-N propanoyl chloride Chemical compound CCC(Cl)=O RZWZRACFZGVKFM-UHFFFAOYSA-N 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 230000006337 proteolytic cleavage Effects 0.000 description 1
- 239000002212 purine nucleoside Substances 0.000 description 1
- 125000003226 pyrazolyl group Chemical group 0.000 description 1
- 125000002098 pyridazinyl group Chemical group 0.000 description 1
- 125000000168 pyrrolyl group Chemical group 0.000 description 1
- 125000002294 quinazolinyl group Chemical group N1=C(N=CC2=CC=CC=C12)* 0.000 description 1
- 125000005493 quinolyl group Chemical group 0.000 description 1
- 150000003254 radicals Chemical class 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 229940063627 rescriptor Drugs 0.000 description 1
- 229940064914 retrovir Drugs 0.000 description 1
- 238000012340 reverse transcriptase PCR Methods 0.000 description 1
- 108010025554 ribonucleoside-triphosphate reductase Proteins 0.000 description 1
- 150000003378 silver Chemical class 0.000 description 1
- 239000002002 slurry Substances 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 235000015424 sodium Nutrition 0.000 description 1
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 description 1
- QDRKDTQENPPHOJ-UHFFFAOYSA-N sodium ethoxide Chemical compound [Na+].CC[O-] QDRKDTQENPPHOJ-UHFFFAOYSA-N 0.000 description 1
- 235000011121 sodium hydroxide Nutrition 0.000 description 1
- RMBAVIFYHOYIFM-UHFFFAOYSA-M sodium methanethiolate Chemical compound [Na+].[S-]C RMBAVIFYHOYIFM-UHFFFAOYSA-M 0.000 description 1
- 239000007909 solid dosage form Substances 0.000 description 1
- 238000007920 subcutaneous administration Methods 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- NCEXYHBECQHGNR-QZQOTICOSA-N sulfasalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-QZQOTICOSA-N 0.000 description 1
- 150000003457 sulfones Chemical class 0.000 description 1
- 125000004434 sulfur atom Chemical group 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 229940054565 sustiva Drugs 0.000 description 1
- 239000003765 sweetening agent Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
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- 229960001967 tacrolimus Drugs 0.000 description 1
- QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 description 1
- 125000001544 thienyl group Chemical group 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
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- QORWJWZARLRLPR-UHFFFAOYSA-H tricalcium bis(phosphate) Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 description 1
- 238000001665 trituration Methods 0.000 description 1
- 150000003672 ureas Chemical class 0.000 description 1
- 230000029812 viral genome replication Effects 0.000 description 1
- 229940098802 viramune Drugs 0.000 description 1
- 210000002845 virion Anatomy 0.000 description 1
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- XOFLBQFBSOEHOG-UUOKFMHZSA-N γS-GTP Chemical compound C1=2NC(N)=NC(=O)C=2N=CN1[C@@H]1O[C@H](COP(O)(=O)OP(O)(=O)OP(O)(O)=S)[C@@H](O)[C@H]1O XOFLBQFBSOEHOG-UUOKFMHZSA-N 0.000 description 1
Classifications
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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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
-
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Virology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- AIDS & HIV (AREA)
- Transplantation (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Molecular Biology (AREA)
- Pain & Pain Management (AREA)
- Tropical Medicine & Parasitology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30518799A | 1999-05-04 | 1999-05-04 | |
| PCT/US2000/011633 WO2000066559A1 (en) | 1999-05-04 | 2000-05-01 | Piperidine derivatives useful as ccr5 antagonists |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| SK15672001A3 SK15672001A3 (sk) | 2002-06-04 |
| SK286968B6 true SK286968B6 (sk) | 2009-08-06 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK1567-2001A SK286968B6 (sk) | 1999-05-04 | 2000-05-01 | Piperidín-piperidinyl ako CCR5 antagonista, farmaceutický prostriedok s jeho obsahom a jeho použitie |
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| JP (3) | JP3894729B2 (cs) |
| KR (1) | KR100439357B1 (cs) |
| CN (2) | CN1524527A (cs) |
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| AT (1) | ATE299866T1 (cs) |
| AU (2) | AU780983B2 (cs) |
| BR (1) | BR0010607A (cs) |
| CA (1) | CA2371587C (cs) |
| CO (1) | CO5170522A1 (cs) |
| CZ (1) | CZ301161B6 (cs) |
| DE (1) | DE60021371T2 (cs) |
| DK (1) | DK1175402T3 (cs) |
| EG (1) | EG24533A (cs) |
| ES (1) | ES2246233T3 (cs) |
| HK (1) | HK1039330B (cs) |
| HU (1) | HUP0203528A3 (cs) |
| IL (1) | IL145742A0 (cs) |
| MY (1) | MY141473A (cs) |
| NO (1) | NO322044B1 (cs) |
| NZ (1) | NZ514675A (cs) |
| PE (1) | PE20010113A1 (cs) |
| PL (1) | PL203117B1 (cs) |
| PT (1) | PT1175402E (cs) |
| RU (2) | RU2266281C2 (cs) |
| SA (1) | SA00210270B1 (cs) |
| SI (1) | SI1175402T1 (cs) |
| SK (1) | SK286968B6 (cs) |
| TR (2) | TR200402496T2 (cs) |
| TW (1) | TWI283666B (cs) |
| WO (1) | WO2000066559A1 (cs) |
| ZA (1) | ZA200108867B (cs) |
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| AR033517A1 (es) | 2000-04-08 | 2003-12-26 | Astrazeneca Ab | Derivados de piperidina, proceso para su preparacion y uso de estos derivados en la fabricacion de medicamentos |
| US20050065319A1 (en) * | 2000-12-19 | 2005-03-24 | Baroudy Bahige M. | Combination method for treating viral infections |
| PE20020996A1 (es) | 2001-03-29 | 2002-11-01 | Schering Corp | Antagonistas de ccr5 utiles para el tratamiento del sida |
| GB0108876D0 (en) * | 2001-04-09 | 2001-05-30 | Novartis Ag | Organic Compounds |
| PL368041A1 (en) | 2001-07-02 | 2005-03-21 | Astrazeneca Ab | Piperidine derivatives useful as modulators of chemokine receptor activity |
| GB0120461D0 (en) | 2001-08-22 | 2001-10-17 | Astrazeneca Ab | Novel compounds |
| AR036366A1 (es) * | 2001-08-29 | 2004-09-01 | Schering Corp | Derivados de piperidina utiles como antagonistas de ccr5, composiciones farmaceuticas, el uso de dichos derivados para la fabricación de un medicamento y un kit |
| GB0122503D0 (en) | 2001-09-18 | 2001-11-07 | Astrazeneca Ab | Chemical compounds |
| US6818773B2 (en) * | 2001-10-15 | 2004-11-16 | Schering Corporation | Synthesis of 4-[(Z)-4-bromophenyl)(ethoxyimino) methyl]-1'-[(2,4-dimethyl-1-oxido-3-pyridinyl)carbony)]-4'-methyl-1,4-′bipiperidine |
| AR036882A1 (es) | 2001-10-15 | 2004-10-13 | Schering Corp | Sintesis de (4-bromofenil)(4-piperidil)metanona-(z)-o-etiloxima y sales |
| JP2005518424A (ja) * | 2001-11-29 | 2005-06-23 | シェーリング コーポレイション | Ａｉｄｓおよび関連するｈｉｖ感染の処置のためのｃｃｒ５−アンタゴニストとしての４（（ｚ）−（４−ブロモフェニル）エトキシイミノ）メチル）−１’−（（２，４−ジメチル−１−オキシド−３−ピリジニルカルボニル）−４’−メチル−１，４’ビピペリジンの薬学的塩の調製 |
| EP2311818B1 (en) | 2002-02-28 | 2013-01-16 | Novartis AG | Combination of a 5-phenylthiazole compound as PI3 kinase inhibitor with an antiinflammatory, bronchodilatory or antihistamine drug |
| SE0200844D0 (sv) | 2002-03-19 | 2002-03-19 | Astrazeneca Ab | Chemical compounds |
| SE0200843D0 (sv) | 2002-03-19 | 2002-03-19 | Astrazeneca Ab | Chemical compounds |
| CN101139343A (zh) * | 2002-03-29 | 2008-03-12 | 先灵公司 | 作为ccr5拮抗药的哌啶和哌嗪化合物的合成 |
| AU2003235097A1 (en) * | 2002-04-24 | 2003-11-10 | Takeda Pharmaceutical Company Limited | Use of compounds having ccr antagonism |
| JP2004107298A (ja) * | 2002-09-20 | 2004-04-08 | Takeda Chem Ind Ltd | ウレア化合物およびその用途 |
| AU2003266528A1 (en) * | 2002-09-20 | 2004-04-08 | Takeda Pharmaceutical Company Limited | Cyclic amine compound, process for producing the same, and use |
| GB0223223D0 (en) | 2002-10-07 | 2002-11-13 | Novartis Ag | Organic compounds |
| MXPA05006354A (es) * | 2002-12-13 | 2005-08-26 | Smithkline Beecham Corp | Antagonistas ccr5 como agentes terapeuticos. |
| PE20040769A1 (es) * | 2002-12-18 | 2004-11-06 | Schering Corp | Derivados de piperidina utiles como antagonisas ccr5 |
| RU2366655C2 (ru) | 2003-03-14 | 2009-09-10 | Оно Фармасьютикал Ко., Лтд. | Азотсодержащие гетероциклические производные и лекарственные средства, содержащие их в качестве активного ингредиента |
| SE0300957D0 (sv) | 2003-04-01 | 2003-04-01 | Astrazeneca Ab | Chemical compounds |
| EP2364982A1 (en) | 2003-04-18 | 2011-09-14 | ONO Pharmaceutical Co., Ltd. | Spiro-piperidine compounds as chemokine receptor antagonists and medicinal use thereof |
| WO2004092136A1 (ja) * | 2003-04-18 | 2004-10-28 | Ono Pharmaceutical Co., Ltd. | 含窒素複素環化合物およびその用途 |
| TW200519106A (en) | 2003-05-02 | 2005-06-16 | Novartis Ag | Organic compounds |
| MXPA05013474A (es) * | 2003-06-13 | 2006-03-09 | Schering Ag | Derivados de quinolilamida como antagonistas de ccr-5. |
| US7161024B2 (en) | 2003-07-10 | 2007-01-09 | Schering Corporation | Process for the preparation and purification of 2-(alkoxyalkylidene)-3-ketoalkanoic acid esters from 3-ketoalkanoic acid esters |
| SE0302956D0 (sv) * | 2003-11-07 | 2003-11-07 | Astrazeneca Ab | Chemical compounds |
| US7498346B2 (en) * | 2003-12-11 | 2009-03-03 | Genzyme Corporation | Chemokine receptor binding compounds |
| GB0401334D0 (en) | 2004-01-21 | 2004-02-25 | Novartis Ag | Organic compounds |
| EP1716156A2 (en) | 2004-02-10 | 2006-11-02 | F.Hoffmann-La Roche Ag | Chemokine ccr5 receptor modulators |
| SE0400925D0 (sv) * | 2004-04-06 | 2004-04-06 | Astrazeneca Ab | Chemical compounds |
| GEP20094680B (en) | 2004-04-13 | 2009-05-10 | Incyte Corp | Piperazinylpiperidine derivatives as chemokine receptor antagonists |
| JP2008501743A (ja) | 2004-06-09 | 2008-01-24 | エフ．ホフマン−ラ ロシュ アーゲー | 複素環式抗ウイルス性化合物 |
| PE20060598A1 (es) * | 2004-09-13 | 2006-08-21 | Ono Pharmaceutical Co | Derivado heterociclo conteniendo nitrogeno como antagonista de quimiocina ccr5 |
| GT200500281A (es) | 2004-10-22 | 2006-04-24 | Novartis Ag | Compuestos organicos. |
| GB0426164D0 (en) | 2004-11-29 | 2004-12-29 | Novartis Ag | Organic compounds |
| WO2006077499A1 (en) * | 2005-01-20 | 2006-07-27 | Pfizer Limited | Chemical compounds |
| KR20070107046A (ko) * | 2005-02-16 | 2007-11-06 | 쉐링 코포레이션 | Ｃｘｃｒ3 길항제 활성을 지닌 헤테로사이클릭 치환된피페라진 |
| PE20061012A1 (es) * | 2005-02-23 | 2006-10-03 | Schering Corp | Derivados piperidinil piperazina como inhibidores de receptores quiomicina |
| MX2007010257A (es) * | 2005-02-23 | 2007-09-11 | Schering Corp | Derivados de piperidinil piperidina utiles como inhibidores de receptores de quimiocinas. |
| GB0507577D0 (en) | 2005-04-14 | 2005-05-18 | Novartis Ag | Organic compounds |
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