FI112227B - Förfarande för frasmtällning farmaceutiskt användbara pyridinderivat - Google Patents

Förfarande för frasmtällning farmaceutiskt användbara pyridinderivat Download PDF

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Publication number
FI112227B
FI112227B FI952607A FI952607A FI112227B FI 112227 B FI112227 B FI 112227B FI 952607 A FI952607 A FI 952607A FI 952607 A FI952607 A FI 952607A FI 112227 B FI112227 B FI 112227B
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pyridyl
formula
pyrimidinamine
compound
amino
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FI952607A
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Finnish (fi)
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FI952607A (sv
FI952607A0 (sv
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Juerg Zimmermann
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Novartis Ag
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • A61K31/28—Compounds containing heavy metals
    • A61K31/305—Mercury compounds
    • 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
    • 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
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • 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
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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
    • 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
    • A61P37/04—Immunostimulants
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Urology & Nephrology (AREA)
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  • Communicable Diseases (AREA)
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  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
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  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Medicinal Preparation (AREA)

Claims (14)

1. Förfarande för framställning av ett farmaceutiskt an-vändbart N-fenyl-2-pyrimidinaminderivat med formeln I " rVCOCX Rt 20 väri R0 är väte, halogen, lägalkoxi eller lägalkyl, Ri är ; ;,· a) N-(aminolägalkyl)-karbamoyl, •' ‘.j 25 b) N-(hydroxilägalkyl)-karbamoyl, : *; c) hydrazino, d) piperazinyl, som är osubstituerad eller substituerad med aminolägalkyl, e) morfolino eller 30 f) lägalkylamino, som är substituerad med morfolinyl, ; hydroxilägalkylamino, imidazolyl, guanidyl, amino, lägal- :.'-j kanoylamino, lägalkylaminokarbonylamino, amidino, karbo- ; : xi, lägalkoxikarbonyl, karbamoyl, N-hydroxikarbamoyl, hydroxi, dihydroxifosforyloxi eller en grupp med formeln . 35 H2N-CH (R)-C (=0)-NH-, väri R är väte och R2 är Cj^-Cg-alkyl, • · klor, brom, jod, trifluormetyl, karboxi, eller en grupp med formeln -C02R3, väri R3 är C1-C3-alkyl, eller en grupp 112227 64 med formeln -C (=0)-NH-(CH2) n-R4a, väri n är 2 eller 3 och R4a är hydroxi, amino eller imidazolyl, eller ett farma-ceutiskt användbart salt därav, kännetecknat därav, att 5 a) en förening med formeln II C(=0)-CH=CH-N(Rg)-Rg v
10 R, vari R8 och R9 oberoende av varandra är lägalkyl och Rx betecknar detsamma som ovan, da de funktionella grupperna 15 i föreningen med formeln II, med undantag av de i reak- tionen deltagande grupperna, vid behov är i skyddad form, eller ett salt av en sädan förening omsättes med en förening med formeln III Ro'X~)>~R2 NH y_y \~/ ®»· NH, >) : 25 , väri R0 och R2 betecknar detsamma som ovan, da de funktio- ; neliä grupperna i föreningen med formeln III, med undan tag av den i reaktion deltagande guanidinogruppen vid behov är i skyddad form, eller med ett sait av en sädan 30 förening, och alla förekommande skyddsgrupper avlägsnas, eller * · b) för framställning av en förening med formeln I, vari Rx betecknar detsamma som ovan i punkterna c) eller f) och R0 35 och R2 bäda betecknar detsamma som ovan, en förening med • ' · formeln IV 11222/ 65 V"i H Y 10 väri Y är en avlägsningsgrupp och R0 och R2 betecknar detsamma som ovan, da de i formeln IV forekommande funk-tionella grupperna, med undantag av den i reaktionen deltagande avlägsningsgruppen, vid behov är i skyddad 15 form, eller ett salt av en sädan förening omsättes med en amin med formeln V H2N-R12 (V) 2. väri R12 är amino eller lägalkyl, som är substituerad med morfolinyl, hydroxilagalkylamino, imidazolyl, guanidyl, amino, lägalkanoylamino, lägalkylaminokarbonylamino, amidino, karboxi, lägalkoxikarbonyl, karbamoyl, N-hydro-’ ;,· xikarbamoyl, hydroxi, dihydroxifosforyloxi eller en rest 25 med formeln H2N-CH (R)-C (=0)-NH-, väri R är väte, de funk-: *: tionella grupperna i resten R12 är, vid behov, i skyddad ; form, och alla skyddsgrupper avlägsnas, eller c) för framställning av en förening med formeln I, väri Rx 30 är N-(aminolägalkyl)-karbamoyl eller N-(hydroxilägalkyl)-V karbamoyl och R0 och R2 betecknar detsamma som ovan, en ’·· karboxylsyra med formeln IX Ί: 35 rxYx /·: (IX), Il I Νγ^ H COOH 66 11222? väri R0 och R2 betecknar detsamma som ovan, da de funktio-nella grupperna i resten R2 vid behov är i skyddad form, eller dess reaktionsdugliga derivat omsättes med en amin 5 med formeln X H2N-R13 (X) väri R13 är aminolägalkyl eller hydroxilägalkyl, amino-10 eller hydroxigruppen vid behov är i skyddad form och alia förekommande skyddsgrupper avlägsnas, eller d) för framställning av en förening med formeln I, väri R-l är morfolino eller den är piperazinyl, som är osubsti- 15 tuerad eller substituerad med aminolägalkyl, och R0 och R2 betecknar detsamma som ovan, en förening med formeln IV I^Sl (IV), y : 25 : väri Y är en avlägsningsgrupp och R0 och R2 betecknar detsamma som ovan, da de funktionella grupperna i fö-reningen med formeln IV, med undantag av den i reaktion
1 I 30 deltagande avlägsningsgruppen, vid behov är i skyddad “/ form, eller ett sait av en sadan förening omsättes med ,’·· morfolin eller piperazin, som är osubstituerad eller substituerad med aminolägalkyl, och alla förekommande skyddsgrupper avlägsnas, eller 35 e) för framställning av en förening med formeln I, väri R2 är -C02R3 eller -C (=0)-NH-(CH2) n-R4a, väri symbolerna och 67 1 1222? substituenterna betecknar detsamma som ovan, en karbo-xylsyra med formeln XI (T^Y^n^n^V^cooh (χβ,
10 X vari R0 och R-l betecknar detsamma som ovan, da de förekom-mande funktionella grupperna, vid behov är i skyddad 15 form, eller dess reaktionsdugliga karboxylsyraderivat förestras eller amideras pä lämpligt sätt och alla före-kommande skyddsgrupper avlägsnas och en förening med formeln I erhallen enligt nägot som heist av förfarandena a)-e) omvandlas, om sä önskas, till ett farmaceutiskt 2 0 användbart salt därav eller ett erhället salt av fö- reningen med formeln I omvandlas till en fri förening. ..·* 2. Förfarande enligt patentkravet 1, kännetecknat därav, I/. att man framställer en förening med formeln I, som är N- . 25 (3-trifluormetylfenyl) -4-[2-(3-hydroxipropylamino) -4- ·’; pyridyl] -2-pyrimidinamin, . ·. N-(3-klorfenyl)-4-[2-(2-aminoetylamino)-4-pyridyl]-2- pyrimidinamin, . . N-(3-trifluormetylfenyl)-4-[2-(2-aminoetylamino)-4-pyri- 30 dyl]-2-pyrimidinamin, *;·* N- [3-klorfenyl] -4- [2- (N- {2-aminoetyl} -aminokarbonyl) -4- ; pyridyl]-2-pyrimidinamin, ; N- [3-klorfenyl] -4 - [2 - (N- {2-hydroxietyl} - aminokarbonyl) -4- * * · *. pyridyl] -2-pyrimidinamin, * * ;·’ 35 N- [3-klorfenyl] -4- [2- (N- {3-hydroxipropyl}-aminokarbonyl) - i i · * '· 4-pyridyl] -2-pyrimidinamin, N-[3-klorfenyl]-4- [2-(N-{3-aminoprop-l-yl}-aminokarbo- 11222/ 68 nyl)-4-pyridyl]-2-pyrimidinamin, N-[3-klorfenyl]-4-[2-(2-hydroxietylamino)-4-pyridyl]-2-pyrimidinamin, N-[3-karboxifenyl]-4-[2-(3-hydroxipropylamino)-4-pyri-5 dyl]-2-pyrimidinamin, N-[3-metoxikarbonylfenyl]-4-[2-(3-hydroxipropylamino)-4-pyridyl]-2-pyrimidinamin, N-[3-klorfenyl]-4-[2-(4-hydroxibutylamino)-4-pyridyl]-2-pyrimidinamin,
10 N-[3-klorfenyl]-4-{2-[2-(imidazol-4-yl)-etylamino]-4-pyridyl}-2-pyrimidinamin, N-[3-metylfenyl]-4-[2-(3-hydroxipropylamino)-4-pyridyl]-2-pyrimidinamin, N-[3-klorfenyl]-4-[2-(5-hydroxipentylamino)-4-pyridyl]-2-15 pyrimidinamin, N-[3-{N-(3-hydroxipropyl)aminokarbonyl}-fenyl]-4-[2-(3-hydroksipropylamino)-4-pyridyl]-2-pyrimidinamin, N-[3-{N-(3-aminopropyl)aminokarbonyl}-fenyl]-4-[2-(3-hydroxipropylamino)-4-pyridyl]-2-pyrimidinamin,
20 N-[3-{N-(2-imidazol-4-yletyl)aminokarbonyl}-fenyl]-4- [2-(3-hydroxipropylamino)-4-pyridyl]-2-pyrimidinamin, N-[3-klor-6-metylfenyl]-4-[2-(3-hydroxipropylamino)-4-..· pyridyl] -2-pyrimidinamin, N- [3,6-diklorfenyl] -4- [2- (3-hydroxipropylamino) -4-pyri-25 dyl] -2-pyrimidinamin, N- [3-klor-6-metoxifenyl] -4-[2-(3-hydroxipropylamino) -4-; pyridyl] - 2-pyrimidinamin, N-[3-klorfenyl]-4-[2-(1-piperazinyl)-4-pyridyl]-2-pyri-midinamin, • ·
30 N- [3-klorfenyl] -4- (2- [2- {4-morfolinyl}etylamino] -4-pyri-dyl] -2-pyrimidinamin, • · ·,'·· N- [3-klorfenyl] -4-{2 - [4 - (2-aminoetyl) -piperazin-l-yl) ] -4- pyridyl}-2-pyrimidinamin, N-[3-klorfenyl]-4-{2-[3-(2-hydroxietylamino)-propyl-35 amino]-4-pyridyl}-2-pyrimidinamin eller • » » ‘ ’ N-[3-klorfenyl]-4-[2-(4-morfolinyl)-4-pyridyl]-2-pyri midinamin eller 11222Ί 69 ett farmaceutiskt godtagbart salt därav. • m f · * · * · * t * » ί · » » » t
FI952607A 1993-10-01 1995-05-29 Förfarande för frasmtällning farmaceutiskt användbara pyridinderivat FI112227B (sv)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CH296993 1993-10-01
CH296993 1993-10-01
CH228194 1994-07-18
CH228194 1994-07-18
EP9403151 1994-09-21
PCT/EP1994/003151 WO1995009853A1 (en) 1993-10-01 1994-09-21 Pharmacologically active pyridine derivatives and processes for the preparation thereof

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FI952607A FI952607A (sv) 1995-05-29
FI952607A0 FI952607A0 (sv) 1995-05-29
FI112227B true FI112227B (sv) 2003-11-14

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US (1) US5728708A (sv)
EP (1) EP0672041B1 (sv)
JP (1) JP2983636B2 (sv)
KR (1) KR100330553B1 (sv)
CN (1) CN1047776C (sv)
AT (1) ATE208772T1 (sv)
AU (1) AU691834B2 (sv)
CA (1) CA2148928C (sv)
CZ (1) CZ290681B6 (sv)
DE (1) DE69429078T2 (sv)
DK (1) DK0672041T3 (sv)
ES (1) ES2167377T3 (sv)
FI (1) FI112227B (sv)
HU (1) HU228172B1 (sv)
IL (1) IL111077A (sv)
NO (1) NO308794B1 (sv)
NZ (1) NZ273617A (sv)
PL (1) PL179417B1 (sv)
PT (1) PT672041E (sv)
RU (1) RU2135491C1 (sv)
WO (1) WO1995009853A1 (sv)

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NO952132D0 (no) 1995-05-30
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DE69429078D1 (de) 2001-12-20
IL111077A0 (en) 1994-11-28
AU691834B2 (en) 1998-05-28
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IL111077A (en) 1999-10-28
KR950704296A (ko) 1995-11-17
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CN1047776C (zh) 1999-12-29
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ATE208772T1 (de) 2001-11-15
RU2135491C1 (ru) 1999-08-27
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