KR960034184A - 퀴나졸린 유도체 - Google Patents
퀴나졸린 유도체 Download PDFInfo
- Publication number
- KR960034184A KR960034184A KR1019960009659A KR19960009659A KR960034184A KR 960034184 A KR960034184 A KR 960034184A KR 1019960009659 A KR1019960009659 A KR 1019960009659A KR 19960009659 A KR19960009659 A KR 19960009659A KR 960034184 A KR960034184 A KR 960034184A
- Authority
- KR
- South Korea
- Prior art keywords
- amine
- alkyl
- phenyl
- quinazolin
- ethynyl
- Prior art date
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- 125000002294 quinazolinyl group Chemical class N1=C(N=CC2=CC=CC=C12)* 0.000 title 1
- -1 4- (substituted phenylamino) quinazoline Chemical class 0.000 claims abstract 45
- 150000001875 compounds Chemical class 0.000 claims abstract 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 8
- 125000005843 halogen group Chemical group 0.000 claims 31
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 18
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 15
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 239000001301 oxygen Substances 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 7
- 125000005842 heteroatom Chemical group 0.000 claims 7
- 125000004356 hydroxy functional group Chemical group O* 0.000 claims 7
- 125000001424 substituent group Chemical group 0.000 claims 7
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 6
- 125000003282 alkyl amino group Chemical group 0.000 claims 6
- 125000004122 cyclic group Chemical group 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- 125000003545 alkoxy group Chemical group 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 239000011593 sulfur Chemical group 0.000 claims 5
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 4
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- UJOBWOGCFQCDNV-UHFFFAOYSA-N 9H-carbazole Chemical compound C1=CC=C2C3=CC=CC=C3NC2=C1 UJOBWOGCFQCDNV-UHFFFAOYSA-N 0.000 claims 4
- 125000005236 alkanoylamino group Chemical group 0.000 claims 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims 3
- 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
- 230000003463 hyperproliferative effect Effects 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
- 229920000642 polymer Polymers 0.000 claims 3
- MTLKTHNRZJKPRP-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)-6-(2-methoxyethoxy)quinazolin-7-yl]oxyethanol Chemical compound N1=CN=C2C=C(OCCO)C(OCCOC)=CC2=C1NC1=CC=CC(C#C)=C1 MTLKTHNRZJKPRP-UHFFFAOYSA-N 0.000 claims 2
- YWSAEKIQJPQSDJ-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)-7-(2-hydroxyethoxy)quinazolin-6-yl]oxyethanol Chemical compound C=12C=C(OCCO)C(OCCO)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 YWSAEKIQJPQSDJ-UHFFFAOYSA-N 0.000 claims 2
- XSMVZQAPXNUGBP-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)-7-(2-methoxyethoxy)quinazolin-6-yl]oxyethyl acetate Chemical compound C=12C=C(OCCOC(C)=O)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 XSMVZQAPXNUGBP-UHFFFAOYSA-N 0.000 claims 2
- 125000004399 C1-C4 alkenyl group Chemical group 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- XYFCBTPGUUZFHI-UHFFFAOYSA-N Phosphine Chemical compound P XYFCBTPGUUZFHI-UHFFFAOYSA-N 0.000 claims 2
- PPBRXRYQALVLMV-UHFFFAOYSA-N Styrene Chemical compound C=CC1=CC=CC=C1 PPBRXRYQALVLMV-UHFFFAOYSA-N 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 125000003356 phenylsulfanyl group Chemical group [*]SC1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- TZHTWWZUWBDHPB-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)-6-(2-methoxyethoxy)quinazolin-7-yl]oxyethyl acetate Chemical compound N1=CN=C2C=C(OCCOC(C)=O)C(OCCOC)=CC2=C1NC1=CC=CC(C#C)=C1 TZHTWWZUWBDHPB-UHFFFAOYSA-N 0.000 claims 1
- KOQIAZNBAWFSQM-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)-7-(2-methoxyethoxy)quinazolin-6-yl]oxyethanol Chemical compound C=12C=C(OCCO)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 KOQIAZNBAWFSQM-UHFFFAOYSA-N 0.000 claims 1
- COYVNRXIBHVWOA-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)-7-propan-2-yloxyquinazolin-6-yl]acetamide Chemical compound C=12C=C(CC(N)=O)C(OC(C)C)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 COYVNRXIBHVWOA-UHFFFAOYSA-N 0.000 claims 1
- TYRDQXAAPHCGHJ-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)-7-propoxyquinazolin-6-yl]acetamide Chemical compound C=12C=C(CC(N)=O)C(OCCC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 TYRDQXAAPHCGHJ-UHFFFAOYSA-N 0.000 claims 1
- RPBDPTCBOMUIEM-UHFFFAOYSA-N 2-[4-(3-ethynylanilino)quinazolin-6-yl]guanidine Chemical compound C12=CC(NC(=N)N)=CC=C2N=CN=C1NC1=CC=CC(C#C)=C1 RPBDPTCBOMUIEM-UHFFFAOYSA-N 0.000 claims 1
- UBUGNWMTGOQPCM-UHFFFAOYSA-N 2-[7-(2-acetyloxyethoxy)-4-(3-ethynylanilino)quinazolin-6-yl]oxyethyl acetate Chemical compound C=12C=C(OCCOC(C)=O)C(OCCOC(=O)C)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 UBUGNWMTGOQPCM-UHFFFAOYSA-N 0.000 claims 1
- BLEIGNISAJGLGG-UHFFFAOYSA-N 2-[[1-(3-ethynylanilino)-7-(2-hydroxyethoxy)-2h-quinazolin-6-yl]oxy]ethanol Chemical compound C1=2C=C(OCCO)C(OCCO)=CC=2C=NCN1NC1=CC=CC(C#C)=C1 BLEIGNISAJGLGG-UHFFFAOYSA-N 0.000 claims 1
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims 1
- MLFVZJQGCZIVJI-UHFFFAOYSA-N 4-n-(3-ethynylphenyl)quinazoline-4,7-diamine Chemical compound N=1C=NC2=CC(N)=CC=C2C=1NC1=CC=CC(C#C)=C1 MLFVZJQGCZIVJI-UHFFFAOYSA-N 0.000 claims 1
- OPZQXOBOVGSGMM-UHFFFAOYSA-N 6,7-bis(2-chloroethoxy)-n-(3-ethynylphenyl)quinazolin-4-amine Chemical compound C=12C=C(OCCCl)C(OCCCl)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 OPZQXOBOVGSGMM-UHFFFAOYSA-N 0.000 claims 1
- AZMJCKIZWVLDEH-UHFFFAOYSA-N 6,7-diethoxy-n-(3-ethynylphenyl)-2h-quinazolin-1-amine Chemical compound C1=2C=C(OCC)C(OCC)=CC=2C=NCN1NC1=CC=CC(C#C)=C1 AZMJCKIZWVLDEH-UHFFFAOYSA-N 0.000 claims 1
- DBLVDARHJKFUSK-UHFFFAOYSA-N 6-(2-chloroethoxy)-n-(3-ethynylphenyl)-7-(2-methoxyethoxy)quinazolin-4-amine Chemical compound C=12C=C(OCCCl)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 DBLVDARHJKFUSK-UHFFFAOYSA-N 0.000 claims 1
- BIHHIONDWPZXJC-UHFFFAOYSA-N 7-(2-chloroethoxy)-n-(3-ethynylphenyl)-6-(2-methoxyethoxy)quinazolin-4-amine Chemical compound N1=CN=C2C=C(OCCCl)C(OCCOC)=CC2=C1NC1=CC=CC(C#C)=C1 BIHHIONDWPZXJC-UHFFFAOYSA-N 0.000 claims 1
- MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
- 208000009849 Female Genital Neoplasms Diseases 0.000 claims 1
- XOVXNWFRRSMBFV-UHFFFAOYSA-N N-(3-ethynyl-5-methylphenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine Chemical compound COCCOc1cc2ncnc(Nc3cc(C)cc(c3)C#C)c2cc1OCCOC XOVXNWFRRSMBFV-UHFFFAOYSA-N 0.000 claims 1
- XOTGKYTUNDYTBS-UHFFFAOYSA-N N-(3-ethynylphenyl)-6,7-dimethoxy-4-quinazolinamine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 XOTGKYTUNDYTBS-UHFFFAOYSA-N 0.000 claims 1
- 235000001982 Physalis edulis Nutrition 0.000 claims 1
- 244000064622 Physalis edulis Species 0.000 claims 1
- 208000024770 Thyroid neoplasm Diseases 0.000 claims 1
- 125000004423 acyloxy group Chemical group 0.000 claims 1
- 150000001345 alkine derivatives Chemical class 0.000 claims 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 1
- 125000000043 benzamido group Chemical group [H]N([*])C(=O)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 229920006037 cross link polymer Polymers 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 210000003238 esophagus Anatomy 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 206010020718 hyperplasia Diseases 0.000 claims 1
- 125000002962 imidazol-1-yl group Chemical group [*]N1C([H])=NC([H])=C1[H] 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- KWTKAHJFBOHEHR-UHFFFAOYSA-N n-(3-azido-5-chlorophenyl)-6,7-dimethoxyquinazolin-4-amine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC(Cl)=CC(N=[N+]=[N-])=C1 KWTKAHJFBOHEHR-UHFFFAOYSA-N 0.000 claims 1
- VVCIISBATPBTBZ-UHFFFAOYSA-N n-(3-azidophenyl)-6,7-dimethoxyquinazolin-4-amine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=CC(N=[N+]=[N-])=C1 VVCIISBATPBTBZ-UHFFFAOYSA-N 0.000 claims 1
- YVEQUSIQTPNUHB-UHFFFAOYSA-N n-(3-ethynyl-2-methylphenyl)-6,7-bis(2-methoxyethoxy)-2h-quinazolin-1-amine Chemical compound C1=2C=C(OCCOC)C(OCCOC)=CC=2C=NCN1NC1=CC=CC(C#C)=C1C YVEQUSIQTPNUHB-UHFFFAOYSA-N 0.000 claims 1
- PPLYDLMRYZIHOR-UHFFFAOYSA-N n-(3-ethynyl-2-methylphenyl)-6,7-dimethoxyquinazolin-4-amine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1C PPLYDLMRYZIHOR-UHFFFAOYSA-N 0.000 claims 1
- FFNSJZNWHNDAKT-UHFFFAOYSA-N n-(3-ethynyl-4-fluorophenyl)-6,7-bis(2-methoxyethoxy)quinazolin-4-amine Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=C(F)C(C#C)=C1 FFNSJZNWHNDAKT-UHFFFAOYSA-N 0.000 claims 1
- UEKLAZGZLXRYAO-UHFFFAOYSA-N n-(3-ethynyl-4-fluorophenyl)-6,7-dimethoxyquinazolin-4-amine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(C#C)=C1 UEKLAZGZLXRYAO-UHFFFAOYSA-N 0.000 claims 1
- FKTOOVAYMNBBOM-UHFFFAOYSA-N n-(3-ethynylphenyl)-6,7-di(propan-2-yloxy)-2h-quinazolin-1-amine Chemical compound C1=2C=C(OC(C)C)C(OC(C)C)=CC=2C=NCN1NC1=CC=CC(C#C)=C1 FKTOOVAYMNBBOM-UHFFFAOYSA-N 0.000 claims 1
- PXVOMAUMUFQFKF-UHFFFAOYSA-N n-(3-ethynylphenyl)-7-nitroquinazolin-4-amine Chemical compound N=1C=NC2=CC([N+](=O)[O-])=CC=C2C=1NC1=CC=CC(C#C)=C1 PXVOMAUMUFQFKF-UHFFFAOYSA-N 0.000 claims 1
- OVBFNQKSLJYVCB-UHFFFAOYSA-N n-(4-ethynylphenyl)-6,7-dimethoxyquinazolin-4-amine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC=C(C#C)C=C1 OVBFNQKSLJYVCB-UHFFFAOYSA-N 0.000 claims 1
- XWLHBTJRHHRNQM-UHFFFAOYSA-N n-(5-ethynyl-2-methylphenyl)-6,7-dimethoxyquinazolin-4-amine Chemical compound C=12C=C(OC)C(OC)=CC2=NC=NC=1NC1=CC(C#C)=CC=C1C XWLHBTJRHHRNQM-UHFFFAOYSA-N 0.000 claims 1
- NPWROGXMBGWEJT-UHFFFAOYSA-N n-[4-(3-ethynylanilino)quinazolin-6-yl]methanesulfonamide Chemical compound C12=CC(NS(=O)(=O)C)=CC=C2N=CN=C1NC1=CC=CC(C#C)=C1 NPWROGXMBGWEJT-UHFFFAOYSA-N 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 208000025402 neoplasm of esophagus Diseases 0.000 claims 1
- 208000025440 neoplasm of neck Diseases 0.000 claims 1
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 229910000073 phosphorus hydride Inorganic materials 0.000 claims 1
- 125000005544 phthalimido group Chemical group 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000004546 quinazolin-4-yl group Chemical group N1=CN=C(C2=CC=CC=C12)* 0.000 claims 1
- 125000006413 ring segment Chemical group 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 208000013076 thyroid tumor Diseases 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 abstract 2
- 239000000651 prodrug Substances 0.000 abstract 2
- 150000003839 salts Chemical class 0.000 abstract 2
- 206010020772 Hypertension Diseases 0.000 abstract 1
Classifications
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
-
- 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
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- 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
- A61P35/00—Antineoplastic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
본 발명은 하기 일반식의 특정한 4-(치환된 페닐아미노)퀴나졸린 유도체, 그의 전구약물 및 약학적 허용 가능한 염에 관한 것이다.
일반식(Ⅰ)의 화합물, 그의 선구 약물 및 약학적으로 허용가능한 염은 과다중식 질병의 치료에 유용한다:
상기 식에서, R1, R2, R3, R4및 m및 n은 명세서에 개시된 바와 같다.
Description
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Claims (23)
- 하기 일반식의 화합물, 및 그의 약학적으로 허용가능한 염 및 전구약물:상기 식에서, m은 1, 2 또는 3이고; R1은 각각 수소, 할로, 하이드록시, 아미노, 하이드록시아미노, 카복시, (C1-C4)알콕시카보닐, 니트로, 구아니디노, 우레이도, 카바모닐, 시아노, 트리플루오로메틸, (R6)2N-카보닐 및 페닐-W-알킬(이때, W는 단일 결합, O, S 및 NH 중에서 선택된다) 중에서 독립적으로 선택되거나; 또는 R1은 각각 시아노 -(C1-C4)-알킬 및 R9중에서 독립적으로 선택되고, 이때 R9는 R5, R5O, (R6)2N, R7C(=O), R5ONH, A 및 R5Y로 구성된 그룹에서 선택되고, R5는 (C1-C4)일킬이고, R6은 수소 또는 R5이고(이때, R5는 동일하거나 상이하다) R7은 R5, R5O 또는 (R6)2N이고, A는 피페리디노-, 모르폴리노, 피롤리디노 및 4-R6-피페라진-1-일, 아미다졸-1-일, 4-피리돈-1-일, 카복시-(C1-C4)-알킬, 페녹시, 페닐, 페닐설파닐, (C2-C4)-알케닐 및 (R6)2-N-카보닐-(C1-C4)-알킬중에서 선택되고, Y는 S, SO 및 SO2중에서 선택되고, (R6)2N에서의 알킬 잔기는 할로 또는 R9(이때 R9는 상기 정의한 바와 같다)로 선택적으로 치환될 수 있고, R5및 R5O에서의 알킬잔기로 할로, R6O 또는 R9(이때 R9및 R6은 상기 정의된 바와 같다)로 선택적으로 치환되고, 이 결과로 생성된 그룹은 할로 또는 R9로 선택적으로 치환되고, 단, 질소, 산소 도는 황원자 및 다른 헤테로원자는 동일한 탄소원자에 부착될 수 없고, 또한 세개이상의 “R9” 단위는 R1을 포함할 수 없거나; 또는 R1은 각각 R5-설포닐아미노, 프탈이미도-(C1-C4)-알킬설포닐아미노, 벤즈아미도, 벤젠설포닐아미노, 3-페닐우레이도, 2-옥소피롤리딘-1-일, 2,5-디옥소피롤리딘-1-일 및 R10-(C2-C4)-알카노일아미노(이때, R10은 할로, R6O, (C2-C4)-알카노일옥시, R7C(=O) 및 (R6)2N에서 선택됨)중에서 독립적으로 선택되고; R1에서의 상기 벤즈아미도, 벤젠설포닐아미노, 페닐, 페녹시, 아닐리노, 페닐설파닐 치환제는 하나 또는 두개의 할로겐, (C1-C4)-알킬-시아노-메탄설포닐 또는 (C1-C4)-알콕시 치환체를 선택적으로 갖거나; 또는 R1중 임의의 두개는 이들이 부착되어 있는 탄소와 함께, 산소, 항 및 질소중에서 선택된 하나이상의 헤테로 원자를 포함하는, 5내지 8원고 고리를 포함하고; 상기 알킬 그룹, 및 알콕시 또는 알킬아미노 그룹중의 알킬 부분은 직쇄이거나, 또는 세개이상의 탄소를 포함한다면 분지되거나 또는 환상일수 있고; R2는 수소 및 선택적으로 치환된(C1-C6)-알킬중에서 선택되고; n은 1 또는 2이고; R3는 각각 수소, 선택적으로 치환된(C1-C6)-알킬, 선택적으로 치환된 아미노, 할로, 하이드록시, 선택적으로 치환된 하이드록시중에서 독립적으로 선택되고; R4는 아지도 또는 R11-에티닐(이때, R11은 수소, 선택적으로 치환된(C1-C6)-알킬중에서 선택되고, 이 치환체는 수소, 아미노, 하이드록시, R5O, R5NH 및 (R5)2N 중에서 선택됨)이다.
- 제1항에 있어서, R2가 수소이고 R4가 R11-에티닐이고, 이때, R11은 수소, 선택적으로 치환된(C1-C6)-알킬중에서 선택되고, 이 치환체는 수소, 아미노, 하이드록시, R5O, R5NH 및 (R5)2N 중에서 선택되는 화합물.
- 제2항에 있어서, m이 1 또는 2이고; R1은 각각 수소, 하이드록시, 아미노, 하이드록시아미노, 카복시, 니트로, 카바모일, 우레이도, 할로, R6O, HOC(=O),(R6)2NC(=O), A 및 (R6)2N로 선택적으로 치환된 R5; 할로, R6O, (C1-C4)-알카노일옥시 HOC(=O), (R6)2N, A, 페닐로 선택적으로 치환된 R5O; R5NH, (R5)2N, (R5)2NH, R5NHC(=O), (R5)2NC(=O), R5S, 페닐-(C2-C4)-알콕시, R12O(이때, R12는 HK(K는 할로, R6O, (C2-C4)-알카노일옥시, HOC(=O), A 및 (R5)2N으로 선택적으로 치환된 (C2-C4)-알킬), R6OKO, R6OKNH, CN 및 페닐); 할로로 선택적으로 치환된 R5NH, (C2-C4)-알카노일옥시, R6O, R7C(=O), (R6)2N, A, R6OKNH, R6OKNH, C6H5Y, CN; (R5)2NC(=O), R5ONH, R5S, (C1-C4)-알킬설포SLF아미노, 프탈아미도-(C1-C4)-알킬설포닐아미노, 3-페닐우레이도, 2-옥소피롤리딘-1-일, 2,5-디옥소피롤리딘-1-일, 할로-(C2-C4)-알카노일아미노, 하이드록시-(C2-C4)-알카노일아미노, (C2-C4)-알카노일옥시-(C2-C4)-알카노일아미노, (C1-C4)-알콕시-(C2-C4)-알카노일아미노, 카복시-(C2-C4)-알카노일아마노, (C1-C4)-알콕시카보닐-(C2-C4)-알카노일아미노, 카바모일-(C2-C4)-알카노일아미노, N-(C1-C4)-알킬카바모일-(C2-C4)-알카노일아미노, N,N-디[(C1-C4)-알킬]카바모일-(C2-C4)-알카노일아미노, 아미노-(C2-C4)-알카노일아미노, (C1-C4)-알킬-아미노-(C2-C4)-알카노일아미노, 디-(C1-C4)-알킬-아미노-(C2-C4)-알카노일아미노중에서 독립적으로 선택되고, 이때, R1에서의 상기 페닐 또는 페녹시 또는 아닐리노 치환체는 하나 또는 두개의 할로겐, (C1-C4)-알킬 또는 (C1-C4)-알콕시 치환체를 선택적으로 가질 수 있고; 또는 임의의 두개의 R1은 그들이 부착되어 있은 탄소와 함께, 산소, 황 또는 질소중에서의 선택된 하나이상 또는 두개의 헤테로 원자를 포함하는, 5 내지 8원 고리를 포함하고; 상기 알킬 그룹, 및 알콕시 또는 알킬아미노 그룹의 알킬 부분은 직쇄이거나, 또는 세개이상의 탄소를 포함한다면 분지되거나 또는 환상일수 있고; 각 R3는 수소, 메틸, 아미노, 할로 및 하이드록시중에서 독립적으로 선택되고; R4는 R11이 수소인 R11-에티닐인 화합물.
- 제3항에 있어서, 각 R1은 수소, 하이드록시, 아미노, 하이드록시아미노, 니트로, 카바모일, 우레이도; 할로, R6O, HCO(=O),H2NC(=O)로 선택적으로 치환된 R5; 할로, R6O, (C2-C4)-알카노일옥시 HOC(=O), (R6)2N, A, 페닐로 선택적으로 치환된 R5O; R5NH, (R5)2N, R5NH2, (R5)2NH, R5NHC(=O), (R5)2NC(=O), R5S, 페닐-(C2-C4)-알콕시중에서, 독립적으로 선택할 수 있고; 이때, R1에서의 상기 페놀 치환체는 하나 또는 두개의 할로, R5또는 R5O 치환체를 가질고 있고; 또는 임의의 두개의 R1은 그들이 부착되어 있는 탄소와 함께 산소, 황 또는 질소중에서 선택된 하나이상 또는 두개의 헤테로 원자를 포함하는 5 내지 8원 고리를 포함하고; 이때 알킬 그룹, 및 알콕시 또는 알킬아미노 그룹의 알킬 부분은 직쇄이거나, 또는 세개이상의 탄소를 함유할 경우 분지되거나 환상일 수 있는 화합물.
- 제1항에 있어서, R2가 수소이고 R4가 이지도인 화합물.
- 제5항에 있어서, m이 1 또는 2이고; R1은 수소, 하이드록시, 아미노, 하이드록시아미노, 카복시, 니트로, 카바모일, 우레이도, 할로로 선택적으로 치환된 R5, R6O, HOC(=O), (R6)2NC(=O), A 및 (R6)2N; 할로, R6O, HOC(=O), (R6)2NC(=O), A 및 (R6)2N으로 선택적으로 치환된 R5; R12O, (이때, R12는HK(K는 할로, R6O, (C2-C4)-알카노일옥시, HOC(=O), A 및 (R6)2N으로 선택적으로 치환된 (C2-C4)-알킬) R5OKO, R5OKNH, CN 및 페닐); 할로로 선택적으로 치환된 R5NH, (C2-C4)-알카노일옥시, R6O, R7C(=O), (R5)2N, A, R6OKO, R6OKNH, C6H5Y, CN; (R5)2NC(=O), R5ONH, R5S, (C1-C4)-알킬설포니아미노, 프탈아미도-(C1-C4)-알킬설포닐아미노, 3-페닐우레이도, 2-옥소피롤리딘-1-일, 2,5-디옥소피롤리딘-1-일, 할로-(C2-C4)-알카노일아미노, 하이드록시-(C2-C4)-알카노일아미노, (C2-C4)-알카노일옥시-(C2-C4)-알카노일아미노, (C1-C4)-알콕시-(C2-C4)-알카노일아미노, 카복시-(C2-C4)-알카노일아마노, (C1-C4)-알콕시카보닐-(C2-C4)-알카노일아미노, 카바모일-(C2-C4)-알카노일아미노, N-(C1-C4)-알킬카바모일-(C2-C4)-알카노일아미노, N,N-디[(C1-C4)-알킬]카바모일-(C2-C4)-알카노일아미노, 아미노-(C2-C4)-알카노일아미노, (C1-C4)-알킬-아미노-(C2-C4)-알카노일아미노, 디-(C1-C4)-알킬-아미노-(C2-C4)-알카노일아미노중에서 독립적으로 선택되고, 이때, R1에서의 상기 페닐 또는 페녹시 또는 아닐리노 치환체는 하나 또는 두개의 할로겐, (C1-C4)-알킬 또는 (C1-C4)-알콕시 치환체를 선택적으로 가질 수 있고; 또는 임의의 두개의 R1은 그들이 부착되어 있은 탄소와 함께, 산소, 황 또는 질소중에서의 선택된 하나이상 또는 두개의 헤테로 원자를 포함하는, 5 내지 8원 고리를 포함하고; 상기 알킬 그룹, 및 알콕시 또는 알킬아미노 그룹의 알킬 부분은 직쇄이거나, 또는 세개이상의 탄소를 포함한다면 분지되거나 또는 환상일수 있고; 각 R3는 수소, 메틸, 에틸, 아미노, 할로 및 하이드록시중에서 독립적으로 선택되는 화합물.
- 제6항에 있어서, 각 R1은 소수, 하이드록시, 아미노, 하이드록시아미노, 니트로, 카바모일, 우레이도; 할로, R6O, HCO(=O),H2NC(=O)로 선택적으로 치환된 R5; 할로, R6O, (C2-C4)-알카노일옥시 HOC(=O), (R6)2N, A, 페닐로 선택적으로 치환된 R5O; R5NH, (R5)2N, R5NH2, (R5)2NH, R5NHC(=O), (R5)2NC(=O), R5S, 페닐-(C2-C4)-알콕시중에서, 독립적으로 선택할 수 있고; 이때, R1에서의 상기 페놀 치환체는 하나 또는 두개의 할로, R5또는 R5O 치환체를 가질고 있고; 또는 임의의 두개의 R1은 그들이 부착되어 있는 탄소와 함께 산소, 황 또는 질소중에서 선택된 하나이상 또는 두개의 헤테로 원자를 포함하는 5 내지 8원 고리를 포함하고; 이때 알킬 그룹,및 알콕시 또는 알킬아미노 그룹의 알킬 부분은 직쇄이거나, 또는 세개이상의 탄소를 함유할 경우 분지되거나 환상일 수 있는 화합물.
- 제7항에 있어서, R3가 할로이고 R1가 수소 또는 R5O인 화합물.
- 제8항에 있어서, R5가 메틸인 화합물.
- 제1항에 있어서, (6,7-디메톡시퀴나졸린-4-일)-(3-에티닐메닐)-아민; (6,7-디메톡시퀴나졸린-4-일)-[3-(3'-하이드록시프로핀-1-일)페닐]-아민; [3-2'-(아미노메틸)-에티닐)-페닐]-(6,7-디메톡시퀴나졸린-4-일)-아민; [(3-에티닐페닐)-(6-니트로퀴나졸린-4-일)-아민; (6,7-디메톡시퀴나졸린-4-일)-(4-에티닐페닐)-아민; (6,7-디메톡시퀴나졸린-4-일)-(3-에티닐-2-메틸페닐)-아민; (6,7-디메톡시퀴나졸린-4-일)-(3-에티닐페닐)-아민; (3-에티닐페닐)-(6-메탄설포닐아미노퀴나졸린-4-일);-아민; (3-에티닐페닐)-(6,7-메틸렌디옥시노퀴나졸-4-일)-아민; (6,7-디메톡시퀴나졸린-4-일)-(3-에티닐-6-메틸페닐)-아민; (3-에티닐페닐)-(7-니트로퀴나졸린-4-일)-아민; (3-에티닐페닐)-[6-(4'-톨루엔설포닐아미노)-퀴나졸린-4-일]-아민; (3-에티닐페닐)-{6-[2'-프탈이미도-에트-1'-일-설포닐아미도]퀴나졸린-4-일}-아민; (3-에티닐페닐)-(6-구아니디노퀴나졸린-4-일)-아민; (7-아미노퀴나졸린-4-일)-(3-에티닐페닐)-아민; (3-에티닐페닐)-(7-카보메톡시퀴나졸린-4-일)-(3-에티닐페닐)-아민; [6,7-비스(2-메톡시에톡시)퀴나졸린-4-일]-(3-에티닐페닐)아민; (3-아지도페닐)-(6,7-디메톡시퀴나졸-4-일)-아민; (3-아지도-5-클로로페닐)-(6,7-디메톡시퀴나졸린-4-일)-아민; (4-아지도페닐)-(6,7디메톡시퀴나졸린-4-일)아민; (3-에티닐페닐)-(6-메틴설포닐-퀴나졸릴-4-일)-아민; (6-에틴설파닐-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6,7-디메톡시-퀴나졸린-4-일)-(3-에티닐-4-플루오로-페닐)-아민; (6,7-디메톡시-퀴나졸린-4-일)-[3-프로핀-1'-일-페닐]-아민; [6,7-비스-(2-메톡시-에톡시)-퀴나졸린-4-일]-(5-에티닐-3-메틸-페닐)-아민; [6,7-비스-(2-메톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-4-플루오로-페닐)-아민; [6,7-비스-(2-클로로-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)-아민; [6-(2-클로로-에톡시)-7-(2-메톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)-아민; [6,7-비스-(2-아세톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)-아민; 2-[4-(3-에티닐-페닐아미노)-7-(2-하이드록시-에톡시)-퀴나졸린-6-일옥시]-에탄올; [6-(2-아세톡시-에톡시)-7-(2-메톡시-에톡시)-퀴나졸린-4-일](3-에티닐-페닐)-아민; [7-(2-클로로-에톡시)-6-(2-메톡시-에톡시)-퀴나졸린-4-일](3-에티닐-페닐)-아민; [7-(2-아세톡시-에톡시)-6-(2-메톡시-에톡시)-퀴나졸린-4-일](3-에티닐-페닐)-아민; 2-[4-(3-에티닐-페닐아미노)-6-(2-하이드록시-에톡시)-퀴나졸린-7-일옥시]-에탄올; 2-[4-(3-에티닐-페닐아미노)-7-(2-메톡시-에톡시)-퀴나졸린-6-일옥시]-에탄올; 2-[4-(3-에티닐-페닐아미노)-6-(2-메톡시-에톡시)-퀴나졸린-7-일옥시]-에탄올; [6-(2-아세톡시-에톡시)-7-(2-메톡시-에톡시)-퀴나졸린-4-일]-(3-에티닐-페닐)-아민; (3-에티닐-페닐)-{6-(2-메톡시-에톡시)-7-[2-(4-메틸-피페라진-1-일)-에톡시]-퀴나졸린-4-일}-아민; (3-에티닐-페닐)-[7-(2-메톡시-에톡시)-6-(2-모르폴린-4-일)-에톡시)-퀴나졸린-4-일]-아민; (6,7-디에톡시퀴나졸린-1-일)-(3-에티닐페닐)-아민; (6,7-디에톡시퀴나졸린-1-)-(3-에티닐페닐)-아민; (6,7-디이소프로폭시퀴나졸린-1-일)-(3-에티닐페닐)-아민; (6,7-디에톡시퀴나졸린-1-일)-(3-에티닐페닐-2-메틸-페닐)-아민; [6,7-비스-(2-메톡시-에톡시)-퀴나졸린-1-일]-(3-에티닐-2-메틸-페닐)-아민; (3-에틸닐페닐)-[6-(2-하이드록시-에톡시)-7-(2-메톡시-에톡시)-퀴나졸린-1-일]-아민; [6,7-비스-(2-하이드록시-에톡시)-퀴나졸린-1-일]-(3-에티닐-페닐)-아민; 및 2-[4-(3-에티닐-페닐아미노)-6-(2-메톡시-에톡시)-퀴나졸린-7-일옥시]-에탄올로 이루어진 그룹에서 선택된 화합물.
- 제1항에 있어서, (6,7-(디프로폭시-퀴나졸린-4-일)-(3-에티닐-페닐)-아민; (6,7-(디에톡시-퀴나졸린-4-일)-(3-에티닐-5-플루오로-페닐)-아민; (6,7-(디에톡시-퀴나졸린-4-일)-(3-에티닐-4-플루오로-페닐)-아민; (6,7-(디에톡시-퀴나졸린-4-일)-(5-에티닐-2-메틸-페닐)-아민; (6,7-(디에톡시-퀴나졸린-4-일)-(3-에티닐-4-메틸-페닐)-아민; (6-아미노메틸-7-메톡시-퀴나졸린-4-일)-(3-에티닐-페닐)-아민; (6-아미노메틸-7-메톡시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐메틸-7-메톡시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐에틸-7-메톡시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐메틸-7-에톡시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐에틸-7-에톡시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐메틸-7-이소프로폭시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐메틸-7-프로톡시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐메틸-7-메톡시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; (6-아미노카보닐메틸-7-이소프로폭시-퀴나졸린-4-일)-(3-에티닐페닐)-아민; 및 (6-아미노카보닐메틸-7-프로폭시-퀴나졸린-4-일)-(3-에티닐페닐)-아민으로 구성된 그룹에서 선택된 화합물.
- 제1항에 있어서, (6,7-(디에톡시귀나졸린-1-일)-(3-에티닐페닐)-아민; (3-에티닐페닐)-[6-(2-하이드록시-에폭시)-7-(2-메톡시-에톡시)-퀴나졸린-1-일]-아민; [6,7-비스-(2-하이드록시-에폭시)-퀴나졸린-1-일]-(3-에티닐페닐)-아민; [6,7-비스-(2-메톡시-에폭시)-퀴나졸린-1-일]-(3-에티닐페닐)-아민; [6,7-디메톡시퀴나졸린-1-일]-(3-에티닐페닐)-아민; (3-에티닐페닐)-(6-메탄설포닐아미노-퀴나졸린-1-일]-아민; (3-에티닐페닐)-(6-아미노-퀴나졸린-1-일)-(3-에티닐페닐)-아민으로 구성된 그룹에서 선택된 화합물.
- a) 일반식(여기서, R1및 m은 하기 정의한 바와 같다)의 화합물을, 불활성 중합체상에 선택적으로 지지된 일반식 Ar3P(이때, 각 Ar은 선택적으로 치환된 (C6-C10)-아릴 그룹이다)의 선택적으로 치환된 트리아릴포스핀 및 CC14로 처리하는 단계 (각각의 치환체는 (C1-C6)-알킬로부터 독립적으로 선택됨); 및 b) 단계 a)의 생성물을 일반식(여기서, R2 ,R3및 n은 하기 정의한 바와 같고, J가 Y 또는 R4이고, 이때, R4는 하기 정의한 바와 같고, 단 J는 Y이면 b) 단계의 생성물을 알킨으로 추가로 처리해야한다)의 화합물로 처리하는 단계를 포함하는 하기 일반식(Ⅰ)의 화합물의 제조방법:상기 식에서, m은 1, 2 또는 3이고; R1은 각각 수소, 할로, 하이드록시, 아미노, 하이드록시아미노, 카복시, (C1-C4)-알콕시카보닐, 니트로, 구아니디노, 우레이도, 카바모일, 시아노, 트리플루오로메틸, (R6)2N-카보닐 및 페닐-W-알킬(이때, W는 단일 결합, O, S 및 NH임) 중에서 독립적으로 선택되거나; 또는 R1은 시아노 -(C1-C4)-알킬 및 R9중에서 독립적으로 선택되고, 이때 R9는 R5, R5O, (R6)2N, R7C(=O), R5ONH, A 및 R5Y로 구성된 그룹에서 선택되고; 이때 R5는 (C1-C4)일킬이고; R6은 수소 또는 R5이고(이때, R5는 동일하거나 상이함) R7은 R5, R5O 또는 (R6)2N이고; A는 피페리디노-, 모르폴리노, 피롤리디노 및 4-R6-피페라진-1-일, 아미다졸-1-일, 4-피리돈-1-일, 카복시-(C1-C4)-알킬, 페녹시, 페닐, 페닐설파닐, (C2-C4)-알케닐, (R6)2-N-카보닐-(C1-C4)-알킬이고; 및 Y는 S, SO, SO2에서 선택되고; (R6)2N에서의 알킬 잔기는 할로 또는 R9로 선택적으로 치환될 수 있고, 이때, R9는 상기와 같고 정의되고, R5및 R6O에서의 알킬잔기는 할로, R6O 또는 R9로 선택적으로 치환되고, 이때 R9및 R6은 상기 정의된 바와 같고, 이때 결과로 생성된 그룹은 할로 또는 R9로 선택적으로 치환될 수 있고, 단, 질소, 산소 또는 황원자 및 다른 헤테로 원자는 동일한 탄소 원자에 부착될 수 없고, 또한 세개이상의 “R9”단위는 R1을 포하할 수 없고; 또는 각 R1은 R5-설포닐아미도, 프탈이미도-(C1-C4)-알킬설포닐아미노, 벤즈아미노, 벤젠설포닐아미노, 3-페닐우레이도, 2-옥소피롤리딘-1-일, 2,5-디옥소피롤리딘-1-일 및 R10-(C2-C4)-알카노닐아미노(이때, R10은 할로, R6O, (C2-C4)-알카노일옥시, R7C(=O) 및 (R6)2N에서 선택)중에서 독립적으로 선택되고; R1에서의 상기 벤즈아미도 또는 벤젤설포닐아미노 또는 페닐 또는 페닐 또는 페녹시 또는 아닐리노 또는 페닐설파닐 치환체는 하나 또는 두개의 할로겐, (C1-C4)-알킬, 시아노, 메탄설포닐 또는 (C1-C4)-알콕시 치환체를 선택적으로 갖거나; 임의의 두개의 R1은 그들이 부착되어 있는 탄소와 함께, 산소, 황 또는 질소중에서 또는 알킬아미노 그룹의 알킬 부분은 직쇄이거나, 또는 세개이상의 탄소를 포함한다면 분지되거나 또는 환상일수 있고; R2는 수소 및 선택적으로 치환된(C1-C4)-알킬중에서 선택되고; n은 1 또는 2이고 각 R3는 수소, 선택적으로 치환된(C1-C4)-알킬, 선택적으로 치환된 아미노, 할로, 하이드록시 선잭적으로 치환된 하이드록시 중에서 독립적으로 선택되고; R4는 아지도 또한 R11-에티닐(이때, R11은 수소, 선택적으로, 치환된 (C1-C6)-알킬중에서 선택되고, 치환체는 수소, 아미노, 하이드록시, R5O, R5NH 및 (R5)2N 중에서 선택됨)이다.
- 제13항에 있어서, 각 아릴 구룹이 페닐, 나프틸-1-일 및 나프트-2-일으로부터 선택되는 방법.
- 제14항에 있어서, 각 아릴 그룹이 0 내지 최대수의 (C1-C6)알킬 그룹으로 독립적으로 치환되는 방법.
- 제14항에 있어서, 각 Ar이 페닐인 방법.
- 제13항에 있어서, 상기 트리아릴포스핀이 불활성 중합체에 지지된 방법.
- 제17항에 있어서, 상기 중합체가 스티렌의 디비닐벤젠-가교된 중합체인 방법.
- 포유동물의 과다증식 질환이 치료에 효과적인 양의 제1항의 화합물 및 약학적으로 허용가능한 담체를 포함하는, 포유동물의 상기 질환 치료용 약학 조성물.
- 제19항에 있어서, 과다증식 질환이 암인 약학 조성물.
- 제20항에 있어서, 상기 질병이 뇌, 폐, 인상 세포, 방광, 위, 췌장, 유방, 머리, 목, 식도, 부인과 또는 갑상선 종양인 약학 조성물.
- 제19항에 있어서, 과다증식 질환이 암이외의 질환인 약학 조성물.
- 제22항에 있어서, 상기 질환이 피부 또는 전립선의 양성 과형성인 약학 조성물.※ 참고사항 : 최초출원 내용에 의하여 공개하는 것임.
Applications Claiming Priority (6)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US41330095A | 1995-03-30 | 1995-03-30 | |
US8/413300 | 1995-03-30 | ||
US08/413,300 | 1995-03-30 | ||
PCT/IB1995/000436 WO1996030347A1 (en) | 1995-03-30 | 1995-06-06 | Quinazoline derivatives |
WOPCT/IB95/00436 | 1995-06-06 | ||
USPCT/IB95/00436 | 1995-06-06 |
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