HUP0004624A2 - Farnezil-transzferáz inhibitort és HMG CoA reduktáz inhibitort tartalmazó gyógyászati készítmények rák és sejtburjánzás kezelésére - Google Patents
Farnezil-transzferáz inhibitort és HMG CoA reduktáz inhibitort tartalmazó gyógyászati készítmények rák és sejtburjánzás kezeléséreInfo
- Publication number
- HUP0004624A2 HUP0004624A2 HU0004624A HUP0004624A HUP0004624A2 HU P0004624 A2 HUP0004624 A2 HU P0004624A2 HU 0004624 A HU0004624 A HU 0004624A HU P0004624 A HUP0004624 A HU P0004624A HU P0004624 A2 HUP0004624 A2 HU P0004624A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- atom
- alkyl
- substituents
- phenyl
- Prior art date
Links
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 title abstract 2
- 206010028980 Neoplasm Diseases 0.000 title abstract 2
- 201000011510 cancer Diseases 0.000 title abstract 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 title abstract 2
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 title 1
- 239000003528 protein farnesyltransferase inhibitor Substances 0.000 title 1
- -1 cyano- Chemical class 0.000 abstract 11
- 125000001424 substituent group Chemical group 0.000 abstract 5
- 125000000217 alkyl group Chemical group 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- 125000005843 halogen group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000003670 adamantan-2-yl group Chemical group [H]C1([H])C(C2([H])[H])([H])C([H])([H])C3([H])C([*])([H])C1([H])C([H])([H])C2([H])C3([H])[H] 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 229910052731 fluorine Inorganic materials 0.000 abstract 2
- 125000001153 fluoro group Chemical group F* 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 2
- 238000002360 preparation method Methods 0.000 abstract 2
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 abstract 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 abstract 1
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 abstract 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical group [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 abstract 1
- 101100439662 Arabidopsis thaliana CHR5 gene Proteins 0.000 abstract 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical group [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 229910052801 chlorine Inorganic materials 0.000 abstract 1
- 125000001309 chloro group Chemical group Cl* 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 229910052740 iodine Inorganic materials 0.000 abstract 1
- 125000001624 naphthyl group Chemical group 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 230000002062 proliferating effect Effects 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
-
- 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
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
A találmány tárgyát rák vagy jóindulatú burjánzásos rendellenességekkezelésére adható gyógyászati készítmények képezik, a- melyekkészítmények FTáze inhibitort és HMG CoA reduktáz inhibitort, valamintgyógyászatilag megfelelő vivőanyagot tartalmaznak. A készítményekFTáze inhibitorként valamely (I), (IIA), (IIB), (III) általánosképletű vegyületet vagy (IV) képletű vegyületet vagy e vegyületekgyógyászatilag megfelelő sóját tartalmazzák. A vegyületek képletében aszubsztituensek jelentése igen sokféle, így például R1 és R2 jelentéseegymástól függetlenül -(CH2)P-(5-10 tagú heterociklusos) csoport, -(CH2)P-(6-10 szénatomos aril)-, allil-, propargil- vagy 1-6 szénatomosalkilcsoport, ahol p értéke 0, 1, 2 vagy 3, ahol az alkilcsoport,továbbá az R1 és R2 helyében álló alkilcsoportok adott esetben egy-három R9 szubsztituenst hordozhatnak, és ahol az R1 és R2 helyébenálló aril- és heterociklusos csoportok adott esetben egy-háromszubsztituenst hordozhatnak halogénatom és R9 közül választva; R3jelentése -(CH2)m-(1- vagy 2-adamantil), -(CH2)m-(3-10 szénatomoscikloalkil), -(CH2)m-(6-10 szénatomos aril), 1-10 szénatomosalkilcsoport, ahol m értéke 0 vagy 1-től 6-ig terjedő egész szám, ahola fentiekben említett cikloalkil- és alkilcsoportok adott esetben egyvagy kettő kettős vagy hármas kötést tartalmazhatnak; a (IIA) és (IIB)általános képletekben R1 jelentése hidrogénatom, halogénatom, mintklóratom, fluoratom, brómatom vagy jódatom, ciano-, hidroxil-, nitro-,trifluor-metil-csoport, -NHR5, -NR5R5, R5, -OR5 vagy -S(O)m-R5általános képletű csoport; R2 jelentése -(CH2)n-Y vagy -OCOR5általános képletű csoport; R3 jelentése 4-, 3- vagy 2-piridil-,pirimidil-, pirazinil-, 2-fluor-4-piridil- vagy 3-fluor-4-piridil-csoport; R4 jelentése 1-adamantil- vagy 2-adamantil-csoport; Yjelentése hidrogénatom, hidroxil-, amino-, cianocsoport, -NHR5, -NR5R5, -NHCOR5, -NHCO2R5 csoport, halogénatom, -OR5, -S(O)mR5, -CO2H,-CO2R5, -CONR5R5, -CONHR5, -CONH2, -COR5, -CH=CHCO2R5, -OCOR5 csoport,fenil-, továbbá W-vel szubsztituált fenilcsoport, -C<CCO2R5, -CH=CHR5vagy -C<CR5; a (III) általános képletben a szaggatott vonalakjelentése adott esetben jelenlévő kettős kötés; Z jelentése oxigénatomvagy kénatom, amennyiben Z az A gyűrűhöz kettős kötéssel kapcsolódik,és Z jelentése hidroxil-,1-10 szénatomos alkil-S-, 1-10 szénatomosalkil-SO-, 1-10 szénatomos alkil-SO2, adamant-2-il-S-, naftil-S-,benzil-S-, fenil--C(=O)CH2S-, (1-6 szénatomos alkil)-O-C(=O)-CH2S-vagy (H,H), vagyis Z jelentése két hidrogénatom, amelyek az A gyűrűbenlévő azonos szénatomhoz kapcsolódnak, amennyiben Z egyes kötésselkapcsolódik az A gyűrűhöz, és ahol a naftil- és fenil-, valamint abenzilcsoportban lévő fenilcsoport adott esetben egy-háromszubsztituenst hordozhat, ahol szubsztituensként jelen lehet egymástólfüggetlenül adott esetben egy-három fluoratommal szubsz
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US4963897P | 1997-06-16 | 1997-06-16 | |
| PCT/IB1998/000881 WO1998057633A1 (en) | 1997-06-16 | 1998-06-05 | FARNESYL TRANSFERASE INHIBITORS IN COMBINATION WITH HMG CoA REDUCTASE INHIBITORS FOR THE TREATMENT OF CANCER |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0004624A2 true HUP0004624A2 (hu) | 2001-10-28 |
| HUP0004624A3 HUP0004624A3 (en) | 2002-11-28 |
Family
ID=21960890
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0004624A HUP0004624A3 (en) | 1997-06-16 | 1998-06-05 | Farnesyl transferase inhibitors in combination with hmg coa reductase inhibitors for the treatment of cancer |
Country Status (37)
| Country | Link |
|---|---|
| EP (1) | EP0986387B1 (hu) |
| JP (1) | JP3713051B2 (hu) |
| KR (1) | KR100392573B1 (hu) |
| CN (1) | CN1259868A (hu) |
| AP (1) | AP9801261A0 (hu) |
| AR (1) | AR013090A1 (hu) |
| AT (1) | ATE235905T1 (hu) |
| BG (1) | BG103946A (hu) |
| BR (1) | BR9810616A (hu) |
| CA (1) | CA2294399C (hu) |
| CO (1) | CO4950607A1 (hu) |
| DE (1) | DE69812933T2 (hu) |
| DK (1) | DK0986387T3 (hu) |
| DZ (1) | DZ2518A1 (hu) |
| EA (1) | EA199901043A1 (hu) |
| ES (1) | ES2196559T3 (hu) |
| GT (1) | GT199800081A (hu) |
| HN (1) | HN1998000091A (hu) |
| HR (1) | HRP980328B1 (hu) |
| HU (1) | HUP0004624A3 (hu) |
| ID (1) | ID23014A (hu) |
| IL (1) | IL132765A0 (hu) |
| IS (1) | IS5259A (hu) |
| MA (1) | MA24569A1 (hu) |
| NO (1) | NO996206L (hu) |
| NZ (1) | NZ500662A (hu) |
| OA (1) | OA11231A (hu) |
| PA (1) | PA8453601A1 (hu) |
| PE (1) | PE82899A1 (hu) |
| PL (1) | PL337651A1 (hu) |
| PT (1) | PT986387E (hu) |
| SK (1) | SK169699A3 (hu) |
| TN (1) | TNSN98088A1 (hu) |
| TR (1) | TR199903074T2 (hu) |
| UA (1) | UA57081C2 (hu) |
| WO (1) | WO1998057633A1 (hu) |
| ZA (1) | ZA985182B (hu) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1077949A2 (en) | 1998-05-12 | 2001-02-28 | Warner-Lambert Company | Combinations of protein farnesyltransferase and hmg coa reductase inhibitors and their use to treat cancer |
| AU6256499A (en) * | 1998-09-24 | 2000-04-10 | Merck & Co., Inc. | A method of treating cancer |
| EP1006113A1 (en) | 1998-12-02 | 2000-06-07 | Pfizer Products Inc. | Derivatives of 2-(2-oxo-ethylidene)-imidazolidin-4-one and their use to inhibit abnormal cell growth |
| AU4988100A (en) * | 1999-05-07 | 2000-11-21 | Brigham And Women's Hospital | Use of hmgcoa reductase inhibitors in the prevention of diseases whose pathogenesis is dependent on neovascularization |
| US6710058B2 (en) | 2000-11-06 | 2004-03-23 | Bristol-Myers Squibb Pharma Company | Monocyclic or bicyclic carbocycles and heterocycles as factor Xa inhibitors |
| CA2432137C (en) | 2000-12-19 | 2010-12-21 | Pfizer Products Inc. | Crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3h-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1h-quinolin-2-one, 2,3-dihydroxybutanedioate salts and method of production |
| JP4092203B2 (ja) | 2000-12-21 | 2008-05-28 | ニトロメッド，インク． | 新規のシクロオキシゲナーゼ２選択的阻害剤としての置換アリール化合物、組成物、および使用方法 |
| US20020151563A1 (en) * | 2001-03-29 | 2002-10-17 | Pfizer Inc. | Farnesyl transferase inhibitors in combination with HMG CoA reductase inhibitors for the inhibition of abnormal cell growth |
| US6740757B2 (en) | 2001-08-29 | 2004-05-25 | Pfizer Inc | Enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3h-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1h-quinolin-2-one and salts thereof, useful in the treatment of cancer |
| JP2005200419A (ja) * | 2004-01-16 | 2005-07-28 | National Health Research Inst | 癌治療法 |
| US8168667B2 (en) | 2006-05-31 | 2012-05-01 | Galapagos Nv | Imidazolidine derivatives, uses therefor, preparation thereof and compositions comprising such |
| GB2463514C (en) | 2008-09-11 | 2018-09-26 | Galapagos Nv | Imidazolidine compounds and uses therefor |
Family Cites Families (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6083985A (en) * | 1995-08-09 | 2000-07-04 | Banyu Pharmaceutical Co., Ltd. | Medicinal composition |
-
1998
- 1998-05-06 UA UA99126842A patent/UA57081C2/uk unknown
- 1998-06-05 EA EA199901043A patent/EA199901043A1/ru unknown
- 1998-06-05 SK SK1696-99A patent/SK169699A3/sk unknown
- 1998-06-05 TR TR1999/03074T patent/TR199903074T2/xx unknown
- 1998-06-05 BR BR9810616-3A patent/BR9810616A/pt not_active Application Discontinuation
- 1998-06-05 WO PCT/IB1998/000881 patent/WO1998057633A1/en not_active Application Discontinuation
- 1998-06-05 CN CN98805968A patent/CN1259868A/zh active Pending
- 1998-06-05 EP EP98921688A patent/EP0986387B1/en not_active Expired - Lifetime
- 1998-06-05 NZ NZ500662A patent/NZ500662A/en unknown
- 1998-06-05 IL IL13276598A patent/IL132765A0/xx unknown
- 1998-06-05 JP JP50403099A patent/JP3713051B2/ja not_active Expired - Fee Related
- 1998-06-05 HU HU0004624A patent/HUP0004624A3/hu unknown
- 1998-06-05 ID IDW991597A patent/ID23014A/id unknown
- 1998-06-05 DK DK98921688T patent/DK0986387T3/da active
- 1998-06-05 KR KR10-1999-7011860A patent/KR100392573B1/ko not_active IP Right Cessation
- 1998-06-05 AT AT98921688T patent/ATE235905T1/de not_active IP Right Cessation
- 1998-06-05 ES ES98921688T patent/ES2196559T3/es not_active Expired - Lifetime
- 1998-06-05 DE DE69812933T patent/DE69812933T2/de not_active Expired - Fee Related
- 1998-06-05 CA CA002294399A patent/CA2294399C/en not_active Expired - Fee Related
- 1998-06-05 PT PT98921688T patent/PT986387E/pt unknown
- 1998-06-05 PL PL98337651A patent/PL337651A1/xx unknown
- 1998-06-09 HN HN1998000091A patent/HN1998000091A/es unknown
- 1998-06-11 AP APAP/P/1998/001261A patent/AP9801261A0/en unknown
- 1998-06-12 PE PE1998000500A patent/PE82899A1/es not_active Application Discontinuation
- 1998-06-12 AR ARP980102812A patent/AR013090A1/es unknown
- 1998-06-15 GT GT199800081A patent/GT199800081A/es unknown
- 1998-06-15 PA PA19988453601A patent/PA8453601A1/es unknown
- 1998-06-15 TN TNTNSN98088A patent/TNSN98088A1/fr unknown
- 1998-06-15 MA MA25114A patent/MA24569A1/fr unknown
- 1998-06-15 ZA ZA9805182A patent/ZA985182B/xx unknown
- 1998-06-15 DZ DZ980128A patent/DZ2518A1/xx active
- 1998-06-16 CO CO98034148A patent/CO4950607A1/es unknown
- 1998-06-16 HR HR980328A patent/HRP980328B1/xx not_active IP Right Cessation
-
1999
- 1999-11-19 IS IS5259A patent/IS5259A/is unknown
- 1999-12-03 BG BG103946A patent/BG103946A/bg unknown
- 1999-12-10 OA OA9900276A patent/OA11231A/en unknown
- 1999-12-15 NO NO996206A patent/NO996206L/no not_active Application Discontinuation
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