AR055209A1 - Derivados del indol, uso de los mismos para la preparacion de medicamentos, procedimientos para prepararlos y los medicamentos que los contienen - Google Patents
Derivados del indol, uso de los mismos para la preparacion de medicamentos, procedimientos para prepararlos y los medicamentos que los contienenInfo
- Publication number
- AR055209A1 AR055209A1 ARP010103614A ARP010103614A AR055209A1 AR 055209 A1 AR055209 A1 AR 055209A1 AR P010103614 A ARP010103614 A AR P010103614A AR P010103614 A ARP010103614 A AR P010103614A AR 055209 A1 AR055209 A1 AR 055209A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- mono
- unsubstituted
- alkoxy
- halogen
- Prior art date
Links
Classifications
-
- 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
- C07D401/12—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 linked by a chain containing hetero atoms as chain links
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
Abstract
Derivados de indol de la formula general (1) donde R significa H, alquilo C1-6 lineal o ramificado, alquilo C1-6 mono o polisustituido por arilo, donde el radical arilo puede estar insustituido o puede estar mono a pentasustituido, de igual manera o diferente, con halogeno, alquilo C1-6, cicloalquilo C3-7, carboxilo, alcoxicarbonilo C1-6, preferentemente butoxicarbonilo terciario, alquilo C1-6 lineal o ramificado sustituido con uno o varios átomos de F, preferentemente trifluorometilo, hidroxi, alcoxi C1-6 lineal o ramificado, preferentemente metoxi o etoxi; benciloxi, o aril-alquilo C1-6, donde el radical arilo puede estar insustituido o puede estar mono a pentasustituido, de igual manera o diferente, con alquilo C1-6, halogeno o alquilo C1-6 lineal o ramificado sustituido con uno o varios átomos de F, preferentemente trifluorometilo, alcoxi C1-6-alquilo C1-6 lineal o ramificado, aril-alquiloxicarbonilo C1-6 sustituido o insustituido, preferentemente benciloxicarbonilo, alquiloxicarbonilo C1-6 lineal o ramificado, alquilcarbonilo C1-6 lineal o ramificado, preferentemente acetilo, alquenilo C2-6, preferentemente alilo, alquinilo C2-6, preferentemente etinilo o propargilo, o ciano-alquilo C1-6 lineal o ramificado, preferentemente cianometilo; R1 significa un heterociclo C2-14 saturado, insaturado o aromático que contiene uno o varios heteroátomos seleccionados del grupo N, O y S que puede estar unido con el N amídico directamente o a través de un puente de alquilo C1-6, donde el radical alquilo C1-4 puede estar insustituido o puede estar mono o polisustituido, de igual manera o diferente, con alquilo C1-6, halogeno u oxo (=O) y el radical 2-, 4-, 5- o 6- pirimidinilo puede estar en cada caso insustituido o mono a trisustituido, de igual manera o diferente, con H, alquilo C1-6, halogeno, nitro, amino, mono-alquilamino C1-6, di-alquilamino C1-6, hidroxi, alcoxi C1-6, benciloxi, carboxi, alcoxicarbonilo C1-6, alcoxicarbonilamino C1-6 o alquilo C1-6 mono o polisustituido con F, preferentemente trifluorometilo, arilo C6-10, o aril C6-10-alquilo C1-6, con la condicion de que R1 no sea un 2- o 4- pirimidinilo insustituido o un radical 2- pirimidinilo mono o polisustituido con el grupo metilo; y salvo 2-, 3-, 4- y 8- quinolilo y 2-, 3-, y 4- quinolilmetilo insustituidos o sustituidos con alquilo C1-6, halogeno, nitro, amino, y alquilamino C1-6, donde los átomos de carbono del anillo de la parte del piridilmetilo están insustituidos o sustituidos con alquilo C1-6, alcoxi C1-6, nitro, amino, y alcoxicarbonilamino C1-6; R2 significa h, alquilo C1-6, alquilo C1-6 mono o polisustituido con halogeno, alquilo C1-6 mono o polisustituido con fenilo, donde el radical fenilo puede estar insustituido o puede estar mono a pentasustituido, de igual manera o diferente, con halogeno, preferentemente Cl, Br o I, alquilo C1-6, cicloalquilo C3-7, carboxilo, alcoxicarbonilo C1-6, alquilo C1-6 mono o polisustituido con halogeno, preferentemente trifluorometilo, hidroxi, alcoxi C1-6, preferentemente metoxi o etoxi, fenil-alcoxi C1-6, preferentemente benciloxi, nitro, amino, mono-alquilamino C1-6, di-alquilamino C1-6, mono-cicloalquilamino C3-6, di-cicloalquilamino C3-6, acilamino C1-6, fenil-alquilamino C1-6, arilcarbonilamino, heteroarilcarbonilamino, alquilsulfonamido C1-6, arilsulfonamido, maleinimido, succinimido, ftalimido, benciloxicarbonilamino (Z-amino), ter.-butoxicarbonilamino (BOC-amino), 9- fluorenilmetoxi-carbonilamino (Fmoc-amino), trifenilmetilamino (Tr-amino), 2-(4'-piridil)etoxicarbonilamino (Pyoc-amino), difenilmetilsilil-amino (DPMS-amino), con -NH-CH2-COOH; -NH-CH(CH3)-COOH; (CH3)2CH-CH2-CH2-CH(NH-)-COOH, H3C-CH2-CH(CH3)-CH(NH- )-COOH; HOH2C-CH(NH-)-COOH; fenil-CH2CH(N H-)-COOH, (4-imidazolil)-CH2-CH(NH-)-COOH, HN=C(NH2)-NH-(CH2)3-CH(NH-)-COOH, H2N-(CH2)4-CH(NH-)-COOH; H2N-CO-CH2-CH(NH-)-COOH, HOOC-(CH2)2-CH(NH-)-COOH; un radical 2-, 3-, 4-, 5-, 6-, 7-, y 8-quinolil- alquilo C1-6, donde el radical 2-, 3-, 4-, 5-, 6-, 7- y 8-quinolilo puede estar insustituido o puede estar mono o hexasustituido, de la misma manera o diferente, con halogeno, alquilo C1-4 o alcoxi C1-4; un radical 2-, 3- y 4-piridil-alquilo C1-6, donde el radical 2-, 3- y 4-piridilo puede estar insustituido puede estar mono a tetrasustituido, de igual manera o diferente, con halogeno, alquilo C1-4 o alcoxi C1-4; un radical arilcarbonilo, donde el radical arilo pude estar insustituido o puede estar mono a pentasustituido, de igual manera o diferente, co halogeno, alquilo C1-6, cicloalquilo C3-7, carboxilo, ciano, alcoxicarbonilo C1-6, alquilo C1-6 mono o polisustituido con átomos de F, preferentemente trifluorometilo, hidroxilo, alcoxi C1-4 preferentemente metoxi o etoxi, aril-alcoxi C1-4, preferentemente benciloxi; R3 y R4 pueden estar unidos a los átomos de C del indol C-2, C-4, C-5, C-6, o C-7 y pueden significar, independientemente entre sí, H, hidroxi, alquilo C1-6, cicloalquilo C3-7, alquilcarbonilo C1-6, alcoxi C1-6, halogeno, aril-alcoxi C1-4, preferentemente benciloxi, nitro, amino, mono-alquilamino C1-4, di-alquilamino C1-4, alcoxicarbonilamino C1-6, alcoxicarbonilamino C1-6-alquilo C1-6, ciano, ciano- alquilo C1-6 lineal o ramificado, carboxilo, alcoxicarbonilo C1-4, alquilo C1-4 mono o polisustituido con uno varios átomos de F, preferentemente grupo trifluorometilo, carboxi-alquilo C1-6 o alcoxicarbonil C1-6-alquilo C1-6; Z1 significa O o S o H unido en forma geminal e hidroxi; Z2 significa O o S; sus tautomeros, estereoisomeros, incluyendo los diastereomeros y enantiomeros, así como las sales fisiologicamente tolerables de los mismos. el uso de los compuestos de formula (1) para la preparacion de medicamentos, y el procedimiento para preparar dichos compuestos y los medicamentos que lo contienen. Los compuestos de formula (1) son utiles para tratar tumores en mamíferos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE10037310A DE10037310A1 (de) | 2000-07-28 | 2000-07-28 | Neue Indolderivate und deren Verwendung als Arzneimittel |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR055209A1 true AR055209A1 (es) | 2007-08-15 |
Family
ID=7650860
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010103614A AR055209A1 (es) | 2000-07-28 | 2001-07-27 | Derivados del indol, uso de los mismos para la preparacion de medicamentos, procedimientos para prepararlos y los medicamentos que los contienen |
Country Status (31)
| Country | Link |
|---|---|
| US (3) | US7365081B2 (es) |
| EP (3) | EP2163552A1 (es) |
| JP (1) | JP5113973B2 (es) |
| KR (1) | KR100810453B1 (es) |
| CN (1) | CN1215066C (es) |
| AR (1) | AR055209A1 (es) |
| AT (1) | ATE392420T1 (es) |
| AU (2) | AU2001289758B2 (es) |
| BG (1) | BG66457B1 (es) |
| BR (1) | BR0112807A (es) |
| CA (3) | CA2354210C (es) |
| CY (1) | CY1108770T1 (es) |
| CZ (1) | CZ304197B6 (es) |
| DE (2) | DE10037310A1 (es) |
| DK (1) | DK1309585T3 (es) |
| ES (1) | ES2303532T3 (es) |
| HK (1) | HK1058201A1 (es) |
| HU (1) | HU229254B1 (es) |
| IL (2) | IL153930A0 (es) |
| MX (1) | MXPA03000644A (es) |
| NO (1) | NO324594B1 (es) |
| NZ (1) | NZ524404A (es) |
| PL (1) | PL208673B1 (es) |
| PT (1) | PT1309585E (es) |
| RU (1) | RU2270196C9 (es) |
| SI (1) | SI1309585T1 (es) |
| SK (1) | SK288085B6 (es) |
| TW (1) | TWI291955B (es) |
| UA (1) | UA80670C2 (es) |
| WO (1) | WO2002010152A2 (es) |
| ZA (1) | ZA200300584B (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPS52155013A (en) | 1976-06-18 | 1977-12-23 | Hitachi Ltd | Image pickup unit |
| DE10037310A1 (de) * | 2000-07-28 | 2002-02-07 | Asta Medica Ag | Neue Indolderivate und deren Verwendung als Arzneimittel |
| JP2005504790A (ja) * | 2001-09-13 | 2005-02-17 | シンタ ファーマスーティカルズ コーポレイション | 癌を治療するための３−グリオキシリルアミドインドール |
| EP1484329A1 (de) * | 2003-06-06 | 2004-12-08 | Zentaris GmbH | Indolderivate mit Apoptose induzierender Wirkung |
| US7205299B2 (en) * | 2003-06-05 | 2007-04-17 | Zentaris Gmbh | Indole derivatives having an apoptosis-inducing effect |
| EP1641777A1 (de) * | 2003-06-05 | 2006-04-05 | Zentaris GmbH | Indolderivate mit apoptose induzierender wirkung |
| US7211588B2 (en) * | 2003-07-25 | 2007-05-01 | Zentaris Gmbh | N-substituted indolyl-3-glyoxylamides, their use as medicaments and process for their preparation |
| US20050124623A1 (en) | 2003-11-26 | 2005-06-09 | Bender John A. | Diazaindole-dicarbonyl-piperazinyl antiviral agents |
| US20060100432A1 (en) | 2004-11-09 | 2006-05-11 | Matiskella John D | Crystalline materials of 1-(4-benzoyl-piperazin-1-yl)-2-[4-methoxy-7-(3-methyl-[1,2,4]triazol-1-yl)-1H-pyrrolo[2,3-c]pyridin-3-yl]-ethane-1,2-dione |
| US8399666B2 (en) | 2005-11-04 | 2013-03-19 | Panmira Pharmaceuticals, Llc | 5-lipoxygenase-activating protein (FLAP) inhibitors |
| US7977359B2 (en) | 2005-11-04 | 2011-07-12 | Amira Pharmaceuticals, Inc. | 5-lipdxygenase-activating protein (FLAP) inhibitors |
| GB2431927B (en) | 2005-11-04 | 2010-03-17 | Amira Pharmaceuticals Inc | 5-Lipoxygenase-activating protein (FLAP) inhibitors |
| US7851476B2 (en) | 2005-12-14 | 2010-12-14 | Bristol-Myers Squibb Company | Crystalline forms of 1-benzoyl-4-[2-[4-methoxy-7-(3-methyl-1H-1,2,4-triazol-1-YL)-1-[(phosphonooxy)methyl]-1H-pyrrolo[2,3-C]pyridin-3-YL]-1,2-dioxoethyl]-piperazine |
| US7807671B2 (en) | 2006-04-25 | 2010-10-05 | Bristol-Myers Squibb Company | Diketo-piperazine and piperidine derivatives as antiviral agents |
| CA2660704A1 (en) | 2006-08-07 | 2008-02-14 | Ironwood Pharmaceuticals, Inc. | Indole compounds |
| JP5791500B2 (ja) | 2008-05-23 | 2015-10-07 | パンミラ ファーマシューティカルズ，エルエルシー． | ５−リポキシゲナーゼ活性化タンパク質阻害剤 |
| AR084433A1 (es) | 2010-12-22 | 2013-05-15 | Ironwood Pharmaceuticals Inc | Inhibidores de la faah y composiciones farmaceuticas que los contienen |
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| US5480883A (en) * | 1991-05-10 | 1996-01-02 | Rhone-Poulenc Rorer Pharmaceuticals Inc. | Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase |
| EP0775131A2 (de) * | 1994-08-03 | 1997-05-28 | ASTA Medica Aktiengesellschaft | Indol-, indazol-, pyridopyrrol- und pyridopyrazol-derivate mit antiasthmatischer, antiallergischer, entzündungshemmender und immunmodulierender wirkung |
| US5732113A (en) | 1996-06-20 | 1998-03-24 | Stanford University | Timing and frequency synchronization of OFDM signals |
| DE19636150A1 (de) * | 1996-09-06 | 1998-03-12 | Asta Medica Ag | N-substituierte Indol-3-glyoxylamide mit antiasthmatischer, antiallergischer und immunsuppressiver/immunmodulierender Wirkung |
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| EA003876B1 (ru) | 1998-02-25 | 2003-10-30 | Дженетикс Инститьют, Ллс | Ингибиторы фосфолипазных ферментов |
| WO1999046267A1 (en) | 1998-03-12 | 1999-09-16 | Novo Nordisk A/S | Modulators of protein tyrosine phosphatases (ptpases) |
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| AU5947399A (en) | 1998-04-27 | 1999-11-16 | Hoechst Marion Roussel Deutschland Gmbh | A new glucose-6-phosphate translocase inhibitor L 970885 from an actinomycete SP., and chemical derivatives thereof, a process for the preparation and theirv use as pharmaceuticals |
| EP1076657B1 (de) | 1998-04-28 | 2004-08-04 | elbion AG | Neue hydroxyindole, deren verwendung als inhibitoren der phosphodiesterase 4 und verfahren zu deren herstellung |
| CA2319174A1 (en) | 1998-06-08 | 1999-12-16 | Advanced Medicine, Inc. | Novel therapeutic agents that modulate 5-ht receptors |
| EP1087960B1 (en) | 1998-06-17 | 2011-03-23 | Eisai R&D Management Co., Ltd. | Macrocyclic analogs and methods of their use and preparation |
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| US6841685B2 (en) | 2000-06-07 | 2005-01-11 | State Of Oregon Acting By And Through The State Board Of Higher Education On Behalf Of Oregon State University | Methods for making bis-heterocyclic alkaloids |
| DE10035927A1 (de) * | 2000-07-21 | 2002-03-07 | Asta Medica Ag | Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel |
| IT1318641B1 (it) | 2000-07-25 | 2003-08-27 | Novuspharma Spa | Ammidi di acidi 2-(1h-indol-3-il)-2-oxo-acetici ad attivita'antitumorale. |
| DE10037310A1 (de) * | 2000-07-28 | 2002-02-07 | Asta Medica Ag | Neue Indolderivate und deren Verwendung als Arzneimittel |
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2000
- 2000-07-28 DE DE10037310A patent/DE10037310A1/de not_active Withdrawn
-
2001
- 2001-07-20 US US09/910,140 patent/US7365081B2/en not_active Expired - Fee Related
- 2001-07-26 SK SK222-2003A patent/SK288085B6/sk not_active IP Right Cessation
- 2001-07-26 WO PCT/EP2001/008644 patent/WO2002010152A2/de active IP Right Grant
- 2001-07-26 CA CA2354210A patent/CA2354210C/en not_active Expired - Fee Related
- 2001-07-26 SI SI200130834T patent/SI1309585T1/sl unknown
- 2001-07-26 EP EP09175005A patent/EP2163552A1/de not_active Withdrawn
- 2001-07-26 DK DK01969522T patent/DK1309585T3/da active
- 2001-07-26 CZ CZ2003-500A patent/CZ304197B6/cs not_active IP Right Cessation
- 2001-07-26 UA UA2003021677A patent/UA80670C2/uk unknown
- 2001-07-26 HU HU0300677A patent/HU229254B1/hu not_active IP Right Cessation
- 2001-07-26 AU AU2001289758A patent/AU2001289758B2/en not_active Ceased
- 2001-07-26 IL IL15393001A patent/IL153930A0/xx unknown
- 2001-07-26 CA CA2704691A patent/CA2704691A1/en not_active Abandoned
- 2001-07-26 MX MXPA03000644A patent/MXPA03000644A/es active IP Right Grant
- 2001-07-26 PT PT01969522T patent/PT1309585E/pt unknown
- 2001-07-26 RU RU2003105891/04A patent/RU2270196C9/ru not_active IP Right Cessation
- 2001-07-26 DE DE50113867T patent/DE50113867D1/de not_active Expired - Lifetime
- 2001-07-26 EP EP07123142A patent/EP1939195A1/de not_active Withdrawn
- 2001-07-26 BR BR0112807-8A patent/BR0112807A/pt not_active IP Right Cessation
- 2001-07-26 PL PL361356A patent/PL208673B1/pl unknown
- 2001-07-26 JP JP2002515883A patent/JP5113973B2/ja not_active Expired - Fee Related
- 2001-07-26 NZ NZ524404A patent/NZ524404A/en not_active IP Right Cessation
- 2001-07-26 AT AT01969522T patent/ATE392420T1/de active
- 2001-07-26 KR KR1020037001300A patent/KR100810453B1/ko not_active IP Right Cessation
- 2001-07-26 CA CA2704693A patent/CA2704693A1/en not_active Abandoned
- 2001-07-26 ES ES01969522T patent/ES2303532T3/es not_active Expired - Lifetime
- 2001-07-26 CN CNB018143180A patent/CN1215066C/zh not_active Expired - Fee Related
- 2001-07-26 EP EP01969522A patent/EP1309585B1/de not_active Expired - Lifetime
- 2001-07-26 AU AU8975801A patent/AU8975801A/xx active Pending
- 2001-07-27 AR ARP010103614A patent/AR055209A1/es unknown
- 2001-08-07 TW TW090118479A patent/TWI291955B/zh not_active IP Right Cessation
-
2003
- 2003-01-14 IL IL153930A patent/IL153930A/en not_active IP Right Cessation
- 2003-01-22 ZA ZA200300584A patent/ZA200300584B/en unknown
- 2003-01-24 NO NO20030382A patent/NO324594B1/no not_active IP Right Cessation
- 2003-02-14 BG BG107560A patent/BG66457B1/bg unknown
-
2004
- 2004-02-13 HK HK04100997A patent/HK1058201A1/xx not_active IP Right Cessation
-
2007
- 2007-12-20 US US12/004,168 patent/US7989453B2/en not_active Expired - Fee Related
-
2008
- 2008-03-06 US US12/074,845 patent/US8008324B2/en not_active Expired - Fee Related
- 2008-07-01 CY CY20081100685T patent/CY1108770T1/el unknown
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