PE20130386A1 - Derivados de indolizina, su procedimiento de preparacion y su aplicacion en terapeutica - Google Patents
Derivados de indolizina, su procedimiento de preparacion y su aplicacion en terapeuticaInfo
- Publication number
- PE20130386A1 PE20130386A1 PE2013000019A PE2013000019A PE20130386A1 PE 20130386 A1 PE20130386 A1 PE 20130386A1 PE 2013000019 A PE2013000019 A PE 2013000019A PE 2013000019 A PE2013000019 A PE 2013000019A PE 20130386 A1 PE20130386 A1 PE 20130386A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- methylindolizin
- rent
- carbonyl
- phenyl
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 2
- 239000003814 drug Substances 0.000 title 1
- HOBCFUWDNJPFHB-UHFFFAOYSA-N indolizine Chemical class C1=CC=CN2C=CC=C21 HOBCFUWDNJPFHB-UHFFFAOYSA-N 0.000 title 1
- UGFAIRIUMAVXCW-UHFFFAOYSA-N Carbon monoxide Chemical compound [O+]#[C-] UGFAIRIUMAVXCW-UHFFFAOYSA-N 0.000 abstract 3
- CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical class [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000018233 Fibroblast Growth Factor Human genes 0.000 abstract 2
- 108050007372 Fibroblast Growth Factor Proteins 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N Benzoic acid Natural products OC(=O)C1=CC=CC=C1 WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 abstract 1
- 239000005711 Benzoic acid Substances 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 206010019668 Hepatic fibrosis Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 235000010233 benzoic acid Nutrition 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
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- 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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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- A—HUMAN NECESSITIES
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- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4709—Non-condensed quinolines and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- 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
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
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- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
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- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/32—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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
- C07D207/36—Oxygen or sulfur atoms
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- 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
- C07D211/80—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 two double bonds between ring members or between ring members and non-ring members
- C07D211/82—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Urology & Nephrology (AREA)
- Oncology (AREA)
- Rheumatology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Endocrinology (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Child & Adolescent Psychology (AREA)
- Gastroenterology & Hepatology (AREA)
- Neurology (AREA)
- Reproductive Health (AREA)
- Ophthalmology & Optometry (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Neurosurgery (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE INDOLIZINA DE FORMULA (I) DONDE R1 ES H, HALOGENO, ALQUILO SUSTITUIDO OPCIONALMENTE CON -COOR5, ALQUENILO SUSTITUIDO OPCIONALMENTE CON -COOR5, ENTRE OTROS, EN DONDE R5 ES H, HALOGENOALQUILO, CICLOALQUILO, ENTRE OTROS; R2 ES H, ALQUILO O FENILO SUSTITUIDO OPCIONALMENTE CON ALQUILO; R3 Y R4 FORMAN JUNTO CON LOS ATOMOS DE CARBONO DEL NUCLEO FENILO AL QUE ESTAN UNIDOS UN HETEROCICLO NITROGENADO DE 6 MIEMBROS DE FORMULA (A), (B), ENTRE OTROS, DONDE Ra ES H, ALQUILO, HALOGENOALQUILO, ENTRE OTROS; Ra' ES H, ALQUILO, ENTRE OTROS; Rb ES H, ALQUILO, ENTRE OTROS; Rb' ES H, ALQUILO, CICLOALQUILO, FENILO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-{6-[(1-METOXI-2-METILINDOLIZIN-3-IL)CARBONIL]-2,4-DIOXO-1,4-DIHIDROQUINAZOLIN-3(2H)-IL}-N,N'-DIMETILACETAMIDA; 6-[(1-METOXI-2-METILINDOLIZIN-3-IL)CARBONIL]-3-[(3-METIL-1,2,4-OXADIAZOL-5-IL)METIL]QUINAZOLINA-2,4(1H,3H)-DIONA; ACIDO 3-{3-(2,4-DIOXO-3-PROPIL-1,2,3,4-TETRAHIDROQUINAZOLIN-6-IL)CARBONIL}-2-METILINDOLIZIN-1-IL}BENZOICO; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LOS FACTORES DE CRECIMIENTO DE FIBROBLASTOS (FGF) SIENDO UTILES EN EL TRATAMIENTO DE ATEROSCLEROSIS, FIBROSIS HEPATICA, CANCER
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR1055477A FR2962438B1 (fr) | 2010-07-06 | 2010-07-06 | Derives d'indolizines, procedes de preparation et application en therapeutique |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20130386A1 true PE20130386A1 (es) | 2013-04-11 |
Family
ID=43382527
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2013000019A PE20130386A1 (es) | 2010-07-06 | 2011-07-04 | Derivados de indolizina, su procedimiento de preparacion y su aplicacion en terapeutica |
Country Status (39)
| Country | Link |
|---|---|
| US (1) | US8859544B2 (es) |
| EP (1) | EP2590975B1 (es) |
| JP (1) | JP5863788B2 (es) |
| KR (1) | KR101797795B1 (es) |
| CN (1) | CN103080112B (es) |
| AR (1) | AR082768A1 (es) |
| AU (1) | AU2011275426B2 (es) |
| BR (1) | BR112013000306A2 (es) |
| CA (1) | CA2805065C (es) |
| CL (1) | CL2013000018A1 (es) |
| CO (1) | CO6650361A2 (es) |
| CR (1) | CR20130001A (es) |
| CY (1) | CY1116945T1 (es) |
| DK (1) | DK2590975T3 (es) |
| DO (1) | DOP2012000321A (es) |
| EA (1) | EA024160B1 (es) |
| EC (1) | ECSP13012362A (es) |
| ES (1) | ES2552850T3 (es) |
| FR (1) | FR2962438B1 (es) |
| GT (1) | GT201300001A (es) |
| HR (1) | HRP20151162T1 (es) |
| HU (1) | HUE026067T2 (es) |
| IL (1) | IL223844A (es) |
| MA (1) | MA34451B1 (es) |
| MX (1) | MX2012015306A (es) |
| MY (1) | MY163202A (es) |
| NI (1) | NI201200191A (es) |
| PE (1) | PE20130386A1 (es) |
| PH (1) | PH12013500005A1 (es) |
| PL (1) | PL2590975T3 (es) |
| PT (1) | PT2590975E (es) |
| SG (2) | SG186436A1 (es) |
| SI (1) | SI2590975T1 (es) |
| TN (1) | TN2012000609A1 (es) |
| TW (1) | TWI494310B (es) |
| UA (1) | UA109013C2 (es) |
| UY (1) | UY33489A (es) |
| WO (1) | WO2012004731A1 (es) |
| ZA (1) | ZA201300100B (es) |
Families Citing this family (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3 |
| FR2985258A1 (fr) * | 2011-12-28 | 2013-07-05 | Sanofi Sa | Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique |
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| JP6449244B2 (ja) | 2013-04-19 | 2019-01-09 | インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation | Fgfr抑制剤としての二環式複素環 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| JP6854776B2 (ja) * | 2015-01-08 | 2021-04-07 | インぺティス バイオサイエンス リミテッド | 二環式化合物、その組成物および医薬用途 |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| ES2751669T3 (es) | 2015-02-20 | 2020-04-01 | Incyte Corp | Heterociclos bicíclicos como inhibidores FGFR |
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| CN106045994A (zh) * | 2016-06-12 | 2016-10-26 | 上海大学 | 全氟烷基吲嗪衍生物及其合成方法 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| PE20210919A1 (es) | 2018-05-04 | 2021-05-19 | Incyte Corp | Sales de un inhibidor de fgfr |
| CN119241541A (zh) | 2018-05-04 | 2025-01-03 | 因赛特公司 | Fgfr抑制剂的固体形式和其制备方法 |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| IL293001A (en) | 2019-12-04 | 2022-07-01 | Incyte Corp | Derivatives of fgfr repressors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| JP2024513575A (ja) | 2021-04-12 | 2024-03-26 | インサイト・コーポレイション | Fgfr阻害剤及びネクチン-4標的化剤を含む併用療法 |
| AR126101A1 (es) | 2021-06-09 | 2023-09-13 | Incyte Corp | Heterociclos tricíclicos como inhibidores de fgfr |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040116462A1 (en) | 2002-12-12 | 2004-06-17 | Mitsunori Ono | Indolizine compounds |
| EP1490371B1 (en) | 2002-04-03 | 2007-08-15 | Bristol-Myers Squibb Company | Thiophene-based tricyclic compounds and pharmaceutical compositions comprising same |
| FR2838123B1 (fr) * | 2002-04-04 | 2005-06-10 | Sanofi Synthelabo | Nouveaux derives d'indolozine-1,2,3 substituee, inhibiteurs selectifs du b-fgf |
| FR2859997B1 (fr) | 2003-09-18 | 2006-02-03 | Sanofi Synthelabo | Nouveaux derives d'indolizine 1,2,3,6,7,8 substituee, inhibiteurs des fgfs, leur procede de preparation et les compositions pharmaceutiques les contenant. |
| ATE500254T1 (de) | 2003-09-25 | 2011-03-15 | Janssen Pharmaceutica Nv | Die replikation von hiv hemmende purinderivate |
| FR2865934B1 (fr) | 2004-02-05 | 2006-05-05 | Sanofi Synthelabo | Utilisation de derives d'indolizine 1,2,3 substitues, inhibiteurs des fgfs, pour la preparation de medicaments utiles pour le traitement de maladies liees a une angiogenese pathologique choroidienne |
| FR2883286B1 (fr) | 2005-03-16 | 2008-10-03 | Sanofi Aventis Sa | NOUVEAUX DERIVES D'IMIDAZO[1,5-a]PYRIDINES, INHIBITEURS DE FGFs, LEUR PROCEDE DE PREPARATION ET LES COMPOSITIONS PHARMACEUTIQUES LES CONTENANT |
| FR2893616B1 (fr) | 2005-11-23 | 2008-01-04 | Sanofi Aventis Sa | Nouveaux derives d'indolizine, leur procede de preparation et les compositions therapeutiques les comprenant |
| FR2896247B1 (fr) * | 2006-01-13 | 2008-02-29 | Sanofi Aventis Sa | Composes dimeres agonistes des recepteurs des fgfs (fgfrs), leur procede de preparation et leur application en therapeutique |
| EP1891955A1 (en) * | 2006-07-24 | 2008-02-27 | Sanofi-Aventis | Use of 1,2,3-substituted indolizine derivatives, inhibitors of FGFs, for the preparation of a medicament intended for the treatment of degenerative joint diseases |
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