AR052439A1 - Medicamentos para el tratamiento o la prevencion de enfermedades fibroticas - Google Patents
Medicamentos para el tratamiento o la prevencion de enfermedades fibroticasInfo
- Publication number
- AR052439A1 AR052439A1 ARP050105467A ARP050105467A AR052439A1 AR 052439 A1 AR052439 A1 AR 052439A1 AR P050105467 A ARP050105467 A AR P050105467A AR P050105467 A ARP050105467 A AR P050105467A AR 052439 A1 AR052439 A1 AR 052439A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- amino
- group
- carbonyl
- alkoxy
- Prior art date
Links
- 230000003176 fibrotic effect Effects 0.000 title abstract 5
- 201000010099 disease Diseases 0.000 title abstract 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title abstract 3
- 230000002265 prevention Effects 0.000 title abstract 3
- 229940079593 drug Drugs 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 21
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 9
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 8
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 8
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 7
- 125000004429 atom Chemical group 0.000 abstract 6
- -1 thiophene-2-ylcarbonyl Chemical group 0.000 abstract 6
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 5
- 230000004761 fibrosis Effects 0.000 abstract 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 5
- 206010016654 Fibrosis Diseases 0.000 abstract 4
- 125000005097 aminocarbonylalkyl group Chemical group 0.000 abstract 3
- 125000005243 carbonyl alkyl group Chemical group 0.000 abstract 3
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 3
- 238000001727 in vivo Methods 0.000 abstract 3
- 238000007634 remodeling Methods 0.000 abstract 3
- 150000003839 salts Chemical class 0.000 abstract 3
- 125000006698 (C1-C3) dialkylamino group Chemical group 0.000 abstract 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 2
- 208000019693 Lung disease Diseases 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- 125000001841 imino group Chemical group [H]N=* 0.000 abstract 2
- 210000004072 lung Anatomy 0.000 abstract 2
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 abstract 2
- 208000005069 pulmonary fibrosis Diseases 0.000 abstract 2
- 201000002793 renal fibrosis Diseases 0.000 abstract 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 1
- 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 abstract 1
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 abstract 1
- CPELXLSAUQHCOX-UHFFFAOYSA-M Bromide Chemical compound [Br-] CPELXLSAUQHCOX-UHFFFAOYSA-M 0.000 abstract 1
- 206010006458 Bronchitis chronic Diseases 0.000 abstract 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 abstract 1
- 108010036949 Cyclosporine Proteins 0.000 abstract 1
- 206010014561 Emphysema Diseases 0.000 abstract 1
- 206010018367 Glomerulonephritis chronic Diseases 0.000 abstract 1
- 206010020772 Hypertension Diseases 0.000 abstract 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-M Methanesulfonate Chemical compound CS([O-])(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-M 0.000 abstract 1
- 208000032056 Radiation Fibrosis Syndrome Diseases 0.000 abstract 1
- DTQVDTLACAAQTR-UHFFFAOYSA-M Trifluoroacetate Chemical compound [O-]C(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-M 0.000 abstract 1
- 241000700605 Viruses Species 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O ammonium group Chemical group [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 abstract 1
- 238000002399 angioplasty Methods 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 208000006673 asthma Diseases 0.000 abstract 1
- 125000004566 azetidin-1-yl group Chemical group N1(CCC1)* 0.000 abstract 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 abstract 1
- 206010006451 bronchitis Diseases 0.000 abstract 1
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 abstract 1
- 125000005102 carbonylalkoxy group Chemical group 0.000 abstract 1
- 125000005019 carboxyalkenyl group Chemical group 0.000 abstract 1
- 125000005111 carboxyalkoxy group Chemical group 0.000 abstract 1
- 125000004181 carboxyalkyl group Chemical group 0.000 abstract 1
- 208000007451 chronic bronchitis Diseases 0.000 abstract 1
- 229960001265 ciclosporin Drugs 0.000 abstract 1
- 208000019425 cirrhosis of liver Diseases 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 229930182912 cyclosporin Natural products 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- XMBWDFGMSWQBCA-UHFFFAOYSA-N hydrogen iodide Chemical compound I XMBWDFGMSWQBCA-UHFFFAOYSA-N 0.000 abstract 1
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical class C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 abstract 1
- 150000002500 ions Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 208000037803 restenosis Diseases 0.000 abstract 1
- 230000037390 scarring Effects 0.000 abstract 1
- 208000017520 skin disease Diseases 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000004571 thiomorpholin-4-yl group Chemical group N1(CCSCC1)* 0.000 abstract 1
- 230000007838 tissue remodeling Effects 0.000 abstract 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-M toluene-4-sulfonate Chemical compound CC1=CC=C(S([O-])(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-M 0.000 abstract 1
Classifications
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- 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
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
-
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- 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
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Rheumatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Urology & Nephrology (AREA)
- Dermatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Uso de indolinonas de la formula general (1) en las que X es un átomo de O; R1 es un átomo de H; R2 es un átomo de F, Cl o Br o un grupo ciano; R3 es un grupo fenilo o un grupo fenilo que está monosustituido por un átomo de f, Cl, Br o I o por un grupo alcoxi C1-3, en el que los grupos fenilo no sustituidos y monosustituidos mencionados anteriormente pueden estar sustituidos adicionalmente en la posicion 3 o 4 por un átomo de F, Cl o Br, por un grupo ciano, alcoxi C1-3 o (alquil C1- 2)carbonilamino, cianoalquilo C1-3, carboxialquilo C1-3, carboxialcoxi C1-4, carboxi(alquil C1-3)amino, carboxi(alquil C1-3)-N-(alquil C1-3)amino, (alcoxi C1-4) carbonilalquilo C1-3, (alcoxi C1-4)carbonilalcoxi C1-3, (alcoxi C1-4)carbonil(alquil C1- 3)amino, (alcoxi C1-4)carbonil(alquil C1-3)- N-(alquil C1-3)amino, aminoalquilo C1-3, aminocarbonilalquilo C1-3, ((alquil C1-2)amino)carbonilalquilo C1-3, di(alquil c1-2)amino- carbonilalquilo C1-3, ((alquil C1-2)carbonil)aminoalquilo C1-3, ((alcoxi c1-4)carbonil)aminoalquilo C1-3, ((alquil C3-6)carbonil) aminoalquilo C1-3, (fenilcarbonil)aminoalquilo C1-3, ((cicloalquil C3-6)carbonil)aminoalquilo C1-3, ((cicloalquil C3-6)(alquil C1-3) carbonil)aminoalquilo C1-3, (tiofen-2- ilcarbonil)aminoalquiloc1-3, (furan-2-ilcarbonil)-aminoalquilo c1-3, (fenil(alquil C1-3)carbonil) aminoalquilo C1-3, (2-(alcoxi C1-4)benzoil-carbonil)aminoalquilo c1-3, (piridin-2-ilcarbonil)aminoalquilo C1-3, (piridin-3-il-carbonil) aminoalquilo C1- 3, (piridin-4-ilcarbonil)aminoalquilo C1-3 o (alquil C1-3)piperazin-1-ilcarbonilalquilo C1-3, por un grupo carboxialquenilo C2-3, aminocarbonilalquenilo C2-3, ((alquil C1-3)-amino)carbonilalquenilo C2-3, di(alquil C1-3)aminocarbonilalquenilo C2-3 o (alcoxi C1-4)-carbonilalquenilo C2-3,en el que los sustituyentes pueden ser idénticos o diferentes; R4 es un grupo fenilo o un grupo fenilo que está monosustituido por un grupo alquilo C1-3 que está sustituido en el extremo por un grupo amino, guanidino, mono- o di(alquil C1-2)amino, N-[omega-di(alquil C1-3)amino(alquil C2-3)]-N-(alquil C1-3)amino, N-metil(alquil C3-4)amino, N-(alquil C1-3)-N- bencilamino, N-((alcoxi C1-4)-carbonil)amino, N-((alcoxi C1-4)carbonil)(alquil C1-4)amino, 4- (alquil C1-3)piperazin-1-ilo, imidazol-1-ilo, pirrolidin-1-ilo, azetidin-1-ilo, morfolin-4-ilo, piperazin-1-ilo, tiomorfolin-4-ilo, por un grupo di(alquil C1-3)amino(alquil c1-3)sulfonilo, 2-[di(alquilC1-3)-amino]etoxi, 4-(alquil C1-3)piperazin-1- ilcarbonilo, {omega-[di(alquil C1-3)amino](alquil C2-3)}-N-(alquil C1-3) aminocarbonilo, 1-(alquil C1-3)imidazol-2-ilo, (alquil C1-3)sulfonilo, o por un grupo de la formula -N(R8)(R7) en el que R7 es un grupo alquilo C1-2, (alquil C1-2)carbonilo, di(alquil C1-2)amino-carbonilalquilo C1-3 o (alquil C1-3)sulfonilo y R8 es un grupo alquilo C1-3, omega-[di(alquil C1-2)amino]alquilo c2-3, omega-[mono(alquil C1-2)amino]alquilo C2-3, o un grupo (alquil C1-3)carbonilo, (alquil C4-6) carbonilo o carbonilalquilo C1-3 que está sustituido en el extremo por un grupo di(alquil C1-2)amino, piperazin-1-ilo o 4-(alquil C1-3) piperazin-1-ilo, donde todos los grupos dialquilamino presentes en el radical R4 pueden también estar presentes en forma cuaternizada, por ejemplo en forma de un grupo N-metil-(N,N-dialquil)amonio, donde el ion conjugado preferiblemente se selecciona del grupo que consiste en yoduro, cloruro, bromuro, metilsulfonato, para-toluenosulfonato y trifluoroacetato; R5 es un átomo de H y R6 es un átomo de H, donde los grupos alquilo mencionados anteriormente incluyen los grupo alquilo lineales y ramificados en los que además de 1 a 3 átomos de H pueden ser reemplazados por átomos de F, donde además un grupo carboxilo, amino o imino presente puede estar sustituido por un radical que puede escindirse in vivo o puede estar presente en forma de un radical de profármaco, por ejemplo en forma de un grupo que puede convertirse in vivo en un grupo carboxilo o en forma de un grupo que puede convertirse in vivo en un grupo imino o amino, los tautomeros, los diastereoisomeros, los enantiomeros, sus mezclas y sus sales, para la preparacion de un medicamento para la prevencion o el tratamiento de una enfermedad fibrotica que se selecciona del grupo que consiste en fibrosis y en remodelacion de tejido pulmonar en la enfermedad pulmonar obstructiva cronica, fibrosis y remodelacion de tejido pulmonar en la bronquitis cronica, fibrosis y remodelacion de tejido pulmonar en el enfisema, fibrosis pulmonar y enfermedades pulmonares con un componente fibrotico, fibrosis y remodelacion en el asma, fibrosis en la artritis, cirrosis hepática inducida por virus, fibrosis inducida por radiaciones, restenosis tras angioplastía, glomerulonefritis cronica, fibrosis renal en pacientes que reciben ciclosporina y fibrosis renal debida a la tension sanguínea elevada, enfermedades de la piel con un componente fibrotico y cicatrizacion excesiva patologica. Sus isomeros y sales, en particular sus sales fisiologicamente aceptables, como medicamento para la prevencion o el tratamiento de enfermedades fibroticas específicas.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP04030769 | 2004-12-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR052439A1 true AR052439A1 (es) | 2007-03-21 |
Family
ID=35717457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP050105467A AR052439A1 (es) | 2004-12-24 | 2005-12-22 | Medicamentos para el tratamiento o la prevencion de enfermedades fibroticas |
Country Status (26)
| Country | Link |
|---|---|
| US (3) | US20060148883A1 (es) |
| EP (1) | EP1835907B1 (es) |
| JP (1) | JP5748386B2 (es) |
| KR (1) | KR20070092305A (es) |
| CN (1) | CN101087604B (es) |
| AR (1) | AR052439A1 (es) |
| AT (1) | ATE429222T1 (es) |
| AU (1) | AU2005318136B2 (es) |
| BR (1) | BRPI0519351A2 (es) |
| CA (1) | CA2591089C (es) |
| DE (1) | DE602005014145D1 (es) |
| DK (1) | DK1835907T3 (es) |
| EA (1) | EA200701181A1 (es) |
| ES (1) | ES2326277T3 (es) |
| HR (1) | HRP20090312T1 (es) |
| IL (1) | IL184124A0 (es) |
| MX (1) | MX2007007676A (es) |
| NO (1) | NO20073830L (es) |
| PE (1) | PE20061155A1 (es) |
| PL (1) | PL1835907T3 (es) |
| PT (1) | PT1835907E (es) |
| RS (1) | RS50833B (es) |
| SI (1) | SI1835907T1 (es) |
| TW (1) | TW200637544A (es) |
| WO (1) | WO2006067175A1 (es) |
| ZA (1) | ZA200703600B (es) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7514468B2 (en) * | 2002-07-23 | 2009-04-07 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinone derivatives substituted in the 6 position, the preparation thereof and their use as pharmaceutical compositions |
| US7169936B2 (en) * | 2002-07-23 | 2007-01-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments |
| PE20060777A1 (es) | 2004-12-24 | 2006-10-06 | Boehringer Ingelheim Int | Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas |
| WO2007057399A2 (en) * | 2005-11-15 | 2007-05-24 | Boehringer Ingelheim International Gmbh | Treatment of cancer with indole derivatives |
| WO2008108238A1 (ja) * | 2007-03-02 | 2008-09-12 | Mitsui Chemicals, Inc. | 不織布積層体 |
| JP5524852B2 (ja) * | 2007-11-15 | 2014-06-18 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 置換アミド、それらの製造及び医薬品としての使用 |
| US20090131359A1 (en) * | 2007-11-19 | 2009-05-21 | Atamas Sergei P | Antifibrotic therapy |
| JP2011510032A (ja) * | 2008-01-25 | 2011-03-31 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ６−フルオロ−１，２−ジヒドロ−２−オキソ−３ｈ−インドール−３−イリデン誘導体の塩形態、それらの製造方法及びそれらを含有する医薬組成物 |
| EP2334379A2 (en) * | 2008-09-26 | 2011-06-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Host cell kinases as targets for antiviral therapies against hcv infection |
| US20140050728A1 (en) * | 2011-01-28 | 2014-02-20 | Board Of Regents Of The University Of Nebraska | Methods and compositions for inhibiting cyclophilin d for the treatment and prevention of obesity and kidney indications |
| US10450295B2 (en) | 2013-08-09 | 2019-10-22 | Acclaim BioMed USA LLC | Method of using an indolinone molecule and derivatives for inhibiting liver fibrosis and hepatitis |
| US10342786B2 (en) | 2017-10-05 | 2019-07-09 | Fulcrum Therapeutics, Inc. | P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD |
| WO2019071144A1 (en) | 2017-10-05 | 2019-04-11 | Fulcrum Therapeutics, Inc. | USE OF P38 INHIBITORS TO REDUCE DUX4 EXPRESSION |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1115704B1 (de) * | 1998-09-25 | 2003-06-18 | Boehringer Ingelheim Pharma GmbH & Co.KG | Neue substituierte indolinone mit einer inhibierenden wirkung auf verschiedene kinasen und cyclin/cdk-komplexe |
| US6762180B1 (en) * | 1999-10-13 | 2004-07-13 | Boehringer Ingelheim Pharma Kg | Substituted indolines which inhibit receptor tyrosine kinases |
| DE10117204A1 (de) * | 2001-04-06 | 2002-10-10 | Boehringer Ingelheim Pharma | In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| PE20040701A1 (es) * | 2002-07-23 | 2004-11-30 | Boehringer Ingelheim Pharma | Derivados de indolinona sustituidos en posicion 6 y su preparacion como medicamentos |
| US7169936B2 (en) * | 2002-07-23 | 2007-01-30 | Boehringer Ingelheim Pharma Gmbh & Co. Kg | Indolinone derivatives substituted in the 6-position, their preparation and their use as medicaments |
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2005
- 2005-12-16 PE PE2005001477A patent/PE20061155A1/es not_active Application Discontinuation
- 2005-12-20 US US11/275,226 patent/US20060148883A1/en not_active Abandoned
- 2005-12-21 MX MX2007007676A patent/MX2007007676A/es active IP Right Grant
- 2005-12-21 RS RSP-2009/0245A patent/RS50833B/sr unknown
- 2005-12-21 CN CN2005800446331A patent/CN101087604B/zh not_active Expired - Fee Related
- 2005-12-21 SI SI200530719T patent/SI1835907T1/sl unknown
- 2005-12-21 BR BRPI0519351-6A patent/BRPI0519351A2/pt not_active IP Right Cessation
- 2005-12-21 DK DK05823903T patent/DK1835907T3/da active
- 2005-12-21 WO PCT/EP2005/057013 patent/WO2006067175A1/en active Application Filing
- 2005-12-21 KR KR1020077017059A patent/KR20070092305A/ko not_active Application Discontinuation
- 2005-12-21 PL PL05823903T patent/PL1835907T3/pl unknown
- 2005-12-21 CA CA2591089A patent/CA2591089C/en not_active Expired - Fee Related
- 2005-12-21 AT AT05823903T patent/ATE429222T1/de active
- 2005-12-21 EP EP05823903A patent/EP1835907B1/en active Active
- 2005-12-21 ES ES05823903T patent/ES2326277T3/es active Active
- 2005-12-21 PT PT05823903T patent/PT1835907E/pt unknown
- 2005-12-21 DE DE602005014145T patent/DE602005014145D1/de active Active
- 2005-12-21 AU AU2005318136A patent/AU2005318136B2/en not_active Ceased
- 2005-12-21 JP JP2007547510A patent/JP5748386B2/ja not_active Expired - Fee Related
- 2005-12-21 EA EA200701181A patent/EA200701181A1/ru unknown
- 2005-12-22 AR ARP050105467A patent/AR052439A1/es unknown
- 2005-12-23 TW TW094146423A patent/TW200637544A/zh unknown
-
2007
- 2007-05-04 ZA ZA200703600A patent/ZA200703600B/en unknown
- 2007-06-21 IL IL184124A patent/IL184124A0/en unknown
- 2007-07-23 NO NO20073830A patent/NO20073830L/no not_active Application Discontinuation
-
2009
- 2009-05-27 HR HR20090312T patent/HRP20090312T1/xx unknown
-
2011
- 2011-03-31 US US13/077,138 patent/US20120004202A1/en not_active Abandoned
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2014
- 2014-01-13 US US14/153,542 patent/US20140128409A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008525374A (ja) | 2008-07-17 |
| BRPI0519351A2 (pt) | 2009-01-20 |
| WO2006067175A1 (en) | 2006-06-29 |
| ZA200703600B (en) | 2008-07-30 |
| AU2005318136B2 (en) | 2012-02-09 |
| MX2007007676A (es) | 2007-08-14 |
| PL1835907T3 (pl) | 2009-08-31 |
| CA2591089C (en) | 2014-02-11 |
| KR20070092305A (ko) | 2007-09-12 |
| RS50833B (sr) | 2010-08-31 |
| DE602005014145D1 (de) | 2009-06-04 |
| PE20061155A1 (es) | 2006-12-16 |
| CN101087604A (zh) | 2007-12-12 |
| CN101087604B (zh) | 2010-10-13 |
| US20140128409A1 (en) | 2014-05-08 |
| JP5748386B2 (ja) | 2015-07-15 |
| EP1835907B1 (en) | 2009-04-22 |
| US20060148883A1 (en) | 2006-07-06 |
| AU2005318136A1 (en) | 2006-06-29 |
| ES2326277T3 (es) | 2009-10-06 |
| HRP20090312T1 (en) | 2009-07-31 |
| DK1835907T3 (da) | 2009-08-03 |
| ATE429222T1 (de) | 2009-05-15 |
| EP1835907A1 (en) | 2007-09-26 |
| EA200701181A1 (ru) | 2008-02-28 |
| PT1835907E (pt) | 2009-06-16 |
| SI1835907T1 (sl) | 2009-10-31 |
| US20120004202A1 (en) | 2012-01-05 |
| CA2591089A1 (en) | 2006-06-29 |
| TW200637544A (en) | 2006-11-01 |
| NO20073830L (no) | 2007-07-23 |
| IL184124A0 (en) | 2007-10-31 |
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