ES2527770T3 - Derivados de tetrahidroindolona y tetrahidroindazolona - Google Patents

Derivados de tetrahidroindolona y tetrahidroindazolona Download PDF

Info

Publication number
ES2527770T3
ES2527770T3 ES06736330.9T ES06736330T ES2527770T3 ES 2527770 T3 ES2527770 T3 ES 2527770T3 ES 06736330 T ES06736330 T ES 06736330T ES 2527770 T3 ES2527770 T3 ES 2527770T3
Authority
ES
Spain
Prior art keywords
alkyl
aryl
saturated
group
independently
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired - Lifetime
Application number
ES06736330.9T
Other languages
English (en)
Inventor
Kenneth He Huang
Jeron Eaves
James Veal
Thomas Barta
Lifeng Geng
Lindsay Hinkley
Gunnar Hanson
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Serenex Inc
Original Assignee
Serenex Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Serenex Inc filed Critical Serenex Inc
Application granted granted Critical
Publication of ES2527770T3 publication Critical patent/ES2527770T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D209/24—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 with an alkyl or cycloalkyl radical attached to the ring nitrogen atom
    • 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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/535—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/08—Solutions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61N—ELECTROTHERAPY; MAGNETOTHERAPY; RADIATION THERAPY; ULTRASOUND THERAPY
    • A61N5/00—Radiation therapy
    • A61N5/10—X-ray therapy; Gamma-ray therapy; Particle-irradiation therapy
    • 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
    • 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
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • 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
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • 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
    • C07D209/14—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Oncology (AREA)
  • Rheumatology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Radiology & Medical Imaging (AREA)
  • Pathology (AREA)
  • Neurosurgery (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Un compuesto de fórmula XXV, **Fórmula** o una de sus sales farmacéuticamente aceptable, en donde R3 y R4 son independientemente (a) H, (b) halo o (c) un grupo alquilo C1-C15 en donde hasta seis de los átomos de carbono en dicho grupo alquilo están opcionalmente reemplazados independientemente por R22, carbonilo, etenilo, etinilo o un resto seleccionado entre N, O, S, SO2 o SO, con la condición de que dos átomos de O, dos átomos de S, o un átomo de O y S 10 no sean inmediatamente adyacentes entre sí, en donde R22 es (i) heteroarilo, (ii) arilo, (iii) cicloalquilo C3-C10 saturado o insaturado, o (iv) heterocicloalquilo C2-C10 saturado o insaturado, en donde cada arilo, heteroarilo, cicloalquil saturado o insaturado, o heterocicloalquilo saturado o insaturado, independientemente, está opcionalmente sustituido con al menos un grupo, que es independientemente hidroxi, halo, amino, ciano, carboxi, carboxamido, nitro, oxo, -S-alquilo (C1-C6), -SO2-alquilo (C1-C6), -SO2-arilo, -SO-alquilo (C1-C6), -SO-arilo, -SO2NH2, -SO2NH-alquilo (C1-C6), -SO2NH-arilo, alcoxi (C1-C6) o mono- o di-alquilamino (C1-C10); y cada R22 está opcionalmente condensado con un grupo arilo C6-C10, grupo cíclico C5-C8 saturado o un grupo heterocicloalquilo C5-C10; en donde cada (c) está opcionalmente sustituido en cualquier posición disponible con alquil C1-C10, haloalquilo C1-C10, alquenilo C2-C10, alquinilo C2-C10, hidroxi, carboxi, carboxamido, oxo, halo, amino, ciano, nitro, -SH, -S-alquilo (C1-C6), -SO2-alquilo (C1-C6), -SO2NH2, -SO2NH-alquilo (C1-C6), -SO2NH-arilo, -SO2-arilo, - SO-alquilo (C1-C6), -SO2-arilo, alcoxi C1-C6, alqueniloxi C2-C10, alquiniloxi C2-C10, mono o di-alquilamino (C1-C10), -Oalquil C1-C10-Z o R23, en donde Z es OR0 o -N(R30)2, en donde cada R30 es independientemente -H o alquilo C1-C6, o N(R30)2 representa pirrolidinilo, piperidinilo, piperazinilo, 30 azepanilo, 1,3- o 1,4-diazepanilo, o morfolinilo, cada uno de los cuales está opcionalmente sustituido con hidroxi, amino, aminoalquilo, alquilo C1-C6, mono- o di-alquilamino (C1-C6), alcoxi C1-C6 o halógeno; R0 es -H, -alquilo C1-C10, -alquenilo C2-C10, -alquinilo C2-C10, arilo, heteroarilo o -acilo C1-C6; R23 es (1) heteroarilo, (2) arilo.
ES06736330.9T 2005-02-25 2006-02-27 Derivados de tetrahidroindolona y tetrahidroindazolona Expired - Lifetime ES2527770T3 (es)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US65623005P 2005-02-25 2005-02-25
US656230P 2005-02-25
US70571505P 2005-08-04 2005-08-04
US705715P 2005-08-04
US72796505P 2005-10-18 2005-10-18
US727965P 2005-10-18
PCT/US2006/006988 WO2006091963A1 (en) 2005-02-25 2006-02-27 Tetrahydroindolone and tetrahydroindazolone derivatives

Publications (1)

Publication Number Publication Date
ES2527770T3 true ES2527770T3 (es) 2015-01-29

Family

ID=36581601

Family Applications (1)

Application Number Title Priority Date Filing Date
ES06736330.9T Expired - Lifetime ES2527770T3 (es) 2005-02-25 2006-02-27 Derivados de tetrahidroindolona y tetrahidroindazolona

Country Status (24)

Country Link
US (8) US7358370B2 (es)
EP (2) EP1856057B1 (es)
JP (1) JP4377942B2 (es)
KR (3) KR101617774B1 (es)
CN (1) CN101180275B (es)
AR (1) AR054186A1 (es)
AU (2) AU2006216441B2 (es)
BR (1) BRPI0607739A2 (es)
CA (1) CA2598993C (es)
DK (1) DK1856057T3 (es)
EA (1) EA013521B1 (es)
ES (1) ES2527770T3 (es)
GE (1) GEP20104994B (es)
IL (1) IL185280A (es)
MA (1) MA29713B1 (es)
MX (1) MX2007010227A (es)
NO (1) NO20074274L (es)
NZ (2) NZ588960A (es)
PL (1) PL1856057T3 (es)
PT (1) PT1856057E (es)
SI (1) SI1856057T1 (es)
TW (1) TWI382015B (es)
UA (1) UA92907C2 (es)
WO (1) WO2006091963A1 (es)

Families Citing this family (63)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7550499B2 (en) 2004-05-12 2009-06-23 Bristol-Myers Squibb Company Urea antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
KR20070060156A (ko) * 2004-10-04 2007-06-12 미리어드 제네틱스, 인크. 알츠하이머병 치료용 화합물
US7358370B2 (en) 2005-02-25 2008-04-15 Serenex, Inc. Benzene, pyridine, and pyridazine derivatives
US7728008B2 (en) * 2005-06-27 2010-06-01 Bristol-Myers Squibb Company N-linked heterocyclic antagonists of P2Y1 receptor useful in the treatment of thrombotic conditions
WO2007101156A1 (en) * 2006-02-27 2007-09-07 Serenex, Inc. Cyclohexylamino, benzene, pyridine, and pyridazine derivatives
CA2648216C (en) * 2006-04-13 2016-06-07 Michael Gutschow Tetrahalogenated compounds useful as inhibitors of angiogenesis
CN101490052B (zh) 2006-05-12 2012-08-08 美瑞德生物工程公司 治疗性化合物及其在癌症中的用途
RS52062B (sr) * 2006-05-19 2012-06-30 Abbott Laboratories Cns aktivni azabiciklični alkanski derivati koji su supstituisani spojenim bicikloheterociklom
JP5599610B2 (ja) * 2006-06-30 2014-10-01 スローン − ケッタリング インスティチュート フォー キャンサー リサーチ Ｈｓｐ９０の阻害による神経変性疾患の処置
US20080076800A1 (en) * 2006-08-24 2008-03-27 Huang Kenneth H Benzene, Pyridine, and Pyridazine Derivatives
US20080070918A1 (en) * 2006-08-24 2008-03-20 Huang Kenneth H Dihydropyridazine, Tetrahydropyridine, Chromanone, and Dihydronaphthalenone Derivatives
WO2008024981A1 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Piperazine-substituted benzothiophenes for treatment of mental disorders
US20090093452A1 (en) * 2006-08-24 2009-04-09 Pfizer Inc. Pyrrole, Thiophene, Furan, Imidazole, Oxazole, and Thiazole Derivatives
WO2008024970A2 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
JP2010501593A (ja) * 2006-08-24 2010-01-21 セレネックス， インコーポレイテッド イソキノリン、キナゾリンおよびフタラジン誘導体
WO2008024978A2 (en) * 2006-08-24 2008-02-28 Serenex, Inc. Tetrahydroindolone and tetrahydroindazolone derivatives
FR2907453B1 (fr) 2006-10-24 2008-12-26 Sanofi Aventis Sa Nouveaux derives du fluorene,compositions les contenant et utilisation
WO2008057246A2 (en) * 2006-10-26 2008-05-15 Synta Pharmaceuticals Corp. Method for treating inflammatory disorders
CN101273991B (zh) * 2007-03-28 2010-05-26 广东同德药业有限公司 四氢吲哚酮/四氢吲唑酮/四氢咔唑衍生物及其盐在制备抗病毒药物中的应用
CA2684240A1 (en) * 2007-04-16 2008-10-30 Serenex, Inc. Tetrahydroindole and tetrahydroindazole derivatives
EP1997805A1 (en) * 2007-06-01 2008-12-03 Commissariat à l'Energie Atomique Compounds with antiparasitic activity, applications thereof to the treatment of infectious diseases caused by apicomplexans
EP2202223B1 (en) * 2007-10-18 2017-01-25 Takeda Pharmaceutical Company Limited Heterocyclic compound as blood rbp4 lowering agent
FR2943341B1 (fr) * 2009-03-19 2011-03-11 Sanofi Aventis Nouveaux derives d'indazole inhibiteurs d'hsp90,compositions les contenant et utilisation
EP2408762A1 (fr) * 2009-03-19 2012-01-25 Sanofi Derives d'indazole inhibiteurs d'hsp90, compositions les contenant et utilisation
FR2955323B1 (fr) * 2010-01-19 2015-01-16 Sanofi Aventis Nouveaux derives d'indazole inhibiteurs d'hsp90, compositions les contenant et utilisation
ES2529101T3 (es) * 2009-03-30 2015-02-16 Nordic Bioscience A/S Ensayo de biomarcadores para fibrosis
AR077405A1 (es) 2009-07-10 2011-08-24 Sanofi Aventis Derivados del indol inhibidores de hsp90, composiciones que los contienen y utilizacion de los mismos para el tratamiento del cancer
FR2949467B1 (fr) 2009-09-03 2011-11-25 Sanofi Aventis Nouveaux derives de 5,6,7,8-tetrahydroindolizine inhibiteurs d'hsp90, compositions les contenant et utilisation
EP2560640A1 (en) 2010-04-19 2013-02-27 Synta Pharmaceuticals Corp. Cancer therapy using a combination of a hsp90 inhibitory compounds and a egfr inhibitor
CN101872359B (zh) * 2010-06-11 2013-08-14 北京邮电大学 实现演变点发现的社会网络演化分析方法及系统
GB201009853D0 (en) 2010-06-11 2010-07-21 Chroma Therapeutics Ltd HSP90 inhibitors
CN102311389A (zh) * 2010-06-29 2012-01-11 王小龙 一种氮芳香取代吡唑衍生物、及其合成和抗癌应用
CN101955461B (zh) * 2010-10-08 2012-11-21 广州暨南生物医药研究开发基地有限公司 一种Hsp90抑制剂Xbj-B11及其制备方法与应用
CN101967125B (zh) 2010-10-08 2012-07-04 广州暨南生物医药研究开发基地有限公司 一种Hsp90抑制剂Xbj-B16-1及其制备方法与应用
MX2013010524A (es) 2011-03-15 2013-12-06 Univ British Columbia Combinacion de oligonucleotido anti-clusterina con inhibidor hsp90 para el tratamiento de cancer de prostata.
CN102675288B (zh) * 2011-03-18 2014-01-01 北京师范大学 2-((2-(双(2-吡啶甲基)氨基)乙基)氨基)-4-(3，6，6-三甲基-4-氧-4，5，6，7-四氢吲唑基)苯甲酰胺及制备、应用
JP2014534228A (ja) 2011-11-02 2014-12-18 シンタ ファーマシューティカルズ コーポレーション 白金含有剤とｈｓｐ９０阻害剤の組合せ療法
WO2013067162A1 (en) 2011-11-02 2013-05-10 Synta Pharmaceuticals Corp. Cancer therapy using a combination of hsp90 inhibitors with topoisomerase i inhibitors
EP2780010A1 (en) 2011-11-14 2014-09-24 Synta Pharmaceuticals Corp. Combination therapy of hsp90 inhibitors with braf inhibitors
WO2014025395A1 (en) 2012-08-06 2014-02-13 Duke University Compounds and methods for targeting hsp90
CN103467356B (zh) * 2013-08-12 2015-04-01 绍兴文理学院 一种四氢吲哚化合物及其制备方法与应用
CR20170076A (es) 2014-08-04 2017-06-26 Nuevolution As Derivados de pirimidima sustituidos con heterociclilo opcionalmente condensados útiles para el tratamiento de enfermedades inflamatorias, metabólicas, oncológicas y autoinmunitarias
EP3191473A1 (en) * 2014-09-11 2017-07-19 Esanex, Inc. Indazolyl- and indolyl-benzamide derivatives
WO2016086153A2 (en) 2014-11-26 2016-06-02 Esanex, Inc. Use of tetrahydro!ndazolylbeimzamide and tetrahydroindolylbenzamide derivatives for the treatment of human immunodeficiency virus (hiv) and acquired immune deficiency syndrome (aids)
CN104592203A (zh) * 2015-01-30 2015-05-06 广州暨南生物医药研究开发基地有限公司 一种2-氨基-4-四氢吲唑取代的苯甲酰胺化合物及其在制备抗肿瘤药物中的应用
CN104592230B (zh) * 2015-01-30 2017-02-01 广州暨南生物医药研究开发基地有限公司 一种2‑（石榴皮烷‑3‑氨基）‑4‑四氢吲唑取代的苯甲酰胺化合物及其应用
US9737509B1 (en) 2015-05-26 2017-08-22 University Of South Florida Antimicrobial compositions, methods of use, and methods of treatment of infections
WO2017059434A1 (en) 2015-10-02 2017-04-06 Esanex, Inc. Use of tetrahydroindazolylbenzamide and tetrahydroindolylbenzamide derivatives for the treatment of cancer
ES2956011T3 (es) * 2015-10-13 2023-12-11 Nihon Nohyaku Co Ltd Compuesto heterocíclico condensado que contiene un grupo oxima o sales del mismo e insecticida agrícola y hortícola que contiene dicho compuesto y método para el uso del mismo
US11261187B2 (en) 2016-04-22 2022-03-01 Duke University Compounds and methods for targeting HSP90
AU2017268356A1 (en) * 2016-05-18 2018-11-15 Esanex, Inc. Combination therapies using indazolylbenzamide derivatives for the treatment of cancer
EP3515436A1 (en) 2016-09-23 2019-07-31 Esanex, Inc. Combination therapies using indazolylbenzamide derivatives for the treatment of cancer
EP3680241A1 (en) 2017-03-20 2020-07-15 Forma Therapeutics, Inc. Pyrrolopyrrole compositions as pyruvate kinase (pkr) activators
US10675274B2 (en) 2018-09-19 2020-06-09 Forma Therapeutics, Inc. Activating pyruvate kinase R
WO2020061255A1 (en) 2018-09-19 2020-03-26 Forma Therapeutics, Inc. Activating pyruvate kinase r
HUE072832T2 (hu) 2019-09-19 2025-12-28 Novo Nordisk Healthcare Ag Piruvát kináz R-t (PKR) aktiváló készítmények
AU2020405446A1 (en) 2019-12-20 2022-05-26 Nuevolution A/S Compounds active towards nuclear receptors
AU2020408107B2 (en) 2019-12-20 2026-04-23 Nuevolution A/S Compounds active towards nuclear receptors
EP4126874A1 (en) 2020-03-31 2023-02-08 Nuevolution A/S Compounds active towards nuclear receptors
US11613532B2 (en) 2020-03-31 2023-03-28 Nuevolution A/S Compounds active towards nuclear receptors
CA3186769A1 (en) * 2020-06-11 2021-12-16 Betta Pharmaceuticals Co., Ltd Bicyclic compounds and use thereof
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
CN114213332B (zh) * 2022-02-21 2022-05-17 深圳市人民医院 一种四氢吲唑类化合物及其制备方法和应用

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE4024862A1 (de) * 1990-08-04 1992-02-13 Hoechst Ag 4,5,6,7-tetrahydro-3-aryl-indazole, verfahren zu ihrer herstellung und ihre verwendung als herbizide
GB9812038D0 (en) * 1998-06-04 1998-07-29 Merck Sharp & Dohme Therapeutic compound
GB9900222D0 (en) * 1999-01-06 1999-02-24 Merck Sharp & Dohme Therapeutic compounds
GB9911053D0 (en) * 1999-05-12 1999-07-14 Pharmacia & Upjohn Spa 4,5,6,7-tetrahydroindazole derivatives process for their preparation and their use as antitumour agents
MXPA03001951A (es) * 2000-09-06 2003-10-15 Neurogen Corp Pirroliminas y pirazoliminas fusionadas substituidas.
NZ531153A (en) 2001-08-09 2005-10-28 Ono Pharmaceutical Co Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient
DE10148618B4 (de) * 2001-09-25 2007-05-03 Schering Ag Substituierte N-(1,4,5,6-Tetrahydro-cyclopentapyrazol-3-yl)-Derivate, deren Herstellung und Verwendung als Arzneimittel
WO2003073999A2 (en) * 2002-03-01 2003-09-12 Pintex Pharmaceuticals, Inc. Pini-modulating compounds and methods of use thereof
WO2004052862A1 (ja) 2002-12-10 2004-06-24 Ono Pharmaceutical Co., Ltd. 含窒素複素環化合物およびその医薬用途
PE20040804A1 (es) 2002-12-19 2004-12-31 Boehringer Ingelheim Pharma DERIVADOS DE CARBOXAMIDAS COMO INHIBIDORES DEL FACTOR Xa
US7358370B2 (en) * 2005-02-25 2008-04-15 Serenex, Inc. Benzene, pyridine, and pyridazine derivatives
JPWO2006109846A1 (ja) 2005-04-06 2008-11-20 武田薬品工業株式会社 トリアゾール誘導体およびその用途
CA2684240A1 (en) 2007-04-16 2008-10-30 Serenex, Inc. Tetrahydroindole and tetrahydroindazole derivatives

Also Published As

Publication number Publication date
US7928135B2 (en) 2011-04-19
EP1856057A1 (en) 2007-11-21
CN101180275B (zh) 2014-09-10
HK1117535A1 (en) 2009-01-16
KR20070114763A (ko) 2007-12-04
EP2380879A1 (en) 2011-10-26
WO2006091963A1 (en) 2006-08-31
EA200701808A1 (ru) 2008-02-28
AU2011201700B2 (en) 2013-08-22
US8309548B2 (en) 2012-11-13
US20090163493A9 (en) 2009-06-25
IL185280A (en) 2014-09-30
US20140343037A1 (en) 2014-11-20
TWI382015B (zh) 2013-01-11
US20110034529A1 (en) 2011-02-10
KR20150029766A (ko) 2015-03-18
NZ560685A (en) 2010-12-24
US20170260174A1 (en) 2017-09-14
US20080096887A1 (en) 2008-04-24
NZ588960A (en) 2012-06-29
CA2598993A1 (en) 2006-08-31
US7358370B2 (en) 2008-04-15
KR20130103801A (ko) 2013-09-24
JP4377942B2 (ja) 2009-12-02
PT1856057E (pt) 2015-02-04
MA29713B1 (fr) 2008-09-01
NO20074274L (no) 2007-11-23
PL1856057T3 (pl) 2015-04-30
AU2011201700A1 (en) 2011-05-12
KR101617774B1 (ko) 2016-05-04
CA2598993C (en) 2013-09-03
US9656956B2 (en) 2017-05-23
DK1856057T3 (en) 2015-01-19
JP2008531599A (ja) 2008-08-14
CN101180275A (zh) 2008-05-14
BRPI0607739A2 (pt) 2009-09-29
SI1856057T1 (sl) 2015-05-29
US20200071308A1 (en) 2020-03-05
TW200720250A (en) 2007-06-01
EP2380879B1 (en) 2017-07-12
GEP20104994B (en) 2010-05-25
AR054186A1 (es) 2007-06-06
EP1856057B1 (en) 2014-10-15
MX2007010227A (es) 2007-11-07
UA92907C2 (uk) 2010-12-27
AU2006216441B2 (en) 2011-03-24
US20110183977A1 (en) 2011-07-28
US7906529B2 (en) 2011-03-15
EA013521B1 (ru) 2010-06-30
AU2006216441A1 (en) 2006-08-31
US20060211737A1 (en) 2006-09-21
US20130137686A1 (en) 2013-05-30
IL185280A0 (en) 2008-02-09

Similar Documents

Publication Publication Date Title
CO6150158A2 (es) Piperidinas sustituidas que aumentan la actividad de p53 y su uso
BR112014001175A2 (pt) composto heterocíclico fundido e uso do mesmo para controle de peste
AR073114A1 (es) Derivados tetraciclicos que tienen propiedades insecticidas y composiciones de los mismos
AR057209A1 (es) Compuestos para el tratamiento de trastornos inflamatorios y enfermedades microbianas
CO6160322A2 (es) Derivados de quinazolinona e isoquinolinona acetamida
BRPI0719008A2 (pt) Inibidores de vírus da hepatite c
AR039665A1 (es) Fenilacetamidas sustituidas y su uso como activadores de glucoquinasa
AR083070A1 (es) Analogos de nucleotidos sustituidos con heterociclos nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos para tratar enfermedades virales, en particular infecciones por vhc
NO20054856D0 (no) 4-anilo-kinazolinderivater som antiproliferative midler
TNSN07252A1 (en) Indole derivatives for treating viral infections
EA200900676A1 (ru) Ингибиторы вируса гепатита с
AR106944A2 (es) Compuestos de isoindolina y composiciones farmacéuticas de los mismos
BR112016006262A2 (pt) composto, composição, material de acabamento automotivo interior ou exterior, artigo agrícola, e, métodos para estabilização de um material orgânico e preparação de um composto
MX389728B (es) Conjugados de farmacos proteinas de union que comprenden derivados de antraciclina.
AR073412A1 (es) Derivados de espiro imidazolona como antagonistas del receptor glucagon y composiciones que los comprende.
CO6251243A2 (es) Nuevos inhibidores macrocíclicos de la replicación del virus de hepatitis c
NO20084637L (no) Cyklopropyl-kondenserte indolobenzaepin HCV NS5B inhibitorer
BR112016001979A2 (pt) composto de tetrazolinona e uso do mesmo
AR106987A1 (es) Compuestos de diamina-arilsulfonamida sustituidos con hidroxialquilamina e hidroxicicloalquilamina con actividad selectiva en canales de sodio activados por voltaje
ATE484645T1 (de) Schrankförmiges möbel
UY32308A (es) Nucleótidos uracil ciclopropílicos
BR112015019790A2 (pt) derivado de piridina monocíclica
AR054186A1 (es) Derivados de tetrahidroindazolona y tetrahidroindolona
BRPI0516535A (pt) elemento de atuação para um apoio de cabeça que age em colisões
EA201070839A1 (ru) Новые производные ацилцианопирролидинов