AR078535A1 - PIRROLO DERIVATIVES [2,3-B] PYRIDINE LIGANDOS OF STROGEN RECEPTORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN THE TREATMENT OF THE OSTEOPOROSIS AND DISEASES OF THE CENTRAL NERVOUS SYSTEM, AMONG OTHER - Google Patents

PIRROLO DERIVATIVES [2,3-B] PYRIDINE LIGANDOS OF STROGEN RECEPTORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN THE TREATMENT OF THE OSTEOPOROSIS AND DISEASES OF THE CENTRAL NERVOUS SYSTEM, AMONG OTHER

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Publication number
AR078535A1
AR078535A1 ARP100103628A ARP100103628A AR078535A1 AR 078535 A1 AR078535 A1 AR 078535A1 AR P100103628 A ARP100103628 A AR P100103628A AR P100103628 A ARP100103628 A AR P100103628A AR 078535 A1 AR078535 A1 AR 078535A1
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Argentina
Prior art keywords
alkyl
group
alkynyl
alkenyl
halogen
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ARP100103628A
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Spanish (es)
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Karobio Ab
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Publication of AR078535A1 publication Critical patent/AR078535A1/en

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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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • 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
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P35/00—Antineoplastic agents
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
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  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto de la formula (1) o un éster, amida, solvato o sal farmacéuticamente aceptable del mismo, incluyendo una sal de dicho éster o amida, y un solvato de dicho éster, amida o sal, en el cual uno de uno de A, B, D y E representa nitrogeno, y los otros tres de A, B, D y E representan CR3, CR4 y CR5; R1 es seleccionado del grupo constituido por hidrogeno, halogeno, ciano, nitro, ORA, N(RB)2, -C(O)alquilo C1-4, -SO2-alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6, trihaloalquilo C1-6, haloalquenilo C2-6, dihaloalquenilo C2-6, trihaloalquenilo C2-6, cianoalquilo C1-6, alcoxi C1-4alquilo C1-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, bencilo y heterociclilo de 5 - 10 miembros, donde dicho grupo fenilo, bencilo o heterociclilo puede estar no sustituido o sustituido con 1 a 3 sustituyentes, cada uno de los cuales es independientemente seleccionado del grupo que consiste en ORA, halogeno, ciano, nitro, -C(O)alquilo C1-4, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; R2 es seleccionado del grupo constituido por halogeno, ciano, nitro, ORC, N(RB)2, N(OH)2, -CHO, -CH=N-OH, -C(O)alquilo C1-4 opcionalmente sustituido con 1 a 3 halogenos, -SO2-alquilo C1-4, -C(O)NH-OH, -C(NH2)N=OH, -C(CO2H)=N-OH, -C(NH2)=NH, -C(O-alquil C1-4)=NH, -C(NH2)=N-NH2, -NH-C(NH2)=NH, -NH-C(O)NH2, -N=C(-NH-CH2CH2-NH-), -S-CN, -S-C(NH2)=NH, -S-C(NH2)=N-OH, -CO2H, -CH2-CO2H, -CH(OH)CO2H, -C(O)N(RC)2, SO2N(RC)2, -C(O)-C(O)-NH2, -CH2NH-CONH2, NHSO2RB, -C(O)CO2H, SO3H, CH2SO3H y heterociclilo de 5 - 10 miembros donde dicho grupo heterociclilo puede estar no sustituido o sustituido con 1 a 3 sustituyentes, cada uno de los cuales es independientemente seleccionado del grupo que consiste en ORA, halogeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; cada uno de R3, R4, R5, R6, R7, R8 y R9 es independientemente seleccionado del grupo que consiste en hidrogeno, ORA, halogeno, ciano, nitro, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-6, dihaloalquilo C1-6 y trihaloalquilo C1-6; cada RA es seleccionado, de manera independiente, del grupo conformado por hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6, fenilo, bencilo y heterociclilo de 5 - 10 miembros, cada uno de los cuales está opcionalmente sustituido con 1 a 3 átomos de halogeno; cada RB es seleccionado, de manera independiente, del grupo conformado por hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, cicloalquil C3-8alquilo C1-6 y heterociclilo de 5 - 10 miembros, cada uno de los cuales está opcionalmente sustituido con 1 a 3 átomos de halogeno; y cada RC es seleccionado, de manera independiente, del grupo conformado por hidrogeno y alquilo C1-6.Claim 1: A compound of the formula (1) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of said ester or amide, and a solvate of said ester, amide or salt, in which one of one of A, B, D and E represents nitrogen, and the other three of A, B, D and E represent CR3, CR4 and CR5; R1 is selected from the group consisting of hydrogen, halogen, cyano, nitro, ORA, N (RB) 2, -C (O) C1-4 alkyl, -SO2-C1-4 alkyl, C1-6 alkyl, C2-6 alkenyl C2-6 alkynyl, C1-6 haloalkyl, C1-6 dihaloalkyl, C1-6 trihaloalkyl, C2-6 haloalkenyl, C2-6 dihaloalkenyl, C2-6 trihaloalkenyl, C1-6 cyanoalkyl, C1-4alkoxy C1-6 alkyl, cycloalkyl C3-8, C3-8 cycloalkylC 1-6 alkyl, benzyl and 5-10 membered heterocyclyl, wherein said phenyl, benzyl or heterocyclyl group may be unsubstituted or substituted with 1 to 3 substituents, each of which is independently selected from the group consisting of ORA, halogen, cyano, nitro, -C (O) C1-4 alkyl, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, C1-6 dihaloalkyl and C1- trihaloalkyl 6; R2 is selected from the group consisting of halogen, cyano, nitro, ORC, N (RB) 2, N (OH) 2, -CHO, -CH = N-OH, -C (O) C1-4 alkyl optionally substituted with 1 at 3 halogens, -SO2-C1-4 alkyl, -C (O) NH-OH, -C (NH2) N = OH, -C (CO2H) = N-OH, -C (NH2) = NH, -C (O-C1-4 alkyl) = NH, -C (NH2) = N-NH2, -NH-C (NH2) = NH, -NH-C (O) NH2, -N = C (-NH-CH2CH2- NH-), -S-CN, -SC (NH2) = NH, -SC (NH2) = N-OH, -CO2H, -CH2-CO2H, -CH (OH) CO2H, -C (O) N (RC ) 2, SO2N (RC) 2, -C (O) -C (O) -NH2, -CH2NH-CONH2, NHSO2RB, -C (O) CO2H, SO3H, CH2SO3H and 5-10 membered heterocyclyl wherein said heterocyclyl group it may be unsubstituted or substituted with 1 to 3 substituents, each of which is independently selected from the group consisting of ORA, halogen, cyano, nitro, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1 haloalkyl -6, C1-6 dihaloalkyl and C1-6 trihaloalkyl; each of R3, R4, R5, R6, R7, R8 and R9 is independently selected from the group consisting of hydrogen, ORA, halogen, cyano, nitro, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, haloalkyl C1-6, dihaloalkyl C1-6 and trihaloalkyl C1-6; each RA is independently selected from the group consisting of hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkyl C1-6 alkyl, phenyl, benzyl and heterocyclyl of 5 - 10 members, each of which is optionally substituted with 1 to 3 halogen atoms; each RB is independently selected from the group consisting of hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-8 cycloalkyl, C 3-8 cycloalkyl, C 1-6 alkyl and 5-10 membered heterocyclyl, each of which is optionally substituted with 1 to 3 halogen atoms; and each RC is independently selected from the group consisting of hydrogen and C1-6 alkyl.

ARP100103628A 2009-10-07 2010-10-06 PIRROLO DERIVATIVES [2,3-B] PYRIDINE LIGANDOS OF STROGEN RECEPTORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USE OF THE SAME IN THE TREATMENT OF THE OSTEOPOROSIS AND DISEASES OF THE CENTRAL NERVOUS SYSTEM, AMONG OTHER AR078535A1 (en)

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GBGB0917571.2A GB0917571D0 (en) 2009-10-07 2009-10-07 Novel estrogen receptor ligands

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AR (1) AR078535A1 (en)
GB (1) GB0917571D0 (en)
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WO (1) WO2011042474A1 (en)

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GB201113538D0 (en) 2011-08-04 2011-09-21 Karobio Ab Novel estrogen receptor ligands
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WO2014026125A1 (en) 2012-08-10 2014-02-13 Incyte Corporation Pyrazine derivatives as fgfr inhibitors
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WO2015082643A1 (en) 2013-12-05 2015-06-11 Karo Bio Ab Estrogen receptor beta agonists for use in treating mesothelioma
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
MA41551A (en) 2015-02-20 2017-12-26 Incyte Corp BICYCLIC HETEROCYCLES USED AS FGFR4 INHIBITORS
ES2751669T3 (en) 2015-02-20 2020-04-01 Incyte Corp Bicyclic heterocycles as FGFR inhibitors
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
JP6790222B2 (en) * 2016-03-25 2020-11-25 羅欣薬業（上海）有限公司Ｌｕｏｘｉｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌ （Ｓｈａｎｇｈａｉ） Ｃｏ．， Ｌｔｄ． Substituted indole compound as an estrogen receptor down regulator
JOP20190086A1 (en) 2016-10-21 2019-04-18 Novartis Ag Naphthyridinone derivatives and their use in the treatment of arrhythmia
AR111960A1 (en) 2017-05-26 2019-09-04 Incyte Corp CRYSTALLINE FORMS OF A FGFR INHIBITOR AND PROCESSES FOR ITS PREPARATION
AU2019262195B2 (en) 2018-05-04 2024-09-12 Incyte Corporation Solid forms of an FGFR inhibitor and processes for preparing the same
MA52493A (en) 2018-05-04 2021-03-10 Incyte Corp FGFR INHIBITOR SALTS
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN115835908A (en) 2019-10-14 2023-03-21 因赛特公司 Bicyclic heterocycles as FGFR inhibitors
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JP2023505258A (en) 2019-12-04 2023-02-08 インサイト・コーポレイション Tricyclic heterocycles as FGFR inhibitors
US11407750B2 (en) 2019-12-04 2022-08-09 Incyte Corporation Derivatives of an FGFR inhibitor
WO2021146424A1 (en) 2020-01-15 2021-07-22 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CA3215903A1 (en) 2021-04-12 2022-10-20 Incyte Corporation Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent
CA3220274A1 (en) 2021-06-09 2022-12-15 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2023198199A1 (en) * 2022-04-15 2023-10-19 先声再明医药有限公司 Myt1 kinase inhibitor

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