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 OTHERInfo
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- 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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- alkyl
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- alkynyl
- alkenyl
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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
- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
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- 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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- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
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- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
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- Hospice & Palliative Care (AREA)
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- 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.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0917571.2A GB0917571D0 (en) | 2009-10-07 | 2009-10-07 | Novel estrogen receptor ligands |
Publications (1)
Publication Number | Publication Date |
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AR078535A1 true AR078535A1 (en) | 2011-11-16 |
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Family Applications (1)
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ARP100103628A AR078535A1 (en) | 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 |
Country Status (4)
Country | Link |
---|---|
AR (1) | AR078535A1 (en) |
GB (1) | GB0917571D0 (en) |
TW (1) | TW201118094A (en) |
WO (1) | WO2011042474A1 (en) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
GB201113538D0 (en) | 2011-08-04 | 2011-09-21 | Karobio Ab | Novel estrogen receptor ligands |
RS55908B1 (en) | 2012-06-13 | 2017-09-29 | Incyte Holdings Corp | Substituted tricyclic compounds as fgfr inhibitors |
WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
MX367878B (en) | 2013-04-19 | 2019-09-10 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors. |
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 |
WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
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 |
Family Cites Families (3)
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US7250440B2 (en) | 2003-08-12 | 2007-07-31 | Wyeth | (Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents |
US8013006B2 (en) | 2004-07-14 | 2011-09-06 | Ptc Therapeutics, Inc. | Methods for treating hepatitis C |
WO2008064830A1 (en) * | 2006-11-27 | 2008-06-05 | Ucb Pharma, S.A. | Bicyclic and heterobicyclic derivatives, processes for preparing them and their pharmaceutical uses |
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2009
- 2009-10-07 GB GBGB0917571.2A patent/GB0917571D0/en not_active Ceased
-
2010
- 2010-10-06 TW TW099133971A patent/TW201118094A/en unknown
- 2010-10-06 AR ARP100103628A patent/AR078535A1/en unknown
- 2010-10-06 WO PCT/EP2010/064940 patent/WO2011042474A1/en active Application Filing
Also Published As
Publication number | Publication date |
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WO2011042474A1 (en) | 2011-04-14 |
GB0917571D0 (en) | 2009-11-25 |
TW201118094A (en) | 2011-06-01 |
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