AR038276A1 - Metodos para incrementar la formacion osea. - Google Patents
Metodos para incrementar la formacion osea.Info
- Publication number
- AR038276A1 AR038276A1 ARP030100043A ARP030100043A AR038276A1 AR 038276 A1 AR038276 A1 AR 038276A1 AR P030100043 A ARP030100043 A AR P030100043A AR P030100043 A ARP030100043 A AR P030100043A AR 038276 A1 AR038276 A1 AR 038276A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- heteroalkyl
- hydrogen
- heterocyclic
- cycloalkyl
- Prior art date
Links
- 125000000217 alkyl group Chemical group 0.000 abstract 7
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 7
- 239000001257 hydrogen Substances 0.000 abstract 7
- 125000004435 hydrogen atom Chemical class [H]* 0.000 abstract 6
- -1 cyano, nitro, amino Chemical group 0.000 abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 abstract 5
- 125000004442 acylamino group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000004414 alkyl thio group Chemical group 0.000 abstract 3
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 108010001483 Glycogen Synthase Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- YAEMHJKFIIIULI-UHFFFAOYSA-N n-(4-methoxybenzyl)-n'-(5-nitro-1,3-thiazol-2-yl)urea Chemical compound C1=CC(OC)=CC=C1CNC(=O)NC1=NC=C([N+]([O-])=O)S1 YAEMHJKFIIIULI-UHFFFAOYSA-N 0.000 abstract 1
- 230000011164 ossification Effects 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Rheumatology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Uso de inhibidores de la sintasa quinasa-3b de glucógeno para aumentar la formación ósea. Reivindicación 9: El uso o método de acuerdo con cualquiera de las reivindicaciones 1 a 8, en el cual el inhibidor de GSK-3b es un compuesto representado por la Fórmula (1), en la cual: R1 y R2 representan independientemente hidrógeno, alquilo, halo, haloalquilo, alquiltio, hidroxi, alcoxi, ciano, nitro, amino, acilamino, monoalquilamino, o dialquilamino; R3 representa hidrógeno, alquilo, cicloalquilo, heteroalquilo, -COR7 (en donde R7 es hidrógeno o alquilo), o fenilo optativamente sustituido con uno o dos sustituyentes independientemente seleccionados entre el grupo que consiste en hidrógeno, alquilo, haloalquilo, alquiltio, hidroxi, alcoxi, ciano, nitro, amino, acilamino, monoalquilamino y dialquilamino; R4 y R5 representan independientemente hidrógeno, alquilo, halo, haloalquilo, alquiltio, hidroxi, alcoxi, ciano, nitro, amino, acilamino, monoalquilamino o dialquilamino; R6 es heteroalquilo, heterociclico, heterociclialquilo, heterociclico sustituido con heteroalquilo, cicloalquilo sustituido con heteroalquilo, cicloalquilo hetereosustituido, -OR8, -S(O)nR8 (en donde n es 0 a 2; y R8 es heteroalquilo, heteroaralquilo, heterociclico o heterociclialquilo), -NR9R10 (en donde R9 es hidrógeno o alquilo y R10 es heteroalquilo, heteroaralquilo, cicloalquilo heterosustituido, heterociclilo o heterociclialquilo) o -X- (alquilen)-Y-Z (en donde X es un enlace covalente, o, -NH- ó -S(O)n1- donde n1 es 0 a 2, e Y es -O-, -NH- ó -S- y Z es heteroalquilo o SiR11R12R13 donde R11, R12 y R13 son independientemente hidrógeno o alquilo) o R6 junto con R4 forma un grupo metilendioxi o etilendioxi cuando son adyacentes entre sí; o su sal farmacéuticamente aceptable.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US34805502P | 2002-01-10 | 2002-01-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038276A1 true AR038276A1 (es) | 2005-01-12 |
Family
ID=23366458
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP030100043A AR038276A1 (es) | 2002-01-10 | 2003-01-08 | Metodos para incrementar la formacion osea. |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US7476676B2 (es) |
| EP (1) | EP1465610B1 (es) |
| JP (1) | JP4237066B2 (es) |
| CN (1) | CN100409840C (es) |
| AR (1) | AR038276A1 (es) |
| AU (1) | AU2003235798A1 (es) |
| CA (1) | CA2471565C (es) |
| DE (1) | DE60325551D1 (es) |
| ES (1) | ES2316756T3 (es) |
| WO (1) | WO2003057202A1 (es) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20060056377A (ko) * | 2003-08-13 | 2006-05-24 | 카이론 코포레이션 | Gsk-3 억제제 및 그것의 사용 |
| US20050064044A1 (en) * | 2003-09-19 | 2005-03-24 | Georges Rawadi | GSK-3beta inhibitors in the treatment of bone-related diseases |
| US20050171015A1 (en) * | 2003-10-31 | 2005-08-04 | Crabtree Gerald R. | Methods and agents for enhancing bone formation or preventing bone loss |
| WO2006061212A1 (en) | 2004-12-08 | 2006-06-15 | Johannes Gutenberg-Universität Mainz | 3-(indolyl)-4-arylmaleimide derivatives and their use as angiogenesis inhibitors |
| US7670742B2 (en) | 2005-03-15 | 2010-03-02 | Ricoh Company, Ltd. | Recording material, toner, liquid developer and image forming method using the same |
| EP1885454A2 (en) | 2005-05-04 | 2008-02-13 | DeveloGen Aktiengesellschaft | Use of gsk-3 inhibitors for preventing and treating pancreatic autoimmune disorders |
| EP1757607A1 (en) | 2005-08-24 | 2007-02-28 | Molisa GmbH | N5-substituted benzo¬2,3|azepino¬4,5-b|indol-6-ones for treating tropical diseases |
| TW200800203A (en) | 2006-03-08 | 2008-01-01 | Astrazeneca Ab | New use |
| EP2125683B1 (en) * | 2006-12-19 | 2013-10-23 | The Board of Trustees of the University of Illinois | 3-benzofuranyl-4-indolyl-maleimides as potent gsk-3 inhibitors for neurodegenerative disorders |
| US20100137330A1 (en) * | 2007-03-08 | 2010-06-03 | Ratan Bhat | Use |
| EP2343291A1 (en) | 2009-12-18 | 2011-07-13 | Johannes Gutenberg-Universität Mainz | 3-(Indolyl)- or 3-(Azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment |
| KR20120120307A (ko) | 2010-01-19 | 2012-11-01 | 아스트라제네카 아베 | 피라진 유도체 |
| TWI507381B (zh) | 2010-09-08 | 2015-11-11 | Sumitomo Chemical Co | 製造嗒酮化合物的方法及其中間物 |
| WO2012035770A1 (ja) * | 2010-09-15 | 2012-03-22 | 国立大学法人 新潟大学 | グリコーゲンを含有する骨形成促進剤 |
| EP2474541A1 (en) | 2010-12-23 | 2012-07-11 | Johannes- Gutenberg-Universität Mainz | Conjugated 3-(indolyl)- and 3-(azaindolyl)-4-arylmaleimide compounds and their use in tumor treatment |
| EP3187495A1 (en) | 2015-12-30 | 2017-07-05 | Johannes Gutenberg-Universität Mainz | 3-(5-fluoroindolyl)-4-arylmaleimide compounds and their use in tumor treatment |
| WO2018132636A1 (en) * | 2017-01-12 | 2018-07-19 | The Research Foundation For The State University Of New York | [18f]maleimide-based glycogen synthase kinase-3beta ligands for positron emission tomography imaging and radiosynthesis method |
| CN113248472B (zh) * | 2020-02-12 | 2022-06-28 | 中国药科大学 | 抗骨质疏松化合物及其衍生物,药物组合物、制备方法和应用 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE274510T1 (de) * | 1998-06-19 | 2004-09-15 | Chiron Corp | Glycogen synthase kinase 3 inhibitoren |
| ATE284387T1 (de) * | 1998-10-08 | 2004-12-15 | Smithkline Beecham Plc | 3-(3-chloro-4-hydroxyphenylamino)-4-(2- nitrophenyl)-1h-pyrrol-2,5-dion als glykogen synthase kinase-3 inhibitor (gsk-3) |
| GB9828640D0 (en) * | 1998-12-23 | 1999-02-17 | Smithkline Beecham Plc | Novel method and compounds |
| US6455525B1 (en) * | 1999-11-04 | 2002-09-24 | Cephalon, Inc. | Heterocyclic substituted pyrazolones |
| EP1200422A2 (en) * | 2000-02-05 | 2002-05-02 | Vertex Pharmaceuticals Incorporated | Pyrazole compositions useful as inhibitors of erk |
| JP4739632B2 (ja) * | 2000-02-05 | 2011-08-03 | バーテックス ファーマシューティカルズ インコーポレイテッド | Erkのインヒビターとして有用なピラゾール組成物 |
| HUP0301431A2 (hu) * | 2000-07-27 | 2003-08-28 | F. Hoffmann-La Roche Ag. | 3-Indolil-4-fenil-1H-pirrol-2,5-dion-származékok, mint glikogén szintáz kináz-3béta inhibitorok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények |
| MXPA03005609A (es) * | 2000-12-21 | 2003-10-06 | Vertex Pharma | Compuestos de pirazol utiles como inhibidores de la proteina cinasa. |
| MY130778A (en) * | 2001-02-09 | 2007-07-31 | Vertex Pharma | Heterocyclic inhibitiors of erk2 and uses thereof |
-
2003
- 2003-01-07 EP EP03729222A patent/EP1465610B1/en not_active Expired - Lifetime
- 2003-01-07 CN CNB038021269A patent/CN100409840C/zh not_active Expired - Lifetime
- 2003-01-07 AU AU2003235798A patent/AU2003235798A1/en not_active Abandoned
- 2003-01-07 CA CA002471565A patent/CA2471565C/en not_active Expired - Lifetime
- 2003-01-07 JP JP2003557560A patent/JP4237066B2/ja not_active Expired - Lifetime
- 2003-01-07 WO PCT/EP2003/000049 patent/WO2003057202A1/en not_active Ceased
- 2003-01-07 ES ES03729222T patent/ES2316756T3/es not_active Expired - Lifetime
- 2003-01-07 DE DE60325551T patent/DE60325551D1/de not_active Expired - Lifetime
- 2003-01-08 AR ARP030100043A patent/AR038276A1/es unknown
- 2003-01-09 US US10/339,193 patent/US7476676B2/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| EP1465610A1 (en) | 2004-10-13 |
| WO2003057202A8 (en) | 2003-12-11 |
| WO2003057202A1 (en) | 2003-07-17 |
| US20030176484A1 (en) | 2003-09-18 |
| CA2471565A1 (en) | 2003-07-17 |
| CN100409840C (zh) | 2008-08-13 |
| JP4237066B2 (ja) | 2009-03-11 |
| ES2316756T3 (es) | 2009-04-16 |
| EP1465610B1 (en) | 2008-12-31 |
| AU2003235798A1 (en) | 2003-07-24 |
| CN1703207A (zh) | 2005-11-30 |
| AU2003235798A8 (en) | 2003-07-24 |
| DE60325551D1 (de) | 2009-02-12 |
| CA2471565C (en) | 2009-10-27 |
| US7476676B2 (en) | 2009-01-13 |
| JP2005519056A (ja) | 2005-06-30 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |