AR077050A1 - Derivados de bencimidazol e imidazo[4, 5-c]piridina, una composicion farmaceutica que los comprende y su uso para la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la via hedgehog - Google Patents
Derivados de bencimidazol e imidazo[4, 5-c]piridina, una composicion farmaceutica que los comprende y su uso para la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la via hedgehogInfo
- Publication number
- AR077050A1 AR077050A1 ARP100102048A ARP100102048A AR077050A1 AR 077050 A1 AR077050 A1 AR 077050A1 AR P100102048 A ARP100102048 A AR P100102048A AR P100102048 A ARP100102048 A AR P100102048A AR 077050 A1 AR077050 A1 AR 077050A1
- Authority
- AR
- Argentina
- Prior art keywords
- branched
- alkyl
- linear
- optionally substituted
- compounds
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- GAMYYCRTACQSBR-UHFFFAOYSA-N 4-azabenzimidazole Chemical compound C1=CC=C2NC=NC2=N1 GAMYYCRTACQSBR-UHFFFAOYSA-N 0.000 title 1
- 241000027355 Ferocactus setispinus Species 0.000 title 1
- 201000010099 disease Diseases 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title 1
- 230000005764 inhibitory process Effects 0.000 title 1
- 230000001404 mediated effect Effects 0.000 title 1
- 229940126601 medicinal product Drugs 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000000623 heterocyclic group Chemical group 0.000 abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000005842 heteroatom Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- -1 oxaalquilcarbonilo Chemical group 0.000 abstract 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 1
- 241000289669 Erinaceus europaeus Species 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 125000003342 alkenyl group Chemical group 0.000 abstract 1
- 125000005089 alkenylaminocarbonyl group Chemical group 0.000 abstract 1
- 125000005090 alkenylcarbonyl group Chemical group 0.000 abstract 1
- 125000005092 alkenyloxycarbonyl group Chemical group 0.000 abstract 1
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 1
- 125000004457 alkyl amino carbonyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000003806 alkyl carbonyl amino group Chemical group 0.000 abstract 1
- 125000004448 alkyl carbonyl group Chemical group 0.000 abstract 1
- 125000004414 alkyl thio group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000006165 cyclic alkyl group Chemical group 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000004663 dialkyl amino group Chemical group 0.000 abstract 1
- 230000007717 exclusion Effects 0.000 abstract 1
- 125000001153 fluoro group Chemical group F* 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 230000019491 signal transduction Effects 0.000 abstract 1
- 125000003003 spiro group Chemical group 0.000 abstract 1
- PXQLVRUNWNTZOS-UHFFFAOYSA-N sulfanyl Chemical group [SH] PXQLVRUNWNTZOS-UHFFFAOYSA-N 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 1
Classifications
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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
- 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
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- 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
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
Compuestos heterocíclicos que modulan la vía de senales hedgehog, sus composiciones farmacéuticas y sus aplicaciones terapéuticas, para el cáncer y la osteoporosis. Reivindicacion 1: Compuestos de la formula 1 y sus sales farmacéuticamente aceptables en donde, segun lo permita la valencia, i es 1 o 2; R1 es H; grupo alquilo C1-4 lineal, ramificado o cíclico; R2 es H, CI o F; X es N o CR3; R3 es H; halogeno; un grupo alquilo C1-4 o alcoxi lineal, ramificado o cíclico; Y es como en formulas (2); Z es O o NRx; Rx es H o un alquilo C1-4 lineal, ramificado o cíclico k es 1, 2, 3 o 4; n y p son, de modo independiente, 1, 2 o 3 y la suma de n + p no puede exceder 5; T es H o un grupo alquilo C1-4 lineal o ramificado; T' es una cadena de alquilo C1-3 lineal o ramificado sustituido con un grupo dialquil C1-6-amino o un heterociclo saturado de 4 a 6 miembros que contiene un átomo de nitrogeno y que opcionalmente contiene un segundo heteroátomo seleccionado de N y O, donde cada anillo heterocíclico está opcionalmente sustituido en los átomos de nitrogeno con una cadena de alquilo C1-4; o un heterociclo saturado de 4 a 6 miembros que contiene un átomo de nitrogeno y que opcionalmente contiene un segundo heteroátomo seleccionado de N y O, donde cada anillo heterocíclico está opcionalmente sustituido en los átomos de nitrogeno con una cadena de alquilo C1-4; r es cero, 1, 2 o 3; R' es halogeno; hidroxi; amino; ciano; nitro; oxo; grupo alquilo C1-6 lineal o ramificado, dihaloalquilo, azaalquilo, oxaalquilo, alquilcarbonilo, oxaalquilcarbonilo, alcoxicarbonilo, alquilaminocarbonilo, alquilcarbonilamino, alquenilo, oxaalquenilo, azaalquenilo, alquenilcarbonilo, oxaalquenilcarbonilo, alqueniloxicarbonilo, alquenilaminocarbonilo, alquilamino, dialquilamino, mercaptoalquilo, alcoxi, alquiltio opcionalmente sustituido con uno o varios átomos de fluor; en donde dos grupos R' pueden formar un anillo de 5 a 8 miembros con union espiro o fusionada; con exclusion de los compuestos de formulas (3).
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09007726 | 2009-06-11 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR077050A1 true AR077050A1 (es) | 2011-07-27 |
Family
ID=42331024
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100102048A AR077050A1 (es) | 2009-06-11 | 2010-06-10 | Derivados de bencimidazol e imidazo[4, 5-c]piridina, una composicion farmaceutica que los comprende y su uso para la preparacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la via hedgehog |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US8835648B2 (es) |
| EP (1) | EP2440544B1 (es) |
| JP (1) | JP2012529449A (es) |
| KR (1) | KR20120026534A (es) |
| CN (1) | CN102803246A (es) |
| AR (1) | AR077050A1 (es) |
| AU (1) | AU2010257802A1 (es) |
| BR (1) | BR112012000303A2 (es) |
| CA (1) | CA2765114A1 (es) |
| IL (1) | IL216844A0 (es) |
| MX (1) | MX2011013294A (es) |
| RU (1) | RU2533825C2 (es) |
| TW (1) | TW201102375A (es) |
| WO (1) | WO2010142426A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ586121A (en) * | 2007-12-13 | 2012-03-30 | Siena Biotech Spa | Benzimidazole derivatives as hedgehog pathway antagonists and therapeutic applications thereof |
| JP6240063B2 (ja) | 2011-04-28 | 2017-11-29 | ザ ブロード インスティテュート， インコーポレイテッド | ヒストンデアセチラーゼ阻害剤 |
| CA2880117C (en) * | 2012-07-27 | 2021-04-06 | The Broad Institute, Inc. | Inhibitors of histone deacetylase |
| KR102196882B1 (ko) * | 2012-12-20 | 2020-12-30 | 머크 샤프 앤드 돔 코포레이션 | Hdm2 억제제로서의 치환된 이미다조피리딘 |
| US9914717B2 (en) | 2012-12-20 | 2018-03-13 | The Broad Institute, Inc. | Cycloalkenyl hydroxamic acid derivatives and their use as histone deacetylase inhibitors |
| UY36547A (es) * | 2015-02-05 | 2016-06-01 | Bayer Cropscience Ag | Derivados heterocíclicos condensados bicíclicos sustituidos por 2-(het)arilo como pesticidas |
| US10548908B2 (en) * | 2016-09-15 | 2020-02-04 | Nostopharma, LLC | Compositions and methods for preventing and treating heterotopic ossification and pathologic calcification |
| CN109232533A (zh) * | 2017-09-28 | 2019-01-18 | 北京越之康泰生物医药科技有限公司 | 氮杂环类衍生物、其制备方法及其医药用途 |
| WO2019062657A1 (zh) * | 2017-09-30 | 2019-04-04 | 北京越之康泰生物医药科技有限公司 | 氮杂环类衍生物、其制备方法及其医药用途 |
| JP2021510733A (ja) | 2018-01-12 | 2021-04-30 | ケーディーエーシー セラピューティクス，インコーポレーテッドＫｄａｃ Ｔｈｅｒａｐｅｕｔｉｃｓ， Ｉｎｃ． | がんの処置のための選択的ヒストンデアセチラーゼ３（ｈｄａｃ３）インヒビターと免疫治療剤との組み合わせ |
| CN112805000A (zh) * | 2018-08-06 | 2021-05-14 | 小利兰·斯坦福大学董事会 | 作为ppargc1a激活剂用于治疗神经退行性疾病的2-芳基苯并咪唑 |
| CA3109386A1 (en) | 2018-08-17 | 2020-03-19 | Ptc Therapeutics, Inc. | Use of 5-fluoro-2-(6-fluoro-2-methyl-1h-benzo(d)imidazol-1-yl)-n4-(4-(trifluoromethyl)phenyl)pyrimidine-4,6-diamine in the treatment of pancreatic cancer |
| US10689360B1 (en) * | 2019-01-30 | 2020-06-23 | Insilico Medicine Ip Limited | TLR inhibitors |
| CN114790177B (zh) * | 2021-01-26 | 2024-03-26 | 首都医科大学附属北京天坛医院 | 新型Hedgehog信号通路抑制剂 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SU879945A1 (ru) * | 1980-06-13 | 1998-05-27 | Институт физико-органической химии и углехимии АН Украинской ССР | Производные имидазо[4,5-c]пиридина, обладающие акарицидной активностью |
| FR2674856B1 (fr) * | 1991-04-05 | 1993-07-30 | Esteve Labor Dr | Nouveaux antihistaminiques non sedatifs, derives de benzimidazole, leur procede de preparation et leur utilisation en tant que medicaments. |
| DE59911249D1 (de) * | 1998-11-03 | 2005-01-13 | Abbott Gmbh & Co Kg | Substituierte 2-phenylbenzimidazole, deren herstellung und anwendung |
| KR20040031782A (ko) * | 2001-07-27 | 2004-04-13 | 쿠리스 인코퍼레이션 | 헤지호그 신호전달 경로의 조절물질, 이를 함유하는조성물 및 이의 용도 |
| EP1651631A1 (en) * | 2003-08-01 | 2006-05-03 | Genelabs Technologies, Inc. | Bicyclic imidazol derivatives against flaviviridae |
| JP2008519044A (ja) * | 2004-11-03 | 2008-06-05 | キューリス，インコーポレーテッド | ヘッジホッグ・シグナル伝達経路の伝達物質、調合物、及び、それに関連する使用 |
| PE20080948A1 (es) * | 2006-07-25 | 2008-09-10 | Irm Llc | Derivados de imidazol como moduladores de la senda de hedgehog |
| NZ581889A (en) * | 2007-06-29 | 2011-05-27 | Pfizer | Benzimidazole derivatives |
| NZ586121A (en) * | 2007-12-13 | 2012-03-30 | Siena Biotech Spa | Benzimidazole derivatives as hedgehog pathway antagonists and therapeutic applications thereof |
-
2010
- 2010-06-09 US US13/377,290 patent/US8835648B2/en not_active Expired - Fee Related
- 2010-06-09 CA CA2765114A patent/CA2765114A1/en not_active Abandoned
- 2010-06-09 WO PCT/EP2010/003441 patent/WO2010142426A1/en not_active Ceased
- 2010-06-09 RU RU2011150250/04A patent/RU2533825C2/ru not_active IP Right Cessation
- 2010-06-09 BR BR112012000303A patent/BR112012000303A2/pt not_active IP Right Cessation
- 2010-06-09 MX MX2011013294A patent/MX2011013294A/es active IP Right Grant
- 2010-06-09 EP EP10724710.8A patent/EP2440544B1/en active Active
- 2010-06-09 AU AU2010257802A patent/AU2010257802A1/en not_active Abandoned
- 2010-06-09 KR KR1020117029632A patent/KR20120026534A/ko not_active Withdrawn
- 2010-06-09 JP JP2012514381A patent/JP2012529449A/ja not_active Ceased
- 2010-06-09 CN CN2010800256535A patent/CN102803246A/zh active Pending
- 2010-06-10 TW TW099118879A patent/TW201102375A/zh unknown
- 2010-06-10 AR ARP100102048A patent/AR077050A1/es unknown
-
2011
- 2011-12-08 IL IL216844A patent/IL216844A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| US20120088752A1 (en) | 2012-04-12 |
| WO2010142426A1 (en) | 2010-12-16 |
| JP2012529449A (ja) | 2012-11-22 |
| US8835648B2 (en) | 2014-09-16 |
| EP2440544A1 (en) | 2012-04-18 |
| MX2011013294A (es) | 2012-01-12 |
| EP2440544B1 (en) | 2013-08-14 |
| RU2011150250A (ru) | 2013-07-20 |
| KR20120026534A (ko) | 2012-03-19 |
| CN102803246A (zh) | 2012-11-28 |
| CA2765114A1 (en) | 2010-12-16 |
| IL216844A0 (en) | 2012-03-01 |
| RU2533825C2 (ru) | 2014-11-20 |
| AU2010257802A1 (en) | 2012-01-12 |
| TW201102375A (en) | 2011-01-16 |
| BR112012000303A2 (pt) | 2016-11-16 |
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