AR075006A1 - Derivados de quinazolinona utiles comoantagonistas de vanilloides - Google Patents
Derivados de quinazolinona utiles comoantagonistas de vanilloidesInfo
- Publication number
- AR075006A1 AR075006A1 ARP100100055A ARP100100055A AR075006A1 AR 075006 A1 AR075006 A1 AR 075006A1 AR P100100055 A ARP100100055 A AR P100100055A AR P100100055 A ARP100100055 A AR P100100055A AR 075006 A1 AR075006 A1 AR 075006A1
- Authority
- AR
- Argentina
- Prior art keywords
- carbon atoms
- alkyl
- alkoxy
- formula
- compound
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
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- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
- A61P11/00—Drugs for disorders of the respiratory system
- A61P11/06—Antiasthmatics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/04—Antipruritics
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
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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
-
- 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
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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
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- 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
- A61P25/06—Antimigraine agents
-
- 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
- A61P25/08—Antiepileptics; Anticonvulsants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- 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
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/10—Antioedematous agents; Diuretics
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/90—Oxygen atoms with acyclic radicals attached in position 2 or 3
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Neurology (AREA)
- Pain & Pain Management (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Ophthalmology & Optometry (AREA)
- Immunology (AREA)
- Urology & Nephrology (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Reivindicacion 1: La forma del cristal B del 4-(7-hidroxi-2-isopropil-4-oxo-4H-quinazolin-3-il)-benzonitrilo, la cual tiene la formula estructural (4), caracterizada por un patron de difraccion de rayos-X que tiene tres o más picos en valores 2q seleccionados a partir de 9.3, 10.6 y 14.4 +- 0.2 s2q. Reivindicacion 7: Un proceso o método para la fabricacion de un compuesto de quinazolinona de la formula (1); en donde R1 es alquilo de 1 a 6 átomos de carbono, (alquilo de 1 a 6 átomos de carbono)-alquilo de 1 a 6 átomos de carbono, di-(alquilo de 1 a 6 átomos de carbono)-alquilo de 1 a 6 átomos de carbono, o cicloalquilo de 3 a 6 átomos de carbono, di(trifluorometil)-alquilo de 1 a 6 átomos de carbono, R9-O-(alquilo de 1 a 6 átomos de carbono)-, en donde la cadena de alquilo está opcionalmente sustituida por trifluorometilo, (NC)-alquilo de 1 a 6 átomos de carbono-, (R10R11N-)alquilo de 1 a 6 átomos de carbono-, o (alquilo de 1 a 6 átomos de carbono)-SO2-(alquilo de 1 a 6 átomos de carbono)-, en donde R9, R10 y R11, son cada uno independientemente H o alquilo de 1 a 6 átomos de carbono; cada R2 es independientemente halogeno, alquilo de 1 a 6 átomos de carbono, alquilo de 1 a 6 átomos de carbono sustituido por halogeno, hidroxi-alquilo de 1 a 6 átomos de carbono, ciano, un grupo -C(=O)-R2a, en donde R2a es alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, R10R11N-, R10R11N-(alquilo de 1 a 6 átomos de carbono)-, -SO2-(alquilo de 1 a 6 átomos de carbono), R9-O-(C=O)-, en donde R9, R10 y R11 son como se definen anteriormente, fenilo insustituido o sustituido, en donde los sustituyentes son de 1 a 4 sustituyentes independientemente seleccionados a partir del grupo que consiste en halogeno, hidroxilo, y alquilo de 1 a 6 átomos de carbono, o un anillo heterocíclico saturado o insaturado de 5 o 6 miembros, que tiene uno, dos o tres heteroátomos seleccionados a partir de N, O y S, y opcionalmente incluyendo un sustituyente adicional seleccionado a partir de halogeno; R3 es hidrogeno, halogeno, alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, alquinilo de 2 a 6 átomos de carbono, hidroxilo, alquilo de 1 a 6 átomos de carbono sustituido por hidroxilo, alcoxilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 6 átomos de carbono, ciano, -C(=O)H, fenilo, (cicloalquilo de 3 a 6 átomos de carbono)-alcoxilo de 1 a 6 átomos de carbono, (alcoxilo de 1 a 6 átomos de carbono-carbonil-amino)-alcoxilo de 1 a 6 átomos de carbono, o (alquilo de 1 a 6 átomos de carbono-carbonil-amino)-alcoxilo de 1 a 6 átomos de carbono; R4 es H (= hidrogeno), o R4-O es hidroxilo esterificado o hidroxilo eterificado; en especial R4 es H; R5 es hidrogeno o hidroxilo; R6 es hidrogeno, halogeno, alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, alquinilo de 2 a 6 átomos de carbono, hidroxilo, alquilo de 1 a 6 átomos de carbono sustituido por hidroxilo, alcoxilo de 1 a 6 átomos de carbono, cicloalquilo de 3 a 6 átomos de carbono, ciano, -C(=O)H, fenilo, (cicloalquilo de 3 a 6 átomos de carbono)-alquilo de 1 a 6 átomos de carbono, (cicloalquilo de 3 a 6 átomos de carbono)-alcoxilo de 1 a 6 átomos de carbono, (alcoxilo de 1 a 6 átomos de carbono-carbonilamino)-alcoxilo de 1 a 6 átomos de carbono o (alquilo de 1 a 6 átomos de carbono-carbonil-amino)-alcoxilo de 1 a 6 átomos de carbono, (amino)-alcoxilo de 1 a 6 átomos de carbono, (dimetil-amino)-alcoxilo de 1 a 6 átomos de carbono, o (alcoxilo de 1 a 6 átomos de carbono-carbonil)-alcoxilo de 1 a 6 átomos de carbono; m es de 1 a 5, por ejemplo, 1 o 2, en forma libre o en forma de sal, comprendiendo este método o proceso, hacer reaccionar un compuesto de la formula (2) en donde R4* es R1*-C(=O)-, en donde R1* se selecciona independientemente a partir del grupo de significados de R1 como se definen para un compuesto de la formula (1), de tal manera que R1* y R1 son idénticos o diferentes uno del otro, o R4* es H, y R1 y R3, R5 y R6 son como se definen para un compuesto de la formula (1), o una sal del mismo, bajo condiciones de condensacion y ciclacion simultáneas o en secuencia, con un compuesto de anilina de la formula (3) en donde R2 y m son como se definen anteriormente para un compuesto de la formula (1), para dar un compuesto correspondiente de la formula (1), en donde R4 es R1*-C(=O)- con R1* como se define para un compuesto de la formula (2), o R4 es H, y los sustituyentes restantes son como se definen para la formula (1) respectivamente; y, si se desea, acilar o eterificar un grupo hidroxilo libre R4-O con un compuesto de la formula: R4''-X, en donde X es OH o un derivado activo del mismo, y R4'' es una fraccion de acilo esterificante o una fraccion eterificante que completa el hidroxilo esterificado o eterificado R4-O, como se define para un compuesto de la formula (1), respectivamente; y/o, si se desea, convertir un compuesto libre resultante de la formula (1), o de preferencia (1a), en su sal, o convertir una sal resultante de un compuesto de la formula (1), o de preferencia (1a), en su forma libre.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US14425009P | 2009-01-13 | 2009-01-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR075006A1 true AR075006A1 (es) | 2011-03-02 |
Family
ID=42167396
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP100100055A AR075006A1 (es) | 2009-01-13 | 2010-01-11 | Derivados de quinazolinona utiles comoantagonistas de vanilloides |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US8349852B2 (es) |
| EP (1) | EP2387440B1 (es) |
| JP (1) | JP2012515150A (es) |
| KR (1) | KR20110104996A (es) |
| CN (1) | CN102281920A (es) |
| AR (1) | AR075006A1 (es) |
| AU (1) | AU2010206233B2 (es) |
| BR (1) | BRPI1006909A2 (es) |
| CA (2) | CA2946304A1 (es) |
| CO (1) | CO6400202A2 (es) |
| CR (1) | CR20110369A (es) |
| CU (1) | CU20110148A7 (es) |
| EA (1) | EA201101063A1 (es) |
| EC (1) | ECSP11011195A (es) |
| ES (1) | ES2614612T3 (es) |
| IL (1) | IL213869A0 (es) |
| MA (1) | MA32957B1 (es) |
| MX (1) | MX2011007444A (es) |
| NZ (1) | NZ593877A (es) |
| PE (1) | PE20110776A1 (es) |
| PL (1) | PL2387440T3 (es) |
| PT (1) | PT2387440T (es) |
| SG (1) | SG172808A1 (es) |
| TN (1) | TN2011000326A1 (es) |
| TW (1) | TW201036951A (es) |
| UY (1) | UY32381A (es) |
| WO (1) | WO2010084050A2 (es) |
| ZA (1) | ZA201104873B (es) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0412769D0 (en) | 2004-06-08 | 2004-07-07 | Novartis Ag | Organic compounds |
| PE20142083A1 (es) * | 2011-09-16 | 2014-12-30 | Fovea Pharmaceuticals | Derivados de anilina, su preparacion y su aplicacion terapeutica |
| KR101789430B1 (ko) * | 2016-06-28 | 2017-10-25 | 동국대학교 산학협력단 | Smo 저해 활성을 갖는 신규 화합물 및 이를 유효성분으로 포함하는 암 예방 또는 치료용 조성물 |
| CN108863949B (zh) * | 2018-07-09 | 2021-01-15 | 湖南博隽生物医药有限公司 | 一种用于治疗慢性炎性痛的辣椒素受体拮抗剂及合成方法 |
| JP6994061B2 (ja) * | 2019-02-15 | 2022-01-14 | ノバルティス アーゲー | ４－（７－ヒドロキシ－２－イソプロピル－４－オキソ－４ｈ－キナゾリン－３－イル）－ベンゾニトリルの製剤 |
| EP4431497A1 (en) | 2019-02-15 | 2024-09-18 | Bausch + Lomb Ireland Limited | Crystalline forms of 4-(7-hydroxy-2-isopropyl-4-oxo-4h-quinazolin-3-yl)-benzonitrile and formulations thereof |
| CA3130038A1 (en) * | 2019-02-15 | 2020-08-20 | Novartis Ag | Methods for treating ocular surface pain |
| WO2021009664A1 (en) | 2019-07-15 | 2021-01-21 | Novartis Ag | Methods for treating meibomian gland dysfunction with liver x receptor agonists |
| MX2022006783A (es) | 2019-12-10 | 2022-07-11 | Hoffmann La Roche | Nuevos derivados de metilquinazolinona. |
| CN116419918A (zh) | 2020-08-06 | 2023-07-11 | 诺华股份有限公司 | 4-(7-羟基-2-异丙基-4-氧代-4h-喹唑啉-3-基)-苄腈的结晶形式及其配制品 |
| EP4225279A1 (en) | 2020-10-07 | 2023-08-16 | Novartis AG | Drug containing dissolvable ocular inserts and method of using same |
| WO2022105792A1 (zh) * | 2020-11-17 | 2022-05-27 | 苏州晶云药物科技股份有限公司 | 一种喹唑啉酮衍生物的新晶型及其制备方法 |
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| GB9802251D0 (en) | 1998-02-03 | 1998-04-01 | Ciba Geigy Ag | Organic compounds |
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- 2011-07-01 ZA ZA2011/04873A patent/ZA201104873B/en unknown
- 2011-07-11 CU CU20110148A patent/CU20110148A7/es unknown
- 2011-07-11 EC EC2011011195A patent/ECSP11011195A/es unknown
- 2011-07-22 CO CO11092089A patent/CO6400202A2/es not_active Application Discontinuation
- 2011-07-29 TN TN2011000326A patent/TN2011000326A1/fr unknown
-
2012
- 2012-09-12 US US13/612,259 patent/US20130060029A1/en not_active Abandoned
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