ECSP11011412A - Atropisómeros de derivados de 2-purinil-3-tolil-quinazolinona y métodos de uso - Google Patents
Atropisómeros de derivados de 2-purinil-3-tolil-quinazolinona y métodos de usoInfo
- Publication number
- ECSP11011412A ECSP11011412A ECSP11011412A ECSP11011412A EC SP11011412 A ECSP11011412 A EC SP11011412A EC SP11011412 A ECSP11011412 A EC SP11011412A EC SP11011412 A ECSP11011412 A EC SP11011412A
- Authority
- EC
- Ecuador
- Prior art keywords
- methods
- quinazolinona
- atropisomeros
- purinil
- tolil
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 abstract 4
- 102000001708 Protein Isoforms Human genes 0.000 abstract 2
- 108010029485 Protein Isoforms Proteins 0.000 abstract 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 abstract 1
- GNWHRHGTIBRNSM-UHFFFAOYSA-N IC-87114 Chemical compound CC1=CC=CC=C1N1C(=O)C2=C(C)C=CC=C2N=C1CN1C2=NC=NC(N)=C2N=C1 GNWHRHGTIBRNSM-UHFFFAOYSA-N 0.000 abstract 1
- 108091007960 PI3Ks Proteins 0.000 abstract 1
- 230000004968 inflammatory condition Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D473/00—Heterocyclic compounds containing purine ring systems
- C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
- C07D473/32—Nitrogen atom
- C07D473/34—Nitrogen atom attached in position 6, e.g. adenine
-
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- 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
- A61P11/02—Nasal agents, e.g. decongestants
-
- 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
-
- 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
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- 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
- A61P25/00—Drugs for disorders of the nervous system
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- 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
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/08—Antiallergic agents
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pulmonology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pain & Pain Management (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Otolaryngology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La invención proporciona compuestos, composiciones y métodos para tratar ciertas afecciones inflamatorias y / o oncología mediante la administración de un compuesto que inhibe las isoformas de PI3K, en particular, la isoforma delta. Además, proporciona estereoisómeros específicos de un compuesto útil para estos métodos. En particular, el compuesto es un atropisómero ópticamente activo de 2-((6 amino-9H-purin-9-il) metil)-5-metil-3-o-tolylquinazolin-4 (3H)-ona.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16298009P | 2009-03-24 | 2009-03-24 | |
| US23155009P | 2009-08-05 | 2009-08-05 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP11011412A true ECSP11011412A (es) | 2012-03-30 |
Family
ID=42289320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP11011412 ECSP11011412A (es) | 2009-03-24 | 2011-10-21 | Atropisómeros de derivados de 2-purinil-3-tolil-quinazolinona y métodos de uso |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US8440677B2 (es) |
| EP (1) | EP2411391A1 (es) |
| JP (1) | JP2012521994A (es) |
| KR (1) | KR20120002995A (es) |
| CN (1) | CN102439012A (es) |
| AP (1) | AP2011005943A0 (es) |
| AU (1) | AU2010229968A1 (es) |
| BR (1) | BRPI1012333A2 (es) |
| CA (1) | CA2756347A1 (es) |
| CL (1) | CL2011002359A1 (es) |
| CO (1) | CO6450655A2 (es) |
| EA (1) | EA019499B1 (es) |
| EC (1) | ECSP11011412A (es) |
| IL (1) | IL215251A0 (es) |
| MX (1) | MX2011009955A (es) |
| NZ (1) | NZ595307A (es) |
| PE (1) | PE20120602A1 (es) |
| SG (1) | SG174529A1 (es) |
| WO (1) | WO2010111432A1 (es) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6667300B2 (en) | 2000-04-25 | 2003-12-23 | Icos Corporation | Inhibitors of human phosphatidylinositol 3-kinase delta |
| US20050043239A1 (en) * | 2003-08-14 | 2005-02-24 | Jason Douangpanya | Methods of inhibiting immune responses stimulated by an endogenous factor |
| LT2612862T (lt) | 2004-05-13 | 2017-01-25 | Icos Corporation | Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai |
| US9492449B2 (en) | 2008-11-13 | 2016-11-15 | Gilead Calistoga Llc | Therapies for hematologic malignancies |
| KR20170060179A (ko) | 2008-11-13 | 2017-05-31 | 길리아드 칼리스토가 엘엘씨 | 혈액 종양에 대한 요법 |
| AU2010229968A1 (en) | 2009-03-24 | 2011-10-13 | Gilead Calistoga Llc | Atropisomers of2-purinyl-3-tolyl-quinazolinone derivatives and methods of use |
| JP2012524126A (ja) * | 2009-04-20 | 2012-10-11 | ギリアド カリストガ リミテッド ライアビリティ カンパニー | 固形腫瘍の治療方法 |
| ES2739973T3 (es) | 2009-05-29 | 2020-02-05 | Merck Sharp & Dohme | Inhibidores de PDE10 radiomarcados |
| CA2768843A1 (en) * | 2009-07-21 | 2011-01-27 | Gilead Calistoga Llc | Treatment of liver disorders with pi3k inhibitors |
| GB0918249D0 (en) | 2009-10-19 | 2009-12-02 | Respivert Ltd | Compounds |
| UY33337A (es) | 2010-10-18 | 2011-10-31 | Respivert Ltd | DERIVADOS SUSTITUIDOS DE 1H-PIRAZOL[ 3,4-d]PIRIMIDINA COMO INHIBIDORES DE LAS FOSFOINOSITIDA 3-QUINASAS |
| EP2518071A1 (en) * | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Imidazopyridine derivatives as PI3K inhibitors |
| EP2518070A1 (en) * | 2011-04-29 | 2012-10-31 | Almirall, S.A. | Pyrrolotriazinone derivatives as PI3K inhibitors |
| ES2661510T3 (es) | 2011-12-15 | 2018-04-02 | Novartis Ag | Uso de inhibidores de la actividad o función de PI3K |
| ES2848273T3 (es) | 2012-03-05 | 2021-08-06 | Gilead Calistoga Llc | Formas polimórficas de (S)-2-(1-(9H-purin-6-ilamino)propilo)-5-fluoro-3-fenilquinazolina-4(3H)-ona |
| NZ627963A (en) | 2012-03-13 | 2015-08-28 | Respivert Ltd | Dry powder pharmaceutical formulations for inhalation of a compound that inhibits pi3 kinase |
| PT2870157T (pt) | 2012-07-04 | 2017-11-27 | Rhizen Pharmaceuticals S A | Inibidores seletivos de delta pi3k |
| WO2014015523A1 (en) * | 2012-07-27 | 2014-01-30 | Hutchison Medipharma Limited | Novel heteroaryl and heterocycle compounds, compositions and methods |
| WO2014060431A1 (en) * | 2012-10-16 | 2014-04-24 | Almirall, S.A. | Pyrrolotriazinone derivatives as pi3k inhibitors |
| GEP201706623B (en) | 2012-10-16 | 2017-02-10 | Almirall Sa | Pyrrolotriazinone derivatives as pi3k inhibitors |
| HK1214159A1 (zh) | 2012-11-08 | 2016-07-22 | Rhizen Pharmaceuticals S.A. | 含有PDE4抑制剂和PI3δ或双重PI3δ-γ激酶抑制剂的药物组合物 |
| TW201522341A (zh) * | 2013-03-15 | 2015-06-16 | Respivert Ltd | 化合物 |
| AR095353A1 (es) | 2013-03-15 | 2015-10-07 | Respivert Ltd | Compuesto |
| UY35675A (es) | 2013-07-24 | 2015-02-27 | Novartis Ag | Derivados sustituidos de quinazolin-4-ona |
| CN104513235B (zh) * | 2013-09-02 | 2017-12-05 | 广东东阳光药业有限公司 | 取代的氨基嘧啶类化合物及其使用方法和用途 |
| KR20160060100A (ko) * | 2013-09-22 | 2016-05-27 | 칼리토르 사이언시즈, 엘엘씨 | 치환된 아미노피리미딘 화합물 및 이용 방법 |
| JP2017500319A (ja) | 2013-12-20 | 2017-01-05 | ギリアード カリストガ エルエルシー | (s)−2−(1−(9h−プリン−6−イルアミノ)プロピル)−5−フルオロ−3−フェニルキナゾリン−4(3h)−オンの塩酸塩の多形形態 |
| EP3083630B1 (en) | 2013-12-20 | 2019-08-21 | Gilead Calistoga LLC | Process methods for phosphatidylinositol 3-kinase inhibitors |
| SG11201606763VA (en) * | 2014-05-27 | 2016-09-29 | Almirall Sa | Medical use |
| AU2015265542B2 (en) | 2014-05-27 | 2019-05-09 | Rhizen Pharmaceuticals Sa | Improved forms of a PI3K delta selective inhibitor for use in pharmaceutical formulations |
| US11021467B2 (en) | 2014-06-13 | 2021-06-01 | Gilead Sciences, Inc. | Phosphatidylinositol 3-kinase inhibitors |
| EA201692557A1 (ru) | 2014-07-04 | 2017-05-31 | Люпин Лимитед | Хинолизиноновые производные в качестве ингибиторов pi3k |
| WO2017027883A1 (en) * | 2015-08-13 | 2017-02-16 | San Diego State University Research Foundation | Atropisomerism for increased kinase inhibitor selectivity |
| HUE063428T2 (hu) | 2016-01-11 | 2024-01-28 | Univ London Queen Mary | PI3K P-DELTA 110 gátlószerei rák kezelésében vírusok bejuttatására történõ alkalmazásra |
| JP6987798B2 (ja) | 2016-06-22 | 2022-01-05 | ザ ユナイテッド ステイツ オブ アメリカ, アズ リプレゼンテッド バイ ザ セクレタリー, デパートメント オブ ヘルス アンド ヒューマン サービシーズ | 癌の治療に変異体idh1阻害剤として有用なチアゾール誘導体 |
| US10016425B2 (en) | 2016-11-03 | 2018-07-10 | King Saud University | Anti-ulcerative colitis compound |
| CN112601746B (zh) * | 2018-08-21 | 2022-09-16 | 南京明德新药研发有限公司 | 吡唑并嘧啶衍生物及其作为pi3k抑制剂的应用 |
| WO2021207549A1 (en) | 2020-04-10 | 2021-10-14 | Gb005, Inc. | Kinase inhibitors |
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-
2010
- 2010-03-24 AU AU2010229968A patent/AU2010229968A1/en not_active Abandoned
- 2010-03-24 SG SG2011068822A patent/SG174529A1/en unknown
- 2010-03-24 KR KR1020117024913A patent/KR20120002995A/ko not_active Withdrawn
- 2010-03-24 US US12/731,089 patent/US8440677B2/en not_active Expired - Fee Related
- 2010-03-24 WO PCT/US2010/028554 patent/WO2010111432A1/en not_active Ceased
- 2010-03-24 AP AP2011005943A patent/AP2011005943A0/xx unknown
- 2010-03-24 CA CA2756347A patent/CA2756347A1/en not_active Abandoned
- 2010-03-24 BR BRPI1012333A patent/BRPI1012333A2/pt not_active IP Right Cessation
- 2010-03-24 PE PE2011001710A patent/PE20120602A1/es not_active Application Discontinuation
- 2010-03-24 EA EA201171160A patent/EA019499B1/ru not_active IP Right Cessation
- 2010-03-24 MX MX2011009955A patent/MX2011009955A/es active IP Right Grant
- 2010-03-24 NZ NZ595307A patent/NZ595307A/xx not_active IP Right Cessation
- 2010-03-24 CN CN2010800226099A patent/CN102439012A/zh active Pending
- 2010-03-24 JP JP2012502219A patent/JP2012521994A/ja active Pending
- 2010-03-24 EP EP10722454A patent/EP2411391A1/en not_active Withdrawn
-
2011
- 2011-09-20 IL IL215251A patent/IL215251A0/en unknown
- 2011-09-23 CL CL2011002359A patent/CL2011002359A1/es unknown
- 2011-10-20 CO CO11140750A patent/CO6450655A2/es not_active Application Discontinuation
- 2011-10-21 EC ECSP11011412 patent/ECSP11011412A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AP2011005943A0 (en) | 2011-10-31 |
| EP2411391A1 (en) | 2012-02-01 |
| EA201171160A1 (ru) | 2012-04-30 |
| CO6450655A2 (es) | 2012-05-31 |
| EA019499B1 (ru) | 2014-04-30 |
| PE20120602A1 (es) | 2012-05-21 |
| WO2010111432A1 (en) | 2010-09-30 |
| NZ595307A (en) | 2013-11-29 |
| CN102439012A (zh) | 2012-05-02 |
| IL215251A0 (en) | 2011-12-29 |
| MX2011009955A (es) | 2011-11-18 |
| US20100249155A1 (en) | 2010-09-30 |
| SG174529A1 (en) | 2011-10-28 |
| AU2010229968A1 (en) | 2011-10-13 |
| KR20120002995A (ko) | 2012-01-09 |
| CL2011002359A1 (es) | 2012-04-09 |
| BRPI1012333A2 (pt) | 2016-03-29 |
| US8440677B2 (en) | 2013-05-14 |
| CA2756347A1 (en) | 2010-09-30 |
| JP2012521994A (ja) | 2012-09-20 |
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