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)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Pulmonology (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Endocrinology (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Otolaryngology (AREA)
- Transplantation (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (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 |
| WO2005016348A1 (en) * | 2003-08-14 | 2005-02-24 | Icos Corporation | Method of inhibiting immune responses stimulated by an endogenous factor |
| WO2005113556A1 (en) | 2004-05-13 | 2005-12-01 | Icos Corporation | Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta |
| KR20160091440A (ko) | 2008-11-13 | 2016-08-02 | 길리아드 칼리스토가 엘엘씨 | 혈액 종양에 대한 요법 |
| US9492449B2 (en) | 2008-11-13 | 2016-11-15 | Gilead Calistoga Llc | Therapies for hematologic malignancies |
| BRPI1012333A2 (pt) | 2009-03-24 | 2016-03-29 | Gilead Calistoga Llc | atropisômeros de derivados de 2-purinil-3-tolil-quinazolinonas e métodos de uso |
| AP2011005956A0 (en) * | 2009-04-20 | 2011-10-31 | Gilead Calistoga Llc | Methods of treatment for solid tumors. |
| AU2010254149B2 (en) * | 2009-05-29 | 2014-08-21 | Merck Sharp & Dohme Llc | Radiolabeled PDE10 inhibitors |
| 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 |
| EP2790705B1 (en) | 2011-12-15 | 2017-12-06 | Novartis AG | Use of inhibitors of the activity or function of pi3k |
| NZ629684A (en) | 2012-03-05 | 2016-10-28 | Gilead Calistoga Llc | Polymorphic forms of (s)-2-(1-(9h-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3h)-one |
| UA115544C2 (uk) | 2012-03-13 | 2017-11-27 | Респіверт Лімітед | Спосіб підвищення стабільності до хімічного розкладання фармацевтичної композиції та застосування стабілізуючого агента у фармацевтичній коипозиції |
| RS56494B1 (sr) | 2012-07-04 | 2018-01-31 | Rhizen Pharmaceuticals S A | Selektivni inhibitori pi3k delta |
| 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 |
| HK1211027A1 (en) * | 2012-10-16 | 2016-05-13 | Almirall, S.A. | Pyrrolotriazinone derivatives as pi3k inhibitors |
| WO2014072937A1 (en) * | 2012-11-08 | 2014-05-15 | Rhizen Pharmaceuticals Sa | Pharmaceutical compositions containing a pde4 inhibitor and a pi3 delta or dual pi3 delta-gamma kinase inhibitor |
| US9227977B2 (en) | 2013-03-15 | 2016-01-05 | Respivert Ltd. | Phosphoinositide 3-kinase inhibitors |
| TW201522341A (zh) | 2013-03-15 | 2015-06-16 | Respivert Ltd | 化合物 |
| 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 |
| WO2015095605A1 (en) | 2013-12-20 | 2015-06-25 | Gilead Calistoga Llc | Polymorphic forms of a hydrochloride salt of (s) -2-(9h-purin-6-ylamino) propyl) -5-fluoro-3-phenylquinazolin-4 (3h) -one |
| NZ736970A (en) | 2013-12-20 | 2018-11-30 | Gilead Calistoga Llc | Process methods for phosphatidylinositol 3-kinase inhibitors |
| CN106414449A (zh) * | 2014-05-27 | 2017-02-15 | 阿尔米雷尔有限公司 | 医药用途 |
| AU2015265542B2 (en) | 2014-05-27 | 2019-05-09 | Rhizen Pharmaceuticals Sa | Improved forms of a PI3K delta selective inhibitor for use in pharmaceutical formulations |
| MA40059A (fr) | 2014-06-13 | 2015-12-17 | Gilead Sciences Inc | Inhibiteurs de la phosphatidylinositol 3-kinase |
| HK1232227A1 (zh) | 2014-07-04 | 2018-01-05 | Lupin Limited | 作为pi3k抑制剂的喹嗪酮衍生物 |
| 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 |
| ES2880347T3 (es) | 2016-06-22 | 2021-11-24 | Us Health | Derivados de tiazol útiles como inhibidores de IDH1 mutante para el tratamiento del cáncer |
| US10016425B2 (en) | 2016-11-03 | 2018-07-10 | King Saud University | Anti-ulcerative colitis compound |
| JP2021535907A (ja) * | 2018-08-21 | 2021-12-23 | 南京明徳新薬研発有限公司 | ピラゾロピリミジン誘導体及びそのpi3k抑制剤とする適用 |
| BR112022020342A2 (pt) | 2020-04-10 | 2022-12-13 | Gb005 Inc | Inibidores da quinase |
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2010
- 2010-03-24 BR BRPI1012333A patent/BRPI1012333A2/pt not_active IP Right Cessation
- 2010-03-24 NZ NZ595307A patent/NZ595307A/xx not_active IP Right Cessation
- 2010-03-24 US US12/731,089 patent/US8440677B2/en not_active Expired - Fee Related
- 2010-03-24 JP JP2012502219A patent/JP2012521994A/ja active Pending
- 2010-03-24 MX MX2011009955A patent/MX2011009955A/es active IP Right Grant
- 2010-03-24 WO PCT/US2010/028554 patent/WO2010111432A1/en not_active Ceased
- 2010-03-24 EP EP10722454A patent/EP2411391A1/en not_active Withdrawn
- 2010-03-24 PE PE2011001710A patent/PE20120602A1/es not_active Application Discontinuation
- 2010-03-24 SG SG2011068822A patent/SG174529A1/en unknown
- 2010-03-24 CN CN2010800226099A patent/CN102439012A/zh active Pending
- 2010-03-24 AU AU2010229968A patent/AU2010229968A1/en not_active Abandoned
- 2010-03-24 KR KR1020117024913A patent/KR20120002995A/ko not_active Withdrawn
- 2010-03-24 EA EA201171160A patent/EA019499B1/ru not_active IP Right Cessation
- 2010-03-24 CA CA2756347A patent/CA2756347A1/en not_active Abandoned
- 2010-03-24 AP AP2011005943A patent/AP2011005943A0/xx unknown
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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 |
|---|---|
| IL215251A0 (en) | 2011-12-29 |
| AP2011005943A0 (en) | 2011-10-31 |
| PE20120602A1 (es) | 2012-05-21 |
| NZ595307A (en) | 2013-11-29 |
| CO6450655A2 (es) | 2012-05-31 |
| EA019499B1 (ru) | 2014-04-30 |
| CL2011002359A1 (es) | 2012-04-09 |
| CA2756347A1 (en) | 2010-09-30 |
| US8440677B2 (en) | 2013-05-14 |
| EP2411391A1 (en) | 2012-02-01 |
| US20100249155A1 (en) | 2010-09-30 |
| BRPI1012333A2 (pt) | 2016-03-29 |
| KR20120002995A (ko) | 2012-01-09 |
| EA201171160A1 (ru) | 2012-04-30 |
| WO2010111432A1 (en) | 2010-09-30 |
| CN102439012A (zh) | 2012-05-02 |
| SG174529A1 (en) | 2011-10-28 |
| JP2012521994A (ja) | 2012-09-20 |
| AU2010229968A1 (en) | 2011-10-13 |
| MX2011009955A (es) | 2011-11-18 |
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