PE20120602A1 - ATROPISOMEROS DE 2-[(6-AMINO-9H-PURIN-9-IL)METIL]-5-METIL-3-o-TOLILQUINAZOLIN-4(3H)-ONA - Google Patents
ATROPISOMEROS DE 2-[(6-AMINO-9H-PURIN-9-IL)METIL]-5-METIL-3-o-TOLILQUINAZOLIN-4(3H)-ONAInfo
- Publication number
- PE20120602A1 PE20120602A1 PE2011001710A PE2011001710A PE20120602A1 PE 20120602 A1 PE20120602 A1 PE 20120602A1 PE 2011001710 A PE2011001710 A PE 2011001710A PE 2011001710 A PE2011001710 A PE 2011001710A PE 20120602 A1 PE20120602 A1 PE 20120602A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- purin
- amino
- atropisomer
- tolilquinazolin
- Prior art date
Links
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 title abstract 2
- LGIBDQRYOFBMTC-UHFFFAOYSA-N dnc010031 Chemical compound C1=CC(O)=CC=C1C1C(=O)NC2=CC=CC=C2C2=C3C1=CNC3=NC=C2 LGIBDQRYOFBMTC-UHFFFAOYSA-N 0.000 abstract 2
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 102000038030 PI3Ks Human genes 0.000 abstract 1
- 108091007960 PI3Ks Proteins 0.000 abstract 1
- 108091000080 Phosphotransferase Proteins 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 229940125782 compound 2 Drugs 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 150000003916 phosphatidylinositol 3,4,5-trisphosphates Chemical class 0.000 abstract 1
- 102000020233 phosphotransferase Human genes 0.000 abstract 1
- 238000000926 separation method Methods 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)
- Pulmonology (AREA)
- Immunology (AREA)
- Diabetes (AREA)
- Dermatology (AREA)
- Hematology (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Transplantation (AREA)
- Otolaryngology (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
SE REFIERE A UN ATROPISOMERO OPTICAMENTE ACTIVO DEL COMPUESTO 2-((6-AMINO-9H-PURIN-9-IL)METIL)-5-METIL-3-O-TOLILQUINAZOLIN-4(3H)-ONA QUE SE OBTIENE POR SEPARACION DE UNA MEZCLA RACEMICA, EL CUAL COMPRENDE EL ATROPISOMERO 1(R) Y EL ATROPISOMERO 1(S). TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHO COMPUESTO INHIBE LAS ISOFORMAS DE LA FOSFATIDILINOSITOL-3,4,5-TRIFOSFATO QUINASA ? (PI3K?) SIENDO UTIL EN EL TRATAMIENTO DE ENFERMEDADES INFLAMATORIAS Y CANCER
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 |
|---|---|
| PE20120602A1 true PE20120602A1 (es) | 2012-05-21 |
Family
ID=42289320
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2011001710A PE20120602A1 (es) | 2009-03-24 | 2010-03-24 | ATROPISOMEROS DE 2-[(6-AMINO-9H-PURIN-9-IL)METIL]-5-METIL-3-o-TOLILQUINAZOLIN-4(3H)-ONA |
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 |
| RS55551B1 (sr) | 2004-05-13 | 2017-05-31 | Icos Corp | Hinazolinoni kao inhibitori humane fosfatidilinozitol 3-kinaze delta |
| US9492449B2 (en) | 2008-11-13 | 2016-11-15 | Gilead Calistoga Llc | Therapies for hematologic malignancies |
| KR101664511B1 (ko) | 2008-11-13 | 2016-10-11 | 길리아드 칼리스토가 엘엘씨 | 혈액 종양에 대한 요법 |
| BRPI1012333A2 (pt) | 2009-03-24 | 2016-03-29 | Gilead Calistoga Llc | atropisômeros de derivados de 2-purinil-3-tolil-quinazolinonas e métodos de uso |
| 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 |
| WO2010138577A1 (en) * | 2009-05-29 | 2010-12-02 | Merck Sharp & Dohme Corp. | Radiolabeled pde10 inhibitors |
| CN102647987A (zh) * | 2009-07-21 | 2012-08-22 | 吉里德卡利斯托加公司 | 使用pi3k抑制剂治疗肝脏障碍 |
| 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 |
| US9949979B2 (en) | 2011-12-15 | 2018-04-24 | Novartis Ag | Use of inhibitors of the activity or function of PI3K |
| PT2834241T (pt) | 2012-03-05 | 2021-02-05 | Gilead Calistoga Llc | Formas polimórficas de (s)-2-(1-(9h-purin-6-ilamino)propil)-5-fluoro-3-fenil quinazolina-4(3h)-ona |
| TWI617561B (zh) | 2012-03-13 | 2018-03-11 | 瑞斯比維特有限公司 | 呈晶體型式之新穎化合物,包含其之醫藥組成物,製備該化合物之方法及包括該組成物之吸入裝置 |
| AU2013285081B2 (en) | 2012-07-04 | 2017-01-12 | Rhizen Pharmaceuticals Sa | Selective PI3K delta inhibitors |
| 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 |
| CN111904962A (zh) | 2012-11-08 | 2020-11-10 | 理森制药股份公司 | 含有PDE4抑制剂和PI3 δ或双重PI3 δ-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 |
| CN104418849B (zh) * | 2013-09-02 | 2020-04-21 | 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 |
| RU2683793C2 (ru) | 2013-09-22 | 2019-04-02 | Калитор Сайенсез, ЛЛС | Замещенные аминопиримидиновые соединения и способы их использования |
| US9567337B2 (en) | 2013-12-20 | 2017-02-14 | Gilead Calistoga Llc | Process methods for phosphatidylinositol 3-kinase inhibitors |
| US9708327B2 (en) | 2013-12-20 | 2017-07-18 | Gilead Calistoga Llc | Polymorphic forms of a hydrochloride salt of (S)-2-(1-(9H-purin-6-ylamino)propyl)-5-fluoro-3-phenylquinazolin-4(3H)-one |
| BR112016027674A2 (pt) | 2014-05-27 | 2017-08-15 | Rhizen Pharmaceuticals Sa | Formas melhoradas de um inibidor seletivo de pi3k delta para uso em formulações farmacêuticas |
| BR112016024538A2 (pt) * | 2014-05-27 | 2017-08-15 | Almirall Sa | sais de adição de (s)-2-(1-(6-amino-5-cianopirimidin-4-ilamino)etil)-4-oxo-3-fenil-3,4-di-hidro¬pirrolo[1,2-f][1,2,4]triazina-5-carbonitrila |
| HK1231476A1 (zh) | 2014-06-13 | 2017-12-22 | 吉利德科学公司 | 磷脂酰肌醇3-激酶抑制剂 |
| CU24428B1 (es) | 2014-07-04 | 2019-06-04 | Lupin Ltd | Derivados de quinolizinona como inhibidores de pi3k |
| EP3334430B1 (en) * | 2015-08-13 | 2025-02-26 | San Diego State University Research Foundation | Atropisomerism for increased kinase inhibitor selectivity |
| ES2959563T3 (es) | 2016-01-11 | 2024-02-27 | Univ London Queen Mary | Inhibidores de pi3k p-delta 110 para su uso en la administración de virus en el tratamiento del cáncer |
| EP3475276B1 (en) | 2016-06-22 | 2021-03-31 | The United States of America, as represented by the Secretary, Department of Health and Human Services | Thiazole derivatives useful as mutant idh1 inhibitors for treating cancer |
| US10016425B2 (en) | 2016-11-03 | 2018-07-10 | King Saud University | Anti-ulcerative colitis compound |
| EP3828184A4 (en) * | 2018-08-21 | 2022-05-04 | Medshine Discovery Inc. | PYRAZOLOPYRIMIDI DERIVATIVES AND USE THEREOF AS A PI3K INHIBITOR |
| EP4132910A1 (en) | 2020-04-10 | 2023-02-15 | GB002, Inc. | Kinase inhibitors |
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-
2010
- 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 CA CA2756347A patent/CA2756347A1/en not_active Abandoned
- 2010-03-24 JP JP2012502219A patent/JP2012521994A/ja active Pending
- 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 SG SG2011068822A patent/SG174529A1/en unknown
- 2010-03-24 AU AU2010229968A patent/AU2010229968A1/en not_active Abandoned
- 2010-03-24 MX MX2011009955A patent/MX2011009955A/es active IP Right Grant
- 2010-03-24 KR KR1020117024913A patent/KR20120002995A/ko not_active Withdrawn
- 2010-03-24 AP AP2011005943A patent/AP2011005943A0/xx unknown
- 2010-03-24 CN CN2010800226099A patent/CN102439012A/zh active Pending
- 2010-03-24 EP EP10722454A patent/EP2411391A1/en not_active Withdrawn
- 2010-03-24 EA EA201171160A patent/EA019499B1/ru not_active IP Right Cessation
- 2010-03-24 NZ NZ595307A patent/NZ595307A/xx not_active IP Right Cessation
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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 |
|---|---|
| EA019499B1 (ru) | 2014-04-30 |
| SG174529A1 (en) | 2011-10-28 |
| IL215251A0 (en) | 2011-12-29 |
| EA201171160A1 (ru) | 2012-04-30 |
| US20100249155A1 (en) | 2010-09-30 |
| AU2010229968A1 (en) | 2011-10-13 |
| US8440677B2 (en) | 2013-05-14 |
| JP2012521994A (ja) | 2012-09-20 |
| MX2011009955A (es) | 2011-11-18 |
| EP2411391A1 (en) | 2012-02-01 |
| AP2011005943A0 (en) | 2011-10-31 |
| NZ595307A (en) | 2013-11-29 |
| BRPI1012333A2 (pt) | 2016-03-29 |
| ECSP11011412A (es) | 2012-03-30 |
| CO6450655A2 (es) | 2012-05-31 |
| CN102439012A (zh) | 2012-05-02 |
| CA2756347A1 (en) | 2010-09-30 |
| WO2010111432A1 (en) | 2010-09-30 |
| KR20120002995A (ko) | 2012-01-09 |
| CL2011002359A1 (es) | 2012-04-09 |
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