CA2756347A1 - Atropisomers of 2-purinyl-3-tolyl-quinazolinone derivatives and methods of use - Google Patents

Atropisomers of 2-purinyl-3-tolyl-quinazolinone derivatives and methods of use Download PDF

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Publication number
CA2756347A1
CA2756347A1 CA2756347A CA2756347A CA2756347A1 CA 2756347 A1 CA2756347 A1 CA 2756347A1 CA 2756347 A CA2756347 A CA 2756347A CA 2756347 A CA2756347 A CA 2756347A CA 2756347 A1 CA2756347 A1 CA 2756347A1
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CA
Canada
Prior art keywords
compound
atropisomer
formula
optically active
pharmaceutically acceptable
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Abandoned
Application number
CA2756347A
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English (en)
French (fr)
Inventor
Jerry B. Evarts
Roger G. Ulrich
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Calistoga LLC
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Gilead Calistoga LLC
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Filing date
Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42289320&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2756347(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Calistoga LLC filed Critical Gilead Calistoga LLC
Publication of CA2756347A1 publication Critical patent/CA2756347A1/en
Abandoned legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32Nitrogen atom
    • C07D473/34Nitrogen atom attached in position 6, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/52Purines, e.g. adenine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Endocrinology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Neurology (AREA)
  • Obesity (AREA)
  • Transplantation (AREA)
  • Oncology (AREA)
  • Emergency Medicine (AREA)
  • Otolaryngology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
CA2756347A 2009-03-24 2010-03-24 Atropisomers of 2-purinyl-3-tolyl-quinazolinone derivatives and methods of use Abandoned CA2756347A1 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US16298009P 2009-03-24 2009-03-24
US61/162,980 2009-03-24
US23155009P 2009-08-05 2009-08-05
US61/231,550 2009-08-05
PCT/US2010/028554 WO2010111432A1 (en) 2009-03-24 2010-03-24 Atropisomers of2-purinyl-3-tolyl-quinazolinone derivatives and methods of use

Publications (1)

Publication Number Publication Date
CA2756347A1 true CA2756347A1 (en) 2010-09-30

Family

ID=42289320

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2756347A Abandoned CA2756347A1 (en) 2009-03-24 2010-03-24 Atropisomers of 2-purinyl-3-tolyl-quinazolinone derivatives and methods of use

Country Status (19)

Country Link
US (1) US8440677B2 (enExample)
EP (1) EP2411391A1 (enExample)
JP (1) JP2012521994A (enExample)
KR (1) KR20120002995A (enExample)
CN (1) CN102439012A (enExample)
AP (1) AP2011005943A0 (enExample)
AU (1) AU2010229968A1 (enExample)
BR (1) BRPI1012333A2 (enExample)
CA (1) CA2756347A1 (enExample)
CL (1) CL2011002359A1 (enExample)
CO (1) CO6450655A2 (enExample)
EA (1) EA019499B1 (enExample)
EC (1) ECSP11011412A (enExample)
IL (1) IL215251A0 (enExample)
MX (1) MX2011009955A (enExample)
NZ (1) NZ595307A (enExample)
PE (1) PE20120602A1 (enExample)
SG (1) SG174529A1 (enExample)
WO (1) WO2010111432A1 (enExample)

Families Citing this family (38)

* Cited by examiner, † Cited by third party
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
EP1761540B1 (en) 2004-05-13 2016-09-28 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
US9492449B2 (en) 2008-11-13 2016-11-15 Gilead Calistoga Llc Therapies for hematologic malignancies
EP2355828B1 (en) 2008-11-13 2018-05-30 Gilead Calistoga LLC Therapies for hematologic malignancies
JP2012521994A (ja) 2009-03-24 2012-09-20 ギリアード カリストガ エルエルシー 2−プリニル−3−トリル−キナゾリノン誘導体のアトロプ異性体および使用方法
CN102458410A (zh) * 2009-04-20 2012-05-16 吉联亚·卡利斯托加有限责任公司 治疗实体瘤的方法
AU2010254149B2 (en) * 2009-05-29 2014-08-21 Merck Sharp & Dohme Llc Radiolabeled PDE10 inhibitors
EA201270184A1 (ru) * 2009-07-21 2012-08-30 ГИЛИЭД КАЛИСТОГА ЭлЭлСи Лечение расстройств печени ингибиторами pi3k
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
AR090253A1 (es) 2012-03-05 2014-10-29 Gilead Calistoga Llc Formas polimorficas de (s)-2-(1-(9h-purin-6-ilamino)propil)-5-fluor-3-fenilquinazolin-4(3h)-ona
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
KR101988079B1 (ko) * 2012-07-04 2019-06-11 리젠 파마슈티컬스 소시에떼 아노님 선택적 pi3k 델타 억제제
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
EA027277B1 (ru) 2012-10-16 2017-07-31 Альмираль, С.А. Производные пирроллотриазинона в качестве ингибиторов pi3k
CA2889905A1 (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
TW201522341A (zh) * 2013-03-15 2015-06-16 Respivert Ltd 化合物
US9227977B2 (en) 2013-03-15 2016-01-05 Respivert Ltd. Phosphoinositide 3-kinase inhibitors
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
SG11201600707QA (en) 2013-09-22 2016-02-26 Calitor Sciences Llc Substituted aminopyrimidine compounds and methods of use
CA2934534A1 (en) 2013-12-20 2015-06-25 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
JP2017502021A (ja) 2013-12-20 2017-01-19 ギリアード カリストガ エルエルシー ホスファチジルイノシトール3−キナーゼ阻害剤のためのプロセス方法
MX2016014861A (es) * 2014-05-27 2017-04-06 Almirall Sa Uso medico.
CN111635406A (zh) 2014-05-27 2020-09-08 理森制药股份公司 用于药物制剂中的PI3Kδ选择性抑制剂的改良形式
SG11201609877XA (en) 2014-06-13 2016-12-29 Gilead Sciences Inc Phosphatidylinositol 3-kinase inhibitors
JP6291601B2 (ja) 2014-07-04 2018-03-14 ルピン・リミテッド Pi3k阻害剤としてのキノリジノン誘導体
WO2017027883A1 (en) 2015-08-13 2017-02-16 San Diego State University Research Foundation Atropisomerism for increased kinase inhibitor selectivity
SMT202300244T1 (it) 2016-01-11 2023-09-06 Univ London Queen Mary Inibitori di pi3k p-delta 110 per uso nell’erogazione di virus nel trattamento di cancro
WO2017223202A1 (en) 2016-06-22 2017-12-28 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
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
WO2021207549A1 (en) 2020-04-10 2021-10-14 Gb005, Inc. Kinase inhibitors

Family Cites Families (98)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1249281B (enExample) 1963-05-18
US3691016A (en) 1970-04-17 1972-09-12 Monsanto Co Process for the preparation of insoluble enzymes
DE2027645A1 (de) 1970-06-05 1971-12-09 Byk Gulden Lomberg Chemische Fa bnk GmbH, 7750 Konstanz Piperazinylalkyl chinazolon (4) den vate, Verfahren zu deren Herstellung und sie enthaltende Arzneimittel
NL7204972A (enExample) 1971-04-21 1972-10-24
US3897432A (en) 1971-04-21 1975-07-29 Merck & Co Inc Substituted benzimidazole derivatives
CA1023287A (en) 1972-12-08 1977-12-27 Boehringer Mannheim G.M.B.H. Process for the preparation of carrier-bound proteins
US4179337A (en) 1973-07-20 1979-12-18 Davis Frank F Non-immunogenic polypeptides
US4195128A (en) 1976-05-03 1980-03-25 Bayer Aktiengesellschaft Polymeric carrier bound ligands
DE2644265C2 (de) 1976-09-30 1983-02-10 Bayer Ag, 5090 Leverkusen Chinazoline
US4330440A (en) 1977-02-08 1982-05-18 Development Finance Corporation Of New Zealand Activated matrix and method of activation
CA1093991A (en) 1977-02-17 1981-01-20 Hideo Hirohara Enzyme immobilization with pullulan gel
US4183931A (en) 1977-09-08 1980-01-15 Research Corporation 2-Ketoalkyl-4(3H)-quinazolinones
US4229537A (en) 1978-02-09 1980-10-21 New York University Preparation of trichloro-s-triazine activated supports for coupling ligands
DE2812635A1 (de) 1978-03-22 1979-09-27 Bayer Ag Heterocyclische verbindungen
JPS55118917A (en) 1979-03-06 1980-09-12 Mitsubishi Electric Corp Production of quinazolone ring-containing epoxy resin
JPS55118918A (en) 1979-03-06 1980-09-12 Mitsubishi Electric Corp Production of quinazolone ring-containing epoxy resin
US4289872A (en) 1979-04-06 1981-09-15 Allied Corporation Macromolecular highly branched homogeneous compound based on lysine units
JPS6017375B2 (ja) 1979-06-20 1985-05-02 三菱電機株式会社 ポリアミド樹脂の製造方法
JPS6023084B2 (ja) 1979-07-11 1985-06-05 味の素株式会社 代用血液
US4640835A (en) 1981-10-30 1987-02-03 Nippon Chemiphar Company, Ltd. Plasminogen activator derivatives
US4496689A (en) 1983-12-27 1985-01-29 Miles Laboratories, Inc. Covalently attached complex of alpha-1-proteinase inhibitor with a water soluble polymer
EP0206448B1 (en) 1985-06-19 1990-11-14 Ajinomoto Co., Inc. Hemoglobin combined with a poly(alkylene oxide)
US4791192A (en) 1986-06-26 1988-12-13 Takeda Chemical Industries, Ltd. Chemically modified protein with polyethyleneglycol
USRE35862E (en) 1986-08-18 1998-07-28 Emisphere Technologies, Inc. Delivery systems for pharmacological agents encapsulated with proteinoids
JP2876058B2 (ja) 1986-08-18 1999-03-31 エミスフィア・テクノロジーズ・インコーポレイテッド 薬物送達システム
US6696250B1 (en) 1986-12-03 2004-02-24 Competitive Technologies, Inc. RNA ribozyme polymerases, dephosphorylases, restriction endoribonucleases and methods
US5229490A (en) 1987-05-06 1993-07-20 The Rockefeller University Multiple antigen peptide system
EP0364598A4 (en) 1988-03-02 1992-01-15 Yoshitomi Pharmaceutical Industries, Ltd. 3,4-dihydrothieno 2,3-d¨pyrimidine compounds and pharmaceutical application thereof
US5225347A (en) 1989-09-25 1993-07-06 Innovir Laboratories, Inc. Therapeutic ribozyme compositions and expression vectors
US5013556A (en) 1989-10-20 1991-05-07 Liposome Technology, Inc. Liposomes with enhanced circulation time
FR2675803B1 (fr) 1991-04-25 1996-09-06 Genset Sa Oligonucleotides fermes, antisens et sens et leurs applications.
DK0525960T3 (da) 1991-06-18 1996-04-15 American Home Prod Anvendelse af rapamycin til behandling af T-celle leukæmi/lymfon
WO1993021259A1 (en) 1992-04-14 1993-10-28 Cornell Research Foundation Inc. Dendritic based macromolecules and method of production
US5658780A (en) 1992-12-07 1997-08-19 Ribozyme Pharmaceuticals, Inc. Rel a targeted ribozymes
GB9301000D0 (en) 1993-01-20 1993-03-10 Glaxo Group Ltd Chemical compounds
US5378725A (en) 1993-07-19 1995-01-03 The Arizona Board Of Regents Inhibition of phosphatidylinositol 3-kinase with wortmannin and analogs thereof
GB9404485D0 (en) 1994-03-09 1994-04-20 Cancer Res Campaign Tech Benzamide analogues
FI951367A7 (fi) 1994-03-28 1995-09-29 Japan Energy Corp Puriinijohdannaiset ja tulehdustautien tukahduttajat (suppressantit)
US5480906A (en) 1994-07-01 1996-01-02 Eli Lilly And Company Stereochemical Wortmannin derivatives
EP0771204A4 (en) 1994-08-12 1999-10-20 Pro Neuron Inc METHOD FOR TREATING SEPSIS OR FLAMMABLE DISEASES WITH OXYPURINE NUCLEOSIDES
US5561138A (en) 1994-12-13 1996-10-01 American Home Products Corporation Method of treating anemia
JP3233802B2 (ja) 1994-12-15 2001-12-04 関西電力株式会社 燃焼排ガス中の炭酸ガスと窒素酸化物を除去する方法
US6043062A (en) 1995-02-17 2000-03-28 The Regents Of The University Of California Constitutively active phosphatidylinositol 3-kinase and uses thereof
US6096871A (en) 1995-04-14 2000-08-01 Genentech, Inc. Polypeptides altered to contain an epitope from the Fc region of an IgG molecule for increased half-life
US5948664A (en) 1996-02-29 1999-09-07 The Regents Of The University Of California PI 3-kinase polypeptides
JP4046354B2 (ja) 1996-03-18 2008-02-13 ボード オブ リージェンツ,ザ ユニバーシティ オブ テキサス システム 増大した半減期を有する免疫グロブリン様ドメイン
CA2252907C (en) 1996-05-15 2005-05-17 Pfizer Inc. Novel 2,3 disubstituted-4(3h)-quinazolinones
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
CN1190434C (zh) 1996-12-31 2005-02-23 雷迪实验室有限公司 新的杂环化合物、其制备方法和含有它们的药物组合物及其在治疗糖尿病和相关疾病中的应用
GB9702701D0 (en) 1997-02-01 1997-04-02 Univ Newcastle Ventures Ltd Quinazolinone compounds
HUP0000935A3 (en) 1997-02-28 2002-04-29 Pfizer Prod Inc Atropisomers of 3-heteroaryl-4(3h)-quinazolinones and their use for the treatment of neurodegenerative and cns-trauma related conditions
NZ336628A (en) 1997-02-28 2001-03-30 Pfizer Prod Inc Atropisomers of 3-aryl-4(3H)-quinazolinones and their use as AMPA-receptor antagonists
ES2245015T3 (es) 1997-06-09 2005-12-16 Pfizer Products Inc. Quinazolin-4-onas como antagonistas de ampa.
AU8280798A (en) 1997-07-03 1999-01-25 Thomas Jefferson University An improved method for design and selection of efficacious antisense oligonucleotides
IL125950A0 (en) 1997-09-05 1999-04-11 Pfizer Prod Inc Methods of administering ampa receptor antagonists to treat dyskinesias associated with dopamine agonist therapy
CA2317093A1 (en) 1998-01-08 1999-07-15 Joel M. Linden A2a adenosine receptor agonists
AU1120599A (en) 1998-04-23 1999-03-08 Dr. Reddy's Research Foundation New heterocyclic compounds and their use in medicine, process for their reparation and pharmaceutical compositions containing them
US6048970A (en) 1998-05-22 2000-04-11 Incyte Pharmaceuticals, Inc. Prostate growth-associated membrane proteins
US6100090A (en) 1999-06-25 2000-08-08 Isis Pharmaceuticals Inc. Antisense inhibition of PI3K p85 expression
US6046049A (en) 1999-07-19 2000-04-04 Isis Pharmaceuticals Inc. Antisense modulation of PI3 kinase p110 delta expression
EP1939203B1 (en) 2000-04-25 2014-11-19 ICOS Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta isoform
RS51458B (sr) * 2000-04-25 2011-04-30 Icos Corporation Inhibitori humane fosfatidil-inozitol 3-kinaze delta
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
HRP20041207A2 (en) 2002-07-10 2005-04-30 Applied Research Systems Ars Holding N.V. Azolidinone-vinyl fused-benzene derivatives
US20040092561A1 (en) 2002-11-07 2004-05-13 Thomas Ruckle Azolidinone-vinyl fused -benzene derivatives
GB0217777D0 (en) 2002-07-31 2002-09-11 Novartis Ag Organic compounds
US20040023390A1 (en) 2002-08-05 2004-02-05 Davidson Beverly L. SiRNA-mediated gene silencing with viral vectors
CA2400254A1 (en) 2002-09-19 2004-03-19 University Health Network Compositions and methods for treating heart disease
KR101059652B1 (ko) 2002-09-30 2011-08-25 바이엘 파마 악티엔게젤샤프트 접합 아졸-피리미딘 유도체
WO2004052373A1 (en) 2002-12-06 2004-06-24 Warner-Lambert Company Llc Benzoxazin-3-ones and derivatives thereof as inhibitors of pi3k
EP1581529A1 (en) 2002-12-20 2005-10-05 Warner-Lambert Company Benzoxazines and derivatives thereof as inhibitors of pi3ks
EP1611119A1 (en) 2003-04-03 2006-01-04 Semafore Pharmaceuticals, Inc. Pi-3 kinase inhibitor prodrugs
CA2527573A1 (en) 2003-06-05 2004-12-16 Warner-Lambert Company Llc Cycloalkyl and heterocycloalkyl substituted benzothiophenes as therapeutic agents
EP1644360A1 (en) 2003-06-05 2006-04-12 Warner-Lambert Company LLC 3-substituted indoles and derivatives thereof as therapeutic agents
WO2004108716A1 (en) 2003-06-05 2004-12-16 Warner-Lambert Company Llc 3-arylsulfanyl and 3-heteroarylsulfanyl substituted benzo[b]thiophenes as therapeutic agents
MXPA05012894A (es) 2003-06-05 2006-02-22 Warner Lambert Co Benzofuranos 3-sustituidos como agentes terapeuticos.
ATE365735T1 (de) 2003-06-05 2007-07-15 Warner Lambert Co Cycloalkylsulfanyl-substituierte benzo böthiophene als therapeutische mittel
US20040259926A1 (en) 2003-06-05 2004-12-23 Bruendl Michelle M. 3-Aryloxy and 3-heteroaryloxy substituted benzo[b]thiophenes as therapeutic agents
WO2005016349A1 (en) 2003-08-14 2005-02-24 Icos Corporation Methods of inhibiting leukocyte accumulation
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
CA2552664A1 (en) 2004-01-08 2005-07-28 Michigan State University Methods for treating and preventing hypertension and hypertension-related disorders
WO2005112935A1 (en) 2004-05-13 2005-12-01 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
EP1761540B1 (en) 2004-05-13 2016-09-28 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
EP1755609A1 (en) 2004-05-25 2007-02-28 Icos Corporation Methods for treating and/or preventing aberrant proliferation of hematopoietic cells
JP2008501707A (ja) * 2004-06-04 2008-01-24 アイコス、コーポレーション マスト細胞障害を処置するための方法
WO2006089106A2 (en) 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
US20090170834A1 (en) 2005-12-22 2009-07-02 Prolexys Pharmaceuticals, Inc. Fused Pyrimidones and Thiopyrimidones, and Uses Thereof
EP2097422A4 (en) 2006-11-13 2010-04-14 Lilly Co Eli THIENOPYRIMIDINONE FOR THE TREATMENT OF INFLAMMATORY DISEASES AND CARCINOMAS
US20110160232A1 (en) 2007-10-04 2011-06-30 Pingda Ren Certain chemical entities and therapeutic uses thereof
US20090131512A1 (en) 2007-10-31 2009-05-21 Dynavax Technologies Corp. Inhibition of type I in IFN production
SG187426A1 (en) 2008-01-04 2013-02-28 Intellikine Llc Certain chemical entities, compositions and methods
EP2355828B1 (en) 2008-11-13 2018-05-30 Gilead Calistoga LLC Therapies for hematologic malignancies
AU2009322187B2 (en) 2008-12-04 2015-02-19 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Phosphatidylinositol-3-kinase p110 delta-targeted drugs in the treatment of CNS disorders
JP2012521994A (ja) 2009-03-24 2012-09-20 ギリアード カリストガ エルエルシー 2−プリニル−3−トリル−キナゾリノン誘導体のアトロプ異性体および使用方法
CN102458410A (zh) 2009-04-20 2012-05-16 吉联亚·卡利斯托加有限责任公司 治疗实体瘤的方法
EA201270184A1 (ru) * 2009-07-21 2012-08-30 ГИЛИЭД КАЛИСТОГА ЭлЭлСи Лечение расстройств печени ингибиторами pi3k
CA3113343C (en) 2010-06-03 2024-10-08 Pharmacyclics Llc USE OF BRUTON'S TYROSINE KINASE INHIBITORS IN THE TREATMENT OF FOLLICULAR LYMPHOMA

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