JP2012521994A - 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 - Google Patents

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 Download PDF

Info

Publication number
JP2012521994A
JP2012521994A JP2012502219A JP2012502219A JP2012521994A JP 2012521994 A JP2012521994 A JP 2012521994A JP 2012502219 A JP2012502219 A JP 2012502219A JP 2012502219 A JP2012502219 A JP 2012502219A JP 2012521994 A JP2012521994 A JP 2012521994A
Authority
JP
Japan
Prior art keywords
compound
formula
atropisomer
optically active
atropisomers
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.)
Pending
Application number
JP2012502219A
Other languages
English (en)
Japanese (ja)
Other versions
JP2012521994A5 (enExample
Inventor
ジェリー ビー. エバーツ,
ロジャー ジー. ウルリッヒ,
Original Assignee
ギリアード カリストガ エルエルシー
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
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=JP2012521994(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by ギリアード カリストガ エルエルシー filed Critical ギリアード カリストガ エルエルシー
Publication of JP2012521994A publication Critical patent/JP2012521994A/ja
Publication of JP2012521994A5 publication Critical patent/JP2012521994A5/ja
Pending legal-status Critical Current

Links

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

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)
JP2012502219A 2009-03-24 2010-03-24 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 Pending JP2012521994A (ja)

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 (2)

Publication Number Publication Date
JP2012521994A true JP2012521994A (ja) 2012-09-20
JP2012521994A5 JP2012521994A5 (enExample) 2013-05-09

Family

ID=42289320

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012502219A Pending JP2012521994A (ja) 2009-03-24 2010-03-24 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

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)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012528176A (ja) * 2009-05-29 2012-11-12 メルク・シャープ・エンド・ドーム・コーポレイション 放射標識されたpde10阻害剤
JP2015536973A (ja) * 2012-11-08 2015-12-24 ライゼン・ファーマシューティカルズ・エスアー PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物
JP2016510802A (ja) * 2013-03-15 2016-04-11 レスピバート・リミテツド 2−((4−アミノ−3−(3−フルオロ−5−ヒドロキシフェニル)−1h−ピラゾロ[3,4−d]ピリミジン−1−イル)メチル)−3−(2−トリフルオロ−メチル)ベンジル)キナゾリン−4(3h)−オン誘導体及びホスホイノシチド3−キナーゼ阻害剤としてのそれらの使用

Families Citing this family (35)

* 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
US20050043239A1 (en) * 2003-08-14 2005-02-24 Jason Douangpanya Methods of inhibiting immune responses stimulated by an endogenous factor
CA2566609C (en) 2004-05-13 2012-06-26 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
CN102271683B (zh) 2008-11-13 2014-07-09 吉里德卡利斯托加公司 恶性血液病的治疗
PE20120602A1 (es) 2009-03-24 2012-05-21 Gilead Calistoga Llc ATROPISOMEROS DE 2-[(6-AMINO-9H-PURIN-9-IL)METIL]-5-METIL-3-o-TOLILQUINAZOLIN-4(3H)-ONA
US8546409B2 (en) * 2009-04-20 2013-10-01 Gilead Calistoga Llc Methods of treatment for solid tumors
WO2011011550A1 (en) * 2009-07-21 2011-01-27 Calistoga Pharmaceuticals Inc. 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
EP2518070A1 (en) * 2011-04-29 2012-10-31 Almirall, S.A. Pyrrolotriazinone derivatives as PI3K inhibitors
EP2518071A1 (en) * 2011-04-29 2012-10-31 Almirall, S.A. Imidazopyridine derivatives as PI3K inhibitors
EA029473B1 (ru) 2011-12-15 2018-03-30 Новартис Аг Применение ингибиторов pi3k для лечения острой и церебральной малярии
PE20141792A1 (es) 2012-03-05 2014-12-07 Gilead Calistoga Llc Formas polimorficas de (s)-2-(1-(9h-purin-6-ilamino)propil)-5-fluor-3-fenilquinazolin-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
EA027277B1 (ru) * 2012-10-16 2017-07-31 Альмираль, С.А. Производные пирроллотриазинона в качестве ингибиторов pi3k
WO2014060431A1 (en) * 2012-10-16 2014-04-24 Almirall, S.A. Pyrrolotriazinone derivatives as pi3k inhibitors
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
RU2675105C9 (ru) * 2013-09-22 2019-01-09 Саншайн Лейк Фарма Ко., Лтд. Замещенные аминопиримидиновые соединения и способы их использования
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
AU2014364410B2 (en) 2013-12-20 2017-11-16 Gilead Calistoga Llc Process methods for phosphatidylinositol 3-kinase inhibitors
HRP20211151T1 (hr) 2014-05-27 2021-10-15 Rhizen Pharmaceuticals S.A. Kristalinska tosilatna sol pi3k delta selektivnog inhibitora za uporabu u farmaceutskim formulacijama
MD20160132A2 (ro) * 2014-05-27 2017-05-31 Almirall S.A. Săruri de adiţie ale (S)-2-(1-(6-amino-5-cianopirimidin-4-ilamino)etil)-4-oxo-3-fenil-3,4-dihidropirolo[1,2-f][1,2,4]triazin-5-carbonitrilului
KR20170012560A (ko) 2014-06-13 2017-02-02 길리애드 사이언시즈, 인코포레이티드 포스파티딜이노시톨 3-키나제 억제제
PE20170640A1 (es) 2014-07-04 2017-05-26 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
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
CA3028999A1 (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
EP3828184A4 (en) * 2018-08-21 2022-05-04 Medshine Discovery Inc. PYRAZOLOPYRIMIDI DERIVATIVES AND USE THEREOF AS A PI3K INHIBITOR
BR112022020342A2 (pt) 2020-04-10 2022-12-13 Gb005 Inc Inibidores da quinase

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005509635A (ja) * 2001-10-19 2005-04-14 アイコス コーポレイション 人間のホスファチジルイノシトール3−キナーゼデルタの阻害
JP2008500338A (ja) * 2004-05-25 2008-01-10 イコス・コーポレイション 造血細胞の異常増殖を治療及び/又は予防する方法
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

Family Cites Families (95)

* 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
US3897432A (en) 1971-04-21 1975-07-29 Merck & Co Inc Substituted benzimidazole derivatives
NL7204972A (enExample) 1971-04-21 1972-10-24
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
JPS55118918A (en) 1979-03-06 1980-09-12 Mitsubishi Electric Corp Production of quinazolone ring-containing epoxy resin
JPS55118917A (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
DE3675588D1 (de) 1985-06-19 1990-12-20 Ajinomoto Kk Haemoglobin, das an ein poly(alkenylenoxid) gebunden ist.
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
WO1988001213A1 (en) 1986-08-18 1988-02-25 Clinical Technologies Associates, Inc. Delivery systems for pharmacological agents
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.
SG43072A1 (en) 1991-06-18 1997-10-17 American Home Prod Method of treating adult t-cell leukemia/lymphoma
DE69312700T2 (de) 1992-04-14 1998-02-19 Cornell Res Foundation Inc Makromoleküle auf basis von dendritischen polymeren und verfahren zur herstellung
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
WO1996004923A1 (en) 1994-08-12 1996-02-22 Pro-Neuron, Inc. Methods for treating sepsis or inflammatory 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
EP0904107B1 (en) 1996-03-18 2004-10-20 Board Of Regents, The University Of Texas System Immunoglobin-like domains with increased half lives
SI0901487T1 (en) 1996-05-15 2003-10-31 Pfizer Inc. 2,3,6 trisubstituted-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
DE69723869T2 (de) 1996-12-31 2004-04-22 Dr. Reddy's Laboratories Ltd. Heterozyklische verbindungen, verfahren zu ihrer herstellung, pharmazeutische zusammensetzungen die diese enthalten und ihre anwendung in der behandlung von diabetis und verwandten krankheiten
GB9702701D0 (en) 1997-02-01 1997-04-02 Univ Newcastle Ventures Ltd Quinazolinone compounds
EP0968194B1 (en) 1997-02-28 2004-05-26 Pfizer Products Inc. Atropisomers of 3-aryl-4(3h)-quinazolinones and their use as ampa-receptor antagonists
PT964860E (pt) * 1997-02-28 2004-07-30 Pfizer Prod Inc Atropisomeros de 3-heteroaril-4(3h)-quinazolinonas para o tratamento de condicoes neurogenerativas e relacionadas com trauma do sistema nervoso central
ES2245015T3 (es) 1997-06-09 2005-12-16 Pfizer Products Inc. Quinazolin-4-onas como antagonistas de ampa.
US6277981B1 (en) 1997-07-03 2001-08-21 Thomas Jefferson University 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
AU2108299A (en) 1998-01-08 1999-07-26 University Of Virginia Patent Foundation A2A adenosine receptor agonists
ATE286032T1 (de) 1998-04-23 2005-01-15 Reddys Lab Ltd Dr Heterozyklische verbindungen,und deren verwendung in arzneimittel,verfahren zu deren herstellung und diese enthaltende pharmazeutische zusammenstellungen
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
ES2567260T3 (es) * 2000-04-25 2016-04-21 Icos Corporation Inhibidores de la fosfatidilinositol 3-quinasa delta humana
PL374718A1 (en) 2002-07-10 2005-10-31 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
ATE511510T1 (de) 2002-09-30 2011-06-15 Bayer Schering Pharma Ag Kondensierte azol-pyrimidin-derivate
CA2508601A1 (en) 2002-12-06 2004-06-24 Warner-Lambert Company Llc Benzoxazin-3-ones and derivatives thereof as inhibitors of pi3k
AU2003303231A1 (en) 2002-12-20 2004-07-14 Warner-Lambert Company Llc Benzoxazines and derivatives thereof as inhibitors of pi3ks
CA2518916A1 (en) 2003-04-03 2004-10-21 Joseph R. Garlich Pi-3 kinase inhibitor prodrugs
WO2004108708A1 (en) 2003-06-05 2004-12-16 Warner-Lambert Company Llc 3-substituted indoles and derivatives thereof as therapeutic agents
EP1644364A1 (en) 2003-06-05 2006-04-12 Warner-Lambert Company LLC Tetrazol benzofurancarboxamides with pi3k activity 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
US20040259926A1 (en) 2003-06-05 2004-12-23 Bruendl Michelle M. 3-Aryloxy and 3-heteroaryloxy substituted benzo[b]thiophenes as therapeutic agents
DE602004007268D1 (de) 2003-06-05 2007-08-09 Warner Lambert Co CYCLOALKYLSULFANYL-SUBSTITUIERTE BENZOiBöTHIOPHENE ALS THERAPEUTISCHE MITTEL
EP1636210A1 (en) 2003-06-05 2006-03-22 Warner-Lambert Company LLC Cycloalkyl and heterocycloalkyl substituted benzothiophenes as therapeutic agents
US20050054614A1 (en) 2003-08-14 2005-03-10 Diacovo Thomas G. Methods of inhibiting leukocyte accumulation
US20050043239A1 (en) 2003-08-14 2005-02-24 Jason Douangpanya Methods of inhibiting immune responses stimulated by an endogenous factor
WO2005067901A2 (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
CA2566609C (en) 2004-05-13 2012-06-26 Icos Corporation Quinazolinones as inhibitors of human phosphatidylinositol 3-kinase delta
EP1885356A2 (en) 2005-02-17 2008-02-13 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
WO2007076085A2 (en) 2005-12-22 2007-07-05 Prolexys Pharmaceuticals, Inc . Fused pyrimidones and thiopyrimidones, and uses thereof
KR20090087027A (ko) 2006-11-13 2009-08-14 일라이 릴리 앤드 캄파니 염증 질환 및 암의 치료를 위한 티에노피리미디논
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
CN101965335B (zh) 2008-01-04 2015-01-14 英特利凯恩有限责任公司 某些化学实体、组合物和方法
CN102271683B (zh) 2008-11-13 2014-07-09 吉里德卡利斯托加公司 恶性血液病的治疗
EP2365810A2 (en) 2008-12-04 2011-09-21 The U.S.A. As Represented By The Secretary, Department Of Health And Human Services Phosphatidylinositol-3-kinase p110 delta-targeted drugs in the treatment of cns disorders
PE20120602A1 (es) 2009-03-24 2012-05-21 Gilead Calistoga Llc ATROPISOMEROS DE 2-[(6-AMINO-9H-PURIN-9-IL)METIL]-5-METIL-3-o-TOLILQUINAZOLIN-4(3H)-ONA
US8546409B2 (en) 2009-04-20 2013-10-01 Gilead Calistoga Llc Methods of treatment for solid tumors
WO2011011550A1 (en) * 2009-07-21 2011-01-27 Calistoga Pharmaceuticals Inc. Treatment of liver disorders with pi3k inhibitors
MX342405B (es) 2010-06-03 2016-09-28 Pharmacyclics Inc El uso de inhibidores de la tirosina quinasa de bruton (btk).

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005509635A (ja) * 2001-10-19 2005-04-14 アイコス コーポレイション 人間のホスファチジルイノシトール3−キナーゼデルタの阻害
JP2008500338A (ja) * 2004-05-25 2008-01-10 イコス・コーポレイション 造血細胞の異常増殖を治療及び/又は予防する方法
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

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JPN6014025719; Topics in Stereochemistry 14, 1983, 1-81 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2012528176A (ja) * 2009-05-29 2012-11-12 メルク・シャープ・エンド・ドーム・コーポレイション 放射標識されたpde10阻害剤
JP2015536973A (ja) * 2012-11-08 2015-12-24 ライゼン・ファーマシューティカルズ・エスアー PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物
JP2018203760A (ja) * 2012-11-08 2018-12-27 ライゼン・ファーマシューティカルズ・エスアー PDE4阻害剤とPI3δ阻害剤または二重PI3δ−γキナーゼ阻害剤とを含有する薬学的組成物
JP7030656B2 (ja) 2012-11-08 2022-03-07 ライゼン・ファーマシューティカルズ・エスアー PDE4阻害剤とPI3δ阻害剤または二重PI3δ-γキナーゼ阻害剤とを含有する薬学的組成物
JP2016510802A (ja) * 2013-03-15 2016-04-11 レスピバート・リミテツド 2−((4−アミノ−3−(3−フルオロ−5−ヒドロキシフェニル)−1h−ピラゾロ[3,4−d]ピリミジン−1−イル)メチル)−3−(2−トリフルオロ−メチル)ベンジル)キナゾリン−4(3h)−オン誘導体及びホスホイノシチド3−キナーゼ阻害剤としてのそれらの使用

Also Published As

Publication number Publication date
SG174529A1 (en) 2011-10-28
EA201171160A1 (ru) 2012-04-30
CO6450655A2 (es) 2012-05-31
ECSP11011412A (es) 2012-03-30
NZ595307A (en) 2013-11-29
US20100249155A1 (en) 2010-09-30
CN102439012A (zh) 2012-05-02
MX2011009955A (es) 2011-11-18
WO2010111432A1 (en) 2010-09-30
BRPI1012333A2 (pt) 2016-03-29
AU2010229968A1 (en) 2011-10-13
CL2011002359A1 (es) 2012-04-09
CA2756347A1 (en) 2010-09-30
IL215251A0 (en) 2011-12-29
EP2411391A1 (en) 2012-02-01
KR20120002995A (ko) 2012-01-09
PE20120602A1 (es) 2012-05-21
EA019499B1 (ru) 2014-04-30
US8440677B2 (en) 2013-05-14
AP2011005943A0 (en) 2011-10-31

Similar Documents

Publication Publication Date Title
JP2012521994A (ja) 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
JP2013540758A (ja) Pi3k阻害化合物のアトロプ異性体
JP2022071072A (ja) (s)-7-(1-アクリロイルピペリジン-4-イル)-2-(4-フェノキシフェニル)-4,5,6,7-テトラ-ヒドロピラゾロ[1,5-a]ピリミジン-3-カルボキサミドの結晶形、その調製、及びその使用
US12180184B2 (en) Pyrimidopyrazolone derivative as Wee1 inhibitor and use thereof
JP7535537B2 (ja) タンパク質キナーゼ阻害剤としての置換ピロロ[2,3-b]ピリジン及びピラゾロ[3,4-b]ピリジン誘導体
JP7261428B2 (ja) ピロロピリミジン類化合物及びその使用
JP6244353B2 (ja) ピリジニルピラゾロキノリン化合物
EP3612519B1 (en) Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds
TW201321379A (zh) 吡唑并喹啉(Pyrazoloquinoline)衍生物
US11161854B2 (en) Indazolyl-spiro[2.2]pentane-carbonitrile derivatives as LRRK2 inhibitors, pharmaceutical compositions, and uses thereof
EP2125803A1 (fr) Composes pyrrolo[2,3-b]pyridine, composes azaindoles utiles dans la synthese de ces composes pyrrolo[2,3-b]pyridine, leurs procedes de fabrication et leurs utilisations
EP3845532B1 (en) Quinolino-pyrrolidin-2-one derivative and application thereof
EP3858833B1 (en) Aminonorbornane derivative and manufacture method thereof and use thereof
EP3144310A1 (en) Aminotetrahydropyran derivative used as dipeptidyl peptidase-iv inhibitor
CN113614090A (zh) 含有异噻唑烷1,1-二氧化物和1,4-丁烷磺内酯的雷帕霉素衍生物及其用途
US9458165B2 (en) DOT1L inhibitors
KR101886136B1 (ko) 신규한 항진균성 5,6-디하이드로-4-[(디플루오로에틸)페닐]-4H-피롤로[1,2-α][1,4]벤조디아제핀 및 4-(디플루오로에틸)페닐-6H-피롤로[1,2-α][1,4]벤조디아제핀 유도체
US20180111942A1 (en) Fused azaheterocyclic compounds and their use as ampa receptor modulators
RU2596823C2 (ru) ПРОИЗВОДНЫЕ 7-(ГЕТЕРОАРИЛ-АМИНО)-6,7,8,9-ТЕТРАГИДРОПИРИДО[1,2-a]ИНДОЛ-УКСУСНОЙ КИСЛОТЫ И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ МОДУЛЯТОРОВ РЕЦЕПТОРА ПРОСТАГЛАНДИНА D2
CN115968362A (zh) 作为pet放射性示踪剂的[18f]-标记的咪唑并吡啶衍生物
RU2809188C2 (ru) Аминонорборнановое производное и способ его получения, а также его применение
KR20130115304A (ko) 페닐 유도체로 치환된, 항진균성 5,6-디하이드로-4H-피롤로-[1,2-α][1,4]벤조디아제핀 및 6H-피롤로-[1,2-α][1,4]벤조디아제핀
KR20250164854A (ko) 치환된 인다졸 프로피온산 유도체 화합물 및 ampk 활성제로서의 이의 용도
HK40079392A (en) Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds
HK40024453A (en) Phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20130322

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20130322

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20140619

A02 Decision of refusal

Free format text: JAPANESE INTERMEDIATE CODE: A02

Effective date: 20150409