BRPI0807146A2 - Inibidores da atividade da akt - Google Patents

Inibidores da atividade da akt

Info

Publication number
BRPI0807146A2
BRPI0807146A2 BRPI0807146-2A2A BRPI0807146A BRPI0807146A2 BR PI0807146 A2 BRPI0807146 A2 BR PI0807146A2 BR PI0807146 A BRPI0807146 A BR PI0807146A BR PI0807146 A2 BRPI0807146 A2 BR PI0807146A2
Authority
BR
Brazil
Prior art keywords
akt activity
activity inhibitors
inhibitors
akt
activity
Prior art date
Application number
BRPI0807146-2A2A
Other languages
English (en)
Inventor
Mark Andrew Seefeld
Megan B Rouse
Dirk A Heerding
Simon Peace
Dennis S Yamashita
Kenneth C Mcnulty
Original Assignee
Smithkline Beecham Corp
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=39682107&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BRPI0807146(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of BRPI0807146A2 publication Critical patent/BRPI0807146A2/pt
Publication of BRPI0807146B1 publication Critical patent/BRPI0807146B1/pt
Publication of BRPI0807146B8 publication Critical patent/BRPI0807146B8/pt

Links

Classifications

    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
    • 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
    • A61K31/12—Ketones
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4192—1,2,3-Triazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/20—Pills, tablets, discs, rods
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • 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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Oncology (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
BRPI0807146A 2007-02-07 2008-02-07 compostos inibidores da atividade da akt, seu uso no tratamento de câncer e artrite, bem como composição farmacêutica compreendendo os mesmos BRPI0807146B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US88858607P 2007-02-07 2007-02-07
US60/888.586 2007-02-07
PCT/US2008/053269 WO2008098104A1 (en) 2007-02-07 2008-02-07 Inhibitors of akt activity

Publications (3)

Publication Number Publication Date
BRPI0807146A2 true BRPI0807146A2 (pt) 2014-04-15
BRPI0807146B1 BRPI0807146B1 (pt) 2020-05-26
BRPI0807146B8 BRPI0807146B8 (pt) 2021-05-25

Family

ID=39682107

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0807146A BRPI0807146B8 (pt) 2007-02-07 2008-02-07 compostos inibidores da atividade da akt, seu uso no tratamento de câncer e artrite, bem como composição farmacêutica compreendendo os mesmos

Country Status (35)

Country Link
US (7) US8273782B2 (pt)
EP (1) EP2117523B1 (pt)
JP (3) JP4723677B2 (pt)
KR (3) KR20140140570A (pt)
CN (1) CN101646427B (pt)
AR (1) AR066184A1 (pt)
AU (1) AU2008213694B2 (pt)
BR (1) BRPI0807146B8 (pt)
CA (1) CA2678255C (pt)
CL (1) CL2008000348A1 (pt)
CO (1) CO6220930A2 (pt)
CR (1) CR10995A (pt)
CY (1) CY1115535T1 (pt)
DK (1) DK2117523T3 (pt)
DO (1) DOP2009000196A (pt)
EA (1) EA018038B1 (pt)
ES (1) ES2501518T3 (pt)
HK (1) HK1132676A1 (pt)
HR (1) HRP20140790T1 (pt)
IL (1) IL200212A (pt)
JO (1) JO3134B1 (pt)
MA (1) MA31167B1 (pt)
MX (2) MX367398B (pt)
MY (1) MY164480A (pt)
NZ (1) NZ579177A (pt)
PE (1) PE20090058A1 (pt)
PL (1) PL2117523T3 (pt)
PT (1) PT2117523E (pt)
SG (1) SG193678A1 (pt)
SI (1) SI2117523T1 (pt)
TW (2) TWI381836B (pt)
UA (1) UA102992C2 (pt)
UY (1) UY30892A1 (pt)
WO (1) WO2008098104A1 (pt)
ZA (1) ZA200905363B (pt)

Families Citing this family (107)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7625890B2 (en) 2005-11-10 2009-12-01 Smithkline Beecham Corp. Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
WO2009094224A1 (en) 2008-01-25 2009-07-30 Millennium Pharmaceuticals, Inc. Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors
US20100048913A1 (en) 2008-03-14 2010-02-25 Angela Brodie Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens;Synthesis In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity
SG171914A1 (en) 2008-12-02 2011-07-28 Chiralgen Ltd Method for the synthesis of phosphorus atom modified nucleic acids
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
CN102395585A (zh) 2009-01-30 2012-03-28 米伦纽姆医药公司 杂芳基化合物和其作为pi3k抑制剂的用途
PE20120003A1 (es) * 2009-01-30 2012-02-12 Glaxosmithkline Llc Hidrocloruro de n-{(1s)-2-amino-1-[(3-fluorofenil)metil)etil}-5-cloro-4-(4-cloro-1-metil-1h-pirazol-5-il)-2-tiofenocarboxamida cristalino
EP2393827B1 (en) 2009-02-05 2015-10-07 Tokai Pharmaceuticals, Inc. Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens
AU2010270714B2 (en) 2009-07-06 2015-08-13 Wave Life Sciences Ltd. Novel nucleic acid prodrugs and methods use thereof
MX2012003546A (es) * 2009-09-23 2012-09-07 Glaxosmithkline Llc Combinacion.
ES2527831T3 (es) 2009-09-23 2015-01-30 Glaxosmithkline Llc Combinación que comprende el inhibidor de MEK: N-{3-[3-ciclopropil-5-(2-fluoro-4-yodo-fenilamino)-6,8-dimetil-2,4,7-trioxo-3,4,6,7-tetrahidro-2H-pirido[4,3-d]pirimidin-1-il]fenil}acetamida y el inhibidor de Akt: N-{(1S)-2-amino-1-[(3-fluorofenil)metil]etil}-5-cloro-4-(4-cloro-1-metil-1H-pirazol-5-il)-2-tiofenocarboxamida
KR101696003B1 (ko) 2009-10-08 2017-01-13 노파르티스 아게 조합물
PT2485593E (pt) * 2009-10-08 2015-04-28 Glaxosmithkline Llc Associação
WO2011060380A1 (en) * 2009-11-14 2011-05-19 The Regents Of The University Of California Pik3ca mutation status and sash1 expression predicts synergy between lapatinib and an akt inhibitor in her2 positive breast cancer
CA2794153C (en) 2010-03-25 2018-01-02 Glaxosmithkline Llc Substituted indoline derivatives as perk inhibitors
CA2829790C (en) 2010-03-30 2018-06-05 Verseon Corporation Multisubstituted aromatic compounds as inhibitors of thrombin
JP2013526578A (ja) 2010-05-21 2013-06-24 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー 組合せ
WO2011150044A1 (en) * 2010-05-26 2011-12-01 Glaxosmithkline Llc Combination
EP2603216A4 (en) 2010-08-11 2013-12-18 Millennium Pharm Inc HETEROARYLE AND USES THEREOF
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
CA2807971A1 (en) 2010-08-11 2012-02-16 Millenium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US10428019B2 (en) 2010-09-24 2019-10-01 Wave Life Sciences Ltd. Chiral auxiliaries
UY33671A (es) 2010-10-13 2012-04-30 Millenium Pharmaceuticals Inc Heteroarilos y sus usos
TWI505828B (zh) 2010-12-20 2015-11-01 葛蘭素史克智慧財產（第二）有限公司 新穎醫藥組成物
KR20140053836A (ko) 2011-01-11 2014-05-08 글락소스미스클라인 엘엘씨 조합물
US20120184548A1 (en) 2011-01-19 2012-07-19 Romyr Dominique Carboxylic acid aryl amides
US20120184542A1 (en) 2011-01-19 2012-07-19 Kevin Anderson Pyrido pyrimidines
US8362023B2 (en) 2011-01-19 2013-01-29 Hoffmann-La Roche Inc. Pyrazolo pyrimidines
US20120184562A1 (en) 2011-01-19 2012-07-19 Kin-Chun Luk 1,6- and 1,8-naphthyridines
US8673905B2 (en) 2011-03-17 2014-03-18 Hoffmann-La Roche Inc. Imidazo pyrazines
WO2012177925A1 (en) 2011-06-21 2012-12-27 The Board Institute, Inc. Akt inhibitors for treating cancer expressing a magi3 - akt3 fusion gene
DK2734208T3 (en) 2011-07-19 2017-06-19 Wave Life Sciences Ltd PROCEDURES FOR SYNTHESIS OF FUNCTIONALIZED NUCLEIC ACIDS
JP2015503505A (ja) * 2011-12-23 2015-02-02 ミレニアム ファーマシューティカルズ， インコーポレイテッドＭｉｌｌｅｎｎｉｕｍ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ， Ｉｎｃ． ヘテロアリールおよびその使用
NZ628394A (en) * 2012-04-24 2016-02-26 Glaxosmithkline Ip No 2 Ltd Treatment method for steroid responsive dermatoses
JP6246121B2 (ja) 2012-07-13 2017-12-13 株式会社新日本科学 キラル核酸アジュバント
US9598458B2 (en) 2012-07-13 2017-03-21 Wave Life Sciences Japan, Inc. Asymmetric auxiliary group
SG11201500232UA (en) 2012-07-13 2015-04-29 Wave Life Sciences Pte Ltd Chiral control
JP6254169B2 (ja) 2012-09-28 2017-12-27 ファイザー・インク ベンズアミドおよびヘテロベンズアミド化合物
CN105073729A (zh) 2012-10-16 2015-11-18 詹森药业有限公司 RORγt的苯基连接的喹啉基调节剂
KR20150070348A (ko) 2012-10-16 2015-06-24 얀센 파마슈티카 엔.브이. RoRγt의 헤테로아릴 결합 퀴놀리닐 조절제
PL2909192T3 (pl) 2012-10-16 2017-09-29 Janssen Pharmaceutica Nv Połączone metylenem modulatory chinolinylowe ROR-GAMMA-T
EP2908815A4 (en) * 2012-10-22 2016-06-22 Novartis Ag COMBINATION
ES2686730T3 (es) 2012-11-30 2018-10-19 Novartis Ag Composición farmacéutica novedosa
KR20150103735A (ko) 2013-01-09 2015-09-11 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 조합물
WO2014134267A1 (en) 2013-02-27 2014-09-04 Bristol-Myers Squibb Company Carbazole compounds useful as bromodomain inhibitors
US9884067B2 (en) 2013-03-14 2018-02-06 University Of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
AU2014238478B2 (en) * 2013-03-15 2018-07-19 Verseon Corporation Halogenopyrazoles as inhibitors of thrombin
MX2015012867A (es) 2013-03-15 2016-06-10 Verseon Corp Compuestos aromaticos multisustituidos como inhibidores de serina proteasa.
KR20160104612A (ko) 2013-07-26 2016-09-05 업데이트 파마 인코포레이트 비산트렌의 치료 효과 개선용 조성물
US9808472B2 (en) 2013-08-12 2017-11-07 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
AU2014330780B2 (en) 2013-10-01 2017-05-25 Novartis Ag Enzalutamide in combination with Afuresertib for the treatment of cancer
EP3718544A1 (en) * 2013-10-01 2020-10-07 Novartis AG Combination
WO2015057629A1 (en) 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv ALKYL LINKED QUINOLINYL MODULATORS OF RORyt
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
JP6320523B2 (ja) 2013-10-15 2018-05-09 ヤンセン ファーマシューティカ エヌ．ベー． ＲＯＲγＴの第二級アルコールキノリニルモジュレータ
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of RORγt
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
WO2015057626A1 (en) 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv QUINOLINYL MODULATORS OF RORyT
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
WO2015056180A1 (en) 2013-10-15 2015-04-23 Glaxosmithkline Intellectual Property (No.2) Limited Indoline derivatives as inhibitors of perk
TWI726544B (zh) 2013-12-24 2021-05-01 美商必治妥美雅史谷比公司 作為抗癌劑之新穎三環化合物
EP3095460A4 (en) 2014-01-15 2017-08-23 Shin Nippon Biomedical Laboratories, Ltd. Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent
JPWO2015108047A1 (ja) 2014-01-15 2017-03-23 株式会社新日本科学 免疫誘導活性を有するキラル核酸アジュバンド及び免疫誘導活性剤
JPWO2015108048A1 (ja) 2014-01-15 2017-03-23 株式会社新日本科学 抗腫瘍作用を有するキラル核酸アジュバンド及び抗腫瘍剤
US10160969B2 (en) 2014-01-16 2018-12-25 Wave Life Sciences Ltd. Chiral design
JP2017507963A (ja) * 2014-03-12 2017-03-23 ノバルティス アーゲー Ｂｔｋ阻害薬とａｋｔ阻害薬を含む組み合わせ
CN104926801B (zh) * 2014-03-22 2019-06-04 浙江大学 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用
MX2016013027A (es) 2014-04-04 2017-05-23 Del Mar Pharmaceuticals Uso de dianhidrogalactitol y analogos o derivados del mismo para tratar cancer de celulas no pequeñas del pulmon y cancer de ovario.
BR112016028119A2 (pt) 2014-06-06 2017-08-22 Res Triangle Inst Agonistas receptores de apelina (apj) e usos dos mesmos
WO2016044662A1 (en) 2014-09-17 2016-03-24 Verseon Corporation Pyrazolyl-substituted pyridone compounds as serine protease inhibitors
WO2016059602A2 (en) 2014-10-16 2016-04-21 Glaxo Group Limited Methods of treating cancer and related compositions
TW201630907A (zh) 2014-12-22 2016-09-01 必治妥美雅史谷比公司 ＴＧＦβＲ拮抗劑
SG10201907699YA (en) 2015-02-27 2019-09-27 Verseon Corp Substituted pyrazole compounds as serine protease inhibitors
CN107921026A (zh) 2015-08-28 2018-04-17 诺华股份有限公司 药物组合物包含(a)α‑同种型特异性PI3K抑制剂alpelisib(BYL719)和(b)AKT抑制剂,优选MK‑2206,afuresertib或uprosertib及其在治疗/预防癌症中的应用
WO2017098421A1 (en) 2015-12-08 2017-06-15 Glaxosmithkline Intellectual Property Development Limited Benzothiadiazine compounds
EP3386976A1 (en) 2015-12-09 2018-10-17 Research Triangle Institute, International Improved apelin receptor (apj) agonists and uses thereof
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
WO2017153952A1 (en) 2016-03-10 2017-09-14 Glaxosmithkline Intellectual Property Development Limited 5-sulfamoyl-2-hydroxybenzamide derivatives
CN109311908B (zh) * 2016-06-16 2021-05-07 哈尔滨珍宝制药有限公司 作为Akt抑制剂的二氢吡唑氮杂卓类化合物
JP7104690B2 (ja) * 2016-10-12 2022-07-21 リサーチ トライアングル インスティテュート 複素環式アペリン受容体（ａｐｊ）アゴニスト及びそれらの使用
BR112019011365A2 (pt) 2016-12-01 2019-10-22 Glaxosmithkline Ip Dev Ltd métodos para tratar câncer
CN107011377B (zh) * 2017-05-03 2019-02-26 南通书创药业科技有限公司 一种β-羰基磷酸酯的制备方法
CN110831582B (zh) 2017-07-05 2023-08-11 诺华股份有限公司 药物组合物
UY37866A (es) 2017-09-07 2019-03-29 Glaxosmithkline Ip Dev Ltd Nuevos compuestos derivados de benzoimidazol sustituidos que reducen la proteína myc (c-myc) en las células e inhiben la histona acetiltransferasa de p300/cbp.
WO2019053617A1 (en) 2017-09-12 2019-03-21 Glaxosmithkline Intellectual Property Development Limited CHEMICAL COMPOUNDS
JP7101781B2 (ja) * 2017-12-13 2022-07-15 ハルビン チェンバオ ファーマシューティカル カンパニー リミテッド Ａｋｔ阻害剤としての塩形態及びその結晶形態
EP3827006A4 (en) 2018-07-23 2022-04-06 Signalrx Pharmaceuticals, Inc. SINGLE MOLECULE COMPOUNDS PROVIDING MULTI-TARGET INHIBITION OF BTK AND OTHER PROTEINS AND METHODS OF USING THEM
JP2022512706A (ja) 2018-10-16 2022-02-07 エフ．ホフマン－ラ ロシュ アーゲー 眼科におけるＡｋｔ阻害剤の使用
US20220033775A1 (en) 2018-11-05 2022-02-03 Iovance Biotherapeutics, Inc. Expansion of tils utilizing akt pathways inhibitors
JP7406556B2 (ja) 2018-11-30 2023-12-27 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド Ｈｉｖ療法に有用な化合物
JPWO2020130125A1 (ja) 2018-12-21 2021-11-04 第一三共株式会社 抗体−薬物コンジュゲートとキナーゼ阻害剤の組み合わせ
CN110031626A (zh) * 2019-04-02 2019-07-19 浙江理工大学 一种用于胃肠道间质肿瘤迁移的标志物ack1及其应用
WO2021018941A1 (en) 2019-07-31 2021-02-04 Glaxosmithkline Intellectual Property Development Limited Methods of treating cancer
KR20220047589A (ko) 2019-08-08 2022-04-18 래크나 리미티드 암 치료 방법
US12014835B2 (en) 2020-02-19 2024-06-18 Vanderbilt University Methods for evaluating therapeutic benefit of combination therapies
EP4125840A1 (en) 2020-03-27 2023-02-08 Som Innovation Biotech, S.A. Compounds for use in the treatment of synucleinopathies
CN111592531B (zh) * 2020-06-23 2023-08-15 上海鲲博玖瑞医药科技发展有限公司 福瑞塞替的制备方法
CN111620860B (zh) * 2020-06-23 2023-02-03 济南健丰化工有限公司 一种福瑞塞替的制备方法
TW202222790A (zh) 2020-10-01 2022-06-16 德商拜耳廠股份有限公司 製備4-溴呋喃-2-羧酸酯之方法
WO2023174210A1 (en) 2022-03-14 2023-09-21 Laekna Limited Combination treatment for cancer
WO2023187037A1 (en) 2022-03-31 2023-10-05 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
TW202412757A (zh) 2022-05-27 2024-04-01 美商 Ｖｉｉｖ 醫療保健公司 用於hiv治療之化合物
WO2024083716A1 (en) 2022-10-17 2024-04-25 Astrazeneca Ab Combinations of a serd for the treatment of cancer
WO2024100236A1 (en) 2022-11-11 2024-05-16 Astrazeneca Ab Combination therapies for the treatment of cancer

Family Cites Families (178)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1030415A (zh) 1987-02-20 1989-01-18 山之内制药株式会社 饱和的杂环碳酰胺衍生物和它的制备方法
ES2005163A6 (es) 1987-04-14 1989-03-01 Lilly S A E Un procedimiento para la produccion de derivados de tiofen-2-carboxamida.
ES2075849T3 (es) 1988-03-16 1995-10-16 Smithkline Beecham Farma Derivados heterociclicos.
DE3810848A1 (de) 1988-03-30 1989-10-19 Boehringer Ingelheim Kg Neue 2,3,4-substituierte imidazole und 3,4,5-substituierte 1,2,4-triazole, ihre herstellung und verwendung
DE3927483A1 (de) 1989-08-19 1991-02-21 Boehringer Ingelheim Kg Neue substituierte heterocyclische fuenfringe, ihre herstellung und verwendung
US5258357A (en) 1989-10-07 1993-11-02 Basf Aktiengesellschaft Carboxamides, their preparation and their use as herbicides
DE3933573A1 (de) 1989-10-07 1991-04-18 Basf Ag Carbonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide
US6645969B1 (en) * 1991-05-10 2003-11-11 Aventis Pharmaceuticals Inc. Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase
US5559235A (en) 1991-10-29 1996-09-24 Glaxo Wellcome Inc. Water soluble camptothecin derivatives
GB9201755D0 (en) 1992-01-28 1992-03-11 British Bio Technology Compounds
US5595872A (en) * 1992-03-06 1997-01-21 Bristol-Myers Squibb Company Nucleic acids encoding microsomal trigyceride transfer protein
US5342947A (en) 1992-10-09 1994-08-30 Glaxo Inc. Preparation of water soluble camptothecin derivatives
AU674553B2 (en) 1992-10-14 1997-01-02 Merck & Co., Inc. Fibrinogen receptor antagonists
ES2133416T3 (es) 1992-10-23 1999-09-16 Merck Sharp & Dohme Ligandos de subtipos de receptores de dopamina.
FR2707295A1 (fr) 1993-06-07 1995-01-13 Rhone Poulenc Agrochimie Fongicides pyrazoles substitués en position 3 par un hétérocycle.
EP0712397B1 (en) * 1993-08-06 1999-04-21 Smithkline Beecham Plc Amide derivatives as 5ht1d receptor antagonists
US5739135A (en) * 1993-09-03 1998-04-14 Bristol-Myers Squibb Company Inhibitors of microsomal triglyceride transfer protein and method
US5681835A (en) 1994-04-25 1997-10-28 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
US5491237A (en) 1994-05-03 1996-02-13 Glaxo Wellcome Inc. Intermediates in pharmaceutical camptothecin preparation
US5668148A (en) 1995-04-20 1997-09-16 Merck & Co., Inc. Alpha1a adrenergic receptor antagonists
JP3964478B2 (ja) * 1995-06-30 2007-08-22 エーザイ・アール・アンド・ディー・マネジメント株式会社 ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬
US5846990A (en) * 1995-07-24 1998-12-08 Bristol-Myers Squibb Co. Substituted biphenyl isoxazole sulfonamides
PT783501E (pt) * 1995-08-02 2001-04-30 Uriach & Cia Sa J Derivados de pirimidona com actividade antifungica
AU6788996A (en) * 1995-08-02 1997-02-26 J. Uriach & Cia S.A. New carboxamides with antifungal activity
AU6709596A (en) 1995-08-22 1997-03-19 Japan Tobacco Inc. Amide compounds and use of the same
US5972980A (en) 1995-10-05 1999-10-26 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US6001866A (en) * 1995-10-05 1999-12-14 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
AU6966696A (en) * 1995-10-05 1997-04-28 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US5942544A (en) 1996-02-22 1999-08-24 Dupont Pharmaceuticals Company α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors
AU706497B2 (en) 1996-04-03 1999-06-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0891343A1 (en) 1996-04-03 1999-01-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AU706314B2 (en) 1996-04-03 1999-06-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507595A (ja) 1996-04-03 2000-06-20 メルク エンド カンパニー インコーポレーテッド ファルネシルプロテイントランスフェラーゼの阻害剤
CA2249639A1 (en) 1996-04-03 1997-10-09 Neville J. Anthony Inhibitors of farnesyl-protein transferase
AU706150B2 (en) 1996-04-03 1999-06-10 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2249665A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000504024A (ja) 1996-04-03 2000-04-04 メルク エンド カンパニー インコーポレーテッド ファルネシル―タンパク質トランスフェラーゼ阻害剤
WO1997036890A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
AUPO163896A0 (en) * 1996-08-14 1996-09-05 Resmed Limited Determination of respiratory airflow
AU6320998A (en) * 1997-02-21 1998-09-09 Bristol-Myers Squibb Company Benzoic acid derivatives and related compounds as antiarrhythmic agents
US5998336A (en) 1997-02-26 1999-12-07 The Board Of Trustees Of The Leland Stanford Junior University Ceramic/metal and A15/metal superconducting composite materials exploiting the superconducting proximity effect and method of making the same
AU7453498A (en) * 1997-05-30 1998-12-30 Takeda Chemical Industries Ltd. Sulfonamide derivatives, their production and use
GB9716557D0 (en) 1997-08-06 1997-10-08 Glaxo Group Ltd Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity
DE19744026A1 (de) 1997-10-06 1999-04-08 Hoechst Marion Roussel De Gmbh Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln
AU751139B2 (en) * 1997-10-13 2002-08-08 Astellas Pharma Inc. Amide derivative
AU1723099A (en) 1997-12-12 1999-07-05 Euro-Celtique S.A. 3-substituted adenines via2-thioxanthines
US6232320B1 (en) 1998-06-04 2001-05-15 Abbott Laboratories Cell adhesion-inhibiting antiinflammatory compounds
AUPP433398A0 (en) 1998-06-25 1998-07-16 Australian National University, The Compounds and processes
US6192967B1 (en) 1998-10-19 2001-02-27 Sunny En Liung Huang Collapsible auto shade
US6130333A (en) * 1998-11-27 2000-10-10 Monsanto Company Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use
GB9827882D0 (en) 1998-12-17 1999-02-10 Smithkline Beecham Plc Novel compounds
DE19904397A1 (de) 1999-02-04 2000-08-10 Bayer Ag Verwendung von Pyrazol-Carbonsäureamiden
DE19904396A1 (de) 1999-02-04 2000-08-10 Bayer Ag Substituierte Pyrazolbenzylamin-Derivate
JP2000256358A (ja) 1999-03-10 2000-09-19 Yamanouchi Pharmaceut Co Ltd ピラゾール誘導体
EP1171435A2 (de) 1999-04-13 2002-01-16 Basf Aktiengesellschaft Pyrimidin-2-on derivate als integrinrezeptorliganden
JP2003500376A (ja) 1999-05-24 2003-01-07 シーオーアール セラピューティクス インコーポレイテッド Ｘａ因子の阻害剤
WO2000071510A2 (en) * 1999-05-24 2000-11-30 Cor Therapeutics, Inc. INHIBITORS OF FACTOR Xa
JP2001247569A (ja) 1999-08-12 2001-09-11 Japan Tobacco Inc ピロリジン誘導体又はピペリジン誘導体及びその医薬用途
US6632815B2 (en) 1999-09-17 2003-10-14 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
WO2001038309A1 (en) 1999-11-24 2001-05-31 Cor Therapeutics, Inc. β-AMINO ACID-, ASPARTIC ACID- AND DIAMINOPROPIONIC-BASED INHIBITORS OF FACTOR Xa
US6770666B2 (en) 1999-12-27 2004-08-03 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs
AU763356C (en) 1999-12-27 2004-08-26 Japan Tobacco Inc. Fused-ring compounds and use thereof as drugs
AU782878B2 (en) 2000-02-05 2005-09-08 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
WO2001056557A2 (en) 2000-02-05 2001-08-09 Vertex Pharmaceuticals Incorporated Compositions useful as inhibitors of erk
BR0104424A (pt) * 2000-02-05 2002-01-08 Vertex Pharma Composições de pirazol úteis como inibidores de erk
US6376515B2 (en) * 2000-02-29 2002-04-23 Cor Therapeutics, Inc. Benzamides and related inhibitors of factor Xa
GB0011098D0 (en) 2000-05-08 2000-06-28 Black James Foundation Pharmaceutical compositions comprising protpn pump inhibitors and gastrin/cholecystokinin receptor ligands
WO2001087287A2 (en) 2000-05-19 2001-11-22 Applied Research Systems Ars Holding N.V. Use of pyrazole derivatives for treating infertility
US6589195B1 (en) * 2000-05-26 2003-07-08 Orthomerica Products, Inc. Modular adjustable prophylactic hip orthosis and adduction/abduction joint
WO2002000647A1 (en) * 2000-06-23 2002-01-03 Bristol-Myers Squibb Pharma Company Heteroaryl-phenyl substituted factor xa inhibitors
WO2002007823A2 (en) 2000-07-24 2002-01-31 Davide Riccardo Grassetti Inhibition of mutagenic effects of carcinogens
GB0018758D0 (en) 2000-07-31 2000-09-20 Smithkline Beecham Plc Novel use and compunds
JO2654B1 (en) 2000-09-04 2012-06-17 شركة جانسين فارماسوتيكا ان. في Multiple aryl caroxa amides are useful as lipid - lowering agents
JP4267920B2 (ja) 2001-01-26 2009-05-27 中外製薬株式会社 代謝調節剤として有用なマロニル−ＣｏＡ脱炭酸酵素阻害剤
MXPA03009846A (es) * 2001-04-27 2004-05-05 Vertex Pharma Derivados de triazol inhibidores de cinasa y usos de los mismos.
DE10223912A1 (de) * 2001-06-28 2003-01-16 Merck Patent Gmbh TN- und STN-Flüssigkristallanzeigen
US20030015823A1 (en) * 2001-07-18 2003-01-23 Hydranautics Method for forming a thick section, thermoset, solid casting
EP1423382B1 (en) * 2001-08-03 2008-04-16 Vertex Pharmaceuticals Incorporated Pyrazole-derived kinase inhibitors and uses thereof
US6875789B2 (en) 2001-08-03 2005-04-05 Vertex Pharmaceuticals Incorporated Pyrazole-derived kinase inhibitors and uses thereof
US6562816B2 (en) 2001-08-24 2003-05-13 Pharmacia & Upjohn Company Substituted-heteroaryl-7-aza[2.2.1]bicycloheptanes for the treatment of disease
ATE372114T1 (de) 2001-09-27 2007-09-15 Applied Research Systems Verfahren zur erhöhung des testosteronspiegels
US6794252B2 (en) * 2001-09-28 2004-09-21 Texas Instruments Incorporated Method and system for forming dual work function gate electrodes in a semiconductor device
WO2003035619A1 (en) 2001-10-25 2003-05-01 Merck & Co., Inc. Tyrosine kinase inhibitors
US6897208B2 (en) * 2001-10-26 2005-05-24 Aventis Pharmaceuticals Inc. Benzimidazoles
WO2003039529A1 (en) * 2001-11-07 2003-05-15 4Sc A.G. Selective antibacterial agents
TW200306819A (en) * 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
RU2004126671A (ru) 2002-02-06 2005-04-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Гетероарилсоединения, полезные в качестве ингибиторов gsk-3
US7335779B2 (en) 2002-03-08 2008-02-26 Quonova, Llc Modulation of pathogenicity
GB0206861D0 (en) 2002-03-22 2002-05-01 Glaxo Group Ltd Medicaments
GB0206860D0 (en) 2002-03-22 2002-05-01 Glaxo Group Ltd Compounds
CA2480856A1 (en) 2002-04-05 2003-10-23 Merck & Co., Inc. Substituted aryl amides
EP1507535A1 (en) * 2002-04-26 2005-02-23 Pfizer Products Inc. Pyrimidine-2,4,6-trione metallo-proteinase inhibitors
WO2003104778A1 (en) 2002-06-05 2003-12-18 Pharmacia & Upjohn Company Methods for identifying ligands using competitive binding 1h nmr experiments
GB0216224D0 (en) 2002-07-12 2002-08-21 Glaxo Group Ltd Compounds
KR20050034732A (ko) 2002-08-02 2005-04-14 아젠터 디스커버리 리미티드 히스톤 디아세틸라제 억제제로서의 치환된티에닐-히드록사믹산
AR041508A1 (es) 2002-08-09 2005-05-18 Astra Ab Compuestos con actividad en los receptores de glutamato metabotropicos
EP1534680B1 (en) * 2002-08-14 2012-02-22 Pharmaco Investments, Inc. Prenylation inhibitors and methods of their synthesis and use
US6649638B1 (en) 2002-08-14 2003-11-18 Ppd Discovery, Inc. Prenylation inhibitors and methods of their synthesis and use
CA2496246A1 (en) * 2002-08-23 2004-03-04 Chiron Corporation Pyrrole based inhibitors of glycogen synthase kinase 3
DE10239443A1 (de) 2002-08-28 2004-03-11 Boehringer Ingelheim International Gmbh Blockiervorrichtung für ein Sperrspannwerk mit federbetätigtem Abtrieb
EP1398029A1 (en) 2002-09-10 2004-03-17 LION Bioscience AG NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives
US20060084682A1 (en) 2002-12-13 2006-04-20 Heerding Dirk A Thrombopoietin mimetics
RU2005119173A (ru) * 2002-12-20 2006-02-27 Фармация Корпорейшн (Us) Ациклические пиразольные соединения
US20060247260A1 (en) 2003-02-10 2006-11-02 Bayer Healthcare Ag Bis (hetero) aryl carboxamide derivatives for use as PG12 antagonists
WO2004072018A1 (ja) 2003-02-12 2004-08-26 Takeda Pharmaceutical Company Limited アミン誘導体
US7223788B2 (en) 2003-02-14 2007-05-29 Sanofi-Aventis Deutschland Gmbh Substituted N-aryl heterocycles, process for their preparation and their use as medicaments
WO2004076418A1 (en) 2003-02-28 2004-09-10 Galderma Research & Development, S.N.C. Ligands that modulate lxr-type receptors
US7517887B2 (en) 2003-04-09 2009-04-14 General Atomics Reversible inhibitors of S-adenosyl-L-homocysteine hydrolase and uses thereof
TW200512195A (en) 2003-04-21 2005-04-01 Elan Pharm Inc Benzamide 2-hydroxy-3-diaminoalkanes
US7612064B2 (en) 2003-05-26 2009-11-03 Takeda Pharmaceutical Company Limited Sulfopyrroles
MXPA05013645A (es) * 2003-06-20 2006-02-24 Galderma Res & Dev Nuevos compuestos moduladores de los receptores de tipo ppar gama y su utilizacion en composiciones cosmeticas o farmaceuticas.
DE10331305A1 (de) 2003-07-10 2005-02-17 Siemens Ag Kommunikationssystem, Peer-to-Peer-Nachrichten-Filter-Rechner und Verfahren zum Verarbeiten einer Peer-to-Peer-Nachricht
FR2857666B1 (fr) 2003-07-15 2005-08-26 Oreal Composition tinctoriale comprenant a titre de coupleur un derive du furane et nouveaux derives du furane
PL1651232T3 (pl) 2003-07-23 2011-05-31 Synta Pharmaceuticals Corp Związki do zastosowań związanych z zapaleniami i odpornością
WO2005019200A2 (en) 2003-08-14 2005-03-03 Icos Corporation Aryl piperidine derivatives as vla-1 integrin antagonists and uses thereof
CA2536470A1 (en) 2003-08-15 2005-02-24 Vertex Pharmaceuticals Incorporated Pyrrole compositions useful as inhibitors of c-met
WO2005019182A1 (en) 2003-08-20 2005-03-03 Bayer Healthcare Ag Pyrazolylmethylbenzamide derivatives as p2xt-receptor antagonists
JP2007507549A (ja) * 2003-10-06 2007-03-29 グラクソ　グループ　リミテッド キナーゼ阻害剤としての１，６，７−三置換アザベンゾイミダゾールの調製
US20070123561A1 (en) 2003-10-06 2007-05-31 Dennis Lee Preparation of 1,7-disubstituted azabensimidazoles as kinase inhibitors
US20050148605A1 (en) 2003-11-13 2005-07-07 Ambit Biosciences Corporation Amide derivatives as ABL modulators
CN1882347A (zh) 2003-11-21 2006-12-20 阿雷生物药品公司 Akt蛋白激酶抑制剂
WO2005077435A1 (en) 2004-01-19 2005-08-25 Atul Kumar A system for distending body tissue cavities by continuous flow irrigation
EP1708697A4 (en) 2004-01-30 2007-11-28 Smithkline Beecham Corp CHEMICAL COMPOUNDS
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005081954A2 (en) 2004-02-25 2005-09-09 Wyeth Inhibitors of protein tyrosine phosphatase 1b
WO2005095386A1 (en) * 2004-03-30 2005-10-13 Chiron Corporation Substituted thiophene derivatives as anti-cancer agents
WO2005099200A1 (en) * 2004-03-30 2005-10-20 Matsushita Electric Industrial Co., Ltd. Content relay server, content relay system, content relay method, and program using the same
WO2005097765A1 (en) 2004-03-31 2005-10-20 Exelixis, Inc. Anaplastic lymphoma kinase modulators and methods of use
JP2005336172A (ja) 2004-04-26 2005-12-08 Japan Tobacco Inc 腎虚血再灌流障害治療又は予防薬
TW200600492A (en) * 2004-05-18 2006-01-01 Achillion Pharmaceuticals Inc Substituted aryl acylthioureas and related compounds; inhibitors of viral replication
EP1758874A1 (en) 2004-05-29 2007-03-07 7TM Pharma A/S Substituted thiazoleacetic acids as crth2 ligands
WO2006009876A2 (en) 2004-06-17 2006-01-26 Cengent Therapeutics, Inc. Trisubstituted nitrogen modulators of tyrosine phosphatases
AU2005260689B2 (en) * 2004-06-30 2012-05-10 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of protein kinases
US7671077B2 (en) * 2004-07-19 2010-03-02 Leu-Fen Hou Lin Neuroprotective small organic molecules, compositions and uses related thereto
US20060019967A1 (en) * 2004-07-21 2006-01-26 Su-Ying Wu SARS CoV main protease inhibitors
US20060019968A1 (en) * 2004-07-24 2006-01-26 Laboratorios Dr. Esteve S.A. Use of compounds active on the sigma receptor for the treatment of neuropathic pain
US7269099B2 (en) 2004-07-30 2007-09-11 Bolt Technology Corporation Air gun
JP2006066488A (ja) * 2004-08-25 2006-03-09 Mitsubishi Electric Corp 半導体受光素子およびその製造方法
US7365385B2 (en) * 2004-08-30 2008-04-29 Micron Technology, Inc. DRAM layout with vertical FETs and method of formation
US20060043513A1 (en) * 2004-09-02 2006-03-02 Deok-Hoon Kim Method of making camera module in wafer level
TW200616969A (en) 2004-09-17 2006-06-01 Tanabe Seiyaku Co Imidazole compound
US20060062453A1 (en) * 2004-09-23 2006-03-23 Sharp Laboratories Of America, Inc. Color highlighting document image processing
WO2006043518A1 (ja) 2004-10-18 2006-04-27 Santen Pharmaceutical Co., Ltd. 神経疾患治療剤
JP2006120339A (ja) 2004-10-19 2006-05-11 Matsushita Electric Ind Co Ltd 高周波加熱電源装置
TW200619843A (en) 2004-10-20 2006-06-16 Sumitomo Bakelite Co Semiconductor wafer and semiconductor device
DE102004051277A1 (de) * 2004-10-21 2006-04-27 Merck Patent Gmbh Heterocyclische Carbonylverbindungen
DE102004054666A1 (de) 2004-11-12 2006-05-18 Bayer Cropscience Gmbh Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren
WO2006058012A2 (en) 2004-11-23 2006-06-01 Wyeth Gonadotropin releasing hormone receptor antagonists
JP2008521776A (ja) 2004-11-30 2008-06-26 ノイロサーチ アクティーゼルスカブ コリン作動性リガンドとしての新規なジアザ二環式アリール誘導体
SE527990C2 (sv) 2004-12-06 2006-08-01 Mora Of Sweden Ab Isborr
JP2008528700A (ja) 2005-02-03 2008-07-31 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｐｐａｒモジュレーターとしての化合物および組成物
JP2006232707A (ja) 2005-02-23 2006-09-07 Japan Tobacco Inc 癌転移抑制剤
AU2006235438A1 (en) 2005-04-11 2006-10-19 Achillion Pharmaceuticals, Inc. Pharmaceutical compositions for and methods of inhibiting HCV replication
TW200720272A (en) 2005-04-22 2007-06-01 Kalypsys Inc Novel ortho-terphenyl inhibitors of p38 kinase and methods of treating inflammatory disorders
GB0510139D0 (en) 2005-05-18 2005-06-22 Addex Pharmaceuticals Sa Novel compounds B1
JP2008543919A (ja) 2005-06-21 2008-12-04 アステックス・セラピューティクス・リミテッド 医薬化合物
US20060288588A1 (en) 2005-06-22 2006-12-28 Frank Morabito Garden tool
US8541461B2 (en) * 2005-06-23 2013-09-24 Astex Therapeutics Limited Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators
WO2006136637A2 (es) * 2005-06-24 2006-12-28 Eloy Antonio Martinez Albal Implante dental de corona rotatoria
CA2613261A1 (en) 2005-06-24 2006-12-28 Genelabs Technologies, Inc. Heteroaryl derivatives for treating viruses
MX2008000141A (es) 2005-06-27 2008-04-07 Exelixis Inc Moduladores de lxr basados en imidazol.
CN100494167C (zh) 2005-08-02 2009-06-03 天津大学 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用
GB0518237D0 (en) 2005-09-07 2005-10-19 Angeletti P Ist Richerche Bio Therapeutic compounds
WO2007052843A1 (ja) 2005-11-04 2007-05-10 Takeda Pharmaceutical Company Limited 複素環アミド化合物およびその用途
US7838676B2 (en) 2005-11-21 2010-11-23 Amgen Inc. Beta-secretase modulators and methods of use
EP1966141A1 (en) 2005-12-14 2008-09-10 Brystol-Myers Squibb Company Six-membered heterocycles useful as serine protease inhibitors
JP2009521504A (ja) 2005-12-22 2009-06-04 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性阻害剤
MX2008008320A (es) * 2005-12-23 2008-09-03 Smithkline Beecham Corp Inhibidores de azaindol de aurora cinasas.
AR056882A1 (es) 2006-02-01 2007-10-31 Bayer Cropscience Sa Derivados del fungicida n- cicloalquil- bencil- amida
AU2007221020B9 (en) 2006-02-28 2013-04-04 Dart Neuroscience (Cayman) Ltd. Therapeutic compounds
JP2007277230A (ja) 2006-03-15 2007-10-25 Tanabe Seiyaku Co Ltd 医薬組成物
WO2008080056A2 (en) 2006-12-21 2008-07-03 Sloan-Kettering Institute For Cancer Research Pyridazinones and furan-containing compounds
EP2125739A1 (en) 2006-12-22 2009-12-02 Encysive Pharmaceuticals, Inc. Modulators of c3a receptor and methods of use thereof
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
US8420690B2 (en) 2007-02-07 2013-04-16 Glaxosmithkline Llc Inhibitors of Akt activity
WO2008121685A1 (en) 2007-03-28 2008-10-09 Smithkline Beecham Corporation Methods of use for inhibitors of akt activity
WO2008121786A1 (en) 2007-03-29 2008-10-09 Smithkline Beecham Corporation Inhibitors of akt activity

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