HRP20140790T1 - Inhibitori aktivnosti akt - Google Patents

Inhibitori aktivnosti akt Download PDF

Info

Publication number
HRP20140790T1
HRP20140790T1 HRP20140790AT HRP20140790T HRP20140790T1 HR P20140790 T1 HRP20140790 T1 HR P20140790T1 HR P20140790A T HRP20140790A T HR P20140790AT HR P20140790 T HRP20140790 T HR P20140790T HR P20140790 T1 HRP20140790 T1 HR P20140790T1
Authority
HR
Croatia
Prior art keywords
methyl
ethyl
pyrazol
amino
chloro
Prior art date
Application number
HRP20140790AT
Other languages
English (en)
Croatian (hr)
Inventor
Mark Andrew Seefeld
Meagan B. Rouse
Dirk A. Heerding
Simon Peace
Dennis S. Yamashita
Kenneth C. Mcnulty
Original Assignee
Glaxosmithkline Llc
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=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HRP20140790(T1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Glaxosmithkline Llc filed Critical Glaxosmithkline Llc
Publication of HRP20140790T1 publication Critical patent/HRP20140790T1/hr

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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Physiology (AREA)
  • Nutrition Science (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Immunology (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)
HRP20140790AT 2007-02-07 2008-02-07 Inhibitori aktivnosti akt HRP20140790T1 (hr)

Applications Claiming Priority (2)

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

Publications (1)

Publication Number Publication Date
HRP20140790T1 true HRP20140790T1 (hr) 2014-10-10

Family

ID=39682107

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20140790AT HRP20140790T1 (hr) 2007-02-07 2008-02-07 Inhibitori aktivnosti akt

Country Status (34)

Country Link
US (7) US8273782B2 (en:Method)
EP (1) EP2117523B1 (en:Method)
JP (3) JP4723677B2 (en:Method)
KR (3) KR101537825B1 (en:Method)
CN (1) CN101646427B (en:Method)
AR (1) AR066184A1 (en:Method)
AU (1) AU2008213694B2 (en:Method)
BR (1) BRPI0807146B8 (en:Method)
CA (1) CA2678255C (en:Method)
CL (1) CL2008000348A1 (en:Method)
CO (1) CO6220930A2 (en:Method)
CR (1) CR10995A (en:Method)
CY (1) CY1115535T1 (en:Method)
DK (1) DK2117523T3 (en:Method)
DO (1) DOP2009000196A (en:Method)
EA (1) EA018038B1 (en:Method)
ES (1) ES2501518T3 (en:Method)
HR (1) HRP20140790T1 (en:Method)
IL (1) IL200212A (en:Method)
JO (1) JO3134B1 (en:Method)
MA (1) MA31167B1 (en:Method)
MX (2) MX2009008550A (en:Method)
MY (1) MY164480A (en:Method)
NZ (1) NZ579177A (en:Method)
PE (1) PE20090058A1 (en:Method)
PL (1) PL2117523T3 (en:Method)
PT (1) PT2117523E (en:Method)
SG (1) SG193678A1 (en:Method)
SI (1) SI2117523T1 (en:Method)
TW (2) TWI381836B (en:Method)
UA (1) UA102992C2 (en:Method)
UY (1) UY30892A1 (en:Method)
WO (1) WO2008098104A1 (en:Method)
ZA (1) ZA200905363B (en:Method)

Families Citing this family (112)

* 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
JP5581219B2 (ja) 2008-01-25 2014-08-27 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 チオフェンおよびホスファチジルイノシトール３−キナーゼ（ｐｉ３ｋ）阻害薬としてのその使用
US20100048524A1 (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
JP5645840B2 (ja) 2008-12-02 2014-12-24 株式会社Ｗａｖｅ Ｌｉｆｅ Ｓｃｉｅｎｃｅｓ Ｊａｐａｎ リン原子修飾核酸の合成方法
US9090601B2 (en) 2009-01-30 2015-07-28 Millennium Pharmaceuticals, Inc. Thiazole derivatives
US8796314B2 (en) 2009-01-30 2014-08-05 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
WO2010088331A1 (en) * 2009-01-30 2010-08-05 Glaxosmithkline Llc Crystalline n-{(1-s)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1h-pyrazol-5-yl)-2-thiophenecarboxamide hydrochloride
CA2750935A1 (en) 2009-01-30 2010-08-12 Millennium Pharmaceuticals, Inc. Heteroaryls and their use as pi3k inhibitors
BRPI1008745A2 (pt) 2009-02-05 2019-09-17 Tokai Pharmaceuticals Inc pró-fármacos de inibidores esteroidais de cyp17/antiandrogênios
EP2451461A4 (en) 2009-07-06 2013-05-29 Ontorii Inc NOVEL NUCLEIC ACID PRODRUGS AND METHOD OF USE THEREOF
SG179144A1 (en) * 2009-09-23 2012-05-30 Glaxosmithkline Llc Combination
JP2013505939A (ja) * 2009-09-23 2013-02-21 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
EA022982B1 (ru) 2009-10-08 2016-04-29 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Комбинация для лечения рака или предраковых синдромов
WO2011044415A1 (en) * 2009-10-08 2011-04-14 Glaxosmithkline Llc Combination
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
US8598156B2 (en) 2010-03-25 2013-12-03 Glaxosmithkline Llc Chemical compounds
KR101955691B1 (ko) 2010-03-30 2019-03-07 베르선 코포레이션 트롬빈 억제제로서의 다중치환된 방향족 화합물
EP2572199B1 (en) 2010-05-21 2017-03-08 Novartis AG Combination
US20130237554A1 (en) * 2010-05-26 2013-09-12 Rakesh Kumar Combination
BR112013003358A2 (pt) 2010-08-11 2016-07-12 Millennium Pharm Inc heteroaris e seus usos
US8859768B2 (en) 2010-08-11 2014-10-14 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US9062038B2 (en) 2010-08-11 2015-06-23 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
US10428019B2 (en) 2010-09-24 2019-10-01 Wave Life Sciences Ltd. Chiral auxiliaries
MX2013004003A (es) 2010-10-13 2013-10-01 Millenium Pharmaceuticals Inc Heteroarilos y usos de los mismos.
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
AU2012205601B2 (en) 2011-01-11 2016-03-24 Novartis Ag Combination
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
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
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
WO2013012758A1 (en) 2011-07-19 2013-01-24 Ontorii, Inc. Methods for the synthesis of functionalized nucleic acids
WO2013096637A1 (en) * 2011-12-23 2013-06-27 Millennium Pharmaceuticals, Inc. Heteroaryls and uses thereof
KR20150010943A (ko) * 2012-04-24 2015-01-29 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 스테로이드 반응성 피부병의 치료 방법
SG11201500243WA (en) 2012-07-13 2015-04-29 Shin Nippon Biomedical Lab Ltd Chiral nucleic acid adjuvant
SG11201500232UA (en) 2012-07-13 2015-04-29 Wave Life Sciences Pte Ltd Chiral control
RU2693381C2 (ru) 2012-07-13 2019-07-02 Уэйв Лайф Сайенсес Лтд. Асимметричная вспомогательная группа
US20150239842A1 (en) 2012-09-28 2015-08-27 Pfizer Inc. Benzamide and heterobenzamide compounds
PE20151203A1 (es) 2012-10-16 2015-08-31 Janssen Pharmaceutica Nv MODULADORES DE QUINOLINILO UNIDOS A FENILO DE ROR-GAMMA-t
MY189505A (en) 2012-10-16 2022-02-16 Janssen Pharmaceutica Nv Methylene linked quinolinyl modulators of roryt
HK1213250A1 (zh) 2012-10-16 2016-06-30 Janssen Pharmaceutica, N.V. RORγT的雜芳基連接的喹啉基調節劑
JP2015534986A (ja) * 2012-10-22 2015-12-07 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ＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ 組合せ
IL300664A (en) 2012-11-30 2023-04-01 Novartis Ag Innovative pharmaceutical composition
CA2897559A1 (en) 2013-01-09 2014-07-17 Glaxosmithkline Intellectual Property (No.2) Limited Combination
CN105189488B (zh) 2013-02-27 2018-07-24 百时美施贵宝公司 用作溴区结构域抑制剂的咔唑化合物
EP4066841A1 (en) 2013-03-14 2022-10-05 University of Maryland, Baltimore Androgen receptor down-regulating agents and uses thereof
SG10201707486XA (en) * 2013-03-15 2017-10-30 Verseon Corp Halogenopyrazoles as inhibitors of thrombin
CA2901637C (en) 2013-03-15 2019-09-24 Kevin Michael Short Multisubstituted aromatic compounds as serine protease inhibitors
AU2014293011A1 (en) 2013-07-26 2016-03-17 Race Oncology Ltd. Compositions to improve the therapeutic benefit of bisantrene
WO2015023710A1 (en) 2013-08-12 2015-02-19 Tokai Pharmaceuticals, Inc. Biomarkers for treatment of neoplastic disorders using androgen-targeted therapies
EP3718544A1 (en) 2013-10-01 2020-10-07 Novartis AG Combination
US20160235714A1 (en) * 2013-10-01 2016-08-18 Novartis Ag Enzalutamide in combination with afuresertib for the treatment of cancer
BR112016008257A2 (pt) 2013-10-15 2017-09-26 Janssen Pharmaceutica Nv moduladores de roryt de álcool quinolínico secundário
US9221804B2 (en) 2013-10-15 2015-12-29 Janssen Pharmaceutica Nv Secondary alcohol quinolinyl modulators of RORγt
CA2927182A1 (en) 2013-10-15 2015-04-23 Janssen Pharmaceutica Nv Quinolinyl modulators of ror.gamma.t
US9328095B2 (en) 2013-10-15 2016-05-03 Janssen Pharmaceutica Nv Heteroaryl linked quinolinyl modulators of RORgammat
US9403816B2 (en) 2013-10-15 2016-08-02 Janssen Pharmaceutica Nv Phenyl linked quinolinyl modulators of RORγt
US10555941B2 (en) 2013-10-15 2020-02-11 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORγt
AU2014334619A1 (en) 2013-10-15 2016-04-21 Janssen Pharmaceutica Nv Alkyl linked quinolinyl modulators of RORyt
US9284308B2 (en) 2013-10-15 2016-03-15 Janssen Pharmaceutica Nv Methylene 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
AU2014369982B2 (en) 2013-12-24 2019-04-18 Bristol-Myers Squibb Company Tricyclic compounds as anticancer agents
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
WO2015108046A1 (ja) 2014-01-15 2015-07-23 株式会社新日本科学 抗アレルギー作用を有するキラル核酸アジュバンド及び抗アレルギー剤
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
ES2917473T3 (es) 2014-01-16 2022-07-08 Wave Life Sciences Ltd Diseño quiral
MX2016011674A (es) 2014-03-12 2017-04-27 Novartis Ag Combinacion que comprende un inhibidor de btk y un inhibidor de akt.
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
KR102359214B1 (ko) 2014-04-04 2022-02-07 델 마 파마슈티컬스 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체
MA39999A (fr) 2014-06-06 2015-12-10 Res Triangle Inst Agonistes du récepteur de l'apeline (apj) et leurs utilisations
MX2017003624A (es) 2014-09-17 2017-07-13 Verseon Corp Compuestos de piridona sustituida con pirazolilo como inhibidores de serina proteasas.
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
LT3261639T (lt) 2015-02-27 2022-11-25 Verseon International Corporation Pakaitiniai pirazolo junginiai kaip serino proteazės inhibitoriai
JP2018526375A (ja) 2015-08-28 2018-09-13 ノバルティス アーゲー 組み合わせ療法
WO2017098421A1 (en) 2015-12-08 2017-06-15 Glaxosmithkline Intellectual Property Development Limited Benzothiadiazine compounds
RU2021133849A (ru) 2015-12-09 2022-03-21 Рисерч Трайэнгл Инститьют Улучшенные агонисты апелинового рецептора (apj) и их использование
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
EP3473628B1 (en) * 2016-06-16 2019-12-11 Harbin Zhenbao Pharmaceutical Co., Ltd. Dihydropyrazole azepine compound serving as akt inhibitor
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
CN110225983A (zh) 2016-12-01 2019-09-10 葛兰素史密斯克莱知识产权发展有限公司 治疗癌症的方法
WO2018140730A1 (en) 2017-01-27 2018-08-02 Signalrx Pharmaceuticals, Inc. Thienopyranones and furanopyranones as kinase, bromodomain, and checkpoint inhibitors
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
US11504333B2 (en) 2017-07-05 2022-11-22 Novartis Ag Pharmaceutical composition
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
US20210300939A1 (en) 2018-07-23 2021-09-30 Signalrx Pharmaceuticals, Inc. Single Molecule Compounds Providing Multi-Target Inhibition of BTK and Other Proteins and Methods of Use Thereof
CN112888440A (zh) 2018-10-16 2021-06-01 豪夫迈·罗氏有限公司 Akt抑制剂在眼科中的用途
US12343380B2 (en) 2018-11-05 2025-07-01 Iovance Biotherapeutics, Inc. Expansion of TILs utilizing AKT pathways inhibitors
MY202884A (en) 2018-11-30 2024-05-28 Univ North Carolina Chapel Hill Compounds useful in hiv therapy
SG11202106635WA (en) 2018-12-21 2021-07-29 Daiichi Sankyo Co Ltd Combination of antibody-drug conjugate and kinase inhibitor
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
BR112022003490A2 (pt) 2019-08-26 2022-05-24 Arvinas Operations Inc Método de tratamento do câncer de mama e mama metastático, método para degradação seletiva, método para inibir uma quinase, kit, composição líquida, e, método de produção de uma composição líquida
EP4073102A4 (en) 2019-12-12 2024-05-08 Ting Therapeutics LLC Compositions and methods for the prevention and treatment of hearing loss
US12014835B2 (en) 2020-02-19 2024-06-18 Vanderbilt University Methods for evaluating therapeutic benefit of combination therapies
WO2021191417A1 (en) 2020-03-27 2021-09-30 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
WO2022069554A1 (de) 2020-10-01 2022-04-07 Bayer Aktiengesellschaft Verfahren zur herstellung von 4-bromfuran-2-carboxylaten
WO2023174210A1 (en) 2022-03-14 2023-09-21 Laekna Limited Combination treatment for cancer
US20250205233A1 (en) 2022-03-31 2025-06-26 Astrazeneca Ab Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer
AR129423A1 (es) 2022-05-27 2024-08-21 Viiv Healthcare Co Compuestos útiles en la terapia contra el hiv
KR20250089532A (ko) 2022-10-17 2025-06-18 아스트라제네카 아베 암 치료를 위한 serd의 조합
JP2025539034A (ja) 2022-11-11 2025-12-03 アストラゼネカ・アクチエボラーグ 癌の治療のための併用療法
CN121218987A (zh) 2023-06-02 2025-12-26 阿尔维纳斯运营股份有限公司 雌激素受体降解剂和akt抑制剂的组合
CN117486856B (zh) * 2023-11-02 2026-02-06 上海毕得医药科技股份有限公司 一种4-溴-5-(三氟甲基)噻吩-2-羧酸甲酯的合成方法

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.
US4999359A (en) 1988-03-16 1991-03-12 Dr. Lo Zambeletti S.P.A. Heterocyclic ethylene diamine compounds and their pharmaceutical compositions and methods
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
DE3933573A1 (de) * 1989-10-07 1991-04-18 Basf Ag Carbonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide
US5258357A (en) 1989-10-07 1993-11-02 Basf Aktiengesellschaft Carboxamides, their preparation and their use as herbicides
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
WO1994008577A1 (en) 1992-10-14 1994-04-28 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.
DE69418045T2 (de) * 1993-08-06 1999-10-07 Smithkline Beecham P.L.C., Brentford Amidderivate als 5ht1d rezeptor antagonisten
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
BR9606547A (pt) * 1995-08-02 1997-10-14 Uriach & Cia Sa J Novos derivados de pirimidona com atividade fungicida
US5888941A (en) * 1995-08-02 1999-03-30 J. Uriach & Cia. S.A. Carbozamides with antifungal activity
KR100284382B1 (ko) 1995-08-22 2001-03-02 미즈노 마사루 아미드화합물 및 그의 용도
US6001866A (en) 1995-10-05 1999-12-14 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
US5972980A (en) 1995-10-05 1999-10-26 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
AU721952B2 (en) 1996-04-03 2000-07-20 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2249665A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
CA2249639A1 (en) 1996-04-03 1997-10-09 Neville J. Anthony Inhibitors of farnesyl-protein transferase
WO1997036901A1 (en) 1996-04-03 1997-10-09 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
JP2000507591A (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―タンパク質トランスフェラーゼ阻害剤
WO1997036898A1 (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
AU706497B2 (en) 1996-04-03 1999-06-17 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1997036896A1 (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
BR9815170A (pt) 1997-12-12 2000-10-10 Euro Celtique S A Luxembourg "método de obter composto aplicável no tratamento de asma em mamìferos"
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
DE19904396A1 (de) 1999-02-04 2000-08-10 Bayer Ag Substituierte Pyrazolbenzylamin-Derivate
DE19904397A1 (de) 1999-02-04 2000-08-10 Bayer Ag Verwendung von Pyrazol-Carbonsäureamiden
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
US6638980B1 (en) * 1999-05-24 2003-10-28 Millennium Pharmaceuticals, Inc. Inhibitors of factor Xa
CA2374641A1 (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
CA2392576A1 (en) 1999-11-24 2001-05-31 Lingyan Wang .beta.-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
ID30204A (id) 1999-12-27 2001-11-15 Japan Tobacco Inc Senyawa-senyawa cincin terfusi dan penggunaannya sebagai obat
AU782878B2 (en) 2000-02-05 2005-09-08 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of erk
AU2001236720A1 (en) 2000-02-05 2001-08-14 Bemis, Guy Compositions useful as inhibitors of erk
AU782775B2 (en) * 2000-02-05 2005-08-25 Vertex Pharmaceuticals Incorporated Pyrazole compositions useful as inhibitors of 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
JP4371295B2 (ja) * 2000-05-19 2009-11-25 メルク セローノ ソシエテ アノニム 医薬として活性な化合物およびその使用方法
US6589195B1 (en) * 2000-05-26 2003-07-08 Orthomerica Products, Inc. Modular adjustable prophylactic hip orthosis and adduction/abduction joint
JP2004501913A (ja) * 2000-06-23 2004-01-22 ブリストル−マイヤーズ　スクイブ　ファーマ　カンパニー ヘテロアリール−フェニル置換Ｘａ因子阻害剤
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
WO2002064136A2 (en) * 2001-01-26 2002-08-22 Chugai Seiyaku Kabushiki Kaisha Malonyl-coa decarboxylase inhibitors useful as metabolic modulators
CA2445568A1 (en) 2001-04-27 2002-11-07 Vertex Pharmaceuticals Incorporated Triazole-derived kinase inhibitors and uses thereof
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
JP4357295B2 (ja) * 2001-08-03 2009-11-04 バーテックス ファーマシューティカルズ インコーポレイテッド ピラゾール誘導キナーゼインヒビターとその使用
MXPA04001088A (es) * 2001-08-03 2004-05-20 Vertex Pharma Derivados de pirazol como inhibidores de cinasa y uso de los mismos.
US6562816B2 (en) * 2001-08-24 2003-05-13 Pharmacia & Upjohn Company Substituted-heteroaryl-7-aza[2.2.1]bicycloheptanes for the treatment of disease
CA2458661A1 (en) * 2001-09-27 2003-04-03 Applied Research Systems Ars Holding N.V. Methods of increasing endogenous testosterone levels
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
EP2322521B1 (en) * 2002-02-06 2013-09-04 Vertex Pharmaceuticals, Inc. Heteroaryl compounds useful as inhibitors of 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
AU2003226149A1 (en) 2002-04-05 2003-10-27 Merck & Co., Inc. Substituted aryl amides
AU2003223012A1 (en) * 2002-04-26 2003-11-10 Pfizer Products Inc. Pyrimidine-2, 4, 6-trione metallo-proteinase inhibitors
EP1511988A4 (en) * 2002-06-05 2005-07-06 Pharmacia & Upjohn Co Llc METHOD OF IDENTIFYING LIGANDS USING 1H NMR COMPETITIVE BINDING EXPERIMENTS
GB0216224D0 (en) * 2002-07-12 2002-08-21 Glaxo Group Ltd Compounds
AU2003255724A1 (en) * 2002-08-02 2004-02-23 Argenta Discovery Limited Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors
US20040132726A1 (en) * 2002-08-09 2004-07-08 Astrazeneca Ab And Nps Pharmaceuticals, Inc. New compounds
AU2003265395A1 (en) 2002-08-14 2004-03-03 Ppd Discovery, 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
JP2006501243A (ja) 2002-08-23 2006-01-12 カイロン コーポレイション グリコーゲンシンターゼキナーゼ３のピロールベースのインヒビター
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
AU2003297925A1 (en) 2002-12-13 2004-07-09 Smithkline Beecham Corporation Thrombopoietin mimetics
AU2003297431A1 (en) * 2002-12-20 2004-07-22 Pharmacia Corporation Mitogen activated protein kinase-activated protein kinase-2 inhibiting compounds
CA2515235A1 (en) * 2003-02-10 2004-08-19 Bayer Healthcare Ag Bis(hetero)aryl carboxamide derivatives for use as pgi2 antagonists
EP1593667A4 (en) 2003-02-12 2009-03-04 Takeda Pharmaceutical Amine derivative
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
EP1599447A1 (en) * 2003-02-28 2005-11-30 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
WO2004094384A2 (en) * 2003-04-21 2004-11-04 Elan Pharmaceuticals, Inc. (hetero) arylamide 2-hydroxy-3-diaminoalkanes for use in the treatment of alzheimer’s disease
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
DE602004030689D1 (de) 2003-07-23 2011-02-03 Synta Pharmaceuticals Corp Verbindungen gegen entzündungen und immun-relevante verwendungen
WO2005019200A2 (en) 2003-08-14 2005-03-03 Icos Corporation Aryl piperidine derivatives as vla-1 integrin antagonists and uses thereof
EP1660487B1 (en) 2003-08-15 2008-03-19 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
EP1670466A4 (en) 2003-10-06 2007-04-25 Glaxo Group Ltd PREPARATION OF 1,6,7-TRISUBSTITUTED AZABENIC ZIMIDAZOLES AS KINASE-INHIBITORS
US20070123561A1 (en) * 2003-10-06 2007-05-31 Dennis Lee Preparation of 1,7-disubstituted azabensimidazoles as kinase inhibitors
JP2007512255A (ja) * 2003-11-13 2007-05-17 アンビット バイオサイエンシス コーポレーション キナーゼ調節因子としての尿素誘導体
RU2006121990A (ru) * 2003-11-21 2007-12-27 Эррэй Биофарма Инк. (Us) Ингибиторы протеинкиназ акт
EP1706159B1 (en) 2004-01-19 2013-06-26 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
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
AR047894A1 (es) 2004-02-25 2006-03-01 Wyeth Corp Derivados de tiofeno como inhibidores de la proteina tirosina fosfatasa 1b (ptpasa 1b); metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por ptpasa 1b
JP2007531354A (ja) * 2004-03-30 2007-11-01 松下電器産業株式会社 コンテンツ中継サーバ、コンテンツ中継システム、コンテンツ中継方法及びそのプログラム
US7470701B2 (en) * 2004-03-30 2008-12-30 Novartis Vaccines And Diagnostics, Inc. Substituted 2,5-heterocyclic derivatives
AU2005230847B2 (en) 2004-03-31 2012-11-08 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
CA2572058A1 (en) * 2004-06-30 2006-01-12 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
MX2007005765A (es) * 2004-11-23 2007-07-19 Wyeth Corp Antagonistas del receptor de la hormona que libera gonadotropina.
AU2005311311A1 (en) * 2004-11-30 2006-06-08 Neurosearch A/S Novel diazabicyclic aryl derivatives as cholinergy ligands
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
EP1874952A2 (en) 2005-04-11 2008-01-09 Achillion Pharmaceuticals, Inc. Pharmaceutical compositions for and methods of inhibiting hcv replication
EP1871770A1 (en) * 2005-04-22 2008-01-02 Kalypsys, Inc. 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
EP1933832A2 (en) * 2005-06-23 2008-06-25 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
AU2006261132A1 (en) * 2005-06-24 2006-12-28 Genelabs Technologies, Inc. Heteroaryl derivatives for treating viruses
CA2613517A1 (en) 2005-06-27 2007-01-04 Exelixis, Inc. Pyrazole based lxr modulators
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
CN101341124A (zh) 2005-12-14 2009-01-07 布里斯托尔-迈尔斯斯奎布公司 可用作丝氨酸蛋白酶抑制剂的6元杂环
EP1968568A4 (en) 2005-12-22 2011-04-13 Glaxosmithkline Llc HEMMER OF NUTS ACTIVITY
BRPI0620341A2 (pt) * 2005-12-23 2011-11-08 Smithkline Beecham Corparation azaindóis inibidores de cinases aurora
AR056882A1 (es) 2006-02-01 2007-10-31 Bayer Cropscience Sa Derivados del fungicida n- cicloalquil- bencil- amida
EP1989185B8 (en) 2006-02-28 2013-06-26 Dart NeuroScience LLC Therapeutic compounds
JP2007277230A (ja) 2006-03-15 2007-10-25 Tanabe Seiyaku Co Ltd 医薬組成物
US9562019B2 (en) 2006-12-21 2017-02-07 Sloan-Kettering Institute For Cancer Research Substituted pyridazines as EGFR and/or KRAS inhibitors
CN101611008A (zh) 2006-12-22 2009-12-23 恩希赛弗制药公司 C3a受体调节剂及其使用方法
UY30892A1 (es) 2007-02-07 2008-09-02 Smithkline Beckman Corp Inhibidores de la actividad akt
JP5363997B2 (ja) 2007-02-07 2013-12-11 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 Ａｋｔ活性の阻害剤
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

Also Published As

Publication number Publication date
UY30892A1 (es) 2008-09-02
JO3134B1 (ar) 2017-09-20
AU2008213694A1 (en) 2008-08-14
KR20140140570A (ko) 2014-12-09
PT2117523E (pt) 2014-09-29
EP2117523B1 (en) 2014-06-25
ZA200905363B (en) 2010-05-26
IL200212A0 (en) 2010-04-29
KR101537825B1 (ko) 2015-07-22
PL2117523T3 (pl) 2014-11-28
US20160287561A1 (en) 2016-10-06
KR101521002B1 (ko) 2015-05-19
CR10995A (es) 2009-10-16
JP2011126896A (ja) 2011-06-30
CY1115535T1 (el) 2017-01-04
BRPI0807146A2 (pt) 2014-04-15
EA018038B1 (ru) 2013-05-30
SI2117523T1 (sl) 2014-10-30
WO2008098104A8 (en) 2009-07-30
TWI507194B (zh) 2015-11-11
UA102992C2 (en) 2013-09-10
AR066184A1 (es) 2009-08-05
US20150152092A1 (en) 2015-06-04
CN101646427A (zh) 2010-02-10
MA31167B1 (fr) 2010-02-01
AU2008213694B2 (en) 2013-07-04
US20110071182A1 (en) 2011-03-24
WO2008098104A1 (en) 2008-08-14
US20100267759A1 (en) 2010-10-21
DK2117523T3 (da) 2014-09-08
US20130231378A1 (en) 2013-09-05
MY164480A (en) 2017-12-29
US8410158B2 (en) 2013-04-02
BRPI0807146B1 (pt) 2020-05-26
MX367398B (es) 2019-08-20
ES2501518T3 (es) 2014-10-02
KR20090110866A (ko) 2009-10-22
US8273782B2 (en) 2012-09-25
SG193678A1 (en) 2013-10-30
EP2117523A4 (en) 2011-05-25
TWI381836B (zh) 2013-01-11
KR20120130298A (ko) 2012-11-30
EA200970738A1 (ru) 2010-06-30
US8946278B2 (en) 2015-02-03
BRPI0807146B8 (pt) 2021-05-25
CO6220930A2 (es) 2010-11-19
TW201130490A (en) 2011-09-16
PE20090058A1 (es) 2009-04-03
JP5010038B2 (ja) 2012-08-29
US20100041726A1 (en) 2010-02-18
US20090209607A1 (en) 2009-08-20
TW200845964A (en) 2008-12-01
JP2012167096A (ja) 2012-09-06
NZ579177A (en) 2012-01-12
DOP2009000196A (es) 2009-10-31
IL200212A (en) 2015-07-30
AU2008213694A2 (en) 2010-06-24
CL2008000348A1 (es) 2008-08-18
CA2678255A1 (en) 2008-08-14
CN101646427B (zh) 2013-06-12
JP5511879B2 (ja) 2014-06-04
EP2117523A1 (en) 2009-11-18
JP4723677B2 (ja) 2011-07-13
JP2010518110A (ja) 2010-05-27
CA2678255C (en) 2014-06-03
MX2009008550A (es) 2009-11-09
HK1132676A1 (en) 2010-03-05

Similar Documents

Publication Publication Date Title
HRP20140790T1 (hr) Inhibitori aktivnosti akt
JP2010518110A5 (en:Method)
JP2011126896A5 (en:Method)
ME02663B (me) Derivati benzimidazola kao inhibitori pi3 kinaze
JP2012516344A5 (en:Method)
CN103857657B (zh) 杂环衍生物及医药
HRP20131051T1 (hr) Inhibitori proteinskih kinaza
JP5746185B2 (ja) 三置換１ｈ−ピロール類と、芳香族スペーサーおよびヘテロ芳香族スペーサーとに同時に基づく新規ヒストンデアセチラーゼ阻害剤
HRP20170634T4 (hr) Kristalni oblik od 4-metil-n-[3-(4-metil-imidazol-1-il)-5-trifluorometil-fenil]-3-(4-piridin-3-il-pirimidin-2-ilamino)-benzamida
JP2010528026A5 (en:Method)
JP2007502821A (ja) Ｎ−置換ベンズイミダゾリルｃ−Ｋｉｔ阻害剤
MXPA06003435A (es) Benzazoles substituidos y uso de los mismos como inhibidores de la cinasa raf.
HRP20210447T1 (hr) Piridinski spoj
JP2010522770A5 (en:Method)
JP2020536863A5 (en:Method)
HRP20211406T1 (hr) Biciklični heterociklični spojevi i njihove uporabe u liječenju
RU2009122242A (ru) Кристаллические формы сольватированного илапразола
JP2017530185A5 (en:Method)
WO2013129622A1 (ja) 複素環化合物およびその用途
MY160394A (en) Novel phenol derivative
HRP20141034T1 (hr) Spojevi koji sadrže (s)-2-amino-1-(4-klorofenil)-1-[4-(1h-pirazol-4-il)-fenil]-etanol kao modulator proteinskih kinaza
CN107001271B (zh) 羟基脒类衍生物、其制备方法及其在医药上的应用
CA2944959A1 (en) Substituted nitrogen-containing heterocyclic derivatives, pharmaceutical compositions comprising the same and applications of antitumor thereof
HRP20140246T1 (hr) DERIVATI PIRIDO[2,3-d]PIRIMIDINA, POSTUPAK NJIHOVOG DOBIVANJA I NJIHOVA UPOTREBA U TERAPIJI
JP2016537326A5 (en:Method)