TWI657085B - 雜環化合物及其用途 - Google Patents

雜環化合物及其用途 Download PDF

Info

Publication number
TWI657085B
TWI657085B TW103134648A TW103134648A TWI657085B TW I657085 B TWI657085 B TW I657085B TW 103134648 A TW103134648 A TW 103134648A TW 103134648 A TW103134648 A TW 103134648A TW I657085 B TWI657085 B TW I657085B
Authority
TW
Taiwan
Prior art keywords
alkyl
compound
cancer
heteroaryl
group
Prior art date
Application number
TW103134648A
Other languages
English (en)
Chinese (zh)
Other versions
TW201605829A (zh
Inventor
阿福多Ｃ 卡司頭
凱瑟林納Ａ 伊凡絲
蘇麻拉安傑爾 傑納丹安奈爾
安德 麗絲卡爾畢
陶 盧
馬丁Ｒ 亭博利
Original Assignee
英菲尼提製藥股份有限公司
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
Application filed by 英菲尼提製藥股份有限公司 filed Critical 英菲尼提製藥股份有限公司
Publication of TW201605829A publication Critical patent/TW201605829A/zh
Application granted granted Critical
Publication of TWI657085B publication Critical patent/TWI657085B/zh

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
    • A61K31/435—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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine 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
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • C07D403/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Transplantation (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW103134648A 2013-10-04 2014-10-03 雜環化合物及其用途 TWI657085B (zh)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US201361887259P 2013-10-04 2013-10-04
US61/887,259 2013-10-04
US201361888958P 2013-10-09 2013-10-09
US61/888,958 2013-10-09
US201461938026P 2014-02-10 2014-02-10
US61/938,026 2014-02-10

Publications (2)

Publication Number Publication Date
TW201605829A TW201605829A (zh) 2016-02-16
TWI657085B true TWI657085B (zh) 2019-04-21

Family

ID=51743565

Family Applications (1)

Application Number Title Priority Date Filing Date
TW103134648A TWI657085B (zh) 2013-10-04 2014-10-03 雜環化合物及其用途

Country Status (27)

Country Link
US (6) US9359365B2 (https=)
EP (2) EP3052485B1 (https=)
JP (1) JP6466924B2 (https=)
KR (1) KR102365651B1 (https=)
CN (1) CN105793255B (https=)
AU (1) AU2014329392B2 (https=)
BR (1) BR112016007467B1 (https=)
CA (1) CA2925944C (https=)
CL (1) CL2016000783A1 (https=)
CY (1) CY1124998T1 (https=)
DK (1) DK3052485T3 (https=)
EA (1) EA201690713A1 (https=)
ES (1) ES2900806T3 (https=)
HU (1) HUE057734T2 (https=)
IL (1) IL244818B (https=)
MX (2) MX2021012208A (https=)
MY (1) MY175778A (https=)
NZ (1) NZ718430A (https=)
PE (1) PE20160685A1 (https=)
PH (1) PH12016500582B1 (https=)
PL (1) PL3052485T3 (https=)
PT (1) PT3052485T (https=)
SG (2) SG10201902074UA (https=)
TW (1) TWI657085B (https=)
UA (1) UA121104C2 (https=)
WO (1) WO2015051244A1 (https=)
ZA (1) ZA201602220B (https=)

Families Citing this family (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3219705B1 (en) 2005-12-28 2020-03-11 Vertex Pharmaceuticals Incorporated Pharmaceutical compositions of the amorphous form of n-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
KR20140075693A (ko) 2011-08-29 2014-06-19 인피니티 파마슈티칼스, 인코포레이티드 헤테로사이클릭 화합물 및 그의 용도
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
MX2021012208A (es) * 2013-10-04 2023-01-19 Infinity Pharmaceuticals Inc Compuestos heterocíclicos y usos de los mismos.
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
NZ724368A (en) * 2014-03-19 2023-07-28 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN107250113B (zh) 2014-10-07 2019-03-29 弗特克斯药品有限公司 囊性纤维化跨膜传导调节蛋白的调节剂的共晶
EP4585268A3 (en) 2015-09-14 2025-10-15 Twelve Therapeutics, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
CN110730819A (zh) 2016-10-26 2020-01-24 索尼克马斯特有限公司 肌肉谱系细胞的改善产生及其治疗用途
CN108017641B (zh) * 2016-11-02 2021-01-05 深圳铂立健医药有限公司 吡唑并嘧啶化合物作为pi3k抑制剂及其应用
CN106769807A (zh) * 2016-12-07 2017-05-31 王兰英 一种利用流式细胞仪检测HeLa细胞凋亡的方法
IL315310A (en) 2017-12-26 2024-10-01 Kymera Therapeutics Inc Irak degraders and uses thereof
WO2019140380A1 (en) 2018-01-12 2019-07-18 Kymera Therapeutics, Inc. Protein degraders and uses thereof
AU2019209960B2 (en) 2018-01-20 2023-11-23 Sunshine Lake Pharma Co., Ltd. Substituted aminopyrimidine compounds and methods of use
CN112292374B (zh) * 2018-05-31 2023-01-03 信达生物制药(苏州)有限公司 一种新型磷酸肌醇3-激酶抑制剂及其制备方法和用途
WO2020010227A1 (en) 2018-07-06 2020-01-09 Kymera Therapeutics, Inc. Protein degraders and uses thereof
JP7623943B2 (ja) 2018-11-30 2025-01-29 カイメラ セラピューティクス， インコーポレイテッド Ｉｒａｋ分解剤およびそれらの使用
CN113195492B (zh) * 2018-12-12 2022-07-08 信达生物制药(苏州)有限公司 一种新颖的三并环结构化合物及其制备方法和用途
CN110025621A (zh) * 2019-03-13 2019-07-19 中国农业科学院上海兽医研究所(中国动物卫生与流行病学中心上海分中心) 替唑尼特和硝唑尼特在制备抗炎药物中的应用
KR20220047247A (ko) * 2019-06-04 2022-04-15 아르커스 바이오사이언시즈 인코포레이티드 2,3,5-삼치환 피라졸로[1,5-a]피리미딘 화합물
WO2020264490A1 (en) * 2019-06-28 2020-12-30 Kymera Therapeutics, Inc. Irak degraders and uses thereof
BR112021026517A2 (pt) 2019-06-28 2022-05-10 Kymera Therapeutics Inc Degradadores de irak e usos dos mesmos
CN112194659A (zh) * 2019-07-08 2021-01-08 浙江海正药业股份有限公司 炔类衍生物及其制备方法和用途
WO2021011868A1 (en) 2019-07-17 2021-01-21 Kymera Therapeutics, Inc. Irak degraders and uses thereof
JP2022545467A (ja) 2019-08-22 2022-10-27 ジュノー セラピューティクス インコーポレイテッド Ｔ細胞療法とｚｅｓｔｅホモログ２エンハンサー（ＥＺＨ２）阻害剤との併用療法および関連方法
CN110627827B (zh) * 2019-09-11 2022-11-08 杭州澳赛诺生物科技有限公司 4-乙炔基-四氢吡喃或4-乙炔基哌啶的合成方法
US12551564B2 (en) 2019-12-10 2026-02-17 Kymera Therapeutics, Inc. IRAK degraders and uses thereof
WO2021127190A1 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
WO2021127283A2 (en) 2019-12-17 2021-06-24 Kymera Therapeutics, Inc. Irak degraders and uses thereof
TW202210483A (zh) 2020-06-03 2022-03-16 美商凱麥拉醫療公司 Irak降解劑之結晶型
US12383547B2 (en) 2020-07-01 2025-08-12 Vanderbilt University Methods of treatment for a kidney disease
EP4259149A1 (en) 2020-12-08 2023-10-18 Infinity Pharmaceuticals, Inc. Eganelisib for use in the treatment of pd-l1 negative cancer
PH12023500015A1 (en) 2020-12-30 2024-03-11 Kymera Therapeutics Inc Irak degraders and uses thereof
CN116867494A (zh) 2021-02-15 2023-10-10 凯麦拉医疗公司 Irak4降解剂和其用途
WO2022174268A1 (en) 2021-02-15 2022-08-18 Kymera Therapeutics, Inc. Irak4 degraders and uses thereof
WO2022212890A1 (en) * 2021-04-02 2022-10-06 Endpoint Health Inc. Companion diagnostic and therapies for dysregulated host response
KR20220138655A (ko) * 2021-04-06 2022-10-13 주식회사 온코크로스 신장 질환의 예방 또는 치료용 화합물
WO2022226052A1 (en) * 2021-04-20 2022-10-27 The Regents Of The University Of Michigan Pi3k inhibitors, nanoformulations, and uses thereof
WO2023051495A1 (zh) * 2021-09-28 2023-04-06 中山医诺维申新药研发有限公司 异喹啉酮类及喹唑啉酮类化合物及其组合物和用途
US12187744B2 (en) 2021-10-29 2025-01-07 Kymera Therapeutics, Inc. IRAK4 degraders and synthesis thereof
WO2023105119A1 (en) * 2021-12-07 2023-06-15 Sartar Therapeutics Oy Synergistic compositions for use in the treatment of cancer
EP4472967A4 (en) 2022-01-31 2026-04-15 Kymera Therapeutics Inc Iraqi Degradation Agents and Their Uses
CN117186072B (zh) * 2022-06-01 2026-03-27 安驰达生物医药技术(广州)有限公司 一种抑制磷脂酰肌醇-3-激酶γ亚型活性的化合物及其制备方法与应用
WO2025003769A2 (zh) * 2023-06-30 2025-01-02 杭州百新生物医药科技有限公司 芳杂环并吡咯烷酮类衍生物及其用途

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130029982A1 (en) * 2011-07-19 2013-01-31 Intellikine, Llc Heterocyclic compounds and uses thereof

Family Cites Families (777)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB812366A (en) 1955-08-18 1959-04-22 Wellcome Found Improvements in and relating to derivatives of pyrimidine and the preparation thereof
GB937725A (en) 1960-05-11 1963-09-25 Ciba Ltd Pyrazolo[3:4-d]pyrimidines
US3536809A (en) 1969-02-17 1970-10-27 Alza Corp Medication method
US3598123A (en) 1969-04-01 1971-08-10 Alza Corp Bandage for administering drugs
DE2139107A1 (de) 1971-08-04 1973-02-15 Merck Patent Gmbh Heterocyclisch substituierte adenosinverbindungen
US3845770A (en) 1972-06-05 1974-11-05 Alza Corp Osmatic dispensing device for releasing beneficial agent
US3916899A (en) 1973-04-25 1975-11-04 Alza Corp Osmotic dispensing device with maximum and minimum sizes for the passageway
US4008719A (en) 1976-02-02 1977-02-22 Alza Corporation Osmotic system having laminar arrangement for programming delivery of active agent
JPS5569437U (https=) 1978-11-06 1980-05-13
US4270537A (en) 1979-11-19 1981-06-02 Romaine Richard A Automatic hypodermic syringe
IT1153216B (it) 1981-10-16 1987-01-14 Schering Ag Procedimento per la preparazione di composti cianoeterociclici
DE3244594A1 (de) 1982-12-02 1984-06-07 Hoechst Ag, 6230 Frankfurt 1-phenylisochinolinderivate und verfahren zu ihrer herstellung, diese verbindung enthaltende pharmazeutische praeparate und deren anwendung
DE3406533A1 (de) 1984-02-23 1985-08-29 Boehringer Mannheim Gmbh, 6800 Mannheim Verwendung von adenosin-derivaten als antiallergica und arzneimittel, die diese enthalten
US5310731A (en) 1984-06-28 1994-05-10 Whitby Research, Inc. N-6 substituted-5'-(N-substitutedcarboxamido)adenosines as cardiac vasodilators and antihypertensive agents
HU196714B (en) 1984-10-04 1989-01-30 Monsanto Co Process for producing non-aqueous composition comprising somatotropin
US4795627A (en) 1984-10-18 1989-01-03 University Of Pittsburgh Tritium labelled N-mustard type compounds and a process for their production
IE58110B1 (en) 1984-10-30 1993-07-14 Elan Corp Plc Controlled release powder and process for its preparation
US4656159A (en) 1984-10-31 1987-04-07 Georgetown University Galactose-C-6 nitrogen mustard compounds and their uses
JPS61109797A (ja) 1984-11-01 1986-05-28 Yuki Gosei Yakuhin Kogyo Kk 標識化ヌクレオチドおよび標識化ポリヌクレオチド
US4596556A (en) 1985-03-25 1986-06-24 Bioject, Inc. Hypodermic injection apparatus
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US4886499A (en) 1986-12-18 1989-12-12 Hoffmann-La Roche Inc. Portable injection appliance
GB8704027D0 (en) 1987-02-20 1987-03-25 Owen Mumford Ltd Syringe needle combination
GB8707053D0 (en) 1987-03-25 1987-04-29 Ici Plc Anti-tumour agents
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4940460A (en) 1987-06-19 1990-07-10 Bioject, Inc. Patient-fillable and non-invasive hypodermic injection device assembly
US4790824A (en) 1987-06-19 1988-12-13 Bioject, Inc. Non-invasive hypodermic injection device
US4941880A (en) 1987-06-19 1990-07-17 Bioject, Inc. Pre-filled ampule and non-invasive hypodermic injection device assembly
US5339163A (en) 1988-03-16 1994-08-16 Canon Kabushiki Kaisha Automatic exposure control device using plural image plane detection areas
US5073543A (en) 1988-07-21 1991-12-17 G. D. Searle & Co. Controlled release formulations of trophic factors in ganglioside-lipsome vehicle
WO1990003370A1 (en) 1988-09-28 1990-04-05 Microprobe Corporation DERIVATIVES OF PYRAZOLO[3,4-d]PYRIMIDINE
FR2638359A1 (fr) 1988-11-03 1990-05-04 Tino Dalto Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau
GB8827305D0 (en) 1988-11-23 1988-12-29 British Bio Technology Compounds
IT1229203B (it) 1989-03-22 1991-07-25 Bioresearch Spa Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative.
PH30995A (en) 1989-07-07 1997-12-23 Novartis Inc Sustained release formulations of water soluble peptides.
US5442039A (en) 1989-07-17 1995-08-15 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5428125A (en) 1989-07-17 1995-06-27 The Dow Chemical Company Mesogenic polycyanates and thermosets thereof
US5721356A (en) 1989-09-15 1998-02-24 Gensia, Inc. Orally active adenosine kinase inhibitors
US5646128A (en) 1989-09-15 1997-07-08 Gensia, Inc. Methods for treating adenosine kinase related conditions
US5763597A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. Orally active adenosine kinase inhibitors
US5674998A (en) 1989-09-15 1997-10-07 Gensia Inc. C-4' modified adenosine kinase inhibitors
US5795977A (en) 1989-09-15 1998-08-18 Metabasis Therapeutics, Inc. Water soluble adenosine kinase inhibitors
US5763596A (en) 1989-09-15 1998-06-09 Metabasis Therapeutics, Inc. C-4' modified adenosine kinase inhibitors
US5120548A (en) 1989-11-07 1992-06-09 Merck & Co., Inc. Swelling modulated polymeric drug delivery device
US5064413A (en) 1989-11-09 1991-11-12 Bioject, Inc. Needleless hypodermic injection device
US5312335A (en) 1989-11-09 1994-05-17 Bioject Inc. Needleless hypodermic injection device
GB9009542D0 (en) 1990-04-27 1990-06-20 Beecham Group Plc Novel compounds
US5733566A (en) 1990-05-15 1998-03-31 Alkermes Controlled Therapeutics Inc. Ii Controlled release of antiparasitic agents in animals
GB9113137D0 (en) 1990-07-13 1991-08-07 Ici Plc Thioxo heterocycles
DE4026265A1 (de) 1990-08-20 1992-02-27 Boehringer Mannheim Gmbh Neue phospholipid-derivate von nucleosiden, deren herstellung sowie deren verwendung als antivirale arzneimittel
US5563257A (en) 1990-08-20 1996-10-08 Boehringer Mannheim Gmbh Phospholipid derivatives of nucleosides
US5190521A (en) 1990-08-22 1993-03-02 Tecnol Medical Products, Inc. Apparatus and method for raising a skin wheal and anesthetizing skin
SG80526A1 (en) 1990-09-25 2001-05-22 Rhone Poulenc Rorer Int Compounds having antihypertensive and anti- ischemic properies
US5652366A (en) 1990-09-25 1997-07-29 Rhone-Poulenc Rorer Pharmaceuticals Inc. DI (1R)-(-)camphosulfonic acid) salt, preparation thereof and use thereof
US5561134A (en) 1990-09-25 1996-10-01 Rhone-Poulenc Rorer Pharmaceuticals Inc. Compounds having antihypertensive, cardioprotective, anti-ischemic and antilipolytic properties
US5527288A (en) 1990-12-13 1996-06-18 Elan Medical Technologies Limited Intradermal drug delivery device and method for intradermal delivery of drugs
GB9103839D0 (en) 1991-02-23 1991-04-10 Smithkline Beecham Plc Pharmaceuticals
US5409930A (en) 1991-05-10 1995-04-25 Rhone-Poulenc Rorer Pharmaceuticals Inc. Bis mono- and bicyclic aryl and heteroaryl compounds which inhibit EGF and/or PDGF receptor tyrosine kinase
GB9118204D0 (en) 1991-08-23 1991-10-09 Weston Terence E Needle-less injector
SE9102652D0 (sv) 1991-09-13 1991-09-13 Kabi Pharmacia Ab Injection needle arrangement
US5272158A (en) 1991-10-29 1993-12-21 Merck & Co., Inc. Fibrinogen receptor antagonists
US5580578A (en) 1992-01-27 1996-12-03 Euro-Celtique, S.A. Controlled release formulations coated with aqueous dispersions of acrylic polymers
MX9300141A (es) 1992-01-13 1994-07-29 Smithkline Beecham Corp Compuestos de imidazol novedosos, procedimiento para su preparacion y composiciones farmaceuticas que lo contienen.
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
DE4204031A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue lipidphosphonsaeure-nucleosid-konjugate sowie deren verwendung als antivirale arzneimittel
DE4204032A1 (de) 1992-02-12 1993-08-19 Boehringer Mannheim Gmbh Neue liponucleotide, deren herstellunmg sowie deren verwendung als antivirale arzneimittel
JPH05239036A (ja) 1992-02-27 1993-09-17 Nissan Chem Ind Ltd 含窒素複素環化合物の製造方法
US5328483A (en) 1992-02-27 1994-07-12 Jacoby Richard M Intradermal injection device with medication and needle guard
WO1993018035A1 (en) 1992-03-04 1993-09-16 Abbott Laboratories Angiotensin ii receptor antagonists
JP2737518B2 (ja) 1992-03-16 1998-04-08 富士通株式会社 赤外線検知器の冷却構造
US5294612A (en) 1992-03-30 1994-03-15 Sterling Winthrop Inc. 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
EP1488805A2 (en) 1992-04-07 2004-12-22 The Regents of the University of Michigan CD28 pathway immunoregulation
GB9208135D0 (en) 1992-04-13 1992-05-27 Ludwig Inst Cancer Res Polypeptides having kinase activity,their preparation and use
JPH07506252A (ja) 1992-04-24 1995-07-13 エス・アール・アイ・インターナシヨナル 真核細胞内でのイン・ビボ相同配列ターゲッティング
DE69328440T3 (de) 1992-06-19 2009-05-07 Honeywell, Inc., Minneapolis Infrarot kamera mit thermoelektrischer temperaturstabilisierung
US5383851A (en) 1992-07-24 1995-01-24 Bioject Inc. Needleless hypodermic injection device
US6057305A (en) 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
US5569189A (en) 1992-09-28 1996-10-29 Equidyne Systems, Inc. hypodermic jet injector
US5334144A (en) 1992-10-30 1994-08-02 Becton, Dickinson And Company Single use disposable needleless injector
TW333456B (en) 1992-12-07 1998-06-11 Takeda Pharm Ind Co Ltd A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide.
TW370529B (en) 1992-12-17 1999-09-21 Pfizer Pyrazolopyrimidines
US5455258A (en) 1993-01-06 1995-10-03 Ciba-Geigy Corporation Arylsulfonamido-substituted hydroxamic acids
US5591767A (en) 1993-01-25 1997-01-07 Pharmetrix Corporation Liquid reservoir transdermal patch for the administration of ketorolac
IL108523A0 (en) 1993-02-03 1994-05-30 Gensia Inc Pharmaceutical compositions containing adenosine kinase inhibitors for preventing or treating conditions involving inflammatory responses and pain
EP0684953A4 (en) 1993-02-03 1999-12-22 Gensia Inc ADENOSINE KINASE INHIBITORS COMPRISING LYXOFURANOSYL DERIVATIVES.
GB9308957D0 (en) 1993-04-30 1993-06-16 Cancer Res Campaign Tech Novel produgs
EP0700430B1 (en) 1993-06-04 2005-04-20 The United States of America as Represented by the Secretary of the Navy Methods for selectively stimulating proliferation of t cells
US6087324A (en) 1993-06-24 2000-07-11 Takeda Chemical Industries, Ltd. Sustained-release preparation
EP0634402A1 (en) 1993-07-14 1995-01-18 Takeda Chemical Industries, Ltd. Isochinolinone derivatives, their production and use
US5504103A (en) 1993-08-25 1996-04-02 Eli Lilly And Company Inhibition of phosphatidylinositol 3-kinase with 17 β-hydroxywortmannin and analogs thereof
US5525503A (en) 1993-09-28 1996-06-11 Dana-Farber Cancer Institute, Inc. Signal transduction via CD28
DE4333761A1 (de) 1993-10-04 1995-04-06 Luitpold Pharma Gmbh Heterocyclische Carbamate, Verfahren zu ihrer Herstellung und Arzneimittel
WO1995012588A1 (en) 1993-11-05 1995-05-11 Biochem Pharma Inc. Antineoplastic heteronaphthoquinones
IL112249A (en) 1994-01-25 2001-11-25 Warner Lambert Co Pharmaceutical compositions containing di and tricyclic pyrimidine derivatives for inhibiting tyrosine kinases of the epidermal growth factor receptor family and some new such compounds
US5679683A (en) 1994-01-25 1997-10-21 Warner-Lambert Company Tricyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family
WO1995024176A1 (en) 1994-03-07 1995-09-14 Bioject, Inc. Ampule filling device
US5466220A (en) 1994-03-08 1995-11-14 Bioject, Inc. Drug vial mixing and transfer device
US6632789B1 (en) 1994-04-29 2003-10-14 The United States Of America As Represented By The Secretary Of The Navy Methods for modulating T cell responses by manipulating intracellular signal transduction
DE4418690A1 (de) 1994-05-28 1996-01-11 Boehringer Mannheim Gmbh Neue Lipidester von Nucleosid-Monophosphaten und deren Verwendung als immunsuppressive Arzneimittel
IT1270594B (it) 1994-07-07 1997-05-07 Recordati Chem Pharm Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida
US5756502A (en) 1994-08-08 1998-05-26 Warner-Lambert Company Quinazolinone derivatives as cholyecystokinin (CCK) ligands
US6323201B1 (en) 1994-12-29 2001-11-27 The Regents Of The University Of California Compounds for inhibition of ceramide-mediated signal transduction
US5599302A (en) 1995-01-09 1997-02-04 Medi-Ject Corporation Medical injection system and method, gas spring thereof and launching device using gas spring
US5863949A (en) 1995-03-08 1999-01-26 Pfizer Inc Arylsulfonylamino hydroxamic acid derivatives
ES2150113T3 (es) 1995-04-03 2000-11-16 Novartis Ag Derivados de pirazol y procedimientos para la preparacion de los mismos.
US6312894B1 (en) 1995-04-03 2001-11-06 Epoch Pharmaceuticals, Inc. Hybridization and mismatch discrimination using oligonucleotides conjugated to minor groove binders
DK0821671T3 (da) 1995-04-20 2001-04-23 Pfizer Arylsulfonylhydroxamsyrederivater som MMP- og TNF-inhibitorer
US5977061A (en) 1995-04-21 1999-11-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic N6 - substituted nucleotide analagues and their use
JPH08295667A (ja) 1995-04-27 1996-11-12 Takeda Chem Ind Ltd 複素環化合物、その製造法および剤
WO1996037777A1 (en) 1995-05-23 1996-11-28 Nelson Randall W Mass spectrometric immunoassay
US5593997A (en) 1995-05-23 1997-01-14 Pfizer Inc. 4-aminopyrazolo(3-,4-D)pyrimidine and 4-aminopyrazolo-(3,4-D)pyridine tyrosine kinase inhibitors
US5730723A (en) 1995-10-10 1998-03-24 Visionary Medical Products Corporation, Inc. Gas pressured needle-less injection device and method
US6403599B1 (en) 1995-11-08 2002-06-11 Pfizer Inc Corticotropin releasing factor antagonists
WO1996040258A2 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Spironolactone and angiotensin ii antagonist combination therapy for treatment of congestive heart failure
WO1996040256A1 (en) 1995-06-07 1996-12-19 G.D. Searle & Co. Method to treat cardiofibrosis with a combination of an angiotensin ii antagonist and spironolactone
US5665721A (en) 1995-06-07 1997-09-09 Abbott Laboratories Heterocyclic substituted cyclopentane compounds
DK0831910T3 (da) 1995-06-07 2002-05-21 Searle & Co Kombinationsterapi med epoxy-steroid aldosteronantagonist og angiotensin II-receptorantagonist til behandling af kongestivt hjertesvigt
AU6242096A (en) 1995-06-27 1997-01-30 Takeda Chemical Industries Ltd. Method of producing sustained-release preparation
TW448055B (en) 1995-09-04 2001-08-01 Takeda Chemical Industries Ltd Method of production of sustained-release preparation
AU4858596A (en) 1995-09-15 1997-04-01 Torrey Pines Institute For Molecular Studies Synthesis of quinazolinone libraries
JP2909418B2 (ja) 1995-09-18 1999-06-23 株式会社資生堂 薬物の遅延放出型マイクロスフイア
US5763885A (en) 1995-12-19 1998-06-09 Loral Infrared & Imaging Systems, Inc. Method and apparatus for thermal gradient stabilization of microbolometer focal plane arrays
JPH09143163A (ja) 1995-11-29 1997-06-03 Fuji Photo Film Co Ltd 含窒素ヘテロ芳香族アミド類の製造方法
DE69624081T2 (de) 1995-12-20 2003-06-12 Agouron Pharmaceuticals, Inc. Matrix-metalloprotease Inhibitoren
US5893397A (en) 1996-01-12 1999-04-13 Bioject Inc. Medication vial/syringe liquid-transfer apparatus
US5980945A (en) 1996-01-16 1999-11-09 Societe De Conseils De Recherches Et D'applications Scientifique S.A. Sustained release drug formulations
US5747235A (en) 1996-01-26 1998-05-05 Eastman Kodak Company Silver halide light sensitive emulsion layer having enhanced photographic sensitivity
CH690773A5 (de) 1996-02-01 2001-01-15 Novartis Ag Pyrrolo(2,3-d)pyrimide und ihre Verwendung.
DE19603576A1 (de) 1996-02-01 1997-08-07 Bayer Ag Acylierte 4-Amino und 4-Hydrazinopyrimidine
US5763608A (en) 1996-02-05 1998-06-09 Hoechst Celanese Corporation Process for preparing pyrimidine derivatives
GB2310952B (en) 1996-03-05 1998-08-19 Mitsubishi Electric Corp Infrared detector
US5872136A (en) 1996-04-03 1999-02-16 Merck & Co., Inc. Arylheteroaryl inhibitors of farnesyl-protein transferase
AU706150B2 (en) 1996-04-03 1999-06-10 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
GB9607549D0 (en) 1996-04-11 1996-06-12 Weston Medical Ltd Spring-powered dispensing device
GB9611460D0 (en) 1996-06-01 1996-08-07 Ludwig Inst Cancer Res Novel lipid kinase
HUP9904567A3 (en) 1996-06-20 2001-10-29 Univ Texas Use of azo, thioalkyl, thiocarbonyl derivatives substituted by fused heterocycles and/or phenyl group for the preparation of pharmaceutical compositions stimulating bone growth
US6264970B1 (en) 1996-06-26 2001-07-24 Takeda Chemical Industries, Ltd. Sustained-release preparation
JP3195756B2 (ja) 1996-07-04 2001-08-06 公子 吉水 潤滑補助体
FR2750862B1 (fr) 1996-07-12 1998-10-16 Dupin Jean Pierre Utilisation d'heterocycles diazotes fusionnes avec un systeme aromatique ou heteroaromatique pour le traitement des maladies thrombo-emboliques
EP0923585B1 (en) 1996-07-18 2002-05-08 Pfizer Inc. Phosphinate based inhibitors of matrix metalloproteases
WO1998007697A1 (en) 1996-08-23 1998-02-26 Pfizer Inc. Arylsulfonylamino hydroxamic acid derivatives
US6419961B1 (en) 1996-08-29 2002-07-16 Takeda Chemical Industries, Ltd. Sustained release microcapsules of a bioactive substance and a biodegradable polymer
CA2217134A1 (en) 1996-10-09 1998-04-09 Sumitomo Pharmaceuticals Co., Ltd. Sustained release formulation
US5922753A (en) 1996-10-23 1999-07-13 Zymogenetics, Inc. Methods for treating bone deficit conditions with benzothiazole
US5948776A (en) 1996-10-23 1999-09-07 Zymogenetic, Inc. Compositions and methods for treating bone deficit conditions
US5965573A (en) 1996-10-23 1999-10-12 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5990169A (en) 1996-10-23 1999-11-23 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6153631A (en) 1996-10-23 2000-11-28 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5994358A (en) 1996-10-23 1999-11-30 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6342514B1 (en) 1996-10-23 2002-01-29 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US5919808A (en) 1996-10-23 1999-07-06 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
US6251901B1 (en) 1996-10-23 2001-06-26 Zymogenetics, Inc. Compositions and methods for treating bone deficit conditions
DE69730093T2 (de) 1996-10-31 2006-07-20 Takeda Pharmaceutical Co. Ltd. Zubereitung mit verzögerter Freisetzung
US5858753A (en) 1996-11-25 1999-01-12 Icos Corporation Lipid kinase
US5977134A (en) 1996-12-05 1999-11-02 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
EP0942925B1 (en) 1996-12-06 2006-11-22 Vertex Pharmaceuticals Incorporated Inhibitors of interleukin-1 beta converting enzyme
WO1998027980A2 (en) 1996-12-20 1998-07-02 Takeda Chemical Industries, Ltd. Method of producing a sustained-release preparation
US6093737A (en) 1996-12-30 2000-07-25 Merck & Co., Inc. Inhibitors of farnesyl-protein transferase
WO1998030566A1 (en) 1997-01-06 1998-07-16 Pfizer Inc. Cyclic sulfone derivatives
JPH10206995A (ja) 1997-01-21 1998-08-07 Konica Corp ハロゲン化銀写真感光材料
US5891474A (en) 1997-01-29 1999-04-06 Poli Industria Chimica, S.P.A. Time-specific controlled release dosage formulations and method of preparing same
EP0977733B1 (en) 1997-02-03 2003-09-03 Pfizer Products Inc. Arylsulfonylamino hydroxamic acid derivatives
AU755062B2 (en) 1997-02-07 2002-12-05 Princeton University Engineered protein kinases which can utilize modified nucleotide triphosphate substrates
JP2000507975A (ja) 1997-02-07 2000-06-27 ファイザー・インク Ｎ−ヒドロキシ−β−スルホニルプロピオンアミド誘導体類及びそれらのマトリックスメタロプロテイナーゼ阻害薬としての使用
EA002546B1 (ru) 1997-02-11 2002-06-27 Пфайзер Инк. Производные арилсульфонилгидроксамовой кислоты
DK0970084T3 (da) 1997-03-19 2003-09-29 Abbott Gmbh & Co Kg Pyrrolo[2,3-d]pyrimidiner og deres anvendelse som inhibitorer for tyrosinkinase
US7863444B2 (en) 1997-03-19 2011-01-04 Abbott Laboratories 4-aminopyrrolopyrimidines as kinase inhibitors
US5993412A (en) 1997-05-19 1999-11-30 Bioject, Inc. Injection apparatus
AU7449598A (en) 1997-05-23 1998-12-11 Nippon Shinyaku Co. Ltd. Medicinal composition for prevention or treatment of hepatopathy
US6207679B1 (en) 1997-06-19 2001-03-27 Sepracor, Inc. Antimicrobial agents uses and compositions related thereto
EP1015429B1 (en) 1997-09-09 2004-05-12 Bristol-Myers Squibb Pharma Company Benzimidazolinones, benzoxazolinones, benzopiperazinones, indanones, and derivatives thereof as inhibitors of factor xa
ATE404539T1 (de) 1997-10-02 2008-08-15 Eisai R&D Man Co Ltd Kondensierte pyridinderivate
US6649631B1 (en) 1997-10-23 2003-11-18 The Board Of Regents Of The University Of Texas System Compositions and methods for treating bone deficit conditions
US6040321A (en) 1997-11-12 2000-03-21 Bristol-Myers Squibb Company Aminothiazole inhibitors of cyclin dependent kinases
WO1999024432A1 (fr) 1997-11-12 1999-05-20 Mitsubishi Chemical Corporation Derives de purine et medicament les renfermant en tant qu'ingredient actif
GB9725782D0 (en) 1997-12-05 1998-02-04 Pfizer Ltd Therapeutic agents
US6184377B1 (en) 1997-12-15 2001-02-06 Sepracor Inc. Compositions containing N-amino- and N-hydroxy-quinazolinones and methods for preparing libraries thereof
IT1298087B1 (it) 1998-01-08 1999-12-20 Fiderm S R L Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni
US6191170B1 (en) 1998-01-13 2001-02-20 Tularik Inc. Benzenesulfonamides and benzamides as therapeutic agents
GB9801690D0 (en) 1998-01-27 1998-03-25 Pfizer Ltd Therapeutic agents
US6613358B2 (en) 1998-03-18 2003-09-02 Theodore W. Randolph Sustained-release composition including amorphous polymer
EP0945441A3 (de) 1998-03-27 2002-07-17 Degussa AG Verfahren zur Herstellung von cyclischen 4-Oxoamidinen
US7715989B2 (en) 1998-04-03 2010-05-11 Elitech Holding B.V. Systems and methods for predicting oligonucleotide melting temperature (TmS)
US6127121A (en) 1998-04-03 2000-10-03 Epoch Pharmaceuticals, Inc. Oligonucleotides containing pyrazolo[3,4-D]pyrimidines for hybridization and mismatch discrimination
US6432970B2 (en) 1998-04-09 2002-08-13 Johns Hopkins University School Of Medicine Inhibitors of hedgehog signaling pathways, compositions and uses related thereto
PA8469401A1 (es) 1998-04-10 2000-05-24 Pfizer Prod Inc Derivados biciclicos del acido hidroxamico
PA8469501A1 (es) 1998-04-10 2000-09-29 Pfizer Prod Inc Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico
KR19990085365A (ko) 1998-05-16 1999-12-06 허영섭 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법
JP2000072773A (ja) 1998-08-28 2000-03-07 Zeria Pharmaceut Co Ltd プリン誘導体
CA2344262A1 (en) 1998-09-18 2000-03-30 Basf Aktiengesellschaft 4-aminopyrrolopyrimidines as kinase inhibitors
BR9916371A (pt) 1998-12-19 2001-09-18 Janssen Pharmaceutica Nv Composto de espiro anti-histamìnico
DK1140938T3 (da) 1999-01-11 2003-12-22 Univ Princeton Højaffinitetsinhibitorer for målvalidering og anvendelser heraf
CZ27399A3 (cs) 1999-01-26 2000-08-16 Ústav Experimentální Botaniky Av Čr Substituované dusíkaté heterocyklické deriváty, způsob jejich přípravy, tyto deriváty pro použití jako léčiva, farmaceutická kompozice a kombinovaný farmaceutický přípravek tyto deriváty obsahující a použití těchto derivátů pro výrobu léčiv
US6248363B1 (en) 1999-11-23 2001-06-19 Lipocine, Inc. Solid carriers for improved delivery of active ingredients in pharmaceutical compositions
US6596497B1 (en) 1999-03-17 2003-07-22 New York Blood Center, Inc. Screening of antiviral compounds targeted to the HIV-1 gp41 core structure
EP1040831A3 (en) 1999-04-02 2003-05-02 Pfizer Products Inc. Use of corticotropin releasing factor (CRF) antagonists to prevent sudden death
SE515856C2 (sv) 1999-05-19 2001-10-22 Ericsson Telefon Ab L M Bärare för elektronikkomponenter
JP2003501429A (ja) 1999-06-03 2003-01-14 クノール・ゲー・エム・ベー・ハー ベンゾチアジノンおよびベンゾオキサジノン化合物
US6387894B1 (en) 1999-06-11 2002-05-14 Pfizer Inc. Use of CRF antagonists and renin-angiotensin system inhibitors
TWI262914B (en) 1999-07-02 2006-10-01 Agouron Pharma Compounds and pharmaceutical compositions for inhibiting protein kinases
PE20010306A1 (es) 1999-07-02 2001-03-29 Agouron Pharma Compuestos de indazol y composiciones farmaceuticas que los contienen utiles para la inhibicion de proteina kinasa
GB9919588D0 (en) 1999-08-18 1999-10-20 Hoechst Schering Agrevo Gmbh Fungicidal compounds
DE19940859A1 (de) 1999-08-27 2001-03-01 Bayer Ag Selektive Herbizide auf Basis eines substituierten Phenylsulfonylaminocarbonyltriazolinons und Safenern
JP4831906B2 (ja) 1999-08-27 2011-12-07 ケモセントリックス， インコーポレイテッド Ｃｘｃｒ３機能を調節するための複素環式化合物および方法
DE19940860A1 (de) 1999-08-27 2001-03-01 Bayer Ag Selektive Herbizide auf Basis eines substituierten Phenylsulfonyl aminocarbonyltriazolinons und Safenern II
US20070021493A1 (en) 1999-09-16 2007-01-25 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
AU780846B2 (en) 1999-09-16 2005-04-21 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US20050080138A1 (en) 1999-09-16 2005-04-14 Curis, Inc. Mediators of hedgehog signaling pathways, compositions and uses related thereto
US6921763B2 (en) 1999-09-17 2005-07-26 Abbott Laboratories Pyrazolopyrimidines as therapeutic agents
CA2385747A1 (en) 1999-09-17 2001-03-22 Gavin C. Hirst Pyrazolopyrimidines as therapeutic agents
US6506769B2 (en) 1999-10-06 2003-01-14 Boehringer Ingelheim Pharmaceuticals, Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
EP1222187B1 (en) 1999-10-06 2004-09-22 Boehringer Ingelheim Pharmaceuticals Inc. Heterocyclic compounds useful as inhibitors of tyrosine kinases
CA2386190C (en) 1999-10-13 2009-04-14 Johns Hopkins University School Of Medicine Regulators of the hedgehog pathway, compositions and uses related thereto
CA2388468C (en) 1999-10-14 2011-01-25 Curis, Inc. Mediators of hedgehog signalling pathways, compositions and uses related thereto
US6472153B1 (en) 1999-10-26 2002-10-29 Epoch Biosciences, Inc. Hybridization-triggered fluorescent detection of nucleic acids
US6545004B1 (en) 1999-10-27 2003-04-08 Cytokinetics, Inc. Methods and compositions utilizing quinazolinones
US7671200B2 (en) 1999-10-27 2010-03-02 Cytokinetics, Inc. Quinazolinone KSP inhibitors
US7230000B1 (en) 1999-10-27 2007-06-12 Cytokinetics, Incorporated Methods and compositions utilizing quinazolinones
US6660845B1 (en) 1999-11-23 2003-12-09 Epoch Biosciences, Inc. Non-aggregating, non-quenching oligomers comprising nucleotide analogues; methods of synthesis and use thereof
IL133809A0 (en) 1999-12-30 2001-04-30 Yeda Res & Dev Steroidal alkaloids and pharmaceutical compositions comprising them
GB0002032D0 (en) 2000-01-28 2000-03-22 Zeneca Ltd Chemical compounds
US7217722B2 (en) 2000-02-01 2007-05-15 Kirin Beer Kabushiki Kaisha Nitrogen-containing compounds having kinase inhibitory activity and drugs containing the same
JP2001250689A (ja) 2000-03-07 2001-09-14 Toray Ind Inc 発光素子
WO2001072712A1 (en) 2000-03-24 2001-10-04 Cor Therapeutics, Inc. ISOQUINOLONE INHIBITORS OF FACTOR Xa
US6683108B1 (en) 2000-03-30 2004-01-27 Curis, Inc. Agonists of hedgehog signaling pathways and uses related thereto
US20050070578A1 (en) 2000-03-30 2005-03-31 Baxter Anthony David Small organic molecule regulators of cell proliferation
US6683192B2 (en) 2000-03-30 2004-01-27 Curis, Inc. Small organic molecule regulators of cell proliferation
CA2404413C (en) 2000-03-30 2015-10-20 Curis, Inc. Small organic molecule regulators of cell proliferation
US6613798B1 (en) 2000-03-30 2003-09-02 Curis, Inc. Small organic molecule regulators of cell proliferation
US7115653B2 (en) 2000-03-30 2006-10-03 Curis, Inc. Small organic molecule regulators of cell proliferation
US20020127625A1 (en) 2000-03-31 2002-09-12 Forskarpatent Is Syd Ab Methods of diagnosing immune related diseases
ES2788383T3 (es) 2000-04-25 2020-10-21 Icos Corp Inhibidores de delta fosfatidilo-inositol 3-quinasa humana
US6667300B2 (en) 2000-04-25 2003-12-23 Icos Corporation Inhibitors of human phosphatidylinositol 3-kinase delta
US6777439B2 (en) 2000-05-30 2004-08-17 Advanced Research & Technology Institute, Inc. Compositions and methods for identifying agents which modulate PTEN function and PI-3 kinase pathways
NZ522839A (en) 2000-06-27 2004-11-26 Genelabs Tech Inc Novel compounds possessing antibacterial, antifungal or antitumor activity
US6534691B2 (en) 2000-07-18 2003-03-18 E. I. Du Pont De Nemours And Company Manufacturing process for α-olefins
EP1322619B1 (en) 2000-09-20 2008-01-23 Merck & Co., Inc. Isoquinolinone potassium channel inhibitors
EP1578341A2 (en) 2000-10-11 2005-09-28 Tularik Inc. Modulation of ccr4 function
AU1312502A (en) 2000-10-11 2002-04-22 Pe Corp Ny Fluorescent nucleobase conjugates having anionic linkers
JP2002131859A (ja) 2000-10-19 2002-05-09 Konica Corp 撮影用赤外感光性ハロゲン化銀写真感光材料及び赤外感光性ハロゲン化銀乳剤
US6890747B2 (en) 2000-10-23 2005-05-10 Warner-Lambert Company Phosphoinositide 3-kinases
MXPA03005152A (es) 2000-12-11 2004-10-14 Tularik Inc Antogonista de cxcr3.
CN1492874A (zh) 2000-12-21 2004-04-28 大环内酯
US7157487B2 (en) 2000-12-28 2007-01-02 Daiichi Pharmaceutical Co., Ltd. Vla-4 inhibitors
WO2002057425A2 (en) 2001-01-22 2002-07-25 Merck & Co., Inc. Nucleoside derivatives as inhibitors of rna-dependent rna viral polymerase
US7105499B2 (en) 2001-01-22 2006-09-12 Merck & Co., Inc. Nucleoside derivatives as inhibitors of RNA-dependent RNA viral polymerase
GB0102239D0 (en) 2001-01-29 2001-03-14 Cancer Res Ventures Ltd Methods of chemical synthisis
GB2373186A (en) 2001-02-23 2002-09-18 Astrazeneca Ab Pharmaceutical combinations of a CCR3 antagonist and a compound which is usefulreatment of asthma, allergic disease or inflammation
MXPA03008560A (es) 2001-03-22 2004-06-30 Abbot Gmbh & Co Kg Pirazolopirimidinas como agentes terapeuticos.
DE10118698A1 (de) 2001-04-17 2002-11-07 Jerini Ag Verfahren zur Immobilisierung und damit hergestellte Anordnungen von Verbindungen auf einer planaren Oberfläche
US7250569B2 (en) 2001-04-26 2007-07-31 New York University School Of Medicine Method for dissolving nanostructural materials
US7405235B2 (en) 2001-05-04 2008-07-29 Paratek Pharmaceuticals, Inc. Transcription factor modulating compounds and methods of use thereof
DE60218458T2 (de) 2001-05-08 2007-11-15 Kudos Pharmaceuticals Ltd. Isochinolinon derivate als parp inhibitoren
US7144903B2 (en) 2001-05-23 2006-12-05 Amgen Inc. CCR4 antagonists
US6794379B2 (en) 2001-06-06 2004-09-21 Tularik Inc. CXCR3 antagonists
US20030236198A1 (en) 2001-06-13 2003-12-25 Genesoft, Inc. Antipathogenic benzamide compounds
EP1470119A4 (en) 2001-06-13 2005-10-19 Genesoft Pharmaceuticals Inc BENZOTHIOPHENE COMPOUNDS WITH ANTI-INFECTIOUS ACTIVITY
US6777425B2 (en) 2001-06-13 2004-08-17 Genesoft Pharmaceuticals, Inc. Isoquinoline compounds having antiinfective activity
AU2002315389A1 (en) 2001-06-21 2003-01-08 Ariad Pharmaceuticals, Inc. Novel pyrazolo-and pyrrolo-pyrimidines and uses thereof
US6689782B2 (en) 2001-07-16 2004-02-10 Essential Therapeutics, Inc. Fungal efflux pump inhibitors
US6596723B1 (en) 2001-07-16 2003-07-22 Essential Therapeutics, Inc. Fungal efflux pump inhibitors
US20030220338A1 (en) 2001-07-16 2003-11-27 Watkins Will J. Fungal efflux pump inhibitors
WO2003007888A2 (en) 2001-07-20 2003-01-30 Adipogenix, Inc. Fat accumulation-modulating compounds
JP4658473B2 (ja) 2001-07-27 2011-03-23 キュリス，インコーポレイテッド ヘッジホッグシグナル伝達経路メディエーター、それに関連した組成物及び利用
EP1414443B1 (en) 2001-08-01 2006-11-15 Merck & Co., Inc. BENZIMIDAZO 4,5-f|ISOQUINOLINONE DERIVATIVES
WO2003020880A2 (en) 2001-08-03 2003-03-13 Abbott Laboratories Method of identifying inhibitors of lck
BR0211750A (pt) 2001-08-10 2004-10-13 Shionogi & Co Agente antiviral
JP2003073357A (ja) 2001-09-03 2003-03-12 Mitsubishi Pharma Corp アミド化合物を含有するＲｈｏキナーゼ阻害剤
JP2005507876A (ja) 2001-09-05 2005-03-24 ミナーバ バイオテクノロジーズ コーポレイション 癌を治療する組成物および方法
CA2458926A1 (en) 2001-09-13 2003-03-13 Genesoft Pharmaceuticals, Inc. Methods of treating infection by drug resistant bacteria
US7101884B2 (en) 2001-09-14 2006-09-05 Merck & Co., Inc. Tyrosine kinase inhibitors
AUPR769501A0 (en) 2001-09-14 2001-10-11 Biomolecular Research Institute Limited Cytokine receptor 1
US7269663B2 (en) 2001-09-28 2007-09-11 Intel Corporation Tagging packets with a lookup key to facilitate usage of a unified packet forwarding cache
TWI330183B (https=) 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
MXPA04004178A (es) 2001-11-01 2004-09-06 Janssen Pharmaceutica Nv Heteroarilaminas como inhibidores de glucogeno cintasa cinasa 3beta.
US20030113828A1 (en) 2001-11-09 2003-06-19 Ginsberg Mark H. Compositions and methods for modulating Syk function
AU2002366103A1 (en) 2001-11-19 2003-06-10 Iconix Pharmaceuticals, Inc. Modulators of rho c activity
AU2002346471A1 (en) 2001-11-20 2003-06-10 Cytokinetics, Inc. Process for the racemization of chiral quinazolinones
DE60226063T2 (de) 2001-11-27 2009-05-20 F. Hoffmann-La Roche Ag Benzothiazole derivative
AU2002350217A1 (en) 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
US20050107404A1 (en) 2001-12-06 2005-05-19 Fraley Mark E. Mitotic kinesin inhibitors
US7262187B2 (en) 2001-12-06 2007-08-28 Merck & Co., Inc. Substituted oxazolo- and thizaolopyrimidinones as a mitotic kinesin inhibitor
WO2003059884A1 (en) 2001-12-21 2003-07-24 X-Ceptor Therapeutics, Inc. Modulators of lxr
JP4085237B2 (ja) 2001-12-21 2008-05-14 日本電気株式会社 携帯電話の利用契約システムと通信方法
US20030158195A1 (en) 2001-12-21 2003-08-21 Cywin Charles L. 1,6 naphthyridines useful as inhibitors of SYK kinase
US7064218B2 (en) 2001-12-26 2006-06-20 Genelabs Technologies, Inc. Aromatic compounds and poly(oxyalkylene) containing aromatic compounds possessing antibacterial, antifungal or antitumor activity
US7414036B2 (en) 2002-01-25 2008-08-19 Muscagen Limited Compounds useful as A3 adenosine receptor agonists
WO2003070701A2 (en) 2002-02-15 2003-08-28 Cytokinetics, Inc. Syntheses of quinazolinones
US20040043959A1 (en) 2002-03-04 2004-03-04 Bloom Laura A. Combination therapies for treating methylthioadenosine phosphorylase deficient cells
ES2361403T3 (es) 2002-03-07 2011-06-16 X-Ceptor Therapeutics, Inc. Moduladores de quinazolinona de receptores nucleares.
US6995144B2 (en) 2002-03-14 2006-02-07 Eisai Co., Ltd. Nitrogen containing heterocyclic compounds and medicines containing the same
WO2003082341A1 (en) 2002-03-22 2003-10-09 Cellular Genomics, Inc. AN IMPROVED FORMULATION OF CERTAIN PYRAZOLO[3,4-d] PYRIMIDINES AS KINASE MODULATORS
EP1503988B1 (de) 2002-03-26 2009-07-22 Biofrontera Discovery Gmbh Fredericamycin-derivate
US7166293B2 (en) 2002-03-29 2007-01-23 Carlsbad Technology, Inc. Angiogenesis inhibitors
US6900219B2 (en) 2002-04-04 2005-05-31 Cv Therapeutics, Inc. ABCA-1 elevating compounds
DE10217046A1 (de) 2002-04-17 2003-11-06 Bioleads Gmbh Fredericamycin-Derivate
DE60322869D1 (de) 2002-04-22 2008-09-25 Univ Johns Hopkins Modulatoren von hedgehog signalpfaden, zusammensetzungen und verwandte verwendungen
WO2003090751A1 (en) 2002-04-26 2003-11-06 Pfizer Products Inc. Pyrimidine-2, 4, 6-trione metallo-proteinase inhibitors
US6794562B2 (en) 2002-05-01 2004-09-21 Stine Seed Farm, Inc. Soybean cultivar 0332143
US7214800B2 (en) 2002-05-09 2007-05-08 Cytokinetics, Inc. Compounds, compositions, and methods
CA2485148A1 (en) 2002-05-09 2003-11-20 Cytokinetics, Inc. Pyrimidinone compounds, compositions and methods
TW200407143A (en) 2002-05-21 2004-05-16 Bristol Myers Squibb Co Pyrrolotriazinone compounds and their use to treat diseases
WO2004039774A2 (en) 2002-05-23 2004-05-13 Merck & Co., Inc. Mitotic kinesin inhibitors
EP1513820A4 (en) 2002-05-23 2006-09-13 Cytokinetics Inc COMPOUNDS, COMPOSITIONS AND METHODS
WO2003106426A1 (en) 2002-06-14 2003-12-24 Cytokinetics, Inc. Compounds, compositions, and methods
RU2340605C2 (ru) 2002-06-27 2008-12-10 Ново Нордиск А/С Арилкарбонильные производные в качестве терапевтических средств
US7265111B2 (en) 2002-06-27 2007-09-04 Sanofi-Aventis Deutschland Gmbh Adenosine analogues and their use as pharmaceutical agents
BR0312023A (pt) 2002-06-27 2005-03-22 Novo Nordisk As Composto, composto ativador da glicose cinase, método para evitar a hipoglicemia, uso de um composto, e, composição farmacêutica
DE10230917A1 (de) 2002-07-09 2004-02-05 Bioleads Gmbh Fredericamycin-Derivate
CN1681811B (zh) 2002-07-10 2010-05-26 默克雪兰诺有限公司 唑烷酮-乙烯基稠合的-苯衍生物
AU2003249244A1 (en) 2002-07-15 2004-02-02 Combinatorx, Incorporated Methods for the treatment of neoplasms
WO2004014377A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc 4-hydroxyquinoline derivatives as matrix metalloproteinase inhibitors
JP4646626B2 (ja) 2002-08-16 2011-03-09 アストラゼネカ アクチボラグ ホスホイノシチド３−キナーゼβの阻害
US20040048853A1 (en) 2002-08-21 2004-03-11 Gustave Bergnes Compounds, compositions, and methods
US20030139427A1 (en) 2002-08-23 2003-07-24 Osi Pharmaceuticals Inc. Bicyclic pyrimidinyl derivatives and methods of use thereof
AU2003265853A1 (en) 2002-08-29 2004-03-19 Curis, Inc. Hedgehog antagonists, methods and uses related thereto
GB0220319D0 (en) 2002-09-02 2002-10-09 Cancer Res Campaign Tech Enzyme activated self-immolative nitrogen mustard drugs
JP4487774B2 (ja) 2002-09-30 2010-06-23 萬有製薬株式会社 ２−アミノベンズイミダゾール誘導体
US20040132732A1 (en) 2002-10-21 2004-07-08 Wei Han Quinazolinones and derivatives thereof as factor Xa inhibitors
JP2004161716A (ja) 2002-11-15 2004-06-10 Takeda Chem Ind Ltd Ｊｎｋ阻害剤
CN1281590C (zh) 2002-11-27 2006-10-25 南京凯衡科贸有限公司 具有抑制血管生成活性的六员氨基酰胺类衍生物
ATE496893T1 (de) 2002-12-20 2011-02-15 X Ceptor Therapeutics Inc Isochinolinonderivate und deren verwendung als medikamente
US7247736B2 (en) 2002-12-23 2007-07-24 4Sc Ag Method of identifying inhibitors of DHODH
US7365094B2 (en) 2002-12-23 2008-04-29 4Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
US7071355B2 (en) 2002-12-23 2006-07-04 4 Sc Ag Compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
BRPI0406647A (pt) 2003-01-06 2005-12-06 Angiochem Inc Método para transportar um composto através da barreira sanguìnea do cérebro
FR2850022B1 (fr) 2003-01-22 2006-09-08 Centre Nat Rech Scient Nouvelle utilisation de la mifepristone et de ses derives comme modulateurs de la voie de signalisation des proteines hedgehog et ses applications
WO2004069145A2 (en) 2003-02-07 2004-08-19 Dr. Reddy's Laboratories Ltd. Anticancer compounds, process for their preparation and pharmaceutical compositions containing them
CA2517942A1 (en) 2003-03-06 2004-09-16 Dsm Ip Assets B.V. Process for the preparation of an .alpha.-amino carbonyl compound
AR050920A1 (es) 2003-03-07 2006-12-06 Astrazeneca Ab Enantiomeros de heterociclos fusionados seleccionados y usos de los mismos
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
GB0306907D0 (en) 2003-03-26 2003-04-30 Angiogene Pharm Ltd Boireductively-activated prodrugs
US7217794B2 (en) 2003-04-02 2007-05-15 Daiamed, Inc. Compounds and methods for treatment of thrombosis
WO2004092123A2 (en) 2003-04-10 2004-10-28 Microbia, Inc. Inhibitors of fungal invasion
EP2387998A1 (en) * 2003-04-29 2011-11-23 Glaxosmithkline LLC Methods for treating degenerative diseases/injuries
EP1638963B1 (en) 2003-05-20 2009-09-09 Novartis AG N-acyl nitrogen heterocycles as ligands of peroxisome proliferator-activated receptors
US7022850B2 (en) 2003-05-22 2006-04-04 Bristol-Myers Squibb Co. Bicyclicpyrimidones and their use to treat diseases
US7345046B2 (en) 2003-05-30 2008-03-18 Chiron Corporation Heteroaryl-fused pyrimidinyl compounds as anticancer agents
DE602004022819D1 (de) 2003-06-06 2009-10-08 Vertex Pharma Von atp-bindende kassette transportern
EP1637523A4 (en) 2003-06-18 2009-01-07 Ube Industries PROCESS FOR PRODUCING A PYRIMIDIN-4-ONE COMPOUND
US7429596B2 (en) 2003-06-20 2008-09-30 The Regents Of The University Of California 1H-pyrrolo [2,3-D] pyrimidine derivatives and methods of use thereof
WO2005002585A1 (en) 2003-07-02 2005-01-13 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 and a ligand to an alpha-2-delta receptor
US7173015B2 (en) 2003-07-03 2007-02-06 The Trustees Of The University Of Pennsylvania Inhibition of Syk kinase expression
JP2009513523A (ja) 2003-07-08 2009-04-02 ノバルティス アクチエンゲゼルシャフト ベンゼンスルホニルアミノ化合物およびそれらを含む医薬組成物
JP2005035933A (ja) 2003-07-15 2005-02-10 Takeda Chem Ind Ltd 含窒素縮合複素環化合物の製造方法
WO2005013800A2 (en) 2003-07-15 2005-02-17 The Johns Hopkins University Elevated hedgehog pathway activity in digestive system tumors, and methods of treating digestive system tumors having elevated hedgehog pathway activity
GB0317951D0 (en) 2003-07-31 2003-09-03 Trigen Ltd Compounds
US7501538B2 (en) 2003-08-08 2009-03-10 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
US7208601B2 (en) 2003-08-08 2007-04-24 Mjalli Adnan M M Aryl and heteroaryl compounds, compositions, and methods of use
US20050054614A1 (en) 2003-08-14 2005-03-10 Diacovo Thomas G. Methods of inhibiting leukocyte accumulation
WO2005016348A1 (en) 2003-08-14 2005-02-24 Icos Corporation Method of inhibiting immune responses stimulated by an endogenous factor
EP1656378A4 (en) 2003-08-15 2011-05-11 Irm Llc COMPOUNDS AND COMPOSITIONS INHIBITING TYROSINE KINASE RECEPTOR ACTIVITY
US7390820B2 (en) 2003-08-25 2008-06-24 Amgen Inc. Substituted quinolinone derivatives and methods of use
WO2005044181A2 (en) 2003-09-09 2005-05-19 Temple University-Of The Commonwealth System Of Higher Education Protection of tissues and cells from cytotoxic effects of ionizing radiation by abl inhibitors
GB0321710D0 (en) 2003-09-16 2003-10-15 Novartis Ag Organic compounds
GB0322409D0 (en) 2003-09-25 2003-10-29 Astrazeneca Ab Quinazoline derivatives
US8067608B2 (en) 2003-09-29 2011-11-29 The Johns Hopkins University Hedgehog pathway antagonists
WO2005032343A2 (en) 2003-10-01 2005-04-14 The Johns Hopkins University Hedgehog signaling in prostate regeneration neoplasia and metastasis
US20080057071A1 (en) 2003-10-20 2008-03-06 Watkins David N Use Of Hedgehog Pathway Inhibitors In Small-Cell Lung Cancer
AU2004289303A1 (en) 2003-11-10 2005-05-26 Synta Pharmaceuticals, Corp. Fused heterocyclic compounds
WO2005049613A1 (en) 2003-11-14 2005-06-02 Merck Sharp & Dohme Limited Bicyclic pyrimidin-4-(3h)-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (vr1)
WO2005049838A2 (en) 2003-11-14 2005-06-02 Yale University Syk-targeted nucleic acid interference
CA2546192C (en) 2003-11-17 2010-04-06 Pfizer Products Inc. Pyrrolopyrimidine compounds useful in treatment of cancer
US7939539B2 (en) 2003-11-25 2011-05-10 Novartis Vaccines And Diagnostics, Inc. Quinazolinone compounds as anticancer agents
WO2005054202A1 (en) 2003-11-25 2005-06-16 Eli Lilly And Company 7-phenyl-isoquinoline-5-sulfonylamino derivatives as inhibitors of akt (proteinkinase b)
EP1692112A4 (en) 2003-12-08 2008-09-24 Cytokinetics Inc COMPOUNDS, COMPOSITIONS, AND METHODS
CA2548951A1 (en) 2003-12-22 2005-07-14 Gilead Sciences, Inc. Kinase inhibitor phosphonate conjugates
US20050152940A1 (en) 2003-12-23 2005-07-14 Medtronic Vascular, Inc. Medical devices to treat or inhibit restenosis
US7569571B2 (en) 2003-12-23 2009-08-04 Novartis Ag Substituted pyrazolo [3,4-d]pyrimidines as cytokine modulators
WO2005061707A1 (ja) 2003-12-24 2005-07-07 Kyowa Hakko Kogyo Co., Ltd. 癌細胞のEg5阻害剤に対する感受性を判定する方法
US20050239809A1 (en) 2004-01-08 2005-10-27 Watts Stephanie W Methods for treating and preventing hypertension and hypertension-related disorders
WO2005070457A1 (en) 2004-01-23 2005-08-04 Seattle Genetics, Inc. Melphalan prodrugs
JP2007520559A (ja) 2004-02-03 2007-07-26 アボット・ラボラトリーズ 治療薬としてのアミノベンゾオキサゾール類
UA83416C2 (en) 2004-02-13 2008-07-10 Баниу Фармасьютикал Ко., Лтд. Fused ring 4-oxopyrimidine derivative
US7650848B2 (en) 2004-02-17 2010-01-26 University Of Florida Research Foundation, Inc. Surface topographies for non-toxic bioadhesion control
US9016221B2 (en) 2004-02-17 2015-04-28 University Of Florida Research Foundation, Inc. Surface topographies for non-toxic bioadhesion control
US7117807B2 (en) 2004-02-17 2006-10-10 University Of Florida Research Foundation, Inc. Dynamically modifiable polymer coatings and devices
US20050187418A1 (en) 2004-02-19 2005-08-25 Small Brooke L. Olefin oligomerization
US20070049593A1 (en) 2004-02-24 2007-03-01 Japan Tobacco Inc. Tetracyclic fused heterocyclic compound and use thereof as HCV polymerase inhibitor
WO2005080394A1 (en) 2004-02-24 2005-09-01 Bioaxone Therapeutique Inc. 4-substituted piperidine derivatives
KR100843526B1 (ko) 2004-02-27 2008-07-03 에프. 호프만-라 로슈 아게 피라졸의 접합 유도체
TWI378934B (en) 2004-04-02 2012-12-11 Osi Pharm Inc 6,6-bicyclic ring substituted heterobicyclic protein kinase inhibitors
US8057815B2 (en) 2004-04-19 2011-11-15 Portola Pharmaceuticals, Inc. Methods of treatment with Syk inhibitors
BRPI0510305A (pt) 2004-04-30 2007-10-02 Takeda Pharmaceutical composto ou um sal do mesmo, pródroga ou um sal da mesma, agente farmacêutico, método de produção do composto ou um sal do mesmo, inibidor de metaloproteinase de matriz ou um sal do mesmo ou uma pródroga do mesmo, método de inibir uma metaloproteinase de matriz, e, uso de um composto ou de um sal do mesmo ou de uma pródroga do mesmo
US8273743B2 (en) 2004-04-30 2012-09-25 Curis, Inc. Quinoxaline inhibitors of the hedgehog signalling
DE102004022897A1 (de) 2004-05-10 2005-12-08 Bayer Cropscience Ag Azinyl-imidazoazine
CA2730540A1 (en) 2004-05-13 2005-12-01 Vanderbilt University Phosphoinositide 3-kinase delta selective inhibitors for inhibiting angiogenesis
SI2612862T1 (sl) 2004-05-13 2017-04-26 Icos Corporation Kinazolini kot inhibitorji humane fosfatidilinozitol 3-kinaze delta
JP2008500338A (ja) 2004-05-25 2008-01-10 イコス・コーポレイション 造血細胞の異常増殖を治療及び／又は予防する方法
GB0412467D0 (en) 2004-06-04 2004-07-07 Astrazeneca Ab Chemical compounds
CA2569406A1 (en) 2004-06-04 2005-12-22 Icos Corporation Methods for treating mast cell disorders
US20050282834A1 (en) 2004-06-09 2005-12-22 Fady Malik Compositions, devices and methods for treating cardiovascular disease
US7939538B2 (en) 2004-06-28 2011-05-10 Amgen Inc. Compounds, compositions and methods for prevention and treatment of inflammatory and immunoregulatory disorders and diseases
US7375102B2 (en) 2004-06-28 2008-05-20 Amgen Sf, Llc Tetrahydroquinazolin-4(3H)-one-related and tetrahydropyrido[2,3-D]pyrimidin-4(3H)-one-related compounds, compositions and methods for their use
WO2006023381A1 (en) 2004-08-16 2006-03-02 Taigen Biotechnology Pyrimidinone compounds
US20060041128A1 (en) 2004-08-18 2006-02-23 Astrazeneca Ab Selected fused heterocyclics and uses thereof
CN101027309B (zh) 2004-08-18 2010-10-27 阿斯利康(瑞典)有限公司 所选择的稠合嘧啶酮的对映体和在治疗和预防癌症中的用途
EP2316832B1 (en) 2004-08-27 2017-03-08 Infinity Pharmaceuticals, Inc. Cyclopamine analogues and methods of use thereof
EP1786265A4 (en) 2004-08-30 2009-08-19 Smithkline Beecham Corp NEW COMPOSITIONS AND PROCESSING METHODS
BRPI0514691A (pt) 2004-08-31 2008-06-17 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, processo para preparar o mesmo, composição farmacêutica, e, uso de um composto ou um sal farmaceuticamente aceitável do mesmo
DK1789390T3 (da) 2004-09-02 2012-02-27 Genentech Inc Pyridyl-inhibitorer af hedgehog-signalering
JP2008512457A (ja) 2004-09-09 2008-04-24 アメリカ合衆国 Ａ３及びａ１アデノシン受容体作用薬としてのプリン誘導体
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
WO2006038865A1 (en) 2004-10-01 2006-04-13 Betagenon Ab Nucleotide derivatives for the treatment of type 2 diabetes and other disorders
CN101083996A (zh) 2004-10-28 2007-12-05 Irm责任有限公司 作为hedgehog途径调节剂的化合物和组合物
US8212011B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues
US8212012B2 (en) 2004-11-03 2012-07-03 University Of Kansas Novobiocin analogues having modified sugar moieties
WO2006050501A2 (en) 2004-11-03 2006-05-11 University Of Kansas Novobiocin analogues as anticancer agents
US7622451B2 (en) 2004-11-03 2009-11-24 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
GB0425035D0 (en) 2004-11-12 2004-12-15 Novartis Ag Organic compounds
US9512125B2 (en) 2004-11-19 2016-12-06 The Regents Of The University Of California Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents
US8143257B2 (en) 2004-11-23 2012-03-27 Ptc Therapeutics, Inc. Substituted phenols as active agents inhibiting VEGF production
US20060156485A1 (en) 2005-01-14 2006-07-20 The Procter & Gamble Company Keratin dyeing compounds, keratin dyeing compositions containing them, and use thereof
CA2593166A1 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Mitotic kinesin inhibitors
WO2006078575A2 (en) 2005-01-19 2006-07-27 Merck & Co., Inc. Fluorinated aminoalkyl-4-oxo-3,4-dihydropyrido[3,4- d] pyrimidines as inhibitors of mitotic kinesins
NZ560320A (en) 2005-01-25 2011-02-25 Prolexys Pharmaceuticals Inc Quinoxaline derivatives as antitumor agents
US20070161644A1 (en) 2005-01-25 2007-07-12 Stockwell Brent R Erastin analogs and uses thereof
GB0501999D0 (en) 2005-02-01 2005-03-09 Sentinel Oncology Ltd Pharmaceutical compounds
WO2006089106A2 (en) 2005-02-17 2006-08-24 Icos Corporation Phosphoinositide 3-kinase inhibitors for inhibiting leukocyte accumulation
US7579348B2 (en) 2005-02-25 2009-08-25 Pgxhealth, Llc Derivatives of 8-substituted xanthines
WO2006093247A1 (ja) 2005-02-28 2006-09-08 Japan Tobacco Inc. Ｓｙｋ阻害活性を有する新規なアミノピリジン化合物
US20090124654A1 (en) 2005-03-01 2009-05-14 Mjalli Adnan M M Aryl and Heteroaryl Compounds, Compositions, Methods of Use
US7872050B2 (en) 2005-03-14 2011-01-18 Yaupon Therapeutics Inc. Stabilized compositions of volatile alkylating agents and methods of using thereof
JP2006265107A (ja) 2005-03-22 2006-10-05 Kyowa Hakko Kogyo Co Ltd 緑内障治療剤
GB0506147D0 (en) 2005-03-24 2005-05-04 Merck Sharp & Dohme Therapeutic agents
BRPI0609650A2 (pt) 2005-03-25 2010-04-20 Tibotec Pharm Ltd inibidores heterobicìlicos de hvc
US20070066632A1 (en) 2005-03-25 2007-03-22 Scios, Inc. Fused bicyclic inhibitors of TGFbeta
EP1893605A2 (en) 2005-03-31 2008-03-05 AstraZeneca AB Saminopyrimidine derivates with tie2 inhibiting activity
RU2007140733A (ru) 2005-04-06 2009-05-20 Айрм Ллк (Bm) Диариламинсодержащие соединения и композиции, и их применение в качестве модуляторов ядерных рецепторов стероидного гормона
KR100781704B1 (ko) 2005-04-20 2007-12-03 에스케이케미칼주식회사 피리딘 유도체와 이의 제조방법, 및 이를 포함하는약제조성물
WO2006114064A2 (en) 2005-04-25 2006-11-02 Institute Of Organic Chemistry And Biochemistry Ofthe Academy Of Sciences Of The Czech Republic Use of compounds to enhance processivity of telomerase
WO2006135479A2 (en) 2005-05-10 2006-12-21 Angiotech International Ag Anti-scarring agents, therapeutic compositions, and use thereof
WO2006121522A2 (en) 2005-05-10 2006-11-16 Angiotech International Ag Implantable sensors and pumps, anti-scarring agents, and therapeutic compositions
WO2006121518A2 (en) 2005-05-10 2006-11-16 Angiotech International Ag Electrical devices, anti-scarring agents, and therapeutic compositions
US20090298856A1 (en) 2005-05-11 2009-12-03 Rebecca Elizabeth Brown 2,3 Substituted fused bicyclic pyrimidin-4(3H)-ones modulating the function of the vanilliod-1receptor (VR1)
GB0509573D0 (en) 2005-05-11 2005-06-15 Merck Sharp & Dohme Therapeutic compounds
DE102005024017A1 (de) 2005-05-25 2006-11-30 Merck Patent Gmbh Chinazolinone
CN100526315C (zh) 2005-06-16 2009-08-12 浙江医药股份有限公司新昌制药厂 N2-喹啉或异喹啉取代的嘌呤衍生物及其制备方法和其用途
BRPI0612112A8 (pt) 2005-06-22 2017-12-26 Chemocentryx Inc composto, composição farmacêutica, e, método de tratar doenças ou condições mediadas por ccr1.
CA2612585A1 (en) 2005-06-27 2007-01-04 Amgen Inc. Anti-inflammatory aryl nitrile compounds
WO2007008541A2 (en) 2005-07-08 2007-01-18 Kalypsys, Inc. Cellular cholesterol absorption modifiers
JP2009505948A (ja) 2005-07-11 2009-02-12 デブジェン エヌブイ キナーゼ阻害剤としてのアミド誘導体
JP2009500437A (ja) 2005-07-11 2009-01-08 デブジェン エヌブイ キナーゼ阻害剤としてのアミド誘導体
WO2007015877A2 (en) 2005-07-20 2007-02-08 Kalypsys, Inc. Inhibitors of p38 kinase and methods of treating inflammatory disorders
US20070017915A1 (en) 2005-07-22 2007-01-25 Weder Donald E Collapsible and/or erectable substantially egg-shaped container
GB0516723D0 (en) 2005-08-15 2005-09-21 Novartis Ag Organic compounds
WO2007025090A2 (en) 2005-08-25 2007-03-01 Kalypsys, Inc. Heterobicyclic and - tricyclic inhibitors of mapk/erk kinase
RU2008110941A (ru) 2005-08-25 2009-09-27 Ф.Хоффманн-Ля Рош Аг (Ch) ИНГИБИТОРЫ КИНАЗЫ p38 МАР И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
EP1940805A4 (en) 2005-08-26 2009-11-11 Methylgene Inc BENZODIAZEPIN AND BENZOPIPERAZINANALOGA AS INHIBITORS OF HISTONDEACETYLASE
US20080318942A1 (en) 2005-09-01 2008-12-25 Bioagency Ag Fredericamycin Derivatives
CA2624220A1 (en) 2005-09-29 2007-04-12 Wyeth 1- (1h- indol- 1-yl) -3- (methylamino) -1- phenylpropan-2-ol derivatives and related compounds as modulators of the monoamine reuptake for the treatment of vasomotor symptoms (vms)
EP1960382A1 (en) 2005-11-03 2008-08-27 ChemBridge Research Laboratories, Inc. Heterocyclic compounds as tyrosine kinase modulators
US7893260B2 (en) 2005-11-04 2011-02-22 Hydra Biosciences, Inc. Substituted quinazolin-4-one compounds for antagonizing TRPV3 function
EP1945202A2 (en) 2005-11-11 2008-07-23 Licentia OY Mammalian hedgehog signaling inhiabitors
US8101610B2 (en) 2005-11-14 2012-01-24 Genentech, Inc. Bisamide inhibitors of hedgehog signaling
EP2385053B1 (en) 2005-11-17 2013-10-02 OSI Pharmaceuticals, Inc. Intermediates for the preparation of fused bicyclic mTOR inhibitors
AU2006316321A1 (en) 2005-11-22 2007-05-31 Merck & Co., Inc. Indole orexin receptor antagonists
US20070265231A1 (en) 2005-11-30 2007-11-15 Michael Hofmann Hydrazide Compounds for Combating Animal Pests
WO2007067752A2 (en) 2005-12-08 2007-06-14 Cytokinetics, Inc. Certain compositions and methods of treatment
JP2009520028A (ja) 2005-12-19 2009-05-21 オーエスアイ・ファーマスーティカルズ・インコーポレーテッド Ｉｇｆｒ抑制剤および抗癌剤の併用
US7572809B2 (en) 2005-12-19 2009-08-11 Hoffmann-La Roche Inc. Isoquinoline aminopyrazole derivatives
WO2007076055A2 (en) 2005-12-22 2007-07-05 Entremed, Inc. Compositions and methods comprising proteinase activated receptor antagonists
WO2007076085A2 (en) 2005-12-22 2007-07-05 Prolexys Pharmaceuticals, Inc . Fused pyrimidones and thiopyrimidones, and uses thereof
TW200801008A (en) 2005-12-29 2008-01-01 Abbott Lab Protein kinase inhibitors
PE20070946A1 (es) 2006-01-25 2007-10-16 Smithkline Beecham Corp COMPUESTOS DERIVADOS DE IMIDAZO[1,2-a]PIRIDINA COMO MODULADORES DEL RECEPTOR DE QUIMIOQUINA (CXCR4)
WO2007089669A2 (en) 2006-01-26 2007-08-09 Wyeth Processes for the preparation of compounds which modulate cell proliferation
BRPI0708615A2 (pt) 2006-03-07 2011-06-07 Array Biopharma Inc compostos de pirazol heterobicìclicos e métodos de uso
JP2009530342A (ja) 2006-03-20 2009-08-27 エフ．ホフマン−ラ ロシュ アーゲー Ｂｔｋおよびｓｙｋ蛋白キナーゼを阻害する方法
TW200800997A (en) 2006-03-22 2008-01-01 Astrazeneca Ab Chemical compounds
EP2004683B1 (en) 2006-03-24 2016-05-11 Biogen Hemophilia Inc. Pc5 as a factor ix propeptide processing enzyme
CA2647543A1 (en) 2006-03-29 2007-11-08 Foldrx Pharmaceuticals, Inc. Inhibition of alpha-synuclein toxicity
WO2007114926A2 (en) 2006-04-04 2007-10-11 The Regents Of The University Of California Kinase antagonists
CN101415688A (zh) 2006-04-05 2009-04-22 阿斯利康(瑞典)有限公司 具有b-raf抑制活性的喹唑啉酮衍生物
WO2007113557A1 (en) 2006-04-05 2007-10-11 Astrazeneca Ab Substituted quinazolines with anti-cancer activity
EP2010170A2 (en) 2006-04-14 2009-01-07 Novartis AG Use of biarylcarboxamides in the treatment of hedgehog pathway-related disorders
WO2007121453A2 (en) 2006-04-17 2007-10-25 The Regents Of The University Of California 2-hydroxy-1-oxo 1,2 dihydro isoquinoline chelating agents
CN101421253A (zh) 2006-04-18 2009-04-29 阿斯利康(瑞典)有限公司 喹唑啉-4-酮衍生物、其制备方法及含有它们的药用组合物
BRPI0710548B8 (pt) 2006-04-20 2021-05-25 Janssen Pharmaceutica Nv inibidores de c-fms cinase, composição farmacêutica e forma de dosagem farmacêutica
EP2322525B1 (en) 2006-04-21 2013-09-18 Novartis AG Purine derivatives for use as adenosin A2A receptor agonists
GB0607950D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
GB0607948D0 (en) 2006-04-21 2006-05-31 Novartis Ag Organic compounds
WO2007125315A2 (en) 2006-04-25 2007-11-08 Astex Therapeutics Limited Pharmaceutical compounds
EP2037931A2 (en) 2006-04-25 2009-03-25 Astex Therapeutics Limited Pharmaceutical combinations of pk inhibitors and other active agents
DE102006020327A1 (de) 2006-04-27 2007-12-27 Bayer Healthcare Ag Heterocyclisch substituierte, anellierte Pyrazol-Derivate und ihre Verwendung
UA93548C2 (uk) 2006-05-05 2011-02-25 Айерем Елелсі Сполуки та композиції як модулятори хеджхогівського сигнального шляху
EP2026775B1 (en) 2006-05-09 2015-04-29 Novaremed Ltd. Use of syk tyrosine kinase inhibitors for the treatment of cell proliferative disorders
WO2007135398A1 (en) 2006-05-22 2007-11-29 Astrazeneca Ab Indole derivatives
GB0610242D0 (en) 2006-05-23 2006-07-05 Novartis Ag Organic compounds
DE602006018877D1 (de) 2006-05-24 2011-01-27 Guardant S R L Alkalisiertes Lokalanästhetikum im Beutel
GB0610317D0 (en) 2006-05-24 2006-07-05 Medical Res Council Antiparasitic compounds and compositions
WO2008005303A2 (en) 2006-06-30 2008-01-10 Janssen Pharmaceutica N.V. Thiazolopyrimidine modulators of trpv1
ES2344760T3 (es) 2006-07-20 2010-09-06 Amgen Inc. Compuestos de piridona sustituidos y metodo de uso.
WO2008013987A2 (en) 2006-07-27 2008-01-31 Prolexys Pharmaceuticals, Inc. N-alkyl substituted piperazinylmethylquinazolinones and azepanylmethylquinazolinones
US20090291442A1 (en) 2006-07-27 2009-11-26 Smithkline Beecham Corporation Hspa1a as a marker for sensitivity to ksp inhibitors
EP2049502B1 (en) 2006-07-28 2012-01-04 Novartis AG 2,4-substituted quinazolines as lipid kinase inhibitors
WO2008023357A1 (en) 2006-08-22 2008-02-28 Technion Research And Development Foundation Ltd. Heterocyclic derivatives binding to the peripheral-type benzodiazepine receptor (pbr)
JP2010501593A (ja) 2006-08-24 2010-01-21 セレネックス， インコーポレイテッド イソキノリン、キナゾリンおよびフタラジン誘導体
US7956064B2 (en) 2006-09-01 2011-06-07 Cylene Pharmaceuticals, Inc. Fused tricyclic compounds as serine-threonine protein kinase and PARP modulators
WO2008025755A1 (de) 2006-09-01 2008-03-06 Basf Se Verwendung von n-haltigen heterozyklen in dermokosmetika
EP1903044A1 (en) 2006-09-14 2008-03-26 Novartis AG Adenosine Derivatives as A2A Receptor Agonists
EP2077267A4 (en) 2006-10-18 2010-04-07 Takeda Pharmaceutical CONDENSED HETEROCYCLIC COMPOUND
CN103435694A (zh) 2006-10-31 2013-12-11 美国政府卫生与公共服务部 Smoothened多肽及使用方法
RU2333211C1 (ru) 2006-11-01 2008-09-10 Институт физиологически активных веществ Российской Академии наук N,n`-замещенные 3, 7-диазабицикло[3.3.1]нонаны, обладающие фармакологической активностью, фармацевтические композиции на их основе и способ их применения
US7772180B2 (en) 2006-11-09 2010-08-10 Bristol-Myers Squibb Company Hepatitis C virus inhibitors
KR20090087027A (ko) 2006-11-13 2009-08-14 일라이 릴리 앤드 캄파니 염증 질환 및 암의 치료를 위한 티에노피리미디논
WO2008063625A2 (en) 2006-11-20 2008-05-29 Adolor Corporation Pyridine compounds and methods of their use
RS53335B (sr) 2006-11-20 2014-10-31 Novartis Ag Kristalna monotozilatna so 2-metil-2-[4-(3-metil-2-okso-8-hinolin-3-il-2,3-dihidro-imidazo[4,5-c]hinolin-1-il)-fenil]-propionitrila
EP2102170A2 (en) 2006-12-06 2009-09-23 Boehringer Ingelheim International GmbH Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
AU2007332493A1 (en) 2006-12-14 2008-06-19 Daiichi Sankyo Company, Limited Imidazothiazole derivatives
CN101611007A (zh) 2006-12-20 2009-12-23 先灵公司 新颖的jnk抑制剂
EP2114925B8 (en) 2006-12-22 2013-04-10 Industrial Research Limited Azetidine analogues of nucleosidase and phosphorylase inhibitors
TWI433674B (zh) 2006-12-28 2014-04-11 Infinity Discovery Inc 環杷明（ｃｙｃｌｏｐａｍｉｎｅ）類似物類
WO2008092292A1 (en) 2007-01-17 2008-08-07 The Hong Kong University Of Science And Technology Isoquinolone compounds as subtype-selective agonists for melatonin receptors mt1 and mt2
US20130116277A1 (en) 2007-01-22 2013-05-09 James T. Dalton Aldo-keto reductase subfamily 1c3 (akr1c3) inhibitors
ES2475193T3 (es) 2007-01-22 2014-07-10 Gtx, Inc. Agentes de unión al receptor nuclear
US20170014401A1 (en) 2007-01-22 2017-01-19 Gtx, Inc. Nuclear receptor binding agents
CN101622001A (zh) 2007-01-26 2010-01-06 Irm责任有限公司 作为激酶抑制剂用于治疗疟原虫相关疾病的嘌呤化合物和组合物
AR065081A1 (es) 2007-01-29 2009-05-13 Xenon Pharmaceuticals Inc Compuestos de quinazolinona y pirimidona fusionados y composicion farmaceutica
NZ579356A (en) 2007-03-07 2012-04-27 Infinity Pharmaceuticals Inc Cyclopamine lactam analogs and methods of use thereof
WO2008109184A1 (en) 2007-03-07 2008-09-12 Infinity Pharmaceuticals, Inc. Heterocyclic cyclopamine analogs and methods of use thereof
US8586619B2 (en) 2007-03-12 2013-11-19 Vm Therapeutics Llc Agents of calcium ion channel modulators
CN101679308B (zh) 2007-03-14 2014-05-07 埃克塞里艾克西斯公司 Hedgehog途径抑制剂
PE20090188A1 (es) 2007-03-15 2009-03-20 Novartis Ag Compuestos heterociclicos como moduladores de la senda de hedgehog
EA017389B1 (ru) 2007-03-23 2012-12-28 Амген Инк. Гетероциклические соединения и их применение
WO2008118454A2 (en) 2007-03-23 2008-10-02 Amgen Inc. Derivatives of quinoline or benzopyrazine and their uses for the treatment of (inter alia) inflammatory diseases, autoimmune diseases or various kinds of cancer
RS53151B (sr) 2007-03-23 2014-06-30 Amgen Inc. 3-supstituisani derivati hinolina ili hinoksalina i njihova upotreba kao inhibitora fosfatidilinozitol 3-kinaze (pi3k)
US7867983B2 (en) 2007-03-29 2011-01-11 The University Of Connecticut Methods to protect skeletal muscle against injury
EP1977765A1 (en) 2007-04-03 2008-10-08 Diatos Peptide prodrugs
CN101636397B (zh) 2007-04-13 2012-06-13 中国人民解放军军事医学科学院毒物药物研究所 脲类化合物、其制备方法及其医药用途
WO2008125207A1 (en) 2007-04-13 2008-10-23 Sanofi-Aventis A transition metal catalyzed synthesis of n-aminoindoles
WO2008131354A2 (en) 2007-04-20 2008-10-30 The Curators Of The University Of Missouri Phytoestrogens as regulators of hedgehog signaling and methods of their use in cancer treatment
JP2010163361A (ja) 2007-04-27 2010-07-29 Dainippon Sumitomo Pharma Co Ltd キノリン誘導体
WO2008138126A1 (en) 2007-05-09 2008-11-20 Neuromed Pharmaceuticals Ltd. Bicyclic pyrimidine derivatives as calcium channel blockers
US7960353B2 (en) 2007-05-10 2011-06-14 University Of Kansas Novobiocin analogues as neuroprotective agents and in the treatment of autoimmune disorders
WO2008143963A1 (en) 2007-05-17 2008-11-27 Cortex Pharmaceuticals, Inc. Di-substituted amides for enhancing glutamatergic synaptic responses
WO2008147852A1 (en) 2007-05-22 2008-12-04 Taigen Biotechnology Co., Ltd. Kinesin inhibitors
JP2010528051A (ja) 2007-05-23 2010-08-19 シガ・テクノロジーズ・インコーポレーテッド デング感染症の治療または予防のための抗ウイルス薬
WO2008153701A1 (en) 2007-05-24 2008-12-18 Schering Corporation Compounds for inhibiting ksp kinesin activity
US9603848B2 (en) 2007-06-08 2017-03-28 Senomyx, Inc. Modulation of chemosensory receptors and ligands associated therewith
US7928111B2 (en) 2007-06-08 2011-04-19 Senomyx, Inc. Compounds including substituted thienopyrimidinone derivatives as ligands for modulating chemosensory receptors
AU2008268613A1 (en) 2007-06-22 2008-12-31 Arqule, Inc. Quinazolinone compounds and methods of use thereof
US20110217300A1 (en) 2007-06-22 2011-09-08 Arqule, Inc. Quinazolinone Compounds and Methods of Use Thereof
BRPI0812970A2 (pt) 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
US20110123486A1 (en) 2007-06-25 2011-05-26 Prolexys Pharmaceuticals, Inc. Methods of treating multiple myeloma and resistant cancers
BRPI0813273A2 (pt) 2007-06-26 2014-12-30 Sanofi Aventis Síntese catalisada por metal regiosseletivo de benzimidazóis e azabenzimidazóis anelados
EP2170274A1 (en) 2007-07-02 2010-04-07 Technion Research and Development Foundation, Ltd. Compositions, articles and methods comprising tspo ligands for preventing or reducing tobacco-associated damage
US20090012031A1 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
RU2345996C1 (ru) 2007-07-17 2009-02-10 Андрей Александрович Иващенко Аннелированные азагетероциклические амиды, включающие пиримидиновый фрагмент, способ их получения и применения
KR20100042287A (ko) 2007-07-31 2010-04-23 쉐링 코포레이션 항암요법으로서의 항-유사분열제 및 아우로라 키나제 억제제 조합물
WO2009018811A1 (de) 2007-08-06 2009-02-12 Schebo Biotech Ag Neue pharmazeutika, verfahren zu ihrer herstellung und ihre verwendung in der medizinischen therapie
WO2009021163A2 (en) 2007-08-08 2009-02-12 University Of Rochester Enhancing gene transfer
CA2696113A1 (en) 2007-08-10 2009-04-02 Burnham Institute For Medical Research Tissue-nonspecific alkaline phosphatase (tnap) activators and uses thereof
WO2009023718A2 (en) 2007-08-13 2009-02-19 Metabasis Therapeutics, Inc. Novel activators of glucokinase
WO2009029617A1 (en) 2007-08-27 2009-03-05 Kalypsys, Inc. Diarylamine-substituted quinolones useful as inducible nitric oxide synthase inhibitors
EP3050566B1 (en) 2007-09-10 2018-11-28 Boston Biomedical, Inc. A novel group of stat3 pathway inhibitors and cancer stem cell pathway inhibitors
JP5227965B2 (ja) 2007-10-03 2013-07-03 独立行政法人理化学研究所 ニトロトリアゾール誘導体、およびそれを用いる化合物の製造方法
WO2009050506A2 (en) 2007-10-15 2009-04-23 Astrazeneca Ab Combination 059
CA2716334A1 (en) 2007-11-13 2009-05-22 Icos Corporation Inhibitors of human phosphatidyl-inositol 3-kinase delta
CA2705405A1 (en) 2007-11-22 2009-05-28 Boehringer Ingelheim International Gmbh New compounds
EP2070932A1 (en) 2007-12-13 2009-06-17 4Sc Ag Pyrazolotriazines
US20090163481A1 (en) 2007-12-13 2009-06-25 Murphy Brian J Ppar-delta ligands and methods of their use
CA2709203A1 (en) 2007-12-13 2009-06-18 Siena Biotech S.P.A. Hedgehog pathway antagonists and therapeutic applications thereof
CA2709784A1 (en) 2007-12-21 2009-07-09 University Of Rochester Method for altering the lifespan of eukaryotic organisms
WO2009081105A2 (en) 2007-12-21 2009-07-02 Ucb Pharma S.A. Quinoxaline and quinoline derivatives as kinase inhibitors
US7960397B2 (en) 2007-12-28 2011-06-14 Institute Of Experimental Botany, Academy Of Sciences Of The Czech Republic 6,9-disubstituted purine derivatives and their use as cosmetics and cosmetic compositions
US7894450B2 (en) 2007-12-31 2011-02-22 Nortel Network, Ltd. Implementation of VPNs over a link state protocol controlled ethernet network
US8193182B2 (en) 2008-01-04 2012-06-05 Intellikine, Inc. Substituted isoquinolin-1(2H)-ones, and methods of use thereof
EP3613743B1 (en) 2008-01-04 2022-03-16 Intellikine, LLC Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives
JP2011509305A (ja) 2008-01-09 2011-03-24 ピージーエックスヘルス、リミテッド、ライアビリティー、カンパニー Ａ２ａｒアゴニストによる神経障害性疼痛の髄腔内治療
EP2228350A4 (en) 2008-01-10 2010-12-29 Asahi Glass Co Ltd GLASS, COATING MATERIAL FOR A LIGHT EMITTING DEVICE AND LIGHT EMITTING DEVICE
WO2009089598A2 (en) 2008-01-18 2009-07-23 Katholieke Universiteit Leuven Msmb-gene methylation based diagnosis, staging and prognosis of prostate cancer
MX2010007587A (es) 2008-01-24 2010-08-04 Ucb Pharma Sa Compuestos que comprenden un grupo ciclobutoxi.
CA2710929A1 (en) 2008-01-28 2009-08-06 Schering Corporation Imidazopyrazines as protein kinase inhibitors
EP2244709A4 (en) 2008-02-07 2012-02-29 Synta Pharmaceuticals Corp TOPICAL FORMULATIONS FOR THE TREATMENT OF PSORIASIS
CN101983062A (zh) 2008-02-07 2011-03-02 吉利德帕洛阿尔托股份有限公司 提高abca-1的化合物及其用途
TWI444384B (zh) 2008-02-20 2014-07-11 Gilead Sciences Inc 核苷酸類似物及其在治療惡性腫瘤上的用途
CN101531638B (zh) 2008-03-13 2011-12-28 中国科学院广州生物医药与健康研究院 用作雌激素相关受体调节剂的化合物及其应用
WO2009114826A2 (en) 2008-03-13 2009-09-17 Angiodynamics, Inc. Treatment systems and methods for renal-related diseases
US8637542B2 (en) 2008-03-14 2014-01-28 Intellikine, Inc. Kinase inhibitors and methods of use
US8993580B2 (en) 2008-03-14 2015-03-31 Intellikine Llc Benzothiazole kinase inhibitors and methods of use
ES2413806T3 (es) 2008-03-20 2013-07-17 Amgen Inc. Moduladores de la aurora cinasa y método de uso
WO2009118292A1 (en) 2008-03-24 2009-10-01 Novartis Ag Arylsulfonamide-based matrix metalloprotease inhibitors
ES2480994T3 (es) 2008-03-31 2014-07-29 Genentech, Inc. Compuestos de tipo benzopirano y benzoxepina inhibidores de PI3K y métodos de uso
FR2929851B1 (fr) 2008-04-09 2012-11-30 Centre Nat Rech Scient Molecules inhibant une voie metabolique impliquant la proteine tyrosine kinase syk et procede d'identification de ces molecules
MX2010011463A (es) 2008-04-16 2011-06-03 Portola Pharm Inc 2,6-diamino-pirimidin-5-il-carboxamidas como inhibidores de syk o jak quinasas.
GB0808282D0 (en) 2008-05-07 2008-06-11 Medical Res Council Compounds for use in stabilizing p53 mutants
US8148408B2 (en) 2008-05-09 2012-04-03 Abbott Laboratories Selective substituted pyridine ligands for neuronal nicotinic receptors
JP2011521968A (ja) 2008-05-30 2011-07-28 ジェネンテック， インコーポレイテッド プリンｐｉ３ｋ阻害剤化合物および使用方法
JP2011522860A (ja) 2008-06-10 2011-08-04 ノバルティス アーゲー 上皮性ナトリウムチャネルブロッカーとしてのピラジン誘導体
US20090312406A1 (en) 2008-06-12 2009-12-17 Hsing-Pang Hsieh Coumarin compounds and their use for treating viral infection
JP5788316B2 (ja) 2008-07-08 2015-09-30 インテリカイン， エルエルシー キナーゼインヒビターおよび使用方法
US20110224223A1 (en) 2008-07-08 2011-09-15 The Regents Of The University Of California, A California Corporation MTOR Modulators and Uses Thereof
JP2011528368A (ja) 2008-07-16 2011-11-17 シェーリング コーポレイション 二環式ヘテロ環誘導体およびｇｐｃｒモジュレーターとしてのその使用
UY31984A (es) 2008-07-16 2010-02-26 Boehringer Ingelheim Int DERIVADOS DE 1-(3,4-difluorobencil)-6-oxo-1,6-dihidropirimidin-5-carboxamidas N-sustituidas y de 2-(3,4-difluorobencil)-3-oxo-2,3-dihidro-1H-pirazol-4-carboxamidas N-sustituidas.
US8450344B2 (en) 2008-07-25 2013-05-28 Aerie Pharmaceuticals, Inc. Beta- and gamma-amino-isoquinoline amide compounds and substituted benzamide compounds
WO2010014739A2 (en) 2008-07-29 2010-02-04 Kalypsys, Inc. Heterocyclic modulators of tgr5
US9284297B2 (en) 2008-08-11 2016-03-15 President And Fellows Of Harvard College Halofuginone analogs for inhibition of tRNA synthetases and uses thereof
US20100099871A1 (en) 2008-08-15 2010-04-22 Miller Dwight W Anti-psychotic compounds and pharmaceutical compositions thereof
WO2010039534A2 (en) 2008-09-23 2010-04-08 Georgetown University Viral and fungal inhibitors
US8703778B2 (en) 2008-09-26 2014-04-22 Intellikine Llc Heterocyclic kinase inhibitors
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
BRPI0921433A2 (pt) 2008-10-31 2017-06-06 Abbott Biotherapeutics Corp uso de anticorpos anti-cs1 para o tratamento de linfomas raros
US9107942B2 (en) 2008-10-31 2015-08-18 University Of Rochester Methods of diagnosing and treating fibrosis
US8476431B2 (en) 2008-11-03 2013-07-02 Itellikine LLC Benzoxazole kinase inhibitors and methods of use
WO2010056758A1 (en) 2008-11-12 2010-05-20 Yangbo Feng Quinazoline derivatives as kinase inhibitors
WO2010059593A1 (en) 2008-11-18 2010-05-27 Intellikine, Inc. Methods and compositions for treatment of ophthalmic conditions
KR101807319B1 (ko) 2008-11-22 2017-12-11 제넨테크, 인크. 유방암의 치료를 위한, 화학요법과 조합된 항-ｖｅｇｆ 항체의 용도
AU2009322187B2 (en) 2008-12-04 2015-02-19 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Phosphatidylinositol-3-kinase p110 delta-targeted drugs in the treatment of CNS disorders
CA2746220A1 (en) 2008-12-08 2010-07-08 Vm Pharma Llc Compositions of protein receptor tyrosine kinase inhibitors
EA021293B1 (ru) 2008-12-08 2015-05-29 Джилид Коннектикут, Инк. ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ ИМИДАЗОПИРАЗИНОВЫЕ ИНГИБИТОРЫ Syk, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ
US8450321B2 (en) 2008-12-08 2013-05-28 Gilead Connecticut, Inc. 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor
HUE025547T2 (en) 2008-12-19 2016-02-29 Boehringer Ingelheim Int Cyclic pyrimidine-4-carboxamides as CCR2 receptor antagonists for the treatment of inflammation, asthma and COPD
US20120046242A1 (en) 2008-12-24 2012-02-23 Massachusetts Institute Of Technology Molecular activators of the wnt/beta-catenin pathway
AU2010219097A1 (en) 2009-01-13 2011-08-04 Glaxo Group Limited Pyrimidinecarboxamide derivatives as inhibitors of SYK kinase
CA2749585A1 (en) 2009-01-13 2010-07-22 Van Andel Research Institute Methods of using substituted isoxazolo pyridinones as dissociated glucocorticoids
US8642602B2 (en) 2009-02-04 2014-02-04 University Of Georgia Research Foundation, Inc. Method of inhibiting fibrogenesis and treating fibrotic disease
WO2010092340A1 (en) 2009-02-13 2010-08-19 Ucb Pharma S.A. Fused pyridine and pyrazine derivatives as kinase inhibitors
JP5603883B2 (ja) 2009-02-17 2014-10-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｂ−Ｒａｆキナーゼを阻害するためのピリミドピリミジン誘導体
EP2399136B1 (en) 2009-02-20 2016-06-22 Sunyoung Kim Protein structural biomarkers to guide targeted chemotherapies
US8591943B2 (en) 2009-04-09 2013-11-26 Merck Sharp & Dohme Corp. Pyrazolo[1,5-a]pyrimidine derivatives as mTOR inhibitors
WO2010127208A1 (en) 2009-04-30 2010-11-04 Forest Laboratories Holdings Limited Inhibitors of acetyl-coa carboxylase
EP2427195B1 (en) 2009-05-07 2019-05-01 Intellikine, LLC Heterocyclic compounds and uses thereof
GB0908957D0 (en) 2009-05-22 2009-07-01 Ucb Pharma Sa Therapeutic agents
CA2772371A1 (en) 2009-05-27 2010-12-02 F. Hoffmann-La Roche Ag Bicyclic indole-pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use
CN102459272B (zh) 2009-05-27 2014-08-06 健泰科生物技术公司 对P110δ具有选择性的为PI3K抑制剂的二环嘧啶化合物和使用方法
WO2010141275A1 (en) 2009-06-01 2010-12-09 Merck Sharp & Dohme Corp. Pyrazine carboxamide orexin receptor antagonists
WO2010147898A2 (en) 2009-06-15 2010-12-23 Rigel Pharmaceuticals, Inc. Small molecule inhibitors of spleen tyrosine kinase (syk)
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
CN101602768B (zh) 2009-07-17 2012-05-30 河南省农科院农副产品加工研究所 一种芝麻素和芝麻林素的提纯方法
JP2013501002A (ja) 2009-07-30 2013-01-10 アイアールエム・リミテッド・ライアビリティ・カンパニー Ｓｙｋキナーゼ阻害剤としての化合物および組成物
TW201105669A (en) 2009-07-30 2011-02-16 Irm Llc Compounds and compositions as Syk kinase inhibitors
EP2286808A1 (en) 2009-08-18 2011-02-23 Rheinische Friedrich-Wilhelms Universität Cytohesin inhibitors
TWI481601B (zh) 2009-08-21 2015-04-21 Otsuka Pharma Co Ltd 含氮化合物及藥學組成物
MX2012002366A (es) 2009-08-27 2012-03-29 Merck Sharp & Dohme Agonistas novedosos de receptores beta 3 andrenergicos derivados de pirrolidina.
US20130005802A1 (en) 2009-09-21 2013-01-03 Wei Chen Treatment of wnt/frizzled-related diseases
WO2011038163A1 (en) 2009-09-23 2011-03-31 Medivation Technologies, Inc. Pyrido[3,4-b]indoles and methods of use
CA2773827A1 (en) 2009-09-25 2011-03-31 Vertex Pharmaceuticals Incorporated Methods for preparing pyrimidine derivatives useful as protein kinase inhibitors
KR20120081164A (ko) 2009-09-29 2012-07-18 엑스커버리 홀딩 컴퍼니 엘엘씨 Ｐｉ3ｋ(델타) 선택적 억제제
US8106146B2 (en) 2009-10-06 2012-01-31 Medtronic, Inc. Therapeutic polymers and methods of generation
WO2011047129A1 (en) 2009-10-15 2011-04-21 Southern Research Institute Treatment of neurodegenerative diseases, causation of memory enhancement, and assay for screening compounds for such
GB0918249D0 (en) 2009-10-19 2009-12-02 Respivert Ltd Compounds
EP2491030B1 (en) 2009-10-22 2015-07-15 Fibrotech Therapeutics PTY LTD Fused ring analogues of anti-fibrotic agents
EP2499144B1 (en) 2009-11-12 2013-10-23 UCB Pharma, S.A. Quinoline and quinoxaline derivatives as kinase inhibitors
WO2011058109A1 (en) 2009-11-12 2011-05-19 Ucb Pharma S.A. Fused bicyclic pyrrole and imidazole derivatives as kinase inhibitors
ES2520345T3 (es) 2009-11-12 2014-11-11 Ucb Pharma, S.A. Derivados de quinolina y quinoxalina en calidad de inhibidores de quinasa
US8735417B2 (en) 2009-12-17 2014-05-27 Merck Sharp & Dohme Corp. Aminopyrimidines as Syk inhibitors
WO2011075517A1 (en) 2009-12-17 2011-06-23 Merck Sharp & Dohme Corp. Aminopyrimidines as syk inhibitors
US8633313B2 (en) 2009-12-18 2014-01-21 Amgen Inc. Heterocyclic compounds and their uses
AU2010341573B2 (en) 2009-12-22 2016-10-13 Vertex Pharmaceuticals Incorporated Isoindolinone inhibitors of phosphatidylinositol 3-kinase
SG181857A1 (en) 2009-12-23 2012-07-30 Takeda Pharmaceutical Fused heteroaromatic pyrrolidinones as syk inhibitors
WO2011103016A2 (en) 2010-02-19 2011-08-25 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US8247436B2 (en) 2010-03-19 2012-08-21 Novartis Ag Pyridine and pyrazine derivative for the treatment of CF
DE102010013716A1 (de) 2010-03-31 2011-10-06 Rheinische Friedrich-Wilhelms-Universität Bonn Körperschaft des öffentlichen Rechts Verwendung von Cytohesin-Inhibitoren
GB201007203D0 (en) 2010-04-29 2010-06-16 Glaxo Group Ltd Novel compounds
EP2564340B1 (en) 2010-04-29 2020-01-08 The Regents of The University of California Pathway recognition algorithm using data integration on genomic models (paradigm)
CA2799579A1 (en) 2010-05-21 2011-11-24 Intellikine, Inc. Chemical compounds, compositions and methods for kinase modulation
WO2011150201A2 (en) 2010-05-27 2011-12-01 Ambit Biosciences Corporation Azolyl amide compounds and methods of use thereof
US20130210733A1 (en) 2010-06-17 2013-08-15 Cytokinetics, Inc. Methods of treating lung disease
US20130195843A1 (en) 2010-06-23 2013-08-01 British Columbia Cancer Agency Branch Biomarkers for Non-Hodgkin Lymphomas and Uses Thereof
CN103228141B (zh) 2010-09-03 2016-04-20 拜耳知识产权有限责任公司 取代的稠合的嘧啶酮和二氢嘧啶酮
AR082799A1 (es) 2010-09-08 2013-01-09 Ucb Pharma Sa Derivados de quinolina y quinoxalina como inhibidores de quinasa
BR112013005806B1 (pt) 2010-09-10 2022-05-10 Epizyme, Inc Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
EP2616442B8 (en) * 2010-09-14 2018-10-17 Exelixis, Inc. Inhibitors of pi3k-delta and methods of their use and manufacture
EP2619209A1 (en) 2010-09-24 2013-07-31 Gilead Calistoga LLC Atropisomers of pi3k-inhibiting compounds
WO2012054332A1 (en) 2010-10-18 2012-04-26 Millennium Pharmaceuticals, Inc. Substituted hydroxamic acids and uses thereof
UY33337A (es) 2010-10-18 2011-10-31 Respivert Ltd DERIVADOS SUSTITUIDOS DE 1H-PIRAZOL[ 3,4-d]PIRIMIDINA COMO INHIBIDORES DE LAS FOSFOINOSITIDA 3-QUINASAS
EP2635556B1 (en) 2010-11-01 2017-06-21 Portola Pharmaceuticals, Inc. Benzamides and nicotinamides as syk modulators
EP2635565A1 (en) 2010-11-04 2013-09-11 Amgen Inc. 5 -cyano-4, 6 -diaminopyrimidine or 6 -aminopurine derivatives as pi3k- delta inhibitors
JP2013545749A (ja) 2010-11-10 2013-12-26 インフィニティー ファーマシューティカルズ， インコーポレイテッド 複素環化合物及びその使用
WO2012065057A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Phosphatidylinositol 3-kinase inhibitors and methods of their use
WO2012065019A2 (en) 2010-11-12 2012-05-18 Exelixis, Inc. Pyridopyrimidinone inhibitors of p13k alpha
DK2649075T3 (en) 2010-12-08 2018-07-30 Us Health SUBSTITUTED PYRAZOLOPYRIMIDINES AS GLUCOCEREBROSIDASE ACTIVATORS
GB201021104D0 (en) 2010-12-13 2011-01-26 Univ Leuven Kath Novel compounds for the treatment of neurodegenerative diseases
TWI674262B (zh) 2011-01-10 2019-10-11 美商英菲尼提製藥股份有限公司 製備異喹啉酮之方法及異喹啉酮之固體形式
JP2012184225A (ja) 2011-02-18 2012-09-27 Otsuka Pharmaceut Co Ltd 医薬組成物
JP5940562B2 (ja) 2011-02-18 2016-06-29 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ イオンチャネルのモジュレーターとしてのクロマン−スピロ環式ピペリジンアミド
CA2827770A1 (en) 2011-02-25 2012-11-01 Takeda Pharmaceutical Company Limited N-substituted oxazinopteridines and oxazinopteridinones
JP5569437B2 (ja) 2011-03-09 2014-08-13 コニカミノルタ株式会社 光学フィルム及びそれを用いた偏光板、液晶表示装置
KR20140093610A (ko) 2011-04-21 2014-07-28 재단법인 한국파스퇴르연구소 소염 화합물
BR112013028430A2 (pt) 2011-05-04 2017-08-01 Merck Sharp & Dohme composto, composição farmacêutica, método para tratar uma doença ou condição mediada por tirosina quinase do baço (syk), e, uso de uma quantidade terapeuticamente eficiente do composto
CA2834164A1 (en) 2011-05-10 2012-11-15 Gilead Sciences, Inc. Fused benzoxazinones as ion channel modulators
JP2013010734A (ja) 2011-06-03 2013-01-17 Sumitomo Chemical Co Ltd Ｎ−置換ラクタム化合物の製造方法
WO2012177997A1 (en) 2011-06-22 2012-12-27 The General Hospital Corporation Treatment of proteinopathies
US8716297B2 (en) 2011-07-15 2014-05-06 Abbvie Inc. Chemical entities to be used for Wee1 inhibition for the treatment of cancer
MX2014000648A (es) * 2011-07-19 2014-09-25 Infinity Pharmaceuticals Inc Compuestos heterociclicos y sus usos.
KR20140075693A (ko) 2011-08-29 2014-06-19 인피니티 파마슈티칼스, 인코포레이티드 헤테로사이클릭 화합물 및 그의 용도
WO2013038381A1 (en) 2011-09-16 2013-03-21 Novartis Ag Pyridine/pyrazine amide derivatives
HK1199028A1 (en) 2011-09-30 2015-06-19 Kineta, Inc. Anti-viral compounds
JP2015027951A (ja) 2011-11-02 2015-02-12 日本農薬株式会社 フタルアミド誘導体及び該誘導体を含有する農園芸用殺虫剤並びにその使用方法
WO2013082540A1 (en) 2011-12-02 2013-06-06 Gilead Calistoga Llc Compositions and methods of treating a proliferative disease with a quinazolinone derivative
NZ628072A (en) 2012-03-13 2015-08-28 Respivert Ltd Crystalline pi3 kinase inhibitors
WO2013154870A1 (en) 2012-04-10 2013-10-17 Annji Pharmaceutical Co., Ltd. Histone deacetylases (hdacs) inhibitors
US8940742B2 (en) 2012-04-10 2015-01-27 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2013188432A2 (en) 2012-06-11 2013-12-19 New York University Asymmetric catalysts
EP2744830A4 (en) 2012-06-21 2015-06-17 Compugen Ltd LSR ANTIBODIES AND USES THEREOF FOR THE TREATMENT OF CANCER
US8828998B2 (en) 2012-06-25 2014-09-09 Infinity Pharmaceuticals, Inc. Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors
PT2891492T (pt) 2012-08-30 2022-12-13 Univ Tokyo Agente de controlo de endoparasitas
US20140120060A1 (en) 2012-11-01 2014-05-01 Infinity Pharmaceuticals, Inc. Treatment of rheumatoid arthritis and asthma using pi3 kinase inhibitors
US20140120083A1 (en) 2012-11-01 2014-05-01 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
JP2016505012A (ja) 2013-01-10 2016-02-18 ニンバス アイリス， インコーポレイテッド Ｉｒａｋ阻害剤およびその使用
US20140275082A1 (en) 2013-03-14 2014-09-18 Abbvie Inc. Apoptosis-inducing agents for the treatment of cancer and immune and autoimmune diseases
AU2014247953A1 (en) 2013-04-05 2015-11-12 Mitobridge, Inc. PPAR agonists
UY35675A (es) 2013-07-24 2015-02-27 Novartis Ag Derivados sustituidos de quinazolin-4-ona
SG10201802061TA (en) 2013-09-25 2018-05-30 Vertex Pharma A selective inhibitor of phosphatidylinositol 3-kinase-gamma
WO2015051241A1 (en) 2013-10-04 2015-04-09 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
MX2021012208A (es) 2013-10-04 2023-01-19 Infinity Pharmaceuticals Inc Compuestos heterocíclicos y usos de los mismos.
EA201691169A1 (ru) 2013-12-05 2016-09-30 Асерта Фарма Б.В. Терапевтическая комбинация ингибитора pi3k и ингибитора btk
TWI672297B (zh) 2013-12-18 2019-09-21 義大利商吉斯藥品公司 作為磷脂肌醇－３－激酶抑制劑之異唏衍生物
WO2015095601A1 (en) 2013-12-20 2015-06-25 Gilead Calistoga Llc Process methods for phosphatidylinositol 3-kinase inhibitors
NZ724368A (en) * 2014-03-19 2023-07-28 Infinity Pharmaceuticals Inc Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders
AU2015247817C1 (en) 2014-04-14 2022-02-10 Arvinas Operations, Inc. Imide-based modulators of proteolysis and associated methods of use
EP3197982B1 (de) 2014-09-24 2020-05-06 Merck Patent GmbH Materialien für organische elektrolumineszenzvorrichtungen
WO2016054491A1 (en) 2014-10-03 2016-04-07 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
WO2016057322A1 (en) 2014-10-08 2016-04-14 Salk Institute For Biological Studies Ppar agonists and methods of use thereof
US10144724B2 (en) 2015-07-22 2018-12-04 Araxes Pharma Llc Substituted quinazoline compounds and methods of use thereof
GB201513614D0 (en) 2015-07-31 2015-09-16 Univ College Cork Nat Univ Ie Compositions, compounds and methods and uses relating thereto
EP4585268A3 (en) * 2015-09-14 2025-10-15 Twelve Therapeutics, Inc. Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same
CN106632243B (zh) 2015-10-28 2019-03-15 华领医药技术（上海）有限公司 吡咯烷衍生物
JP7114076B2 (ja) 2015-12-22 2022-08-08 シャイ・セラピューティクス・エルエルシー がん及び炎症性疾患の処置のための化合物
US10759806B2 (en) 2016-03-17 2020-09-01 Infinity Pharmaceuticals, Inc. Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors
AU2017259654B2 (en) 2016-05-06 2020-02-27 Shanghai De Novo Pharmatech Co., Ltd. Benzazepine derivative, preparation method, pharmaceutical composition and use thereof
WO2017214269A1 (en) 2016-06-08 2017-12-14 Infinity Pharmaceuticals, Inc. Heterocyclic compounds and uses thereof
HUE059242T2 (hu) 2016-07-29 2022-11-28 Rapt Therapeutics Inc Azetidin-származékok mint kemokin receptor modulátorok és felhasználásuk
FI3922279T3 (fi) 2016-08-30 2025-02-04 Dana Farber Cancer Inst Inc Lääkkeenantokoostumuksia ja niiden käyttötapoja
US10246462B2 (en) 2016-09-09 2019-04-02 Flx Bio, Inc. Chemokine receptor modulators and uses thereof
US20180154142A1 (en) 2016-12-05 2018-06-07 Old Dominion University Research Foundation Methods and devices for treatment of tumors with nano-pulse stimulation
US11241500B2 (en) 2016-12-14 2022-02-08 Tarveda Therapeutics, Inc. HSP90-targeting conjugates and formulations thereof
US20190070166A1 (en) 2017-09-02 2019-03-07 Richard Postrel Optimized Method for Treating and Curing Arthritis, Diabetes, Multiple Sclerosis and Other Autoimmune Disease
CN108658937A (zh) 2017-03-28 2018-10-16 中国海洋大学 一种双环生物碱类化合物及其制备方法和应用
JP7514005B2 (ja) 2017-06-21 2024-07-10 シャイ・セラピューティクス・エルエルシー がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物
WO2018237007A1 (en) 2017-06-22 2018-12-27 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Inhibitors of phosphoinositide 3-kinase and histone deacetylase for treatment of cancer
CN111386264A (zh) 2017-07-31 2020-07-07 纽约市哥伦比亚大学理事会 用于治疗t-细胞急性淋巴细胞白血病的化合物、组合物和方法
US12144241B2 (en) 2017-09-05 2024-11-12 Samsung Electronics Co., Ltd. Organometallic compound, organic light-emitting device including the organometallic compound, and diagnostic composition including the organometallic compound
CN111868039A (zh) 2017-09-26 2020-10-30 加利福尼亚大学董事会 用于治疗癌症的组合物和方法
CN111971070A (zh) 2017-12-14 2020-11-20 塔弗达治疗有限公司 Hsp90-靶向缀合物及其制剂
CN108310384B (zh) 2018-02-05 2021-06-15 苏州大学 Pi3k抑制剂在制备治疗血小板数量减少相关疾病药物中的用途
WO2019200224A1 (en) 2018-04-13 2019-10-17 The Broad Institute, Inc. Synergistic drug combinations predicted from genomic features and single-agent response profiles
CN112292374B (zh) 2018-05-31 2023-01-03 信达生物制药(苏州)有限公司 一种新型磷酸肌醇3-激酶抑制剂及其制备方法和用途
KR20210040355A (ko) 2018-06-19 2021-04-13 바이오엔테크 유에스 인크. 네오항원 및 이의 용도
CA3106563A1 (en) 2018-07-26 2020-01-30 Atyr Pharma, Inc. Compositions and methods for treating nrp2-associated diseases
WO2020037069A1 (en) 2018-08-14 2020-02-20 Camp4 Therapeutics Corporation Methods of treating liver diseases
CN110833546B (zh) 2018-08-17 2022-06-28 中国科学院分子细胞科学卓越创新中心 通佐溴胺在治疗胃癌中的用途
KR20210087938A (ko) 2018-09-28 2021-07-13 이미지냅 인코포레이티드 Cd8 이미징 구조체 및 이의 사용 방법
WO2020072445A1 (en) 2018-10-01 2020-04-09 Verastem, Inc. Combination therapies
US20210355545A1 (en) 2018-10-15 2021-11-18 The Johns Hopkins University Methods and materials for assessing and treating cancer
TW202136261A (zh) 2018-10-31 2021-10-01 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
TWI721623B (zh) 2018-10-31 2021-03-11 美商基利科學股份有限公司 經取代之6-氮雜苯并咪唑化合物
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
CA3139416A1 (en) 2019-02-13 2020-08-20 Vasgene Therapeutics Inc Ephb4-ephrin b2 receptor ligand pair as a novel marker for the treatment of prostate cancer
WO2020172618A2 (en) 2019-02-21 2020-08-27 Bambu Vault Llc Remotely triggered therapy
US12440494B2 (en) 2019-02-25 2025-10-14 Albert Einstein College Of Medicine Compounds useful for inhibiting RAF dimers
EP3952870B1 (en) 2019-04-10 2025-09-24 Nanjing Zenshine Pharmaceuticals Co., Ltd. Phosphatidylinositol 3-kinase inhibitors
US11453681B2 (en) 2019-05-23 2022-09-27 Gilead Sciences, Inc. Substituted eneoxindoles and uses thereof
US20220324880A1 (en) 2019-06-10 2022-10-13 Kymara Therapeutics, Inc. Smarca inhibitors and uses thereof
WO2020257412A1 (en) 2019-06-19 2020-12-24 Orionis Biosciences, Inc. Combination therapy with cd13-targeted chimeric proteins or chimeric protein complexes
CN112194659A (zh) 2019-07-08 2021-01-08 浙江海正药业股份有限公司 炔类衍生物及其制备方法和用途
US20210017607A1 (en) 2019-07-18 2021-01-21 The University Of Chicago Methods of Predicting Responsiveness to Cancer Therapies
WO2021024191A2 (en) 2019-08-05 2021-02-11 Bristol-Myers Squibb Company Combination treatments with benzodiazepinone compounds and phosphoinositide 3-kinase pathway inhibitors for treating cancer
CN112409331B (zh) 2019-08-21 2024-02-20 上海翰森生物医药科技有限公司 杂环类衍生物抑制剂、其制备方法和应用
US20220348558A1 (en) 2019-09-05 2022-11-03 Wisconsin Alumni Research Foundation Inhibitors of encephalitic alphaviruses
CN112707905B (zh) 2019-10-25 2024-07-02 武汉誉祥医药科技有限公司 一种三并杂环化合物及其制备方法和用途
CA3151629A1 (en) 2019-11-07 2021-05-14 Laura E. BENJAMIN Classification of tumor microenvironments
CN115379851A (zh) 2019-11-07 2022-11-22 因斯瑞拜奥有限公司 使用生长因子抗体与非酪氨酸靶向激酶抑制剂的组合的方法和组合物
EP4073516A1 (en) 2019-12-09 2022-10-19 Celcuity Inc. Methods of treating cancer patients with ras node or rtk targeted therapeutic agents
KR20220119657A (ko) 2019-12-20 2022-08-30 리커리엄 아이피 홀딩스, 엘엘씨 조합
US12458630B2 (en) 2020-01-14 2025-11-04 The Regents Of The University Of California Combination therapy for cancer
EP4093406A4 (en) 2020-01-24 2024-02-28 Taiho Pharmaceutical Co., Ltd. IMPROVEMENT OF THE ANTI-TUMORAL ACTIVITY OF SHP2 INHIBITOR PYRIMIDINONE IN COMBINATION WITH NEW ANTI-CANCER DRUGS AGAINST CANCER
WO2021155580A1 (en) 2020-02-07 2021-08-12 Cothera Bioscience, Inc. Combination therapies and biomarkers for treating cancer
WO2021178595A2 (en) 2020-03-04 2021-09-10 Foundation Medicine, Inc. Bcor rearrangements and uses thereof
EP3875078A1 (en) 2020-03-06 2021-09-08 Dompe' Farmaceutici S.P.A. Compounds for the treatment of covid-19
WO2021207230A1 (en) 2020-04-06 2021-10-14 Verastem, Inc. Methods of treating cytokine release syndrome using a pi3k inhibitor
US11739101B2 (en) 2020-05-06 2023-08-29 Nurix Therapeutics, Inc. Bifunctional degraders of hematopoietic progenitor kinase and therapeutic uses thereof
WO2021242859A1 (en) 2020-05-27 2021-12-02 Duke University Compositions and methods for sensitizing acute myeloid leukemias to chemotherapy
CN112546025B (zh) 2020-12-09 2023-06-06 武汉理工大学 一种Ce6@CMCS-DSP-IPI549抗肿瘤纳米传递系统的制备方法
CN113143867B (zh) 2020-12-25 2023-09-26 武汉理工大学 一种cmcs-dsp-ipi549抗肿瘤纳米传递系统及其制备方法

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130029982A1 (en) * 2011-07-19 2013-01-31 Intellikine, Llc Heterocyclic compounds and uses thereof

Also Published As

Publication number Publication date
US20220372038A1 (en) 2022-11-24
SG10201902074UA (en) 2019-04-29
TW201605829A (zh) 2016-02-16
UA121104C2 (uk) 2020-04-10
PH12016500582B1 (en) 2023-06-30
BR112016007467B1 (pt) 2022-09-20
PT3052485T (pt) 2021-10-22
DK3052485T3 (da) 2021-10-11
PE20160685A1 (es) 2016-07-23
US10329299B2 (en) 2019-06-25
US12152032B2 (en) 2024-11-26
HUE057734T2 (hu) 2022-06-28
JP6466924B2 (ja) 2019-02-06
CL2016000783A1 (es) 2017-05-19
IL244818A0 (en) 2016-05-31
US9828377B2 (en) 2017-11-28
JP2016536283A (ja) 2016-11-24
EP3052485B1 (en) 2021-07-28
PL3052485T3 (pl) 2022-02-28
SG11201602445SA (en) 2016-04-28
ES2900806T3 (es) 2022-03-18
MX389256B (es) 2025-03-20
AU2014329392B2 (en) 2018-12-20
US20190367521A1 (en) 2019-12-05
BR112016007467A2 (pt) 2017-08-01
US20150111874A1 (en) 2015-04-23
MY175778A (en) 2020-07-08
WO2015051244A1 (en) 2015-04-09
NZ718430A (en) 2021-12-24
KR102365651B1 (ko) 2022-02-21
ZA201602220B (en) 2018-05-30
US20250171453A1 (en) 2025-05-29
MX2016004340A (es) 2016-08-08
KR20160068832A (ko) 2016-06-15
PH12016500582A1 (en) 2016-05-16
US20180044346A1 (en) 2018-02-15
EA201690713A1 (ru) 2016-08-31
EP3964507A1 (en) 2022-03-09
IL244818B (en) 2021-08-31
CN105793255A (zh) 2016-07-20
MX2021012208A (es) 2023-01-19
CN105793255B (zh) 2018-11-16
CY1124998T1 (el) 2023-01-05
US20150225410A1 (en) 2015-08-13
CA2925944C (en) 2023-01-10
EP3052485A1 (en) 2016-08-10
CA2925944A1 (en) 2015-04-09
US9359365B2 (en) 2016-06-07

Similar Documents

Publication Publication Date Title
TWI657085B (zh) 雜環化合物及其用途
US20240050437A1 (en) Heterocyclic compounds and uses thereof
US10941162B2 (en) Heterocyclic compounds and uses thereof
US9751888B2 (en) Heterocyclic compounds and uses thereof
TWI565709B (zh) 雜環化合物及其用途
US10919914B2 (en) Heterocyclic compounds and uses thereof
TW201311663A (zh) 雜環化合物及其用途
AU2014329392A1 (en) Heterocyclic compounds and uses thereof