[go: up one dir, main page]

TWI562992B - Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity - Google Patents

Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity

Info

Publication number
TWI562992B
TWI562992B TW104135940A TW104135940A TWI562992B TW I562992 B TWI562992 B TW I562992B TW 104135940 A TW104135940 A TW 104135940A TW 104135940 A TW104135940 A TW 104135940A TW I562992 B TWI562992 B TW I562992B
Authority
TW
Taiwan
Prior art keywords
inhibitors
pharmaceutical composition
kinase activity
indazole derivative
indazole
Prior art date
Application number
TW104135940A
Other languages
English (en)
Other versions
TW201604192A (zh
Inventor
Julie Nicole Hamblin
Paul Spencer Jones
Suzanne Elaine Keeling
Joelle Le
Charlotte Jane Mitchell
Nigel James Parr
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of TW201604192A publication Critical patent/TW201604192A/zh
Application granted granted Critical
Publication of TWI562992B publication Critical patent/TWI562992B/zh

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • 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
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Oncology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Cardiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Pregnancy & Childbirth (AREA)
TW104135940A 2009-04-30 2010-04-28 Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity TWI562992B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US17403309P 2009-04-30 2009-04-30

Publications (2)

Publication Number Publication Date
TW201604192A TW201604192A (zh) 2016-02-01
TWI562992B true TWI562992B (en) 2016-12-21

Family

ID=42225106

Family Applications (3)

Application Number Title Priority Date Filing Date
TW99113559A TWI466884B (zh) 2009-04-30 2010-04-28 6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑、其醫藥組合物及作為激酶活性抑制劑之用途
TW103127990A TWI516487B (zh) 2009-04-30 2010-04-28 新穎化合物、其醫藥組合物及作為激酶活性抑制劑之用途
TW104135940A TWI562992B (en) 2009-04-30 2010-04-28 Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity

Family Applications Before (2)

Application Number Title Priority Date Filing Date
TW99113559A TWI466884B (zh) 2009-04-30 2010-04-28 6-(1h-吲哚-4-基)-4-(5-{[4-(1-甲基乙基)-1-哌嗪基]甲基}-1,3-噁唑-2-基)-1h-吲唑、其醫藥組合物及作為激酶活性抑制劑之用途
TW103127990A TWI516487B (zh) 2009-04-30 2010-04-28 新穎化合物、其醫藥組合物及作為激酶活性抑制劑之用途

Country Status (39)

Country Link
US (14) US8575162B2 (zh)
EP (3) EP2899191B1 (zh)
JP (1) JP5570589B2 (zh)
KR (2) KR101679642B1 (zh)
CN (1) CN102459253B (zh)
AR (2) AR076435A1 (zh)
AU (1) AU2010243613B2 (zh)
BR (1) BRPI1016219B8 (zh)
CA (1) CA2759476C (zh)
CL (1) CL2011002706A1 (zh)
CO (1) CO6390057A2 (zh)
CR (1) CR20110603A (zh)
CY (1) CY1119515T1 (zh)
DK (2) DK2899191T3 (zh)
DO (1) DOP2011000328A (zh)
EA (1) EA021056B1 (zh)
ES (3) ES2531274T3 (zh)
HR (2) HRP20150173T1 (zh)
HU (1) HUE034724T2 (zh)
IL (1) IL215803A (zh)
JO (1) JO3025B1 (zh)
LT (1) LT2899191T (zh)
MA (1) MA33304B1 (zh)
ME (2) ME02053B (zh)
MX (1) MX2011011534A (zh)
MY (1) MY160454A (zh)
NZ (1) NZ596071A (zh)
PE (1) PE20120321A1 (zh)
PL (2) PL2899191T3 (zh)
PT (2) PT2899191T (zh)
RS (2) RS56433B1 (zh)
SG (2) SG175782A1 (zh)
SI (2) SI2424864T1 (zh)
SM (2) SMT201700481T1 (zh)
TW (3) TWI466884B (zh)
UA (1) UA101098C2 (zh)
UY (1) UY32585A (zh)
WO (1) WO2010125082A1 (zh)
ZA (1) ZA201107878B (zh)

Families Citing this family (77)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009147190A1 (en) * 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
EP2300437B1 (en) * 2008-06-05 2013-11-20 Glaxo Group Limited Benzpyrazol derivatives as inhibitors of pi3 kinases
ES2526966T3 (es) 2008-06-05 2015-01-19 Glaxo Group Limited Compuestos novedosos
WO2010102958A1 (en) 2009-03-09 2010-09-16 Glaxo Group Limited 4-oxadiazol-2 -yl- indazoles as inhibitors of p13 kinases
PL2899191T3 (pl) 2009-04-30 2018-01-31 Glaxo Group Ltd Indazole podstawione oksazolem jako inhibitory kinazy PI3
CN102372675B (zh) * 2010-08-14 2013-12-18 王娜 6-氯-4-碘吲唑及其制备方法与应用
US9102668B2 (en) * 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
HUE026059T2 (en) * 2010-09-08 2016-05-30 Glaxosmithkline Ip Dev Ltd N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazol-6-yl ] Polymorphs and salts of 2 - (methyloxy) -3-pyridinyl] methanesulfonamide
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
GB201018124D0 (en) * 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
EP2638014B1 (en) * 2010-11-08 2017-01-04 Lycera Corporation N-sulfonylated tetrahydroquinolines and related bicyclic compounds for inhibition of ror-gamma activity and the treatment of diseases
ES2661510T3 (es) 2011-12-15 2018-04-02 Novartis Ag Uso de inhibidores de la actividad o función de PI3K
JP6242868B2 (ja) 2012-05-08 2017-12-06 リセラ・コーポレイションＬｙｃｅｒａ Ｃｏｒｐｏｒａｔｉｏｎ ＲＯＲγのアゴニストとしての使用のためおよび疾患の処置のためのテトラヒドロ［１，８］ナフチリジンスルホンアミドおよび関連化合物
RU2014149136A (ru) 2012-05-08 2016-07-10 Мерк Шарп И Доум Корп. ТЕТРАГИДРОНАФТИРИДИНОВЫЕ И РОДСТВЕННЫЕ БИЦИКЛИЧЕСКИЕ СОЕДИНЕНИЯ ДЛЯ ИНГИБИРОВАНИЯ RORγ АКТИВНОСТИ И ЛЕЧЕНИЯ ЗАБОЛЕВАНИЯ
AU2013290361A1 (en) 2012-07-16 2015-02-05 Neuropore Therapies, Inc. Di-and tri-heteroaryl derivatives as inhibitors of protein aggregation
EP2914260A1 (en) 2012-10-31 2015-09-09 INSERM (Institut National de la Santé et de la Recherche Médicale) Methods for preventing antiphospholipid syndrome (aps)
JPWO2014098232A1 (ja) * 2012-12-21 2017-01-12 学校法人東京理科大学 Ｐｉ３キナーゼ阻害剤を含む医薬組成物、ビタミンｄ受容体に作用する化合物を含む医薬組成物、凍結乾燥組成物、凍結乾燥組成物の製造方法、及び経肺投与用医薬組成物
WO2015055691A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
CA2923995A1 (en) * 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
WO2015095792A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Carbamate benzoxaxine propionic acids and acid derivatives for modulation of rorgamma activity and the treatment of disease
WO2015095795A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. TETRAHYDRONAPHTHYRIDINE, BENZOXAZINE, AZA-BENZOXAZINE, AND RELATED BICYCLIC COMPOUNDS FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
WO2015095788A1 (en) 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. 2-ACYLAMIDOMETHYL AND SULFONYLAMIDOMETHYL BENZOXAZINE CARBAMATES FOR INHIBITION OF RORgamma ACTIVITY AND THE TREATMENT OF DISEASE
US20160376240A1 (en) * 2014-01-24 2016-12-29 Abbvie Inc. 6 Phenyl or 6 Pyridin 3 YL Indazole Derivatives and Methods of Use
US10532088B2 (en) 2014-02-27 2020-01-14 Lycera Corporation Adoptive cellular therapy using an agonist of retinoic acid receptor-related orphan receptor gamma and related therapeutic methods
US10952889B2 (en) 2016-06-02 2021-03-23 Purewick Corporation Using wicking material to collect liquid for transport
US11806266B2 (en) 2014-03-19 2023-11-07 Purewick Corporation Apparatus and methods for receiving discharged urine
US11376152B2 (en) 2014-03-19 2022-07-05 Purewick Corporation Apparatus and methods for receiving discharged urine
US10226376B2 (en) 2014-03-19 2019-03-12 Purewick Corporation Apparatus and methods for receiving discharged urine
US10390989B2 (en) 2014-03-19 2019-08-27 Purewick Corporation Apparatus and methods for receiving discharged urine
US9896441B2 (en) 2014-05-05 2018-02-20 Lycera Corporation Tetrahydroquinoline sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
US10189777B2 (en) 2014-05-05 2019-01-29 Lycera Corporation Benzenesulfonamido and related compounds for use as agonists of RORγ and the treatment of disease
US9127069B1 (en) * 2014-06-11 2015-09-08 Antecip Bioventures LLC Compositions comprising rank/rankl antagonists and related compounds for treating pain
CN104086538B (zh) * 2014-06-13 2016-07-06 南京药石科技股份有限公司 一种pi3k激酶抑制剂的中间体及其制备方法与应用
WO2016059220A1 (en) 2014-10-16 2016-04-21 INSERM (Institut National de la Santé et de la Recherche Médicale) Tcr-activating agents for use in the treatment of t-all
CA2975997A1 (en) 2015-02-11 2016-08-18 Merck Sharp & Dohme Corp. Substituted pyrazole compounds as rorgammat inhibitors and uses thereof
US10421751B2 (en) 2015-05-05 2019-09-24 Lycera Corporation Dihydro-2H-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of RORγ and the treatment of disease
GB201509492D0 (en) * 2015-06-02 2015-07-15 Glaxosmithkline Ip Dev Ltd Novel processes
WO2016201225A1 (en) 2015-06-11 2016-12-15 Lycera Corporation Aryl dihydro-2h-benzo[b][1,4]oxazine sulfonamide and related compounds for use as agonists of rory and the treatment of disease
US10287272B2 (en) 2015-10-27 2019-05-14 Merck Sharp & Dohme Corp. Substituted indazole compounds as RORgammaT inhibitors and uses thereof
EP3368535B1 (en) 2015-10-27 2020-12-02 Merck Sharp & Dohme Corp. Heteroaryl substituted benzoic acids as rorgammat inhibitors and uses thereof
WO2017075178A1 (en) 2015-10-27 2017-05-04 Merck Sharp & Dohme Corp. SUBSTITUTED BICYCLIC PYRAZOLE COMPOUNDS AS RORgammaT INHIBITORS AND USES THEREOF
KR102758609B1 (ko) * 2016-01-14 2025-01-22 주식회사 한독 A3 아데노신 수용체 길항 화합물, 그의 제조 방법 및 그의 의학적 용도
US10376406B2 (en) 2016-07-27 2019-08-13 Purewick Corporation Male urine collection device using wicking material
EP3497100A1 (en) * 2016-08-08 2019-06-19 GlaxoSmithKline Intellectual Property Development Limited Chemical compounds
WO2018144463A1 (en) 2017-01-31 2018-08-09 Purewick Corporation Apparatus and methods for receiving discharged urine
JP7072084B2 (ja) 2018-05-01 2022-05-19 ピュアウィック コーポレイション 流体収集装置、関連システム、及び関連方法
JP7129493B2 (ja) 2018-05-01 2022-09-01 ピュアウィック コーポレイション 流体収集デバイス、及び関連のシステム
JP7093852B2 (ja) 2018-05-01 2022-06-30 ピュアウィック コーポレイション 流体収集装置及びその使用方法
WO2021138414A1 (en) 2020-01-03 2021-07-08 Purewick Corporation Urine collection devices having a relatively wide portion and an elongated portion and related methods
WO2021195384A1 (en) 2020-03-26 2021-09-30 Purewick Corporation Multi-layered urine capture device and related methods
WO2021211801A1 (en) 2020-04-17 2021-10-21 Purewick Corporation Fluid collection assemblies including a fluid impermeable barrier having a sump and a base
US12465514B2 (en) 2020-04-17 2025-11-11 Purewick Corporation Fluid collection devices, systems, and methods securing a protruding portion in position for use
WO2021211599A1 (en) 2020-04-17 2021-10-21 Purewick Corporation Female external catheter devices having a urethral cup, and related systems and methods
US12491104B2 (en) 2020-04-20 2025-12-09 Purewick Corporation Fluid collection devices adjustable between a vacuum-based orientation and a gravity-based orientation, and related systems and methods
US12048643B2 (en) 2020-05-27 2024-07-30 Purewick Corporation Fluid collection assemblies including at least one inflation device and methods and systems of using the same
US12440371B2 (en) 2020-08-06 2025-10-14 Purewick Corporation Fluid collection system including a garment and a fluid collection device
US12350187B2 (en) 2020-08-11 2025-07-08 Purewick Corporation Fluid collection assemblies defining waist and leg openings
EP4210643A1 (en) 2020-09-09 2023-07-19 Purewick Corporation Fluid collection devices, systems, and methods
US11801186B2 (en) 2020-09-10 2023-10-31 Purewick Corporation Urine storage container handle and lid accessories
IL301285A (en) 2020-09-10 2023-05-01 Precirix N V A portion of an antibody against FAP
US12042423B2 (en) 2020-10-07 2024-07-23 Purewick Corporation Fluid collection systems including at least one tensioning element
US12440370B2 (en) 2020-10-21 2025-10-14 Purewick Corporation Apparatus with compressible casing for receiving discharged urine
US12208031B2 (en) 2020-10-21 2025-01-28 Purewick Corporation Adapters for fluid collection devices
US12257174B2 (en) 2020-10-21 2025-03-25 Purewick Corporation Fluid collection assemblies including at least one of a protrusion or at least one expandable material
US12048644B2 (en) 2020-11-03 2024-07-30 Purewick Corporation Apparatus for receiving discharged urine
US12268627B2 (en) 2021-01-06 2025-04-08 Purewick Corporation Fluid collection assemblies including at least one securement body
US12478499B2 (en) 2021-01-07 2025-11-25 Purewick Corporation Wheelchair securable urine collection systems and related methods
ES2975761T3 (es) 2021-01-19 2024-07-15 Purewick Corp Dispositivo de recogida de líquido de ajuste variable
CN116615162A (zh) 2021-02-26 2023-08-18 普奥维克有限公司 在管口与屏障之间具有储液槽的流体收集装置以及相关系统和方法
US12029677B2 (en) 2021-04-06 2024-07-09 Purewick Corporation Fluid collection devices having a collection bag, and related systems and methods
US12251333B2 (en) 2021-05-21 2025-03-18 Purewick Corporation Fluid collection assemblies including at least one inflation device and methods and systems of using the same
US12324767B2 (en) 2021-05-24 2025-06-10 Purewick Corporation Fluid collection assembly including a customizable external support and related methods
US12150885B2 (en) 2021-05-26 2024-11-26 Purewick Corporation Fluid collection system including a cleaning system and methods
US20250059172A1 (en) 2021-12-28 2025-02-20 Nippon Shinyaku Co., Ltd. Indazole compound and pharmaceutical
US20250129087A1 (en) * 2022-01-31 2025-04-24 Intra-Cellular Therapies, Inc. Salt crystals
WO2023203135A1 (en) 2022-04-22 2023-10-26 Precirix N.V. Improved radiolabelled antibody
WO2023213801A1 (en) 2022-05-02 2023-11-09 Precirix N.V. Pre-targeting

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200413379A (en) * 2002-09-30 2004-08-01 Bayer Ag Fused azole-pyrimidine derivatives
CN1816549A (zh) * 2003-05-02 2006-08-09 诺瓦提斯公司 磷脂酰肌醇3－激酶抑制剂
US20080032960A1 (en) * 2006-04-04 2008-02-07 Regents Of The University Of California PI3 kinase antagonists

Family Cites Families (149)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB9127376D0 (en) 1991-12-24 1992-02-19 Wellcome Found Amidino derivatives
HU225869B1 (en) 1992-04-02 2007-11-28 Smithkline Beecham Corp Compounds with antiallergic and antiinflammatory activity and pharmaceutical compns. contg. them
ATE191470T1 (de) 1994-06-15 2000-04-15 Wellcome Found Enzymhemmer
EP0820279B1 (en) 1995-04-14 2002-07-03 Smithkline Beecham Corporation Metered dose inhaler for albuterol
US5821243A (en) 1996-07-22 1998-10-13 Viropharma Incorporated Compounds compositions and methods for treating influenza
MY117948A (en) 1997-01-13 2004-08-30 Glaxo Group Ltd Nitride oxide synthase inhibitors.
DE19723722A1 (de) 1997-05-30 1998-12-10 Schering Ag Nichtsteroidale Gestagene
TW533865U (en) 1997-06-10 2003-05-21 Glaxo Group Ltd Dispenser for dispensing medicament and actuation indicating device
AU9281298A (en) 1997-10-01 1999-04-23 Kyowa Hakko Kogyo Co. Ltd. Benzodioxole derivatives
US6506766B1 (en) 1998-02-13 2003-01-14 Abbott Laboratories Glucocortiocoid-selective antinflammatory agents
JP2002506856A (ja) 1998-03-14 2002-03-05 ビイク グルデン ロンベルク ヒエーミツシエ フアブリーク ゲゼルシヤフト ミツト ベシユレンクテル ハフツング フタラジノンｐｄｅｉｉｉ／ｉｖ阻害剤
GB9811599D0 (en) 1998-05-30 1998-07-29 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6390291B1 (en) 1998-12-18 2002-05-21 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6352152B1 (en) 1998-12-18 2002-03-05 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6315112B1 (en) 1998-12-18 2001-11-13 Smithkline Beecham Corporation Method and package for storing a pressurized container containing a drug
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. Method and package for storing a pressurized container containing a drug
CN1353717A (zh) 1999-05-04 2002-06-12 莱加制药公司 四环黄体酮受体调节剂化合物及其方法
ES2165768B1 (es) 1999-07-14 2003-04-01 Almirall Prodesfarma Sa Nuevos derivados de quinuclidina y composiciones farmaceuticas que los contienen.
CO5180649A1 (es) 1999-09-01 2002-07-30 Abbott Lab Antagonistas de los receptores de los glucocorticoides para el tratamiento de la diabetes para el tratamiento de la diabetes
OA11558A (en) 1999-12-08 2004-06-03 Advanced Medicine Inc Beta 2-adrenergic receptor agonists.
KR100889426B1 (ko) 2000-08-05 2009-03-23 글락소 그룹 리미티드 항염증제로서의 6.알파.,9.알파.-디플루오로-17.알파.-'(2-푸라닐카르복실)옥시-11.베타.-히드록시-16.알파.-메틸-3-옥소-안드로스트-1,4-디엔-17-카르보티오산 ｓ-플루오로메틸 에스테르
NZ525056A (en) 2000-09-29 2004-11-26 Glaxo Group Ltd Morpholin-acetamide derivatives for the treatment of inflammatory diseases
GB0031179D0 (en) 2000-12-21 2001-01-31 Glaxo Group Ltd Nitric oxide synthase inhibitors
US6484903B2 (en) 2001-01-09 2002-11-26 Riverwood International Corporation Carton with an improved dispensing feature in combination with a unique handle
GB0103630D0 (en) 2001-02-14 2001-03-28 Glaxo Group Ltd Chemical compounds
WO2002067683A1 (en) 2001-02-26 2002-09-06 Merck & Co., Inc. Hiv protease inhibitors supported on cation exchange resins for oral administration
JP2004526720A (ja) 2001-03-08 2004-09-02 グラクソ　グループ　リミテッド βアドレナリン受容体のアゴニスト
ATE381537T1 (de) 2001-03-22 2008-01-15 Glaxo Group Ltd Formanilid-derivative als beta2-adrenorezeptor- agonisten
KR100863659B1 (ko) 2001-04-16 2008-10-15 미쓰비시 타나베 파마 코퍼레이션 질소-함유 헤테로시클릭 화합물 및 이를 포함하는 제약 조성물
AU2002253342B2 (en) 2001-04-30 2007-01-04 Glaxo Group Limited Novel anti-inflammatory androstane derivatives
JP2005500290A (ja) 2001-06-12 2005-01-06 グラクソ　グループ　リミテッド 抗炎症性の、１７β−カルボチオアートアンドロスタン誘導体である１７α複素環エステル
CA2452114C (en) 2001-06-26 2010-11-16 Takeda Chemical Industries, Ltd. Tgf-.beta. superfamily production/secretion promoter
AU2002326026B2 (en) 2001-09-14 2005-04-28 Glaxo Group Limited Phenethanolamine derivatives for treatment of respiratory diseases
WO2003042160A1 (en) 2001-11-13 2003-05-22 Theravance, Inc. Aryl aniline beta-2 adrenergic receptor agonists
WO2003051847A1 (en) 2001-12-19 2003-06-26 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
JP2005519897A (ja) 2002-01-14 2005-07-07 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド グルココルチコイドミメチックス、その製造方法、それを含む医薬製剤及びその使用
WO2003061651A1 (en) 2002-01-22 2003-07-31 The Regents Of The University Of California Non-steroidal ligands for the glucocorticoid receptor, compositions and uses thereof
TW200306819A (en) 2002-01-25 2003-12-01 Vertex Pharma Indazole compounds useful as protein kinase inhibitors
GB0204719D0 (en) 2002-02-28 2002-04-17 Glaxo Group Ltd Medicinal compounds
FR2836915B1 (fr) 2002-03-11 2008-01-11 Aventis Pharma Sa Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant
KR101022977B1 (ko) 2002-03-26 2011-03-18 베링거 인겔하임 파마슈티칼즈, 인코포레이티드 글루코코르티코이드 모사체, 이의 제조방법, 약제학적조성물 및 이의 용도
US7268152B2 (en) 2002-03-26 2007-09-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
DE10215316C1 (de) 2002-04-02 2003-12-18 Schering Ag Chinolin- und Isochinolin-Derivate, ein pharmazeutisches Mittel und ihre Verwendung als Entzündungshemmer
US7282591B2 (en) 2002-04-11 2007-10-16 Merck & Co., Inc. 1h-benzo{f}indazol-5-yl derivatives as selective glucocorticoid receptor modulators
ATE381535T1 (de) 2002-04-25 2008-01-15 Glaxo Group Ltd Phenethanolaminderivate
US7186864B2 (en) 2002-05-29 2007-03-06 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
US7074806B2 (en) 2002-06-06 2006-07-11 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
WO2004002480A1 (en) 2002-06-27 2004-01-08 Novo Nordisk A/S Novel glucagon antagonists/inverse agonists
BR0312575A (pt) 2002-07-08 2005-05-03 Pfizer Prod Inc Moduladores do receptor de glicocorticóides
AU2003251970A1 (en) 2002-07-18 2004-02-09 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
AR041508A1 (es) 2002-08-09 2005-05-18 Astra Ab Compuestos con actividad en los receptores de glutamato metabotropicos
US7074809B2 (en) 2002-08-09 2006-07-11 Astrazeneca Ab Compounds
IL166510A0 (en) 2002-08-09 2006-01-15 Nps Pharma Inc 1,2,4"oxadiazole as modulators of metabotropic glutamate receptor-5
US20040224986A1 (en) 2002-08-16 2004-11-11 Bart De Corte Piperidinyl targeting compounds that selectively bind integrins
DE60322713D1 (de) 2002-08-21 2008-09-18 Boehringer Ingelheim Pharma Substituierte dihydrochinoline als glucocorticoid-mmimetika,verfahren zu deren herstellung, pharmazeutische zubereitungen und deren verwendung
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
CN100387598C (zh) 2002-09-16 2008-05-14 葛兰素集团有限公司 吡唑并[3,4-b]吡啶化合物及其作为磷酸二酯酶抑制剂的用途
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
JP4520309B2 (ja) 2002-09-20 2010-08-04 メルク・シャープ・エンド・ドーム・コーポレイション 選択的糖質コルチコイド受容体調節剤としてのオクタヒドロ−２−Ｈ−ナフト［１，２−ｆ］インドール−４−カルボキサミド誘導体
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
JP2006506373A (ja) 2002-10-22 2006-02-23 グラクソ　グループ　リミテッド 医薬アリールエタノールアミン化合物
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
AU2003286143A1 (en) 2002-10-28 2004-05-13 Glaxo Group Limited Phenethanolamine derivative for the treatment of respiratory diseases
GB0225540D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
GB0225535D0 (en) 2002-11-01 2002-12-11 Glaxo Group Ltd Medicinal compounds
US7202257B2 (en) 2003-12-24 2007-04-10 Deciphera Pharmaceuticals, Llc Anti-inflammatory medicaments
TWI328009B (en) 2003-05-21 2010-08-01 Glaxo Group Ltd Quinoline derivatives as phosphodiesterase inhibitors
CA2528938A1 (en) 2003-06-13 2005-02-24 Zentaris Gmbh Compounds having inhibitive activity of phosphatidylinositol 3-kinase and methods of use thereof
GB0316290D0 (en) 2003-07-11 2003-08-13 Glaxo Group Ltd Novel compounds
US20050090529A1 (en) 2003-07-31 2005-04-28 Pfizer Inc 3,5 Disubstituted indazole compounds with nitrogen-bearing 5-membered heterocycles, pharmaceutical compositions, and methods for mediating or inhibiting cell proliferation
GB0320197D0 (en) * 2003-08-28 2003-10-01 Novartis Ag Organic compounds
TW200811172A (en) 2003-10-14 2008-03-01 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
CA2542609C (en) * 2003-10-15 2013-06-04 Ube Industries, Ltd. Novel indazole derivatives
CN1901958B (zh) 2003-11-03 2011-03-09 葛兰素集团有限公司 流体分配装置
TW200524577A (en) 2003-11-04 2005-08-01 Glaxo Group Ltd Muscarinic acetylcholine receptor antagonists
JP2007514704A (ja) 2003-12-19 2007-06-07 グラクソ　グループ　リミテッド ピラゾロ［３，４−ｂ］ピリジン化合物およびホスホジエステラーゼ阻害剤としてのその使用
WO2005077368A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077345A1 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Compounds for the treatment of gastro-esophageal reflux disease
CA2555311A1 (en) 2004-02-04 2005-08-18 Neurosearch A/S Diazabicyclic aryl derivatives as nicotinic acetylcholine receptor ligands
GB0405933D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
EP1735314A1 (en) 2004-03-16 2006-12-27 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compound, and its use as a pde4 inhibitor
PE20060259A1 (es) 2004-04-27 2006-03-25 Glaxo Group Ltd Compuestos de quinuclidina como antagonistas del receptor de acetilcolina muscarinico
WO2006012226A2 (en) 2004-06-24 2006-02-02 Incyte Corporation N-substituted piperidines and their use as pharmaceuticals
WO2006000401A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited Substituted oxazines as glucocorticoid receptor modulators
WO2006000398A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators
US20060013540A1 (en) 2004-07-19 2006-01-19 Chao Zhang Single fiber optical transceiver module
WO2006135383A2 (en) 2004-08-04 2006-12-21 Myriad Genetics, Inc. Indazoles
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
AU2005299018B2 (en) 2004-10-19 2011-07-07 F. Hoffmann-La Roche Ag Quinoline derivatives
KR20070097441A (ko) 2004-11-18 2007-10-04 인사이트 산 디에고 인코포레이티드 11-β 하이드록실 스테로이드 데하이드로게나제 유형 1의억제제 및 이를 사용하는 방법
US20060135540A1 (en) 2004-11-30 2006-06-22 Jack Lin PPAR active compounds
US20090124588A1 (en) 2005-01-10 2009-05-14 Glaxo Group Limited Androstane 17-Alpha-Carbonate for Use in the Treatment of Inflammatory and Allergic Conditions
WO2006072599A2 (en) 2005-01-10 2006-07-13 Glaxo Group Limited Androstane 17-alpha carbonate derivatives for use in the treatment of allergic and inflammatory conditions
US7728009B1 (en) 2005-02-18 2010-06-01 Neurogen Corporation Thiazole amides, imidazole amides and related analogues
EP1863913A2 (en) 2005-03-31 2007-12-12 Ronen Kahana Creating poultry and other animals resistant to viral disease
US20060264433A1 (en) 2005-05-23 2006-11-23 Backes Bradley J Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
TW200800946A (en) 2005-08-15 2008-01-01 Astrazeneca Ab Substituted piperazines as metabotropic glutamate receptor antagonists
CA2619881A1 (en) 2005-08-16 2007-02-22 Genzyme Corporation Chemokine receptor binding compounds
WO2007105637A1 (ja) 2006-03-10 2007-09-20 Ono Pharmaceutical Co., Ltd. 含窒素複素環誘導体およびそれらを有効成分とする薬剤
EP2007373A4 (en) 2006-03-29 2012-12-19 Foldrx Pharmaceuticals Inc INHIBITION OF ALPHA SYNUCLEINE TOXICITY
JP5255559B2 (ja) 2006-03-31 2013-08-07 アボット・ラボラトリーズ インダゾール化合物
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
WO2008016123A1 (en) 2006-08-03 2008-02-07 Takeda Pharmaceutical Company Limited GSK-3β INHIBITOR
WO2008020229A2 (en) 2006-08-17 2008-02-21 Astrazeneca Ab Antibacterial pyrrolecarboxamides
CN101541758A (zh) 2006-08-25 2009-09-23 艾博特公司 抑制trpv1的吲唑衍生物及其用途
US7948877B2 (en) * 2006-09-07 2011-05-24 Via Technologies, Inc. Systems and methods for packet forward control
EP2104671A2 (en) 2006-09-25 2009-09-30 Mutabilis SA Substituted heterocyclylcarbonylamino-acetic-acid-derivatives as inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
MX2009003185A (es) 2006-09-29 2009-04-03 Novartis Ag Pirazolopirimidinas como inhibidores de lipido cinasa pi3k.
TWI404532B (zh) 2006-11-02 2013-08-11 Targacept Inc 菸鹼乙醯膽鹼受體亞型選擇性之二氮雜雙環烷類醯胺
GB0701426D0 (en) 2007-01-25 2007-03-07 Univ Sheffield Compounds and their use
US8450348B2 (en) 2007-02-21 2013-05-28 Forma Tm, Llc Derivatives of squaric acid with anti-proliferative activity
JP2010116389A (ja) 2008-10-17 2010-05-27 Bayer Cropscience Ag 殺虫性アリールピロリジン類
GB0709031D0 (en) 2007-05-10 2007-06-20 Sareum Ltd Pharmaceutical compounds
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
WO2009000832A2 (en) 2007-06-25 2008-12-31 Boehringer Ingelheim International Gmbh Chemical compounds
EP2183229B1 (en) 2007-07-26 2012-04-18 Vitae Pharmaceuticals, Inc. Synthesis of inhibitors of 11beta-hydroxysteroid dehydrogenase type 1
WO2009042607A1 (en) 2007-09-24 2009-04-02 Genentech, Inc. Thiazolopyrimidine p13k inhibitor compounds and methods of use
JP2009127226A (ja) * 2007-11-21 2009-06-11 Seiji Ohara 温水プールに雪を落し込む手段を持つ融雪装置
CA2723039A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
CA2723034A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
ES2421537T3 (es) 2008-05-01 2013-09-03 Vitae Pharmaceuticals Inc Inhibidores cíclicos de la 11beta-hidroxiesteroide deshidrogenasa 1
JP5451752B2 (ja) 2008-05-01 2014-03-26 ヴァイティー ファーマシューティカルズ，インコーポレイテッド １１β−ヒドロキシステロイドデヒドロゲナーゼ１の環状インヒビター
EP2300437B1 (en) 2008-06-05 2013-11-20 Glaxo Group Limited Benzpyrazol derivatives as inhibitors of pi3 kinases
ES2526966T3 (es) 2008-06-05 2015-01-19 Glaxo Group Limited Compuestos novedosos
WO2009147187A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited 4-carboxamide indazole derivatives useful as inhibitors of p13-kinases
WO2009147190A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
JP5535652B2 (ja) 2008-06-11 2014-07-02 浜松ホトニクス株式会社 ガラス溶着方法
DK2324018T3 (da) 2008-07-25 2013-10-14 Boehringer Ingelheim Int Cykliske inhibitorer af 11 beta-hydroxysteroid dehydrogenase 1
US8245111B2 (en) * 2008-12-09 2012-08-14 Intel Corporation Performing multi-bit error correction on a cache line
US20110237633A1 (en) 2008-12-11 2011-09-29 Bijoy Panicker Small molecule modulators of hepatocyte growth factor (scatter factor) activity
US20120039905A1 (en) 2009-01-13 2012-02-16 The Babraham Institute The Role of p110 delta Signaling in Morbidity and Lung Pathology Induced by Influenza Virus Infection
WO2010102958A1 (en) 2009-03-09 2010-09-16 Glaxo Group Limited 4-oxadiazol-2 -yl- indazoles as inhibitors of p13 kinases
KR20120061771A (ko) 2009-04-30 2012-06-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
NZ595698A (en) 2009-04-30 2014-01-31 Abbvie Inc N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-ht6 receptor
US8343959B2 (en) 2009-04-30 2013-01-01 Abbott Gmbh & Co. Kg N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds suitable for treating disorders that respond to modulation of the serotonin 5-HT6 receptor
US8680093B2 (en) 2009-04-30 2014-03-25 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
PL2899191T3 (pl) * 2009-04-30 2018-01-31 Glaxo Group Ltd Indazole podstawione oksazolem jako inhibitory kinazy PI3
BRPI1014641A2 (pt) 2009-04-30 2019-09-24 Bayer Cropscience Ag arilpirrolidinas pesticidas
EP2507231A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Indazole derivatives as pi 3 - kinase inhibitors
WO2011067365A1 (en) 2009-12-03 2011-06-09 Glaxo Group Limited Benzpyrazole derivatives as inhibitors of p13 kinases
US20120238559A1 (en) 2009-12-03 2012-09-20 Glaxo Group Limited Novel compounds
US9102668B2 (en) 2010-09-08 2015-08-11 Glaxo Group Limited Polymorphs and salts
US9326987B2 (en) 2010-09-08 2016-05-03 Glaxo Group Limited Indazole derivatives for use in the treatment of influenza virus infection
HUE026059T2 (en) 2010-09-08 2016-05-30 Glaxosmithkline Ip Dev Ltd N- [5- [4- (5 - {[(2R, 6S) -2,6-dimethyl-4-morpholinyl] methyl} -1,3-oxazol-2-yl) -1H-indazol-6-yl ] Polymorphs and salts of 2 - (methyloxy) -3-pyridinyl] methanesulfonamide
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
US10642898B1 (en) * 2017-04-11 2020-05-05 Northrop Grumman Systems Corporation Three-dimensional graph

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW200413379A (en) * 2002-09-30 2004-08-01 Bayer Ag Fused azole-pyrimidine derivatives
CN1816549A (zh) * 2003-05-02 2006-08-09 诺瓦提斯公司 磷脂酰肌醇3－激酶抑制剂
US20080032960A1 (en) * 2006-04-04 2008-02-07 Regents Of The University Of California PI3 kinase antagonists

Also Published As

Publication number Publication date
US10624898B2 (en) 2020-04-21
EP2899191B1 (en) 2017-08-09
ES2876933T3 (es) 2021-11-15
EA021056B1 (ru) 2015-03-31
BRPI1016219B1 (pt) 2020-09-01
US20130131080A1 (en) 2013-05-23
EP2424864B1 (en) 2014-12-03
CN102459253A (zh) 2012-05-16
HUE034724T2 (hu) 2018-02-28
CL2011002706A1 (es) 2012-04-09
CO6390057A2 (es) 2012-02-29
DK2899191T3 (da) 2017-11-13
US20120046286A1 (en) 2012-02-23
HK1165801A1 (zh) 2012-10-12
SMT201700481T1 (it) 2017-11-15
PE20120321A1 (es) 2012-04-19
UA101098C2 (xx) 2013-02-25
BRPI1016219B8 (pt) 2021-05-25
US20190175608A1 (en) 2019-06-13
AU2010243613B2 (en) 2015-05-07
US20150328226A1 (en) 2015-11-19
KR20120079852A (ko) 2012-07-13
CY1119515T1 (el) 2018-03-07
US8609657B2 (en) 2013-12-17
US20190328744A1 (en) 2019-10-31
US10383879B2 (en) 2019-08-20
US20180325911A1 (en) 2018-11-15
PT2424864E (pt) 2015-02-27
KR101771193B1 (ko) 2017-09-05
CA2759476A1 (en) 2010-11-04
KR101679642B1 (ko) 2016-11-25
TW201444832A (zh) 2014-12-01
DK2424864T3 (en) 2015-02-23
SMT201500043B (it) 2015-05-05
US20170015656A1 (en) 2017-01-19
CA2759476C (en) 2018-10-09
US10946025B2 (en) 2021-03-16
HK1209102A1 (zh) 2016-03-24
CN102459253B (zh) 2015-03-25
MY160454A (en) 2017-03-15
SG175782A1 (en) 2011-12-29
ZA201107878B (en) 2013-04-24
AU2010243613A1 (en) 2011-11-17
SG10201401881QA (en) 2014-07-30
US20140080830A1 (en) 2014-03-20
NZ596071A (en) 2013-12-20
WO2010125082A1 (en) 2010-11-04
HRP20171450T1 (hr) 2017-11-17
EP2899191A1 (en) 2015-07-29
KR20160135852A (ko) 2016-11-28
US20130029985A1 (en) 2013-01-31
AR076435A1 (es) 2011-06-08
ES2644724T3 (es) 2017-11-30
MX2011011534A (es) 2012-02-28
EA201190227A1 (ru) 2012-05-30
DOP2011000328A (es) 2016-12-30
US20200206237A1 (en) 2020-07-02
JO3025B1 (ar) 2016-09-05
ME02053B (me) 2015-05-20
US20170157136A1 (en) 2017-06-08
ME02900B (me) 2018-04-20
TW201103927A (en) 2011-02-01
PL2424864T3 (pl) 2015-05-29
US8575162B2 (en) 2013-11-05
IL215803A0 (en) 2012-01-31
TWI466884B (zh) 2015-01-01
JP2012525349A (ja) 2012-10-22
EP3260453A1 (en) 2017-12-27
JP5570589B2 (ja) 2014-08-13
AR108388A2 (es) 2018-08-15
US20130096117A1 (en) 2013-04-18
MA33304B1 (fr) 2012-05-02
IL215803A (en) 2014-11-30
US8586583B2 (en) 2013-11-19
ES2531274T3 (es) 2015-03-12
EP2424864A1 (en) 2012-03-07
EP3260453B1 (en) 2021-03-31
US20100280045A1 (en) 2010-11-04
US20100280029A1 (en) 2010-11-04
BRPI1016219A2 (pt) 2016-04-26
RS53830B1 (sr) 2015-06-30
US8580797B2 (en) 2013-11-12
HRP20150173T1 (hr) 2015-05-22
UY32585A (es) 2010-11-30
SI2899191T1 (sl) 2017-11-30
LT2899191T (lt) 2017-10-25
RS56433B1 (sr) 2018-01-31
TWI516487B (zh) 2016-01-11
TW201604192A (zh) 2016-02-01
CR20110603A (es) 2012-02-28
SI2424864T1 (sl) 2015-03-31
PT2899191T (pt) 2017-11-14
US8586590B2 (en) 2013-11-19
PL2899191T3 (pl) 2018-01-31

Similar Documents

Publication Publication Date Title
TWI562992B (en) Indazole derivative, pharmaceutical composition thereof, and use thereof as inhibitors of kinase activity
HUS2000049I1 (hu) Kináz aktivitással rendelkezõ helyettesített imidazol származékok
IL210843A0 (en) Certain kynurenine-3-monooxygenase inhibitors, pharmaceutical compositions, and methods of use thereof
IL214822A0 (en) Substituted azoanthracene derivatives, pharmaceutical compositions, and methods of use thereof
IL216132A (en) Heterocyclic carboxamide diamine compounds, their uses and their medicinal products and inhibitors
ZA201206223B (en) Certain kynurenine-3-monooxygenase inhibitors,pharmaceutical compositions, and methods of use thereof
IL220863A (en) Oxazole derivatives of kinase inhibitors, medicinal preparations containing them and their uses
ZA201008387B (en) Azacarboline derivatives,preparation thereof,and therapeutic use thereof as kinase inhibitors
IL219646A0 (en) Novelnaphthyridine derivatives and the use thereof as kinase inhibitors
IL216741A0 (en) 1,3-disubstituted imidazolidin-2-one derivatives as inhibitors of cyp 17
ZA201101586B (en) Aminotriazolopyridines and their use as kinase inhibitors
IL214175A (en) Derivatives of aminotetralin, their pharmaceutical compositions and their use
SG10201506114UA (en) Pharmaceutical formulations comprising 1 - (beta-d-glucopyranosyl) - 2 -thienylmethylbenzene derivatives as inhibitors of sglt
IL216113A (en) Processed derivatives of indazole and azaza-indazole, pharmaceutical preparations containing them and their uses
IL212755A0 (en) Pyrazinopyrazines and derivatives as kinase inhibitors
SI2242740T1 (sl) SF5-derivati kot PAR1 inhibitorji, njihova priprava in uporaba kot zdravila
PT2448927E (pt) Novos derivados de (6-oxo-1,6-di-hidro-pirimidin-2-il)-amida, sua preparação e sua utilização farmacêutica como inibidores da fosforilação de akt
IL220586A (en) Carboxamide compound, a pharmaceutical composition containing it and its use
IL207205A0 (en) Triazolopyridazines as par1 inhibitors, their preparation and use as medicaments
EP2320738A4 (en) SUBSTITUTED AMINOTHIAZOL DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF AND USE THEREOF
ZA201306905B (en) Novel octahydrothienoquinonline derivative,pharmaceutical composition comprising derivative, and use of these
EP2424533A4 (en) SUBSTITUTED ISOQUINOLINE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND THEIR METHODS OF USE AS-SECRETASE INHIBITORS
IL214408A0 (en) Derivatives of 6-(6-substituted-triazolopyidazine-sulfanyl) 5-fluoro-benzothiazoles and 5-fluoro-benzimidazoles, preparation thereof, use thereof as drugs, and use thereof as met inhibitors
PL2484661T3 (pl) Pochodna 2,3-dihydro-1h-inden-2-ylomocznika i jej zastosowanie farmaceutyczne
HK1177101A (zh) 某些犬尿氨酸-3-單加氧酶抑製劑、藥劑學組合物、和其用法

Legal Events

Date Code Title Description
MM4A Annulment or lapse of patent due to non-payment of fees