HRP20182059T1 - Polimorfi i soli 6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazola kao inhibitori pi3k, namijenjeni upotrebi u liječenju, primjerice, dišnih poremećaja - Google Patents

Polimorfi i soli 6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazola kao inhibitori pi3k, namijenjeni upotrebi u liječenju, primjerice, dišnih poremećaja

Info

Publication number
HRP20182059T1
HRP20182059T1 HRP20182059TT HRP20182059T HRP20182059T1 HR P20182059 T1 HRP20182059 T1 HR P20182059T1 HR P20182059T T HRP20182059T T HR P20182059TT HR P20182059 T HRP20182059 T HR P20182059T HR P20182059 T1 HRP20182059 T1 HR P20182059T1
Authority
HR
Croatia
Prior art keywords
oxazol
indazole
polymorphs
indol
methylethyl
Prior art date
Application number
HRP20182059TT
Other languages
English (en)
Inventor
Julie Nicole Hamblin
Paul Spencer Jones
Suzanne Elaine Keeling
Joelle Le
Nigel James Parr
Robert David Willacy
Original Assignee
Glaxo Group Limited
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 Limited filed Critical Glaxo Group Limited
Publication of HRP20182059T1 publication Critical patent/HRP20182059T1/hr

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/06Antiasthmatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
HRP20182059TT 2010-10-27 2018-12-06 Polimorfi i soli 6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazola kao inhibitori pi3k, namijenjeni upotrebi u liječenju, primjerice, dišnih poremećaja HRP20182059T1 (hr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1018124.6A GB201018124D0 (en) 2010-10-27 2010-10-27 Polymorphs and salts
EP11776738.4A EP2632921B1 (en) 2010-10-27 2011-10-25 Polymorphs and salts of 6-(1h-indol-4-yl)-4-(5-{[4-(1-methylethyl)-1-piperazinyl]methyl}-1,3-oxazol-2-yl)-1h-indazole as pi3k inhibitors for use in the treatment of e.g. respiratory disorders
PCT/EP2011/068604 WO2012055846A1 (en) 2010-10-27 2011-10-25 Polymorphs and salts of 6-(1h-indol-4-yl)-4-(5- { [4-(1-methylethyl)-1-pi perazinyl] methyl} -1,3-oxazol-2-yl)-1h-indazole as pi3k inhibitors for use in the treatment of e.g. respiratory disorders

Publications (1)

Publication Number Publication Date
HRP20182059T1 true HRP20182059T1 (hr) 2019-02-08

Family

ID=43365584

Family Applications (1)

Application Number Title Priority Date Filing Date
HRP20182059TT HRP20182059T1 (hr) 2010-10-27 2018-12-06 Polimorfi i soli 6-(1h-indol-4-il)-4-(5-{[4-(1-metiletil)-1-piperazinil]metil}-1,3-oksazol-2-il)-1h-indazola kao inhibitori pi3k, namijenjeni upotrebi u liječenju, primjerice, dišnih poremećaja

Country Status (26)

Country Link
US (1) US8993576B2 (hr)
EP (2) EP2632921B1 (hr)
JP (1) JP5894603B2 (hr)
KR (1) KR101774026B1 (hr)
CN (1) CN103270037B (hr)
AU (1) AU2011322649B2 (hr)
BR (1) BR112013010126B1 (hr)
CA (1) CA2814436C (hr)
CY (1) CY1121248T1 (hr)
DK (1) DK2632921T3 (hr)
EA (1) EA022872B1 (hr)
ES (1) ES2703716T3 (hr)
GB (1) GB201018124D0 (hr)
HR (1) HRP20182059T1 (hr)
HU (1) HUE042754T2 (hr)
IL (1) IL225704A (hr)
LT (1) LT2632921T (hr)
MX (1) MX347619B (hr)
PL (1) PL2632921T3 (hr)
PT (1) PT2632921T (hr)
RS (1) RS58072B1 (hr)
SG (1) SG189179A1 (hr)
SI (1) SI2632921T1 (hr)
TR (1) TR201819939T4 (hr)
WO (1) WO2012055846A1 (hr)
ZA (1) ZA201302480B (hr)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5502077B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド 新規な化合物
WO2009147189A1 (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
JP5656880B2 (ja) 2009-03-09 2015-01-21 グラクソ グループ リミテッドGlaxo Group Limited Pi3キナーゼの阻害剤としての4−オキサジアゾール−2−イル−インダゾール
DK2899191T3 (da) 2009-04-30 2017-11-13 Glaxo Group Ltd Oxazol-substituerede indazoler som pi3-kinaseinhibitorer
JP5876051B2 (ja) * 2010-09-08 2016-03-02 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited インフルエンザウィルス感染の治療に使用するためのインダゾール誘導体
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts
CA2880178C (en) * 2012-07-27 2021-10-26 Sato Pharmaceutical Co., Ltd. Difluoromethylene compound
CN104870017B (zh) 2012-11-08 2020-08-14 理森制药股份公司 含有PDE4抑制剂和PI3δ或双重PI3δ-γ激酶抑制剂的药物组合物
JP6475707B2 (ja) * 2013-10-17 2019-02-27 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited 呼吸器疾患の治療のためのpi3k阻害剤
CA2923995A1 (en) 2013-10-17 2015-04-23 Glaxosmithkline Intellectual Property Development Limited Pi3k inhibitor for treatment of respiratory disease
GB201509492D0 (en) * 2015-06-02 2015-07-15 Glaxosmithkline Ip Dev Ltd Novel processes

Family Cites Families (138)

* 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
US5552438A (en) 1992-04-02 1996-09-03 Smithkline Beecham Corporation Compounds useful for treating allergic and inflammatory diseases
US5889056A (en) 1994-06-15 1999-03-30 Glaxo Wellsome Inc. Enzyme inhibitors
CA2361954C (en) 1995-04-14 2003-07-08 Smithkline Beecham Corporation Metered dose inhaler for albuterol
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
US6255303B1 (en) 1998-03-14 2001-07-03 Byk Gulden Lomberg Chemische Fabrik Gmbh Phthalazinone PDE III/IV inhibitors
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
US6119853A (en) 1998-12-18 2000-09-19 Glaxo Wellcome Inc. 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
CA2371273A1 (en) 1999-05-04 2000-11-09 Andrew Fensome Tetracyclic progesterone receptor modulator compounds and methods
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.
EP1305329B2 (en) 2000-08-05 2015-03-18 Glaxo Group Limited 6.alpha.,9.alpha.-difluoro-17.alpha.-(2-furanylcarboxyl)oxy-11.beta.-hydroxy-16.alpha.-methyl-3-oxo-androst-1,4-diene-17-carbothioic acid s-fluoromethyl ester as an anti-inflammatory agent
CN1678594A (zh) 2000-09-29 2005-10-05 葛兰素集团有限公司 用于治疗炎性疾病的吗啉-乙酰胺衍生物
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
ATE365720T1 (de) 2001-03-08 2007-07-15 Glaxo Group Ltd Agonisten von beta-adrenorezeptoren
ATE381537T1 (de) 2001-03-22 2008-01-15 Glaxo Group Ltd Formanilid-derivative als beta2-adrenorezeptor- agonisten
BR0208956A (pt) 2001-04-16 2004-07-13 Tanabe Seiyaku Co Abridor de canais de k ativados por cálcio de grande condutância
BR0209271A (pt) 2001-04-30 2004-06-15 Glaxo Group Ltd Composto, uso de um composto composição farmacêutica, formulação em aerossol farmacêutica, método para o tratamento de um paciente humano ou animal com uma condição inflamatória e/ou alérgica, e, processo para a preparação de um composto
US20040248867A1 (en) 2001-06-12 2004-12-09 Keith Biggadike Novel anti-inflammatory 17.alpha.-heterocyclic-esters of 17.beta.carbothioate androstane derivatives
CA2452114C (en) 2001-06-26 2010-11-16 Takeda Chemical Industries, Ltd. Tgf-.beta. superfamily production/secretion promoter
SI1425001T1 (sl) 2001-09-14 2009-04-30 Glaxo Group Ltd Glaxo Welcome Fenetanolaminski derivati za zdravljenje respiratornih bolezni
US6653323B2 (en) 2001-11-13 2003-11-25 Theravance, Inc. Aryl aniline β2 adrenergic receptor agonists
AU2002353186A1 (en) 2001-12-19 2003-06-30 Smithkline Beecham P.L.C. (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors
CA2472746A1 (en) 2002-01-14 2003-07-24 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof
AU2003214879B2 (en) 2002-01-22 2008-02-07 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
ES2298508T3 (es) 2002-03-26 2008-05-16 Boehringer Ingelheim Pharmaceuticals Inc. Mimeticos de glucocorticoides, metodos para prepararlos, composiciones farmaceuticas y sus usos.
CA2477764A1 (en) 2002-03-26 2003-10-09 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
DE60335869D1 (de) 2002-04-11 2011-03-10 Merck Sharp & Dohme 1h-benzo(f)indazol-5-yl-derivate als selektive glucocorticoid-rezeptor-modulatoren
EP1497261B1 (en) 2002-04-25 2007-12-19 Glaxo Group Limited Phenethanolamine derivatives
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
PT1521733E (pt) 2002-07-08 2014-10-29 Pfizer Prod Inc Moduladores do recetor de glucocorticoides
WO2004009017A2 (en) 2002-07-18 2004-01-29 Bristol-Myers Squibb Company Modulators of the glucocorticoid receptor and method
GB0217225D0 (en) 2002-07-25 2002-09-04 Glaxo Group Ltd Medicinal compounds
EP1581525A2 (en) 2002-08-09 2005-10-05 AstraZeneca AB Compounds having an activity at metabotropic glutamate receptors
EP1536790A2 (en) 2002-08-09 2005-06-08 AstraZeneca AB Oxadiazoles as modulators of metabotropic glutamate receptor-5
WO2004014881A2 (en) 2002-08-09 2004-02-19 Astra Zeneca Ab '1,2,4'oxadiazoles 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
CA2496175A1 (en) 2002-08-21 2004-03-04 Boehringer Ingelheim Pharmaceuticals, Inc. Substituted hihydroquinolines as glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof
GB0220730D0 (en) 2002-09-06 2002-10-16 Glaxo Group Ltd Medicinal compounds
PL375993A1 (en) 2002-09-16 2005-12-12 Glaxo Group Limited Pyrazolo[3,4-b]pyridine compounds, and their use as phosphodiesterase inhibitors
GB0230045D0 (en) 2002-12-23 2003-01-29 Glaxo Group Ltd Compounds
AU2003270783C1 (en) 2002-09-20 2010-05-20 Merck Sharp & Dohme Corp. Octahydro-2-H-naphtho[1,2-F] indole-4-carboxamide derivatives as selective glucocorticoid receptor modulators
GB0224084D0 (en) 2002-10-16 2002-11-27 Glaxo Group Ltd Novel compounds
AU2003298094A1 (en) 2002-10-22 2004-05-13 Glaxo Group Limited Medicinal arylethanolamine compounds
ATE390407T1 (de) 2002-10-28 2008-04-15 Glaxo Group Ltd Phenethanolamin-derivate zur behandlung von atemwegserkrankungen
GB0225030D0 (en) 2002-10-28 2002-12-04 Glaxo Group Ltd Medicinal compounds
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
AU2004264834A1 (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
NZ556424A (en) 2003-10-14 2008-12-24 Glaxo Group Ltd Muscarinic Acetylcholine receptor antagonists
CN1863779B (zh) 2003-10-15 2010-05-05 宇部兴产株式会社 吲唑衍生物
EP1699512B1 (en) 2003-11-03 2012-06-20 Glaxo Group Limited A fluid dispensing device
PE20050489A1 (es) 2003-11-04 2005-09-02 Glaxo Group Ltd Antagonistas de receptores de acetilcolina muscarinicos
US20070111995A1 (en) 2003-12-19 2007-05-17 Allen David G Pyrazolo [3,4-B] pyridine Compounds and Their Use as Phosphodiesterase Inhibitors
WO2005077373A2 (en) 2004-02-03 2005-08-25 Astrazeneca Ab Treatment of gastro-esophageal reflux disease (gerd)
WO2005077368A2 (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
JP2007520527A (ja) 2004-02-04 2007-07-26 ノイロサーチ アクティーゼルスカブ ニコチン性アセチルコリン受容体リガンドとしてのジアザ2環式アリール誘導体
GB0405937D0 (en) 2004-03-16 2004-04-21 Glaxo Group Ltd Compounds
GB0405933D0 (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
UY28871A1 (es) 2004-04-27 2005-11-30 Glaxo Group Ltd Antagonistas del receptor de acetilcolina muscarinico
BRPI0512535A (pt) 2004-06-24 2008-03-25 Incyte Corp compostos de piperidinas n-substituìdas, suas composições e métodos de modulações
WO2006000398A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited 2,3-benzoxazin derivatives as non-steroidal glucocorticoid receptor modulators
WO2006000401A1 (en) 2004-06-28 2006-01-05 Glaxo Group Limited Substituted oxazines as glucocorticoid receptor modulators
GB0418045D0 (en) 2004-08-12 2004-09-15 Glaxo Group Ltd Compounds
MX2007004465A (es) 2004-10-19 2007-05-07 Hoffmann La Roche Derivados de quinolina.
WO2006055752A2 (en) 2004-11-18 2006-05-26 Incyte Corporation INHIBITORS OF 11-β HYDROXYL STEROID DEHYDROGENASE TYPE 1 AND METHODS OF USING THE SAME
EP1833787A2 (en) 2004-11-30 2007-09-19 Plexxikon, Inc. Indole derivatives for use as 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
ATE517908T1 (de) 2005-01-10 2011-08-15 Glaxo Group Ltd Androstan-17-alpha-carbonat-derivate zur verwendung bei der behandlung allergischer und entzündlicher zustände
EP1848428A4 (en) 2005-02-18 2012-04-18 Neurogen Corp THIAZOLE AMIDES, IMIDAZOLE AMIDES AND RELATED ANALOGS
US20060264433A1 (en) 2005-05-23 2006-11-23 Backes Bradley J Pharmaceutical compositions as inhibitors of dipeptidyl peptidase-IV (DPP-IV)
WO2007011759A2 (en) 2005-07-15 2007-01-25 Kalypsys, Inc. Inhibitors of mitotic kinesin
TW200800946A (en) 2005-08-15 2008-01-01 Astrazeneca Ab Substituted piperazines as metabotropic glutamate receptor antagonists
CN101309690A (zh) 2005-08-16 2008-11-19 阿诺麦德股份有限公司 趋化因子受体结合化合物
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
JP2009531443A (ja) 2006-03-29 2009-09-03 フォールドアールエックス ファーマシューティカルズ インコーポレーティッド α−シヌクレイン毒性の抑制
NZ571182A (en) 2006-04-04 2010-09-30 Univ California Pyrazolo[3,4-d]pyrimidines
GB0608820D0 (en) 2006-05-04 2006-06-14 Piramed Ltd Pharmaceutical compounds
US8492378B2 (en) 2006-08-03 2013-07-23 Takeda Pharmaceutical Company Limited GSK-3β inhibitor
WO2008020229A2 (en) 2006-08-17 2008-02-21 Astrazeneca Ab Antibacterial pyrrolecarboxamides
MX2009002018A (es) 2006-08-25 2009-03-05 Abbott Lab Derivados de indazol que inhiben vanilloide-1 potencial de receptor pasajero (trpv1) y usos de los mismos.
AU2007301607A1 (en) 2006-09-25 2008-04-03 Mutabilis Sa Substituted heterocyclylcarbonylamino-acetic-acid-derivatives as inhibitors of bacterial heptose synthesis, methods for their preparation and biological applications of said inhibitors
ATE502943T1 (de) 2006-09-29 2011-04-15 Novartis Ag Pyrazolopyrimidine als pi3k-lipidkinasehemmer
TWI454262B (zh) 2006-11-02 2014-10-01 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
US8648069B2 (en) 2007-06-08 2014-02-11 Abbvie Inc. 5-substituted indazoles as kinase inhibitors
US20100210644A1 (en) 2007-06-25 2010-08-19 Boehringer Ingelheim International Gmbh Chemical compounds
EP2183228B1 (en) 2007-07-26 2014-08-20 Vitae Pharmaceuticals, Inc. CYCLIC INHIBITORS OF 11ß -HYDROXYSTERIOD DEHYDROGENASE 1
JP5301563B2 (ja) 2008-05-01 2013-09-25 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
CA2723039A1 (en) 2008-05-01 2009-11-05 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2291370B1 (en) 2008-05-01 2013-11-27 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2291373B1 (en) 2008-05-01 2013-09-11 Vitae Pharmaceuticals, Inc. Cyclic inhibitors of 11beta-hydroxysteroid dehydrogenase 1
EP2300437B1 (en) 2008-06-05 2013-11-20 Glaxo Group Limited Benzpyrazol derivatives as inhibitors of pi3 kinases
ES2566339T3 (es) 2008-06-05 2016-04-12 Glaxo Group Limited Derivados de 4-carboxamida indazol útiles como inhibidores de PI3-quinasas
WO2009147189A1 (en) 2008-06-05 2009-12-10 Glaxo Group Limited Novel compounds
JP5502077B2 (ja) 2008-06-05 2014-05-28 グラクソ グループ リミテッド 新規な化合物
KR101665727B1 (ko) 2008-06-11 2016-10-12 하마마츠 포토닉스 가부시키가이샤 유리 용착 방법
NZ590495A (en) 2008-07-25 2012-10-26 Vitae Pharmaceuticals Inc Dihydropyridin-phenyl-3-oxazinan-2-ones as inhibitors of 11beta-hydroxysteroid dehydrogenase 1
WO2010068287A2 (en) 2008-12-11 2010-06-17 Angion Biomedica Corp. Small molecule modulators of hepatocyte growth factor (scatter factor) activity
CA2754749C (en) 2009-03-04 2019-04-30 Opko Curna, Llc Treatment of sirtuin 1 (sirt1) related diseases by inhibition of natural antisense transcript to sirt1
JP5656880B2 (ja) * 2009-03-09 2015-01-21 グラクソ グループ リミテッドGlaxo Group Limited Pi3キナーゼの阻害剤としての4−オキサジアゾール−2−イル−インダゾール
EP2424838A1 (en) 2009-04-30 2012-03-07 Bayer CropScience AG Pesticidal arylpyrrolidines
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
DK2899191T3 (da) * 2009-04-30 2017-11-13 Glaxo Group Ltd Oxazol-substituerede indazoler som pi3-kinaseinhibitorer
KR20120061771A (ko) 2009-04-30 2012-06-13 비타이 파마슈티컬즈, 인코포레이티드 11베타-하이드록시스테로이드 탈수소효소 1의 고리형 억제제
AU2010243585B2 (en) 2009-04-30 2014-08-07 AbbVie Deutschland 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
UA109255C2 (ru) 2009-04-30 2015-08-10 Берінгер Інгельхайм Інтернешнл Гмбх Циклические ингибиторы 11бета-гидроксистероиддегидрогеназы 1
JP2013512880A (ja) 2009-12-03 2013-04-18 グラクソ グループ リミテッド Pi3−キナーゼ阻害剤としてのインダゾール誘導体
EP2507226A1 (en) 2009-12-03 2012-10-10 Glaxo Group Limited Novel compounds
JP2013512879A (ja) 2009-12-03 2013-04-18 グラクソ グループ リミテッド Pi3キナーゼの阻害剤としてのベンズピラゾール誘導体
RS54286B1 (en) 2010-09-08 2016-02-29 Glaxosmithkline Intellectual Property Development Limited POLYMORPHS AND SALTS N- [5- [4- (5 - {[(2R, 6S) -2,6-DIMETHYL-4-MORPHOLINYL] METHYL} -1,3-OXAZOL-2-yl) -1H-INDAZZOL- 6-IL] -2 (methyloxy) -3-pyridinyl] -methanesulfonamide
JP5876051B2 (ja) * 2010-09-08 2016-03-02 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited インフルエンザウィルス感染の治療に使用するためのインダゾール誘導体
GB201018124D0 (en) 2010-10-27 2010-12-08 Glaxo Group Ltd Polymorphs and salts

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