PE20090058A1 - Compuestos carboxamida heterociclicos como inhibidores de la actividad akt - Google Patents
Compuestos carboxamida heterociclicos como inhibidores de la actividad aktInfo
- Publication number
- PE20090058A1 PE20090058A1 PE2008000249A PE2008000249A PE20090058A1 PE 20090058 A1 PE20090058 A1 PE 20090058A1 PE 2008000249 A PE2008000249 A PE 2008000249A PE 2008000249 A PE2008000249 A PE 2008000249A PE 20090058 A1 PE20090058 A1 PE 20090058A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- inhibitors
- carboxamide compounds
- heterocyclic carboxamide
- akt activity
- Prior art date
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/12—Ketones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4196—1,2,4-Triazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
Abstract
SE REFIERE A COMPUESTOS DE CARBOXAMIDA HETEROCICLICOS DE FORMULA (I), EN DONDE R41Y R42 SON INDEPENDIENTEMENTE H, UN GRUPO DE FORMULA a), HALOGENO, ALQUILO(C1-C4), ALQUILOXI(C1-C4), OPCIONALMENTE SUSTITUIDOS, FURANO, TIOFENO, ENTRE OTROS; R43 ES H, ALQUILO(C1-C4), ALQUILOXI(C1-C4), ENTRE OTROS; R44 ESTA AUSENTE O ES -(CR60R61)mAR; R45 ES H O ALQUILO(C1-C4); R20 ES H O ALQUILO(C1-C4), E HIDROXI; X ES O, S Y NR49, DONDE R49 ES H O ALQUILO(C1-C4); n ES DE 0 A 2 Y ESTE RESTO SI ES APLICABLE ESTA SUSTITUIDO CON HIDROXIALQUILO(C1-C4). SON SELECCIONADOS N-[2-AMINO-1-(FENILMETIL)ETIL]-4-BROMO-5-(1-METHYL-1H-PIRAZOL-5-IL)-2-FURANOCARBOXAMIDA, N-[2-AMINO-1-(FENILMETIL)ETIL]-5-(1-METIL-1H-PIRAZOL-5-IL)-2-TIENOCARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y UNA COMPOSICION FARMACEUTICA. ESTOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD DE LA PROTEINA QUINASA B (PKB O AKT), SIENDO UTILES EN EL TRATAMIENTO DE CANCER Y ARTRITIS
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US88858607P | 2007-02-07 | 2007-02-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20090058A1 true PE20090058A1 (es) | 2009-04-03 |
Family
ID=39682107
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2008000249A PE20090058A1 (es) | 2007-02-07 | 2008-02-05 | Compuestos carboxamida heterociclicos como inhibidores de la actividad akt |
Country Status (35)
Country | Link |
---|---|
US (7) | US8273782B2 (es) |
EP (1) | EP2117523B1 (es) |
JP (3) | JP4723677B2 (es) |
KR (3) | KR101521002B1 (es) |
CN (1) | CN101646427B (es) |
AR (1) | AR066184A1 (es) |
AU (1) | AU2008213694B2 (es) |
BR (1) | BRPI0807146B8 (es) |
CA (1) | CA2678255C (es) |
CL (1) | CL2008000348A1 (es) |
CO (1) | CO6220930A2 (es) |
CR (1) | CR10995A (es) |
CY (1) | CY1115535T1 (es) |
DK (1) | DK2117523T3 (es) |
DO (1) | DOP2009000196A (es) |
EA (1) | EA018038B1 (es) |
ES (1) | ES2501518T3 (es) |
HK (1) | HK1132676A1 (es) |
HR (1) | HRP20140790T1 (es) |
IL (1) | IL200212A (es) |
JO (1) | JO3134B1 (es) |
MA (1) | MA31167B1 (es) |
MX (2) | MX2009008550A (es) |
MY (1) | MY164480A (es) |
NZ (1) | NZ579177A (es) |
PE (1) | PE20090058A1 (es) |
PL (1) | PL2117523T3 (es) |
PT (1) | PT2117523E (es) |
SG (1) | SG193678A1 (es) |
SI (1) | SI2117523T1 (es) |
TW (2) | TWI381836B (es) |
UA (1) | UA102992C2 (es) |
UY (1) | UY30892A1 (es) |
WO (1) | WO2008098104A1 (es) |
ZA (1) | ZA200905363B (es) |
Families Citing this family (104)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20100047338A1 (en) | 2008-03-14 | 2010-02-25 | Angela Brodie | Novel C-17-Heteroaryl Steroidal CYP17 Inhibitors/Antiandrogens, In Vitro Biological Activities, Pharmacokinetics and Antitumor Activity |
US7625890B2 (en) | 2005-11-10 | 2009-12-01 | Smithkline Beecham Corp. | Substituted imidazo[4,5-c]pyridine compounds as Akt inhibitors |
UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
EP2250160B1 (en) | 2008-01-25 | 2015-11-11 | Millennium Pharmaceuticals, Inc. | Thiophenes and their use as phosphatidylinositol 3-kinase (pi3k) inhibitors |
ES2616051T3 (es) | 2008-12-02 | 2017-06-09 | Wave Life Sciences Japan, Inc. | Método para la síntesis de ácidos nucleicos modificados en el átomo de fósforo |
US8796314B2 (en) | 2009-01-30 | 2014-08-05 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
CA2750935A1 (en) | 2009-01-30 | 2010-08-12 | Millennium Pharmaceuticals, Inc. | Heteroaryls and their use as pi3k inhibitors |
US9090601B2 (en) | 2009-01-30 | 2015-07-28 | Millennium Pharmaceuticals, Inc. | Thiazole derivatives |
BRPI1006896B1 (pt) | 2009-01-30 | 2022-05-24 | Novartis Ag | Cloridrato de n-{(1s)-2-amino-1-[(3-fluorfenil)metil]etil}-5-cloro-4-(4-cloro-1-metil-1h- pirazol-5-il)-2-tiofenocarboxamida cristalino, composição farmacêutica compreendendo o mesmo e uso do dito composto para tratar ou diminuir a gravidade de câncer e artrite |
US20110312916A1 (en) | 2009-02-05 | 2011-12-22 | Tokai Pharmaceuticals, Inc. | Novel prodrugs of steroidal cyp17 inhibitors/antiandrogens |
AU2010270714B2 (en) | 2009-07-06 | 2015-08-13 | Wave Life Sciences Ltd. | Novel nucleic acid prodrugs and methods use thereof |
ES2527831T3 (es) * | 2009-09-23 | 2015-01-30 | Glaxosmithkline Llc | Combinación que comprende el inhibidor de MEK: N-{3-[3-ciclopropil-5-(2-fluoro-4-yodo-fenilamino)-6,8-dimetil-2,4,7-trioxo-3,4,6,7-tetrahidro-2H-pirido[4,3-d]pirimidin-1-il]fenil}acetamida y el inhibidor de Akt: N-{(1S)-2-amino-1-[(3-fluorofenil)metil]etil}-5-cloro-4-(4-cloro-1-metil-1H-pirazol-5-il)-2-tiofenocarboxamida |
AU2010298277B2 (en) * | 2009-09-23 | 2014-07-03 | Novartis Ag | Combination |
JP5881607B2 (ja) * | 2009-10-08 | 2016-03-09 | ノバルティス アーゲー | 組合せ |
EP2485593B1 (en) | 2009-10-08 | 2015-01-07 | GlaxoSmithKline LLC | Combination |
WO2011060380A1 (en) * | 2009-11-14 | 2011-05-19 | The Regents Of The University Of California | Pik3ca mutation status and sash1 expression predicts synergy between lapatinib and an akt inhibitor in her2 positive breast cancer |
US8598156B2 (en) | 2010-03-25 | 2013-12-03 | Glaxosmithkline Llc | Chemical compounds |
JP6155187B2 (ja) | 2010-03-30 | 2017-06-28 | ヴァーセオン コーポレイション | トロンビンの阻害剤としての多置換芳香族化合物 |
WO2011146710A1 (en) | 2010-05-21 | 2011-11-24 | Glaxosmithkline Llc | Combination |
EP2575460A4 (en) * | 2010-05-26 | 2013-10-16 | Glaxosmithkline Llc | COMBINATION |
WO2012021611A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
WO2012021615A1 (en) | 2010-08-11 | 2012-02-16 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
JP2013536193A (ja) | 2010-08-11 | 2013-09-19 | ミレニアム ファーマシューティカルズ, インコーポレイテッド | ヘテロアリール類およびその使用 |
US10428019B2 (en) | 2010-09-24 | 2019-10-01 | Wave Life Sciences Ltd. | Chiral auxiliaries |
WO2012051410A2 (en) | 2010-10-13 | 2012-04-19 | Millennium Pharmaceuticals, Inc. | Heteroaryls and uses thereof |
TWI505828B (zh) | 2010-12-20 | 2015-11-01 | 葛蘭素史克智慧財產(第二)有限公司 | 新穎醫藥組成物 |
EA029000B1 (ru) | 2011-01-11 | 2018-01-31 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | КОМБИНАЦИЯ БОРТЕЗОМИДА И Akt-ИНГИБИТОРА ДЛЯ ЛЕЧЕНИЯ МНОЖЕСТВЕННОЙ МИЕЛОМЫ |
US20120184562A1 (en) | 2011-01-19 | 2012-07-19 | Kin-Chun Luk | 1,6- and 1,8-naphthyridines |
US20120184548A1 (en) | 2011-01-19 | 2012-07-19 | Romyr Dominique | Carboxylic acid aryl amides |
US8362023B2 (en) | 2011-01-19 | 2013-01-29 | Hoffmann-La Roche Inc. | Pyrazolo pyrimidines |
US20120184542A1 (en) | 2011-01-19 | 2012-07-19 | Kevin Anderson | Pyrido pyrimidines |
US8673905B2 (en) | 2011-03-17 | 2014-03-18 | Hoffmann-La Roche Inc. | Imidazo pyrazines |
WO2012177925A1 (en) | 2011-06-21 | 2012-12-27 | The Board Institute, Inc. | Akt inhibitors for treating cancer expressing a magi3 - akt3 fusion gene |
EP2734208B1 (en) | 2011-07-19 | 2017-03-01 | Wave Life Sciences Ltd. | Methods for the synthesis of functionalized nucleic acids |
JP2015506347A (ja) * | 2011-12-23 | 2015-03-02 | ミレニアム ファーマシューティカルズ, インコーポレイテッドMillennium Pharmaceuticals, Inc. | ヘテロアリールおよびその使用 |
UA113875C2 (uk) | 2012-04-24 | 2017-03-27 | Новартіс Аг | Спосіб лікування стероїдзалежних дерматозів |
MX2015000577A (es) | 2012-07-13 | 2015-08-14 | Wave Life Sciences Pte Ltd | Control quiral. |
JP6246121B2 (ja) | 2012-07-13 | 2017-12-13 | 株式会社新日本科学 | キラル核酸アジュバント |
CN107011400B (zh) | 2012-07-13 | 2021-05-25 | 波涛生命科学有限公司 | 不对称辅助基团 |
JP6254169B2 (ja) | 2012-09-28 | 2017-12-27 | ファイザー・インク | ベンズアミドおよびヘテロベンズアミド化合物 |
EA201590750A1 (ru) | 2012-10-16 | 2015-09-30 | Янссен Фармацевтика Нв | СВЯЗАННЫЕ С ФЕНИЛОМ ХИНОЛИНИЛОВЫЕ МОДУЛЯТОРЫ RORγT |
BR112015008515A2 (pt) | 2012-10-16 | 2017-07-04 | Janssen Pharmaceutica Nv | moduladores de ror t de quinolinila ligada à heteroarila |
PT2909192T (pt) | 2012-10-16 | 2017-08-04 | Janssen Pharmaceutica Nv | Moduladores de ror-gama-t quinolinilo ligados por metileno |
BR112015008924A2 (pt) * | 2012-10-22 | 2017-07-04 | Glaxosmithkline Llc | combinação |
MY170427A (en) | 2012-11-30 | 2019-07-31 | Glaxosmithkline Llc | Novel pharmaceutical composition |
BR112015016559A2 (pt) | 2013-01-09 | 2017-07-11 | Glaxosmithkline Ip No 2 Ltd | combinação |
US10053454B2 (en) | 2013-02-27 | 2018-08-21 | Bristol-Myers Squibb Company | Carbazole compounds useful as bromodomain inhibitors |
EP4066841A1 (en) | 2013-03-14 | 2022-10-05 | University of Maryland, Baltimore | Androgen receptor down-regulating agents and uses thereof |
RU2015144193A (ru) * | 2013-03-15 | 2017-04-24 | Версеон Корпорейшн | Галогенпиразолы в качестве ингибиторов тромбина |
SG11201506449QA (en) | 2013-03-15 | 2015-09-29 | Verseon Corp | Multisubstituted aromatic compounds as serine protease inhibitors |
AU2014293011A1 (en) | 2013-07-26 | 2016-03-17 | Race Oncology Ltd. | Compositions to improve the therapeutic benefit of bisantrene |
CN105636594A (zh) | 2013-08-12 | 2016-06-01 | 托凯药业股份有限公司 | 使用雄激素靶向疗法用于治疗肿瘤性疾病的生物标记物 |
KR101797415B1 (ko) | 2013-10-01 | 2017-11-13 | 노파르티스 아게 | 암의 치료를 위한 아푸레세르팁과 조합된 엔잘루타미드 |
KR20160065910A (ko) * | 2013-10-01 | 2016-06-09 | 노파르티스 아게 | 조합물 |
US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
WO2015056180A1 (en) | 2013-10-15 | 2015-04-23 | Glaxosmithkline Intellectual Property (No.2) Limited | Indoline derivatives as inhibitors of perk |
US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
AU2014334619A1 (en) | 2013-10-15 | 2016-04-21 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORyt |
US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
EP3560920A1 (en) | 2013-10-15 | 2019-10-30 | Janssen Pharmaceutica NV | Secondary alcohol quinolinyl modulators of ror gamma t |
EP3057422B1 (en) | 2013-10-15 | 2019-05-15 | Janssen Pharmaceutica NV | Quinolinyl modulators of ror(gamma)t |
US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
EA201990240A1 (ru) | 2013-12-24 | 2019-06-28 | Бристол-Маерс Сквибб Компани | Новые трициклические соединения в качестве противораковых средств |
US10144933B2 (en) | 2014-01-15 | 2018-12-04 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having immunity induction activity, and immunity induction activator |
US10322173B2 (en) | 2014-01-15 | 2019-06-18 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having anti-allergic activity, and anti-allergic agent |
US10149905B2 (en) | 2014-01-15 | 2018-12-11 | Shin Nippon Biomedical Laboratories, Ltd. | Chiral nucleic acid adjuvant having antitumor effect and antitumor agent |
KR102423317B1 (ko) | 2014-01-16 | 2022-07-22 | 웨이브 라이프 사이언시스 리미티드 | 키랄 디자인 |
CA2942204A1 (en) | 2014-03-12 | 2015-09-17 | Novartis Ag | Combination comprising a btk inhibitor and an akt inhibitor |
CN104926801B (zh) * | 2014-03-22 | 2019-06-04 | 浙江大学 | 取代氮杂环类衍生物、含其的药物组合物及其在抗肿瘤中的应用 |
EP3125920B1 (en) | 2014-04-04 | 2020-12-23 | Del Mar Pharmaceuticals | Dianhydrogalactitol, diacetyldianhydrogalactitol or dibromodulcitol to treat non-small-cell carcinoma of the lung and ovarian cancer |
MX2016014890A (es) | 2014-06-06 | 2017-05-01 | Res Triangle Inst | Agonistas del receptor de apelina (apj) y usos de los mismos. |
WO2016044662A1 (en) | 2014-09-17 | 2016-03-24 | Verseon Corporation | Pyrazolyl-substituted pyridone compounds as serine protease inhibitors |
WO2016059602A2 (en) | 2014-10-16 | 2016-04-21 | Glaxo Group Limited | Methods of treating cancer and related compositions |
AR103232A1 (es) | 2014-12-22 | 2017-04-26 | Bristol Myers Squibb Co | ANTAGONISTAS DE TGFbR |
HUE060104T2 (hu) | 2015-02-27 | 2023-01-28 | Verseon Int Corporation | Szubsztituált pirazol vegyületek mint szerinproteázinhibitorok |
WO2017037578A2 (en) | 2015-08-28 | 2017-03-09 | Novartis Ag | Combination therapy |
WO2017098421A1 (en) | 2015-12-08 | 2017-06-15 | Glaxosmithkline Intellectual Property Development Limited | Benzothiadiazine compounds |
PE20190258A1 (es) | 2015-12-09 | 2019-02-25 | Res Triangle Inst | Antagonistas del receptor de la apelina (apj) mejorados y usos de los mismos |
WO2017156350A1 (en) | 2016-03-09 | 2017-09-14 | K-Gen, Inc. | Methods of cancer treatment |
WO2017153952A1 (en) | 2016-03-10 | 2017-09-14 | Glaxosmithkline Intellectual Property Development Limited | 5-sulfamoyl-2-hydroxybenzamide derivatives |
CN109311908B (zh) * | 2016-06-16 | 2021-05-07 | 哈尔滨珍宝制药有限公司 | 作为Akt抑制剂的二氢吡唑氮杂卓类化合物 |
WO2018071526A1 (en) * | 2016-10-12 | 2018-04-19 | Research Triangle Institute | Heterocyclic apelin receptor (apj) agonists and uses thereof |
CA3045752A1 (en) | 2016-12-01 | 2018-06-07 | Glaxosmithkline Intellectual Property Development Limited | Methods of treating cancer |
CN107011377B (zh) * | 2017-05-03 | 2019-02-26 | 南通书创药业科技有限公司 | 一种β-羰基磷酸酯的制备方法 |
US11504333B2 (en) | 2017-07-05 | 2022-11-22 | Novartis Ag | Pharmaceutical composition |
UY37866A (es) | 2017-09-07 | 2019-03-29 | Glaxosmithkline Ip Dev Ltd | Nuevos compuestos derivados de benzoimidazol sustituidos que reducen la proteína myc (c-myc) en las células e inhiben la histona acetiltransferasa de p300/cbp. |
WO2019053617A1 (en) | 2017-09-12 | 2019-03-21 | Glaxosmithkline Intellectual Property Development Limited | CHEMICAL COMPOUNDS |
PT3725791T (pt) * | 2017-12-13 | 2023-04-04 | Harbin Zhenbao Pharmaceutical Co Ltd | Sal que serve como inibidor de akt e seu cristal |
EP3827006A4 (en) | 2018-07-23 | 2022-04-06 | Signalrx Pharmaceuticals, Inc. | SINGLE MOLECULE COMPOUNDS PROVIDING MULTI-TARGET INHIBITION OF BTK AND OTHER PROTEINS AND METHODS OF USING THEM |
EP3866807A1 (en) | 2018-10-16 | 2021-08-25 | F. Hoffmann-La Roche AG | Use of akt inhibitors in ophthalmology |
CA3118493A1 (en) | 2018-11-05 | 2020-05-14 | Iovance Biotherapeutics, Inc. | Expansion of tils utilizing akt pathway inhibitors |
JP7406556B2 (ja) | 2018-11-30 | 2023-12-27 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッド | Hiv療法に有用な化合物 |
SG11202106635WA (en) | 2018-12-21 | 2021-07-29 | Daiichi Sankyo Co Ltd | Combination of antibody-drug conjugate and kinase inhibitor |
CN110031626A (zh) * | 2019-04-02 | 2019-07-19 | 浙江理工大学 | 一种用于胃肠道间质肿瘤迁移的标志物ack1及其应用 |
WO2021018941A1 (en) | 2019-07-31 | 2021-02-04 | Glaxosmithkline Intellectual Property Development Limited | Methods of treating cancer |
JP2022543679A (ja) | 2019-08-08 | 2022-10-13 | ラークナ・リミテッド | 癌を処置する方法 |
WO2021191417A1 (en) | 2020-03-27 | 2021-09-30 | Som Innovation Biotech, S.A. | Compounds for use in the treatment of synucleinopathies |
CN111592531B (zh) * | 2020-06-23 | 2023-08-15 | 上海鲲博玖瑞医药科技发展有限公司 | 福瑞塞替的制备方法 |
CN111620860B (zh) * | 2020-06-23 | 2023-02-03 | 济南健丰化工有限公司 | 一种福瑞塞替的制备方法 |
WO2022069554A1 (de) | 2020-10-01 | 2022-04-07 | Bayer Aktiengesellschaft | Verfahren zur herstellung von 4-bromfuran-2-carboxylaten |
WO2023174210A1 (en) | 2022-03-14 | 2023-09-21 | Laekna Limited | Combination treatment for cancer |
WO2023187037A1 (en) | 2022-03-31 | 2023-10-05 | Astrazeneca Ab | Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer |
WO2023230541A1 (en) | 2022-05-27 | 2023-11-30 | Viiv Healthcare Company | Piperazine derivatives useful in hiv therapy |
Family Cites Families (178)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1030415A (zh) | 1987-02-20 | 1989-01-18 | 山之内制药株式会社 | 饱和的杂环碳酰胺衍生物和它的制备方法 |
ES2005163A6 (es) | 1987-04-14 | 1989-03-01 | Lilly S A E | Un procedimiento para la produccion de derivados de tiofen-2-carboxamida. |
DK124089A (da) | 1988-03-16 | 1989-09-17 | Zambeletti Spa L | Heterocykliske derivater |
DE3810848A1 (de) | 1988-03-30 | 1989-10-19 | Boehringer Ingelheim Kg | Neue 2,3,4-substituierte imidazole und 3,4,5-substituierte 1,2,4-triazole, ihre herstellung und verwendung |
DE3927483A1 (de) | 1989-08-19 | 1991-02-21 | Boehringer Ingelheim Kg | Neue substituierte heterocyclische fuenfringe, ihre herstellung und verwendung |
US5258357A (en) | 1989-10-07 | 1993-11-02 | Basf Aktiengesellschaft | Carboxamides, their preparation and their use as herbicides |
DE3933573A1 (de) | 1989-10-07 | 1991-04-18 | Basf Ag | Carbonsaeureamide, verfahren zu ihrer herstellung und ihre verwendung als herbizide |
US6645969B1 (en) | 1991-05-10 | 2003-11-11 | Aventis Pharmaceuticals Inc. | Aryl and heteroaryl quinazoline compounds which inhibit CSF-1R receptor tyrosine kinase |
US5559235A (en) | 1991-10-29 | 1996-09-24 | Glaxo Wellcome Inc. | Water soluble camptothecin derivatives |
GB9201755D0 (en) | 1992-01-28 | 1992-03-11 | British Bio Technology | Compounds |
US5595872A (en) | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
US5342947A (en) | 1992-10-09 | 1994-08-30 | Glaxo Inc. | Preparation of water soluble camptothecin derivatives |
EP0667773A4 (en) | 1992-10-14 | 1996-09-25 | Merck & Co Inc | FIBRINOGEN RECEPTOR ANTAGONISTS. |
JPH08502508A (ja) | 1992-10-23 | 1996-03-19 | メルク シヤープ エンド ドーム リミテツド | ドーパミンレセプターサブタイプリガンド |
FR2707295A1 (fr) | 1993-06-07 | 1995-01-13 | Rhone Poulenc Agrochimie | Fongicides pyrazoles substitués en position 3 par un hétérocycle. |
WO1995004729A1 (en) * | 1993-08-06 | 1995-02-16 | Smithkline Beecham Plc | Amide derivatives as 5ht1d receptor antagonists |
US5739135A (en) | 1993-09-03 | 1998-04-14 | Bristol-Myers Squibb Company | Inhibitors of microsomal triglyceride transfer protein and method |
US5681835A (en) | 1994-04-25 | 1997-10-28 | Glaxo Wellcome Inc. | Non-steroidal ligands for the estrogen receptor |
US5491237A (en) | 1994-05-03 | 1996-02-13 | Glaxo Wellcome Inc. | Intermediates in pharmaceutical camptothecin preparation |
US5668148A (en) * | 1995-04-20 | 1997-09-16 | Merck & Co., Inc. | Alpha1a adrenergic receptor antagonists |
JP3964478B2 (ja) | 1995-06-30 | 2007-08-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | ヘテロ環含有カルボン酸誘導体及びそれを含有する医薬 |
US5846990A (en) | 1995-07-24 | 1998-12-08 | Bristol-Myers Squibb Co. | Substituted biphenyl isoxazole sulfonamides |
KR970705560A (ko) | 1995-08-02 | 1997-10-09 | 호아껭 우리아치 토렐로 | 항진균 활성을 갖는 신규한 카르복사미드(new carboxamides with antifungal activity) |
ES2153975T3 (es) | 1995-08-02 | 2001-03-16 | Uriach & Cia Sa J | Derivados de pirimidona con actividad antifungica. |
DE69634822T2 (de) | 1995-08-22 | 2006-04-27 | Japan Tobacco Inc. | Amid-verbindungen und ihre anwendung |
WO1997012613A1 (en) | 1995-10-05 | 1997-04-10 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
US6001866A (en) | 1995-10-05 | 1999-12-14 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
US5972980A (en) | 1995-10-05 | 1999-10-26 | Warner-Lambert Company | Method for treating and preventing inflammation and atherosclerosis |
US5942544A (en) | 1996-02-22 | 1999-08-24 | Dupont Pharmaceuticals Company | α-branched anilines, toluenes, and analogs thereof as factor Xa inhibitors |
CA2250204A1 (en) | 1996-04-03 | 1997-10-09 | Neville J. Anthony | Inhibitors of farnesyl-protein transferase |
CA2249665A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
JP2000509371A (ja) | 1996-04-03 | 2000-07-25 | メルク エンド カンパニー インコーポレーテッド | ファルネシル―タンパク質トランスフェラーゼ阻害剤 |
JP2000504024A (ja) | 1996-04-03 | 2000-04-04 | メルク エンド カンパニー インコーポレーテッド | ファルネシル―タンパク質トランスフェラーゼ阻害剤 |
JP2000507595A (ja) | 1996-04-03 | 2000-06-20 | メルク エンド カンパニー インコーポレーテッド | ファルネシルプロテイントランスフェラーゼの阻害剤 |
WO1997036896A1 (en) | 1996-04-03 | 1997-10-09 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
EP0891361A1 (en) | 1996-04-03 | 1999-01-20 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
JP2000507591A (ja) | 1996-04-03 | 2000-06-20 | メルク エンド カンパニー インコーポレーテッド | ファルネシル―タンパク質トランスフェラーゼ阻害剤 |
AU721952B2 (en) | 1996-04-03 | 2000-07-20 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
AUPO163896A0 (en) | 1996-08-14 | 1996-09-05 | Resmed Limited | Determination of respiratory airflow |
AU6320998A (en) | 1997-02-21 | 1998-09-09 | Bristol-Myers Squibb Company | Benzoic acid derivatives and related compounds as antiarrhythmic agents |
US5998336A (en) | 1997-02-26 | 1999-12-07 | The Board Of Trustees Of The Leland Stanford Junior University | Ceramic/metal and A15/metal superconducting composite materials exploiting the superconducting proximity effect and method of making the same |
ATE334975T1 (de) * | 1997-05-30 | 2006-08-15 | Takeda Pharmaceutical | Sulfonamidderivate, ihre herstellung und verwendung |
GB9716557D0 (en) | 1997-08-06 | 1997-10-08 | Glaxo Group Ltd | Benzylidene-1,3-dihydro-indol-2-one derivatives having anti-cancer activity |
DE19744026A1 (de) | 1997-10-06 | 1999-04-08 | Hoechst Marion Roussel De Gmbh | Pyrazol-Derivate, ihre Herstellung und ihre Verwendung in Arzneimitteln |
AU751139B2 (en) | 1997-10-13 | 2002-08-08 | Astellas Pharma Inc. | Amide derivative |
EP1044201A4 (en) | 1997-12-12 | 2001-10-31 | Euro Celtique Sa | 3-SUBSTITUTED ADENINE FROM 2-THIOXANTHINES |
US6232320B1 (en) | 1998-06-04 | 2001-05-15 | Abbott Laboratories | Cell adhesion-inhibiting antiinflammatory compounds |
AUPP433398A0 (en) | 1998-06-25 | 1998-07-16 | Australian National University, The | Compounds and processes |
US6192967B1 (en) | 1998-10-19 | 2001-02-27 | Sunny En Liung Huang | Collapsible auto shade |
US6130333A (en) | 1998-11-27 | 2000-10-10 | Monsanto Company | Bicyclic imidazolyl derivatives as phosphodiesterase inhibitors, pharmaceutical compositions and method of use |
GB9827882D0 (en) | 1998-12-17 | 1999-02-10 | Smithkline Beecham Plc | Novel compounds |
DE19904397A1 (de) | 1999-02-04 | 2000-08-10 | Bayer Ag | Verwendung von Pyrazol-Carbonsäureamiden |
DE19904396A1 (de) | 1999-02-04 | 2000-08-10 | Bayer Ag | Substituierte Pyrazolbenzylamin-Derivate |
JP2000256358A (ja) | 1999-03-10 | 2000-09-19 | Yamanouchi Pharmaceut Co Ltd | ピラゾール誘導体 |
US7125883B1 (en) | 1999-04-13 | 2006-10-24 | Abbott Gmbh & Co. Kg | Integrin receptor ligands |
EP1181270A2 (en) | 1999-05-24 | 2002-02-27 | Cor Therapeutics, Inc. | Inhibitors of factor xa |
CA2374793A1 (en) | 1999-05-24 | 2000-11-30 | Penglie Zhang | Inhibitors of factor xa |
JP2001247569A (ja) | 1999-08-12 | 2001-09-11 | Japan Tobacco Inc | ピロリジン誘導体又はピペリジン誘導体及びその医薬用途 |
US6632815B2 (en) * | 1999-09-17 | 2003-10-14 | Millennium Pharmaceuticals, Inc. | Inhibitors of factor Xa |
WO2001038309A1 (en) | 1999-11-24 | 2001-05-31 | Cor Therapeutics, Inc. | β-AMINO ACID-, ASPARTIC ACID- AND DIAMINOPROPIONIC-BASED INHIBITORS OF FACTOR Xa |
RU2223761C2 (ru) | 1999-12-27 | 2004-02-20 | Джапан Тобакко Инк. | Соединения с конденсированным кольцом и их использование в качестве лекарственных средств |
US6770666B2 (en) | 1999-12-27 | 2004-08-03 | Japan Tobacco Inc. | Fused-ring compounds and use thereof as drugs |
WO2001056557A2 (en) | 2000-02-05 | 2001-08-09 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of erk |
CA2369076A1 (en) | 2000-02-05 | 2001-08-09 | Vertex Pharmaceuticals Incorporated | Pyrazole compositions useful as inhibitors of erk |
KR20010111298A (ko) * | 2000-02-05 | 2001-12-17 | 버텍스 파마슈티칼스 인코포레이티드 | Erk의 억제제로서 유용한 피라졸 조성물 |
WO2001064642A2 (en) * | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
GB0011098D0 (en) | 2000-05-08 | 2000-06-28 | Black James Foundation | Pharmaceutical compositions comprising protpn pump inhibitors and gastrin/cholecystokinin receptor ligands |
AU2001264694B8 (en) | 2000-05-19 | 2006-05-04 | Laboratoires Serono Sa | Use of pyrazole derivatives for treating infertility |
US6589195B1 (en) * | 2000-05-26 | 2003-07-08 | Orthomerica Products, Inc. | Modular adjustable prophylactic hip orthosis and adduction/abduction joint |
JP2004501913A (ja) | 2000-06-23 | 2004-01-22 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | ヘテロアリール−フェニル置換Xa因子阻害剤 |
AU2001277143A1 (en) | 2000-07-24 | 2002-02-05 | Davide Riccardo Grassetti | Inhibition of mutagenic effects of carcinogens |
GB0018758D0 (en) | 2000-07-31 | 2000-09-20 | Smithkline Beecham Plc | Novel use and compunds |
JO2654B1 (en) * | 2000-09-04 | 2012-06-17 | شركة جانسين فارماسوتيكا ان. في | Multiple aryl caroxa amides are useful as lipid - lowering agents |
JP4267920B2 (ja) | 2001-01-26 | 2009-05-27 | 中外製薬株式会社 | 代謝調節剤として有用なマロニル−CoA脱炭酸酵素阻害剤 |
CA2445568A1 (en) | 2001-04-27 | 2002-11-07 | Vertex Pharmaceuticals Incorporated | Triazole-derived kinase inhibitors and uses thereof |
DE10223912A1 (de) * | 2001-06-28 | 2003-01-16 | Merck Patent Gmbh | TN- und STN-Flüssigkristallanzeigen |
US20030015823A1 (en) * | 2001-07-18 | 2003-01-23 | Hydranautics | Method for forming a thick section, thermoset, solid casting |
DE60238620D1 (de) | 2001-08-03 | 2011-01-27 | Vertex Pharma | Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung |
ATE392421T1 (de) | 2001-08-03 | 2008-05-15 | Vertex Pharma | Von pyrazol abgeleitete kinaseinhibitoren und deren verwendung |
BR0212101A (pt) | 2001-08-24 | 2004-08-24 | Pharmacia & Up John Company | 7-aza [2.2.1] biciclo-heptanos substituìdos com heteroarila para o tratamento de doenças |
US20040198799A1 (en) | 2001-09-27 | 2004-10-07 | Brondyk William H. | Methods of increasing endogenous testosterone levels |
US6794252B2 (en) * | 2001-09-28 | 2004-09-21 | Texas Instruments Incorporated | Method and system for forming dual work function gate electrodes in a semiconductor device |
WO2003035619A1 (en) | 2001-10-25 | 2003-05-01 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
US6897208B2 (en) | 2001-10-26 | 2005-05-24 | Aventis Pharmaceuticals Inc. | Benzimidazoles |
WO2003039529A1 (en) | 2001-11-07 | 2003-05-15 | 4Sc A.G. | Selective antibacterial agents |
TW200306819A (en) | 2002-01-25 | 2003-12-01 | Vertex Pharma | Indazole compounds useful as protein kinase inhibitors |
MXPA04007697A (es) | 2002-02-06 | 2004-11-10 | Vertex Pharma | Compuestos de heteroarilo utiles como inhibidores de gsk-3. |
US7335779B2 (en) | 2002-03-08 | 2008-02-26 | Quonova, Llc | Modulation of pathogenicity |
GB0206861D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Medicaments |
GB0206860D0 (en) | 2002-03-22 | 2002-05-01 | Glaxo Group Ltd | Compounds |
JP2005527586A (ja) | 2002-04-05 | 2005-09-15 | メルク エンド カムパニー インコーポレーテッド | 置換アリールアミド |
BR0309556A (pt) * | 2002-04-26 | 2005-02-09 | Pfizer Prod Inc | Inibidores de metaloproteinase pirimidina-2,4,6-triona |
JP2005529328A (ja) | 2002-06-05 | 2005-09-29 | ファーマシア アンド アップジョン カンパニー | 競合的結合1hnmr実験を用いたリガンドの同定方法 |
GB0216224D0 (en) | 2002-07-12 | 2002-08-21 | Glaxo Group Ltd | Compounds |
PL374970A1 (en) | 2002-08-02 | 2005-11-14 | Argenta Discovery Limited | Substituted thienyl-hydroxamic acids as histone deacetylase inhibitors |
TW200812986A (en) * | 2002-08-09 | 2008-03-16 | Nps Pharma Inc | New compounds |
EP1534680B1 (en) | 2002-08-14 | 2012-02-22 | Pharmaco Investments, Inc. | Prenylation inhibitors and methods of their synthesis and use |
US6649638B1 (en) | 2002-08-14 | 2003-11-18 | Ppd Discovery, Inc. | Prenylation inhibitors and methods of their synthesis and use |
US7250443B2 (en) | 2002-08-23 | 2007-07-31 | Chiron Corporation | Pyrrole based inhibitors of glycogen synthase kinase 3 |
DE10239443A1 (de) | 2002-08-28 | 2004-03-11 | Boehringer Ingelheim International Gmbh | Blockiervorrichtung für ein Sperrspannwerk mit federbetätigtem Abtrieb |
EP1398029A1 (en) | 2002-09-10 | 2004-03-17 | LION Bioscience AG | NR3B1 nuclear receptor binding 3-substituted pyrazole derivatives |
US20060084682A1 (en) | 2002-12-13 | 2006-04-20 | Heerding Dirk A | Thrombopoietin mimetics |
MXPA05006569A (es) | 2002-12-20 | 2005-09-22 | Pharmacia Corp | Compuestos que inhiben la proteina cinasa-2 activada por la proteina cinasa activada por el mitogeno. |
CA2515235A1 (en) | 2003-02-10 | 2004-08-19 | Bayer Healthcare Ag | Bis(hetero)aryl carboxamide derivatives for use as pgi2 antagonists |
WO2004072018A1 (ja) | 2003-02-12 | 2004-08-26 | Takeda Pharmaceutical Company Limited | アミン誘導体 |
US7223788B2 (en) | 2003-02-14 | 2007-05-29 | Sanofi-Aventis Deutschland Gmbh | Substituted N-aryl heterocycles, process for their preparation and their use as medicaments |
WO2004076418A1 (en) | 2003-02-28 | 2004-09-10 | Galderma Research & Development, S.N.C. | Ligands that modulate lxr-type receptors |
US7517887B2 (en) | 2003-04-09 | 2009-04-14 | General Atomics | Reversible inhibitors of S-adenosyl-L-homocysteine hydrolase and uses thereof |
WO2004094384A2 (en) | 2003-04-21 | 2004-11-04 | Elan Pharmaceuticals, Inc. | (hetero) arylamide 2-hydroxy-3-diaminoalkanes for use in the treatment of alzheimer’s disease |
ES2351393T3 (es) | 2003-05-26 | 2011-02-03 | Takeda Pharmaceutical Company Limited | Sulfopirroles. |
CA2529154C (en) | 2003-06-20 | 2013-05-07 | Galderma Research & Development, S.N.C. | Novel compounds that modulate ppar.gamma. type receptors, and use thereof in cosmetic or pharmaceutical compositions |
DE10331305A1 (de) | 2003-07-10 | 2005-02-17 | Siemens Ag | Kommunikationssystem, Peer-to-Peer-Nachrichten-Filter-Rechner und Verfahren zum Verarbeiten einer Peer-to-Peer-Nachricht |
FR2857666B1 (fr) | 2003-07-15 | 2005-08-26 | Oreal | Composition tinctoriale comprenant a titre de coupleur un derive du furane et nouveaux derives du furane |
CN102793692A (zh) | 2003-07-23 | 2012-11-28 | 幸讬制药公司 | 用于发炎与免疫相关用途的化合物 |
WO2005019200A2 (en) | 2003-08-14 | 2005-03-03 | Icos Corporation | Aryl piperidine derivatives as vla-1 integrin antagonists and uses thereof |
CA2536470A1 (en) | 2003-08-15 | 2005-02-24 | Vertex Pharmaceuticals Incorporated | Pyrrole compositions useful as inhibitors of c-met |
WO2005019182A1 (en) | 2003-08-20 | 2005-03-03 | Bayer Healthcare Ag | Pyrazolylmethylbenzamide derivatives as p2xt-receptor antagonists |
EP1670466A4 (en) | 2003-10-06 | 2007-04-25 | Glaxo Group Ltd | PREPARATION OF 1,6,7-TRISUBSTITUTED AZABENIC ZIMIDAZOLES AS KINASE-INHIBITORS |
US20070123561A1 (en) | 2003-10-06 | 2007-05-31 | Dennis Lee | Preparation of 1,7-disubstituted azabensimidazoles as kinase inhibitors |
US20050148605A1 (en) | 2003-11-13 | 2005-07-07 | Ambit Biosciences Corporation | Amide derivatives as ABL modulators |
BRPI0416852A (pt) | 2003-11-21 | 2007-02-27 | Array Biopharma Inc | inibidores da quinase akt |
US8652089B2 (en) | 2004-01-19 | 2014-02-18 | Arthrex, Inc. | System for distending body tissue cavities by continuous flow irrigation |
EP1708697A4 (en) | 2004-01-30 | 2007-11-28 | Smithkline Beecham Corp | CHEMICAL COMPOUNDS |
WO2005077345A1 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Compounds for the treatment of gastro-esophageal reflux disease |
WO2005077373A2 (en) | 2004-02-03 | 2005-08-25 | Astrazeneca Ab | Treatment of gastro-esophageal reflux disease (gerd) |
AR047894A1 (es) | 2004-02-25 | 2006-03-01 | Wyeth Corp | Derivados de tiofeno como inhibidores de la proteina tirosina fosfatasa 1b (ptpasa 1b); metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades mediadas por ptpasa 1b |
JP2007531757A (ja) | 2004-03-30 | 2007-11-08 | カイロン コーポレイション | 抗癌剤としての置換チオフェン誘導体 |
CN1934836A (zh) * | 2004-03-30 | 2007-03-21 | 松下电器产业株式会社 | 内容中继服务器、内容中继系统、内容中继方法和采用该方法的程序 |
EP1730128A1 (en) | 2004-03-31 | 2006-12-13 | Exelixis, Inc. | Anaplastic lymphoma kinase modulators and methods of use |
JP2005336172A (ja) | 2004-04-26 | 2005-12-08 | Japan Tobacco Inc | 腎虚血再灌流障害治療又は予防薬 |
TW200600492A (en) * | 2004-05-18 | 2006-01-01 | Achillion Pharmaceuticals Inc | Substituted aryl acylthioureas and related compounds; inhibitors of viral replication |
US20080119456A1 (en) | 2004-05-29 | 2008-05-22 | Trond Ulven | Substituted Thiazoleacetic Acid as Crth2 Ligands |
WO2006009876A2 (en) | 2004-06-17 | 2006-01-26 | Cengent Therapeutics, Inc. | Trisubstituted nitrogen modulators of tyrosine phosphatases |
AU2005260689B2 (en) * | 2004-06-30 | 2012-05-10 | Vertex Pharmaceuticals Incorporated | Azaindoles useful as inhibitors of protein kinases |
US7671077B2 (en) * | 2004-07-19 | 2010-03-02 | Leu-Fen Hou Lin | Neuroprotective small organic molecules, compositions and uses related thereto |
US20060019967A1 (en) * | 2004-07-21 | 2006-01-26 | Su-Ying Wu | SARS CoV main protease inhibitors |
US20060019968A1 (en) * | 2004-07-24 | 2006-01-26 | Laboratorios Dr. Esteve S.A. | Use of compounds active on the sigma receptor for the treatment of neuropathic pain |
US7269099B2 (en) | 2004-07-30 | 2007-09-11 | Bolt Technology Corporation | Air gun |
JP2006066488A (ja) * | 2004-08-25 | 2006-03-09 | Mitsubishi Electric Corp | 半導体受光素子およびその製造方法 |
US7365385B2 (en) * | 2004-08-30 | 2008-04-29 | Micron Technology, Inc. | DRAM layout with vertical FETs and method of formation |
US20060043513A1 (en) * | 2004-09-02 | 2006-03-02 | Deok-Hoon Kim | Method of making camera module in wafer level |
TW200616969A (en) | 2004-09-17 | 2006-06-01 | Tanabe Seiyaku Co | Imidazole compound |
US20060062453A1 (en) * | 2004-09-23 | 2006-03-23 | Sharp Laboratories Of America, Inc. | Color highlighting document image processing |
WO2006043518A1 (ja) | 2004-10-18 | 2006-04-27 | Santen Pharmaceutical Co., Ltd. | 神経疾患治療剤 |
JP2006120339A (ja) | 2004-10-19 | 2006-05-11 | Matsushita Electric Ind Co Ltd | 高周波加熱電源装置 |
TW200619843A (en) | 2004-10-20 | 2006-06-16 | Sumitomo Bakelite Co | Semiconductor wafer and semiconductor device |
DE102004051277A1 (de) | 2004-10-21 | 2006-04-27 | Merck Patent Gmbh | Heterocyclische Carbonylverbindungen |
DE102004054666A1 (de) | 2004-11-12 | 2006-05-18 | Bayer Cropscience Gmbh | Substituierte Pyrazol-3-carboxamide, Verfahren zur Herstellung und Verwendung als Herbizide und Pflanzenwachstumsregulatoren |
CA2587853A1 (en) * | 2004-11-23 | 2006-06-01 | Wyeth | Gonadotropin releasing hormone receptor antagonists |
EP1819709B1 (en) | 2004-11-30 | 2009-02-11 | Neurosearch A/S | Novel diazabicyclic aryl derivatives as cholinergy ligands |
SE527990C2 (sv) | 2004-12-06 | 2006-08-01 | Mora Of Sweden Ab | Isborr |
JP2008528700A (ja) | 2005-02-03 | 2008-07-31 | アイアールエム・リミテッド・ライアビリティ・カンパニー | Pparモジュレーターとしての化合物および組成物 |
JP2006232707A (ja) | 2005-02-23 | 2006-09-07 | Japan Tobacco Inc | 癌転移抑制剤 |
US20090081636A1 (en) | 2005-04-11 | 2009-03-26 | Mingjun Huang | Pharmaceutical compositions for and methods of inhibiting HCV replication |
US20060252807A1 (en) | 2005-04-22 | 2006-11-09 | Kalypsys, Inc. | Novel ortho-terphenyl inhibitors of p38 kinase and methods of treating inflammatory disorders |
GB0510139D0 (en) | 2005-05-18 | 2005-06-22 | Addex Pharmaceuticals Sa | Novel compounds B1 |
EP1919875A2 (en) | 2005-06-21 | 2008-05-14 | Astex Therapeutics Limited | Pyrazole derivatives and their use as pka and pkb modulators |
US20060288588A1 (en) | 2005-06-22 | 2006-12-28 | Frank Morabito | Garden tool |
EP1933832A2 (en) * | 2005-06-23 | 2008-06-25 | Astex Therapeutics Limited | Pharmaceutical combinations comprising pyrazole derivatives as protein kinase modulators |
US20060293320A1 (en) | 2005-06-24 | 2006-12-28 | Genelabs Technologies, Inc. | Heteroaryl derivatives for treating viruses |
WO2006136637A2 (es) * | 2005-06-24 | 2006-12-28 | Eloy Antonio Martinez Albal | Implante dental de corona rotatoria |
CA2613517A1 (en) | 2005-06-27 | 2007-01-04 | Exelixis, Inc. | Pyrazole based lxr modulators |
CN100494167C (zh) | 2005-08-02 | 2009-06-03 | 天津大学 | 抗乙肝病毒的叔胺氧化物及制备方法和制备药物的应用 |
GB0518237D0 (en) | 2005-09-07 | 2005-10-19 | Angeletti P Ist Richerche Bio | Therapeutic compounds |
WO2007052843A1 (ja) | 2005-11-04 | 2007-05-10 | Takeda Pharmaceutical Company Limited | 複素環アミド化合物およびその用途 |
US7838676B2 (en) | 2005-11-21 | 2010-11-23 | Amgen Inc. | Beta-secretase modulators and methods of use |
US8163749B2 (en) | 2005-12-14 | 2012-04-24 | Bristol-Myers Squibb Company | Six-membered heterocycles useful as serine protease inhibitors |
EP1968568A4 (en) * | 2005-12-22 | 2011-04-13 | Glaxosmithkline Llc | HEMMER OF NUTS ACTIVITY |
JP5140600B2 (ja) | 2005-12-23 | 2013-02-06 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | オーロラキナーゼのアザインドール阻害薬 |
AR056882A1 (es) | 2006-02-01 | 2007-10-31 | Bayer Cropscience Sa | Derivados del fungicida n- cicloalquil- bencil- amida |
US7919626B2 (en) | 2006-02-28 | 2011-04-05 | Helicon Therapeutics, Inc. | Pyrazole compounds and uses thereof |
JP2007277230A (ja) | 2006-03-15 | 2007-10-25 | Tanabe Seiyaku Co Ltd | 医薬組成物 |
EP2518063B1 (en) | 2006-12-21 | 2017-02-01 | Sloan-Kettering Institute For Cancer Research | Pyridazinones and furan-containing compounds |
JP2010513530A (ja) | 2006-12-22 | 2010-04-30 | エンサイシブ・ファーマシューティカルズ・インコーポレイテッド | C3a受容体の調節剤およびその使用方法 |
UY30892A1 (es) | 2007-02-07 | 2008-09-02 | Smithkline Beckman Corp | Inhibidores de la actividad akt |
EP2114388B1 (en) | 2007-02-07 | 2015-05-20 | GlaxoSmithKline LLC | Inhibitors of akt activity |
WO2008121685A1 (en) | 2007-03-28 | 2008-10-09 | Smithkline Beecham Corporation | Methods of use for inhibitors of akt activity |
EP2134175A4 (en) | 2007-03-29 | 2012-01-11 | Glaxosmithkline Llc | HAMMER OF ACT ACTIVITY |
-
2008
- 2008-02-01 UY UY30892A patent/UY30892A1/es not_active Application Discontinuation
- 2008-02-04 CL CL200800348A patent/CL2008000348A1/es unknown
- 2008-02-05 PE PE2008000249A patent/PE20090058A1/es not_active Application Discontinuation
- 2008-02-05 AR ARP080100487A patent/AR066184A1/es active IP Right Grant
- 2008-02-05 TW TW097104414A patent/TWI381836B/zh active
- 2008-02-05 JO JOP/2008/0045A patent/JO3134B1/ar active
- 2008-02-05 TW TW100116246A patent/TWI507194B/zh active
- 2008-02-07 DK DK08729249.6T patent/DK2117523T3/da active
- 2008-02-07 WO PCT/US2008/053269 patent/WO2008098104A1/en active Application Filing
- 2008-02-07 EP EP08729249.6A patent/EP2117523B1/en active Active
- 2008-02-07 PT PT87292496T patent/PT2117523E/pt unknown
- 2008-02-07 PL PL08729249T patent/PL2117523T3/pl unknown
- 2008-02-07 US US12/027,454 patent/US8273782B2/en active Active
- 2008-02-07 SG SG2012025235A patent/SG193678A1/en unknown
- 2008-02-07 MX MX2009008550A patent/MX2009008550A/es active IP Right Grant
- 2008-02-07 AU AU2008213694A patent/AU2008213694B2/en active Active
- 2008-02-07 SI SI200831277T patent/SI2117523T1/sl unknown
- 2008-02-07 ES ES08729249.6T patent/ES2501518T3/es active Active
- 2008-02-07 US US12/526,111 patent/US8410158B2/en active Active
- 2008-02-07 UA UAA200908388A patent/UA102992C2/ru unknown
- 2008-02-07 KR KR1020127026684A patent/KR101521002B1/ko active IP Right Grant
- 2008-02-07 KR KR1020097018537A patent/KR101537825B1/ko active IP Right Grant
- 2008-02-07 CA CA2678255A patent/CA2678255C/en active Active
- 2008-02-07 NZ NZ579177A patent/NZ579177A/en not_active IP Right Cessation
- 2008-02-07 KR KR1020147027676A patent/KR20140140570A/ko not_active Application Discontinuation
- 2008-02-07 MX MX2013002178A patent/MX367398B/es unknown
- 2008-02-07 CN CN2008800106329A patent/CN101646427B/zh active Active
- 2008-02-07 JP JP2009549232A patent/JP4723677B2/ja active Active
- 2008-02-07 EA EA200970738A patent/EA018038B1/ru not_active IP Right Cessation
- 2008-02-07 BR BRPI0807146A patent/BRPI0807146B8/pt active IP Right Grant
- 2008-02-07 MY MYPI20093241A patent/MY164480A/en unknown
- 2008-12-23 US US12/342,620 patent/US20110071182A1/en not_active Abandoned
-
2009
- 2009-07-31 ZA ZA200905363A patent/ZA200905363B/xx unknown
- 2009-08-03 IL IL200212A patent/IL200212A/en active IP Right Grant
- 2009-08-05 DO DO2009000196A patent/DOP2009000196A/es unknown
- 2009-08-06 CO CO09082387A patent/CO6220930A2/es active IP Right Grant
- 2009-08-06 MA MA32146A patent/MA31167B1/fr unknown
- 2009-08-26 CR CR10995A patent/CR10995A/es unknown
- 2009-10-01 US US12/571,828 patent/US20100041726A1/en not_active Abandoned
-
2010
- 2010-01-08 HK HK10100158.6A patent/HK1132676A1/xx unknown
-
2011
- 2011-02-07 JP JP2011024171A patent/JP5010038B2/ja active Active
-
2012
- 2012-04-10 JP JP2012089471A patent/JP5511879B2/ja active Active
-
2013
- 2013-02-22 US US13/774,022 patent/US8946278B2/en active Active
-
2014
- 2014-08-20 HR HRP20140790AT patent/HRP20140790T1/hr unknown
- 2014-09-08 CY CY20141100723T patent/CY1115535T1/el unknown
- 2014-12-08 US US14/562,968 patent/US20150152092A1/en not_active Abandoned
-
2016
- 2016-04-13 US US15/097,608 patent/US20160287561A1/en not_active Abandoned
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
PE20090058A1 (es) | Compuestos carboxamida heterociclicos como inhibidores de la actividad akt | |
UY27224A1 (es) | Inhibidores de la rho-quinasa | |
CL2012000163A1 (es) | Compuestos derivados de quinazolina o pirido[2,3-d]pirimidina, inhibidores de la autofagia; composicion farmaceutica; y su uso para el tratamiento del cancer, pancreatitis, neurodegeneracion, entre otras. | |
GEP20104884B (en) | Monocyclic heterocycles as kinase inhibitors | |
AR072699A1 (es) | Antagonistas especificos del receptor 4 del factor de crecimiento de los fi-broblastos (fgf-r4) | |
CL2004002050A1 (es) | Compuestos derivados de piridinonas sustituidas; su uso en el tratamiento de afecciones causadas o exacerbadas por actividad p38 map kinasa y/o tnf no regulada, tales como inflamaciones, tumores, sida y otros. | |
TR200906131T1 (tr) | Aktivin -actrIIa antagonistleri ve göğüs kanserinin tedavi e | |
CL2008002243A1 (es) | Compuestos derivados de 2-pirazolamino-1,3,5-triazina, inhibidores de kinasa jak; procedimiento de preparacion; composicion farmaceutica; y uso para el tratamiento del cancer. | |
JO2355B1 (en) | Hereditary calcitonin polypeptide receptor antagonists | |
CR11738A (es) | Compuestos de pirimidinona pirrolo 3-metil-2-imino fenil sustituidos como inhibidores bace-1, composiciones y su uso | |
ECSP105253A (es) | Derivados de 5-feniltiazol y uso como inhibidores de pi3 cinasa | |
PE20120575A1 (es) | Derivados de pirazolopirimidina como inhibidores de jak quinasas | |
UY27225A1 (es) | Inhibidores de la rho-quinasa | |
TW200626068A (en) | Active compounds for seed treatment | |
CR20120510A (es) | Derivados de piperidin-4-il azetidina como inhibidores de jak1 | |
CL2008001540A1 (es) | Compuestos derivados de pirrolopiridinas y pirazolopiridinas; composicion farmaceutica; y uso en el tratamiento del cancer. | |
CL2008000670A1 (es) | Compuestos derivados de tiazolidindionas y oxazolidindionas sustituidas; composicion farmaceutica; proceso de preparacion de la composicion farmaceutica; y uso en el tratamiento de enfermedades tales como artritis reumatoide, epoc, cancer, entre otras. | |
TW200714604A (en) | Substituted heterocycles and the uses thereof | |
MX2009006466A (es) | Metodos de tratamiento de cancer con inhibidores del receptor del factor 1 de crecimiento similar a la insulina. | |
GEP20125368B (en) | Kinase inhibitors | |
ATE497496T1 (de) | 2,4-pyridimediamon-derivate als hemmer von jak- kinasen zur behandlung von autoimmunerkrankungen | |
CL2011001215A1 (es) | Compuestos derivados de pirimidina, inhibidores de tirosina quinasa; composiciones farmaceuticas que los comprenden; y su uso en el tratamiento y/o prevencion de cancer, enfermedades inflamatorias y enfermedades autoinmunes. | |
PE20070621A1 (es) | 2-amino-7,8-dihidro-6h-pirido(4,3-d)pirimidina-5-onas | |
TW200608960A (en) | 3-aminocyclopentanecarboxamides as modulators of chemokine receptors | |
MX2009009761A (es) | Composiciones y estuches para tratamiento de la influenza. |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant, registration | ||
FD | Application declared void or lapsed |