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91. 发明专利

ZA201707526B HETEROCYCLIC INHIBITORS OF ERK1 AND ERK2 AND THEIR USE IN THE TREATMENT OF CANCER 未知
公开(公告)号：ZA201707526B
公开(公告)日：2018-11-28
申请号：ZA201707526
申请日：2017-11-07
申请人： ASANA BIOSCIENCES LLC
发明人： REDDY SANJEEVA P , SMITH ROGER A , THOMPSON SCOTT K , VENKATESAN ARANAPAKAM M , ZAINUDDIN MOHD , MULLANGI RAMESH , KETHIRI RAGHAVA REDDY , MULAKALA CHANDRIKA , HALLUR GURULINGAPPA , DEWANG PURUSHOTTAM M
摘要： The present application provides a compound that is N-(2-amino-1-(3 -chloro-5 -fluorophenyl)ethyl)-1-(5-methyl-2-((tetrahydro-2H-pyran-4-yl)amino)pyrimidin-4-yl)-1H-imidazole-4-carboxamide (shown below), or a pharmaceutically acceptable salt or stereoisomer thereof. Also provided are methods for preparing the compound. The compound is useful for inhibiting ERK1/2. By administering to a patient in need a therapeutically effective amount of the compound, the compouns is effective in treating conditions associated with dysregulation of the RAS/RAF/MEK/ERK pathway. A variety of conditions can be treated using the compound and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.

92. 发明专利

DK2748166T3 PYRIMIDO-PYRIDAZINONFORBINDELSER OG ANVENDELSE DERAF 未知
公开(公告)号：DK2748166T3
公开(公告)日：2018-10-29
申请号：DK12756865
申请日：2012-08-23
申请人： ASANA BIOSCIENCES LLC
发明人： VENKATESAN ARANAPAKAM , SMITH ROGER ASTBURY , HOSAHALLI SUBRAMANYA , POTLURI VIJAY , PANIGRAHI SUNIL KUMAR , KUNTU KARUNASREE , BASETTI VISHNU
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , C07D519/00

93. 发明专利

HK1248704A1 氨基茚滿化合物及其治療疼痛的用途未知
公开(公告)号：HK1248704A1
公开(公告)日：2018-10-19
申请号：HK18108618
申请日：2018-07-04
申请人： ASANA BIOSCIENCES LLC
发明人： SCOTT KEVIN THOMPSON , TONY PRIESTLEY , ROGER ASTBURY SMITH , ASHIS K SAHA , SONALI RUDRA , ARUN KUMA HAJRA , DIPANWITA CHATTERJEE , CARL HENRY BEHRENS , YIGANG HE , HUI-YIN LI
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101

94. 发明专利

IL259781D0 Uses of pyrimido-pyridazinones to treat cancer 未知
公开(公告)号：IL259781D0
公开(公告)日：2018-07-31
申请号：IL25978118
申请日：2018-06-03
申请人： ASANA BIOSCIENCES LLC , REDDY SANJEEVA P , GUPTA SANDEEP , SMITH ROGER ASTBURY
发明人： REDDY SANJEEVA P , GUPTA SANDEEP , SMITH ROGER ASTBURY
IPC分类号： A61K20060101

95. 发明专利

MX2017014584A INHIBIDORES HETEROCICLICOS DE ERK1 Y ERK2 Y SU USO EN EL TRATAMIENTO DEL CANCER. 未知
公开(公告)号：MX2017014584A
公开(公告)日：2018-02-26
申请号：MX2017014584
申请日：2016-06-15
申请人： ASANA BIOSCIENCES LLC
发明人： ROGER A SMITH , SCOTT K THOMPSON , CHANDRIKA MULAKALA , SANJEEVA P REDDY , PURUSHOTTAM M DEWANG , GURULINGAPPA HALLUR , RAGHAVA REDDY KETHIRI , RAMESH MULLANGI , MOHD ZAINUDDIN , ARANAPAKAM M VENKATESAN
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/5377 , A61P35/00 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： La presente solicitud proporciona nuevos compuestos heterocíclicos y sales farmacéuticamente aceptables de los mismos. También se proporcionan métodos para preparar estos compuestos. E stos compuestos son útiles para inhibir ERK1/2. Administrando a un paciente que necesita una cantidad terapéuticamente eficaz de uno o más de los compuestos de la fórmula (I), (ver Fórmula) en la que X, Y, Z, J, M y R1 a R8 se definen en la presente, estos compuestos son eficaces en el tratamiento de afecciones asociadas con la desregulación de la vía RAS/RAF/MEK/ERK. Se puede tratar una variedad de afecciones usando estos compuestos e incluyen enfermedades que se caracterizan por una proliferación celular anormal. En una modalidad, la enfermedad es cáncer.

96. 发明专利

HK1226718A1 P2X3及/或P2X2/3化合物及方法未知
公开(公告)号：HK1226718A1
公开(公告)日：2017-10-06
申请号：HK16114126
申请日：2016-12-12
申请人： ASANA BIOSCIENCES LLC
发明人： THOMPSON SCOTT , VENKATESAN ARANAPAKAM , PRIESTLEY TONY , KUNDU MRINAL , SAHA ASHIS
IPC分类号： C07D20060101 , A61K20060101 , A61P20060101

97. 发明专利

CA3006762A1 USES OF PYRIMIDO-PYRIDAZINONES TO TREAT CANCER 未知
公开(公告)号：CA3006762A1
公开(公告)日：2017-06-08
申请号：CA3006762
申请日：2016-11-30
申请人： ASANA BIOSCIENCES LLC
发明人： REDDY SANJEEVA P , GUPTA SANDEEP , SMITH ROGER ASTBURY
IPC分类号： A61K31/519 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K31/551 , A61K31/675 , A61P35/00
摘要： Disclosed are methods of treating cancer, which include administering a therapeutically effective amount of a compound of Formula (I), or a pharmaceutically acceptable salt or ester thereof, to a subject in need thereof. Formula (I) Also disclosed are methods of inhibiting growth and proliferation of cancer cells in vitro or in vivo, which include contacting the cells with an amount of the compound of formula (I) effective to inhibit the growth or proliferation of the cancer cells. Further disclosed are methods of inhibiting tumor growth, which include contacting the tumor with an amount of the compound of formula (I) effective to inhibit the growth of the tumor.

98. 发明专利

ES2596215T3 Ciclohexilaminas 未知
公开(公告)号：ES2596215T3
公开(公告)日：2017-01-05
申请号：ES12781549
申请日：2012-10-24
申请人： ASANA BIOSCIENCES LLC
发明人： THOMPSON SCOTT KEVIN , SMITH ROGER ASTBURY , GUPTA SANDEEP , PRIESTLEY TONY , LAPING NICHOLAS JAMES , SAHA ASHIS K , RUDRA SONALI
IPC分类号： C07D207/34 , A61K31/24 , A61P13/00 , A61P13/10 , A61P29/00 , C07C219/12 , C07C219/14 , C07D309/14 , C07D333/38 , C07D333/40 , C07D333/70
摘要： Un compuesto seleccionado entre el grupo que consiste en: Yoduro de N-[2-((2,6-dimetilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Cloruro de N-[2-(benzoiloxi)propil]-N,N-dietilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((2,4,6-trimetilbenzoil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((2,6-dimetoxibenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2-fluorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2-clorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2,4-diclorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((2-metilbenzoil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((2-isopropilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((4-(terc-butil)benzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((4-clorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((3-fluorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((4-fluoro-2-(trifluorometil)benzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((3-(trifluorometil)benzoil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((2-(trifluorometil)benzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((2-nitrobenzoilo)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((3,5-diclorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((4-etilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((4-(trifluorometil)benzoil)oxi)propil]ciclohexanaminio; Yoduro de (S)-N,N-dimetil-N-[2-((2,4,6-trimetilbenzoil)oxi)propil]ciclohexanaminio; Yoduro de (S)-N-[2-((2,6-dimetilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de (R)-N-[2-((2,6-dimetilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de (R)-N,N-dimetil-N-[2-((2,4,6-trimetilbenzoil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((3-isopropilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2,6-diclorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((2,4,6-trimetilbenzoil)oxi)propil]tetrahidro-2H-piran-4-aminio; Yoduro de N-[2-((2,3-diclorobenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((ciclohexanocarbonil)oxi)propil]-N,N-dietilciclohexanaminio; Yoduro de N-[2-((3-clorobenzo[b]tiofeno-2-carbonil)oxi)propil]N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((tiofeno-2-carbonil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((4-isopropilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((tiofeno-3-carbonil)oxi)propil]ciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((1-metil-1H-pirrol-2-carbonil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((benzo[b]tiofeno-2carbonil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2,6-dimetilbenzoil)oxi)propil]-N,N,4-trimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((3-metil-tiofeno-2-carbonil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((4-(terc-butil)benzoil)oxi)propil]-N,N,4-trimetilciclohexanaminio; Yoduro de N,N,4-trimetil-N-[2-((2,4,6-trimetilbenzoil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((2,6-dimetilbenzoil)oxi)etil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2,4,6-trimetilbenzoil)oxi)etil]-N,N-dimetilciclohexanaminio; Yoduro de N,N-dimetil-N-[2-((4-metilbenzoil)oxi)propil]ciclohexanaminio; Yoduro de N-[2-((4-(terc-butil)benzoil)oxi)etil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2-etilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de N-[2-((2,4-dimetilbenzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de (S)-N-[2-((4-(terc-butil)benzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Yoduro de (R)-N-[2-((4-(terc-butil)benzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Bromuro de (S)-N-[2-((4-(terc-butil)benzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Bromuro de (R)-N-[2-((4-(terc-butil)benzoil)oxi)propil]-N,N-dimetilciclohexanaminio; Bromuro de 1-ciclohexil-1-[2-((2-isopropilbenzoil)oxi)propil]pirrolidin-1-io; Bromuro de 1-ciclohexil-1-[2-((2-isopropilbenzoil)oxi)propil] piperidin-1-io; Bromuro de 1-[2-((4-(terc-butil)benzoil)oxi)propil]-1-ciclohexilpirrolidin-1-io; Bromuro de 1-[2-((4-(terc-butil)benzoil)oxi)propil]-1-ciclohexilpiperidin-1-io; Bromuro de 1-[2-((3-clorobenzo[b]tiofeno-2-carbonil)oxi)propil]-1-ciclohexilpirrolidin-1-io; y Bromuro de 1-[2-((3-clorobenzo[b]tiofeno-2-carbonil)oxi)propil]-1-ciclohexilpiperidin-1-io.

99. 发明专利

IL245009D0 Protein-polymer-drug conjugates 未知
公开(公告)号：IL245009D0
公开(公告)日：2016-05-31
申请号：IL24500916
申请日：2016-04-10
申请人： ASANA BIOSCIENCES LLC , ROGER A SMITH , NITIN K DAMLE , ALEKSANDR V YURKOVETSKIY , MAO YIN , TIMOTHY B LOWINGER , JOSHUA D THOMAS , CHERI A STEVENSON , VENU R GURIJALA
发明人： ROGER A SMITH , NITIN K DAMLE , ALEKSANDR V YURKOVETSKIY , MAO YIN , TIMOTHY B LOWINGER , JOSHUA D THOMAS , CHERI A STEVENSON , VENU R GURIJALA
IPC分类号： A61K20060101
摘要： A polymeric scaffold useful for conjugating with a protein based recognition-molecule (PBRM) to form a PBRM-polymer-drug conjugate is described herein. The scaffold includes one or more terminal maleimido groups. Also disclosed is a PBRM-polymer-drug conjugate prepared from the scaffold. Compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions are also described.

100. 发明专利

CA2956315A1 STEROID-FREE DISEASE MANAGEMENT 未知
公开(公告)号：CA2956315A1
公开(公告)日：2016-02-04
申请号：CA2956315
申请日：2014-07-31
申请人： ASANA BIOSCIENCES LLC
发明人： SMITH ROGER ASTBURY , LAPING NICHOLAS JAMES , GUPTA SANDEEP
IPC分类号： A61K31/4439 , A61P35/00
摘要： The present invention relates to the use of the compound l-(2- (4-fluorophenyl)thiazol-5-yl)-l-(pyridin-4-yl)ethanol ("ASNOOl") in treatments without concomitant use of a steroid and/or in the form of a racemic mixture, e.g. in prostate cancer treatment. It also relates to its use in methods that are food indifferent.

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