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公开(公告)号：US20180289690A1
公开(公告)日：2018-10-11
申请号：US15574060
申请日：2016-06-24
发明人： Akio FUJIOKA
CPC分类号： A61K31/47 , A61P11/00 , C07D215/50
摘要： Provided are a therapeutic agent and a pharmaceutical composition exerting an excellent prophylactic or therapeutic effect on fibrosis and symptoms associated with fibrosis. The therapeutic agent for fibrosis comprises 4-[2-fluoro-4-[[[(2-phenylacetyl)amino]thioxomethyl]amino]-phenoxy]-7-methoxy-N-methyl-6-quinolinecarboxamide or a salt thereof as an active ingredient.
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公开(公告)号：US10092556B2
公开(公告)日：2018-10-09
申请号：US15131372
申请日：2016-04-18
IPC分类号： A61K31/4545 , C07D401/14 , C07D413/14 , A61K31/337 , C07D417/14 , A61K45/06
摘要： A novel compound which has an excellent aurora A-selective inhibitory action and is useful as an orally administrable anticancer agent is provided. Also, a novel agent for potentiation of anti-tumor effect of microtubule agonists, which include a taxane anticancer agent, and a combination therapy are provided. A piperidine compound represented by a general formula (I) or a salt thereof: wherein, R1 represents a carboxyl group, —C(═O)NR5R6, or an oxadiazolyl group optionally having a C1-C6 alkyl group or a trifluoromethyl group as a substituent; R2 represents a halogen atom or a C1-C6 alkoxy group; R3 represents a phenyl group optionally having 1 to 3 same or different group(s) selected from a halogen atom, a C1-C6 alkyl group, a C1-C6 alkoxy group, and a trifluoromethyl group as a substituent; R4 represents a hydrogen atom or a C1-C6 alkyl group; and R5 and R6 are the same or different and each represent a hydrogen atom, a C1-C6 alkyl group, or a C3-C6 cycloalkyl group, or R5 and R6 optionally form a 3 to 6-membered nitrogen-containing saturated heterocyclic group together with a nitrogen atom to which R5 and R6 are bound, are provided.
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公开(公告)号：US10071146B2
公开(公告)日：2018-09-11
申请号：US15030678
申请日：2014-10-20
发明人： Satoshi Fukaya , Toshihiro Osada , Hiroshi Wada
摘要： This invention provides a cancer antigen peptide that can be administered to a wide range of cancer patients in the form of a peptide vaccine for cancer without the need for HLA typing and regardless of the HLA types of patients. Such peptide having 4 linked CTL epitopes is obtained by linking 4 CTL epitope peptides selected from among CTL epitope peptides derived from tumor antigen molecules that are reported to have the capacity for CTL induction via linkers.
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公开(公告)号：US20180148443A1
公开(公告)日：2018-05-31
申请号：US15572398
申请日：2016-05-11
发明人： Takao UNO
IPC分类号： C07D471/04 , A61P35/00
摘要： Provided are crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide which are stable and show excellent oral absorbability.The crystals are Form II crystals of 3-ethyl-4-{3-isopropyl-4-(4-(1-methyl-1H-pyrazol-4-yl)-1H-imidazol-1-yl)-1H-pyrazolo[3,4-b]pyridin-1-yl}benzamide showing an X-ray powder diffraction spectrum having at least three characteristic diffraction peaks at angles (2θ±0.2°) selected from the group consisting of 7.7°, 8.0°, 11.1°, 12.5°, 12.9°, 15.2°, 15.8°, 17.2°, 19.0°, 22.5°, 26.1°, and 27.4°.
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公开(公告)号：US09889136B2
公开(公告)日：2018-02-13
申请号：US15203059
申请日：2016-07-06
发明人： Kazuhisa Minamiguchi , Shigeo Okajima , Shinichi Aoki , Masanori Asai , Takahiro Asai , Hiroyoshi Yamanaka , Suguru Dohi
IPC分类号： C07D471/04 , A61K31/519 , A61K31/553 , A61P5/28 , A61P35/00 , A61K9/00 , A61K31/53
CPC分类号： A61K31/519 , A61K9/0019 , A61K31/53 , A61K31/553 , C07D471/04
摘要： A method for inhibiting androgen activity, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof, and a method for treating tumor, including administering an effective amount of a tetrahydropyridopyrimidine compound of formula (I) or a pharmaceutically acceptable salt thereof to a subject in need thereof
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36.发明申请公开(公告)号：US20180030067A1
公开(公告)日：2018-02-01
申请号：US15553286
申请日：2016-02-26
发明人： Masaya HASHIMOTO
IPC分类号： C07D498/14
CPC分类号： C07D498/14 , A61K31/5365 , C07B2200/13
摘要： An object of the present invention is to provide a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having excellent stability and favorable characteristics in terms of its production and formulation into drugs. The present invention provides a crystal of trans-3-amino-1-methyl-3-(4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenylcyclobutanol having characteristic peaks of diffraction angle (2θ±0.1°) at 7.7°, 9.5°, 10.3°, 12.3°, 14.5°, 15.6°, 16.3°, 17.8°, 18.3°, 19.3°, 20.9°, 22.8°, 24.2°, 25.7°, 26.8°, 27.7°, 29.0° and 30.1° in a powder X-ray diffraction spectrum.
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公开(公告)号：US09758526B2
公开(公告)日：2017-09-12
申请号：US15382883
申请日：2016-12-19
IPC分类号： C07D487/14 , C07D471/14
CPC分类号： C07D487/14 , C07D471/14
摘要： An object to be achieved by the present invention is to provide a novel compound having EGFR inhibitory effects and cell growth inhibitory effects, as well as a medication useful for the prevention and/or treatment of cancer based on the EGFR inhibitory effects.The present invention provides a compound represented by Formula (I) below, or a salt thereof.
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公开(公告)号：US09676773B2
公开(公告)日：2017-06-13
申请号：US15112070
申请日：2015-02-04
IPC分类号： C07D401/14 , A61K31/437 , C07D471/04
CPC分类号： A61K31/437 , A61K31/444 , A61K31/5377 , A61K31/695 , C07D471/04
摘要： Provided is a novel compound having a selective JAK3-inhibitory effect and also having excellent oral absorbability. Also provided is a pharmaceutical agent, which is based on a JAK3-inhibitory effect and is useful for preventing and/or treating a disease involving the JAK3, and in particular, rheumatoid arthritis or multiple sclerosis.An azaindole derivative having a cycloalkenyl group, which is represented by the following formula (I), or a salt thereof, and a pharmaceutical composition containing the same: where R1 to R4, m and n have the same meanings as those defined in the description.
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公开(公告)号：US20170157131A1
公开(公告)日：2017-06-08
申请号：US15435493
申请日：2017-02-17
发明人： Junji UCHIDA , Koyo SHUDO
IPC分类号： A01N43/66
CPC分类号： A61K31/53 , A61K31/44 , A61K31/513 , A61K31/519 , C07D239/553
摘要： The present invention provides an antitumor effect potentiator for enhancing antitumor activity of an antitumor agent comprising tegafur in a therapeutically effective amount, gimeracil in an amount effective for enhancing an antitumor effect, and oteracil potassium in an amount effective for inhibiting a side effect. The antitumor effect potentiator comprising at least one member selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof. The present invention also provides a method for enhancing an antitumor effect of an antitumor agent comprising the step of administering to a patient the aforementioned antitumor effect potentiator; a method for inhibiting the growth of a tumor comprising the step of administering to a patient the aforementioned antitumor effect potentiator and a method for cancer treatment comprising the step of administering to a patient the aforementioned antitumor agent.
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公开(公告)号：US09616081B2
公开(公告)日：2017-04-11
申请号：US14779759
申请日：2014-03-27
发明人： Hiroyuki Okabe
IPC分类号： A61K31/70 , A01N43/04 , A61K31/7072 , A61K31/4745 , A61K31/506 , A61K31/513 , A61K31/706 , A61K31/7064 , A61K31/7068
CPC分类号： A61K31/7072 , A61K31/4745 , A61K31/506 , A61K31/513 , A61K31/706 , A61K31/7064 , A61K31/7068 , A61K2300/00
摘要： Provided is a novel combination therapy using an FTD/TPI combination drug which exhibits remarkable antitumor effects, and few side effects.An antitumor agent is characterized in that the FTD/TPI combination drug is administered, using a reduced amount of trifluridine, at a dose in the range of 35 to 70 mg/m2/day and CPT-11 is administered at a dose in the range of 45 to 144 mg/m2/day.
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