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公开(公告)号：US20180215782A1
公开(公告)日：2018-08-02
申请号：US15555484
申请日：2016-03-02
Applicant: JITSUBO Co., Ltd.
Inventor： Yusuke KONO , Hideaki SUZUKI , Susumu MUTO
CPC classification number: C07K1/026 , C07C43/225 , C07C43/23 , C07C217/58 , C07K1/10 , C07K1/306
Abstract: The present invention has an object of providing a peptide synthesis method using a carrier capable of reversibly repeating the dissolved state and the insolubilized state, wherein the problem of an amino acid active species existing in the reaction system in de-protection reaction can be easily solved. The present invention provides a peptide synthesis method comprising the following steps: a step of condensing an N-Fmoc protected amino acid with a peptide having a C-terminal protected with a carrier which is crystallized according to a change of a composition of a dissolving solvent, in the presence of a condensing agent, to obtain an N-Fmoc-C-carrier protected peptide, a step of adding an alkylamine having 1 to 14 carbon atoms or hydroxyl amine to the reaction system, a step of de-protecting the N-terminal, and a step of changing the composition of the solvent dissolving the C-carrier protected peptide, to crystallize and separate the peptide.
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公开(公告)号：US20180186725A1
公开(公告)日：2018-07-05
申请号：US15577393
申请日：2016-05-27
Applicant: BASF SE
Inventor： Thomas SCHAUB , Joan GALLARDO DONAIRE , Martin ERNST
IPC: C07C209/26 , C07D265/30 , C07D317/58 , C07F17/02 , B01J31/24 , B01J31/22
CPC classification number: C07C209/26 , B01J31/185 , B01J31/20 , B01J31/2295 , B01J31/2409 , B01J31/2414 , B01J31/2433 , B01J2231/4283 , B01J2231/44 , B01J2231/643 , B01J2531/821 , C07B2200/07 , C07C213/02 , C07C2602/08 , C07D265/30 , C07D317/58 , C07F17/02 , C07C211/27 , C07C211/29 , C07C217/58 , C07C211/30 , C07C211/42 , C07C211/03
Abstract: The present invention relates to a method for the reductive amination of a carbonyl compound, comprising one or more carbonyl groups amenable to reductive amination, forming the corresponding primary amine, characterized in that the reaction is carried out in the presence of a homogeneously dissolved catalyst complex K, comprising at least one metal atom from Group 8, 9 or 10 of the periodic table, bearing a bidentate phosphane ligand, a carbonyl ligand, a neutral ligand and a hydride ligand, and also an acid as co-catalyst.
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公开(公告)号：US09951033B2
公开(公告)日：2018-04-24
申请号：US15380613
申请日：2016-12-15
Applicant: Universitetet I Oslo
Inventor： Kjetil Tasken , Birgitte Lygren , Ellen Ostensen , Jo Klaveness
IPC: C07D307/81 , C07D213/36 , C07C211/43 , C07D277/28 , C07C217/58 , C07C229/38 , C07C211/49 , C07D257/04 , C07C211/27 , C07C275/40
CPC classification number: C07D307/81 , C07C211/27 , C07C211/29 , C07C211/43 , C07C211/49 , C07C217/58 , C07C229/38 , C07C275/40 , C07D213/36 , C07D257/04 , C07D277/28 , C07D277/56 , C07D307/79
Abstract: The present invention relates to tertiary amines of formula (I) for use in therapy, particularly for use in treating cardiovascular disorders. The compounds have been found to regulate phospholamban phosphorylation by interfering with the A-kinase anchor protein 18delta (AKAP18δ) binding to the PKA substrate phospholamban. The compounds share a tri(alkylaryl/alkylheteroaryl) amine structure.
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公开(公告)号：US09944589B2
公开(公告)日：2018-04-17
申请号：US14650292
申请日：2013-12-03
Applicant: Istituto Europeo de Oncologia S.r.L.
Inventor： Mario Varasi , Paola Vianello , Florian Thaler , Paolo Trifiro′ , Ciro Mercurio , Giuseppe Meroni
IPC: C07C211/40 , A61K31/4025 , A61K31/404 , A61K31/4164 , A61K31/496 , C07D215/12 , C07D295/195 , C07D207/50 , C07D213/61 , C07D311/70 , C07D211/58 , C07D263/04 , C07D233/02 , C07D271/113 , C07C209/00 , C07C231/12 , C07C269/06 , C07C303/36 , C07D319/16 , C07D233/32 , C07D239/42 , C07D249/06 , C07D263/22 , C07D271/10 , C07D295/155 , C07D213/64 , C07D307/54 , C07C271/28 , C07C211/49 , C07C215/42 , C07C217/58 , C07C217/74 , C07C233/44 , C07C233/80 , C07C237/06 , C07C247/16 , C07C311/21
CPC classification number: C07C211/40 , A61K31/4025 , A61K31/404 , A61K31/4164 , A61K31/496 , C07C209/00 , C07C211/49 , C07C215/42 , C07C217/58 , C07C217/74 , C07C231/12 , C07C233/44 , C07C233/80 , C07C237/06 , C07C247/16 , C07C269/06 , C07C271/28 , C07C303/36 , C07C311/21 , C07C2601/02 , C07D207/50 , C07D211/58 , C07D213/61 , C07D213/64 , C07D215/12 , C07D233/02 , C07D233/32 , C07D239/42 , C07D249/06 , C07D263/04 , C07D263/22 , C07D271/10 , C07D271/113 , C07D295/155 , C07D295/195 , C07D307/54 , C07D311/70 , C07D319/16 , A61K2300/00
Abstract: The present invention relates to cyclopropyl derivatives of general formula (I), wherein A, R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.
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公开(公告)号：US09926291B2
公开(公告)日：2018-03-27
申请号：US15370093
申请日：2016-12-06
Inventor： Ouathek Ouerfelli , Anna Dilhas , Guangbin Yang , Hong Zhao
IPC: C07C255/46 , C07D401/04 , C07C209/36 , C07C213/08 , C07C253/00 , C07C253/30 , C07D213/61 , C07D213/64 , C07D213/72 , C07D213/74 , C07D213/84 , C07C231/12 , C07C227/18 , C07D213/643 , C07D213/76
CPC classification number: C07D401/04 , C07C209/36 , C07C213/08 , C07C227/18 , C07C231/12 , C07C253/00 , C07C253/30 , C07C2601/04 , C07D213/61 , C07D213/64 , C07D213/643 , C07D213/72 , C07D213/74 , C07D213/76 , C07D213/84 , C07C211/52 , C07C217/58 , C07C255/46
Abstract: A novel synthesis of the anti-androgen, A52, which has been found to be useful in the treatment of prostate cancer, is provided. A52 as well as structurally related analogs may be prepared via the inventive route. This new synthetic scheme may be used to prepare kilogram scale quantities of pure A52.
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公开(公告)号：US20180057455A1
公开(公告)日：2018-03-01
申请号：US15689115
申请日：2017-08-29
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： KAP-SUN YEUNG , Katharine A. Grant-Young , Juliang Zhu , Mark G. Saulnier , David B. Frennesson , David R. Langley , Piyasena Hewawasam , Tao Wang , Zhongxing Zhang , Zhaoxing Meng , Li-Qiang Sun , Eric Mull , Paul Michael Scola
IPC: C07D207/12 , C07D211/66 , C07D207/16 , C07D403/12 , C07D401/12 , C07D207/14 , C07D211/22 , C07D213/38 , C07D401/14 , C07C237/06 , C07D295/088 , C07D205/04 , C07D213/85 , C07C217/18 , C07D213/73 , C07D405/12 , C07C255/24 , C07D413/14 , C07D405/14 , C07D213/79 , C07D231/12 , C07D239/26 , C07D277/28 , C07D211/90
CPC classification number: C07D207/12 , C07C217/18 , C07C217/28 , C07C217/58 , C07C229/14 , C07C235/08 , C07C237/04 , C07C237/06 , C07C255/24 , C07C255/25 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07D205/04 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/46 , C07D211/58 , C07D211/60 , C07D211/66 , C07D211/90 , C07D213/38 , C07D213/42 , C07D213/55 , C07D213/73 , C07D213/79 , C07D213/85 , C07D231/12 , C07D239/26 , C07D277/28 , C07D295/088 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12
Abstract: The present disclosure generally relates to compounds useful as immunomodulators. Provided herein are compounds, compositions comprising such compounds, and methods of their use. The disclosure further pertains to pharmaceutical compositions comprising at least one compound according to the disclosure that are useful for the treatment of various diseases, including cancer and infectious diseases.
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公开(公告)号：US09872852B2
公开(公告)日：2018-01-23
申请号：US14915782
申请日：2014-09-02
Applicant: BRISTOL-MYERS SQUIBB COMPANY
Inventor： Louis S. Chupak , Xiaofan Zheng
IPC: A61K31/381 , A61K31/396 , A61K31/40 , A61K31/4427 , A61K31/496 , C07C217/58 , C07C229/22 , C07C233/36 , C07C235/76 , C07C311/05 , C07D205/04 , C07D207/14 , C07D211/32 , C07D213/57 , C07D213/69 , C07D217/02 , C07D233/06 , C07D249/08 , C07D265/30 , A61K31/397 , A61K31/5375 , A61K31/44 , A61K31/4523 , A61K31/445 , A61K31/551 , A61K31/55 , C07D309/14 , C07D311/14 , C07D317/50 , C07D223/06 , C07D319/18 , C07D333/20 , C07D333/32 , C07D333/36 , C07D233/61 , C07D401/06 , C07D401/12 , C07D405/12 , C07D487/10 , C07D205/08 , C07D207/08 , C07D207/16 , C07D207/27 , C07C279/12 , C07D211/34 , C07D211/44 , C07D295/12 , C07D211/48 , C07D211/56 , C07D211/60 , C07D211/62 , C07D295/14 , C07D295/18 , C07D295/185 , C07D211/76 , C07D211/78 , C07D213/63 , C07D213/64 , C07D213/65 , C07C255/54 , C07C271/20 , C07C279/14 , C07C229/14 , C07C233/38 , C07C233/47 , C07C233/78 , C07C237/06 , C07K5/083 , C07C275/40 , C07D217/04 , C07D295/13 , C07D295/16 , C07D311/08
CPC classification number: A61K31/381 , A61K31/396 , A61K31/397 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/445 , A61K31/4523 , A61K31/496 , A61K31/5375 , A61K31/55 , A61K31/551 , C07C217/58 , C07C229/14 , C07C229/22 , C07C233/36 , C07C233/38 , C07C233/47 , C07C233/78 , C07C235/76 , C07C237/06 , C07C255/54 , C07C271/20 , C07C275/40 , C07C279/12 , C07C279/14 , C07C311/05 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D205/04 , C07D205/08 , C07D207/08 , C07D207/14 , C07D207/16 , C07D207/27 , C07D211/32 , C07D211/34 , C07D211/44 , C07D211/48 , C07D211/56 , C07D211/60 , C07D211/62 , C07D211/76 , C07D211/78 , C07D213/57 , C07D213/63 , C07D213/64 , C07D213/65 , C07D213/69 , C07D217/02 , C07D217/04 , C07D223/06 , C07D233/61 , C07D249/08 , C07D265/30 , C07D279/12 , C07D295/12 , C07D295/13 , C07D295/14 , C07D295/16 , C07D295/18 , C07D295/185 , C07D309/14 , C07D311/08 , C07D311/14 , C07D317/50 , C07D319/18 , C07D333/20 , C07D333/32 , C07D333/36 , C07D401/06 , C07D401/12 , C07D405/12 , C07D487/10 , C07K5/0806 , C07K5/0808
Abstract: Disclosed are compounds of Formula (I): (I). Also disclosed are methods of using such compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of virological diseases or disorders and cancer.
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公开(公告)号：US20170355669A1
公开(公告)日：2017-12-14
申请号：US15593540
申请日：2017-05-12
Applicant: Lantheus Medical Imaging, Inc.
Inventor： Ajay Purohit , Pedro Benites , Heike S. Radeke , Joel Lazewatsky , L. Veronica Lee
IPC: C07C303/30 , A61K51/04 , C07C53/10 , C07C53/06 , C07C309/66 , C07C303/28 , C07C213/02 , C07C309/73 , C07B59/00 , C07C279/10 , C07C277/08 , C07C279/24 , C07C255/54 , C07C309/04 , C07C217/58 , C07C309/30 , C07C309/65 , C07C63/08 , C07C53/18 , C07C277/00 , A61K51/00
CPC classification number: C07C303/30 , A61K51/00 , A61K51/04 , A61K51/0406 , C07B59/001 , C07B2200/05 , C07C53/06 , C07C53/10 , C07C53/18 , C07C63/08 , C07C213/02 , C07C217/58 , C07C255/54 , C07C277/00 , C07C277/08 , C07C279/10 , C07C279/24 , C07C303/28 , C07C309/04 , C07C309/30 , C07C309/65 , C07C309/66 , C07C309/73 , C07C279/08
Abstract: The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.
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公开(公告)号：US09839219B2
公开(公告)日：2017-12-12
申请号：US15222576
申请日：2016-07-28
Applicant: Curza Global, LLC , University of Utah Research Foundation
Inventor： Ryan Looper , Dustin Williams , Sujeevini Jeyapalina , Travis Haussener , Paul R. Sebahar , Hariprasada R. Kanna Reddy
IPC: A01N47/28 , A61K8/49 , A61L2/232 , A61L29/14 , A61L31/14 , A61Q5/02 , A61Q15/00 , A61Q19/00 , A61Q19/10 , C09D5/14 , A01N33/08 , A61K8/41 , A61K8/42 , A61K31/166 , A01N43/56 , A01N47/12 , A01N43/54 , A01N37/40 , A01N33/10 , A01N37/30 , C07C217/58 , C07C271/20 , C07C211/29 , C07C275/14 , A01N43/40 , A61K31/125 , C07C211/27 , A01N43/10 , C07D317/58 , C07C233/78 , A01N33/04 , A01N37/18 , A01N43/84 , A01N43/30 , C07D295/135 , A61K31/135 , A61L2/18 , A61L2/22 , A61L2/235 , A61L12/14 , C08K5/17
CPC classification number: A01N47/28 , A01N33/04 , A01N33/08 , A01N33/10 , A01N37/18 , A01N37/30 , A01N37/40 , A01N43/10 , A01N43/30 , A01N43/40 , A01N43/54 , A01N43/56 , A01N43/84 , A01N47/12 , A61K8/41 , A61K8/42 , A61K8/49 , A61K8/4926 , A61K8/494 , A61K8/4953 , A61K8/4973 , A61K8/4986 , A61K31/135 , A61K31/166 , A61L2/18 , A61L2/22 , A61L2/232 , A61L2/235 , A61L12/14 , A61L29/14 , A61L31/14 , A61L2202/21 , A61L2202/24 , A61Q5/02 , A61Q15/00 , A61Q19/007 , A61Q19/10 , C07C211/27 , C07C211/29 , C07C217/58 , C07C233/78 , C07C271/20 , C07C275/14 , C07C2601/14 , C07D295/135 , C07D317/58 , C08K5/17 , C09D5/14
Abstract: Compounds, compositions, and methods comprising a polyamine compound are described, which may be used to kill, disperse, treat, or reduce biofilms, or to inhibit or substantially prevent biofilm formation. In certain aspects, the present invention relates to compounds, compositions, and methods comprising polyamine compounds that have antimicrobial or dispersing activity against a variety of bacterial strains capable of forming biofilms.
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公开(公告)号：US09682927B2
公开(公告)日：2017-06-20
申请号：US15170848
申请日：2016-06-01
Applicant: Lantheus Medical Imaging, Inc.
Inventor： Ajay Purohit , Pedro Benites , Edward H. Cheesman , Richard R. Cesati , Richard J. Looby , Heike S. Radeke
IPC: A61K51/00 , A61M36/14 , C07C303/30 , A61K51/04 , C07B59/00 , C07C53/06 , C07C217/58 , C07C255/54 , C07C277/08 , C07C279/10 , C07C279/24 , C07C309/65 , C07C309/66 , C07C309/73 , C07C53/10 , C07C53/18 , C07C63/08 , C07C213/02 , C07C303/28 , C07C309/04 , C07C309/30 , C07C277/00
CPC classification number: C07C303/30 , A61K51/00 , A61K51/04 , A61K51/0406 , C07B59/001 , C07B2200/05 , C07C53/06 , C07C53/10 , C07C53/18 , C07C63/08 , C07C213/02 , C07C217/58 , C07C255/54 , C07C277/00 , C07C277/08 , C07C279/10 , C07C279/24 , C07C303/28 , C07C309/04 , C07C309/30 , C07C309/65 , C07C309/66 , C07C309/73 , C07C279/08
Abstract: The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.
