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1. 发明申请

US20180273531A1 PYRIMIDINE COMPOUND AND MEDICAL USE THEREOF 审中-公开
公开(公告)号：US20180273531A1
公开(公告)日：2018-09-27
申请号：US15795973
申请日：2017-10-27
申请人： Japan Tobacco Inc.
发明人： Hisashi KAWASAKI , Hiroyuki ABE , Kazuhide HAYAKAWA , Tetsuya IIDA , Shinichi KIKUCHI , Takayuki YAMAGUCHI , Toyomichi NANAYAMA , Hironori KURACHI , Masahiro TAMARU , Yoshikazu HORI , Mitsuru TAKAHASHI , Takayuki YOSHIDA , Toshiyuki SAKAI
IPC分类号： C07D471/04 , C07F9/53 , C07D487/04 , C07C275/30 , C07D239/62 , C07D239/545 , C07C275/50 , C07D471/16
CPC分类号： C07D471/04 , A61K31/519 , C07C275/30 , C07C275/50 , C07C2601/16 , C07D239/545 , C07D239/553 , C07D239/62 , C07D471/16 , C07D487/04 , C07F9/53
摘要： The present invention relates to a pyrimidine compound or a pharmaceutically acceptable salt thereof represented by the following formula [I] wherein each symbol is as defined in the specification and a method of therapeutically or prophylactically treating an undesirable cell proliferation, comprising administering such a compound. The compound of the present invention has superior activity in suppressing undesirable cell proliferation, particularly, an antitumor activity, and is useful as an antitumor agent for the prophylaxis or treatment of cancer, rheumatism, and the like. In addition, the compound of the present invention can be a more effective antitumor agent when used in combination with other antitumor agents such as an alkylating agent or metabolism antagonist.

2. 发明授权

US10060892B2 Tripodal nitrate receptor 有权
公开(公告)号：US10060892B2
公开(公告)日：2018-08-28
申请号：US15310601
申请日：2014-12-11
申请人： University of Oregon
发明人： Michelle Watt , Darren W. Johnson , Michael M. Haley
IPC分类号： G01N31/00 , G01N31/22 , C07C275/30 , C07C275/34 , C07C335/18 , C07C275/42 , C07C335/16 , C07D251/24
CPC分类号： G01N31/227 , C07C275/30 , C07C275/34 , C07C275/42 , C07C335/16 , C07C335/18 , C07C335/20 , C07D251/24 , G01N31/22
摘要： A compound, or a protonate or salt thereof, having a formula I of: wherein Y represents an optionally substituted aromatic group; n is 1 or 2; a is 0 to 4; R1 and R2 are each independently H; optionally substituted alkyl; optionally substituted aralkyl; acyl; phosphonyl; —SO2R12; —C(O)R13; —C(O)OR14; —C(O)NR15R16; —C(O)CH2R17; or —C(S)—NR18R19; —S(O)R20; or —SO2NR21R22, wherein R12-R22 are each independently H, optionally substituted alkyl, optionally substituted aralkyl, optionally substituted aryl, or —C(O)R23, wherein R23 is H, optionally substituted alkyl, optionally substituted aralkyl, or optionally substituted aryl; and each R3 is independently optionally substituted alkyl, halogen, optionally substituted alkoxy, optionally substituted carboxyl, amide; amino; or nitro.

3. 发明授权

US09974772B2 Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators 有权
公开(公告)号：US09974772B2
公开(公告)日：2018-05-22
申请号：US15408643
申请日：2017-01-18
申请人： Allergan, Inc.
发明人： Richard L. Beard , Tien T. Duong , John E. Donello , Veena Viswanath , Michael E. Garst
IPC分类号： A61K31/417 , A61K31/198 , A61K31/17 , A61K31/4045 , A61K31/216 , A61K31/197 , C07C323/60 , C07C317/50 , C07C323/44 , C07C317/42 , C07D233/64 , C07C275/30 , C07D209/20 , C07K5/062 , C07K5/078 , C07K5/072
CPC分类号： A61K31/417 , A61K31/17 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/4045 , C07C275/30 , C07C317/42 , C07C317/50 , C07C323/44 , C07C323/60 , C07D209/20 , C07D233/64 , C07K5/06017 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K5/06113 , C07K5/06147 , C07K5/06156 , Y02A50/401
摘要： The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

4. 发明授权

US09868700B2 Carbamoyl hydrazine derivatives as formyl peptide modulators 有权
公开(公告)号：US09868700B2
公开(公告)日：2018-01-16
申请号：US15457049
申请日：2017-03-13
申请人： Allergan, Inc.
发明人： Vidyasagar Vuligonda , Thong Vu , Veena Viswanath , John E. Donello , Richard L. Beard
IPC分类号： C07C281/08 , C07C275/30
CPC分类号： C07C275/30 , C07C281/06
摘要： The present invention relates to carbamoyl hydrazine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the FPR receptor.

5. 发明申请

US20170305840A1 SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
公开(公告)号：US20170305840A1
公开(公告)日：2017-10-26
申请号：US15374329
申请日：2016-12-09
申请人： Paratek Pharmaceuticals, Inc.
发明人： Mark L. Nelson , Kwasi Ohemeng , Paul Abato , Victor Amoo , Haregewein Assefa , Joel Berniac , Beena Bhatia , Todd Bowser , Jackson Chen , Mark Grier , Laura Honeyman , Mohamed Y. Ismail , Oak K. Kim , Jude Mathews , Rachid Mechiche
IPC分类号： C07C237/48 , C07C275/28 , C07C271/54 , C07C271/22 , C07C275/30 , C07C237/26 , C07C2603/46 , A61K31/65 , C07C2601/14 , C07C2601/16 , C07C2601/02
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46 , Y02A50/411 , Y02A50/473
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.

7. 发明申请

US20170231999A1 IDO INHIBITORS 审中-公开
公开(公告)号：US20170231999A1
公开(公告)日：2017-08-17
申请号：US15584818
申请日：2017-05-02
申请人： BRISTOL-MYERS SQUIBB COMPANY
发明人： James Aaron Balog , Emily Charlotte Cherney , Weiwei Guo , Audris Huang , Jay A. Markwalder , Steven P. Seitz , Weifang Shan , David K. Williams , Natesan Murugesan , Susheel Jethanand Nara , Saumya Roy , Soodamani Thangavel , Ramesh Kumar Sistla , Srinivas Cheruku , Srinivasan Thangathirupathy , Yadagiri Kanyaboina , Nagalakshmi Pulicharla
IPC分类号： A61K31/538 , A61K31/17 , A61K31/196 , A61K31/277 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/428 , A61K31/437 , A61K31/445 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/5377 , A61K39/395 , A61K45/06
CPC分类号： C07C275/40 , A61K31/17 , A61K31/196 , A61K31/277 , A61K31/351 , A61K31/382 , A61K31/397 , A61K31/428 , A61K31/437 , A61K31/445 , A61K31/501 , A61K31/505 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/5377 , A61K31/538 , A61K39/3955 , A61K39/39558 , A61K45/06 , C07C229/42 , C07C233/81 , C07C235/38 , C07C235/56 , C07C255/57 , C07C255/58 , C07C275/30 , C07C275/42 , C07D205/04 , C07D207/08 , C07D207/12 , C07D211/08 , C07D211/14 , C07D239/34 , C07D239/47 , C07D265/30 , C07D265/36 , C07D277/64 , C07D295/155 , C07D307/22 , C07D309/04 , C07D309/14 , C07D317/46 , C07D335/02 , C07D401/12 , C07D405/12 , C07D405/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D487/04 , C07D487/08
摘要： There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.

8. 发明申请

US20170119737A1 AMIDE DERIVATIVES OF N-UREA SUBSTITUTED AMINO ACIDS AS FORMYL PEPTIDE RECEPTOR LIKE-1 (FPRL-1) RECEPTOR MODULATORS 有权
公开(公告)号：US20170119737A1
公开(公告)日：2017-05-04
申请号：US15408643
申请日：2017-01-18
申请人： Allergan, Inc.
发明人： Richard L. Beard , Tien T. Duong , John E. Donello , Veena Viswanath , Michael E. Garst
IPC分类号： A61K31/417 , A61K31/4045 , A61K31/216 , A61K31/198 , A61K31/17
CPC分类号： A61K31/417 , A61K31/17 , A61K31/197 , A61K31/198 , A61K31/216 , A61K31/4045 , C07C275/30 , C07C317/42 , C07C317/50 , C07C323/44 , C07C323/60 , C07D209/20 , C07D233/64 , C07K5/06017 , C07K5/06034 , C07K5/06052 , C07K5/0606 , C07K5/06113 , C07K5/06147 , C07K5/06156 , Y02A50/401
摘要： The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.

9. 发明申请

US20160318856A1 Substituted Urea eIF2alpha Kinase Activators 审中-公开
标题翻译：取代尿素eIF2α激酶
公开(公告)号：US20160318856A1
公开(公告)日：2016-11-03
申请号：US14917718
申请日：2014-09-11
申请人： THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
发明人： Bertal Aktas , Michael Chorev
IPC分类号： C07C275/30 , C07D213/65 , C07C275/40 , C07C275/34 , C07C335/16
CPC分类号： C07C275/30 , C07C275/28 , C07C275/34 , C07C275/40 , C07C275/42 , C07C335/16 , C07C335/18 , C07C335/20 , C07C2601/08 , C07C2601/14 , C07D213/64 , C07D213/65 , C07D295/13
摘要： This disclosure relates to substituted urea eIF2α kinase activators including methods of making and using the same. For example, such activators can include cycloalkyl aryl ureas, which activate at least one eIF2α kinase. These compounds may be useful for treatment of diseases such as, for example, cancer, hemolytic anemia not caused by infectious agents, Wolcott-Rallison syndrome, neurodegenerative disease, tuberous sclerosis complex, fragile-X syndrome, autism spectrum disorder, and ribosomal defect disease.
摘要翻译：本公开涉及取代的脲eIF2α激酶激活剂，包括制备和使用其的方法。例如，这种活化剂可以包括活化至少一种eIF2α激酶的环烷基芳基脲。这些化合物可用于治疗疾病，例如癌症，不由感染因素引起的溶血性贫血，Wolcott-Rallison综合征，神经变性疾病，结节性硬化综合征，脆性X综合征，自闭症谱系障碍和核糖体缺陷病。

10. 发明申请

US20160279235A1 Heterodimers of Glutamic Acid 审中-公开
标题翻译：谷氨酸的异二聚体
公开(公告)号：US20160279235A1
公开(公告)日：2016-09-29
申请号：US15068841
申请日：2016-03-14
申请人： Molecular Insight Pharmaceuticals, Inc.
发明人： John W. Babich , Craig N. Zimmerman , Kevin P. Maresca
IPC分类号： A61K39/385
CPC分类号： C07C275/16 , A61K39/385 , C07B59/001 , C07C275/24 , C07C275/30 , C07C311/19 , C07D213/38
摘要： Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR′R′, Q is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Y is C(O), O, NR′, S, S(O)2, C(O)2 (CH2)p Z is H or C1-C4 alkyl, R′ is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR′R′ or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition. Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.
摘要翻译：式（Ia）化合物其中R是C 6 -C 12取代或未取代的芳基，C 6 -C 12取代或未取代的杂芳基，C 1 -C 6取代或未取代的烷基或-NR'R'，Q是 C（O），O，NR'，S，S（O）2，C（O）2（CH 2）p Y是C（O），O，NR'，S，S（O））2（CH 2）p Z是H或C 1 -C 4烷基，R'是H，C（O），S（O）2，C（O）2，C 6 -C 12取代或未取代的芳基，当被取代，芳基，杂芳基和烷基被卤素，C 6 -C 12杂芳基，-NR'R'或COOZ取代时，C 6 -C 12取代或未取代的杂芳基或C 1 -C 6取代或未取代的烷基，其具有诊断和治疗性质，例如前列腺癌的治疗和治疗以及与NAALADase抑制相关的其它疾病。放射性标记可以通过各种通过碳或杂原子连接在X氨基酸侧链附着的假基团并入结构中。

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