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序号 专利名 申请号 申请日 公开(公告)号 公开(公告)日 发明人
41 Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof US15994348 2018-05-31 US10149842B2 2018-12-11 James Densmore Copp; Ann W. Newman; Anne Luong
Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
42 Chimeric compounds targeting proteins, compositions, methods, and uses thereof US15597671 2017-05-17 US10144745B2 2018-12-04 Kyle W. H. Chan; Leah Fung; Robert Sullivan; Paul E. Erdman; Frank Mercurio; Eduardo Torres
The present invention provides chimeric compounds that modulate protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, TNF-alpha activity, CK1-alpha activity and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant rejection, and cancer, are provided.
43 SOLID FORMS OF {[5-(3-CHLOROPHENYL)-3-HYDROXYPYRIDINE-2-CARBONYL]AMINO}ACETIC ACID, COMPOSITIONS, AND USES THEREOF US15994348 2018-05-31 US20180280365A1 2018-10-04 James Densmore Copp; Ann W. Newman; Anne Luong
Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino} acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
44 CHIMERIC COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF US15892267 2018-02-08 US20180230167A1 2018-08-16 Kyle W. H. Chan; Leah Fung; Robert Sullivan; Paul E. Erdman; Frank Mercurio; Eduardo Torres
The present invention provides chimeric compounds that modulate protein function, to restore protein homeostasis, including cytokine, aiolos, and/or ikaros activity, TNF-alpha activity, CK1-alpha activity and cell-cell adhesion. The invention provides methods of modulating protein-mediated diseases, such as cytokine-mediated diseases, disorders, conditions, or responses. Compositions, including in combination with other cytokine and inflammatory mediators, are provided. Methods of treatment, amelioration, or prevention of protein-mediated diseases, disorders, and conditions, such as cytokine-mediated diseases, disorders, and conditions, including inflammation, fibromyalgia, rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, psoriasis, psoriatic arthritis, inflammatory bowel diseases, Crohn's disease, ulcerative colitis, uveitis, inflammatory lung diseases, chronic obstructive pulmonary disease, Alzheimer's disease, organ transplant rejection, and cancer, are provided.
45 Solid forms of {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions, and uses thereof US15608186 2017-05-30 US09987262B2 2018-06-05 James Densmore Copp; Ann W. Newman; Anne Luong
Provided herein are solid forms comprising {[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl]amino}acetic acid, compositions comprising the solid forms, methods of making the solid forms and methods of their use for the treatment of various diseases and/or disorders.
46 NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS US15837048 2017-12-11 US20180099976A1 2018-04-12 Mui Cheung; Michael P. Demartino; Hilary Schenck Eidam; Huiping Amy Guan; Donghui Qin; Chengde Wu; Zhen Gong; Haiying Yang; Haiyu Yu; Zhiliu Zhang
This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
47 Compounds as rearranged during transfection (RET) inhibitors US15509569 2015-09-10 US09879021B2 2018-01-30 Mui Cheung; Michael P. Demartino; Hilary Schenck Eidam; Huiping Amy Guan; Donghui Qin; Chengde Wu; Zhen Gong; Haiying Yang; Haiyu Yu; Zhiliu Zhang
This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
48 Dihydropyrimidinone derivatives US15628476 2017-06-20 US09856232B1 2018-01-02 Mashooq Ahmad Bhat; Mohamed Abdulrahman Al-Omar
A dihydropyrimidinone derivative includes a compound having a chemical structure according to Formula 1: wherein Z is selected from CH2O, O, and N; X is selected from O and S; and R represents aryl, substituted aryl, heteroaryl, or substituted heteroaryl, wherein the substituted aryl or substituted heteroaryl have one or more substituents selected from the group consisting of halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, nitro, hydroxyl, alkylthio, alkylamino, heteroaryl, aryloxy, haloaryloxy, arylthio, arylamino, and pharmaceutically acceptable salts thereof. The present subject matter also relates to a method of making a dihydropyrimidinone derivative, a method of treating a gastrointestinal disease, a method of treating an ulcer, a pharmaceutical composition, and a method of making a pharmaceutical composition.
49 NOVEL COMPOUNDS AS REARRANGED DURING TRANSFECTION (RET) INHIBITORS US15509569 2015-09-10 US20170298074A1 2017-10-19 Mui CHEUNG; Michael P. DEMARTINO; Hilary Schenck EIDAM; Huiping Amy GUAN; Donghui QIN; Chengde WU; Zhen GONG; Haiying YANG; Haiyu YU; Zhiliu ZHANG
This invention relates to novel compounds which are inhibitors of the Rearranged during Transfection (RET) kinase, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination, for the normalization of gastrointestinal sensitivity, motility and/or secretion and/or abdominal disorders or diseases and/or treatment related to diseases related to RET dysfunction or where modulation of RET activity may have therapeutic benefit including but not limited to all classifications of irritable bowel syndrome (IBS) including diarrhea-predominant, constipation-predominant or alternating stool pattern, functional bloating, functional constipation, functional diarrhea, unspecified functional bowel disorder, functional abdominal pain syndrome, chronic idiopathic constipation, functional esophageal disorders, functional gastroduodenal disorders, functional anorectal pain, inflammatory bowel disease, proliferative diseases such as non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, medullary thyroid cancer, follicular thyroid cancer, anaplastic thyroid cancer, papillary thyroid cancer, brain tumors, peritoneal cavity cancer, solid tumors, other lung cancer, head and neck cancer, gliomas, neuroblastomas, Von Hippel-Lindau Syndrome and kidney tumors, breast cancer, fallopian tube cancer, ovarian cancer, transitional cell cancer, prostate cancer, cancer of the esophagus and gastroesophageal junction, biliary cancer, adenocarcinoma, and any malignancy with increased RET kinase activity.
50 Synthesis of substituted salicylaldehyde derivatives US14496514 2014-09-25 US09371334B2 2016-06-21 Jay J. Farmer; Gabriel E. Job
Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).
51 Polymer-bonded polycyclic aromatic hydrocarbons having nitrogen containing substituents US13673418 2012-11-09 US09249320B2 2016-02-02 Cecile Pasquier; Patrick Wyss
A polymer-bonded polycyclic aromatic hydrocarbon compound of general formula (1): (P—O)x-Q-(Y)w  (1) wherein P represents a polymeric moiety having at least three repeating units which comprise an optionally substituted phenyl ring; Q represents a perylene, quaterrylene or terrylene moiety; Y is selected from (i) halogen and (ii) optionally substituted N-heterocycloaliphatic groups having from 3 to about 8 ring members which are bonded to Q through an N atom, provided that at least one Y represents (ii); x represents an integer of from 1 to 4; w represents an integer of from 1 to 4. Also, are provided processes of producing the compounds, polymers, markings and articles, and methods of authenticating.
52 ELECTRONICALLY CONDUCTIVE POLYMER BINDER FOR LITHIUM-ION BATTERY ELECTRODE US14790299 2015-07-02 US20150311529A1 2015-10-29 Gao Liu; Shidi Xun; Vincent S. Battaglia; Honghe Zheng; Mingyan Wu
A family of carboxylic acid groups containing fluorene/fluorenon copolymers is disclosed as binders of silicon particles in the fabrication of negative electrodes for use with lithium ion batteries. Triethyleneoxide side chains provide improved adhesion to materials such as, graphite, silicon, silicon alloy, tin, tin alloy. These binders enable the use of silicon as an electrode material as they significantly improve the cycle-ability of silicon by preventing electrode degradation over time. In particular, these polymers, which become conductive on first charge, bind to the silicon particles of the electrode, are flexible so as to better accommodate the expansion and contraction of the electrode during charge/discharge, and being conductive promote the flow battery current.
53 Electronically conductive polymer binder for lithium-ion battery electrode US13615402 2012-09-13 US09077039B2 2015-07-07 Gao Liu; Shidi Xun; Vincent S. Battaglia; Honghe Zheng; Mingyan Wu
A family of carboxylic acid groups containing fluorene/fluorenon copolymers is disclosed as binders of silicon particles in the fabrication of negative electrodes for use with lithium ion batteries. Triethyleneoxide side chains provide improved adhesion to materials such as, graphite, silicon, silicon alloy, tin, tin alloy. These binders enable the use of silicon as an electrode material as they significantly improve the cycle-ability of silicon by preventing electrode degradation over time. In particular, these polymers, which become conductive on first charge, bind to the silicon particles of the electrode, are flexible so as to better accommodate the expansion and contraction of the electrode during charge/discharge, and being conductive promote the flow battery current.
54 Synthesis of substituted salicylaldehyde derivatives US13825548 2011-09-22 US08859822B2 2014-10-14 Jay J. Farmer; Gabriel E. Job
Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).
55 {[5-(3-클로로페닐)-3-하이드록시피리딘-2-카보닐]아미노}아세트산의 고체형, 이의 조성물 및 용도 KR1020167015508 2014-11-14 KR1020160083118A 2016-07-11 콥,제임스,덴스모어; 뉴먼,앤,더블유.; 르엉,앤
{[5-(3-클로로페닐)-3-하이드록시피리딘-2-카보닐]아미노}아세트산을포함하는고체형, 상기고체형을포함하는조성물, 상기고체형의제조방법및 다양한질환및/또는장애의치료를위한이의사용방법이본원에제공된다.
56 치환된 살리실알데하이드 유도체의 합성 KR1020137009113 2011-09-22 KR1020130109133A 2013-10-07 파머제이제이.; 잡가브리엘이.
본 발명은 무엇보다도 다음 단계를 포함하는 살리실알데하이드 유도체의 합성 방법을 포함한다: a) 살리실알데하이드 또는 이것의 유도체를 제공하는 단계, b) 제공된 살리실알데하이드 화합물의 무수 다이머를 형성하는 단계, c) 무수 다이머 상의 하나 이상의 화학적 변환을 수행하는 단계 및 d) 무수 다이머를 가수분해시켜 단계 (a)에서 제공된 것과 상이한 살리실알데하이드 유도체를 제공하는 단계.
57 질소 함유 치환기를 갖는 중합체 결합 폴리시클릭 방향족 탄화수소 KR1020147013192 2012-10-30 KR101916987B1 2018-11-08 파스키에세실; 위스패트릭
본발명은하기화학식(1)의중합체결합폴리시클릭방향족탄화수소화합물에관한것이다:상기식에서, P는임의로치환된페닐고리를포함하는 3개이상의반복단위를갖는중합체부분을나타내며; Q는퍼릴렌, 쿼터릴렌또는터릴렌부분을나타내고; Y는 (i) 할로겐및 (ii) N 원자를통해 Q에결합되는 3 내지약 8개의고리멤버를갖는임의로치환된 N-헤테로시클로지방족기로부터선택되나, 단하나이상의 Y는 (ii)를나타내며; x는 1 내지 4의정수를나타내고; w는 1 내지 4의정수를나타낸다. 본발명은추가로이러한화합물의제조방법, 및인쇄용잉크조성물에서이의용도에관한것이며, 이조성물은특히마킹(marking) 또는보안피처(security fearture)를만들기위해사용될수 있다.
58 질소 함유 치환기를 갖는 중합체 결합 폴리시클릭 방향족 탄화수소 KR1020147013192 2012-10-30 KR1020140091558A 2014-07-21 파스키에세실; 위스패트릭
본 발명은 하기 화학식(1)의 중합체 결합 폴리시클릭 방향족 탄화수소 화합물에 관한 것이다:

상기 식에서, P는 임의로 치환된 페닐 고리를 포함하는 3개 이상의 반복 단위를 갖는 중합체 부분을 나타내며;
Q는 퍼릴렌, 쿼터릴렌 또는 터릴렌 부분을 나타내고;
Y는 (i) 할로겐 및 (ii) N 원자를 통해 Q에 결합되는 3 내지 약 8개의 고리 멤버를 갖는 임의로 치환된 N-헤테로시클로지방족 기로부터 선택되나, 단 하나 이상의 Y는 (ii)를 나타내며;
x는 1 내지 4의 정수를 나타내고; w는 1 내지 4의 정수를 나타낸다.
본 발명은 추가로 이러한 화합물의 제조 방법, 및 인쇄용 잉크 조성물에서 이의 용도에 관한 것이며, 이 조성물은 특히 마킹(marking) 또는 보안 피처(security fearture)를 만들기 위해 사용될 수 있다.
59 SYNTHESIS OF SUBSTITUTED SALICYLALDEHYDE DERIVATIVES PCT/US2011052748 2011-09-22 WO2012040454A3 2012-05-10 FARMER JAY J; JOB GABRIEL E
Among other things, the present invention encompasses methods of synthesizing salicylaldehyde derivatives comprising the steps of: a) providing salicylaldehyde or a derivative thereof, b) forming an anhydro dimer of the provided salicylaldehyde compound, c) performing one or more chemical transformations on the anhydro dimer and d) hydrolyzing the anhydro dimer to provide a salicylaldehyde derivative different from that provided in step (a).
60 POLYMER-BONDED POLYCYCLIC AROMATIC HYDROCARBONS HAVING NITROGEN CONTAINING SUBSTITUENTS PCT/EP2012071449 2012-10-30 WO2013068275A8 2014-10-02 PASQUIER CÉCILE; WYSS PATRICK
The invention concerns a polymer-bonded polycyclic aromatic hydrocarbon compound of general formula (1): (P—O) x —Q—(Y) w (1) wherein P represents a polymeric moiety having at least three repeating units which comprise an optionally substituted phenyl ring; Q represents a perylene, quaterrylene or terrylene moiety; Y is selected from (i) halogen and(ii) optionally substituted N-heterocycloaliphatic groups having from 3 to about 8 ring members which are bonded to Q through an N atom, provided that at least one Y represents(ii); x represents an integer of from 1 to 4; w represents an integer of from 1 to 4. The invention further concerns a process for making such a compound, and the use thereof in a printing ink composition, which can be used in particular for making marking or security features.
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