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1. 发明申请

WO2023067061A1 PRECURSORS FOR THE PREPARATION OF DL-METHIONINE AND DLLD-METHIONYLMETHIONINE 审中-公开
公开(公告)号：WO2023067061A1
公开(公告)日：2023-04-27
申请号：PCT/EP2022/079209
申请日：2022-10-20
申请人： EVONIK OPERATIONS GMBH
发明人： HÄUßNER, Thomas , BRAUNE, Sascha , HASSEBERG, Hans-Albrecht
IPC分类号： C07D233/76 , C07D241/08
摘要： The invention provides the chemical compound of formula (II), a composition comprising methionine hydantoin, DKP (I), Hyd-Met (II), BMU (III), optionally methionylmethionine and water, and also the use thereof for the optionally simultaneous production of methionylmethionine and methionine, and also corresponding production processes.

2. 发明申请

WO2022133551A1 HISTONE DEACETYLASE INHIBITORS 审中-公开
公开(公告)号：WO2022133551A1
公开(公告)日：2022-06-30
申请号：PCT/AU2021/051558
申请日：2021-12-23
申请人： THE UNIVERSITY OF QUEENSLAND
发明人： FAIRLIE, David , LIU, Ligong , REID, Robert , MAK, Jeffrey
IPC分类号： C07C259/10 , A61P3/00 , A61P9/00 , A61P13/12 , A61P19/02 , A61P29/00 , A61P35/00 , A61P37/00 , A61P43/00 , C07C275/24 , C07C275/28 , C07D207/12 , C07D207/34 , C07D209/18 , C07D209/46 , C07D209/48 , C07D213/56 , C07D213/64 , C07D213/74 , C07D215/40 , C07D233/64 , C07D233/72 , C07D233/90 , C07D235/02 , C07D235/08 , C07D239/36 , C07D239/42 , C07D239/54 , C07D239/91 , C07D239/96 , C07D241/08 , C07D241/20 , C07D243/08 , C07D249/06 , C07D275/06 , C07D471/04
摘要： The present application is directed towards compounds, pharmaceutically acceptable salts or prodrugs thereof, which are inhibitors of Histone Deacetylase (HDAC) binding or function. The compounds especially may have some selectivity for inhibiting Class IIa versus Class I HDACs. The present application also relates to methods of using the compounds and to uses of the compounds, especially in relation to the prevention of a disease, disorder or condition associated with Class IIa HDAC activity. In one form, the compounds are (ortho-phenyl) phenyl hydroxamates. In another form, the compounds are as provided in Formula (I), wherein R1 is a phenyl or cycloalkenyl which may be optionally substituted. Formula (I)

3. 发明申请

WO2021252661A1 ALLOSTERIC EGFR INHIBITORS AND METHODS OF USE THEREOF 审中-公开
公开(公告)号：WO2021252661A1
公开(公告)日：2021-12-16
申请号：PCT/US2021/036657
申请日：2021-06-09
申请人： DANA-FARBER CANCER INSTITUTE, INC. , SCOTT, David A. , GERO, Thomas , BEYETT, Tyler , HEPPNER, David , GIPSON, Krista E. , HUANG, Shih-Chung , STROUD, Steve
发明人： SCOTT, David A. , GERO, Thomas , BEYETT, Tyler , HEPPNER, David , GIPSON, Krista E. , HUANG, Shih-Chung , STROUD, Steve
IPC分类号： A61K31/4985 , C07D241/08 , C07D513/04 , A61P35/00 , C07D401/14 , C07D487/04 , C07D495/04
摘要： The disclosure relates to compounds that act as allosteric inhibitors of epidermal growth factor receptor (EGFR); pharmaceutical compositions comprising the compounds; and methods of treating or preventing kinase-mediated disorders, including cancer and other proliferation diseases.

4. 发明申请

WO2020176501A1 COMPOUNDS USEFUL FOR INHIBITING RAF DIMERS 审中-公开
公开(公告)号：WO2020176501A1
公开(公告)日：2020-09-03
申请号：PCT/US2020/019695
申请日：2020-02-25
申请人： ALBERT EINSTEIN COLLEGE OF MEDICINE
发明人： GAVATHIOTIS, Evripidis , AGIANIAN, Bogos
IPC分类号： C07D211/44 , C07D241/08 , C07D265/32 , C07D265/33 , C07D295/13 , C07D295/205 , C07D401/04 , C07D403/04 , C07D487/04 , A61P35/00 , A61K31/5377 , A61K31/506 , A61K31/495 , A61K31/5025 , A61K31/5375 , A61K31/496 , A61K31/5395 , A61K31/501
摘要： The disclosure provides compounds of Formula I (Formula I) (c) And the pharmaceutically acceptable salts thereof. The A, B, C, and D rings and the variables, R A , R B , R C , R D , L 0 , L 1 , L 2 , and L 2 , are defined herein. Compounds and salts of Formula I are useful as inhibitors of RAF kinase dimerization, including dimerization of wild type and mutant BRAF kinases. The disclosure includes pharmaceutical compositions comprising a compound or salt of Formula I. The disclosure also includes methods of treating a cancer susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization, comprising administering a therapeutically effective amount of a compound or salt of Formula I to a patient in need of such treatment. These cancers susceptible to treatment with an inhibitor of BRAF dimers or BRAF dimerization include melanoma, thyroid cancer, hairy cell leukemia, ovarian cancer, lung cancer, and colorectal cancer.

5. 发明申请

WO2020006341A1 (S)-3-(2-(4-(BENZYL)-3-OXOPIPERAZIN-1-YL)ACETAMIDO)-4-OXO-5-(2,3,5,6-TETRAFLUOROPHENOXY)PENTANOIC ACID DERIVATIVES AND RELATED COMPOUNDS AS CASPASE INHIBITORS FOR TREATING CARDIOVASCULAR DISEASES 审中-公开
公开(公告)号：WO2020006341A1
公开(公告)日：2020-01-02
申请号：PCT/US2019/039702
申请日：2019-06-28
申请人： CONATUS PHARMACEUTICALS, INC.
发明人： SPADA, Alfred, P. , TERNANSKY, Robert, J.
IPC分类号： C07D241/08 , C07D295/22 , C07D401/06 , C07D409/06 , C07D405/06 , C07D403/06 , C07D471/04 , C07D491/04 , C07D239/34 , C07D241/52 , A61K31/495 , A61K31/496 , A61P9/00 , A61P13/12 , A61P1/16 , A61P11/00 , A61P17/00 , A61P19/02 , A61P25/00 , A61P37/00 , A61P29/00 , A61P31/00
摘要： The present invention relates to (S)-3-(2-(4-(benzyl)-3-oxopiperazin-l- yl)acetamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid derivatives and related compounds as caspase inhibitors for treating e.g. cardiovascular, kidney, liver, lung, skin, joints, CNS, inflammatory and autoimmune diseases.

6. 发明申请

WO2018227620A1 SYNTHESIS METHOD FOR PRODUCING ENANTIOMERICALLY PURE CIS-IMIDAZOLINE COMPOUNDS FOR PHARMACEUTICAL USE 审中-公开
公开(公告)号：WO2018227620A1
公开(公告)日：2018-12-20
申请号：PCT/CN2017/088787
申请日：2017-06-16
申请人： UNITY BIOTECHNOLOGY, INC. , CHEN, Bing
发明人： CHEN, Bing , VON GELDERN, Thomas W. , BACKES, Bradley
IPC分类号： C07C233/64 , C07D233/22 , C07D401/04 , C07D241/08 , A61P35/00 , A61Q19/08
摘要： Disclosed is a method for enantioselective synthesis of cis-imidazolines and related structures through chiral resolution. A chiral acid is used to separate enantiomeric precursors of the cis-imidazolines from a racemic mixture by selective crystallization. Both enantiomers can be cyclized into the desired cis-imidazoline by complementary pathways. Compounds can be synthesized with an enantiomeric excess as high as 99％ and may be used for treating cancer, killing senescent cells, or treating senescence-associated conditions.

7. 发明申请

WO2016046398A1 NOVEL CHIRAL SYNTHESIS OF N-ACYL-(3-SUBSTITUTED)-(8-SUBSTITUTED)-5,6-DIHYDRO-[1,2,4]TRIAZOLO[4,3-A]PYRAZINES 审中-公开
标题翻译： N-（3-取代的） - （8-取代的）-5,6-二氢 - [1,2,4]三唑并[4,3-A]吡咯的新颖的合成
公开(公告)号：WO2016046398A1
公开(公告)日：2016-03-31
申请号：PCT/EP2015/072167
申请日：2015-09-25
申请人： EUROSCREEN SA
发明人： HOVEYDA, Hamid , DUTHEUIL, Guillaume
IPC分类号： C07D241/08 , C07D487/04 , C07C231/02 , C07C231/12
CPC分类号： C07D487/04 , C07D241/08
摘要： The present invention relates to a novel chiral synthesis of N-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines of Formula (I), avoiding the use of protection/deprotection steps.
摘要翻译：本发明涉及式（I）的N-酰基 - （3-取代的） - （8-取代）-5,6-二氢 - [1,2,4]三唑并[4,3-a]吡嗪的新型手性合成（一），避免使用保护/脱保护步骤。

8. 发明申请

WO2015194205A1 環状ジペプチド含有組成物审中-公开
标题翻译：循环含肽组合物
公开(公告)号：WO2015194205A1
公开(公告)日：2015-12-23
申请号：PCT/JP2015/054015
申请日：2015-02-13
申请人：サントリーホールディングス株式会社
发明人：鈴木　寿栄 , 富貴澤　伸哉 , 別府　佳紀 , 渡辺　斉志
IPC分类号： C07K5/12 , A23G1/00 , A23G1/30 , A23L1/305 , A23L2/00 , C07D241/08 , C07K5/06
CPC分类号： C07K5/06 , A23G1/00 , A23G1/30 , A23G1/44 , A23L2/00 , A23L2/54 , A23L33/17 , A23L33/18 , A23V2002/00 , C07D241/08 , C07K5/12
摘要：　シクロトリプトファニルチロシン、シクロセリルチロシン、シクロプロリルチロシン、シクロチロシルグリシン、シクロチロシルチロシン、シクロフェニルアラニルチロシン、シクロロイシルチロシン、シクロリシルチロシン、シクロヒスチジルチロシン、シクロアラニルチロシン、シクログルタミルチロシン、シクロバリルチロシン、シクロイソロイシルチロシン、シクロトレオニルチロシン、シクロアスパルチルチロシン、シクロアスパラギニルチロシン、シクログルタミニルチロシン、シクロアルギニルチロシン、及びシクロメチオニルチロシンからなる群より選ばれるチロシン含有環状ジペプチドあるいはその塩を、それぞれ特定量含有する環状ジペプチド含有組成物。本発明の環状ジペプチド含有組成物は、優れた尿酸値低下作用を有するのであり、例えば、高尿酸血症や痛風等の予防又は治療に有用である。
摘要翻译：本发明公开了一种含有特定量的选自以下的含有酪氨酸的环状二肽的环状二肽组合物：环加色素基酪氨酸，环丝氨酸酪氨酸，环丙基酪氨酸，环丙基甘氨酸，环型酪氨酸酪氨酸，环丙基丙氨酰酪氨酸，环己基甲基酪氨酸，环丙基酪氨酸，环组氨基酪氨酸，环丙氨酰酪氨酸，环十二烷基酪氨酸，环戊基酪氨酸，环丙磺酰酪氨酸，环天冬氨酰酪氨酸，环状氨基丁酰酪氨酸，环氨基丁酰酪氨酸，环炔基酪氨酸和环甲硫氨酰酪氨酸; 或其盐。该含有环状二肽的组合物具有优异的尿酸水平降低作用，可用于例如高尿酸血症，痛风等的预防或治疗。

9. 发明申请

WO2015050703A1 INHIBITORS OF BRUTON'S TYROSINE KINASE 审中-公开
标题翻译： BRUTON的酪氨酸激酶抑制剂
公开(公告)号：WO2015050703A1
公开(公告)日：2015-04-09
申请号：PCT/US2014/056050
申请日：2014-09-17
申请人： CHEN, Yi
发明人： CHEN, Yi
IPC分类号： C07D403/10 , C07D241/08 , C07D241/10 , A61K31/496
CPC分类号： C07D403/10 , C07D401/10
摘要： The disclosure includes compounds of Formula (I), wherein R 0 , R 1 , R 2 , R 3 , R 4 , R 5 , and L are defined herein. Also disclosed is a method for treating a neoplastic disease, autoimmune disease, and inflammatory disorder with these compounds.
摘要翻译：本公开内容包括式（I）的化合物，其中R 0，R 1，R 2，R 3，R 4，R 5和L在本文中定义。还公开了用这些化合物治疗肿瘤性疾病，自身免疫性疾病和炎症性疾病的方法。

10. 发明申请

WO2013063468A8 AMINO ACID DERIVATES FUNCTIONALIZED ON THE N- TERMINAL CAPABLE OF FORMING DRUG INCAPSULATING MICROSPHERES 审中-公开
标题翻译：功能化的N-端可能形成药物包封微生物的氨基酸衍生物
公开(公告)号：WO2013063468A8
公开(公告)日：2014-03-06
申请号：PCT/US2012062222
申请日：2012-10-26
申请人： MASSACHUSETTS INST TECHNOLOGY
发明人： DONG YIZHOU , LOVE KEVIN THOMAS , LANGER ROBERT S , ANDERSON DANIEL GRIFFITH , CHEN DELAI , CHEN YI , VEGAS ARTURO JOSE , ALABI AKINLEYE , ZHANG YUNLONG
IPC分类号： C07D207/16 , A61K48/00 , C07C227/18 , C07C229/12 , C07C229/16 , C07C229/22 , C07C229/26 , C07C229/28 , C07D209/20 , C07D233/64 , C07D241/08 , C07D403/06 , C07D487/06 , C12N15/87
CPC分类号： A61K31/7105 , A61K31/711 , A61K47/22 , A61K2121/00 , C07C229/12 , C07C229/22 , C07C229/24 , C07C229/26 , C07C229/36 , C07C237/08 , C07C237/12 , C07C271/22 , C07C279/14 , C07C323/58 , C07D207/16 , C07D209/20 , C07D209/24 , C07D233/64 , C07D241/08 , C07D265/32 , C07D403/06 , C07D413/06 , C07D487/04 , C07D487/06 , C12N15/87 , C12N15/88 , C12Q1/025 , G01N33/15
摘要： Described herein are compounds and compositions that are characterized by the Markush formulae (I), (II), (III), (IV), (V), and (VI) underneath, where at least one terminal amino group is further functionalized by bearing a group of type (i), (ii), or (iii). Such compounds are obtained by reacting a terminal or internal amino group with epoxides, acrylates, or aldehydes bearing lipophilic groups. The resulting amino acid, peptide, polypeptide-lipids (named "APPLs" in the application) are deemed useful as drug delivery systems including nucleotide delivery to cells. Formulae (i), (ii), and (iii).
摘要翻译：本文描述的是其下面具有马库什式（I），（II），（III），（IV），（V）和（VI））的特征的化合物和组合物，其中至少一个末端氨基进一步由（i），（ii）或（iii）类型的组。通过使末端或内部氨基与带有亲脂基团的环氧化物，丙烯酸酯或醛反应来获得这些化合物。所得到的氨基酸，肽，多肽 - 脂质（在本申请中命名为“APPL”）被认为可用作药物递送系统，包括向细胞递送的核苷酸。式（ⅰ），（ⅱ）和（ⅲ）。

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