| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 121 | Takiso - water-soluble onium salt of diterpenoid | JP51870995 | 1995-01-10 | JP3778928B2 | 2006-05-24 | ケー． ガイ，ロドニー; ニコラウ，ケー．シー．; ピトシノス，エマニュエル; ラシドロ，ウォルフギャング |
| 122 | Antiviral substituted 1,3-oxathiolane | JP2001059730 | 2001-03-05 | JP2001226373A | 2001-08-21 | BELLEAU BERNARD; NGUYEN-BA NGHE |
| PROBLEM TO BE SOLVED: To provide a new substituted 1,3-oxathiolane cyclic compound having pharmacological activity. SOLUTION: This new compound is a cis-2-hydroxymethyl-5-(thymine-N-1'- yl)-1,3-oxathiolane compound in the form of a single enantiomer or an enantiomeric mixture. COPYRIGHT: (C)2001,JPO | ||||||
| 123 | Methods for preparing substituted 1,3-oxathiolane having antiviral properties | JP51462194 | 1992-12-21 | JP3160291B2 | 2001-04-25 | エイ． エバンズ，コリーン; ザチャリー，ブロス; ジン，ホールン; エイチ． エル． ツセ，アラン; ヌギューイェン−バ，ヌゲ; ブロー，ベルナール; マンサー，タレック |
| 124 | Anti-viral substituted 1,3-oxathiolane | JP3132490 | 1990-02-08 | JP2644357B2 | 1997-08-25 | ニェイエン―バ ニェ; ベロー ピエレット; ベロー ベルナール |
| 125 | Antiviral substituted 1,3-oxathiolane | JP20893695 | 1995-08-16 | JPH08119967A | 1996-05-14 | BERUNAARU BEROO; NIE NIYUIENNBA |
| PROBLEM TO BE SOLVED: To obtain the subject new compound capable of readily synthesizing a low toxic effective anti-HIV compound. SOLUTION: This 1,3-oxathiolane is represented by formula I [R 1 is H; Z is S, S=O or SO 2; R 2 is represented by the formula (R 3 is H or a 1-6C alkyl; R 4 is H, hydroxymethyl or the like)], its geometric isomer and/or optical isomer, e.g. 2-benzoyloxymethyl-5-ethoxy-1,3-oxathiolane. The compound is obtained by reacting, e.g. a compound represented by formula III (R 1 is H or an OH protecting group; L is an atom or a leaving group which can be replaced) with a compound represented by the formula R 2-H, then as necessary, removing an optional protecting group and converting the resultant compound into a pharmaceutically acceptable salt. COPYRIGHT: (C)1996,JPO | ||||||
| 126 | Substituted 1,3-oxathiolane with antiviral property | JP3132490 | 1990-02-08 | JPH037282A | 1991-01-14 | BERUNAARU BEROO; PIERETSUTO BEROO; NIE NIEIENNBA |
| NEW MATERIAL: A compound of formula I (R 1 is H; R 2 is a purine base, a pyrimidine base or its analogue or derivative; Z is S, S=O or SO 2). EXAMPLE: cis-2-Hydroxymethyl-5-(cytosin-1'-yl)-1,3-oxathiolane. USE: An antiviral agent. PROCESS: A compound represented by formula II (R 1 is H or a OH protective group; L is a substitutable atom or a group) is reacted with a base R 2-H group. COPYRIGHT: (C)1991,JPO | ||||||
| 127 | Inhibitors of cyclin-dependent kinase 7 (CDK7) | US15301815 | 2015-04-03 | US10106526B2 | 2018-10-23 | Kevin Sprott; Jason J. Marineau; Darby Schmidt; Michael Bradley; Stephane Ciblat; M. Arshad Siddiqui; Anzhelika Kabro; Melissa Leblanc; Serge Leger; Stephanie Roy; Dana K. Winter; Tom Miller; Amy Ripka; Dansu Li |
| The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. | ||||||
| 128 | INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7) | US15799661 | 2017-10-31 | US20180208578A1 | 2018-07-26 | Stephane Ciblat; Anzhelika Kabro; Melissa Leblanc; Serge Leger; Jason J. Marineau; Tom Miller; Stephanie Roy; Darby Schmidt; M. Arshad Siddiqui; Kevin Sprott; Dana K. Winter; Amy Ripka; Dansu Li; Michael Bradley |
| The present invention provides novel compounds of Formula (I) and Formula (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase 7 (CDK7), and therefore, induce cellular apoptosis and/or inhibit transcription in the subject. | ||||||
| 129 | 4-methylsulfonyl-substituted piperidine urea compounds | US15003662 | 2016-01-21 | US09925177B2 | 2018-03-27 | Johan Oslob; Danielle Aubele; Jae Kim; Robert McDowell; Yonghong Song; Arvinder Sran; Min Zhong |
| The present invention provides novel 4-methylsulphone-substituted piperidine urea compounds that are useful for the treatment of dilated cardiomyopathy (DCM) and conditions associated with left and/or right ventricular systolic dysfunction or systolic reserve. The synthesis and characterization of the compounds is described, as well as methods for treating DCM and other forms of heart disease. | ||||||
| 130 | Compounds for affinity chromatography and for extending the half-life of a therapeutic agent | US15026725 | 2014-10-01 | US09809558B2 | 2017-11-07 | Peter Kumpalume; Oliver Schon; Christine Patricia Donahue; Ghotas Evindar; David I. Israel; David Paolella; Letian Kuai; Ninad V. Prabhu |
| Compounds useful for affinity chromatography as presented, more particularly for use in affinity chromatography to purify serum albumin, especially human serum albumin (HSA) and fusion proteins thereof. Methods for extending the half-life of therapeutic agents are also presented, particularly therapeutic peptide agents and small molecules, such as by conjugation of compounds described herein to the therapeutic peptide or small molecule, which upon administration, binds to HSA, thereby providing a prolonged release of the therapeutic agent. | ||||||
| 131 | HETEROCYCLIC COMPOUNDS AND USES THEREOF | US15333803 | 2016-10-25 | US20170137407A1 | 2017-05-18 | Alfredo C. Castro; Catherine A. Evans; Somarajannair Janardanannair; Andre Lescarbeau; Tao Liu; Daniel A. Snyder; Martin R. Tremblay; Pingda Ren; Yi Liu; Liansheng Li; Katrina Chan |
| Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein. | ||||||
| 132 | 6-ACYL-1,2,4-TRIAZINE-3,5-DIONE DERIVATIVE AND HERBICIDES | US15393850 | 2016-12-29 | US20170129861A1 | 2017-05-11 | Atsushi Shibayama; Ryu Kajiki; Masami Kobayashi; Takashi Mitsunari; Atsushi Nagamatsu |
| Disclosed are triazine derivative compounds exhibiting sufficient herbicidal activity at low application dosage when they are applied to soils and foliage, and an agrochemical composition using the same, in particular herbicides. | ||||||
| 133 | Method for preparing conjugated compound having phenoxathiin and electron donating group of conjugated aromatic unit, and OLED device having the conjugated compound | US14763827 | 2015-05-22 | US09634260B2 | 2017-04-25 | Xianjie Li; Yuanchun Wu; Shijian Su; Ming Liu; Kunkun Liu |
| The disclosure provides a conjugated compound having phenoxathiinl, method for preparing the same and OLED. The conjugated compound has one of the following formulas: Different kinds of electron-rich conjugated aromatic units are reacted with intermediate having phenoxathiinl by Suzuki coupling, Buchwald-Hartwig coupling, or Cu-catalyzed amination of halogenated aromatic hydrocarbons for forming the conjugated compound having phenoxathiin. The prepared novel compound is fluorescent, so that it can be used as the material of light emitting layer of OLED devices. | ||||||
| 134 | Morpholine derivative or salt thereof | US15052252 | 2016-02-24 | US09586951B2 | 2017-03-07 | Yohei Kubo; Makoto Ando; Hidehiko Tanaka; Shuhei Osaka; Takuya Matsumoto; Hiyoku Nakata; Daisuke Terada; Tatsuya Nitabaru |
| There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like). | ||||||
| 135 | Substituted nicotinamide derivatives as kinase inhibitors | US15069344 | 2016-03-14 | US09567324B2 | 2017-02-14 | Sougato Boral; Shimiao Wang; Thomas C. Malone; Julie Wurster; Jie Shen; Michael Robinson |
| The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | ||||||
| 136 | SUBSTITUTED NICOTINAMIDE DERIVATIVES AS KINASE INHIBITORS | US15069344 | 2016-03-14 | US20160194311A1 | 2016-07-07 | Sougato Boral; Shimiao Wang; Thomas Malone; Julie Wurster; Jie Shen; Michael Robinson |
| The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. | ||||||
| 137 | NOVEL MORPHOLINE DERIVATIVE OR SALT THEREOF | US15052252 | 2016-02-24 | US20160168139A1 | 2016-06-16 | Yohei KUBO; Makoto ANDO; Hidehiko TANAKA; Shuhei OSAKA; Takuya MATSUMOTO; Hiyoku NAKATA; Daisuke TERADA; Tatsuya NITABARU |
| There is provided a morpholine derivative represented by General Formula [1A] or a salt thereof. (In the formula, a ring A represents a ring represented by General Formula [I]; * represents a bonding position; Z2 represents CH or the like; Z1 represents CR6 or the like; R6 represents a hydrogen atom or the like; X1 represents CHR7 or the like; R7 represents a hydrogen atom or the like; X2 represents CH2 or the like; R1 and R2 are the same as or different from each other, and each of R1 and R2 represents a hydrogen atom or the like; R3, R4, and R5 are the same as or different from each other, and each of R3, R4, and R5 represents a hydrogen atom, NRaRb, or the like; and each of Ra and Rb represents a hydrogen atom, a C1-8 alkyl group which may have a substituent, or the like.) | ||||||
| 138 | Novel pesticidal pyrazole compounds | US14931146 | 2015-11-03 | US20160050927A1 | 2016-02-25 | Christian DEFIEBER; Sebastian SOERGEL; Daniel SAELINGER; Ronan LE VEZOUET; Karsten KOERBER; Steffen GROSS; Deborah L. CULBERTSON; Koshi GUNJIMA |
| The present invention relates to novel pyrazoles of formula I wherein the variables are as defined in the description, a method for controlling invertebrate pests, a method for protecting plant propagation material and/or the plants which grow therefrom, to plant propagation material, comprising at least one compound according to the present invention, and to an agricultural composition. | ||||||
| 139 | Substituted isoquinolinones and methods of treatment thereof | US14099831 | 2013-12-06 | US09115141B2 | 2015-08-25 | Alfredo C. Castro; Catherine A. Evans; Somarajannair Janardanannair; Andre Lescarbeau; Tao Liu; Daniel A. Snyder; Martin R. Tremblay; Pingda Ren; Yi Liu; Liansheng Li; Katrina Chan |
| Substituted isoquinolinone compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including PI3 kinase activity, are described herein. | ||||||
| 140 | 6-ACYL-1,2,4-TRIAZINE-3,5-DIONE DERIVATIVE AND HERBICIDES | US14603029 | 2015-01-22 | US20150203457A1 | 2015-07-23 | Atsushi Shibayama; Ryu Kajjiki; Masami Kobayashi; Takashi Mitsunari; Atsushi Nagamatsu |
| Disclosed are triazine derivative compounds exhibiting sufficient herbicidal activity at low application dosage when they are applied to soils and foliage, and an agrochemical composition using the same, in particular herbicides. | ||||||
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