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xingchen7_金蟲 (小有名氣)
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浮米每周專利快訊：2014年3月（一） 已有4人參與
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1. WO 2014023258 標(biāo)題: Pyrazole carboxamide compounds, compositions and methods of use 申請(qǐng)人: 羅氏；基因泰克 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 682063；2013 US 764930；2013 US 764434 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu): 適應(yīng)癥: 炎癥 專利摘要: Provided herein are compounds of formula (AA): N N H HN O N N R R 6 A (R a ) p, (AA) stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, R a, p, R and R 6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases. 備注: ITK (EMT) 激酶抑制劑可以用于治療炎癥。一個(gè)示例性化合物對(duì)ITK的活性為Ki小于0.1 nM. 2. WO 2014025854 標(biāo)題: Piperidine amide derivatives as HIV attachment inhibitors 申請(qǐng)人: 百時(shí)美施貴寶 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 681306 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):201403060102 適應(yīng)癥: HIV感染 專利摘要: Compounds of Formula I, including pharmaceutically acceptable salts thereof: formule (I): wherein A is selected from the group consisting of:formule (II) and wherein Z is selected from the group consisting of: formule (III):,, and. are useful as HIV attachment inhibitors. 備注: HIV 粘附抑制劑可以用于治療HIV感染。一個(gè)示例性的化合物在MT-2細(xì)胞中對(duì)HIV-1的活性為EC50=0.20 nM。 3. WO 2014023815 標(biāo)題: New antibacterial compounds 申請(qǐng)人: 楊森 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 180103 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):201403060103 適應(yīng)癥: 細(xì)菌感染 專利摘要: The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds. 備注: 烯�；� – （�；d體蛋白）還原酶Fabl抑制劑可以用于治療細(xì)菌感染。一個(gè)示例性化合物可以抑制金黃色葡萄球菌ATCC 29213 Fabl，其IC50達(dá)到0.407356 mcg/ml。 4. WO 2014024119 標(biāo)題: Heterocyclic amides as ITK inhibitors 申請(qǐng)人: 格倫馬克 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 IN 2888；2012 IN 2257；2013 IN 762；2012 US 717224；2012 US 696439 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):201403060104 適應(yīng)癥: 哮喘；慢性阻塞性肺��；特異性皮炎；類風(fēng)濕性關(guān)節(jié)炎；過敏性鼻炎 專利摘要: The present invention is directed to heterocyclic amide compounds of formula (I) as Tec kinase inhibitors, in particular ITK (interleukin-2 inducible tyrosine kinase) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by ITK. 備注: ITK (EMT)抑制劑可以用于治療哮喘、慢性阻塞性肺疾病、皮炎、類風(fēng)濕性關(guān)節(jié)炎、過敏性鼻炎、多發(fā)性硬化癥、疼痛等疾病。本專利中的提供的部分示例化合物IC50小于50 nM 。 5. WO 2014023367 標(biāo)題: Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan nuclear receptor RORgamma 申請(qǐng)人: Phenex Pharmaceuticals AG 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 681296；2012 EP 5789 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):201403060105 適應(yīng)癥: 肌萎縮側(cè)索硬化癥；哮喘；I型糖尿病；腸炎；多發(fā)性硬化癥；銀屑��；類風(fēng)濕性關(guān)節(jié)炎；脊柱炎 專利摘要: The invention provides modulators for the orphan nuclear receptor RORy and methods for treating RORy mediated diseases by administering these novel RORy modulators to a human or a mammal in need thereof. Specifically, the present invention provides carboxamide containing cyclic compounds of Formula (1) to Formula (5) and the enantiomers, diastereomers, tautomers, /V-oxides, solvates and pharmaceutically acceptable salts thereof. 備注: ROR gamma 受體調(diào)控劑可以用于治療炎癥、自身免疫，如肌萎縮性脊髓惻索硬化癥、多發(fā)性硬化癥、牛皮癬、類風(fēng)濕性關(guān)節(jié)炎、過敏性濕疹等。一個(gè)示例性的化合物在BL-21細(xì)胞中顯示抑制RORgamma的活性為pIC50為6.3nM。 6. WO 2014023385 標(biāo)題: Pyridopyrimidine derivatives as protein kinase inhibitors 申請(qǐng)人: 默克 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 5716 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):201403060106 適應(yīng)癥: 哮喘；腫瘤；多發(fā)性硬化癥；類風(fēng)濕性關(guān)節(jié)炎；紅斑狼瘡 專利摘要: Compounds of the formula (I) in which R, R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and / or systemic lupus 備注: Syk激酶抑制劑可以用于多種疾病的治療，如腫瘤、類風(fēng)濕性關(guān)節(jié)炎、紅斑狼瘡、哮喘、多發(fā)性硬化癥、糖尿病、唐氏綜合癥等。一個(gè)示例性化合物對(duì)Syk的抑制活性為IC500.1 mcM 。 7. WO 2014023673；US 2014044674 標(biāo)題: Interleukin-10 fusion proteins and uses thereof 申請(qǐng)人: 羅氏 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 179709 相關(guān)候選藥物類型: 融合蛋白 適應(yīng)癥: 炎癥；腸炎；類風(fēng)濕性關(guān)節(jié)炎 專利摘要: The present invention generally relates to fusion proteins of antibodies and interleukin-10 (IL-10). In addition, the present invention relates to polynucleotides encoding such fusion proteins, and vectors and host cells comprising such polynucleotides. The invention further relates to methods for producing the fusion proteins of the invention, and to methods of using them in the treatment of disease. 備注: 由IgG類抗體和IL-10分子組成的融合蛋白可以用于炎癥的治療或預(yù)防，特別是炎癥性腸疾病和類風(fēng)濕關(guān)節(jié)炎的治療。一個(gè)示例性的融合蛋白可以靶向人源FAP。該融合蛋白可以抑制LPS誘導(dǎo)的前炎性細(xì)胞活素（IL-6, IL-1beta和TNF-alpha）的產(chǎn)物，其EC50分別為0.054, 0.049和0.017 nM。 8. WO 2014023674 標(biāo)題: Piperazino[1,2-a]indol-1-ones and [1,4]diazepino[1,2-a]indol-1-one 申請(qǐng)人: 羅氏 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 179381 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):201403060108 適應(yīng)癥: 焦慮；阿爾茲海默；抑郁；中風(fēng) 專利摘要: The present invention relates to compounds of general formula (I), wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkoxy substituted by halogen or cyano; R2 is hydrogen, lower alkyl or lower alkyl substituted by halogen; R3 is phenyl, benzo[1,3]dioxolyl, 2,3-dihydro-benzofuran-5-yl or a 5- and 6-membered heteroaryl, wherein phenyl and the 5- and 6-membered heteroaryl groups may be substituted by one or more substituents, selected from cyano, nitro, amino and lower di-alkylamino, lower alkyl sulfonyl, lower alkoxy, lower alkoxy substituted by halogen, halogen, lower alkyl, lower alkyl substituted by halogen or lower alkyl substituted by hydroxyl; X is -CH(lower alkyl)-, -CH2-, -CH2CH2- or �CH(lower alkyl)CH2-; R is hydrogen or lower alkyl; n is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof. The compounds may be used for the treatment of schizophrenia, obsessive-compulsive personality disorder, major depression, bipolar disorders, anxiety disorders, normal aging, epilepsy, retinal degeneration, traumatic brain injury, spinal cord injury, post-traumatic stress disorder, panic disorder, Parkinson’s disease, dementia, Alzheimer’s disease, mild cognitive impairment, chemotherapy-induced cognitive dysfunction, Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington’s disease, stroke, radiation therapy, chronic stress, abuse of neuro-active drugs, such as alcohol, opiates, methamphetamine, phencyclidine and cocaine. 備注: 神經(jīng)系統(tǒng)調(diào)節(jié)類化合物可以用于治療焦慮、阿爾茲海默、抑郁和中風(fēng)等疾病。一個(gè)示例性的化合物的EC150=0.002 mcM。 9. WO 2014026054 標(biāo)題: CD20 scFv-ELPs methods and therapeutics 申請(qǐng)人: University of Southern California (USC) 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 682029 相關(guān)候選藥物類型: 融合蛋白 適應(yīng)癥: 自身免疫；腫瘤 專利摘要: Disclosed herein are recombinant polypeptides comprising an elastin-like peptide (ELP) and a scFv, or a biological equivalent of the scFv. Also disclosed are compositions containing scFv-ELP polypeptides and methods of use. 備注: 包含彈性蛋白樣肽（ELP）融合單鏈抗體（scFv）的重組多肽可以用于治療癌癥和自身免疫類疾病。一個(gè)由利妥昔單抗衍生的抗CD20的scFv單鏈抗體融合ELP(A-192)的融合蛋白scFv-ELPs可以延緩腫瘤生長并延長生存期。 10. WO 2014023814 標(biāo)題: New antibacterial compounds 申請(qǐng)人: 楊森 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 180100 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601010 適應(yīng)癥: 細(xì)菌感染 專利摘要: The present invention is related to novel compounds of formula (I) that may inhibit the activity of the FabI enzyme, and which are useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds. 備注: 烯�；� – （�；d體蛋白）還原酶Fabl抑制劑可以用于治療細(xì)菌感染。一個(gè)示例性化合物可以抑制金黃色葡萄球菌ATCC 29213 Fabl，其IC50達(dá)到0.27 mcg/ml。此外其也對(duì)S. aureus ATCC 29213 and S. aureus ATCC 29213具有活性，分別為IC90 = 0.24 和0.21 mcg/ml。 11. WO 2014025708 標(biāo)題: Compounds that are S1P modulating agents and/or ATX modulating agents 申請(qǐng)人: Biogen Idec Inc. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 679984 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601011 適應(yīng)癥: 多發(fā)性硬化癥；疼痛；類風(fēng)濕性關(guān)節(jié)炎 專利摘要: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX). 備注: ENPP2抑制劑或SIP調(diào)節(jié)劑可用于類風(fēng)濕性關(guān)節(jié)炎關(guān)節(jié)炎、多發(fā)性硬化癥和疼痛、腫瘤、免疫等疾病的治療。 示例性化合物對(duì)ENPP2的IC50小于0.5 mcM。 12. WO 2014025709 標(biāo)題: Compounds that are S1P modulating agents and/or ATX modulating agents 申請(qǐng)人: Biogen Idec Inc. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 679992 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601012 適應(yīng)癥: 多發(fā)性硬化癥；疼痛；類風(fēng)濕性關(guān)節(jié)炎 專利摘要: Compounds of formula (I) can modulate the activity of one or more SIP receptors and/or the activity of autotaxin (ATX). 備注: ENPP2抑制劑或SIP調(diào)節(jié)劑可用于類風(fēng)濕性關(guān)節(jié)炎關(guān)節(jié)炎、多發(fā)性硬化癥和疼痛、腫瘤、免疫等疾病的治療。 示例性化合物對(duì)ENPP2的IC50小于0.5 mcM。 13. WO 2014025850 標(biāo)題: Tricyclic amidine derivatives as HIV attachment inhibitors 申請(qǐng)人: 百時(shí)美施貴寶 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 681336 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601013 適應(yīng)癥: HIV感染 專利摘要: Compounds of Formula I, including pharmaceutically acceptable salts thereof: (F) wherein A is selected from the group consisting of: (F) and;(F) and wherein Z is: (F) are useful as HIV attachment inhibitors. 備注: HIV 粘附抑制劑可以用于治療HIV感染。一個(gè)示例性的化合物在MT-2細(xì)胞中對(duì)HIV-1的活性為EC50=1.83nM。 14. WO 2014025852 標(biāo)題: Tricyclic alkene derivatives as HIV attachment inhibitors 申請(qǐng)人: 百時(shí)美施貴寶 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 681329 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601014 適應(yīng)癥: HIV感染 專利摘要: Compounds of Formula (I), including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: and wherein Z is: are useful as HIV attachment inhibitors. 備注: HIV 粘附抑制劑可以用于治療HIV感染。一個(gè)示例性的化合物在MT-2細(xì)胞中對(duì)HIV-1的活性為EC50=0.28 nM。 15. WO 2014022936 標(biāo)題: Chlamydia antigen compositions and uses thereof 申請(qǐng)人: University of British Columbia 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 680836 相關(guān)候選藥物類型: 融合蛋白 適應(yīng)癥: 衣原體感染 專利摘要: The present invention provides in part fusion proteins derived from Chlamydia spp. The present invention also provides in part methods for treating or preventing Chlamydia infection using the fusion proteins. 備注: 免疫組合物類的融合蛋白可以作為疫苗，用于衣原體感染的預(yù)防和治療。本專利中，融合蛋白 Chlamydia抗體展示了良好了抗衣原體感染活性。 16. WO 2014022767 標(biāo)題: Dihydropyridone P1 as factor XIa inhibitors 申請(qǐng)人: 百時(shí)美施貴寶 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2013 US 787081；2012 US 679197 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601016 適應(yīng)癥: 血栓 專利摘要: The present invention provides compounds of Formula (X)  Formula(X), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.備注: 凝血因子XIa和/或激肽釋放酶B（血漿激肽釋放酶; KLKB1）可以用于治療血栓。血栓栓塞性病癥如不穩(wěn)定型心絞痛，急性冠狀動(dòng)脈綜合征，心房纖維性顫動(dòng)，心肌梗塞，短暫性缺血發(fā)作，中風(fēng)，動(dòng)脈粥樣硬化，外周阻塞的治療有用的抑制劑動(dòng)脈疾病，靜脈血栓形成，腦動(dòng)脈血栓形成，腦，腎和肺栓塞等。本專利中的的示例化合物對(duì)凝血因子XIa和KLKB1的 Ki值分別為 0.05和 0.56 nM。 17. WO 2014022766；US 2014038969 標(biāo)題: Dihydropyridone P1 as factor XIa inhibitors 申請(qǐng)人: 百時(shí)美施貴寶 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2013 US 957609；2012 US 679197；2013 US 786992 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601017 適應(yīng)癥: 血栓 專利摘要: The present invention provides compounds of Formula (VIII): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. 備注: 凝血因子XIa和/或激肽釋放酶B（血漿激肽釋放酶; KLKB1）可以用于治療血栓。血栓栓塞性病癥如不穩(wěn)定型心絞痛，急性冠狀動(dòng)脈綜合征，心房纖維性顫動(dòng)，心肌梗塞，短暫性缺血發(fā)作，中風(fēng)，動(dòng)脈粥樣硬化，外周阻塞的治療有用的抑制劑動(dòng)脈疾病，靜脈血栓形成，腦動(dòng)脈血栓形成，腦，腎和肺栓塞等。本專利中的的示例化合物對(duì)凝血因子XIa和KLKB1的 Ki值分別為 0.25和 0.7 nM。 18. WO 2014022752 標(biāo)題: Macrocycles as Pim inhibitors 申請(qǐng)人: 安進(jìn) 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 679521 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601018 適應(yīng)癥: 腫瘤 專利摘要: The invention relates to compounds of formula (1), and salts thereof. In some embodiments, the invention relates to inhibitors or modulators of Pim-1 and/or Pim-2, and/or Pim-3 protein kinase activity or enzyme function. In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein, and their use in the prevention and treatment of Pim kinase related conditions and diseases, preferably cancer. 備注: Pim激酶可以用于治療腫瘤。Pim分為Pim1、Pim2、Pim3等三種亞型。 本專利的化合物對(duì) Pim-1, Pim-2, Pim-1-Mn and Pim-2-Mn的活性分別為IC50 = 0.000209、0.000286、0.0000498和0.0000634 mcM。 19. WO 2014022744 標(biāo)題: Indole-substituted pyrrolopyrimidinyl inhibitors of Uba6 申請(qǐng)人: Millennium Pharmaceuticals, Inc. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 679109 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601019 適應(yīng)癥: 腫瘤 專利摘要: Disclosed are chemical entities that inhibit Uba6, each of which is a compound of Formula /: Formula (I) or a pharmaceutically acceptable salt thereof, wherein R*1 is -H or -CH3; and Y is Formula (II) or Formula (III), wherein R2 is -H, -CH3 or C1-4 alkyloxycarbonyl; and RS7.1, RS7.2 and RS8.1 are defined herein; pharmaceutical compositions comprising the chemical entities; and methods of using the chemical entities. These chemical entities are useful for treating disorders, particularly cell proliferation disorders, including cancers. 備注: UBA6酶抑制劑可以用與治療腫瘤疾病。一個(gè)示例性化合物對(duì)人源重組his-UBA6酶的IC50小于50nM。 20. EP 2692357；WO 2014020062 標(biāo)題: Novel anti-Plasmodium parasite antibodies 申請(qǐng)人: Fraunhofer-Gesellschaft zur Foerderung der angewandten Forschung eV 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 679380；2012 EP 179315 相關(guān)候選藥物類型: 抗體 適應(yīng)癥: 診斷；瘧疾 專利摘要: The technology provided herein relates to novel human antibodies against Plasmodium parasites, in particular against the malaria parasite Plasmodium falciparum. The present disclosure pertains to antibodies against merozoite surface protein 10 (MSP10). These antibodies have high affinity e.g. to Plasmodium falciparum schizonts and merozoites, inhibit the reinvasion of merozoites into erythrocytes and thereby neutralize parasitic multiplication. 備注: 人抗體或其抗原可以特異性的結(jié)合MSP10，且可以用于瘧疾的診斷和治療。本專利中列舉的人單克隆IgG1 kappa抗體展示了對(duì)EGF 域1的特異性親和力。 21. WO 2014022343 標(biāo)題: 7-Hydroxy-indolinyl antagonists of P2Y1 receptor 申請(qǐng)人: 百時(shí)美施貴寶 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 678151 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601021 適應(yīng)癥: 血栓 專利摘要: The present invention provides compounds of Formula (I): Formula (I) as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used medicaments. 備注: P2Y1受體拮抗劑可以用于治療血栓。本專利中列舉的化合物在HEK-293細(xì)胞中，Ki=11.3nM。 22. WO 2014022253 標(biāo)題: Amino-heteroaryl 7-hydroxy-spiropiperidine indolinyl antagonists of P2Y1 receptor 申請(qǐng)人: 百時(shí)美施貴寶 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 678190 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601022 適應(yīng)癥: 血栓 專利摘要: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used as medicaments. 備注: P2Y1受體拮抗劑可以用于治療血栓。本專利中列舉的化合物在HEK-293細(xì)胞中，Ki=16 nM。 23. WO 2014021281 標(biāo)題: Partially saturated nitrogen-containing heterocyclic compound 申請(qǐng)人: Taisho Pharmaceutical Co., Ltd. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 JP 168828 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601023 適應(yīng)癥: 貧血 專利摘要: Provided is a compound which is represented by general formula (I’) and has an excellent PHD2-inhibiting activity or a pharmaceutically acceptable salt thereof. (In the general formula (I’), W, Y, R2, R3, R4 and Y4 are as defined in the description.) 備注: 缺氧誘導(dǎo)因子（HIF）脯氨酰羥化酶2（PHD2）抑制劑對(duì)貧血癥的治療有效。本專利中的化合物在293FT細(xì)胞中可以抑制PHD2，其IC50=14 nM。 24. WO 2014020350 標(biāo)題: PAR2 receptor antagonists 申請(qǐng)人: Proximagen Ltd. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 GB 13700；2013 GB 52069 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601024 適應(yīng)癥: 炎癥；腫瘤；特異性皮炎；腸炎；腸易綜合征；疼痛；銀屑病 專利摘要: Compounds of formula (I) or pharmaceutically acceptable salts, solvates or hydrates thereof wherein P, Q, X, Y, R1, R2, R3, R10, R11, and R12 are as defined in the claims, and the use those compounds in medicine. 備注: PAR2拮抗劑可以用于治療炎癥、腫瘤、疼痛、銀屑病等疾病。本專利中的示例化合物對(duì)PAR2的IC500.1 mcM。 25. WO 2014022728；US 2014038952 標(biāo)題: Substituted 5-(quinazolin-2-yl)pyrimidin-2-amine derivatives useful as PI3K/mTOR inhibitors for the treatment of cancer 申請(qǐng)人: Endo Pharmaceuticals Inc. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2013 US 957470；2012 US 678694 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601025 適應(yīng)癥: 腫瘤；炎癥 專利摘要: The present application provides novel substituted quinazoline and pyrido-pyrimidine compounds of formula (I) and pharmaceutically acceptable salts, prodrugs, and solvates thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating PI3K and/or mTOR activity by administering a therapeutically effective amount of one or more of the compounds to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the PI3K/AKT/mTOR pathway. Advantageously, these compounds perform as dual PI3K/mTOR inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer. 備注: PI3Kalpha/mTOR(FRAP1)抑制劑可以用于治療炎癥和腫瘤。 本專利中的化合物在H1047R、E545K 和mTOR的IC50均小于50 nM，對(duì) PI3K beta and gamma的IC50均小于500 nM，對(duì)PI3Kdelta的IC50 1mcM。 26. US 2014045856；US 2014045857；WO 2014019979 標(biāo)題: 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes 申請(qǐng)人: 勃林格殷格翰 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 178713 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601026 適應(yīng)癥: 阿爾茲海默；記憶缺陷 專利摘要: The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention. 備注: PDE2A和/或PDE10A抑制劑可以用于治療阿爾茲海默和記憶缺陷等精神類疾病。本專利中的一個(gè)示例性化合物分別在對(duì)PDE2A的IC50 = 0.071mcM，對(duì)PD10A的IC50 = 3.01mcM。 27. WO 2014019908 標(biāo)題: Substituted pyrroles active as kinases inhibitors 申請(qǐng)人: Nerviano Medical Sciences Srl 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 178946 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601027 適應(yīng)癥: 動(dòng)脈粥樣硬化；腫瘤；免疫；HIV感染；神經(jīng)退行疾�。磺傲邢僭錾�；銀屑�。恢酗L(fēng) 專利摘要: The present invention relates to substituted pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them. 備注: Janus 激酶抑制劑可以用于治療腫瘤、動(dòng)脈粥樣硬化、免疫等多種疾病。本專利中提供的示例化合物對(duì)Jak1, Jak2 和 Tyk2 的 IC50均為0.001 mcM。 28. WO 2014019023 標(biāo)題: alpha7 Nicotinic acetylcholine receptor modulators and uses thereof-I 申請(qǐng)人: Bionomics Ltd. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 AU 903296；2013 AU 900167 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601028 適應(yīng)癥: 認(rèn)知障礙；炎癥；神經(jīng)退行性疾��；神經(jīng)疼痛 專利摘要: The present invention relates to chemical compounds of formula (I), with the substituents as described in the specification, useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (a7 nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of a7 nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also neuropathic pain and inflammatory diseases. 備注: alpha7 煙堿乙酰膽堿受體（nAChR的）的調(diào)節(jié)劑可作為炎癥、認(rèn)知障礙、神經(jīng)疼痛等疾病的治療用途。本專利提供的示例化合物對(duì)于 alpha7受體具有很好的活性。 29. WO 2014018887 標(biāo)題: ATX modulating agents 申請(qǐng)人: Biogen Idec Inc. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 676698 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601029 適應(yīng)癥: 多發(fā)性硬化癥；慢性疼痛；類風(fēng)濕性關(guān)節(jié)炎 專利摘要: Compounds of formula (I) can modulate the activity of autotaxin (ATX). 備注: ENPP2抑制劑或SIP調(diào)節(jié)劑可用于類風(fēng)濕性關(guān)節(jié)炎關(guān)節(jié)炎、多發(fā)性硬化癥和疼痛、腫瘤、免疫等疾病的治療。 示例性化合物對(duì)ENPP2的IC50小于100 nM。 30. WO 2014018881 標(biāo)題: ATX modulating agents 申請(qǐng)人: Biogen Idec Inc. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 676705 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601030 適應(yīng)癥: 多發(fā)性硬化癥；慢性疼痛；類風(fēng)濕性關(guān)節(jié)炎 專利摘要: Disclosed are bicyclic aryl compounds of formula (I), that can modulate the activity of the autotaxin (ATX) enzyme. This invention further relates to compounds that are ATX inhibitors, and methods of making and using such compounds in the treatment of demyelination due to injury or disease, as well as for treating proliferative disorders such as cancer. 備注: ENPP2抑制劑或SIP調(diào)節(jié)劑可用于類風(fēng)濕性關(guān)節(jié)炎關(guān)節(jié)炎、多發(fā)性硬化癥和疼痛、腫瘤、免疫等疾病的治療。 示例性化合物對(duì)ENPP2的IC50小于100 nM。 31. WO 2014018919 標(biāo)題: Seriniquinones, melanoma-specific anticancer agents 申請(qǐng)人: University of California, Oakland 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 676427 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601031 適應(yīng)癥: 腫瘤 專利摘要: Accordingly, there are provided, inter alia, derivatives of seriniquinone and methods useful for the treatment of cancer, and in particular treatment of melanoma and prostate cancer. 備注: Seriniquinones衍生物可以作為dermcidin抑制劑通過誘導(dǎo)凋亡的機(jī)制用于腫瘤，尤其是黑色素瘤和前列腺癌的治療。本專利中的示例化合物對(duì)非小細(xì)胞肺癌細(xì)胞、腎癌、卵巢癌、前列腺癌、乳腺癌等細(xì)胞的抑制活性達(dá)到10 mcM。 32. WO 2014016300 標(biāo)題: Glucagon analogues 申請(qǐng)人: Zealand Pharma A/S 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 674706；2013 DK 360；2013 US 785611 相關(guān)候選藥物類型: 多肽 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601032 適應(yīng)癥: 低血糖 專利摘要: The present invention relates to glucagon analogues and their medical use, for example in the treatment of hypoglycaemia. In particular, the present invention relates to stable glucagon analogues suitable for use in a liquid formulation. 備注: GCGR受體激動(dòng)劑可以用于低血糖、肥胖、高血壓、動(dòng)脈粥樣硬化等疾病的治療。本專利中的示例化合物對(duì)人源GCGR的EC50 = 0.15 nM。 33. EP 2689786；WO 2014016312 標(biāo)題: HPV/CyaA-based chimeric proteins and their uses in the induction of immune responses against HPV infection and HPV-induced disorders 申請(qǐng)人: Genticel SA 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 EP 305898 相關(guān)候選藥物類型: 疫苗 相關(guān)候選藥物化學(xué)結(jié)構(gòu): 適應(yīng)癥: 乳頭狀瘤病毒感染 專利摘要: The invention relates to a chimeric protein comprising or consisting of, from N-terminal to C-terminal, (a) a N-terminal part of a Bordetella CyaA protein (b) a heterologous polypeptide comprising antigens originating from different HPVs, and (c) a C-terminal part of a Bordetella CyaA protein. The invention also relates to a polynucleotide encoding this chimeric protein. A composition comprising at least one chimeric protein(s) of the invention and the prophylactic and/or therapeutic uses of said composition are also part of the invention. 備注: 有E7蛋白衍生物組成的多肽可以作為疫苗，用于HPV感染的治療。本專利提供了對(duì)HPV感染有效的疫苗。 34. FR 2993562;WO 2014016507 標(biāo)題: Novel selective compounds inhibiting CYP26A1 useful in cosmetic and pharmaceutical compositions 申請(qǐng)人: Galderma Research & Development, SNC 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 FR 57128 相關(guān)候選藥物類型: 小分子藥物 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601034 適應(yīng)癥: 皮膚病 專利摘要: The present invention relates to novel compounds or to any of the salts thereof having the general formula (I), to the pharmaceutical and cosmetic compositions containing said compounds as well as to the use of said compounds and compositions for the treatment of diseases. 備注: 細(xì)胞色素 P450 CYP26A1抑制劑可以用于治療皮膚類疾病。本專利中的一個(gè)示例化合物對(duì) CYP26A1的AC50 = 0.19 mcM；對(duì)CYP26B1的AC50 = 50.33 mcM。 35. WO 2014016787 標(biāo)題: Peptide-based compounds and uses thereof to treat beta-amyloid accumulation 申請(qǐng)人: Pharma Bio, LLC. 優(yōu)先權(quán)日期及相關(guān)專利公開號(hào): 2012 US 675205 相關(guān)候選藥物類型: 多肽 相關(guān)候選藥物化學(xué)結(jié)構(gòu):2014030601035 適應(yīng)癥: 阿爾茲海默 專利摘要: The present application relates to novel peptide-based compounds, optionally comprising an immunoactive built-in adjuvant, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with ß- amyloid accumulation. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: [Ra-NP]m-Lp (I). 備注: 可以抑制β-淀粉樣蛋白的多肽可以用作阿爾茲海默、唐氏綜合癥等疾病的治療。本專利提供了經(jīng)修飾的用于抑制β-淀粉樣蛋白的多肽結(jié)構(gòu)。 |
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2樓2014-03-09 22:11:01
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