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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 標題: Pyrazole carboxamide compounds, compositions and methods of use 申請人: 羅氏；基因泰克 優(yōu)先權日期及相關專利公開號: 2012 US 682063；2013 US 764930；2013 US 764434 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構: 適應癥: 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。一個示例性化合物對ITK的活性為Ki小于0.1 nM. 2. WO 2014025854 標題: Piperidine amide derivatives as HIV attachment inhibitors 申請人: 百時美施貴寶 優(yōu)先權日期及相關專利公開號: 2012 US 681306 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:201403060102 適應癥: 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。一個示例性的化合物在MT-2細胞中對HIV-1的活性為EC50=0.20 nM。 3. WO 2014023815 標題: New antibacterial compounds 申請人: 楊森 優(yōu)先權日期及相關專利公開號: 2012 EP 180103 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:201403060103 適應癥: 細菌感染 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菌感染。一個示例性化合物可以抑制金黃色葡萄球菌ATCC 29213 Fabl，其IC50達到0.407356 mcg/ml。 4. WO 2014024119 標題: Heterocyclic amides as ITK inhibitors 申請人: 格倫馬克 優(yōu)先權日期及相關專利公開號: 2012 IN 2888；2012 IN 2257；2013 IN 762；2012 US 717224；2012 US 696439 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:201403060104 適應癥: 哮喘；慢性阻塞性肺病；特異性皮炎；類風濕性關節(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、類風濕性關節(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 標題: Carboxamide or sulfonamide substituted nitrogen-containing 5-membered heterocycles as modulators for the orphan nuclear receptor RORgamma 申請人: Phenex Pharmaceuticals AG 優(yōu)先權日期及相關專利公開號: 2012 US 681296；2012 EP 5789 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:201403060105 適應癥: 肌萎縮側索硬化癥；哮喘；I型糖尿��；腸炎；多發(fā)性硬化癥；銀屑��；類風濕性關節(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、類風濕性關節(jié)炎、過敏性濕疹等。一個示例性的化合物在BL-21細胞中顯示抑制RORgamma的活性為pIC50為6.3nM。 6. WO 2014023385 標題: Pyridopyrimidine derivatives as protein kinase inhibitors 申請人: 默克 優(yōu)先權日期及相關專利公開號: 2012 EP 5716 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:201403060106 適應癥: 哮喘；腫瘤；多發(fā)性硬化癥；類風濕性關節(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、類風濕性關節(jié)炎、紅斑狼瘡、哮喘、多發(fā)性硬化癥、糖尿病、唐氏綜合癥等。一個示例性化合物對Syk的抑制活性為IC500.1 mcM 。 7. WO 2014023673；US 2014044674 標題: Interleukin-10 fusion proteins and uses thereof 申請人: 羅氏 優(yōu)先權日期及相關專利公開號: 2012 EP 179709 相關候選藥物類型: 融合蛋白 適應癥: 炎癥；腸炎；類風濕性關節(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防，特別是炎癥性腸疾病和類風濕關節(jié)炎的治療。一個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誘導的前炎性細胞活素（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 標題: Piperazino[1,2-a]indol-1-ones and [1,4]diazepino[1,2-a]indol-1-one 申請人: 羅氏 優(yōu)先權日期及相關專利公開號: 2012 EP 179381 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:201403060108 適應癥: 焦慮；阿爾茲海默；抑郁；中風 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)調節(jié)類化合物可以用于治療焦慮、阿爾茲海默、抑郁和中風等疾病。一個示例性的化合物的EC150=0.002 mcM。 9. WO 2014026054 標題: CD20 scFv-ELPs methods and therapeutics 申請人: University of Southern California (USC) 優(yōu)先權日期及相關專利公開號: 2012 US 682029 相關候選藥物類型: 融合蛋白 適應癥: 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 標題: New antibacterial compounds 申請人: 楊森 優(yōu)先權日期及相關專利公開號: 2012 EP 180100 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601010 適應癥: 細菌感染 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菌感染。一個示例性化合物可以抑制金黃色葡萄球菌ATCC 29213 Fabl，其IC50達到0.27 mcg/ml。此外其也對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 標題: Compounds that are S1P modulating agents and/or ATX modulating agents 申請人: Biogen Idec Inc. 優(yōu)先權日期及相關專利公開號: 2012 US 679984 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601011 適應癥: 多發(fā)性硬化癥；疼痛；類風濕性關節(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調節(jié)劑可用于類風濕性關節(jié)炎關節(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ENPP2的IC50小于0.5 mcM。 12. WO 2014025709 標題: Compounds that are S1P modulating agents and/or ATX modulating agents 申請人: Biogen Idec Inc. 優(yōu)先權日期及相關專利公開號: 2012 US 679992 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601012 適應癥: 多發(fā)性硬化癥；疼痛；類風濕性關節(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調節(jié)劑可用于類風濕性關節(jié)炎關節(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ENPP2的IC50小于0.5 mcM。 13. WO 2014025850 標題: Tricyclic amidine derivatives as HIV attachment inhibitors 申請人: 百時美施貴寶 優(yōu)先權日期及相關專利公開號: 2012 US 681336 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601013 適應癥: 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。一個示例性的化合物在MT-2細胞中對HIV-1的活性為EC50=1.83nM。 14. WO 2014025852 標題: Tricyclic alkene derivatives as HIV attachment inhibitors 申請人: 百時美施貴寶 優(yōu)先權日期及相關專利公開號: 2012 US 681329 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601014 適應癥: 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。一個示例性的化合物在MT-2細胞中對HIV-1的活性為EC50=0.28 nM。 15. WO 2014022936 標題: Chlamydia antigen compositions and uses thereof 申請人: University of British Columbia 優(yōu)先權日期及相關專利公開號: 2012 US 680836 相關候選藥物類型: 融合蛋白 適應癥: 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 標題: Dihydropyridone P1 as factor XIa inhibitors 申請人: 百時美施貴寶 優(yōu)先權日期及相關專利公開號: 2013 US 787081；2012 US 679197 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601016 適應癥: 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，急性冠狀動脈綜合征，心房纖維性顫動，心肌梗塞，短暫性缺血發(fā)作，中風，動脈粥樣硬化，外周阻塞的治療有用的抑制劑動脈疾病，靜脈血栓形成，腦動脈血栓形成，腦，腎和肺栓塞等。本專利中的的示例化合物對凝血因子XIa和KLKB1的 Ki值分別為 0.05和 0.56 nM。 17. WO 2014022766；US 2014038969 標題: Dihydropyridone P1 as factor XIa inhibitors 申請人: 百時美施貴寶 優(yōu)先權日期及相關專利公開號: 2013 US 957609；2012 US 679197；2013 US 786992 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601017 適應癥: 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，急性冠狀動脈綜合征，心房纖維性顫動，心肌梗塞，短暫性缺血發(fā)作，中風，動脈粥樣硬化，外周阻塞的治療有用的抑制劑動脈疾病，靜脈血栓形成，腦動脈血栓形成，腦，腎和肺栓塞等。本專利中的的示例化合物對凝血因子XIa和KLKB1的 Ki值分別為 0.25和 0.7 nM。 18. WO 2014022752 標題: Macrocycles as Pim inhibitors 申請人: 安進 優(yōu)先權日期及相關專利公開號: 2012 US 679521 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601018 適應癥: 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 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 標題: Indole-substituted pyrrolopyrimidinyl inhibitors of Uba6 申請人: Millennium Pharmaceuticals, Inc. 優(yōu)先權日期及相關專利公開號: 2012 US 679109 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601019 適應癥: 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。一個示例性化合物對人源重組his-UBA6酶的IC50小于50nM。 20. EP 2692357；WO 2014020062 標題: Novel anti-Plasmodium parasite antibodies 申請人: Fraunhofer-Gesellschaft zur Foerderung der angewandten Forschung eV 優(yōu)先權日期及相關專利公開號: 2012 US 679380；2012 EP 179315 相關候選藥物類型: 抗體 適應癥: 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EGF 域1的特異性親和力。 21. WO 2014022343 標題: 7-Hydroxy-indolinyl antagonists of P2Y1 receptor 申請人: 百時美施貴寶 優(yōu)先權日期及相關專利公開號: 2012 US 678151 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601021 適應癥: 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細胞中，Ki=11.3nM。 22. WO 2014022253 標題: Amino-heteroaryl 7-hydroxy-spiropiperidine indolinyl antagonists of P2Y1 receptor 申請人: 百時美施貴寶 優(yōu)先權日期及相關專利公開號: 2012 US 678190 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601022 適應癥: 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細胞中，Ki=16 nM。 23. WO 2014021281 標題: Partially saturated nitrogen-containing heterocyclic compound 申請人: Taisho Pharmaceutical Co., Ltd. 優(yōu)先權日期及相關專利公開號: 2012 JP 168828 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601023 適應癥: 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: 缺氧誘導因子（HIF）脯氨酰羥化酶2（PHD2）抑制劑對貧血癥的治療有效。本專利中的化合物在293FT細胞中可以抑制PHD2，其IC50=14 nM。 24. WO 2014020350 標題: PAR2 receptor antagonists 申請人: Proximagen Ltd. 優(yōu)先權日期及相關專利公開號: 2012 GB 13700；2013 GB 52069 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601024 適應癥: 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PAR2的IC500.1 mcM。 25. WO 2014022728；US 2014038952 標題: Substituted 5-(quinazolin-2-yl)pyrimidin-2-amine derivatives useful as PI3K/mTOR inhibitors for the treatment of cancer 申請人: Endo Pharmaceuticals Inc. 優(yōu)先權日期及相關專利公開號: 2013 US 957470；2012 US 678694 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601025 適應癥: 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 PI3K beta and gamma的IC50均小于500 nM，對PI3Kdelta的IC50 1mcM。 26. US 2014045856；US 2014045857；WO 2014019979 標題: 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes 申請人: 勃林格殷格翰 優(yōu)先權日期及相關專利公開號: 2012 EP 178713 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601026 適應癥: 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。本專利中的一個示例性化合物分別在對PDE2A的IC50 = 0.071mcM，對PD10A的IC50 = 3.01mcM。 27. WO 2014019908 標題: Substituted pyrroles active as kinases inhibitors 申請人: Nerviano Medical Sciences Srl 優(yōu)先權日期及相關專利公開號: 2012 EP 178946 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601027 適應癥: 動脈粥樣硬化；腫瘤；免疫；HIV感染；神經(jīng)退行疾��；前列腺增生；銀屑�。恢酗L 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Jak1, Jak2 和 Tyk2 的 IC50均為0.001 mcM。 28. WO 2014019023 標題: alpha7 Nicotinic acetylcholine receptor modulators and uses thereof-I 申請人: Bionomics Ltd. 優(yōu)先權日期及相關專利公開號: 2012 AU 903296；2013 AU 900167 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601028 適應癥: 認知障礙；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）的調節(jié)劑可作為炎癥、認知障礙、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于 alpha7受體具有很好的活性。 29. WO 2014018887 標題: ATX modulating agents 申請人: Biogen Idec Inc. 優(yōu)先權日期及相關專利公開號: 2012 US 676698 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601029 適應癥: 多發(fā)性硬化癥；慢性疼痛；類風濕性關節(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調節(jié)劑可用于類風濕性關節(jié)炎關節(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ENPP2的IC50小于100 nM。 30. WO 2014018881 標題: ATX modulating agents 申請人: Biogen Idec Inc. 優(yōu)先權日期及相關專利公開號: 2012 US 676705 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601030 適應癥: 多發(fā)性硬化癥；慢性疼痛；類風濕性關節(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調節(jié)劑可用于類風濕性關節(jié)炎關節(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ENPP2的IC50小于100 nM。 31. WO 2014018919 標題: Seriniquinones, melanoma-specific anticancer agents 申請人: University of California, Oakland 優(yōu)先權日期及相關專利公開號: 2012 US 676427 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601031 適應癥: 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抑制劑通過誘導凋亡的機制用于腫瘤，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非小細胞肺癌細胞、腎癌、卵巢癌、前列腺癌、乳腺癌等細胞的抑制活性達到10 mcM。 32. WO 2014016300 標題: Glucagon analogues 申請人: Zealand Pharma A/S 優(yōu)先權日期及相關專利公開號: 2012 US 674706；2013 DK 360；2013 US 785611 相關候選藥物類型: 多肽 相關候選藥物化學結構:2014030601032 適應癥: 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受體激動劑可以用于低血糖、肥胖、高血壓、動脈粥樣硬化等疾病的治療。本專利中的示例化合物對人源GCGR的EC50 = 0.15 nM。 33. EP 2689786；WO 2014016312 標題: HPV/CyaA-based chimeric proteins and their uses in the induction of immune responses against HPV infection and HPV-induced disorders 申請人: Genticel SA 優(yōu)先權日期及相關專利公開號: 2012 EP 305898 相關候選藥物類型: 疫苗 相關候選藥物化學結構: 適應癥: 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HPV感染有效的疫苗。 34. FR 2993562;WO 2014016507 標題: Novel selective compounds inhibiting CYP26A1 useful in cosmetic and pharmaceutical compositions 申請人: Galderma Research & Development, SNC 優(yōu)先權日期及相關專利公開號: 2012 FR 57128 相關候選藥物類型: 小分子藥物 相關候選藥物化學結構:2014030601034 適應癥: 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。本專利中的一個示例化合物對 CYP26A1的AC50 = 0.19 mcM；對CYP26B1的AC50 = 50.33 mcM。 35. WO 2014016787 標題: Peptide-based compounds and uses thereof to treat beta-amyloid accumulation 申請人: Pharma Bio, LLC. 優(yōu)先權日期及相關專利公開號: 2012 US 675205 相關候選藥物類型: 多肽 相關候選藥物化學結構:2014030601035 適應癥: 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構。 |
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