【浮米每周专利快讯：2014年7月（二）】本周共有12篇专利，1、罗氏的Receptor d’Origine Nantais（RON） 激动剂（抗体），对对炎症型肠病,糖尿病和组织损伤的治疗尤其有效。本发明中的抗体对鼠源RON有良好的亲和力（0.9nM），且对pAKT的磷酸化作用的EC50为0.04 nM。等1. WO 2014085676标题: RON compositions and methods of use thereof
申请人: 罗氏
优先权日期及相关专利公开号: 2012 US 732048
相关候选药物类型: 抗体
相关候选药物化学结构:
适应症: 糖尿病、肠炎、组织损伤
专利摘要: This invention relates to RON compositions, in particular RON composition comprising a RON agonist, and methods of using the compositions for the treatment of diseases. The invention also relates to diagnosis of RON-associated or MSP-associated diseases.
备注: Receptor d’Origine Nantais（RON） 激动剂对炎症型肠病,糖尿病和组织损伤的治疗尤其有效。本发明中的抗体对鼠源RON有良好的亲和力（0.9nM），且对pAKT的磷酸化作用的EC50为0.04 nM。
2. WO 2014082979标题: Imidazopyridine derivatives
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 194721
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 焦虑症，阿尔茨海默氏症，抑郁症和中风
专利摘要: The present invention relates to compounds of general formula (I) wherein Ar is phenyl or pyridinyl; X1 is N or CH, X2 is N or CH, with the proviso that only one of X1 or X2 is N and the other is CH; R1 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen, cyano or S(O)2-lower alkyl; R2 is hydrogen, halogen, lower alkyl, lower alkoxy, lower alkyl substituted by halogen or cyano; 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.
备注: 能够刺激神经形成的化合物可用于治疗焦虑症，阿尔茨海默氏症，抑郁症和中风。本发明的化合物在神经干细胞增殖实验中，展示的EC50为0.008 mcM。
3. WO 2014079787标题: Substituted 1,6-naphthyridines
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 193311
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 焦虑症，阿尔茨海默氏症，抑郁症和中风
专利摘要: The present invention relates to the use of compounds of general formula (I) wherein R’ is hydrogen or lower alkyl; R1 is halogen, lower alkyl, cycloalkyl or cyano; or is phenyl, optionally substituted by one to three substituents, selected from lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen, halogen, cyano, hydroxy, C(O)-NH-lower alkyl, CH2-C(O)-NH-lower alkyl, CH2-NH-C(O)-lower alkyl, CH2NH2, S(O)2CH3, S(O)2N(CH3)2, or by heterocycloalkyl groups; or is pyrazol-1, 4 or 5-yl, optionally substituted by lower alkyl; or is thiazol-5-yl, optionally substituted by one or two lower alkyl groups; or is pyridine 2, 3 or 4-yl, optionally substituted by lower alkyl, lower alkoxy, halogen or N(CH3)2; or is 3,6-dihydro-2H-pyran; or is benzo[d][1,3]dioxol-5-yl; or is 2,3-dihydrobenzo[1,4]dioxin-6-yl; R2 is hydrogen, lower alkyl or lower alkyl substituted by alkoxy; R3 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, NH-S(O)2-CH3, -(CH2)m-O-lower alkyl or -(CH2)n-S(O)2-CH3; or is -(CR2)n-phenyl, optionally substituted by -S(O)2CH3 or lower alkoxy; or is -(CH2)n-heterocycloalkyl, optionally substituted by lower alkyl and =O; or is -(CH2)n-heteroaryl, optionally substituted by one or two lower alkyl groups; or is -(CH2)n-cycloalkyl, optionally substituted by cyano; or R2 and R3 form together with the N atom to which they are attached a heterocyclic ring, selected from morpholine, piperidine, 1, 1-dioxo-thiomorpholine or piperazine which may be substituted by lower alkyl or C(O)O-lower alkyl, or may form a pyrrolidine ring, optionally substituted by hydroxy; R is independently from n hydrogen or lower alkyl; n is 0, 1, 2, 3; m is 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture or to its corresponding enantiomer and/or optical isomers thereof, for the treatment of schizophrenia, obsessive-compulsive personality disorder, 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 (“chemobrain”), Down syndrome, autism spectrum disorders, hearing loss, tinnitus, spinocerebellar ataxia, amyotrophic lateral sclerosis, multiple sclerosis, Huntington’s disease, stroke, and disturbances due to radiation therapy, chronic stress, optic neuropathy or macular degeneration, or abuse of neuro-active drugs selected from alcohol, opiates, methamphetamine, phencyclidine or cocaine.
备注: 能够刺激神经形成的化合物可用于治疗焦虑症，阿尔茨海默氏症，抑郁症和中风。本发明的化合物在神经干细胞增殖实验中，展示的EC150为0.01 mcM。
4. WO 2014079850标题: Substituted heterocyclic derivatives
申请人: 罗氏
优先权日期及相关专利公开号: 2012 EP 193945
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 焦虑症，阿尔茨海默氏症，抑郁症和中风
专利摘要: The present invention relates to compounds of general formula (I-1) or (I-2) wherein R1 is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH2)2-lower akoxy, O(CH2)2N(CH3)2, or O(CH2)-morpholinyl; R1′ is hydrogen, lower alkyl, lower alkoxy, halogen, O(CH2)2-lower akoxy, O(CH2)2N(CH3)2, or O(CH2)-morpholinyl; with the proviso that both R1 and R1′ may be simultaneously hydrogen, but only one of R1 and R1′ is lower alkyl, lower alkoxy, halogen, O(CH2)2-lower akoxy, O(CH2)2N(CH3)2, or O(CH2)-morpholinyl; Het is a 5-or 6 membered heteroaryl group, wherein the heteroatom is selected from N, O or S; X is -CRR’-, -CRR’-NR’-, -C(O)-, -CH2-S-, -CH2-S(O)2-, CH2-O- or -CH2-CRR’-; R/R’ are independently from each other hydrogen, lower alkyl, hydroxy or phenyl, or R and R’ may form together with the carbon atom to which they are attached a cyclopropyl ring; R2 is lower alkyl, -C(O)O-lower alkyl, C3-6-cycloalkyl optionally substituted by lower alkyl or =O, bridged cyclohexyl or C3-6-cycloalkenyl, or is a 5-membered heteroaryl group, wherein the heteroatom is selected from N, O or S and which is optionally substituted by one or more lower alkyl, or is pyridinyl, optionally substituted by halogen or lower alkoxy; or is phenyl, optionally substituted by one or more R2′, selected from halogen, cyano, S(O)2-lower alkyl, lower alkyl, lower alkyl substituted by halogen, lower alkoxy, lower alkoxy substituted by halogen or amino, or is benzo[1,3]dioxolyl, naphthyl, indolyl, benzo-isoxazolyl, 2,3-dihydro-1H-indenyl, optionally substituted by lower alkoxy or by an oxo group, or is 3,4-dihydro-2H- [1,4]oxazinyl, optionally substituted by an oxo group, or is a five or six membered heterocycloalkyl group; 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 or prophylaxis 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.
备注: 能够刺激神经形成的化合物可用于治疗焦虑症，阿尔茨海默氏症，抑郁症和中风。本发明的化合物在神经干细胞增殖实验中，展示的EC50为0.01 mcM。
5. WO 2014081643标题: Novel compounds
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2012 US 728380
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 过敏性鼻炎，哮喘，炎症，癌症和感染
专利摘要: Compounds of formula (I) and salts thereof wherein R1 is n-C3-6alkyl; R2 is hydrogen or methyl; R3 is hydrogen or C1-6alkyl, and m is an integer having a value of 1 to 4; are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
备注: Interferon (IFN)-alpha 诱导剂可用于治疗过敏性鼻炎，哮喘，炎症，癌症和感染。本发明的化合物诱导 IFN-alpha的产生(pEC50 = 5.8或更高），且对TNF-alpha的产生具有选择性(pEC50 = 5.3或更低）
6. WO 2014081645标题: Novel compounds
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 US 774087
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 过敏性鼻炎，哮喘，炎症，癌症和感染
专利摘要: Compounds of formula (I) and salts thereof: wherein R1 is n-C4-6alkyl or C1-2alkoxyC1-2alkyl-; R2 is hydrogen or methyl; each R3 is hydroxy, halo or n-C1-3alkyl; m is an integer having a value of 2 to 4; n is an integer having a value of 0 to 3; and p is an integer having a value of 0 to 2, are inducers of human interferon. Compounds which induce human interferon may be useful in the treatment of various disorders, for example the treatment of allergic diseases and other inflammatory conditions, for example allergic rhinitis and asthma, infectious diseases and cancer, and may also be useful as vaccine adjuvants.
备注: Interferon (IFN)-alpha 诱导剂可用于治疗过敏性鼻炎，哮喘，炎症，癌症和感染。本发明的化合物诱导 IFN-alpha的产生(pEC50 = 5.3或更高），且对TNF-alpha的产生具有选择性(pEC50 = 5.3或更低）。
7. WO 2014081994标题: Novel compounds as diacylglycerol acyltransferase inhibitors
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2013 IN 3172
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 肥胖
专利摘要: This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1 ), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit.
备注: DGAT-1抑制剂可用于治疗肥胖。本发明中的化合物对DGAT-1的IC50约为29 nM。
8. WO 2014081995标题: Novel compounds as diacylglycerol acyltransferase inhibitors
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2012 IN 3592
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 肥胖
专利摘要: This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit.
备注: DGAT-1抑制剂可用于治疗肥胖。本发明中的化合物对DGAT-1的IC50约为49 nM。
9. WO 2014081996标题: Novel compounds as diacylglycerol acyltransferase inhibitors
申请人: 葛兰素史克
优先权日期及相关专利公开号: 2012 IN 3591
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 肥胖
专利摘要: This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1 ), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGA T-1 activity may have therapeutic benefit.
备注: DGAT-1抑制剂可用于治疗肥胖。本发明中的化合物对DGAT-1的IC50约为72 nM。
10. WO 2014085596标题: Monoclonal antibodies against activated protein C (aPC)
申请人: 拜耳
优先权日期及相关专利公开号: 2013 US 786472
相关候选药物类型: 抗体
相关候选药物化学结构:
适应症: 抗凝、血友病
专利摘要: Provided herein are antibodies, antigen-binding antibody fragments (Fabs), and other protein scaffolds, directed against human activated Protein C (aPC) with minimal binding to its zymogen Protein C (PC). Moreover, these aPC binding proteins could potentially block the anti-coagulant activity of aPC to induce coagulation. Therapeutic uses of these binders are described herein as are methods of panning and screening specific antibodies.
备注: 结合激活的蛋白C（aPC）的单克隆抗体用于治疗血友病及抗血凝。本发明中的一个人源单克隆IgG1抗体靶向人源结合激活的蛋白C（aPC),分别对兔、狗、鼠源的aPCs的亲和力分别为2.18, 7, 1.68和4.6 nM。对 兔、狗、鼠源的aPCs的EC50分别为2.2, 1.7和1.7 nM。
11. WO 2014082918标题: New indanyloxydihydrobenzofuranylacetic acids
申请人: 勃林格殷格翰
优先权日期及相关专利公开号: 2012 EP 194590
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: II型糖尿病
专利摘要: The present invention relates to compounds of general formula (I), wherein the group (Het)Ar is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
备注: GPR40激动剂可以用于治疗糖尿病。本发明的化合物对GPR40的EC50值为 3 nM。
12. WO 2014081619标题: Pyrimidine PDE10 inhibitors
申请人: 默克
优先权日期及相关专利公开号: 2012 US 728464
相关候选药物类型: 小分子药物
相关候选药物化学结构:
适应症: 精神分裂症，妄想症，药物引起的精神病，焦虑
专利摘要: The present invention is directed to pyrimidine compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington’s disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
备注: PDE10A抑制剂可以治疗神经精神疾病，包括精神分裂症，妄想症，药物引起的精神病，焦虑和神经退行性疾病。本发明的示例化合物对PDE10A的IC50为0.01 nM。
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