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1. 发明申请

WO2010091069A1 GASOLINE DEPOSIT CONTROL ADDITIVE COMPOSITIONS 审中-公开
标题翻译：汽油沉积控制添加剂组合物
公开(公告)号：WO2010091069A1
公开(公告)日：2010-08-12
申请号：PCT/US2010/023027
申请日：2010-02-03
申请人： BUTAMAX™ ADVANCED BIOFUELS LLC , WOLF, Leslie, R.
发明人： WOLF, Leslie, R.
IPC分类号： C10L1/22 , C10L1/228 , C10L1/222 , C10L10/18 , C10L1/2383 , C10L1/2387 , C10L1/232 , C08F8/30 , C08G59/14 , C07C209/78 , C07C223/00 , C07C249/02
CPC分类号： C10L1/22 , C07C249/02 , C10L1/026 , C10L1/1824 , C10L1/221 , C10L1/2222 , C10L1/224 , C10L1/226 , C10L1/228 , C10L1/2283 , C10L1/232 , C10L1/238 , C10L1/2383 , C10L1/2387 , C10L10/18
摘要： [0070] A gasoline deposit control additive composition for use in a fuel comprising from about 70 to about 95 volume percent of hydrocarbons in the gasoline boiling range and from about 5 to about 30 volume percent of at least one alcohol, comprising the imine or tertiary amine product of the reaction between (a) at least one aldehyde or ketone or mixture thereof having the formula R 16 CHO, R 16 CH 2 CHO, R 17 (C=O) R 18 or R 17 CH 2 (C=O) R 18 , wherein R 16 , R 17 , and R 18 are the same or different and are each independently a straight or branched chain hydrocarbyl or aryl group that contains from 1 to 18 carbon atoms, and (b) a primary or secondary amine functionality.
摘要翻译：一种用于燃料的汽油沉积物控制添加剂组合物，其包含约70至约95体积％的汽油沸程中的烃和约5至约30体积％的至少一种醇，其包含亚胺或三级（a）至少一种具有式R 16 CHO，R 16 CH 2 CHO，R 17（C = O）R 18或R 17 CH 2（C = O）R 18的醛或酮或其混合物之间的反应的胺产物，其中R 16，R 17，和R 18相同或不同，并且各自独立地为含有1至18个碳原子的直链或支链烃基或芳基，和（b）伯胺或仲胺官能团。

2. 发明申请

WO00064583A1 METAL CATALYSTS AND METHODS FOR MAKING AND USING SAME 审中-公开
标题翻译：金属催化剂及其制备和使用方法
公开(公告)号：WO00064583A1
公开(公告)日：2000-11-02
申请号：PCT/US2000/011287
申请日：2000-04-26
IPC分类号： B01J23/46 , B01J31/18 , B01J31/22 , C07B53/00 , C07B61/00 , C07C67/343 , C07C69/616 , C07C69/618 , C07C69/732 , C07C69/757 , C07D207/08 , C07D207/26 , C07D207/277 , C07F11/00 , C07F13/00 , C07F15/00 , B01J31/00 , C07C55/00 , C07C223/00 , C07C225/00 , C07C229/00 , C07D207/00 , C07D313/00 , C07D401/00
CPC分类号： C07F15/008 , B01J23/462 , B01J31/1805 , B01J31/2239 , B01J2231/341 , B01J2231/4205 , B01J2231/46 , B01J2531/0219 , B01J2531/0258 , B01J2531/0288 , B01J2531/64 , B01J2531/66 , B01J2531/74 , B01J2531/821 , B01J2531/822 , B01J2531/824 , B01J2540/34 , C07C67/343 , C07D207/08 , C07D207/277 , C07F11/005 , C07F13/005 , C07F15/0053 , C07F15/0066 , C07C69/608 , C07C69/616 , C07C69/618
摘要： Compounds having formula (A) are disclosed. M and M are the same or different and are transition metal atoms or ions; Z and Z , independtly, are the atoms necessary to complete a 3-12 membered heterocyclic ring; Z is an alkylene or arylene group; Q and Q are the same or different and are electron withdrawing groups; L and L , taken together, represent -O-CR -O-; L and L , taken together, represent -O-CR -O-; R and R are the same or different and are selected from the group consisting of akyl groups and aryl groups or R and R represent alkylene or arylene groups that are directly or indirectly bonded to one another. Methods for making such compounds are also disclosed, as are intermediates which can be used in their preparation. Also disclosed are methods for carrying out C-H insertion reactions using bis-transition metal catalysts, such as the above compounds. Procedures for preparing d-threo methylphenidate, tolterodine, CDP-840, nominfensine, and sertraline, are described.
摘要翻译：公开了具有式（A）的化合物。 M 1和M 2相同或不同，为过渡金属原子或离子; Z 2和Z 3独立地是完成3-12元杂环所必需的原子; Z 1是亚烷基或亚芳基; Q 1和Q 2相同或不同，为吸电子基团; L 1和L 3一起表示-O-CR 13 -O-; L 2和L 4一起表示-O-CR 14 -O-。 R 13和R 14相同或不同，并且选自烷基和芳基，或R 13和R 14代表与一个或多个直接或间接键合的亚烷基或亚芳基另一个。还公开了制备这些化合物的方法，以及可以用于其制备的中间体。还公开了使用双过渡金属催化剂如上述化合物进行C-H插入反应的方法。描述了制备D-苏式哌甲酯，托特罗定，CDP-840，延胡素和舍曲林的方法。

3. 发明申请

WO2014106805A3 FATTY ACID CONJUGATES AND THEIR USES 审中-公开
标题翻译：脂肪酸混合物及其用途
公开(公告)号：WO2014106805A3
公开(公告)日：2017-03-23
申请号：PCT/IB2013061385
申请日：2013-12-28
申请人： CELLIXBIO PRIVATE LTD
发明人： KANDULA MAHESH
IPC分类号： A61K31/00 , A61K9/00 , A61P3/10 , C07C223/00
CPC分类号： C07D213/80
摘要： The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing metabolic syndrome, cancer, a metabolic disease, a neurodegenerative disease and insulin resistance and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, neuropathic pain, hypertriglyceridemia, hyperglycemia, hyperinsulinemia, metabolic syndrome, cancer, metabolic disease, neurodegenerative diseases and insulin resistance.
摘要翻译：本发明涉及式I和式II化合物或其药学上可接受的盐，以及多晶型物，溶剂合物，对映体，立体异构体和水合物。药物组合物包含有效量的式I或式II化合物; 并且可以配制用于治疗或预防代谢综合征，癌症，代谢疾病，神经变性疾病和胰岛素抵抗和糖尿病的方法，用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射。这些组合物可用于治疗糖尿病，肥胖，脂质障碍，神经性疼痛，高甘油三酯血症，高血糖症，高胰岛素血症，代谢综合征，癌症，代谢疾病，神经变性疾病和胰岛素抵抗。

4. 发明申请

WO2014083476A3 COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC AND LIPID DISORDERS 审中-公开
标题翻译：用于治疗代谢性和脂肪性疾病的组合物和方法
公开(公告)号：WO2014083476A3
公开(公告)日：2015-11-26
申请号：PCT/IB2013060189
申请日：2013-11-16
申请人： CELLIXBIO PRIVATE LTD
发明人： KANDULA MAHESH
IPC分类号： C07C223/00 , A61K31/202 , A61P3/00
CPC分类号： C07D213/79 , C07D213/80
摘要： The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing metabolic and lipid disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes, insulin resistance, hyperglycemia, hypertriglyceridemia, lipid disorders and cardiovascular diseases.
摘要翻译：本发明涉及式I和式II化合物或其药学上可接受的盐，以及多晶型物，溶剂合物，对映异构体，立体异构体和水合物。药物组合物包含有效量的式I或式II化合物; 并且可以配制用于口服，口腔，直肠，局部，透皮，经粘膜，静脉内，肠胃外给药，糖浆或注射的用于治疗或预防代谢和脂质疾病的方法。这样的组合物可用于治疗糖尿病，胰岛素抵抗，高血糖症，高甘油三酯血症，脂质疾病和心血管疾病。

5. 发明申请

WO2011038572A1 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2011038572A1
公开(公告)日：2011-04-07
申请号：PCT/CN2010/001501
申请日：2010-09-27
申请人： GLAXO GROUP LIMITED , GLAXOSMITHKLINE (CHINA) R&D COMPANY LIMITED , NICHOLS, Paula Louise , EATHERTON, Andrew John , BAMBOROUGH, Paul , JANDU, Karamjit Singh , PHILPS, Oliver James , ANDREOTTI, Daniele
发明人： NICHOLS, Paula Louise , EATHERTON, Andrew John , BAMBOROUGH, Paul , JANDU, Karamjit Singh , PHILPS, Oliver James , ANDREOTTI, Daniele
IPC分类号： C07D265/30 , C07D261/14 , C07D241/04 , C07D237/20 , C07D231/12 , C07C233/00 , C07C223/00 , A61K31/5375 , A61K31/4965 , A61K31/495 , A61K31/44 , A61K31/42 , A61K31/4155 , A61P25/16 , A61P25/28 , A61P25/00
CPC分类号： C07C235/64 , C07D213/75 , C07D231/40 , C07D237/20 , C07D261/14 , C07D263/48 , C07D401/12 , C07D403/12 , C07D413/12
摘要： The present invention discloses novel compounds inhibiting LRRK2 kinase activity, the preparation processes thereof, the compositions containing them, as well as the use in treating diseases characterized by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.
摘要翻译：本发明公开了抑制LRRK2激酶活性的新化合物，其制备方法，含有它们的组合物，以及用于治疗以LRRK2激酶活性为特征的疾病，特别是帕金森病和阿尔茨海默氏病。

6. 发明申请

WO2003106399A2 PROCESS FOR PREPARING N-PROTECTED β-AMINO ALDEHYDE COMPOUNDS 审中-公开
标题翻译：制备N-保护的β-氨基醛酸化合物的方法
公开(公告)号：WO2003106399A2
公开(公告)日：2003-12-24
申请号：PCT/US2003/018847
申请日：2003-06-16
申请人： THERAVANCE, INC. , LEE, Junning , LIU, Jyanwei
发明人： LEE, Junning , LIU, Jyanwei
IPC分类号： C07C223/00
CPC分类号： C07C221/00 , C07C269/06 , C07C225/04 , C07C271/18
摘要： The invention provides processes for preparing N-protected β-amino aldehyde compounds which are useful as synthetic intermediates for preparing glycopeptide antibiotic derivatives. The processes include cleaving a carbon-carbon double bond to form the N-protected β-amino aldehyde compound.
摘要翻译：本发明提供了制备N-保护的β-氨基醛化合物的方法，其可用作制备糖肽抗生素衍生物的合成中间体。该方法包括切割碳 - 碳双键以形成N-保护的β-氨基醛化合物。

7. 发明申请

WO2014087307A3 COMPOSITIONS AND METHODS FOR THE TREATMENT OF METABOLIC SYNDROME AND DIABETES 审中-公开
公开(公告)号：WO2014087307A3
公开(公告)日：2014-06-12
申请号：PCT/IB2013/060502
申请日：2013-11-29
申请人： KANDULA, Mahesh
发明人： KANDULA, Mahesh
IPC分类号： A61K31/202 , A61B3/00 , C07C223/00 , C07C229/03
摘要： The invention relates to the compounds of formula I and formula II or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I or formula II; and methods for treating or preventing metabolic syndrome and diabetes may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of diabetes mellitus, obesity, lipid disorders, hypertriglyceridemia, hyperglycemia, hyperinsulinemia and insulin resistance.

8. 发明申请

WO2012143933A1 A PROCESS FOR PREPARATION OF 4-FLUORO-α-[2-METHYL-L-OXOPROPYL]-γ-OXO-N-β-DIPHENYLBENZENE BUTANE AMIDE 审中-公开
标题翻译：制备4-氟-α-[2-甲基-L-氧杂] -L-肟基-N-β-二苯乙烯丁酸酰胺的方法
公开(公告)号：WO2012143933A1
公开(公告)日：2012-10-26
申请号：PCT/IN2011/000710
申请日：2011-10-13
申请人： VIJAYASRI ORGANICS LIMITED , SRIVATSAVAYI, Jagapathi Raju , POTHUKUCHI, Sairam , RANI, Srinivasa Sastry , CHIKKA, Mallikarjuna Rao , CHEEKATI, Chiranjeevi , GUTTI, Mallikarjuna Rao , SINGAVARAPU, Trimurthulu , THIMMAIPALLY , Venkat Reddy , TADANKI, Venkateswara Rao
发明人： SRIVATSAVAYI, Jagapathi Raju , POTHUKUCHI, Sairam , RANI, Srinivasa Sastry , CHIKKA, Mallikarjuna Rao , CHEEKATI, Chiranjeevi , GUTTI, Mallikarjuna Rao , SINGAVARAPU, Trimurthulu , THIMMAIPALLY , Venkat Reddy , TADANKI, Venkateswara Rao
IPC分类号： C07C223/00
CPC分类号： C07C231/12 , C07C231/22 , C07C235/78
摘要： A process for preparation of 4-fluoro-alpha-[2-methyl-l -oxopropyl]-gama-oxo-N- beta-diphenylbenzene butane amide also known as a diketone intermediate of atorvastatin, completely devoid of impurities 3,4-difluoro-alpha-[2-methyl-l-oxopropyl]-gama-oxo-n-beta-diphenylbenzene butane amide; methyl, 2 {-2[-(4-fluorophenyl)-2-oxo- 1 -phenyl ethyl)] } -4-methyl-3-oxo pentanoate; 1,4-bis(4-fluorophenyl)-2,3-diphenylbutane- 1,4-dione, 1 -(4-fluorophenyl)-2-phenyl ethanone; l-(4-fluorophenyl)-2-phenyl ethanone and containing about 0.05% or less of 2-methyl- l-oxopropyl]-gama-oxo-N-beta- diphenylbenzene butane amide. In that process the said diketone intermediate of formula 1 is obtained by maintaining temperature -25° C to 50° C during Friedel-Crafts acylation, in situ halogenation of formula II in presence of a solvent and nucleophilic substitution from a compound of formula III with formula IV in presence of a base.
摘要翻译：制备4-氟-α-[2-甲基-1-氧代丙基] - 谷 - 氧代-β-二苯基苯丁烷酰胺的方法，也称为阿托伐他汀的二酮中间体，完全没有杂质3,4-二氟 -α-[2-甲基-1-氧代丙基] - 谷 - 氧代-n-β-二苯基苯丁烷酰胺; 甲基，2 {-2 [ - （4-氟苯基）-2-氧代-1-苯基乙基）]} -4-甲基-3-氧代戊酸甲酯; 1,4-双（4-氟苯基）-2,3-二苯基丁烷-1,4-二酮，1-（4-氟苯基）-2-苯基乙酮; 1-（4-氟苯基）-2-苯基乙酮，并含有约0.05％或更少的2-甲基-1-氧代丙基] - 谷 - 氧代-N-β-二苯基苯丁烷酰胺。在该方法中，所述式1的二酮中间体通过在Friedel-Crafts酰化期间保持温度-25℃至50℃，在溶剂存在下在式II的原位卤化和式III化合物的亲核取代与式IV在碱存在下。

9. 发明申请

WO01014313A1 NOVEL AMINE AND QUATERNARY AMMONIUM COMPOUNDS MADE FROM KETONES AND ALDEHYDES, AND COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：来自酮和醛的新型胺和季铵化合物及其组合物
公开(公告)号：WO01014313A1
公开(公告)日：2001-03-01
申请号：PCT/US2000/023071
申请日：2000-08-23
IPC分类号： A61K8/30 , A01N25/04 , A01N25/30 , A61K8/00 , A61K8/31 , A61K8/34 , A61K8/37 , A61K8/40 , A61K8/41 , A61K8/42 , A61K8/44 , A61K8/46 , A61K8/89 , A61K8/891 , A61Q5/00 , A61Q5/02 , A61Q5/06 , A61Q5/12 , A61Q19/00 , A61Q19/10 , C07B43/00 , C07B61/00 , C07C213/02 , C07C213/08 , C07C215/08 , C07C215/40 , C07C217/08 , C07C221/00 , C07C225/00 , C10M133/06 , C10N30/12 , C11D1/46 , C11D1/62 , D06M13/328 , D06M13/463 , C07C223/00 , C07C229/00
CPC分类号： C07C215/40 , A61K8/44 , A61Q5/02 , A61Q5/12 , A61Q19/00 , C07C215/08
摘要： A process for making a tertiary amine ester of formula (I), the process comprising: (a) reacting a ketone or an aldehyde having formula (III) with a glycol to form a ketal or an acetal; (b) reacting the ketal or the acetal with acrylonitrile to form an ether nitrile; (c) reducing the ether nitril to a tertiary amine ketal or a tertiary amine acetal; (d) hydrolyzing the tertiary amine ketal or the tertiary amine acetal to a tertiary amine diol; and (e) esterifying the tertiary amine diol to the tertiary amine ester of formula (I), wherein R and R are each independently a hydrogen atom or a linear, branched, or cyclic alkyl, alkylene, alkaryl, or aryl-containing group containing 1 to 18 carbon atoms; and each R are each independently of one another fatty acid radicals having 6-22 carbon atoms. The process may optionally include the further step of: (f) protonating or quaternizing the tertiary amine ester of formula (I) to a protonated or quaternary amine ester of formula (II) wherein A is an inorganic or organic anion.
摘要翻译：制备式（I）的叔胺酯的方法，该方法包括：（a）使酮或具有式（III）的醛与二醇反应以形成缩酮或缩醛; （b）使缩酮或缩醛与丙烯腈反应形成醚腈; （c）将醚腈还原成叔胺缩酮或叔胺缩醛; （d）将叔胺缩酮或叔胺缩醛水解成叔胺二醇; 和（e）将叔胺二醇酯化为式（I）的叔胺酯，其中R 1和R 2各自独立地为氢原子或直链，支链或环状的烷基，亚烷基，烷芳基，或含有1至18个碳原子的含芳基; 并且每个R 3各自独立地为具有6-22个碳原子的另一个脂肪酸基团。该方法可以任选地包括以下步骤：（f）将式（I）的叔胺酯质子化或季铵化为式（II）的质子化或季胺酯，其中A 1是无机或有机阴离子。

10. 发明申请

WO98045249A1 2-AMINOPROPANE-1,3-DIOL COMPOUNDS, MEDICINAL USE THEREOF, AND INTERMEDIATES IN SYNTHESIZING THE SAME 审中-公开
标题翻译： 2-氨基丙-1,3-二醇化合物，其医药用途及其合成中间体
公开(公告)号：WO98045249A1
公开(公告)日：1998-10-15
申请号：PCT/JP1998/001571
申请日：1998-04-03
IPC分类号： A61K31/00 , A61K31/13 , A61K31/135 , A61P37/00 , A61P37/06 , C07C20060101 , C07C215/00 , C07C215/10 , C07C215/34 , C07C223/00 , C07C223/02 , C07C225/08 , C07C225/16 , C07F7/18
CPC分类号： C07C225/16 , C07C215/34 , C07C223/02 , C07F7/1804
摘要： Compounds represented by general formula (I), pharmaceutically acceptable acid addition salts thereof, or hydrates of the same; drugs containing these compounds; medicinal compositions containing these compounds together with pharmaceutically acceptable carriers; and 2-amino-2-(2-(4-(1-hydroxy-5-phenylpentyl)phenyl)ethyl)propane-1,3-diol or 2-amino-2-(2-(4-formylphenyl)ethyl)-propane-1,3-diol optionally protected at the amino and/or hydroxy group or salts thereof, each useful as an intermediate in synthesizing the above compounds. In said formula, R , R , R and R represent each hydrogen or acyl. Because of having little toxicity, high safety and excellent immunosuppressive effects, these compounds are useful as preventives or depressants for rejection reactions in organ or bone marrow transplantations and preventives or remedies for various autoimmune diseases, various allergic diseases, etc.
摘要翻译：由通式（I）表示的化合物，其药学上可接受的酸加成盐或其水合物; 含有这些化合物的药物; 含有这些化合物与药学上可接受的载体的药物组合物; 和2-氨基-2-（2-（4-（1-羟基-5-苯基戊基）苯基）乙基）丙烷-1,3-二醇或2-氨基-2-（2-（4-甲酰基苯基）乙基）任选在氨基和/或羟基保护的丙烷-1,3-二醇或其盐，各自用作合成上述化合物的中间体。在所述式中，R 1，R 2，R 3和R 4各自代表氢或酰基。由于毒性小，安全性高，免疫抑制效果好，这些化合物可用作器官或骨髓移植排斥反应的预防剂或抑制剂，各种自身免疫性疾病，各种过敏性疾病等的预防措施或治疗方法。

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