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1. 发明申请

WO2003022263A1 PHARMACEUTICAL COMPOSITION COMPRISING GAMMA-BUTYROBETAINE FOR STIMULATING THE SEXUAL ACTIVITY AND POTENCY 审中-公开
标题翻译：包含GAMMA-BUTYROBETAINE用于刺激性活动和兴奋剂的药物组合物
公开(公告)号：WO2003022263A1
公开(公告)日：2003-03-20
申请号：PCT/LV2002/000005
申请日：2002-03-04
申请人： KALVINSH, Ivars , VEVERIS, Maris , BIRMANS, Anatolijs
发明人： KALVINSH, Ivars , VEVERIS, Maris , BIRMANS, Anatolijs
IPC分类号： A61K31/205
CPC分类号： A61K31/519 , A61K31/205 , A61K2300/00
摘要： New medical use for gamma-butyrobetaine is disclosed. Also disclosed are pharmaceutical compositions, containing gamma-butyrobetaine or combination thereof with L-carnitine or sildenafil for oral, parenteral, subcutaneous, transdermal, topical, sublingual, intrauetral, intranasal or rectal application, useful for stimulation of sexual activity and potency in mammals. The disclosed compositions, when applied orally for 6 weeks to non-narcotized male rats substantially increase their sexual activity, decreasing the arousal time, increasing the number of copulations and resultativeness of mounting attempts. When applied by intracavernous or intravenous route said pharmaceutical compositions increase intracorporeal pressure and duration of erection, as well as restore stimulation-induced reflectory erections in anesthetized animals.
摘要翻译：公开了γ-丁基甜菜碱的新用途。还公开了含有γ-丁基甜菜碱或其与L-肉毒碱或西地那非的组合的药物组合物，用于口服，肠胃外，皮下，经皮，局部，舌下，耳内，鼻内或直肠应用，可用于刺激哺乳动物的性活动和效力。所公开的组合物当向非麻醉的雄性大鼠口服6周时大大增加其性活动，减少觉醒时间，增加交配次数和安装尝试的有效性。当通过海绵体内或静脉内途径施用时，所述药物组合物增加体内压力和勃起持续时间，以及恢复麻醉动物中刺激诱导的反射勃起。

2. 发明申请

WO2003022262A1 PHARMACEUTICAL COMPOSITION COMPRISING GAMMA-BUTYROBETAINE 审中-公开
标题翻译：包含γ-丁二醛的药物组合物
公开(公告)号：WO2003022262A1
公开(公告)日：2003-03-20
申请号：PCT/LV2002/000004
申请日：2002-03-04
申请人： KALVINSH, Ivars , VEVERIS, Maris , BIRMANS, Anatolijs
发明人： KALVINSH, Ivars , VEVERIS, Maris , BIRMANS, Anatolijs
IPC分类号： A61K31/205
CPC分类号： A61K31/205 , A61K31/495 , A61K31/505
摘要： New medical use for gamma-butyrobetaine is disclosed. Also disclosed are pharmaceutical compositions, containing gamma-butyrobetaine or combination thereof with 3-(2,2,2-trimethylhydrazinium)propionate or sildenafil for oral, parenteral, subcutaneous, transdermal, topical, sublingual, intrauretral, intranasal or rectal application, useful for stimulation of sexual activity and potency in mammals. The disclosed compositions, when applied orally for 6 weeks to non-narcotized male rats substantially increase their sexual activity, decreasing the arousal time, increasing the number of copulations and resultativeness of mounting attempts. When applied by intracavernous or intravenous route said pharmaceutical compositions increase intracorporeal pressure and duration of erection, as well as restore stimulation-induced reflectory erection in narcotized animals.
摘要翻译：公开了γ-丁基甜菜碱的新用途。还公开了含有γ-丁基甜菜碱或其与3-（2,2,2-三甲基肼）丙酸酯或西地那非的组合的药物组合物用于口服，肠胃外，皮下，透皮，局部，舌下，眼内，鼻内或直肠施用，可用于刺激哺乳动物的性活动和潜力。所公开的组合物当向非麻醉的雄性大鼠口服6周时大大增加其性活动，减少觉醒时间，增加交配次数和安装尝试的有效性。当通过海绵体内或静脉内途径施用时，所述药物组合物增加体内压力和勃起持续时间，以及恢复麻醉动物中刺激诱导的反射勃起。

3. 发明申请

WO2005012233A1 MELDONIUM SALTS, METHOD OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITION ON THEIR BASIS 审中-公开
标题翻译： MELDONIUM盐，它们的制备方法及其基础上的药物组合物
公开(公告)号：WO2005012233A1
公开(公告)日：2005-02-10
申请号：PCT/LV2004/000005
申请日：2004-07-15
申请人： "GRINDEKS" PUBLIC JOINT STOCK COMPANY , KALVINSH, Ivars , BIRMANS, Anatolijs
发明人： KALVINSH, Ivars , BIRMANS, Anatolijs
IPC分类号： C07C243/12
CPC分类号： A61K9/0095 , A61K9/0031 , A61K9/0056 , C07C53/16 , C07C55/07 , C07C55/10 , C07C55/14 , C07C57/145 , C07C57/15 , C07C59/08 , C07C59/265 , C07C243/14
摘要： New salts of Meldonium, the method of their preparation, and pharmaceutical formulation on their basis have been described. The general formula of these salts is X-(CH3)3N+NHCH2CH2COOH where X- is an acid anion selected from the group of pharmaceutically acceptable acids. Practically non-hygroscopicand/or increased thermal stability and/or lasting action Meldonium hydrogen salts of fumaric acid, phosphoric acid, oxalic acid, maleic acid, and pamoic acid as well as Meldoinum orotate and galactarate are especially suitable. Novel pharmaceutical formulations containing non-hygroscopicand/or increased thermal stability and/or lasting action 3-(2,2,2-trimethylhydrazinium) propionate salts for oral, parenteral, rectal and transdermal introduction are concurrently described.
摘要翻译：已经描述了米曲肼的新盐，其制备方法和药物制剂。这些盐的通式是X-（CH 3）3 N + NHCH 2 CH 2 COOH，其中X是选自药学上可接受的酸的酸阴离子。实际上非吸湿性和/或增加的热稳定性和/或持久作用富马酸，磷酸，草酸，马来酸和双羟萘酸的麦角鎓氢盐以及乳清酸乳状芽孢杆菌和乳酸乳状芽孢杆菌特别合适。同时描述了用于口服，肠胃外，直肠和透皮引入的含有非吸湿性和/或增加的热稳定性和/或持久作用的3-（2,2,2-三甲基肼）丙酸盐的新型药物制剂。

4. 发明申请

WO2008080992A2 A PROCESS FOR THE PREPARATION OF 6-[3-(1-ADAMANTYL)-4-METHOXYPHENYL-2-NAPHTOIC ACID 审中-公开
标题翻译：制备6- [3-（1-亚氨基）-4-甲氧基苯基] -2-萘酸的方法
公开(公告)号：WO2008080992A2
公开(公告)日：2008-07-10
申请号：PCT/EP2007/064647
申请日：2007-12-28
申请人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir
发明人： KALVINSH, Ivars , CHERNOBROVIJS, Aleksandrs , TRIBULOVICH, Vyacheslav , LABEISH, Vladimir
CPC分类号： C07C67/343 , C07C51/09 , C07C2603/74 , C07C65/26 , C07C69/94
摘要： A process for preparation of 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid from 2-(1-adamantyl)-4-bromanisolee is disclosed, based on transformation of 2-(1-adamantyl)-4-bromanisole into a Grignard's reagent by using metallic magnesium, anhydrous lithium chloride and dibromoethane followed by transmetallation with borates to 3-(adamantyl)-4-methoxyphenylboronic acid, wich is converted into 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid esters by Suzuki-Miyaura cross-coupling reaction with alkyl-6-halonaftoates catalyzed by Pd [0] or Pd/phosphine ligands and followed by basic hydrolysis in ethylene glycol or 1,2-propanediol of ester thus obtained into 6-[3-(1-adamantyl)-4-methoxyphenyl]-2-naphthoic acid.
摘要翻译：从2-（1-金刚烷基）-4-溴胸苷酸制备6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸的方法公开于，基于通过使用金属镁，无水氯化锂和二溴乙烷将2-（1-金刚烷基）-4-溴甲茴香醚转化为格氏试剂，然后用硼酸酯转化为3-（金刚烷基）-4-甲氧基苯基硼酸，将其转化成6- 通过与Pd [0]或Pd /膦配体催化的烷基-6-卤代芴酯通过Suzuki-Miyaura交叉偶联反应形成[3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸酯，然后在乙二醇或1,2-丙二醇酯转化为6- [3-（1-金刚烷基）-4-甲氧基苯基] -2-萘甲酸。

5. 发明申请

WO2008015271A1 PYRAZOLOPYRIMIDINES, A PROCESS FOR THEIR PREPARATION AND THE USE AS A MEDICINE 审中-公开
标题翻译：吡唑并嘧啶，其制备方法和用作药物的方法
公开(公告)号：WO2008015271A1
公开(公告)日：2008-02-07
申请号：PCT/EP2007/058062
申请日：2007-08-03
申请人： MERZ PHARMA GMBH & CO. KGAA , DANYSZ, Wojciech , DEKUNDY, Andrzej , HECHENBERGER, Mirko , HENRICH, Markus , JATZKE, Claudia , NAGEL, Jens , PARSONS, Christopher Graham Raphael , WEIL, Tanja , FOTINS, Juris , GUTCAITS, Aleksandra , KALVINSH, Ivars , ZEMRIBO, Ronalds , KAUSS, Valerjans
发明人： DANYSZ, Wojciech , DEKUNDY, Andrzej , HECHENBERGER, Mirko , HENRICH, Markus , JATZKE, Claudia , NAGEL, Jens , PARSONS, Christopher Graham Raphael , WEIL, Tanja , FOTINS, Juris , GUTCAITS, Aleksandra , KALVINSH, Ivars , ZEMRIBO, Ronalds , KAUSS, Valerjans
IPC分类号： C07D487/04 , A61K31/519
CPC分类号： C07D487/04 , C07D519/00
摘要： Substituted pyrazolopyrimidine derivatives of formula (I) wherein R 1 represents chloro or bromo; R 2 , R 3 , R 4 , R 5 , R 6 and R 7 independently represent e. g. hydrogen or C 1-6 -alkyl; R 8 represents a radical R 9 or a radical R 10 , whereby one of the two radicals R 8 denotes R 9 and the other radical R 8 denotes R 10 ; R 9 represents e. g. a phenyl or thiophen group, and R 10 represents e. g. hydrogen or methyl; are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
摘要翻译：式（I）的取代的吡唑并嘧啶衍生物其中R 1表示氯或溴; R 2，R 3，R 4，R 5，R 6和R 6，和 R＆lt; 7＆gt;独立地表示e。 G。氢或C 1-6 - 烷基; R 8表示基团R 9或基团R 10，其中两个基团R 8中的一个表示 R 9和另一个基团R 8表示R 10; R 9表示e。 G。苯基或噻吩基，R 10代表e。 G。氢或甲基; 是有效的mGluR5调节剂，可用于预防急性和慢性神经障碍。

6. 发明申请

WO2007021164A1 PHARMACEUTICAL COMPOSITION ON BASIS OF REVERSE TRANSCRIPTASE INHIBITOR AND MELDONIUM 审中-公开
标题翻译：基于逆向转录酶抑制剂和药物的药物组合物
公开(公告)号：WO2007021164A1
公开(公告)日：2007-02-22
申请号：PCT/LV2006/000005
申请日：2006-08-08
申请人： GRINDEKS, joint stock company , KLUSHA, Vija , ISAJEVS, Sergejs , PUPURE, Jolanta , RUMAKS, Juris , GORDJUSHINA, Valentina , TAIVANS, Immanuels , KALVINSH, Ivars
发明人： KLUSHA, Vija , ISAJEVS, Sergejs , PUPURE, Jolanta , RUMAKS, Juris , GORDJUSHINA, Valentina , TAIVANS, Immanuels , KALVINSH, Ivars
IPC分类号： A61K31/15 , A61K31/7072 , A61K31/513 , A61P31/18
CPC分类号： A61K31/513 , A61K31/15 , A61K31/7072 , A61K2300/00
摘要： Novel pharmaceutical compositions which contain one of the reverse transcriptase inhibitors, viz., Zidovudine, Lamivudine or Stavudine in clinically efficacious amount and Meldonium as well as pharmaceutically applicable excipients. It has been proved that inclusion of Meldonium in these pharmaceutical compositions essentially diminishes the cardio- and neuro-toxicity of the reverse transcriptase inhibitor.
摘要翻译：含有临床有效量的逆转录酶抑制剂Zidovudine，拉米夫定或司他夫定之一的新型药物组合物以及药用赋形剂。已经证明，在这些药物组合物中包含Meldonium基本上降低了逆转录酶抑制剂的心脏和神经毒性。

7. 发明申请

WO2006037996A1 NOVEL CYCLIC AND ACYCLIC PROPENONES FOR TREATING CNS DISORDERS 审中-公开
标题翻译：用于治疗CNS疾病的新型循环和ACYCLIC PROPENONES
公开(公告)号：WO2006037996A1
公开(公告)日：2006-04-13
申请号：PCT/GB2005/003817
申请日：2005-10-05
申请人： MERZ PHARMA GMBH & CO. KGAA , PARSONS, Christopher, Graham, Raphael , KALVINSH, Ivars , KAUSS, Valerjans , TRIFANOVA, Dina , ZEMRIBO, Ronalds , DANYSZ, Wojciech , HENRICH, Markus , WEIL, Tanja
发明人： PARSONS, Christopher, Graham, Raphael , KALVINSH, Ivars , KAUSS, Valerjans , TRIFANOVA, Dina , ZEMRIBO, Ronalds , DANYSZ, Wojciech , HENRICH, Markus , WEIL, Tanja
IPC分类号： A61K31/121 , A61K31/122 , A61K31/343 , A61K31/353 , A61K31/404 , A61K31/47 , C07C49/255 , C07C49/553 , C07C49/533 , C07D209/32 , C07D215/14 , C07D307/80 , C07D311/58
CPC分类号： C07D307/80 , C07C45/74 , C07C49/255 , C07C49/553 , C07C49/577 , C07C49/84 , C07D209/12 , C07D209/32 , C07D215/14 , C07D311/58 , C07D319/18 , C07D401/04 , C07D407/06 , C07D413/04 , C07D417/04 , C07D491/04
摘要： The invention relates to novel cyclic and non-cyclic propenone derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are useful as medicaments.
摘要翻译：本发明涉及新的环状和非环状丙烯酮衍生物及其药学上可接受的盐。本发明还涉及制备这些化合物的方法。本发明的化合物可用作药物。

8. 发明申请

WO2004065354A1 CARBAMIC ACID COMPOUNDS COMPRISING AN ESTER OR KETONE LINKAGE AS HDAC INHIBITORS 审中-公开
标题翻译：含有ESET或KETONE连接作为HDAC抑制剂的碳酸化合物
公开(公告)号：WO2004065354A1
公开(公告)日：2004-08-05
申请号：PCT/GB2004/000147
申请日：2004-01-19
申请人： TOPOTARGET UK LIMITED , FINN, Paul, W. , KALVINSH, Ivars , LOZA, Einars , GUTCAITS, Aleksandrs , OLUTNIKA, Irena , SERPIONOVA, Ludmila , GAILITE, Vija , BOKALDERE, Rasma
发明人： FINN, Paul, W. , KALVINSH, Ivars , LOZA, Einars , GUTCAITS, Aleksandrs , OLUTNIKA, Irena , SERPIONOVA, Ludmila , GAILITE, Vija , BOKALDERE, Rasma
IPC分类号： C07C259/10
CPC分类号： C07C251/48 , C07C259/10 , C07C2601/08 , C07C2601/14 , C07D211/32
摘要： This invention pertains to certain carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently: -O-C(=O)- or -C(=O)-O- or - C(=O)-; Cy is a cyclyl group and is independently: C 3-20 carbocyclyl, C 3-20 heterocyclyl, or C 5-20 aryl; and is optionally substituted; Q 1 is a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having from 4 to 7 ring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having from 4 to 7 ring atoms including 1 nitrogen ring atom or 1 oxygen ring atom; and is optionally substituted; Q 2 is an acid leader group, and is independently: C 1-8 alkylene; and is optionally substituted; or: Q 2 is an acid leader group, and is independently: C 5-20 arylene; C 5-20 arylene-C 1-7 alkylene; C 1-7 alkylene-C 5-20 arylene; or C 1-7 alkylene-C 5-20 arylene-C 1-7 alkylene; and is optionally substituted; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC,and in the treatment of conditions mediated by HDAC, cancer, proliferative conditions, psoriasis, etc.
摘要翻译：本发明涉及抑制HDAC（组蛋白脱乙酰酶）活性的某些式（I）的氨基甲酸化合物：其中：J为连接官能团，独立地为：-OC（= O） - 或-C（= O） -O-或-C（= O） - ; Cy是环状基团，独立地为：C 3-20碳环基，C 3-20杂环基或C 5-20芳基; 并且任选被取代; Q 1是环状前导基团，并且独立地是通过从具有4至7个环原子的饱和单环烃的环碳原子中除去两个氢原子或通过从环中除去两个氢原子而获得的二价二齿基团具有4〜7个环原子的饱和单环杂环化合物的碳原子，包括1个氮环原子或1个氧环原子; 并且任选被取代; Q 2是酸性引导基团，独立地为：C 1-8亚烷基; 并且任选被取代; 或：Q 2是酸引导基团，并且独立地为：C 5-20亚芳基; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; 或C 1-7亚烷基-C 5 - 亚芳基-C 1-7亚烷基; 并且任选被取代; 和其药学上可接受的盐，溶剂合物，酰胺，酯，醚，化学保护形式及其前药。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内的用途，以抑制HDAC，以及治疗由HDAC，癌症，增殖性病症，牛皮癣等介导的病症。

9. 发明申请

WO2008015269A1 SUBSTITUTED PYRAZOLOPYRIMIDINES, A PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICINE 审中-公开
标题翻译：取代的吡唑并嘧啶，其制备方法及其作为医药的用途
公开(公告)号：WO2008015269A1
公开(公告)日：2008-02-07
申请号：PCT/EP2007/058060
申请日：2007-08-03
申请人： MERZ PHARMA GMBH & CO. KGAA , DANYSZ, Wojciech , DEKUNDY, Andrzej , HECHENBERGER, Mirko , HENRICH, Markus , JATZKE, Claudia , NAGEL, Jens , PARSONS, Christopher Graham Raphael , WEIL, Tanja , FOTINS, Juris , GUTCAITS, Aleksandra , KALVINSH, Ivars , ZEMRIBO, Ronalds , KAUSS, Valerjans
发明人： DANYSZ, Wojciech , DEKUNDY, Andrzej , HECHENBERGER, Mirko , HENRICH, Markus , JATZKE, Claudia , NAGEL, Jens , PARSONS, Christopher Graham Raphael , WEIL, Tanja , FOTINS, Juris , GUTCAITS, Aleksandra , KALVINSH, Ivars , ZEMRIBO, Ronalds , KAUSS, Valerjans
IPC分类号： C07D487/04 , A61K31/519 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00
摘要： Substituted pyrazolopyrimidine derivatives of formula (I) wherein Y 1 , Y 2 , Y 3 , Y 4 represent N or C-, whereby at least two of the groups Y 1 to Y 4 denote a carbon atom, R 1 represents chloro or bromo, R 2 to R7 represent e.g. hydrogen, methyl or ethyl; and R 10 and R 11 independent ly represent e.g. hydrogen or C 1 -C 6 alkyl, are potent mGluR5 modulators and are useful for the prevention of acute and chronic neurological disorders.
摘要翻译：式（I）的取代的吡唑并嘧啶衍生物，其中Y 1，Y 2，Y 3，Y 4，或以上代表N 或C-，其中Y 1至Y 4中的至少两个表示碳原子，R 1表示氯或溴，R R 7代表例如氢，甲基或乙基; 且R 10和R 11独立地表示例如，氢或C 1 -C 6烷基是有效的mGluR5调节剂，并且可用于预防急性和慢性神经障碍。

10. 发明申请

WO2007148113A1 METABOTROPIC GLUTAMATE RECEPTOR MODULATORS 审中-公开
标题翻译：代谢谷氨酸受体调节剂
公开(公告)号：WO2007148113A1
公开(公告)日：2007-12-27
申请号：PCT/GB2007/002344
申请日：2007-06-22
申请人： MERZ PHARMA GMBH & CO. KGaA , PARSONS, Christopher, Graham, Raphael , KALVINSH, Ivars , KAULINA, Larisa , KAUSS, Valerjans , ZEMRIBO, Ronalds , DANYSZ, Wojciech , HENRICH, Markus , WEIL, Tanja , ERDMANE, Elina
发明人： PARSONS, Christopher, Graham, Raphael , KALVINSH, Ivars , KAULINA, Larisa , KAUSS, Valerjans , ZEMRIBO, Ronalds , DANYSZ, Wojciech , HENRICH, Markus , WEIL, Tanja , ERDMANE, Elina
IPC分类号： C07D513/04 , A61K31/429 , A61P25/28
CPC分类号： C07D513/04
摘要： The invention relates to imidazothiazole derivatives as well as their pharmaceutically acceptable salts. The invention further relates to a process for the preparation of such compounds. The compounds of the invention are group I mGluR modulators and are therefore useful for the control and prevention of various disorders, including acute and/or chronic neurological disorders.
摘要翻译：本发明涉及咪唑并噻唑衍生物及其药学上可接受的盐。本发明还涉及制备这些化合物的方法。本发明的化合物是I组mGluR调节剂，因此可用于控制和预防各种疾病，包括急性和/或慢性神经障碍。

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