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1. 发明申请

US20130267516A1 SUBSTITUTED CYCLOPENTYL-AZINES AS CASR-ACTIVE COMPOUNDS 审中-公开
标题翻译：取代的环己基作为CASR活性化合物
公开(公告)号：US20130267516A1
公开(公告)日：2013-10-10
申请号：US13989440
申请日：2011-11-21
申请人： Kristoffer Månsson , Lars Kristian Albert Blæhr
发明人： Kristoffer Månsson , Lars Kristian Albert Blæhr
IPC分类号： C07D405/12 , C07D213/75 , C07D401/04 , C07D295/125 , C07D239/42
CPC分类号： C07D405/12 , C07D213/61 , C07D213/74 , C07D213/75 , C07D239/38 , C07D239/42 , C07D295/125 , C07D401/04 , C07D401/12 , C07D403/04
摘要： Compounds of general formula I, (formula [I)], their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
摘要翻译：通式I（式[I]]的化合物，它们作为钙受体活性化合物用于预防，治疗或改善生理障碍或与CaSR活性紊乱相关的疾病（例如甲状旁腺机能亢进），包含所述化合物的药物组合物，以及用所述化合物治疗疾病的方法。

2. 发明申请

US20130244995A1 CALCIUM-SENSING RECEPTOR-ACTIVE COMPOUNDS 审中-公开
公开(公告)号：US20130244995A1
公开(公告)日：2013-09-19
申请号：US13989443
申请日：2011-11-21
申请人： Per Vedsø , Lars Kristian Albert Blæhr
发明人： Per Vedsø , Lars Kristian Albert Blæhr
IPC分类号： C07D295/192 , C07D211/58 , C07C237/20 , C07D205/04 , C07D241/08 , C07C317/28
CPC分类号： C07D295/192 , C07C229/46 , C07C235/10 , C07C237/20 , C07C311/05 , C07C311/46 , C07C317/28 , C07C2601/08 , C07D205/04 , C07D211/58 , C07D241/08 , C07D243/08 , C07D317/58
摘要： Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.

3. 发明授权

US08765676B2 Calcium sensing receptor modulating compounds and pharmaceutical use thereof 失效
标题翻译：钙感应受体调节化合物及其药物用途
公开(公告)号：US08765676B2
公开(公告)日：2014-07-01
申请号：US13322514
申请日：2010-05-26
申请人： Bjarne Nørremark , Lars Kristian Albert Blæhr , Anne Eeg Knapp , Kristoffer Månsson
发明人： Bjarne Nørremark , Lars Kristian Albert Blæhr , Anne Eeg Knapp , Kristoffer Månsson
IPC分类号： C07D211/16 , A61K31/33 , A61P19/00 , C07D213/643 , C07D257/04 , C07D265/30 , C07D277/22 , C07D317/62 , A61K38/23 , A61K38/00 , C07K14/585
CPC分类号： C07D211/16 , A61K31/33 , C07D213/643 , C07D257/04 , C07D265/30 , C07D277/22 , C07D317/62 , C07D319/18 , C07D321/10 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要： Calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I (wherein X is CH or N) and pharmaceutical compositions thereof are useful for treating diseases.
摘要翻译：调节取代的式I化合物（其中X为CH或N）的取代环戊烯化合物及其药物组合物可用于治疗疾病的钙感受因受体（CaSR）。

4. 发明申请

US20120122784A1 NOVEL CALCIUM SENSING RECEPTOR MODULATING COMPOUNDS AND PHARMACEUTICAL USE THEREOF 失效
标题翻译：新型钙感受体调节化合物及其药物用途
公开(公告)号：US20120122784A1
公开(公告)日：2012-05-17
申请号：US13322514
申请日：2010-05-26
申请人： Bjarne Nørremark , Lars Kristian Albert Blæhr , Anne Eeg Knapp , Kristoffer Månsson
发明人： Bjarne Nørremark , Lars Kristian Albert Blæhr , Anne Eeg Knapp , Kristoffer Månsson
IPC分类号： A61K38/23 , C07D231/12 , C07D319/18 , C07D307/79 , C07C317/32 , C07D277/28 , C07D215/14 , C07D471/04 , C07D265/36 , C07C317/24 , C07D211/58 , C07D213/64 , C07D257/04 , C07C311/17 , C07D211/46 , C07C235/80 , A61K31/36 , A61K31/415 , A61K31/357 , A61K31/343 , A61K31/145 , A61K31/426 , A61K31/47 , A61K31/437 , A61K31/538 , A61K31/397 , A61P35/00 , A61P9/00 , A61P13/12 , A61P1/00 , A61P25/00 , A61P7/06 , A61P19/08 , A61P19/10 , A61P25/28 , A61P1/12 , A61K31/593 , A61K31/566 , C07D317/58
CPC分类号： C07D211/16 , A61K31/33 , C07D213/643 , C07D257/04 , C07D265/30 , C07D277/22 , C07D317/62 , C07D319/18 , C07D321/10 , C07D401/12 , C07D405/12 , C07D409/12 , C07D471/04
摘要： The invention relates to novel calcium-sensing receptor (CaSR) modulating substituted cyclopentylene compounds represented in formula I and derivatives thereof, to said compounds for use as a medicament, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases with said compounds, and to the use of said compounds in the manufacture of medicaments.
摘要翻译：本发明涉及用于治疗的所述化合物，用于治疗的所述化合物，包含所述化合物的药物组合物的新型钙感受受体（CaSR）调节式I表示的取代的环戊烯化合物及其衍生物，用所述化合物治疗疾病，以及所述化合物在制备药物中的用途。

5. 发明授权

US06784169B2 MMP inhibitors 失效
标题翻译： MMP抑制剂
公开(公告)号：US06784169B2
公开(公告)日：2004-08-31
申请号：US10345304
申请日：2003-01-16
申请人： Mette Knak Christensen , Lars Kristian Albert Blæhr
发明人： Mette Knak Christensen , Lars Kristian Albert Blæhr
IPC分类号： A61K3166
CPC分类号： C07F9/65842 , C07F9/6584
摘要： Novel compounds according to formula I n is 0, 1, 2 or 3; X represents hydroxamic acid (CONHOH), carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R2, R10 and R11 independently represent hydrogen or (C1-8)alkyl, (C2-6)alkenyl, (C3-8)cycloalkyl, aryl(C0-6)alkyl or heteroaryl(C0-6)alkyl, all of which may optionally be substituted; R3 and R4 independently represent hydrogen, hydroxy or alkoxy; provided that if A, A′, Z and R5 are all bonds, and s and t are both 0 (zero), then R6 is different from hydrogen, and that at least one of R3, R4, R10 and R11 is different from hydrogen; or a salt, hydrate or solvate thereof; pharmaceutical compositions comprising said compound; therapeutical methods comprising administering said compounds; and the use of said compounds in the manufacture of medicaments.
摘要翻译：式（I）的新型化合物是0,1,2或3; X代表异羟肟酸（CONHOH），羧酸，膦酸，乙酰硫代甲基或巯基甲基; R2，R10和R11独立地表示氢或（C1-8）烷基，（C2-6）烯基，（C3-8）环烷基，芳基（C0-6）烷基或杂芳基（C0-6）烷基，任选被取代; R3和R4独立地表示氢，羟基或烷氧基; 条件是如果A，A'，Z和R5都是键，并且s和t都是0（零），则R6不同于氢，R3，R4，R10和R11中的至少一个不同于氢 ;或其盐，水合物或溶剂合物; 包含所述化合物的药物组合物; 治疗方法包括施用所述化合物; 以及所述化合物在制备药物中的用途。

6. 发明授权

US06521606B2 Matrix metalloproteinase inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US06521606B2
公开(公告)日：2003-02-18
申请号：US09899017
申请日：2001-07-06
申请人： Morten Dahl Sørensen , Lars Kristian Albert Blæhr , Mette Knak Christensen
发明人： Morten Dahl Sørensen , Lars Kristian Albert Blæhr , Mette Knak Christensen
IPC分类号： A61K3166
CPC分类号： A61K31/675 , C07F9/65842
摘要： A compound of the general formula I wherein Y is O or S; n is 1, 2, 3 or 4; X represents hydroxamic acid, carboxylic acid, phosphonic acid, acetylthiomethyl group or a mercaptomethyl group; R1 is wherein E, when present represents, a bond or optionally substituted methylene or ethylene; s and t are independently 0, 1, 2 or 3; A and A′ independently represent a bond, or a saturated or unsaturated, optionally substituted cyclic or heterocyclic hydrocarbon di- or triradical; Z represents a bond, O, S, C(O), C(O)NR7, NR7C(O) or NR7, wherein R7 is hydrogen, hydroxy, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R5 represents a bond, alkane or alkene diradical, one or more ether diradicals (R—O—R′) or amine diradicals (R—N—R′), wherein R and R′ independently represent alkane or alkene diradicals with a C-content from 0 to 3; R6 represents hydrogen, hydroxy, halogen, cyano, nitro, branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical, unsaturated optionally substituted cyclic or heterocyclic hydrocarbon radical, NR8R9, C(O)NR8R9, C(O)R8, CO(O)R8, S(O)2R9, wherein each R8 and R9 independently represent hydrogen, halogen, a branched or straight, saturated or unsaturated, optionally substituted hydrocarbon radical; R2 represents hydrogen, (C1-8)alkyl, (C2-6)alkenyl, (C3-8)cycloalkyl, aryl(C0-6)alkyl or heteroaryl(C0-6)alkyl; provided that if A, A′, Z and R5 are all bonds, and s and t are both 0 (zero), then R6 is different from hydrogen; or a salt, hydrate or solvate thereof. The compounds are valuable for human and veterinary therapy.
摘要翻译：通式I的化合物，其中Y为O或S; n为1,2,3或4; X为异羟肟酸，羧酸，膦酸，乙酰硫代甲基或巯基甲基; R1为E时，当存在时为键或任选取代的亚甲基或亚乙基; s和t独立地为0,1,2或3; A和A'独立地表示键，或饱和或不饱和的任选取代的环状或杂环烃二取代或杂芳基; Z表示键，O，S，C（O），C（O）NR7，NR7C（O）或NR7，其中R7是氢，羟基，支链或直链，饱和或不饱和的任选取代的烃基; R 5表示键，或二烯基双基，一个或多个醚双基（RO-R'）或胺二基（RN-R'），其中R和R'独立地表示C含量为0至3的烷烃或烯烃双基; R 6表示氢，羟基，卤素，氰基，硝基，支链或直链，饱和或不饱和的，任选取代的氢化物芳基，不饱和的任选取代的环状或杂环烃基，NR 8 R 9，C（O）NR 8 R 9，C（O）R 8，CO（O）R 8，S（O）2 R 9，其中各R 8和R 9分别代表氢，卤素，分支或直链，饱和或不饱和的任选取代的烃基; R 2表示氢，（C 1-8）烷基，（C 2-6）烯基，（C 3-8）环烷基，芳基（C 0-6）烷基或杂芳基 6）烷基;条件是如果A，A'，Z和R5都是键，并且s和t均为0（零），则R6不同于氢;或其盐，水合物或溶剂化物。化合物是有价值的用于人类和兽医治疗。

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