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1. 发明申请

WO2005023241A1 THE USE OF FUMARIC ACID DERIVATIVES FOR TREATING CARDIAC INSUFFICIENCY, AND ASTHMA 审中-公开
标题翻译：用于治疗心脏缺血症的乳酸衍生物的使用和ASTHMA
公开(公告)号：WO2005023241A1
公开(公告)日：2005-03-17
申请号：PCT/EP2004/009835
申请日：2004-09-03
申请人： FUMAPHARM AG , JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter , ZAUGG, Christian , TAMM, Michael
发明人： JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter , ZAUGG, Christian , TAMM, Michael
IPC分类号： A61K31/231
CPC分类号： A61K31/225 , A61K31/197 , A61K31/231 , A61K31/573 , A61K2300/00
摘要： According to a first aspect the invention relates to the use of fumaric acid derivatives selected from the group consisting of dialkyl fumarates, monoalkyl hydrogen fumarates, fumaric acid monoalkyl ester salts, fumaric acid monoamides, monoamido fumaric acid salts, fumaric acid diamides, monoalkyl monoamido fumarates, carbocyclic and oxacarbocyclic oligomers of these compounds and mixtures thereof for preparing a drug for the treatment or prevention of cardiac insufficiency, in particular left ventricular insufficiency, myocardial infarction and angina pectoris. According to a second aspect the invention relates to the use of fumaric acid derivatives, selected from the group consisting of dialkyl fumarates, monoalkyl hydrogen fumarates, fumaric acid monoaklyl ester salts, fumaric acid monoamido fumaric acid salts, fumaric acid diamides, monoalkyl monoamido fumarates, carbocyclic and oxacarbocyclic oligomers of these compounds and mixtures thereof for preparing a drug for the treatment of asthma and chronic obstructive pulmonary diseases, especially asthma caused by allergies, infections, analgesics, job conditions or physical effort, mixed forms of asthma, or asthma cardiale.
摘要翻译：根据第一方面，本发明涉及富马酸衍生物的用途，所述富马酸衍生物选自富马酸二烷基酯，富马酸单烷基酯，富马酸单烷基酯盐，富马酸单酰胺，单酰氨基富马酸盐，富马酸二酰胺，单烷基单酰氨基富马酸盐，这些化合物的碳环和氧杂环低聚物及其混合物，用于制备治疗或预防心功能不全，特别是左心室功能不全，心肌梗塞和心绞痛的药物。根据第二方面，本发明涉及富马酸衍生物的用途，所述富马酸衍生物选自富马酸二烷基酯，富马酸单烷基酯，富马酸单烯基酯盐，富马酸单酰氨基富马酸盐，富马酸二酰胺，单烷基单酰氨基富马酸盐，这些化合物的碳环和恶唑环低聚物及其混合物用于制备用于治疗哮喘和慢性阻塞性肺疾病的药物，特别是由过敏，感染，止痛剂，作业条件或身体力量引起的哮喘，混合形式的哮喘或哮喘心脏病。

2. 发明申请

WO2003087174A3 CARBOCYCLISCHE UND OXACARBOCYCLISCHE FUMARSÄURE-OLIGOMERE 审中-公开
公开(公告)号：WO2003087174A3
公开(公告)日：2003-10-23
申请号：PCT/EP2003/003498
申请日：2003-04-03
申请人： FUMAPHARM AG , JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter
发明人： JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter
IPC分类号： C07C69/74
摘要： Die vorliegende Erfindung betrifft bestimmte carbocyclische und oxacarbocyclische Fumasäure-Oligomere sowie die Verwendung derselbern zur Herstellung eines Arzneimittels und diese Verbindungen enthaltende Arzneimittel.

3. 发明申请

WO03087174A2 CARBOCYCLIC AND OXACARBOCYCLIC FUMARIC ACID OLIGOMERS 审中-公开
标题翻译：碳环和oxacarbocyclic富马酸低聚物
公开(公告)号：WO03087174A2
公开(公告)日：2003-10-23
申请号：PCT/EP0303498
申请日：2003-04-03
申请人： FUMAPHARM AG , JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER
发明人： JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER
IPC分类号： A61K9/22 , A61K31/225 , A61K31/335 , A61P1/04 , A61P1/16 , A61P3/00 , A61P3/10 , A61P7/06 , A61P9/00 , A61P9/10 , A61P13/10 , A61P13/12 , A61P17/00 , A61P19/00 , A61P19/02 , A61P19/06 , A61P21/00 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/12 , A61P31/18 , A61P35/00 , A61P35/02 , A61P37/00 , A61P37/02 , A61P43/00 , C07C61/04 , C07C61/08 , C07C69/74 , C07C69/75 , C07D321/12 , C07D323/00 , C08F22/00
CPC分类号： C07D321/12 , C07D323/00
摘要： The invention relates to defined carbocyclic and oxacarbocyclic fumaric acid oligomers. The invention also relates to the use thereof for producing a drug and to drugs comprising the inventive compounds.
摘要翻译：本发明涉及某些碳环和oxacarbocyclic低聚物Fumasäure和使用DERS Elbern用于制备药物和含有这些化合物的药物。

4. 发明申请

WO2002055063A3 FUMARSÄUREAMIDE 审中-公开
公开(公告)号：WO2002055063A3
公开(公告)日：2002-07-18
申请号：PCT/EP2002/000107
申请日：2002-01-08
申请人： FUMAPHARM AG , JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter
发明人： JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter
IPC分类号： A61K31/197
摘要： Die Erfindung betrifft die Verwendung von Fumarsäureamiden der allgemeinen Formel (I) in der R 1 für OR 3 oder für einen über eine Amidbindung gebundenen D- oder L- Aminosäurerest -NH-CHR 4 -COOH steht, worin R 3 Wasserstoff, ein geradkettiger oder verzweigter, gegebenenfalls substituierter C 1-21 -Alkylrest, ein Phenylrest oder C 6-10 -Aralkylrest und R 4 eine Seitenkette einer natürlichen oder synthetischen Aminosäure ist, und R 2 für einen über eine Amidbindung gebundenen D- oder L-Aminosäurerest -NH-CHR 5 -COOH oder einen über eine Amidbindung gebundenen Peptidrest mit 2 bis 100 Aminosäuren steht, worin R 5 eine Seitenkette einer natürlichen oder synthetischen Aminosäure ist, zur Herstellung eines Arzneimittels (1) zur Therapie einer Autoimmunerkrankung, (2) zur Verwendung in der Transplantationsmedizin, (3) zur Therapie mitochondrialer Erkrankungen, ausgewählt aus der Gruppe bestehend aus dem Parkinson-Syndrom, der Alzheimer-Krankheit, der Chorea-Huntington-Krankheit, der Retinopathia pigmentosa oder mitochondrialen Enzephalomyopathien, sowie (4) zur Therapie von NFkappass vermittelten Erkrankungen.

5. 发明申请

WO0012072A3 THE USE OF FUMARIC ACID DERIVATIVES IN TRANSPLANT MEDICINE 审中-公开
标题翻译：在移植医学富马酸衍生物的用途
公开(公告)号：WO0012072A3
公开(公告)日：2000-05-04
申请号：PCT/EP9906110
申请日：1999-08-20
申请人： FUMAPHARM AG , JOSHI RAJENDRA KUMAR , STREBEL HANS PETER
发明人： JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER
IPC分类号： A61K9/16 , A61K9/26 , A61K9/48 , A61K31/19 , A61K31/225 , A61K31/315 , A61K38/00 , A61K45/00 , A61P37/06 , A61P41/00 , A61K38/13
CPC分类号： A61K31/225 , A61K2300/00
摘要： The invention relates to the use of certain fumaric acid monoalkyl esters in the form of salts or a free acid, alone or combined with a dialkyl fumarate only, for producing pharmaceutical preparations for use in transplant medicine, especially for treating, mitigating or suppressing host-versus-graft reactions. The fumaric acid monoalkyl esters can also be used for this purpose in conjunction with the preparations traditionally used in transplant medicine and with immunosupressants such as cyclosporins in particular.
摘要翻译：本发明涉及使用某些富马酸单烷基酯盐或游离酸，单独或与富马酸二烷基酯用于制备药物制剂用于移植医学中的用途，特别是用于治疗，缓解，或宿主抗移植物反应的抑制组合。富马酸单烷基酯可以是用于该目的，在与常规制剂移植和免疫抑制药物如环孢菌素特定组合使用。

6. 发明申请

WO0023068A2 FUMARIC ACID MICROTABLETS 审中-公开
标题翻译：延胡索MICRO片剂
公开(公告)号：WO0023068A2
公开(公告)日：2000-04-27
申请号：PCT/EP9907568
申请日：1999-10-08
申请人： FUMAPHARM AG , JOSHI RAJENDRA KUMAR , STREBEL HANS PETER
发明人： JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER
IPC分类号： A61J3/06 , A61J3/07 , A61K9/20 , A61K9/28 , A61K9/48 , A61K9/52 , A61K31/22 , A61K31/225 , A61K31/28 , A61K31/295 , A61P1/00 , A61P1/04 , A61P17/00 , A61P17/06 , A61P19/02 , A61P37/00 , A61K9/16 , A61K9/50
CPC分类号： A61K31/22 , A61K9/2054 , A61K9/2059 , A61K9/2866 , A61K9/4858 , A61K2300/00
摘要： The invention relates to the use of one or more fumaric acid monoalkylester salts of general formula (I), optionally mixed with dialkyl fumarate of formula (II), wherein A represents a divalent cation of the series of Ca, Mg, Zn or Fe or a monovalent cation from the series Li, Na or K and n represents 1 or 2 depending on the type of cation, and optionally usual pharmaceutical adjuvants and carriers for the production of a pharmaceutical preparation in the form of microtablets or micropellets for the treatment of psoriatic arthritis, neurodermitis, psoriasis and Crohn's Enteritis regionalis.
摘要翻译：本发明涉及（I）通式中的一个或多个Fumarsäuremonoalkylestersalze，任选混合有式富马酸二烷基酯（II），其中A为Zn，从系列从栗自由Ca，Mg或Fe或一价阳离子的二价阳离子， Na或K，且n是1或2取决于阳离子的类型，以及，任选地，常规的药物赋形剂和载体用于制备微型片剂或微颗粒的形式用于治疗牛皮癣性关节炎，神经性皮炎，银屑病和肠炎的药物制剂regionalis克罗恩。

7. 发明申请

WO2006122652A3 THIOSUCCINIC ACID DERIVATIVES AND THE USE THEREOF 审中-公开
标题翻译：硫代酸衍生物及其用途
公开(公告)号：WO2006122652A3
公开(公告)日：2007-04-05
申请号：PCT/EP2006004134
申请日：2006-05-03
申请人： FUMAPHARM AG , JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER , ULRICHOVA JITKA , SCHMIDT THOMAS J
发明人： JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER , ULRICHOVA JITKA , SCHMIDT THOMAS J
IPC分类号： C07C323/58 , A61K31/198 , A61K38/10 , A61K38/16 , A61P9/04 , A61P9/10 , A61P11/06 , A61P25/28 , C07K7/08 , C07K14/00
CPC分类号： C07K14/001 , C07C323/58 , C07K5/0215
摘要： The present invention relates to compounds of the Formula (I), wherein X 1 and X 2 independently represent O, NH or S; R 1 and R 2 are independently selected from the group consisting of a C1-C30 hydrocarbyl group, an armino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue X 1 or X 2 in this case being NH, and hydrogen, both radicals R 1 and R 2 preferably not being H; and R 3 is a residue selected from group consisting of -S-R 6 , wherein R 6 is a C1-C30 hydrocarbyl group, at least one of R 1 and R 2 not being H when X 1 and X 2 are oxygen, -S-CH 2 -CH(NH 2 )(COOH) (cysteine-S-yl), a homologue or derivative (e.g. N-acetyl cysteine-S-yl) thereof, a peptide having up to 200 amino acids which contains at least one amino acid radical with a thiol group, preferably a cysteine radical, and is bonded via the thio sulfur, preferably via the cysteine sulfur (peptide-S-yl), coenzyme A which is bonded via a thiol group or fragments thereof, acyl carrier protein bonded via a thiol group, and dihydrolipoic acid bonded via a thiol group; and pharmaceutically acceptable salts thereof. The present invention also relates to the use of these compounds for preparing a drug, drugs containing the same and their use for the therapy of diseases such as autoimmune disease, NF-kappaB mediated diseases, psoriasis, psoriatic arthritis, neurodermitis, enteris regionalis Crohn, cardiac insufficiency, chronic obstructive pulmonary diseases and asthma and in transplantation medicine.
摘要翻译：本发明涉及式（I）化合物，其中X 1和X 2独立地代表O，NH或S; R 1和R 2独立地选自C 1 -C 30烃基，通过酰胺键键合的氨基酸或通过酰胺键键合的肽每个具有多达200个氨基酸，在这种情况下，共轭残基X 1或X 2 2是NH，和氢，基团R 1，并且R 2优选不为H; 和R 3是选自-SR 6 S的残基，其中R 6是C 1 -C 30烃基，至少一个的R 1和R 2不是H，而X 1和X 2都是氧，-S-CH （NH 2）（COOH）（半胱氨酸-S-基），其同系物或衍生物（例如N-乙酰半胱氨酸-S-基），一具有至多200个氨基酸的肽，其含有至少一个具有硫醇基的氨基酸基团，优选半胱氨酸基团，并且优选通过硫代硫，优选通过半胱氨酸硫（肽-S-基），辅酶A 通过硫醇基或其片段键合，通过硫醇基键合的酰基载体蛋白和通过硫醇基键合的二氢硫辛酸; 及其药学上可接受的盐。本发明还涉及这些化合物在制备药物中的用途，含有该药物的药物及其用于治疗疾病如自身免疫性疾病，NF-κB介导的疾病，牛皮癣，牛皮癣关节炎，神经性皮炎，局部肠炎克罗恩病，心功能不全，慢性阻塞性肺疾病和哮喘和移植医学。

8. 发明申请

WO2006122652A2 THIOSUCCINIC ACID DERIVATIVES AND THE USE THEREOF 审中-公开
标题翻译：硫代酸衍生物及其用途
公开(公告)号：WO2006122652A2
公开(公告)日：2006-11-23
申请号：PCT/EP2006/004134
申请日：2006-05-03
申请人： FUMAPHARM AG , JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter , ULRICHOVÁ, Jitka , SCHMIDT, Thomas, J.
发明人： JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter , ULRICHOVÁ, Jitka , SCHMIDT, Thomas, J.
IPC分类号： C07C323/58 , C07K7/08 , C07K14/00 , A61K31/198
CPC分类号： C07K14/001 , C07C323/58 , C07K5/0215
摘要： The present invention relates to compounds of the formula (I) wherein X 1 and X 2 independently represent O, NH or S, R 1 and R 2 are independently selected from the group consisting of a C 1 -C 30 hydrocarbyl group, an amino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue X 1 or X 2 in this case being NH, and hydrogen, both radicals R 1 and R 2 preferably not being H, wherein R 3 is a residue selected from group consisting of -S-R 6 , wherein R 6 is a C 1 -C 30 hydrocarbyl group, at least one of R 1 and R 2 not being H when X 1 and X 2 are oxygen, -S-CH 2 -CH(NH 2 )(COOH) (cysteine-S-yl), a homologue or derivative (e.g. N-acetyl cysteine-S-yl) thereof, a peptide having up to 200 amino acids which contains at least one amino acid radical with a thiol group, preferably a cysteine radical, and is bonded via the thio sulfur, preferably via the cysteine sulfur (peptide-S-yl), coenzyme A which is bonded via a thiol troup or fragments thereof, acyl carrier protein bonded via a thiol group, and dihydrolipoic acid bonded via a thiol group, and pharmaceutically acceptable salts thereof. The present invention also relates to the use of these compounds for preparing a drug and drugs containing the same.
摘要翻译：本发明涉及式（I）的化合物，其中X 1和X 2独立地代表O，NH或S，R 1和 R 2 2独立地选自C 1 -C 30烃基，经由酰胺键键合的氨基酸或肽通过各自具有多达200个氨基酸的酰胺键键合，在这种情况下，缀合的残基X 1或X 2 2是NH，和氢，两个基团R _{1＆gt;和R 2优选不是H，其中R 3是选自-SR 6，其中R 6是C 1 -C 30烃基，R 1和R 2中的至少一个，当X 1和X 2都为氧，-S-CH 2 -CH（NH 2）2时，H 2不为H，（COOH）（半胱氨酸-S-基），其同系物或衍生物（例如N-乙酰半胱氨酸-S-基），具有至多200个氨基酸的肽，其含有具有硫醇基，优选半胱氨酸基团的至少一个氨基酸基团，并且优选经由硫硫键合，优选经由半胱氨酸硫（肽-S-基），通过巯基或其片段键合的辅酶A，通过硫醇基键合的酰基载体蛋白和通过硫醇基键合的二氢硫辛酸及其药学上可接受的盐。本发明还涉及这些化合物用于制备药物的用途和含有这些化合物的药物。}

9. 发明申请

WO02055063A2 FUMARIC ACID AMIDES 审中-公开
标题翻译：富马酸酰胺
公开(公告)号：WO02055063A2
公开(公告)日：2002-07-18
申请号：PCT/EP0200107
申请日：2002-01-08
申请人： FUMAPHARM AG , JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER
发明人： JOSHI RAJENDRA KUMAR , STREBEL HANS-PETER
IPC分类号： A61K38/00 , A61K31/00 , A61K31/16 , A61K31/194 , A61K31/198 , A61K31/225 , A61P1/00 , A61P1/04 , A61P1/16 , A61P3/10 , A61P9/00 , A61P9/14 , A61P11/00 , A61P13/12 , A61P17/00 , A61P19/02 , A61P19/06 , A61P25/00 , A61P25/14 , A61P25/16 , A61P25/28 , A61P31/00 , A61P31/04 , A61P31/12 , A61P35/00 , A61P37/02 , C07C235/76 , C07K14/00
CPC分类号： A61K31/198 , A61K31/194 , A61K31/225
摘要： The invention relates to the use of fumaric acid amides of general formula (I) wherein R1 represents OR3 or a D- or L- amino acid radical NH-CHR4-COOH bound by an amide bond, wherein R3 is hydrogen, a straight-chain or branched, optionally substituted C1-21-alkyl radical phenyl radical or a C6-10-aralkyl radical and R4 is a sidechain of a natural or synthetic amino acid, and R2 represents a D- or L- amino acid radical bound by an amide bond or a peptide radical bound by an amide bond having 2-100 amino acids, whereinR5 is a side chain of a natural or synthetic amino acid, in the production of a medicament (1) for therapy of an auto-immune disease, (2) for use in transplantation medicine, (3) for therapy of mitochondrial diseases and (4) for therapy of NfkappaB mediated diseases.
摘要翻译：本发明涉及使用Fumarsäureamiden通式（I）其中R 1表示OR 3或一个通过酰胺键D-或L-氨基酸基-NH-CHR4-COOH其中R3是氢，直链或支链的，任选取代的C1键合 -21 - 烷基，苯基基团或C6-10芳烷基和R 4是一种天然的或合成的氨基酸的侧链，并且R 2一个通过酰胺键的肽残基键合的用于通过酰胺键D-或L-氨基酸残基NH-CHR 5-COOH或粘结具有2至100个氨基酸，其中R 5是一种天然的或合成的氨基酸的侧链，用于制备药物（1），用于自体免疫疾病（2）的用于在用于治疗mmitochondrialer疾病移植医学和（3）与使用的治疗（4），用于治疗的NFκB介导的疾病的。

10. 发明申请

WO2002055067A3 FUMARSÄUREDERIVATE ALS NF-KAPPAB-INHIBITOR 审中-公开
公开(公告)号：WO2002055067A3
公开(公告)日：2002-07-18
申请号：PCT/EP2002/000108
申请日：2002-01-08
申请人： FUMAPHARM AG , JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter , PETZELBAUER, Peter
发明人： JOSHI, Rajendra, Kumar , STREBEL, Hans-Peter , PETZELBAUER, Peter
IPC分类号： A61K31/194
摘要： Die vorliegende Erfindung betrifft die Verwendung eines oder mehrerer Fumarsäurederivate als NF-kappaB-inhibitor. Zur Behandlung von Erkrankungen, wie zum Beispiel die progressive systemische Sklerodermie, die Cutis marmorata, die Behcet-Disease, die Colitis ulcerosa, die Vasculitis, die Osteoarthritis, die Gicht, die Ateriosklerosis, die Reiter's Erkrankung, Encephalitis-Typen, den Endotoxin-Schock. die Pneumonie, die Encephalomyelitis, die Anorexia nervosa, die Hepatitis, die mesangiale Nephritis, das Reperfusionssyndrom, die cytomegalovirale Retinopathie, Adenovirale Erkrankungen wie adenovirale Erkältungserkrankungen, AIDS, Neuralgie, die inflammatorische demyelinisierende Polyneuropathie, die Mononeuropathie multiplex, die Mukoviszidose, Morbus Bechterew, Barett-Oesophagus, EBV-(Epstein-Barr-Virus)-Infection, interstitielle Zystitis, Diabetes mellitus Typ II, die Strahlensensibilisierung maligner Tumore, die Mehrfachresistenz maligner Zellen Krebserkrankungen.

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