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1. 发明申请

WO2003106402A1 2-NAPHTAMIDE DERIVATIVES 审中-公开
公开(公告)号：WO2003106402A1
公开(公告)日：2003-12-24
申请号：PCT/EP2003/005705
申请日：2003-05-30
申请人： BAYER AKTIENGESELLSCHAFT , SHIMAZAKI, Makoto , SAKURAI, Osamu , MURATA, Toshiki , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi , MASUDA, Tsutomu , SHINTANI, Takuya , SHIMIZU, Haruka
发明人： SHIMAZAKI, Makoto , SAKURAI, Osamu , MURATA, Toshiki , URBAHNS, Klaus , YAMAMOTO, Noriyuki , YOSHIKAWA, Satoru , UMEDA, Masaomi , TAJIMI, Masaomi , MASUDA, Tsutomu , SHINTANI, Takuya , SHIMIZU, Haruka
IPC分类号： C07C235/34
CPC分类号： C07C235/66
摘要： The present invention relates to 2-naphthamides, which are useful as an active ingredient of pharmaceutical preparations. The 2-naphthamides of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benign prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the disease is also alleviated by treatment with an IP receptor antagonist.
摘要翻译：本发明涉及可用作药物制剂活性成分的2-萘甲酰胺。本发明的2-萘甲酰胺具有IP受体拮抗活性，可用于预防和治疗与IP受体活性相关的疾病。这些疾病包括尿路疾病或病症如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱高反应性，良性前列腺肥大），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压; 血友病和出血; 和炎症，因为该疾病也通过用IP受体拮抗剂治疗而缓解。

2. 发明申请

WO0244153A8 4-6-DIPHENYL PYRIDINE DERIVATIVES AS ANTIINFLAMMATORY AGENTS 审中-公开
标题翻译： 4-6-二苯基吡啶衍生物作为抗炎剂
公开(公告)号：WO0244153A8
公开(公告)日：2002-11-28
申请号：PCT/EP0113338
申请日：2001-11-19
申请人： BAYER AG , MURATA TOSHIKI , SAKAKIBARA SACHIKO , YOSHINO TAKASHI , IKEGAMI YUKA , MASUDA TSUTOMU , SHIMADA MITSUYUKI , SHINTANI TAKUYA , SHIMAZAKI MAKOTO , LOWINGER TIMOTHY B , ZIEGELBAUER KARL B , FUCHIKAMI KINJI , UMEDA MASAOMI , KOMURA HIROSHI , YOSHIDA NAGAHIRO
发明人： MURATA TOSHIKI , SAKAKIBARA SACHIKO , YOSHINO TAKASHI , IKEGAMI YUKA , MASUDA TSUTOMU , SHIMADA MITSUYUKI , SHINTANI TAKUYA , SHIMAZAKI MAKOTO , LOWINGER TIMOTHY B , ZIEGELBAUER KARL B , FUCHIKAMI KINJI , UMEDA MASAOMI , KOMURA HIROSHI , YOSHIDA NAGAHIRO
IPC分类号： A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/496 , A61K31/5365 , A61K31/5377 , A61P1/04 , A61P9/10 , A61P11/02 , A61P11/06 , A61P17/00 , A61P17/04 , A61P17/06 , A61P19/02 , A61P19/06 , A61P21/00 , A61P27/02 , A61P27/14 , A61P29/00 , A61P31/04 , A61P35/00 , A61P37/00 , A61P37/02 , A61P37/06 , A61P37/08 , A61P43/00 , C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/10 , C07D401/12 , C07D405/12 , C07D405/14 , C07D498/04 , A61K31/44
CPC分类号： C07D213/73 , C07D213/80 , C07D213/82 , C07D213/85 , C07D401/10 , C07D401/12 , C07D405/12
摘要： 4-aryl pyrimidine compounds of general formula and salts thereof:wherein X is CH or N; R is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy, etc.; R is hydrogen, halogen, etc.; R is hydrogen, hydroxy, halogen, amino, etc.; R is hydroxy, amino, carboxy, etc. or R and R together form a ring; R is hydrogen, carbamoyl, cyano, carboxy, C1-16 alkoxycarbonyl, etc. and R is amino or C1-16 alkanoylamino or R and R together form a ring. The compounds (I) or the salts thereof have an excellent anti-inflammatory activity and act as inhibitors of IKK- beta and thus inhibit nuclear factor kappa B(NF-KB).
摘要翻译：通式为4-芳基嘧啶化合物及其盐：其中X为CH或N; R 1是氢，卤素，C 1-6烷基，C 1-6烷氧基等; R 2是氢，卤素等; R 3是氢，羟基，卤素，氨基等; R 4是羟基，氨基，羧基等，或者R 3和R 4一起形成环; R 5是氢，氨基甲酰基，氰基，羧基，C 1-6烷氧基羰基等，R 6是氨基或C 1-6烷酰基氨基或R 5和R 6一起形成环。化合物（I）或其盐具有优异的抗炎活性，并且作为IKK-β的抑制剂，从而抑制核因子κB（NF-κB）。

3. 发明申请

WO1995012611A1 ENDOTHELIN RECEPTOR ANTAGONISTS 审中-公开
标题翻译：内皮素受体拮抗剂
公开(公告)号：WO1995012611A1
公开(公告)日：1995-05-11
申请号：PCT/EP1994003418
申请日：1994-10-17
申请人： JAPAT LTD. , CIBA-GEIGY JAPAN LIMITED , SAIKA, Hideyuki , MURATA, Toshiki , PITTERNA, Thomas , FRÜH, Thomas , SVENSSON, Lene, D. , URADE, Yoshihiro , YAMAMURA, Takaki , OKADA, Toshikazu
发明人： JAPAT LTD. , CIBA-GEIGY JAPAN LIMITED
IPC分类号： C07K05/065
CPC分类号： C07D401/06 , A61K38/00 , C07D209/20 , C07D209/26 , C07K5/0205 , C07K5/06026 , C07K5/06034 , C07K5/06078 , C07K5/06165
摘要： The present invention provides novel compounds represented by general formula (I) wherein R1 is a straight or branched lower alkyl, a cycloalkyl-lower alkyl, an aryl-lower alkyl, a cycloalkyl, an aryl, an aryl-cycloalkyl, lower alkoxy, an aryloxy, or a heteroaryl; R2 is hydrogen, a straight or branched lower alkyl, a cycloakyl, or a cycloalkyl-lower alkyl; R3 and R3' are each the same or different and each is hydrogen atom, a straight or branched lower alkyl, a cycloalkyl, an aryl-lower alkyl, an aryl, or a heteroaryl; or R3 and R3' together form a ring structure; R3'' is hydrogen, lower alkyl or an aryl; or R2 and R3'' together form a lower alkylene group -(CH2)n- wherein n is an integer of 1, 2 or 3; or R2 and R3'' together form a group represented by the formula: -(CH2)p-Ar- or -Ar-(CH2)p-, respectively, wherein p is zero or an integer of 1 or 2, and Ar is an arylene or heteroarylene; C(=X) is C(=O), C(=S), C(=NH), C(=N-lower alkyl); C=NH-OH, or CH2; Y is a direct bond, -NH-, a lower alkyl-N=, an oxygen atom, or methylene; or C(=X) is CHOH and Y is a direct bond or methylene; R4 is -(CH2)s-Ar' wherein s is zero or an integer of 1, 2 or 3; and Ar' is an aryl, or heteroaryl; and R5 is carboxy, substituted or unsubstituted carboxamide, PO(OH)2, tetrazole, CH2OH, CN, or hydrogen; and salts thereof.
摘要翻译：本发明提供由通式（I）表示的新化合物，其中R 1是直链或支链的低级烷基，环烷基 - 低级烷基，芳基 - 低级烷基，环烷基，芳基，芳基 - 环烷基，低级烷氧基，芳氧基或杂芳基; R2是氢，直链或支链低级烷基，环烷基或环烷基 - 低级烷基; R 3和R 3'各自相同或不同，各自为氢原子，直链或支链低级烷基，环烷基，芳基 - 低级烷基，芳基或杂芳基; 或R3和R3'一起形成环结构; R3“是氢，低级烷基或芳基; 或R 2和R 3“一起形成低级亚烷基 - （CH 2）n - ，其中n是1,2或3的整数; 或者R 2和R 3“一起分别由下式表示的基团： - （CH 2）p -Ar-或-Ar-（CH 2）p - ，其中p为0或1或2的整数，Ar为亚芳基或亚杂芳基; C（= X）是C（= O），C（= S），C（= NH），C（= N-低级烷基） C = NH-OH或CH 2; Y是直接键，-NH-，低级烷基-N =，氧原子或亚甲基; 或C（= X）为CHOH，Y为直接键或亚甲基; R4是 - （CH2）s-Ar'，其中s是0或1,2或3的整数; 和Ar'是芳基或杂芳基; 和R 5是羧基，取代或未取代的羧酰胺，PO（OH）2，四唑，CH 2 OH，CN或氢; 及其盐。

4. 发明申请

WO2004043926A1 PHENYL OR HETEROARYL AMINO ALKANE DERIVATIVES AS IP RECEPTOR ANTAGONIST 审中-公开
标题翻译：作为IP受体拮抗剂的苯基或异辛烯氨基酸衍生物
公开(公告)号：WO2004043926A1
公开(公告)日：2004-05-27
申请号：PCT/EP2003/011976
申请日：2003-10-29
申请人： BAYER HEALTHCARE AG , MURATA, Toshiki , UMEDA, Masaomi , YOSHIKAWA, Satoru , URBAHNS, Klaus , GUPTA, Jang , SAKURAI, Osamu
发明人： MURATA, Toshiki , UMEDA, Masaomi , YOSHIKAWA, Satoru , URBAHNS, Klaus , GUPTA, Jang , SAKURAI, Osamu
IPC分类号： C07D213/64
CPC分类号： C07D213/64 , C07C229/36 , C07D213/74 , C07D231/38 , C07D239/42 , C07D241/20 , C07D261/14 , C07D277/42 , C07D401/04 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/10
摘要： The present invention relates to a phenyl or heteroaryl amino alkane derivatives which are useful as an active ingredient of pharmaceutical preparations. The phenyl or heteroaryl amino alkanes of the present invention have IP receptor antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with IP receptor antagonistic activity. Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity. The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension; hemophilia and hemorrhage; and inflammation, since the diseases also is alleviated by treatment with an IP receptor antagonist.
摘要翻译：本发明涉及可用作药物制剂活性成分的苯基或杂芳基氨基烷烃衍生物。本发明的苯基或杂芳基氨基烷烃具有IP受体拮抗活性，可用于预防和治疗与IP受体拮抗活性相关的疾病。这些疾病包括泌尿系统疾病或紊乱，如下：膀胱出口阻塞，膀胱过度活动，尿失禁，逼尿肌反射反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱反应过度，前列腺肥大），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合征，前列腺痛，膀胱炎或自发性膀胱过敏。本发明的化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压; 血友病和出血; 和炎症，因为这些疾病也通过用IP受体拮抗剂治疗而缓解。

5. 发明申请

WO2004029055A1 FUSED AZOLE-PYRIMIDINE DERIVATIVES 审中-公开
标题翻译：熔融的偶氮吡啶衍生物
公开(公告)号：WO2004029055A1
公开(公告)日：2004-04-08
申请号：PCT/EP2003/010377
申请日：2003-09-18
申请人： BAYER HEALTHCARE AG , SHIMADA, Mitsuyuki , MURATA, Toshiki , FUCHIKAMI, Kinji , TSUJISHITA, Hideki , OMORI, Naoki , KATO, Issei , MIURA, Mami , URBAHNS, Klaus , GANTNER, Florian , BACON, Kevin
发明人： SHIMADA, Mitsuyuki , MURATA, Toshiki , FUCHIKAMI, Kinji , TSUJISHITA, Hideki , OMORI, Naoki , KATO, Issei , MIURA, Mami , URBAHNS, Klaus , GANTNER, Florian , BACON, Kevin
IPC分类号： C07D487/04
CPC分类号： C07D471/14 , C07D487/04
摘要： The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (P13K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with P13K and particularly with P13K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to P13K activity in a human or animal subject.
摘要翻译：本发明涉及霍夫唑唑吡啶衍生物，其制备方法和含有它们的药物制剂。本发明的稠合唑类嘧啶衍生物对磷脂酰肌醇-3-激酶（P13K）抑制的效力显着增强，特别是PI3K-γ抑制作用，可用于预防和治疗与P13K相关的疾病，特别是P13K-γ活性。更具体地说，本发明的唑类衍生物可用于治疗和预防以下疾病：炎性和免疫调节性疾病，如哮喘，特应性皮炎，鼻炎，过敏性疾病，慢性阻塞性肺病（COPD），脓毒性休克，关节疾病，自身免疫性疾病如类风湿性关节炎，格雷夫斯病，癌症，心肌收缩性疾病，心力衰竭，血栓栓塞，缺血和动脉粥样硬化。本发明的化合物还可用于肺动脉高压，肾衰竭，心脏肥大，以及神经变性疾病如帕金森病，阿尔茨海默病，糖尿病和局灶性缺血，因为这些疾病还涉及人或动物中的P13K活性学科。

6. 发明申请

WO2003076447A1 AN OPTICALLY ACITVE PYRIDINE DERIVATIVE AND A MEDICAMENT CONTAINING THE SAME 审中-公开
标题翻译：光学诱导吡啶衍生物和含有它的药物
公开(公告)号：WO2003076447A1
公开(公告)日：2003-09-18
申请号：PCT/EP2003/002169
申请日：2003-03-03
申请人： BAYER AKTIENGESELLSCHAFT , MURATA, Toshiki , SASAKI, Sachiko , YOSHINO, Takashi , SATO, Hiroki , KORIYAMA, Yuji , NUNAMI, Noriko , YAMAUCHI, Megumi , FUKUSHIMA, Keiko , GROSSER, Rolf , FUCHIKAMI, Kinji , BACON, Kevin , LOWINGER, Timothy
发明人： MURATA, Toshiki , SASAKI, Sachiko , YOSHINO, Takashi , SATO, Hiroki , KORIYAMA, Yuji , NUNAMI, Noriko , YAMAUCHI, Megumi , FUKUSHIMA, Keiko , GROSSER, Rolf , FUCHIKAMI, Kinji , BACON, Kevin , LOWINGER, Timothy
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： An optically active (-)-7-[2-(cyclopropylmethoxy)-6-hydroxyphenyl]-5-[(3S)-3-piperidinyl]-1,4-dihydro-2H-pyrido [2,3-d][1,3]oxazin-2-one of the formula (I) or salt thereof. The compound has an excellent anti-inflammatory activity, and other biological activity.
摘要翻译：光学活性（ - ） - 7- [2-（环丙基甲氧基）-6-羟基苯基] -5 - [（3S）-3-哌啶基] -1,4-二氢-2H-吡啶并[2,3-d] 1,3]恶嗪-2-酮或其盐。该化合物具有优异的抗炎活性和其他生物活性。

7. 发明申请

WO2003022277A1 ARYLSULFONAMIDE DERIVATIVES FOR USE AS CCR3 ANTAGONISTS IN THE TREATMENT OF INFLAMMATORY AND IMMUNOLOGICAL DISORDERS 审中-公开
标题翻译：用于治疗炎症和免疫疾病的CCR3拮抗剂的磺酰苯胺衍生物
公开(公告)号：WO2003022277A1
公开(公告)日：2003-03-20
申请号：PCT/EP2002/009873
申请日：2002-09-04
申请人： BAYER AKTIENGESELLSCHAFT , LI, Yingfu , WATANABE, Akihiko , LOWINGER, Timothy, B. , BACON, Kevin , KAWAMURA, Norihiro , SHINTANI, Takuya , KIKUCHI, Tetsuo , MORIWAKI, Toshiya , URBAHNS, Klaus , FUKUSHIMA, Keiko , NUNAMI, Noriko , YOSHINO, Takashi , MURATA, Toshiki , YAMAUCHI, Megumi , YOSHINO, Hiroko
发明人： LI, Yingfu , WATANABE, Akihiko , LOWINGER, Timothy, B. , BACON, Kevin , KAWAMURA, Norihiro , SHINTANI, Takuya , KIKUCHI, Tetsuo , MORIWAKI, Toshiya , URBAHNS, Klaus , FUKUSHIMA, Keiko , NUNAMI, Noriko , YOSHINO, Takashi , MURATA, Toshiki , YAMAUCHI, Megumi , YOSHINO, Hiroko
IPC分类号： A61K31/445
CPC分类号： C07D213/70 , C07C311/29 , C07C323/67 , C07D207/14 , C07D207/48 , C07D209/08 , C07D211/28 , C07D211/58 , C07D211/96 , C07D213/65 , C07D213/71 , C07D213/75 , C07D213/76 , C07D213/80 , C07D241/04 , C07D241/06 , C07D243/08 , C07D257/04 , C07D295/088 , C07D295/13 , C07D295/194 , C07D295/26 , C07D307/14 , C07D333/38 , C07D471/04 , C07D487/04 , C07D487/08
摘要： The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.
摘要翻译：本发明涉及可用作药物制剂活性成分的磺酰胺衍生物。本发明的磺酰胺衍生物具有CCR3（CC型趋化因子受体）拮抗活性，可用于预防和治疗与CCR3活性有关的疾病，特别是用于治疗哮喘，特应性皮炎，过敏性鼻炎等炎症 /免疫学障碍。

8. 发明申请

WO1995026360A1 ANTAGONISTS OF ENDOTHELIN RECEPTORS 审中-公开
标题翻译：内皮素受体拮抗剂
公开(公告)号：WO1995026360A1
公开(公告)日：1995-10-05
申请号：PCT/EP1995001013
申请日：1995-03-17
申请人： JAPAT LTD. , CIBA-GEIGY JAPAN LIMITED , FRÜH, Thomas , PITTERNA, Thomas , MURATA, Toshiki , SVENSSON, Lene, D. , YUUMOTO, Yoko , SAKAKI, Junichi
发明人： JAPAT LTD. , CIBA-GEIGY JAPAN LIMITED
IPC分类号： C07K05/065
CPC分类号： C07K5/06078 , A61K38/00 , C07D209/20 , C07K5/06139
摘要： The present invention provides novel compounds having pharmacological properties represented by general formula (I) wherein Ar represents a direct bond or arylene; processes for the manufacture, pharmaceutical compositions and the use of the compounds of formula (I) ans salts thereof.
摘要翻译：本发明提供具有由通式（I）表示的药理学性质的新化合物，其中Ar表示直接键或亚芳基; 制造方法，药物组合物和式（I）化合物及其盐的用途。

9. 发明申请

WO2004069805A1 BIS(HETERO)ARYL CARBOXAMIDE DERIVATIVES FOR USE AS PGI2 ANTAGONISTS 审中-公开
标题翻译：用作PGI2拮抗剂的BIS（HETERO）ARYL CARBOXAMIDE DERIVATIVES
公开(公告)号：WO2004069805A1
公开(公告)日：2004-08-19
申请号：PCT/EP2004/000711
申请日：2004-01-28
申请人： BAYER HEALTHCARE AG , MURATA, Toshiki , SHINTANI, Takuya , UMEDA, Masaomi , LINO, Takashi , MORIWAKI, Toshiya
发明人： MURATA, Toshiki , SHINTANI, Takuya , UMEDA, Masaomi , LINO, Takashi , MORIWAKI, Toshiya
IPC分类号： C07D231/14
CPC分类号： C07D207/325 , C07D211/14 , C07D213/64 , C07D213/82 , C07D231/12 , C07D231/14 , C07D239/34 , C07D261/18 , C07D333/38
摘要： The present invention relates to aryl or heteroaryl amido alkane derivatives of formula (I) wherein R 6 represents carboxy or tetrazolyl, which are useful as an active ingredient of pharmaceutical preparations. The aryl or heteroaryl amido alkanes of the present invention have PGI2 antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with PGI2 activity.Such diseases include urological diseases or disorder as follows: bladder outlet obstruction, overactive bladder, urinary incontinence, detrusor hyper-reflexia, detrusor instability, reduced bladder capacity, frequency of micturition, urge incontinence, stress incontinence, bladder hyperreactivity, benighn prostatic hypertrophy (BPH), prostatitis, urinary frequency, nocturia, urinary urgency, pelvic hypersensitivity, urethritis, pelvic pain syndrome, prostatodynia, cystitis, or idiophatic bladder hypersensitivity.The compounds of the present invention are also useful for treatment of pain including, but not limited to inflammatory pain, neuropathic pain, acute pain, chronic pain, dental pain, premenstrual pain, visceral pain, headaches, and the like; hypotension;hemophilia and hemorrhage; and inflammation, since the diseases also relate to PGI2.
摘要翻译：本发明涉及式（I）的芳基或杂芳基酰氨基烷烃衍生物，其中R 6表示羧基或四唑基，其可用作药物制剂的活性成分。本发明的芳基或杂芳基酰氨基烷烃具有PGI 2拮抗活性，可用于预防和治疗与PGI2活性相关的疾病。这些疾病包括泌尿系统疾病或病症如下：膀胱出口阻塞，膀胱过度活动症，尿失禁，逼尿肌超反射，逼尿肌不稳定，膀胱容量减少，排尿频率，急迫性尿失禁，压力性尿失禁，膀胱过敏反应，前列腺肥大（BPH），前列腺炎，尿频，夜尿症，尿急，盆腔超敏反应，尿道炎，盆腔疼痛综合症，前列腺痛，膀胱炎或自发性膀胱过敏反应。本发明化合物还可用于治疗疼痛，包括但不限于炎性疼痛，神经性疼痛，急性疼痛，慢性疼痛，牙痛，经前痛，内脏痛，头痛等; 低血压;血友病和出血; 和炎症，因为这些疾病也与PGI2有关。

10. 发明申请

WO1997011960A1 ANTAGONISTS OF ENDOTHELIN RECEPTORS 审中-公开
标题翻译：内皮素受体拮抗剂
公开(公告)号：WO1997011960A1
公开(公告)日：1997-04-03
申请号：PCT/EP1996004063
申请日：1996-09-17
申请人： JAPAT LTD. , NOVARTIS AG , CIBA-GEIGY JAPAN LIMITED , SAKAKI, Junichi , MURATA, Toshiki , YUUMOTO, Yoko , NAKAMURA, Ikushi , OKADA, Toshikazu
发明人： JAPAT LTD. , NOVARTIS AG , CIBA-GEIGY JAPAN LIMITED
IPC分类号： C07K05/078
CPC分类号： C07K5/06139 , A61K38/00
摘要： The present invention provides novel compounds represented by general formula (I), wherein (i) R1 represents 1,2,4-triazol-1-yl, R2 represents methyl or hydroxy, R3 represents methyl or hydroxy, and the asterix means that the chiral carbon atom to which said asterix is attached has the (D) or (D,L) configuration, or (ii) R1 represents isoxazol-5-yl, R2 is methyl, R3 is methyl, and the asterix means that the chiral carbon atom to which said asterix is attached has the (D) configuration; and salts thereof; processes for the manufacture, pharmaceutical compositions and the use of the compounds of formula (I) and salts thereof.
摘要翻译：本发明提供由通式（I）表示的新化合物，其中（i）R 1表示1,2,4-三唑-1-基，R 2表示甲基或羟基，R 3表示甲基或羟基，而星号表示所述星状连接的手性碳原子具有（D）或（D，L）构型，或（ii）R 1表示异唑-5-基，R 2为甲基，R 3为甲基，并且所述星号表示手性碳所述星座所附着的原子具有（D）构型; 及其盐; 制备方法，药物组合物和式（I）化合物及其盐的用途。

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