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WO/2001/051125A1 |
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions contai...
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WO/2001/051128A1 |
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions contai...
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WO/2001/028992A2 |
There is provided compounds of formula (I), wherein R?1¿, R?2¿, R?3¿, R?4¿, R?41¿ to R?46¿, A, B and G have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular a...
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WO/2001/018006A1 |
The present invention is directed to macrocyclic compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing th...
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WO/2000/069441A1 |
ET743 is used in the preparation of a medicament for the treatment of the human body for cancer.
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WO/2000/069862A2 |
Methods are provided for preparing a compound with a fused ring structure of formula (XIV) which comprises one or more reactions starting from a 21-cyano compound of formula (XVI) where typically: R?1¿ is an amidomethylene group or an a...
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WO/2000/034278A1 |
Novel triazolo derivatives including the one represented by formula (26), and pharmacologically acceptable salts thereof; and chemokine inhibitors containing the same as the active ingredient. These compounds are useful as remedies for a...
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WO/2000/003722A1 |
Novel thiazolyl peptide antibiotic compounds, including nocathiacin I, II and III, are disclosed. Also, novel microorganism ATCC-202099 is disclosed.
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WO1999051238A9 |
The present invention is directed to several newly prepared semi-synthetic ecteinascidin (Et) species, designated herein as Et 757, Boc-Et 729, Iso-Et 743, Et 875, and Et 1560. The physical properties of these compounds, their preparatio...
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WO/2000/001382A1 |
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions contai...
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WO/2000/001701A1 |
The present invention is directed to peptidomimetic macrocyclic compounds which inhibit prenyl-protein transferase and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions contai...
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WO/1999/064426A1 |
The current invention discloses useful bicyclic and tricyclic amidino derivative compounds represented by Formula (I), pharmaceutical compositions containing these novel compounds, and to their use as nitric oxide synthase inhibitors.
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WO/1999/058125A1 |
The purification and structure elucidation of several products of the metabolism of Et 743 by human cytochrome CYP3A4 have been accomplished. These compounds are abbreviated herein as 'ETM' followed by a numeric value which represents th...
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WO/1998/046080A1 |
Five new nucleophile substituted ecteinascidin (Et) compounds have been isolated from extracts of $i(Ecteinascidia turbinata). These compounds have been purified by chromatographic techniques and their structures and bioactivities have b...
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WO/1998/012198A1 |
The present invention is directed to a synthetic process for the formation of ecteinascidin compounds and related structures, such as the saframycins. In one particularly preferred embodiment, the present invention provides a synthetic r...
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WO/1998/007727A1 |
Compounds having formula (I), wherein R�1? is acyl of formula -C(O)R�2? wherein R�2? is C�1-6? alkyl, C�2-6? alkenyl, C�2-6? alkynyl or aryl; or R�1? is C�2-8? alkenyl or C�2-8? alkynyl, each of which is optionally subs...
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WO/1997/048705A1 |
A series of compounds for blocking calcium activated potassium channels in rat sympathetic neurones and other mammalian cells, and a method for producing them. These compounds with general formulae (I) and (II), where A and B are spacing...
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WO/1996/030377A1 |
Novel macrocyclic compounds are constructed to include large cyclic structures that are interrupted by at least one ring sytem. Each interrupting ring system includes two bridgehead atoms. Bridgehead atoms are bonded to one or more bridg...
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WO/1995/029894A1 |
The invention relates to antimicrobial 5-(N-heterosubstituted amino) quinolone compounds having a structure according to formula (I) or (II), wherein: (1) R1, R2, R3, R9 and R10 form any of a variety of quinolone and related heterocyclic...
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WO/1992/019613A2 |
Therapeutical compositions based on compounds selected from formulas (I) and (Ia), wherein X is selected from =S, =O, =SO, =N-OH, =N-R5, =N-NH-CONH2, =N-NH-CSNH2 and (a); A is selected from group (b), a group having formula (c), a C=O gr...
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WO/1992/009607A1 |
Ecteinascidins 722 and 736 (Et's 722 and 736) have been isolated from the Caribbean tunicate Ecteinascidia turbinata and their structures have been assigned as tetrahydro-beta-carboline-substituted bis(tetrahydro-isoquinolines) related t...
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WO/1988/000826A1 |
Antitumor polycyclic organic compositions and derivatives thereof, a process of producing the compositions and a method for inhibiting tumors utilizing the compositions. More particularly, the compositions are derived from marine organis...
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WO/1987/007610A2 |
Novel compounds ecteinascidins 729, 743, 745, 759A, 759B, and 770 having antibacterial and antitumor properties.
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JP2024516033A |
Provided herein are compounds of formula (I), or a pharmaceutically acceptable salt thereof, where n, m, A1,A2,A3,A4,A5,A6,L1,L2,R1,R2,R3, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a comp...
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JP2024041852A |
The present invention provides methods for treating diseases. The present invention provides compounds of formula (I), pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and their use in the treatme...
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JP7436454B2 |
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). Compounds of this invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection an...
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JP2024506648A |
The present invention is applicable to cancers such as prostate cancer, lung cancer, pancreatic cancer, breast cancer, ovarian cancer, and cervical cancer, melanoma, B-cell chronic lymphocytic leukemia (CLL), acute myeloid leukemia ( AML...
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JP2024503851A |
The present disclosure relates to compounds, pharmaceutical compositions containing the same, and methods of using the compounds and compositions to treat diseases or disorders related to dysregulation of the complement cascade pathway. ...
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JP7422812B2 |
A compound of general formula ID, wherein X, R1-R4 take various meanings, for use in the treatment of cancer.
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JP2023179539A |
To provide diaryl macrocyclic derivatives targeting tyrosine kinase for use in treating cancer, pain, neurological diseases, autoimmune diseases, and inflammation, and pharmaceutical compositions containing them.For example, the compound...
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JP2023545762A |
The present disclosure provides modulators of cystic fibrosis transmembrane conductance regulator (CFTR) having core structure (I), pharmaceutical compositions comprising at least one such modulator, such modulators and pharmaceutical co...
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JP2023545080A |
The present disclosure provides cystic fibrosis transmembrane conductance regulator (CFTR) modulators having core structure (I), pharmaceutical compositions comprising at least one such modulator, and the use of such modulators and pharm...
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JP2023545081A |
The present disclosure provides cystic fibrosis transmembrane conductance regulator (CFTR) modulators having a core structure, pharmaceutical compositions comprising at least one such modulator, and the use of such modulators and pharmac...
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JP2023543331A |
The present invention is directed to macrocyclic urea compounds that are agonists of orexin receptors. The present invention is further directed to the use of the compounds described herein in the potential treatment or prevention of neu...
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JP2023126636A |
To provide methods for treating diseases.The present disclosure provides methods for preparing MCL1 inhibitors or a salt thereof and related key intermediates. The present disclosure relates to methods and intermediates for the synthesis...
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JP7339677B2 |
Disclosed in the present invention were a fluorosulfonyl-containing compound, an intermediate thereof, a preparation method therefor and use thereof. The fluorosulfonyl-containing compound disclosed in the present invention comprises a c...
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JP2023532946A |
The present invention relates to macrocycles, pharmaceutical compositions containing macrocycles and methods of using macrocycles to treat diseases such as cancer.
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JP2023530985A |
The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a subject, pharmaceutical compositions containing such compounds, and their use as MCL-1 inhibitors useful for treating diseases such as canc...
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JP2023530148A |
The present invention relates to pharmaceutical agents useful for the treatment and/or prevention in subjects, pharmaceutical compositions containing such compounds, and their use as MCL-1 inhibitors useful for treating diseases such as ...
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JP2023526985A |
The present invention relates to pharmaceutical agents useful for the treatment and/or prevention in subjects, pharmaceutical compositions containing such compounds, and their use as MCL-1 inhibitors useful for treating diseases such as ...
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JP2023515572A |
Formula (I): [In the formula, Z, Y1, Y2、 R.1~R7is as defined in the specification] and optical isomers thereof and addition salts thereof with pharmaceutically acceptable bases. Medicine.
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JP2023052597A |
To provide novel ecteinascidin derivatives having high tumour selectivity and antitumor activity, reduced systemic toxicity, and improved pharmacokinetic properties.The present invention provides a compound of formula ID or a pharmaceuti...
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JP2023514364A |
The present invention relates to pharmaceutical agents useful for the treatment and/or prevention in subjects, pharmaceutical compositions containing such compounds and their use as MCL-1 inhibitors useful for treating diseases such as c...
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JP2023513935A |
The present invention relates to macrocyclic compounds, such as macrocyclic sulfonyltriazoles. The invention further relates to related salts, solvates, prodrugs and pharmaceutical compositions, and the use of such compounds in the treat...
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JP2023513711A |
The present invention relates to compounds that are inhibitors of hepatitis B virus (HBV). The compounds of the invention are useful alone or in combination with other agents for treating, ameliorating, preventing or curing HBV infection...
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JP2023038270A |
To provide compounds for use in methods for regulating Kelch-like ECH associated protein 1 (KEAP1)-erythroid factor 2-related factor 2 (Nrf2) interaction.The present invention provides a compound selected from a group set forth in Claim ...
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JP2023510135A |
The present application discloses compounds of formula (I). This compound, its pharmaceutically acceptable salts, and compositions thereof, are inhibitors of the Mcl-1 protein and are useful for treating diseases and conditions character...
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JP7221548B2 |
The present invention provides a preparation method for a natural product Trabectedin. Specifically, the present invention provides a preparation method for Et-743. In the method, tyrosine is used as an initial substrate, and after 26 st...
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JP7214743B2 |
Compounds of Formula (I):pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treati...
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JP2023503318A |
Methods are provided for the treatment of SCLC patients by administering a therapeutic amount of lurubinectedin by intravenous infusion. Also provided are methods of treating cancer by administering lurbinectidine in combination with oth...
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