138results about How to "High antagonistic activity" patented technology

There are provided a fused pyrimidine compound having antagonistic activity against luteinizing hormone releasing hormone, and a medicine containing the compound. A luteinizing hormone releasing hormone antagonist containing a compound represented by the formula:

wherein R^1a is a hydrocarbon group which may be substituted or a hydrogen atom,

• • ring A^a is a 6-membered aromatic ring which may be further substituted,
  • ring B^a is a homocyclic or heterocyclic ring which may be further substituted,
  • W^a is an oxygen atom or a sulfur atom,
  • X^a1 and X^a2, which may be identical or different, are each a hydrogen atom, a hydrocarbon group which may be substituted, or a heterocyclic group which may be substituted, or X^a1 and X^a2 together may form an oxygen atom, a sulfur atom or NR^3a (wherein R^3a is a hydrocarbon group which may be substituted or a hydrogen atom), and
  • Y^a is C_1-6 alkylene which may be substituted or a bond, or a salt or prodrug thereof.

CRF antagonists comprising as an active ingredient, the compound of formula (I)

wherein A ring is 5-6 membered mono-cyclic ring which may be substituted; B ring is 5-7 membered unsaturated mono-heterocyclic ring which may be contained another 1-2 of hetero atom(s) and substituted by another substituents; W¹ and W² is carbon atom or nitrogen atom; Z is NR³, oxygen atom, sulfur which may be oxidized or CR⁴R⁵; R¹ is alkyl, alkenyl or alkynyl that may be substituted, amino which may be protected, hydroxyl which may be protected, S(O)_nR⁶, COR⁷, or cyclic group which may be substituted; R² is unsaturated cyclic group which may be substituted.

This invention is to provide a compound of the formula:wherein R1 is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula: wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5 and R6 are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5 and R6 may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof , which is useful for antagonizing CCR5 and also for the prevention and treatment of infectious disease of HIV.

This invention is to provide a compound for antagonizing CCR5, said compound being represented by the formula: wherein R1 is an optionally substituted phenyl or an optionally substituted thienyl; Y is -CH2-, -S- or -O-; and R2, R3 and R4 are independently an optionally substituted aliphatic hydrocarbon group or an optionally substituted alicyclic heterocyclic ring group, and being effective for the prevention and treatment of infectious disease of HIV.

The invention provides an application of a type of berbamine derivatives and salts thereof in the preparation of drugs for the treatment of tumors, which is mainly applied in the preparation of the drugs for the prevention and treatment of nuclear transcription factor NF-kBp65 activity-related diseases and BCR/ABL transcription activity-related diseases. The drugs are combined and prepared by the compounds of the invention and one or more pharmaceutically acceptable excipients. The preparation forms comprise solid preparations, semi-solid preparations or liquid preparations. The type of berbamine derivatives and the salts thereof provided by the invention have broader and stronger anti-leukemia and anti-solid-tumor activity, the tumors proved to be sensitive are leukemia, multiple myeloma, liver cancer, osteosarcoma and breast cancer; the toxicity and the side effects are lighter. An in vitro cell culture system and animal experiments confirm that the berbamine derivatives and the salts thereof have no significant toxicity or side effects to the growth of normal human hematopoietic cells and experimental animals under the anti-tumor dosage, which are superior to the commonly used chemotherapy drugs.

As a substance which pharmacologically regulates the function of a cell surface functional molecule, a substance which has specificity and an activity or efficacy equal or superior to an antibody and does not require an advanced production technique and facility for application thereof to a pharmaceutical product has been demanded. The invention relates to a multimer of an extracellular domain of a cell surface functional molecule, particularly a tetramer of an extracellular domain of PD-1 or PD-L1. Further, the invention relates to an application of such a tetramer as a preventive and/or therapeutic agent for cancer, cancer metastasis, immunodeficiency, an infectious disease or the like and an application of PD-1 or PD-L1 as a testing or diagnostic agent or a research agent for such a disease.

[Problem] To provide a compound which can be used for the prevention and/or treatment of diseases in which 5-HT_2B receptor and 5-HT₇ receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

[Means for Resolution] It was found that an amide derivative characterized by the possession of a nitrogen-containing bicyclic hetero ring (e.g., an indole or the like), or a pharmaceutically acceptable salt thereof, has a strong antagonism for both of the 5-HT_2B receptor and 5-HT₇ receptor. In addition, the compound of the present invention having the antagonistic activity for both of the receptors showed a good pharmacological action in comparison with the case in which an antagonist selective for either one of the receptors was used alone. Based on the above, the compound of the present invention is useful for the prevention and/or treatment of diseases in which 5-HT_2B receptor and 5-HT₇ receptor are concerned, particularly for the treatment of irritable bowel syndrome (IBS).

The invention discloses streptomyces griseoflavus for resisting alfalfa diseases and a screening method thereof. The strain is streptomyces griseoflavus NMG 6-3-9, and the preservation number of the streptomyces griseoflavus is CGMCC No. 3441. The strain of the invention has the excellent antagonistic effect on pathogenic bacteria of alfalfa root rot, can be used for the biological control of alfalfa root rot and other multiple plant diseases, and has the wide application prospect in the field of biological control of diseases. The streptomyces griseoflavus establishes the foundation for the biological control of alfalfa root rot, and provides the scientific basis for the development and application of biocontrol actinomyces preparations of diseases.

The present invention provides a compound represented by the formula (I) and a salt thereof

wherein: ring A is a 5-membered aromatic heterocycle optionally having substituent(s); R¹ is a hydrogen atom or a hydrocarbon group optionally having substituent(s); W is an oxygen atom or a sulfur atom; X¹ and X² may be the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s) or a heterocyclic group, or, X¹ and X² in combination, optionally, form an oxygen atom, a sulfur atom or ═NR²; ring B is an aromatic ring optionally further having substituent(s); Y is a bond, C_1-6 alkylene C_2-6 alkenylene or C_2-6 alkynylene, optionally having substituent(s); and Z is —SO_nR³ or —COR⁴, which are useful as a pharmaceutical agent having GnRH antagonistic action.

The invention discloses an aralkyl piperidine (oxazine) derivative and an application of the derivative in treating neurological and mental diseases. Pharmacological tests show that the derivative has a good effect of resisting schizophrenia and little toxicity. The derivative is free alkali or salt of a compound having the following structure general formula.

The invention relates to a Paenibacillus polymyxa Jaas ed2 with the functions of disease prevention and growth promotion to crops and application thereof, and belongs to the technical field of intensive agriculture production. The bacterial strain Jaas ed2 adopted by the invention has been preserved at the General Microbiological Culture Collection Center of China Microbiological Culture Collection Administration Committee on Sep. 18th, 2012 with the preservation number of CGMCC No.6580. The bacterial strain has the antagonistic activity to verticillium lecanii of eggplant, oxysporum of watermelon and other various pathogenic fungi, can enter plants of eggplants and watermelons in case of lower concentration of bacterium for colonization and conduction in the crops, can be used for promoting growth and preventing diseases of crops, and particularly has excellent control efficiency to soil-borne vascular bundle diseases, is low in production cost, simple to operate, facilitates ecological environment protection for farmlands, and reduces pesticide residue when used as a preparation, thereby meeting requirements for production of nuisance free agricultural products in China.

This invention provides 2-aminoquinoline derivatives represented by a general formula [I]

• • [in which R¹ and R² either stand for lower alkyl, lower cycloalkyl, etc., or R¹ and R² together form an aliphatic nitrogen-containing heterocycle with the nitrogen atom to which they bind; R³, R⁴, R⁵, R⁶ and R⁷ stand for hydrogen, lower alkyl, etc.; R⁸ stands for lower alkyl, lower alkyloxy, etc.; and n stands for an integer of 0-4]. The compounds act as melanin concentrating hormone receptor antagonist, and are useful as medicines for central nervous system disorders, cardiovascular disorders and metabolic disorders.

The invention relates to a special biological disease-resistant vermin-proof culture medium for flowers and a preparation method thereof. The special biological disease-resistant vermin-proof culture medium for flowers is prepared from smoke dross, furfural residue, microbial fermentation inoculum, superphosphate, trichoderma microbial inoculum, bacillus microbial inoculum and expanded perlite. The preparation method comprises the following steps: compounding smoke dross, furfural residue, microbial fermentation inoculum and superphosphate; after the mixture is decomposed, sterilizing, adding trichoderma microbial inoculum and bacillus microbial inoculum with disease-resistant function; and after composting for some time, adding the expanded perlite. Abundant active trichoderma and bacillus and metabolites thereof contained in the culture medium provided by the invention have obvious inhibiting action on flower diseases; and the smoke residue and resolvents thereof have the action of expelling and killing vermins which are easily generated in the medium. When being used for planting flowers, the special culture medium for flowers can protect the environment, and is beneficial to human health.

The invention relates to a bacillus subtilis YBM-4, of which the classification name is Bacillus subtilis. The bacillus subtilis YBM-4 is collected at China General Microbiological Culture Collection Center (CGMCC) on April 15th, 2016 at No.3, Yard 1, Beichen West Road, Chaoyang District, Beijing, with the collection number of CGMCC No.12355. The bacterial strain has the following advantages: (1) excellent biocontrol effect: in a pot experiment, a YBM-4 bacterial solution is used for treating and inoculating a tobacco plant suffering from tobacco black shank, the preventing and controlling effect can reach up to 84.33% and is obviously better than the preventing and controlling effect of 58% metalaxyl manganese zinc and biological agent bacillus subtilis, the bacillus subtilis has a potential application value at the aspect of biological prevention and control of the tobacco black shank, the development and application prospects are excellent, the biological prevention and control are environment-friendly, difficult to generate drug resistance and safe to human and livestock, and conditions are created for the development of green prevention and control of the tobacco; and (2) excellent growth promoting effect: the biomass and agronomic trait of the YBM-4 bacteria tobacco plant have an obvious growth promoting effect and are obviously different from a control group.

The present invention provides a compound represented by the formula:

wherein R¹ is a C_1-4 alkyl; R² is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a hydroxy group, (3′) a C_1-4 alkyl and (4′) a C_1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1′) a halogen, (2′) a C_1-4 alkoxy-C_1-4 alkyl, (3′) a mono-C_1-4 alkyl-carbamoyl-C_1-4 alkyl, (4′) a C_1-4 alkoxy and (5′) a mono-C_1-4 alkylcarbamoyl-C_1-4 alkoxy, or the like; R³ is a C_1-4 alkyl; R⁴ is a C_1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.

This invention is to provide a pharmaceutical composition for antagonizing CCR5 which comprises a compound of the formula:wherein R1 is an optionally substituted 5- to 6-membered ring; W is a divalent group of the formula:wherein the ring A is an optionally substituted 5- to 6-membered aromatic ring, X is an optionally substituted C, N or O atom, and the ring B is an optionally substituted 5- to 7-membered ring; Z is a chemical bond or a divalent group; R2 is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, etc., or a salt thereof.

The invention provides a streptomyces sp. strain YT027 which is preserved in China General Microbiological Culture Collection Center with the address of 3#, No.1 Yard, Beichen West Road, Chaoyang District, Beijing (100101) on January 23rd, 2013, and the preservation number is CGMCC No. 7196. The streptomyces YT027 provided by the invention has higher antagonistic activity to Phytophthora colocasiae Racib., the fermentation culture liquid of the streptomyces YT027 has good biocontrol effects on sweet potato diseases in the preservation period, can avoid or reduce chemical pesticide residue, remarkably prolong the storage period of sweet potatoes and maintain the quality of the sweet potatoes, and has better economic and social benefits.

The invention belongs to the field of biotechnology and agricultural production, especially relates to a Streptomyces termitum ACT-2 strain, its culture and application. Streptomyces termitum ACT-2 strain is preserved in China Center for Type Culture Collection (CCTCC); the address is College of Life Sciences, Wuhan University, Luojia Mountain, Wuchang District, Wuhan, Hubei Province; the collection number is CCTCCCNO: M2011008 and the collection date is Jan. 7, 2010. Streptomyces termitum ACT-2 strain, which has an effect of resisting Xanthomonas oryzae pv. oryzae, is obtained by separating and screening from paddy soil. The strain and its fermented products can be used as a biopesticide and also used to control Xanthomonas oryzae pv. oryzae and the like.

The invention relates to a biological disease-prevention type culture substrate special for a lawn and a preparation method thereof. The biological disease-prevention type culture substrate special for the lawn is prepared by the following steps of: taking xylitol slags, oil slags, fume slags, microbial fermentation bacteria agent, trichoderma and bacillus biological antimicrobial agents, epsom salt, ferrous sulfate and vermiculite as raw materials; utilizing different organic wastes to compound; fermenting and decomposing; inoculating the trichoderma and bacillus biological antimicrobial agents; adding magnesium and ferrum more absorbed by the lawn; and matching with the vermiculite to prepare the substrate. The active bio-control bacteria and metabolic products thereof contained in the culture substrate have obvious inhibiting function on turfgrass diseases, and the various contained nutrition helps to balance nutrients required for the growth of the lawn, so that favorable growth of the lawn is favored.

The invention discloses a strain of bacillus amyloliquefaciens L-1 for antagonizing pear disease, which belongs to the bacillus subtilis, and a preservation number is CGMCC No.14373. The research result displays that the bacillus amyloliquefaciens L-1 can effectively inhibit the development of pear ring rot disease, can cause pathogen mycelia malformation, and has obvious antagonistic activity on the pear ring rot disease as well as apple/pear common fungal diseases. The bacillus amyloliquefaciens L-1 can induce the active expression of fruit resistance-related enzymes(POD, CAT), reduces the accumulation of malonaldehyde in the fruits, and delays fruit aging; the bacillus amyloliquefaciens L-1 has no damage on the fruit quality, can increase the VC content in the fruits; and enables successful and rapid breeding in the wounds of the fruits; the bacterial strain is salt tolerant, the activity of a bioactive secondary metabolite is stable, and the bacterial strain has the characteristics of ultraviolet radiation resistance, acid and alkali resistance, and high temperature and metal ions resistance, and has large application potential.

This invention relates to aryl or heteroaryl amido alkane derivatives of formula (I)

in which Ar₁ and Ar₂ independently represent phenyl or a 5 or 6-membered heteroaromatic ring, R⁶ represents carboxyl or tetrazolyl, and the remaining variables are as defined in the text and claims, 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.